Prodrug 1,3-diamino-2-hydroxypropane derivatives |
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IPC classes for russian patent Prodrug 1,3-diamino-2-hydroxypropane derivatives (RU 2357962):
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                    
 Malononitrile compound as pesticide / 2347779
Present invention pertains to a malononitrile compound with formula (I):
 Cathepsin-cysteine protease inhibitors / 2312861
Invention relates to compounds represented by the formula:
 Prophylactic or therapeutic agent and pharmaceutical composition comprising heterocyclic compound / 2259361
Invention relates to a prophylactic or therapeutic agent used against hyperlipidemia and comprising as an active component the heterocyclic compound of the formula [1]:
 Nitrate salts of heterocyclic compounds, method of their production and pharmaceutical compositions based on them / 2228331
The invention relates to new and nitrate salts of heterocyclic compounds of formulas (a) and (b), where R is hydrogen, alkoxyl, R1- alkyl, alkoxyl, R2is hydrogen, alkyl, R3- alkyl, alkoxyl, X denotes N-R11or oxygen, R11means the free valence, Y represents N-R16, sulfur or alkyl, R16means hydrogen; other values radicals presented in the description of the invention
 New amide derivatives and pharmaceutical composition, promoting insulin secretion and increases sensitivity to insulin / 2191177
The invention relates to new amide derivatives of General formula (I) or their salts, where a means thiazolidin, imidazoline, triazoline, benzimidazolyl, benzothiazolyl, thiadiazolyl, imidazopyridine or imidazothiazole; X is a bond, -NR5-, -NR5CO-, -NR5CONH-, NR5SO2-, -NR5C(= NH)NH-; R1means H, lower alkyl, aryl, pyridyl, thienyl, furyl, thiazolyl, benzimidazolyl, imidazopyridine, triazolyl, thiadiazolyl, imidazolyl, imidazothiazoles, benzothiazolyl, cyclohexyl, which may be optionally substituted with halogen, lower alkyl, -OH, -CN, -NO2, -CF3, -NH2, -O-lower alkyl, and the Deputy of the lower alkyl may be substituted by phenyl, naphthyl, fullam, tanila or pyridium;2a, R2bmean H or lower alkyl; R3means hydrogen or lower alkyl; R4a, R4bmean H or HE, or taken together form a group =O or =N-O-lower alkyl; R5means H or lower alkyl
 Derivatives oxazolyl or triazolylmethyl, methods for their production (options), pharmaceutical preparation and method for the treatment of neuro-degenerative disorders / 2139863
The invention relates to new heterocyclic compounds having therapeutic activity, to processes for their preparation and intermediate compounds used for their production, to pharmaceutical preparations containing these compounds and to the use of these compounds in medicine
 Compounds selectively inhibiting aromatase, the method of preparation and pharmaceutical composition / 2131418
 Phenylacetic acid derivative and its use / 2349587
Present invention pertains to new compounds with formula (I):
Malononitrile compound as pesticide / 2347779
Present invention pertains to a malononitrile compound with formula (I):
 Synthesis of esters of 2-chloromethyl-6-methylbenzoic acid / 2345982
Present invention pertains to new compounds with formula
 Amid derivative / 2336273
Invention relates to amid derivatives of formula (I), method of disease treatment and pharmaceutical composition based on them. Compounds can be applied in treatment of different herpes virus infections. In general formula (I)
 Diarylcycloalkyl derivatives, method of their obtaining, and application as ppar-activators / 2330846
Invention concerns a compound of the formula (I)
 Oxa- and thiazole derivatives as antidiabetic agents and anti-fat agents / 2327692
Oxa- and thiazole derivatives have general formula
 Displaced heterocyclic derivatives and their application / 2325381
Invention relates to new displaced heterocyclic derivatives that can be used in treatment of diabetes and to reduce the content of cholesterol. In formula
 Derivatives of indane acetic acid and pharmaceutical composition / 2314298
Invention relates to novel compounds of the formula (I)
Cathepsin-cysteine protease inhibitors / 2312861
Invention relates to compounds represented by the formula:
 Substituted 4-alkoxyoxazol derivatives as ppar agonists / 2312106
Invention relates to novel compounds of the formula (I)
Method for modifying paraffins / 2313519
Invention relates to modification of oil paraffins, namely, to preparing sulfurous compounds used as additives in manufacturing bitumen in petroleum chemistry. Method involves interaction of paraffin with sulfur in the presence of alkaline metal persulfate or alkaline-earth metal persulfate, or ammonium persulfate. Invention provides preparing modified paraffins for a single step.
 The method of obtaining single-ended diallyldisulfide / 2223265
The invention relates to a method for producing an asymmetrical diallylsulfide General formula (1): R1-S-S-R2(1) where R1=CH3C2H5n-C4H9, R2=n-C6H13the h8H17the h9H19
 A method for production of alkyl - or alkylalkoxysilane / 2220134
The invention relates to a method for producing alkyl - or alkylalkoxysilane, which can serve as extractants of noble metals, flotation reagents, additives in oils, and can be used as starting compounds for the production of biologically active compounds, alkyl - or alkylalkoxysilane interaction of the corresponding mercaptan with alkyl - or alkenylphenol in the presence of an alkaline agent
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FIELD: chemistry. SUBSTANCE: invention relates to the compounds of the formula EFFECT: compounds can be applied to prevent and treat diseases mediated by excess activity of beta-secretase such as Alzheimer's disease. 11 cl, 12 tbl, 3 dwg, 1729 ex
Cross-reference to related applications This application discloses the priority of provisional patent application U.S. No. 60/408783 registered 6 September 2002, included in this description by reference. The technical field The invention relates to proletarienne derived 1,3-diamino-2-hydroxypropane and to such compounds that are useful in the treatment of Alzheimer's disease and related diseases. More specifically, it relates to such compounds that are able to give or generate, or in vitro, or in vivo, compounds inhibiting beta secretase - the enzyme that breaks down amyloid protein precursor with the formation of amyloid beta-peptide (A-beta), a major component of amyloid plaques formed in the brain of patients suffering from Alzheimer's disease. Background of invention Alzheimer's disease (AD) is a progressive, degenerative brain disease associated mainly with aging. The clinical picture of AD is characterized by memory loss, cognitive abilities, the ability to reason and orientation. As the disease progresses, motor, sensory and linguistic ability also affects up to the overall deterioration of many cognitive functions. Such loss of cognitive functions etc which come gradually, but typically lead to severe deterioration and, ultimately, to death in a period of four to twelve years. Alzheimer's disease is characterized by two main pathological paintings in the brain: neurofibrillary plexuses and beta-amyloid (or trigeminus) plaques composed mainly of units of the peptide fragment, known as A-beta. Individuals with AD are detected characteristic of beta-amyloid deposits in the brain (beta-amyloid plaques) in the blood vessels of the brain (beta-amyloid angiopathy), and neurofibrillary plexus. Neurofibrillary plexus are not only in Alzheimer's disease, but also other disorders that cause dementia. According to the autopsy, a large number of such damage typically found in areas of the human brain important for memory and cognitive abilities. A smaller number of such injuries with more limited anatomical distribution found in the brain of elderly people who do not have clinical manifestations of AD. Amyloidogenic plaques and vascular amyloid angiopathy also characterize the brain of individuals with trisomy 21 (down syndrome), hereditary cerebral hemorrhage with amyloidosis-type Dutch (Dutch-Type, HCHWA-D) and other neurodegener the tive disorders. Beta-amyloid is the defining characteristic of AD and is believed to now, a causal predecessor or factor in the development of the disease. The deposition of a-beta in the brain regions responsible for cognitive activity, is a major factor in the development of AD. Beta-amyloid plaques are composed mainly of amyloid beta-peptide (A-beta, also sometimes called beta-A4). Beta-peptide is formed by proteolysis of the amyloid protein precursor (APP) and consists of 39-42 amino acids. In the processing of APP involves some protease called secretase. Cleavage of APP at the N end of the peptide A-beta beta secretases and on the C-end of one or more gamma secretase is beta amelogenic a cascade of reactions, i.e. the cascade, which is formed of a-beta. Cleavage of APP alpha secretases produces alpha-sAPP - secreterial form of ADR, which does not lead to the formation of beta-amyloid plaques. Such an alternative cascade eliminates the formation of peptide A-beta. Description fragments proteolytic processing includes, for example, in U.S. patent No. 5441870, 5721130 and 5942400. Asparaginase identified as the enzyme responsible for the processing of APP at the site of cleavage of beta-secretases. The enzyme beta-secretase describe using a variety of items, including VASA, Asp and Melepsin. With the., for example, Sinha et al., 1999, Nature, 402:537-554 (p.501) and published PCT application WO00/17369. Some data shows that progressive cerebral deposition of beta-amyloid peptide (A-beta) plays a fundamental role in the pathogenesis of AD and can precede cognitive symptoms by years or decades. See, for example, Selkoe, 1991, Neuron, 6:487. Shows the release of A-beta from neurons grown in culture, and the presence of A-beta in the cerebrospinal fluid (CSF) of both healthy individuals and patients with AD. See, for example, Seubert et al., 1992, Nature, 359:325-327. The assumption was made that the peptide A-beta accumulates in the processing of APP by beta secretases, so it is advisable inhibition of this enzymatic activity in the treatment of AD. Suppose that the processing of APP in vivo at the site of cleavage of beta-secretases is the stage that limits the rate of production of A-beta, and is thus a therapeutic target in the case of treatment of AD. See, for example, Sabbagh M. et al., 1997, Alz. Dis. Rev., 3, 1-19. Mouse amazed VASE cannot produce A-beta and represent the normal phenotype. When crossed with transgenic mice, sverkhekspressiya RDAs, the offspring shows reduced amount of A-beta in the brain extracts compared with the control animals (Luo et al., 2001, Nature Neuroscience, 4:231-232). These data also support the suppose the s, that ingibirovanie activity of beta-secretase and reduced levels of a-beta in the brain provides a therapeutic method for the treatment of AD and other beta-amyloid disorders. There are currently no effective treatments to stop, prevent or reverse the development of Alzheimer's disease. Therefore, there is an urgent need for pharmaceuticals that can slow the progression of Alzheimer's disease and/or in the first place, to warn her. Compounds that are effective inhibitors of beta-secretase that inhibit mediated beta-secretases cleavage of APP, which are effective inhibitors of the production of A-beta and/or effective to reduce deposition of amyloid-beta or plaques that are required for the treatment and prevention of diseases characterized by deposits of amyloid-beta or plaques, such as AD. Summary of the invention The invention encompasses compounds of formula (AA), (I) and (X)below, pharmaceutical compositions containing such compounds, and methods of using such compounds or compositions in the treatment of Alzheimer's disease, and more specifically, compounds capable of inhibiting beta-secretase - the enzyme that breaks down amyloid protein precursor, with formation of peptide A-beta, the main components the NTA amyloid plaques, detected in the brain of patients suffering from Alzheimer's disease. In one aspect the invention relates to compounds of formula AA
and their pharmaceutically acceptable salts, where in the formula one of RNand RN'represents hydrogen and the other represents-C(=O)-(CRR')0-6R100-C(=O)-(CRR')1-6-O-R'100-C(=O)-(CRR')1-6-S-R'100-C(=O)-(CRR')1-6-C(=O)-R100-C(=O)-(CRR')1-6-SO2-R100-C(=O)-(CRR')1-6-NR100-R'100or
where R4selected from the group consisting of H; NH2; -NH-(CH2)n6-R4-1; -Other8; -NR50C(O)R5; And (C1-C4)-alkyl-NHC(O)R5; -(CH2)0-4-R8; -O-(C1-C4)-alkanoyl; HE; and (C6-C10)-aryloxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, (C1-C4)-alkyl, -CO2H, -C(O)-(C1-C4)-alkoxy or (C1-C4)-alkoxy, (C1-C6)-alkoxy; aryl-(C1-C4)-alkoxy; -NR50CO2R51; -(C1-C4)-alkyl-NR50CO2R51; -C=N; -CF3; -CF2-CF3; -C≡H; -CH2-CH=CH2; -(CH2)1-4-R4-1; -(CH2)1-4-NH-R4-1; -O-(CH2)n6 -R4-1; -S-(CH2)n6-R4-1; -(CH2)0-4-NHC(O)-(CH2)0-6-R52; -(CH2)0-4-R53-(CH2)0-4-R54; where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3, -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, arylalkyl, alkanoyl or arylalkyl; R4-6represents H or (C1-C6)-alkyl; R5selected from the group consisting of (C3-C7)-cycloalkyl; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, (C6-C10)-aryl, (C3-C7-cycloalkyl-(C1-C4)-alkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl, (C6-C10)-aryloxy; heteros is aryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; geterotsiklicheskie, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; aryl, optionally substituted 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, -SO2-aryl, -SO2-geterotsiklicheskie, -SO2-(C1-C10)-alkyl, -C(O)other9, geterotsiklicheskie, -S-(C1-C6)-alkyl, -S-(C2-C4)-alkanoyl, where R9represents aryl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; R51selected from the group consisting of aryl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, heteroaryl, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, aryl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); aryl; geterotsiklicheskie; and (C3-C8)-cycloalkyl and cycloalkenyl; where the aryl, heterocytolysine, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl (C 1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; R52is heteroseksualci, heteroaryl, aryl, cycloalkyl, -S(O)0-2- (C1-C6)-alkyl, CO2H, -C(O)NH2, -C(O)NH(alkyl), C(O)N(alkyl)(alkyl), -CO2-alkyl, -NHS(O)0-2-(C1-C6)-alkyl, -N(alkyl)S(O)0-2-(C1-C6)-alkyl, -S(O)0-2-heteroaryl, -S(O)0-2-aryl, -NH(arylalkyl), -N(alkyl)(arylalkyl), dialkoxy or alkoxy, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, dialkoxy, halogen, halogenated, halogenoalkane, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl; R53is absent or represents-O-, -C(O)-, -NH-, -N(alkyl)-, -NH-S(O)0-2-, -N(alkyl)-S(O)0-2, -S(O)0-2-NH-, -S(O)0-2-N(alkyl)-, -NH-C(S) -, or-N(alkyl)-C(S)-; R54is heteroaryl, aryl, arylalkyl, heteroseksualci, CO2H, -CO2-alkyl, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -C(O)NH2, (C1-C8)-Ala is l, HE aryloxy, alkoxy, Allakaket, NH2, NH(alkyl), N(alkyl)(alkyl), or -(C1-C6)-alkyl-CO2-(C1-C6)-alkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, CO2H, -CO2-alkyl, dialkoxy, halogen, halogenated, halogenoalkane, hydroxyalkyl, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl; X is chosen from the group consisting of -(C1-C6)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, and-NR4-6; or R4and R4-6combined with education -(CH2)n10-where n10is 1, 2, 3 or 4; Z is chosen from the group consisting of communication, SO2SO, S and S(Oh); Y is chosen from the group consisting of H, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie; and (C6-C10)-aryl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; aryl, optionally substituted with halogen, alkyl, ALK is XI, CN or NO2; arylalkyl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or Y1, Y2and the nitrogen atom to which they are attached, form a cycle selected from the group consisting of piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen; R1represents -(CH2)1-2-S(O)0-2-(C1-C6)-alkyl or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, HE, =O, -SH, -C≡N, -CF3-(C1-C3)-alkoxy, amino, mono - or dialkylamino, -N(R)C(O)R',- OC(=O)-amino and-OC(=O)-mono - or-dialkylamino, or (C2/sub> -C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino and mono - or dialkylamino, or aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or -(C1-C6)-alkoxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C 3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocycla the group is also optionally substituted by oxo; R and R' represent, independently, hydrogen or (C1-C10)-alkyl; R2selected from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and -NR1-aR1-b; where R1-aand R1-brepresent-H or (C1-C6)-alkyl; -(CH2)0-4-aryl; -(CH2)0-4-heteroaryl; and (C2-C6-alkenyl; and (C2-C6)-quinil; -CO-NRN-2RN-3; -SO2-NRN-2RN-3; -CO2H and-CO2-((C1-C4)-alkyl); R3selected from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and -NR1-aR1-b; -(CH2)0-4-aryl; -(CH2)0-4-heteroaryl; and (C2-C6-alkenyl; and (C2-C6)-quinil; -CO-NRN-2RN-3; -SO2-NRN-2RN-3; -CO2H and-CO-O-((C1-C4)-alkyl); or R2, R3and the carbon atom to which they are attached, form carbocycle from three to seven carbon atoms, where one carbon atom is optionally replaced by a group selected from among-O-, -S-, -SO2- or-NRN-2-; Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -(CR245R250)0-4-arylheteroacetic; -(CR245R250)0-4-analgeticalkie; -(CR245R250)0-4-Ariella; -(CR245R250)0-4heteroallyl; -(CR245R250)0-4-heterooligomerization; -(CR245R250)0-4-heteroarylboronic; -(CR245R250)0-4-geterotsiklicheskikh; -(CR245R250)0-4-geterotsiklicheskikh; -(CR245R250)0-4-geterotsiklicheskikh; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); cyclopentene, tsiklogeksilnogo or cycloheptyl rings, condensed with aryl, heteroaryl or heterocyclization, where one carbon atom of cyclopentyl, cyclohexyl or cycloheptyl optionally replaced with NH, NR215, O, or S(=O)0-2and where cyclopentamine, tsiklogeksilnogo or cycloheptyl group may be optionally substituted 1 or 2 groups that represent, independently, R205or =O; -CO-NR235R240; -SO2-(C1-C4)-alkyl, (C2-C10-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C10)-quinil, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-On the Sabbath.)-CH(OH)-phenyl-NO 2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO-((C2-C12-alkenyl); -(CH2)0-4-CO-((C2-C12)-quinil); -(CH2)0-4-CO-((C3-C7)-cycloalkyl); -(CH2)0-4-CO-aryl; -(CH2)0-4-CO-heteroaryl; -(CH2)0-4-CO-geterotsiklicheskie; -(CH2)0-4-CO2R215; -(CH2)0-4-SO2-NR220R225; -(CH2)0-4-SO-(C1-C8)-alkyl; -(CH2)0-4-SO2-(C1-C12)-alkyl; -(CH2)0-4-SO2-(C3-C7)-cycloalkyl; -(CH2)0-4-N(H or R215)-CO2R215; -(CH2)0-4-N(H or R215)-CO-N(R215 )2; -(CH2)0-4-N-CS-N(R215)2; -(CH2)0-4-N(-H or R215)-CO-R220; -(CH2)0-4-NR220R225; -(CH2)0-4-O-CO-(C1-C6)-alkyl; -(CH2)0-4-O-P(O)-(OR240)2; -(CH2)0-4-O-CO-N(R215)2; -(CH2)0-4-O-CS-N(R215)2; -(CH2)0-4-O-(R215)2; -(CH2)0-4-O-(R215)2-COOH; -(CH2)0-4-S-(R215)2; -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); and (C3-C7)-cycloalkyl; and (C2-C6-alkenyl, optionally substituted 1 or 2 groups R205; And (C2-C6)-quinil, optionally substituted 1 or 2 groups R205; -(CH2)0-4-N(H or R215)-SO2-R220and -(CH2)0-4-(C3-C7)-cycloalkyl; where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210; where each gets rohilla group in each case is optionally substituted 1, 2 or 3 groups which are, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C2-C6-alkenyl, (C2-C6)-quinil, (C3-C 7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case chosen, independently, from the group consisting of-H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7)-cycloalkyl), -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -(C2-C6-alkenyl -(C2-C6)-quinil -(C1-C6)-alkyl chain with one double bond and one triple bond, -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270where R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-alkenyl, not necessarily for ewenny 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205; R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, -(CH2)0-4-(C3-C7)-cycloalkyl, (C2-C6-alkenyl, (C2-C6)-quinil, aryl-(C1-C4)-alkyl, heteroaryl-(C1-C4)-alkyl and phenyl; or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, g is e optionally one carbon atom is replaced by a heteroatom, selected from the group consisting of-O-, -S-, -SO2- , and-NR220-; R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6-alkenyl, optionally substituted by 1, 2 or 3 groups R205; And (C2-C6)-quinil, optionally substituted by 1, 2 or 3 groups R205; -(CH2)1-2-S(O)0-2-((C1-C6)-alkyl), -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; -aryl; -heteroaryl; -geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-; each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; each heteroaryl is what I optionally substituted 1, 2, 3, or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210; R100and R'100represent, independently, aryl, heteroaryl, heterocyclyl, -aryl-W-aryl, -aryl-W-heteroaryl, -aryl-W-heterocyclyl-heteroaryl-W-aryl, -heteroaryl-W-heteroaryl-heteroaryl-W-heterocyclyl, -heterocyclyl-W-aryl, -heterocyclyl-W-heteroaryl, -heterocyclyl-W-heterocyclyl, -CH[(CH2)0-2-O-R150]- (CH2)0-2-aryl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-heterocyclyl or-CH[(CH2)0-2-O-R150]- (CH2)0-2-heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -CN, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-What about the-R 130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS- N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4- ((C3-C7)-cycloalkyl), (C2-C10-alkenyl and (C2-C10)-quinil, or R100is a (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups R115or R100represents -((C1-C6)-alkyl)-O-((C1-C6)-alkyl) or -((C1-C6)-alkyl)-S-((C1-C6)-alkyl), to whom gdy of which is optionally substituted 1, 2 or 3 groups R115or R100is a (C3-C8-cycloalkyl, optionally substituted by 1, 2 or 3 groups R115; W represents -(CH2)0-4-, -O-, -S(O)0-2, -N(R135)-, -CR(OH)- or-C(O)-; R102and R102' represent, independently, hydrogen or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, aryl or-R110; R105and R'105represent, independently, -H, -R110, -R120, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), -((C1-C6)-alkyl))-((C1-C3)-alkyl), (C2-C6)-alkenyl, (C2-C6)-quinil or (C1-C6)-alkyl chain with one double bond and one triple bond, or (C1-C6)-alkyl, optionally substituted-HE or-NH2; or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or R105and R'105together with the atom to which they are attached, form a 3-7-membered carbocyclic ring in which one member is an optional heteroatom selected from-O-, -S(O)0-2- , and-NR135-and the cycle is optionally substituted by 1, 2 or 3 groups selected, independently researched the mo, from among the groups R140; R115in each case represents, independently, halogen, -OH, -CO2R102-(C1-C6)-dialkoxy, -CO2-phenyl, -NR105R'135, -SO2-((C1-C8)-alkyl), -C(=O)R180, R180, -CONR105R'105, -SO2-NR105R'105, -NH-CO-((C1-C6)-alkyl), -NH-C(=O)-OH, -NH-C(=O)-OR, -NH-C(=O)-O-phenyl, -O-C(=O)-((C1-C6)-alkyl), -O-C(=O)amino, -O-C(=O)mono - or dialkylamino, -O-C(=O)phenyl, -O-((C1-C6)-alkyl)CO2N, -NH-SO2-((C1-C6)-alkyl), (C1-C6)-alkoxy or (C1-C6)-halogenoalkane; R135is a (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-quinil, (C3-C7-cycloalkyl, -(CH2)0-2-aryl, -(CH2)0-2-heteroaryl or -(CH2)0-2-heterocyclyl; R140represents heterocyclyl, optionally substituted 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)is alkylamino(C 1-C6)alkyl, di(C1-C6)alkylamino(C1-C6)alkyl and =On; R145is a (C1-C6)-alkyl or CF3; R150represents hydrogen, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen; R150' is a (C3-C7-cycloalkyl, -((C1-C3)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen; R155is a (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple SV is su, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy and halogen; R180choose from a number of morpholinyl, thiomorpholine, piperazinil, piperidinyl, homomorpholine, homotaurine, homotaurine-S-oxide, homotaurine-S,S-dioxide, pyrrolidine and pyrrolidinyl, each of which is optionally substituted by 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)-alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino (C1-C6)alkyl and =On; R110represents aryl, optionally substituted 1 or 2 groups R125; R125in each case represents, independently, halogen, amino, mono - or dialkylamino, -OH, -C≡N, -SO2-NH2, -SO2-NH-((C1-C6)-alkyl), -SO2-N((C1-C6)-alkyl)2, -SO2-((C1-C4)-alkyl), -CO-NH2, -CO-NH-((C1-C6 )-alkyl) or-CO-N((C1-C6)-alkyl)2or (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, and mono - and dialkylamino, or (C1-C6)-alkoxy, optionally substituted with one, two or three galactography; R120is heteroaryl, optionally substituted 1 or 2 groups R125; and R130represents heterocyclyl, optionally substituted 1 or 2 groups R125. The invention also relates to compounds of formula I
and their pharmaceutically acceptable salts, where in the formula, R1, R2, R3and RChave the meanings specified for formula (AA), and RNrepresents-C(=O)-(CRR')0-6R100-C(=O)- (CRR')1-6-O-R'100-C(=O)-(CRR')1-6-S-R'100-C(=O)-(CRR')1-6-C(=O)-R100-C(=O)-(CRR')1-6-SO2-R100-C(=O)-(CRR')1-6-NR100-R'100or RNrepresents a
where R4selected from the group consisting of H; NH2; -NH-(CH2)n6-R4-1; -Other8; -NR 50C(O)R5; And (C1-C4)-alkyl-NHC(O)R5; -(CH2)0-4R8; -O-(C1-C4)-alkanoyl; HE; and (C6-C10)-aryloxy, optionally substituted 1, 2, or 3 groups that represent, independently, halogen, (C1-C4)-alkyl, -CO2H, -C(O)-(C1-C4)-alkoxy or (C1-C4)-alkoxy, (C1-C6)-alkoxy; aryl-(C1-C4)-alkoxy; -NR50CO2R51; -(C1-C4)-alkyl-NR50CO2R51; -C≡N; -CF3; -CF2-CF3; -C≡CH; -CH2-CH=CH2; -(CH2)1-4-R4-1; -(CH2)1-4-NH-R4-1; -O-(CH2)n6-R4-1; -S-(CH2)n6-R4-1; -(CH2)0-4-NHC(O)-(CH2)0-6-R52; -(CH2)0-4-R53-(CH2)0-4-R54; where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3;- ((C1-C2)-alkyl), -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, arylalkyl, alkanoyl or arylalkyl; R represents H or (C1-C6)-alkyl; R5selected from the group consisting of (C3-C7)-cycloalkyl; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, (C6-C10)-aryl, (C3-C7-cycloalkyl-(C1-C4)-alkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2H, -CO-NR6R7, -CO2-(C1-C4)-alkyl, (C6-C10)-aryloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; geterotsiklicheskie, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; aryl, optionally substituted 1, 2, 3, or 4 groups that represent, independently, halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6 )-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, -SO2-aryl, -SO2-geterotsiklicheskie, -SO2-(C1-C10)-alkyl, -C(O)other9, geterotsiklicheskie, -S-(C1-C6)-alkyl, -S-(C2-C4)-alkanoyl, where R9represents aryl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; R51selected from the group consisting of aryl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, heteroaryl, -NR6R7-C(O)-NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, aryl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1 -C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); aryl; geterotsiklicheskie; (C3-C8)-cycloalkyl and cycloalkenyl; where the aryl, heterocytolysine, (C3-C8)-cycloalkyl and cycloalkenyl group optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; R52is heteroseksualci, heteroaryl, aryl, cycloalkyl, -S(O)0-2- (C1-C6)-alkyl, CO2H, -C(O)NH2, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -CO2-alkyl, -NHS(O)0-2-(C1-C6)-alkyl, -N(alkyl)S(O)0-2-(C1-C6)-alkyl, -S(O)0-2-heteroaryl, -S(O)0-2-aryl, -NH(arylalkyl), -N(alkyl)(arylalkyl), dialkoxy or Alcock and, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, dialkoxy, halogen, halogenated, halogenoalkane, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl; R53is absent or represents-O-, -C(O)-, -NH-, -N(alkyl)-, -NH-S(O)0-2-, -N(alkyl)-S(O)0-2-, -S(O)0-2-NH-, -S(O)0-2-N(alkyl)-, -NH-C(S) -, or-N(alkyl)-C(S)-; R54is heteroaryl, aryl, arylalkyl, heteroseksualci, CO2H, -CO2-alkyl, -C(O)NH(alkyl), -C(O)N(alkyl)(alkyl), -C(O)NH2, (C1-C8)-alkyl, HE aryloxy, alkoxy, Allakaket, NH2, NH(alkyl), N(alkyl)(alkyl), or -(C1-C6)-alkyl-CO2-(C1-C6)-alkyl, each of which is optionally substituted by 1, 2, 3, 4, or 5 groups that represent, independently, alkyl, alkoxy, CO2H, -CO2-alkyl, dialkoxy, halogen, halogenated, halogenoalkane, hydroxyalkyl, alkanoyl, NO2CN, alkoxycarbonyl or aminocarbonyl; X is chosen from the group consisting of -(C1-C6)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, and-NR4-6or R4and R4-6combined with education -(CH2)n10-where n10is 1, 2, 3 or 4; Z is chosen from the group consisting of communication, SO2SO, S and S(Oh); Y is chosen from the group consisting the th of N; (C1-C4)-halogenoalkane; (C5-C6)-geterotsiklicheskie; (C6-C10)-aryl; IT; N(Y1)(Y2); (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups independently selected from among (C1-C3)-alkyl and halogen; alkoxy; aryl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; arylalkyl, optionally substituted with halogen, alkyl, alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and HE; (C2-C6)-alkenyl; (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl, phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or Y1and Y2and the nitrogen atom to which they are attached, form a cycle selected from the group consisting of piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is long is correctly substituted 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen; R100and R'100represent, independently, aryl, heteroaryl, heterocyclyl, -aryl-W-aryl, -aryl-W-heteroaryl, -aryl-W-heterocyclyl-heteroaryl-W-aryl, -heteroaryl-W-heteroaryl-heteroaryl-W-heterocyclyl, -heterocyclyl-W-aryl, -heterocyclyl-W-heteroaryl, -heterocyclyl-W-heterocyclyl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-aryl, -CH[(CH2)0-2-O-R150]-(CH2)0-2-heterocyclyl or-CH[(CH2)0-2-O-R150]-(CH2)0-2-heteroaryl, where the cyclical part of each substituent optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P (=)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CO-NR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2 )0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2- ((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O- R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl and (C2-C10)-quinil, or R100is a (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups R115or R100represents -((C1-C6)-alkyl)-O-(C1 -C6)-alkyl) or -((C1-C6)-alkyl)-S- ((C1-C6)-alkyl), each of which is optionally substituted by 1, 2 or 3 groups R115or R100is a (C3-C8-cycloalkyl, optionally substituted by 1, 2 or 3 groups R115; W represents -(CH2)0-4-, -O-, -S(O)0-2, -N(R135)-, -CR(OH)- or-C(O)-; R102and R102' represent, independently, hydrogen or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, aryl or-R110; R105and R'105represent, independently, -H, -R110, -R120, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), -((C1-C6)-alkyl))-((C1-C3)-alkyl), (C2-C6)-alkenyl, (C2-C6)-quinil or (C1-C6)-alkyl chain with one double bond and one triple bond, or (C1-C6)-alkyl, optionally substituted-HE or-NH2; or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or R105and R'105together with the atom to which they are attached, form a 3-7-membered carbocyclic ring in which one member is neobyazatel the heteroatom, selected from among-O-, -S(O)0-2- , and-NR135-and the cycle is optionally substituted by 1, 2 or 3 groups selected independently from among the groups R140; R115in each case represents, independently, halogen, -OH, -CO2R102-(C1-C6)-dialkoxy, -CO2-phenyl, -NR105R'135, -SO2-((C1-C8)-alkyl), -C(=O)R180, R180, -CONR105R'105, -SO2-NR105R'105, -NH-CO-((C1-C6)-alkyl), -NH-C(=O)-OH, -NH-C(=O)-OR, -NH-C(=O)-O-phenyl, -O-C(=O)-((C1-C6)-alkyl), -O-C(=O)amino, -O-C(=O)mono - or dialkylamino, -O-C(=O)phenyl, -O-((C1-C6)-alkyl)-CO2N, -NH-SO2-((C1-C6)-alkyl), (C1-C6)-alkoxy or (C1-C6)-halogenoalkane; R135is a (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-quinil, (C3-C7-cycloalkyl, -(CH2)0-2-aryl, -(CH2)0-2-heteroaryl or -(CH2)0-2-heterocyclyl; R140represents heterocyclyl, optionally substituted 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, ( 1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino(C1-C6)alkyl and =On; R145is a (C1-C6)-alkyl or CF3; R150represents hydrogen, (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen; R150' is a (C3-C7-cycloalkyl, -((C1-C3)-alkyl)-((C3-C7-cycloalkyl), (C2-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy, R110and halogen; R155is a (C3-C7-cycloalkyl, -((C1-C2)-alkyl)-((C3-C72-C6)-alkenyl, (C2-C6)-quinil, (C1-C6)-alkyl with one double bond and one triple bond, -R110, -R120or (C1-C6)-alkyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from among-OH, -NH2, (C1-C3)-alkoxy and halogen; R180choose from a number of morpholinyl, thiomorpholine, piperazinil, piperidinyl, homomorpholine, homotaurine, homotaurine-S-oxide, homotaurine-S,S-dioxide, pyrrolidine and pyrrolidinyl, each of which is optionally substituted by 1, 2, 3 or 4 groups selected, independently, from (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-quinil, (C1-C6)-halogenoalkane, (C1-C6)-halogenoalkane, amino(C1-C6)-alkyl, mono(C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino (C1-C6)alkyl and =On; R110represents aryl, optionally substituted 1 or 2 groups R125; R125in each case represents, independently, halogen, amino, mono - or dialkylamino, -OH, -C≡N, -SO2-NH2, -SO2-NH-(C1-C )-alkyl, -SO2-N((C1-C6)-alkyl)2, -SO2-((C1-C4)-alkyl), -CO-NH2, -CO-NH-(C1-C6)-alkyl or-CO-N((C1-C6)-alkyl)2or (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, and mono - and dialkylamino, or (C1-C6)-alkoxy, optionally substituted with one, two or three galactography; R120is heteroaryl, optionally substituted 1 or 2 groups R125; and R130represents heterocyclyl, optionally substituted 1 or 2 groups R125. The invention also relates to compounds of the formula X
and their pharmaceutically acceptable salts, where in the formula, R1, R2, R3, RNand RChave the meanings specified for formula (I). The invention also relates to a process for the production of compounds of formula (AA), (I) or (X) compounds of formula (Y)
where R1, R2, R3, RNand RChave the meanings specified for formula (I). The formation of compounds of formula (Y) is connected to the second formula (AA), (I) or (X) may occur in vivo or in vitro. The compounds of formula (Y) is suitable for the treatment and/or prevention of Alzheimer's disease. The invention also relates to methods for the transformation of compounds of formula AA, I or X in the compounds of formula y-Transformation and/or obtaining compounds of formula Y comprises bringing into contact of the compounds of formulas I and/or X with the aquatic environment. The conversion can occur in vitro or in vivo. The invention also relates to methods of treating or preventing Alzheimer's disease, moderate cognitive impairment, down's syndrome, hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, cerebral amyloid angiopathy, other degenerative dementias, dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, Alzheimer's-type diffusion Taurus levy, including the introduction of a patient in need, a therapeutically effective amount of the compounds of formula AA, I or X or its salts. Preferably the patient is a man. Preferably the disease is an Alzheimer's disease. Preferably the disease is a dementia. The invention targetnode to pharmaceutical compositions, containing the compound of formula AA, I or X or its salt and at least one pharmaceutically acceptable carrier, solvent, adjuvant or diluent. The invention also relates to the use of compounds of formula AA, I or X or its salt to obtain the drug. The invention also relates to the use of compounds of formula (AA), (I) or (X) for treating or preventing Alzheimer's disease, moderate cognitive impairment, down's syndrome, hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, cerebral amyloid angiopathy, other degenerative dementias, dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration or Alzheimer's-type diffusion Taurus Levi. The invention also relates to compounds, pharmaceutical compositions, kits and methods of inhibition mediated beta-secretases cleavage of amyloid protein precursor (APP). More specifically, the compounds, compositions and methods of the invention are effective for inhibiting the production of peptide A-beta for the treatment or prevention of any disease or condition of a person or animal that is associated with PA the ideological form of the peptide A-beta. The invention also relates to methods of preparing compounds of the invention and intermediate compounds used in these methods. Compounds, compositions and methods of the invention are suitable for the treatment of people with Alzheimer's disease (AD), to promote the prevention or delay the occurrence of AD, for treating patients with mild cognitive impairment (MCI) and preventing or delaying the occurrence of AD in these patients, which otherwise can be expected progression from MCI to AD, for treating down's syndrome, for the treatment of hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, for treating cerebral beta-amyloid angiopathy and preventing its potential consequences, such as single and recurring lobes hemorrhages, for treating other degenerative dementias, including dementias of mixed vascular and degenerative origin, for the treatment of dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, and AD-type diffusion Taurus Levi, and for the treatment of fronto-temporal dementia with parkinsonism (FTDP). The compounds of formula Y have activity of inhibiting beta-secretase. Inhibiting activity of the compounds of the invention are easily demonstrated on the example, using one or more assays described herein or known in the art. If the substituents for formula not defined specifically for this formula, we mean that they have the definitions stated in connection with the previous formula, which is given reference. Detailed description of the invention As noted above, the invention relates to compounds of formula (AA), (I) and (X), suitable for the treatment and prevention of Alzheimer's disease. These compounds can be considered as prodrugs of the active compounds of the formula Y, as they form such active compound in vivo and in vitro. Compounds of formula AA, I and X are undergoing migration of the acyl group RNupon contact with water, as shown in scheme I. the Migration related to compounds of formula (I), herein referred to as "N-acyl migration". Migration-related compounds of formula (X), in this description referred to as "O-acyl migration. Migration, shown in figure 1, can occur either in vitro or in vivo and occur when the compound is introduced into contact with the water environment, including the water. Water environment can be neutral, acidic or alkaline. Preferably, the medium had a pH of from about 2 to about 10, preferably from about 3 to p is IMEMO 7. The amount of water required for migration is not a critical parameter. A catalytic amount of aqueous medium is sufficient to cause migration. Aqueous buffer solutions and gastric fluid are good environments for migration occurred. Products rearrangements of compounds of formula AA, of the formula I and/or formula X are compounds of formula (Y). The substituents R1, R2, R3, RNand RCin the compounds of formula (Y) have the values specified above for compounds of formula (I). Scheme 1
Preferred compounds of formula AA are the compounds of formula AA-1, i.e. the compounds of formula AA where R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-Ala is XI, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula AA-1 are also connections R1represents -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR' what if-N(R)SO 2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula AA-1 are also connections R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclic portion of each is the first Deputy optionally substituted 1, 2, 3, or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105 R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula AA-1 are also connections to the verge R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3. Preferred compounds of formula AA-1 are also connections R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline parts, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO2. Preferred compounds of formula AA-1 are compounds in which R1represents-CH2-phenyl, where the phenyl portion is optional substituted 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2. Preferred compounds of formula AA-1 are also compounds in which R1represents benzyl or 3,5-gifthorse the ZIL. Preferred compounds of formula AA and AA-1 are the compounds of formula AA-2, i.e. compounds of formula AA or AA-1, in which R2and R3chosen, independently, from the group consisting of H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and -NR1-aR1-b. Preferred compounds of formula AA-2 are compounds in which Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heterocyclic is) 2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent what they themselves independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210; where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case chosen, independently, from the group consisting of (C1 -C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case chosen, independently, from the group consisting of-H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy (C 1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205; R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN; R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)het is of recycleable; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-; each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210. Preferred compounds of formula AA-2 are compounds in which Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula AA-2 are also connections Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula AA-2 are also connections Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optional what about the substituted 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225. Preferred compounds of formula AA-2 are also connections Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula AA-2 are also connections Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula AA-2 are also compounds in which Rwithrepresents benzyl. Other preferred compounds of formula AA, AA-1 and AA-2 are the compounds of formula AA-3, i.e. compounds of formula AA, AA-1 and AA-2, in which one of RNand RN' represents hydrogen and the other represents a
where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51, where n6is 0, 1, 2 or 3; n7is 0, 1, 2 is 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, Fe is Il, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where R9depict is to place a phenyl-(C 1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted 1, 2, or 3 groups that represent what they themselves independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1- With6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy. Preferred compounds of formula AA-3 are compounds in which one of RNand RN' represents hydrogen and the other represents a
where X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or R4and R4-6combined with education -(CH2)n10-where n10is 1, 2, 3 or 4; Z is chosen from among communication, SO2SO, S IS C(O); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) to form a cycle selected from a number of the and piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula AA-3 are compounds in which X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups; Z is chosen from among SO2SO, S and S(Oh); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y 1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula AA-3 are compounds in which one of RNand RN' represents hydrogen and the other represents a
where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1 -C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R , -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-the 6)-alkyl; and R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1 -C6)-alkyl or N((C1- With6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane. Preferred compounds of formula AA-3 are also connections Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(The h 2)0-3-(C3-C8-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C -C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C7-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case represent, independently, -H, -(C1-C6)-Alki is, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, form carbocycle of 3, 4, 5, 6 or 7 carbon atoms. Preferred compounds of formula AA-3 are also connections R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3; R2and R3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-is Lila) and N((C 1-C6)-alkyl)((C1-C6)-alkyl); Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -SH, -C=ONR235 R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl; -(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200; -(CR245 R250)0-3-imidazolidinyl; (CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250) 0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, 2, 3 or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)- (CH2)0-1-pyridyl; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, not necessarily samewe the hydrated 1 or 2 groups R 205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210; R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, halogen-(C1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R 245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms. Other preferred compounds of formula AA-3 are compounds in which X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups; Z represents SO2, SO, S, or C(O); Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optional the nutrient substituted 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula AA-3 are also the compounds of formula AA-4, i.e. the compounds of formula AA-3, in which X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group; Z represents SO2, SO, S, or C(O); Y is HE, -N(Y1)(Y2), phenyl, benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, ethoxy, dimethoxy, diethoxy and CF3; where Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents, selected and from among halogen, methoxy, ethoxy, cyclopropyl and HE; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen; R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE; R2and R3represent, independently, H or (C1-C4)-alkyl, Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, and the 2 groups of R 210; R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen; R205in each case chosen, independently, from (C1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy; R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms. Preferred compounds of formula AA, AA-1 and AA-2 are the compounds of formula AA-5, i.e. compounds of formula AA, AA-1 and AA-2, in which one of RNand RN' represents hydrogen and the other represents-C(=O)-(CRR')0-6R100; and R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 FCU is the groups, selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N (R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2) 0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula AA-5 are compounds in which one of RNand RN' represents hydrogen and the other represents-C(=O)- R100; and R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)04 -CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N (R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula AA-5 are also connections one of RNand RN' represents hydrogen and the other represents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclic portion of each is a group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O- R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Other preferred compounds of formula AA-5 are compounds in which one of RNand RN' represents hydrogen and the other represents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. Other preferred compounds of formula AA-5 are compounds in which one of RNand RN' represents hydrogen and the other represents-C(=O)-phenyl, where the phenyl cycle optionally substituted 1 or 2 groups selected, independently, from (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH )0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. Other preferred compounds of formula AA-5 are compounds in which one of RNand RN' represents hydrogen and the other represents a
where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. The preferred stereocilia compounds of formula AA is
Preferred compounds of formula I are the compounds of formula I-1, i.e. the compounds of formula I, in which R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -H, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula I-1 are also connections R1represents -(C1-C6-alkylaryl,- ( 1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and GE is eroticline the group is also optionally substituted by oxo. Preferred compounds of formula I-1 are also connections R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105 R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from among halog is on, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula I-1 are also connections R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3. Preferred compounds of formula I-1 are also connections R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline cycles, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO2. Preferred compounds of formula I-1 are compounds in which R1represents-CH2-phenyl, where the phenyl cycle optionally substituted 2 groups, select the tion, independently from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2. Preferred compounds of formula I-1 are compounds in which R1represents benzyl or 3,5-diferensial. Preferred compounds of formulas I and I-1 are the compounds of formula I-2, i.e. compounds of formula I or I-1 in which R2and R3chosen, independently, from H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and-NR1-aR1-b. Preferred compounds of formula I-2 are compounds in which Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4 -aryl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); the de each aryl group in each case is optionally substituted 1, 2 or 3 groups which are, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210; where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2- NR235R240 ; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case chosen, independently, from the group consisting of-H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where R270in each case, before the hat is, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205; R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN; R255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, neobyazatel is substituted 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-; each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210. Preferred compounds of formula I-2 are compounds in which Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula I-2 are also connections Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula I-2 are also with the unity, in which Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225. Preferred compounds of formula I-2 are also connections Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula I-2 are also connections Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula I-2 also include compounds in which Rwithrepresents benzyl. Other preferred compounds of formulas I, I-1 and I-2 are the compounds of formula I-3, i.e. compounds of formulas I, I-1 or I-2, in which RNrepresents a
where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2 51, where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (the 5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9that gets the rockleesmile, -S-(C2-C4)-alkanoyl, where R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-al is Il); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy. Preferred compounds of formula I-3 include compounds in which RNrepresents a
where X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or R4and R4-6combined with education -(CH2)n10-where n10is 1, 2, 3 or 4; Z is chosen and the number of communication SO2SO, S and S(Oh); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) forms the CEC is, selected from among piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula I-3 include compounds in which X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups; Z is chosen from among SO2SO, S and S(Oh); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)and is coxi, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula I-3 include compounds in which RNrepresents a
and where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-(( -C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C )-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; and R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-alkyl or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-al is silt)((C 1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane. Preferred compounds of formula I-3 are also connections Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8-cycloalkyl, where qi is loukil optionally substituted 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6-alcox is, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C7-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case represent, independently, -H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C 7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms. Preferred compounds of formula I-3 are also connections R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3; R2and R3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); Rwithis a (C 1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl; -(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200; -(CR245 R250)0-3-imidazolidinyl; (CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250)0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; to whom each of the above geterotsiklicheskikh groups optionally substituted 1, 2, 3, or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)- (CH2)0-1-pyridyl; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted 1 or 2 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215each of the beam is independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210; R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, halogen-(C1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4-GoLoG is alkoxy, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms. Other preferred compounds of formula I-3 include compounds in which X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups; Z represents SO2, SO, S, or C(O); Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1- 4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula I-3 are also the compounds of formula I-4, i.e. the compounds of formula I-3 in which X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group; Z represents SO2, SO, S, or C(O); Y is HE; -N(Y1)(Y2); phenyl; benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, ethoxy, dimethoxy, diethoxy and CF3; where Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents selected from halogen, methoxy, ethoxy, cyclopropyl and HE; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where ka is every cycle optionally substituted 1 or 2 groups represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen; R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE; R2and R3represent, independently, H or (C1-C4)-alkyl, Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1 or 2 groups R210; R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen; R205in each case, in baraut, regardless of the numbers (1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy; R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms. Preferred compounds of formulas I, I-1 and I-2 are the compounds of formula I-5, i.e. compounds of formulas I, I-1 or I-2, in which RNrepresents-C(=O)-(CRR')0-6R100; and R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4 -CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS- N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105,-(CH 2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula I-5 include compounds in which RNrepresents-C(=O)-R100; and R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4- (( 3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N (R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula I-5 are also connections RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C 2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O- R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Other preferred compounds of formula I-5 include compounds in which RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2) 0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. Other preferred compounds of formula I-5 include compounds in which RNrepresents a
where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. The preferred stereocilia compounds of the formula I is
(I) Preferred compounds of formula X are the compounds of formula X-1, i.e. the compounds of formula X, in which R1represents aryl, heteroaryl, heterocyclyl -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1- 6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group also optional samewe is and oxo. Preferred compounds of formula X-1 are also connections R1represents -(C1-C6-alkylaryl -(C1-C6-alkylglycerol or -(C1-C6)-Alkylglucoside, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dialkylamino and -(C1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups, is abusive, independently from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula X-1 are also connections R1represents -(CH2)-aryl, -(CH2-heteroaryl or -(CH2)-heterocyclyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, -OH, -SH, -C≡N, -NO2, -NR105 R'105, -CO2R, -N(R)COR', or-N(R)SO2R', -C(=O)-(C1-C4)-alkyl, -SO2-amino, -SO2-mono - or-dialkylamino, -C(=O)-amino, -C(=O)-mono - or-dialkylamino, -SO2-(C1-C4)-alkyl, or (C1-C6)-alkoxy, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, or (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, -(C1-C6)-alkyl and mono - or dialkylamino, or (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, mono - or dial the laminitis and -(C 1-C3)-alkyl, or (C2-C10)-alkenyl or (C2-C10)-quinil, each of which is optionally substituted by 1, 2 or 3 groups selected, independently, from halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, amino, (C1-C6)-alkyl and mono - or dialkylamino; and heterocyclyl the group is also optionally substituted by oxo. Preferred compounds of formula X-1 are also connections R1represents-CH2-phenyl or-CH2-pyridinyl, where the cyclical part of each substituent optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy, -NO2and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents selected, independently, from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N-((C1-C6)-alkyl)((C1-C6)-alkyl, -C≡N, -CF3. Preferred compounds of formula X-1 are also connections R1represents-CH2-phenyl or-CH2-pyridinyl where the phenyl or pyridinoline cycles, each optionally substituted by 1 or 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, -CF3and-NO . Preferred compounds of formula X-1 are compounds in which R1represents-CH2-phenyl, where the phenyl cycle optionally substituted 2 groups selected, independently, from halogen, (C1-C2)-alkyl, (C1-C2)-alkoxy, hydroxy, and-NO2. Preferred compounds of formula X-1 are also compounds in which R1represents benzyl or 3,5-diferensial. Preferred compounds of formula X or X-1 are the compounds of formula X-2, i.e. compounds of formula X or X-1, in which R2and R3chosen, independently, from H or (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of (C1-C3)-alkyl, halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy and-NR1-aR1-b. Preferred compounds of formula X-2 are compounds in which Rwithselected from the group consisting of (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -NR235C=ONR235R240, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8)-cyclo is Lila, where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-aryl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-geterotsiklicheskie; -[C(R255)(R260)]1-3-CO-N(R255)2; -CH(aryl)2; -CH(heteroaryl)2; -CH(heteroseksualci)2; -CH(aryl)(heteroaryl); -CO-NR235R240; -(CH2)0-1-CH((CH2)0-6-OH)-(CH2)0-1-aryl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-aryl or-heteroaryl)-CO-O((C1-C4)-alkyl); -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl) -;- CH2-NH-CH2-CH(-O-CH2-CH3)2; -N and -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225 ; -(CH2)0-4-CO-((C1-C12)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); where each aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R210; where each heteroaryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210; R205in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, optionally substituted by 1, 2, and 3 groups of R 205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case chosen, independently, from the group consisting of (C1-C6)-alkyl, (CH2)0-2-aryl, (C3-C7)-cycloalkyl, (CH2)0-2-heteroaryl and (CH2)0-2-geterotsiklicheskie, where the aryl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case chosen, independently, from the group consisting of-H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, amino-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, (C3-C7)-cycloalkyl, -((C1-C6)-alkyl)-O-((C1-C3)-alkyl), -aryl, -heteroaryl and-geterotsiklicheskie, where the aryl group in each SL is tea is optionally substituted 1, 2 or 3 groups R270each heteroaryl is optionally substituted by 1, 2, 3 or 4 R200each heteroseksualci is optionally substituted by 1, 2, 3 or 4 R210where R270in each case represents, independently, R205, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; NR235R240; OH; C≡N; -CO-((C1-C4)-alkyl) and =O, where heterocytolysine group in each case is optionally substituted by 1, 2 or 3 groups R205; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 groups R205; R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case chosen, independently, from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms, where carbocycle optionally substituted 1 or 2 groups that represent, independently, HE, methyl, Cl, F, och3, CF3, NO2or CN; 255and R260in each case chosen, independently, from the group consisting of H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; -(CH2)0-4-(C3-C7)-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -((C1-C4)-alkyl)aryl; -((C1-C4)-alkyl)heteroaryl; -((C1-C4)-alkyl)geterotsiklicheskie; aryl; heteroaryl; geterotsiklicheskie; -(CH2)1-4-R265-(CH2)0-4-aryl; -(CH2)1-4-R265-(CH2)0-4-heteroaryl and -(CH2)1-4-R265-(CH2)0-4-geterotsiklicheskie; where R265in each case represents, independently, -O-, -S - or-N((C1-C6)-alkyl)-; each aryl or phenyl optionally substituted by 1, 2, or 3 groups that represent, independently, R205, R210or (C1-C6)-alkyl, substituted 1, 2, or 3 groups that represent, independently, R205or R210. Preferred compounds of formula X-2 are compounds in which Rwithrepresents -(CR245R250)0-4-aryl or -(CR245R250)0-4-heteroaryl, where aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula X-2 are also connections to the verge Rwithrepresents -(CR245R250)-aryl or -(CR245R250-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups R200. Preferred compounds of formula X-2 are also connections Rwithrepresents -(CH2)-aryl or -(CH2-heteroaryl, where each aryl and heteroaryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N, C≡N, -(CH2)0-4-CO-NR220R225, -(CH2)0-4-CO-((C1-C12)-alkyl) and -(CH2)0-4-SO2-NR220R225. Preferred compounds of formula X-2 are also connections Rwithrepresents -(CH2)-aryl, where aryl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula X-2 are also connections Rwithrepresents -(CH2)-phenyl, where phenyl optionally substituted by 1, 2 or 3 groups selected from HE, " NO2, halogen, -CO2N and C≡N. Preferred compounds of formula X-2 are also compounds in which Rwithrepresents benzyl. Other preferred compounds of formula X, X-1 or X-2 are the joint is of the formula X-3, i.e. compounds of formula X, X-1 or X-2, in which RNrepresents a
where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR50C(O)R5or-NR50CO2R51, where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 the 2 groups, represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R 8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; Alki the sludge; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy. Preferred compounds of formula X-3 are compounds in which RNrepresents a
where X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups, or-NR4-6; or R4and R4-6combined with education -(CH2)n10-where n10is 1, 2, 3 or 4; Z is chosen from among communication, SO2SO, S and S(Oh); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-alkyl and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C10)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, ( 3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl and (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula X-3 are compounds in which X is a (C1-C4)-alkylidene, optionally substituted by 1, 2 or 3 methyl groups; Z is chosen from among SO2SO, S and S(Oh); Y is chosen from among N, (C1-C4)-halogenoalkane; and (C5-C6)-geterotsiklicheskie containing at least one N, O or S; phenyl; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from the group consisting of halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane; and (C3-C8)-cycloalkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from (C1-C3)-Ala is La and halogen; alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; phenyl-(C1-C4)-alkyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, (C1-C4)-alkoxy, (C3-C8)-cycloalkyl and IT; and (C2-C6)-alkenyl; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; phenyl-(C1-C4)-alkyl or (C3-C8-cycloalkyl-(C1-C4)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula X-3 are compounds in which RNrepresents a
and where R4represents NH2, -NH-(CH2)n6-R4-1-The other8, -NR 50C(O)R5or-NR50CO2R51where n6is 0, 1, 2 or 3; n7is 0, 1, 2 or 3; R4-1selected from the group consisting of-SO2-((C1-C8)-alkyl), -SO-((C1-C8)-alkyl), -S-((C1-C8)-alkyl), -S-CO-((C1-C6)-alkyl), -SO2-NR4-2R4-3; -CO-(C1-C2)-alkyl, -CO-NR4-3R4-4; R4-2and R4-3represent, independently, H, (C1-C3)-alkyl or (C3-C6-cycloalkyl; R4-4represents alkyl, phenylalkyl, (C2-C4-alkanoyl or phenylalkanoic; R5is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, where each cycloalkyl group optionally substituted by one or two groups representing a (C1-C6)-alkyl, preferably - (C1-C2)-alkyl, (C1-C6)-alkoxy, preferably - (C1-C2)-alkoxy, CF3, OH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), halogen, CN or NO2; or cycloalkyl group substituted by 1 or 2 groups that represent, independently, CF3, Cl, F, methyl, ethyl or cyano; (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, -NR6 R7, (C1-C4)-alkoxy, (C5-C6-heteroseksualci, (C5-C6-heteroaryl, phenyl, (C3-C7-cycloalkyl, -S-(C1-C4)-alkyl, -SO2-(C1-C4)-alkyl, -CO2N, -CONR6R7, -CO2-(C1-C4)-alkyl or phenyloxy; heteroaryl, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C1-C4-halogenated or HE; heteroseksualci, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen or (C2-C4-alkanoyl; phenyl, optionally substituted by 1, 2, 3, or 4 groups that represent, independently, halogen, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy or (C1-C4-halogenated; and-NR6R7; where R6and R7chosen, independently, from the group consisting of H, (C1-C6)-alkyl, (C2-C6)-alkanoyl, phenyl, -SO2-(C1-C4)-alkyl and phenyl-(C1-C4)-alkyl; R8selected from the group consisting of-SO2-heteroaryl, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl or halogen; -SO2-aryl, -SO 2-geterotsiklicheskie, -C(O)other9, geterotsiklicheskie, -S-(C2-C4)-alkanoyl, where R9represents phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl or H; R50represents H or (C1-C6)-alkyl; and R51selected from the group consisting of phenyl-(C1-C4)-alkyl, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups which are, independently, halogen, cyano, -NR6R7-C(O)NR6R7, (C3-C7-cycloalkyl or -(C1-C4)-alkoxy; geterotsiklicheskie, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl- (C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; geterotsiklicheskikh, optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, (C2-C4-alkanoyl, phenyl-(C1-C4)-alkyl and-SO2-(C1-C4)-alkyl; alkenyl; quinil; heteroaryl, optionally substituted 1, 2, or 3 groups that represent, independently, HE, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH(C1-C6)-and the keel or N((C 1-C6)-alkyl)((C1-C6)-alkyl); heteroaromatic, optionally substituted by 1, 2 or 3 groups which are, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy, halogen, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); phenyl; and (C3-C8)-cycloalkyl and cycloalkenyl, where phenyl, (C3-C8)-cycloalkyl and cycloalkenyl group substituted by optionally 1, 2, 3, 4, or 5 groups that represent, independently, halogen, CN, NO2, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C2-C6-alkanoyl, (C1-C6-halogenated, (C1-C6)-halogenoalkane, hydroxy, (C1-C6-hydroxyalkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-dialkoxy, (C1-C6)-dialkoxy-(C1-C6)-alkyl or (C1-C6)-alkoxy-(C1-C6)-alkoxy; and Y represents a (C1-C10)-alkyl, optionally substituted by 1-3 substituents, which may be the same or different and are selected from among halogen, hydroxy, alkoxy, dialkoxy, halogenoalkane. Preferred compounds of formula X-3 are also connections Rwithis a (C1-C8)-Ala is l, optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -OC=ONR235R240, -S(=O)0-2((C1-C6)-alkyl), -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C8-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from the group consisting of R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4-phenyl; -(CR245R250)0-4-heteroaryl; -(CR245R250)0-4-heteroseksualci; -(CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CHRS-6-(CH2)0-1-heteroaryl; -CH(-CH2-OH)-CH(OH)-phenyl-NO2; ((C1-C6)-alkyl)-O-((C1-C6)-alkyl)-or -(CH2)0-6-C(=NR235)(NR235R240); where each aryl optionally substituted by 1, 2 or 3 R200; each heteroaryl optionally substituted by 1, 2, 3 or 4 R200; each heteroseksualci optionally substituted by 1, 2, 3 or 4 R210; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4WITH((C 1-C12)-alkyl); -(CH2)0-4-CO2R215or -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) or N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; halogen; (C1-C6)-alkoxy, (C1-C6)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted by 1, 2 or 3 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case represents, independently, (C1-C6)-alkyl, -(CH2)0-2-phenyl, (C3-C7-cycloalkyl, -(CH2)0-2-heteroaryl and -(CH2)0-2-heteroseksualci, where the phenyl group in each case is optionally substituted by 1, 2, or 3 groups that represent, independently, R205or R210; where heterocytolysine group in each case is not necessarily samewe the Noi 1, 2 or 3 R210; where each heteroaryl group in each case is optionally substituted by 1, 2 or 3 R210; R220and R225in each case represent, independently, -H, -(C1-C6)-alkyl, hydroxy-(C1-C6)-alkyl, halogen-(C1-C6)-alkyl, -(C3-C7-cycloalkyl and((C1-C6)-alkyl)-O-((C1-C3)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5, 6 or 7 carbon atoms. Preferred compounds of formula X-3 are compounds in which R1represents benzyl, optionally substituted by 1, 2, 3 or 4 groups selected, independently, from halogen, (C1-C4)-alkoxy, hydroxy and (C1-C4)-alkyl, optionally substituted by 1, 2 or 3 substituents from halogen, HE, SH, NH2, NH((C1-C6)-alkyl), N((C1-C6)-alkyl)((C1-C6)-alkyl), C≡N, CF3; R2and 3chosen, independently, from H or (C1-C4)-alkyl, optionally substituted by 1 Deputy, selected from among halogen, -OH, -SH, -C≡N, -CF3, (C1-C3)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); Rwithis a (C1-C8)-alkyl, optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -SH, -C=ONR235R240and-S(=O)2NR235R240; -(CH2)0-3-(C3-C6-cycloalkyl where cycloalkyl optionally substituted by 1, 2 or 3 groups selected, independently, from among the R205, -CO2H and CO2-((C1-C4)-alkyl); -(CR245R250)0-4is phenyl, optionally substituted by 1, 2 or 3 R200; -(CR245R250)0-3-pyridyl; -(CR245R250)0-3-pyridazinyl; -(CR245R250)0-3-pyrimidinyl; -(CR245R250)0-3-pyrazinyl; -(CR245R250)0-3-furyl; -(CR245R250)0-3-indolyl; -(CR245R250)0-3-thienyl; -(CR245R250)0-3-pyrrolyl; -(CR245R250)0-3-pyrazolyl; -(CR245R250)0-3-benzoxazolyl; -(CR245R250)0-3-imidazolyl; each of the above heteroaryl groups is optionally substituted by 1, 2, 3 or 4 R200/sub> ; -(CR245R250)0-3-imidazolidinyl; (CR245R250)0-3-tetrahydrofuryl; (CR245R250)0-3-tetrahydropyranyl; (CR245R250)0-3-piperazinil; (CR245R250)0-3-pyrrolidinyl; (CR245R250)0-3-piperidinyl; (CR245R250)0-3-indolinyl; each of the above geterotsiklicheskikh group optionally substituted by 1, 2, 3 or 4 R210; (CH2)0-1-CH((CH2)0-4-OH)-(CH2)0-1-phenyl; -(CH2)0-1-CH((C1-C4-hydroxyalkyl)- (CH2)0-1-pyridyl; R200in each case represents, independently, (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; HE; -NO2; halogen; -CO2N; C≡N; -(CH2)0-4-CO-NR220R225; -(CH2)0-4-CO-((C1-C8)-alkyl); -(CH2)0-4-CO2R215and -(CH2)0-4-O-((C1-C6)-alkyl, optionally substituted by 1, 2, 3, or 5-F); R205in each case represents, independently, (C1-C6)-alkyl, halogen, -OH, -O-phenyl, -SH, -C≡N, -CF3, (C1-C6)-alkoxy, NH2, NH((C1-C6)-alkyl) and N((C1-C6)-alkyl)((C1-C6)-alkyl); R210in each case represents, independently, (C1-C6 )-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy, (C1-C4)-halogenoalkane; -NR220R225; OH; C≡N; and (C3-C7-cycloalkyl, optionally substituted 1 or 2 groups R205; -CO-((C1-C4)-alkyl); -SO2-NR235R240; -CO-NR235R240; -SO2-((C1-C4)-alkyl) and =O, where R215in each case represents, independently, (C1-C6)-alkyl, (CH2)0-2-phenyl, (C3-C6-cycloalkyl, -(CH2)0-2-pyridyl, -(CH2)0-2-pyrrolyl, -(CH2)0-2-imidazolyl, -(CH2)0-2pirimidil, -(CH2)0-2-pyrrolidinyl, -(CH2)0-2-imidazolidinyl, -(CH2)0-2-piperazinil, -(CH2)0-2-piperidinyl and (CH2)0-2-morpholinyl, where the phenyl group in each case is optionally substituted 1 or 2 groups that represent, independently, R205or R210; where each heterocytolysine group in each case is optionally substituted by 1 or 2 R210; where each heteroaryl group in each case is optionally substituted by 1 or 2 R210; R220and R225in each case represent, independently, -H, -(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl halogen-(C 1-C4)-alkyl, -(C3-C6-cycloalkyl and((C1-C4)-alkyl)-O-((C1-C2)-alkyl); R235and R240in each case represent, independently, H or (C1-C6)-alkyl; R245and R250in each case represent, independently, H, (C1-C4)-alkyl, (C1-C4-hydroxyalkyl, (C1-C4)-alkoxy, (C1-C4)-halogenoalkane, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 4, 5 or 6 carbon atoms. Other preferred compounds of formula X-3 are compounds in which X is a (C1-C3)-alkylidene, optionally substituted by 1 or 2 methyl groups; Z represents SO2, SO, S, or C(O); Y represents a (C1-C4-halogenated; HE; -N(Y1)(Y2); And (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-dialkoxy and (C1-C4)-halogenoalkane; and (C1-C4)-alkoxy; phenyl, optionally substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; and benzyl, it is certainly substituted with halogen, (C1-C4)-alkyl, (C1-C4)-alkoxy, CN or NO2; where Y1and Y2are the same or different and represent H; and (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 substituents selected from among halogen, (C1-C2)-alkoxy, (C3-C6)-cycloalkyl and IT; and (C2-C6-alkanoyl; phenyl; -SO2-(C1-C4)-alkyl; benzyl and (C3-C6-cycloalkyl-(C1-C2)-alkyl; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted by 1, 2, 3, or 4 groups that represent, independently, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl or halogen. Preferred compounds of formula X-3 are also the compounds of formula X-4, i.e. the compounds of formula X-3, in which X is a (C1-C3)-alkylidene, optionally substituted 1 methyl group; Z represents SO2, SO, S, or C(O); Y is HE, -N(Y1)(Y2), phenyl, benzyl or (C1-C10)-alkyl, optionally substituted by 1 or 2 substituents, which may be the same or different and are selected from among halogen, hydroxy, methoxy, e is hydroxy, dimethoxy, diethoxy and CF3; where Y1and Y2are the same or different and represent H; and (C1-C4)-alkyl, optionally substituted by 1 or 2 substituents selected from halogen, methoxy, ethoxy, cyclopropyl and HE; or -N(Y1)(Y2) to form a cycle selected from the piperazinil, piperidinyl, morpholinyl and pyrrolidinyl, where each cycle is optionally substituted 1 or 2 groups that represent, independently, (C1-C4)-alkyl, (C1-C4)-alkoxy or halogen; R1represents benzyl, optionally substituted by 1, 2 or 3 groups selected independently from among methyl, ethyl, n-propyl, isopropyl, hydroxymethyl, monohalogenated, dehalogenating, trihalomethyl, -CH2CF3, methoxymethyl, halogen, methoxy, ethoxy, n-propyloxy, isopropoxy and HE; R2and R3represent, independently, H or (C1-C4)-alkyl, Rwithis a (C1-C6)-alkyl, optionally substituted by 1, 2 or 3 groups R205; cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl; -(CR245R250)0-3is phenyl, optionally substituted 1 or 2 groups R200; -(CR245R250)0-3-pyridyl, optionally substituted by 1 or 2 R 200; -(CR245R250)0-3-piperazinil; -(CR245R250)0-3-pyrrolidinyl or -(CR245R250)0-3-piperidinyl; each of the above geterotsiklicheskikh group optionally substituted by 1 or 2 groups R210; R200in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; HE and halogen; R205in each case chosen, independently, from (C1-C4)-alkyl, halogen, -OH, -SH, -C≡N, -CF3and (C1-C4)-alkoxy; R210in each case chosen, independently, from (C1-C4)-alkyl, optionally substituted 1 or 2 groups R205; halogen; (C1-C4)-alkoxy; OCF3; NH2; NH((C1-C6)-alkyl); NH((C1-C6)-alkyl)((C1-C6)-alkyl); and HE CO- ((C1-C4)-alkyl); where R245and R250in each case chosen, independently, from H, (C1-C4)-hydroxyalkyl, (C1-C4)-alkoxy, or R245and R250taken together with the carbon atom to which they are attached, to form carbocycle of 3, 5 or 6 carbon atoms. Preferred compounds of formula X, X-1 and X-2 are the compounds of formula X-5, i.e. compounds of formula X, X-1 or X-2, in which RNnot only is em a-C(=O)-(CRR') 0-6R100; and R100represents aryl, heteroaryl or heterocyclyl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS- N(R150)2, -(CH2)0-4-NR 150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula X-5 are compounds in which RNrepresents-C(=O)-R100; and R100represents aryl or heteroaryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-CO-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-R110, -(CH2) -R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO- R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-SO2-(CH2)0-4-((C3-C7)-cycloalkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N (R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-CS-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-O-R150'-COOH, -(CH2)0-4-S-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cycloalkyl), (C2-C10-alkenyl or (C2-C10)-quinil. Preferred compounds of formula X-5 are also connections RNrepresents-C(=O)-aryl or-C(=O)-heteros is aryl, where the cyclical part of each group optionally substituted by 1, 2 or 3 groups selected, independently, from -OR, -NO2, (C1-C6)-alkyl, halogen, -C≡N, -OCF3, -CF3, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-((C1-C12)-alkyl), -(CH2)0-4-CO-((C2-C12-alkenyl), -(CH2)0-4-CO-((C2-C12)-quinil), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4SO is((C1-C8)-alkyl), -(CH2)0-4-SO2-((C1-C12)-alkyl), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, (CH2)0-4-O-CO-((C1-C6)-alkyl), -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O-(R150), -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-((C3-C7)-cyclol the sludge), (C2-C10-alkenyl or (C2-C10)-quinil. Other preferred compounds of formula X-5 are compounds in which RNrepresents-C(=O)-aryl or-C(=O)-heteroaryl, where the cyclical part of each group optionally substituted by 1 or 2 groups selected, independently, from (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7)-cycloalkyl, (C2-C10-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130or (C2-C10)-quinil. Other preferred compounds of formula X-5 are compounds in which RNrepresents a
where sub is a hydrogen or a (C1-C6)-alkyl, halogen, -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-N(R150)-SO2-R105, -(CH2)0-4-SO2-NR105R'105-(C3-C7-cycloalkyl -(C2-C10)-alkenyl, -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0- -R130or (C2-C10)-quinil. The preferred stereochemistry of the compounds of the formula X is
In another aspect the invention relates to intermediate compounds of formula (IA)
where R1, R2, R3, RNand RChave the values specified above for compounds of formula I, and PROT represents a protective group for the amino group, the definition of which is given below. In another aspect the invention relates to intermediate compounds of the formula (XA)
where R1, R2, R3, RNand RChave the values specified above for compounds of formula I, and PROT represents a protective group for the amino group, the definition of which is given below. The invention also relates to methods for formation of compounds of formula (Y) of the compounds of the formula (AA), formula (I) or formula (X), suitable for the treatment and/or prevention of Alzheimer's disease. The formation of compounds of formula (Y) of the compounds of formula (AA), (I) or (X) may occur in vivo or in vitro. The invention also relates to methods for the transformation of compounds of formula AA, I or X in the compounds of formula Y when exposed to compounds of formula AA, I, or X aquatic environments. The conversion can occur in vitro or in vivo. The invention also about what is worn to a method of treatment of a patient, who has a disease or condition, or prevent the acquisition of the patient's disease or condition selected from the group consisting of Alzheimer's disease, contributing to the prevention or delay of onset of Alzheimer's, patients with mild cognitive impairment (MCI) and preventing or delaying the occurrence of Alzheimer's disease in these patients, which may develop from MCI to AD, down syndrome treatment, treatment of people with hereditary cerebral hemorrhage with amyloidosis (Dutch Type), the treatment of cerebral amyloid angiopathy and preventing its potential consequences, i.e. single and recurrent lobes bleeding, treating other degenerative dementias including dementias of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, or Alzheimer's-type diffusion Taurus levy, including the introduction of those needing such treatment, a therapeutically effective amount of the compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts. In the embodiment of this method of treatment can be used when a disease is a disease of Alzheimer's. In embodied and this method of treatment may help prevent or delay the appearance of Alzheimer's disease. In the embodiment of this method of treatment can be applied when the disease is a mild cognitive impairment. In the embodiment of this method of treatment can be applied when the disease is a syndrome. In the embodiment of this method of treatment can be used when a disease is a hereditary cerebral hemorrhage with amyloidosis (Dutch Type). In the embodiment of this method of treatment can be used when a disease is a cerebral amyloid angiopathy. In the embodiment of this method of treatment can be used when a disease is a degenerative dementia. In the embodiment of this method of treatment can be applied when the disease is an Alzheimer's-type diffusion Taurus Levi. In the embodiment of this method of treatment can treat an existing disease. In the embodiment of this method of treatment can prevent the development of disease. In the embodiment of this method of treatment can be used therapeutically effective amount, comprising, in the case of oral administration, from about 0.1 mg/day to about 1000 mg/day; in the case of parenteral, sublingual, intranasal, vnutriobolochechnoe of administration is from about 0.5 mg/day to about 100 mg/day; in the case of the introduction method depots and implants - from approximately 05 mg/day to about 50 mg/day; in the case of local administration is from about 0.5 mg/day to about 200 mg/day; in the case of rectal administration is from about 0.5 mg to about 500 mg In the embodiment of this method of treatment can be used therapeutically effective amount, comprising, in the case of oral administration, from about 1 mg/day to about 100 mg/day; and in the case of parenteral administration is from about 5 to about 50 mg daily. In the embodiment of this method of treatment can be used therapeutically effective amounts of the components in the case of oral administration from about 5 mg/day to about 50 mg/day. The invention also relates to pharmaceutical compositions comprising a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt. The invention also relates to the use of compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts for obtaining medicines. The invention also relates to a method of inhibiting beta-secretase activity, inhibiting cleavage of amyloid protein precursor (APP) in the reaction mixture in the website between Met596 and Asp597, the numbering of amino acid isotype of APP-695, or in the corresponding website isotype or mutant; inhibiting production of amyloid beta peptide (A-beta) in a cell; ingibirovany the production of amyloid plaque in an animal, and treating or preventing diseases, characterized by beta-amyloid deposits in the brain. Each of these methods includes the introduction of therapeutically effective amounts of compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salts. The invention also relates to a method of inhibiting beta-secretase activity, including effects on specified beta secretshow activity of the compounds of formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt. In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of less than 50 microns. In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 10 μm or less. In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 1 μm or less. In the embodiment in this way is used as a compound inhibiting the enzyme activity by 50% at a concentration of 10 nm or less. In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in vitro. In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in the cell. In the embodiment of this method includes the t effect of the compounds on the specified beta secretase in the cage of the animal. In this embodiment the method comprises exposure to the specified connection on the specified beta secretase in humans. The invention also relates to a method for inhibiting cleavage of amyloid protein precursor (APP) in the reaction mixture in the website between Met596 and Asp597, the numbering of amino acid isotype of APP-695, or in the corresponding website isotype or mutant, including the impact on the specified reaction mixture an effective inhibitory amount of a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt. In the embodiment in such a way use the site of cleavage between Met652 and Asp653, the numbering of amino acid isotype of APP-751; between Met671 and Asp672, the numbering of amino acid isotype of APP-770; between Leu652 and Asp653 Swedish mutation of APP-751 or between Leu671 and Asp672 Swedish mutation of APP-770. In the embodiment in this method, the reaction mixture effect in vitro. In the embodiment in this method, the reaction mixture is exposed in the cell. In the embodiment in this method, the reaction mixture is exposed in the cell of the animal. In the embodiment in this method, the reaction mixture is exposed in the cell. The invention also relates to a method for inhibiting production of amyloid beta peptide (A-beta) in a cell, comprising introducing into the specified cell connection fo the formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt. In the embodiment of this method includes the introduction of the animal. In this embodiment the method includes administration to a human. The invention also relates to a method of inhibiting the production of beta-amyloid plaque in an animal, comprising the introduction of a specified animal compounds of the formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt. In this embodiment the method includes administration to a human. The invention also relates to a method of treating or preventing diseases characterized by beta-amyloid deposits in the brain, including the introduction to the patient an effective therapeutic amount of the compounds of formula (AA), (I) or (X) under conditions when there is an effective inhibitory amount of a compound of formula (Y) or its pharmaceutically acceptable salt. In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of less than 50 microns. In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 10 μm or less. In this embodiment the manual leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 1 μm or less. In the embodiment of this method leads to the compound of formula (Y), the inhibitory activity of the enzyme by 50% at a concentration of 10 nm or less. In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 0.1 to about 1500 mg/day. In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 15 to about 1000 mg/day. In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 1 to about 100 mg/day. In the embodiment of this method of connection is used in a therapeutic quantity in the range of from about 5 to about 50 mg/day. In the embodiment of this method can be used when the disease is a disease of Alzheimer's. In the embodiment of this method can be used when the disease is a mild cognitive impairment, down's syndrome and hereditary cerebral hemorrhage with amyloidosis (Dutch Type). The invention also relates to a set of components, including components that can be assembled, in which at least one component includes a compound of formula AA, I, or X enclosed in the package. In the oploschenii this set of components includes liofilizovane connection, and at least one other component comprises a diluent. The invention also relates to a set of packages that include multiple packages, with each package includes one or more unit doses of the compounds of formula (AA), (I) or (X) or its pharmaceutically acceptable salt. In this embodiment the set of packages includes packages, each of which is adapted for oral delivery, and includes a tablet, gel or capsule. In this embodiment the set of packages includes packages, each of which is adapted for parenteral delivery, and includes the product in the form of a depot, syringe, ampoule or vial. In this embodiment the set of packages includes packages, each of which is adapted for local delivery, and includes a sticker (the patch), pad, ointment or cream. The invention also relates to a kit comprising a compound of formula (AA), (I) or (X) or its pharmaceutically acceptable salt and one or more therapeutic agents selected from the group consisting of antioxidant, anti-inflammatory agent, an inhibitor of gamma-secretase, neurotrophic means of acetylcholinesterase inhibitor, statin drug (statin), peptide A-beta and antibodies against A-beta. The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutical is acceptable salt and an inert diluent or edible carrier. In this embodiment the composition comprises a carrier, representing the oil. The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutically acceptable salt and a binder, excipient, disintegrant, lubricant or glidant. The invention also relates to compositions containing a compound of the formula (AA), (I) or (X) or its pharmaceutically acceptable salt that is included in the cream, ointment or sticker (the patch). The invention relates to compounds of the formula (AA), formula (I) and (X)that can be used to generate compounds of formula (Y), which is suitable for the treatment and prevention of Alzheimer's disease. Compounds according to the invention is a specialist in the art can obtain, based on knowledge of the chemical structure of the compounds. Chemistry of obtaining compounds of this invention are well-known specialists in this field of technology. In fact, there are several ways to obtain the compounds according to the invention. Specific examples of methods of obtaining can be found in the technique. For example, see J. Org. Chem., 1998, 63, 4898-4906; J. Org. Chem., 1997, 62, 9348-9353; J. Org. Chem., 1996, 61, 5528-5531; J. Med. Chem., 1993, 36, 320-330; J. Am. Chem. Soc., 1999, 121, 1145-1155; and references cited in these works. Cm. also U.S. patent No. 6150530, 5892052, 5696270 and 5362912 included in this description as a reference. The use of the s different ways, which you can use to obtain the compounds according to the invention, are described below. General method of preparing compounds of the formula I and X is shown in scheme A. the Chemistry is simple and in the end stage includes the protection of the parent substance of the amino acids (a) N obtaining the appropriate amino acids (II)containing a protective group of the protected amino acid (II)), the interaction of the protected amino acid (II) with diazomethane, followed by processing for adding carbon atoms to obtain the corresponding containing a protective group of the compound (III), the recovery of protected halide to the corresponding alcohol (IV), the formation of the corresponding epoxide (V), the opening of the epoxide (V) With-terminal amine Rc-NH2(VI) to produce the corresponding protected alcohol (VII). The compounds of formula (I) can be obtained by the interaction of the protected alcohol (VII) with amidoamines agent such as, for example, (RN-)2O or RN-X or RN-OH (IX), with the formation of alcohol (IA). Then of alcohol (IA) remove azatadine group and obtain the corresponding compounds of formula (I). The compounds of formula (X) can be obtained by additional protection N alcohol (VII) with the formation of alcohol with two protective groups (XB). Alcohol with two protective groups (XB) enter into interaction with amidoamines agent such to the to, for example, (RN-)2O or RN-X or RN-OH (IX), with the formation of compound (HA). Then from the compound (HA) remove the protective group and obtain the corresponding compounds of formula (X). Specialists in the art it will be clear that all of these interactions are well-known reactions in organic chemistry. Specialist in the field of chemistry, knowing the chemical structure of compounds according to the invention (AA), (I) and (X)will be able to get them by known methods from known starting compounds without any additional information. Therefore, in the explanation below, it is not necessary, but, as expected, will help professionals in the art wishing to obtain compounds of the invention. The main chain of the intermediate compound (VII)from which you can easily obtain compounds of formula (AA), (I) and (X)can be considered as hydroxyethylamino group-NH-CH(R)-CH(OH)-. These key chains can be obtained by methods described in literature and known to experts in this field of technology. For example, in J. Med. Chem., 36, 288-291 (1993), Tetrahedron Letters, 28, 5569-5572 (1987), J. Med. Chem., 38, 581-584 (1995), Tetrahedron Letters, 38, 619-620 (1997) and WO 02/02506 describes methods of making compounds of the type hydroxyethylamine and/or intermediates for them. Chart a shows the General method used in the invention to obtain appropriate is Estulin way of substituted amines I and H. Compounds according to the invention receives from the corresponding amino acids (And). Amino acid (S) known to experts in the art or can be easily obtained by methods known to experts in this field of technology. Compounds of the invention have at least two chiral centers, which provide two sets of diastereomers, each of which is a racemic for all of the at least four stereoisomers. Although biologically active end products are obtained from all of the stereoisomers, the preferred configuration (S,R). The first of these chiral centers (carbon bearing R1it derives from the original amino acid (S). Commercially, it is preferable to obtain or produce the desired enantiomer and not enantiomerically impure mixture, followed by the necessary selection of the desired enantiomer. Thus, it is preferable to start the process with enantiomerically pure (S)-amino acids (And) the same configuration as the desired product X. On the diagram And shows the introduction of a protective group to the free amino acid (A) with the formation of (S)-protected amino acid (II). Group, protection for the amino group, known to experts in the art, and are discussed below. See, for example, "Protecting Groups in Organic Synthesis", John Wiley and sons, New York, N.Y., 1981, Chapter 7; "Protecting Groups in Organic Chemistry", Plenum Press, New York, N.Y., 1973, Chapter 2. F. what nccia group, protective for the amino group, is to protect the free functional amino group (-NH2during subsequent interactions with (S)-amino acid (A), which will not leak or amino groups, which can interact and show functionality on the track or incompatible with the necessity of freedom for subsequent interactions, or a free amino group may intervene in the interaction. When the group, protection for the amino group, then it is not required, it is removed by methods known to experts in this field of technology. By definition, group, protective for amino groups, should be easily removed, as is known to experts in the art by methods known to experts in this field of technology. Suitable protective groups for the amino group are described below. (S)-Protected amino acid (II) is transformed into the corresponding (S)-protected compound (III) in two different ways, depending on the nature of R2and R3. R2and R3may be the same or different. Preferably, R2and R3- both were a-N. If R2and R3are not the same, in the molecule, an additional chiral center or stereogenic center. In order to obtain the compounds of formula (III), where R2and R3- both are the a-N, (S)-protected amino acid (II) enter into interaction with diazomethane, as is well known to specialists in this field of technology, with subsequent interaction with the compound of the formula H-X1and get (S)-protected compound (III). X1includes-Cl, -Br, -I, -O-tosylate, -O-mesilate, -O-nosrat and-About-brasilit. Preferably, X1was a-Br or-Cl. Appropriate interaction terms is to carry out the reaction in inert solvents, such as ether, tetrahydrofuran, and other similar solvents. Reactions of transition from (S)-protected amino acid (II) to (S)-protected compound (III) is carried out for a time from 10 minutes to 1 day, and at temperatures ranging from about -78aboutC to about 20-25ºC. It is preferable to conduct the reaction for about 1-4 hours and at temperatures from-30ºC up to-10ºC. This method allows you to add one methylene group. On the other hand, (S)-protected compound of formula (III) can be obtained by turning the first, (S)-protected amino acid (II) into the corresponding methyl or ethyl ester, according to the methods adopted in the technique, followed by treatment with a reagent of the formula X1-C(R2)(R3)-X1and strong metal base. The reason is to influence the exchange of the halogen-metal, X1undergoing change, made the focus of a halogen, selected from among chlorine, bromine or iodine. Nucleophilic joining ether derivative gives (S)-protected compound (III). Suitable bases are alkality, including, for example, second-utility, n-utility and tert-utility, and other reasons. The reaction is preferably carried out at a low temperature, such as-78ºC. Suitable reaction conditions include carrying out the reaction in inert solvents, such as ether, tetrahydrofuran, and other similar solvents. When R2and R3- both represent hydrogen, then examples X1-C(R2)(R3)-X1are dibromethane, diiodomethane, chloromethane, bromomethane and bromochloromethane. Specialists in this field known in the art, the preferred conditions necessary for such interaction. In addition, if R2and/or R3are not-H, then by adding C(R2)(R3)-X1to the ester (S)-protected amino acid (II) to obtain (S)-protected compound (III) in the reaction product is introduced an additional chiral center, provided that R2and R3are not the same. Then (S)-protected compound (III) restoring means known to specialists in this field of technology for the recovery of the ketone to the corresponding secondary with the IRT, and receive the corresponding alcohol (IV). Means and conditions of the reduction reaction of (S)-protected compound (III) to the corresponding alcohol (IV) include, for example, sodium borohydride, lithium borohydride, borane, hydride diisobutylaluminum and alumoweld lithium. Sodium borohydride is the preferred reducing agent. The restoration carried out in the period of time from 1 hour to 3 days at temperatures ranging from-78ºC to the temperature increased up to the boiling point of the used solvent. It is preferable to carry out the restoration of the between-78ºC and 0ºC. If using borane, it can be used in the form of a complex such as borane complex-metilsulfate, complex, borane-piperidine or a complex of borane-tetrahydrofuran. Preferred combinations necessary reducing agents and reaction conditions known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989. Recovery of (S)-protected compound (III) to the corresponding alcohol (IV) gives the second chiral center (third chiral center, if R2and R3are not the same). Recovery of (S)-protected compound (III) gives a mixture of enantiomers according to the second centre (S, R/S)-alcohol (IV). Then this enantiomeric mixture separated by methods known to experts in the field of technology, such as selective the recrystallization at low temperatures or chromatographic separation, for example HPLC, using commercially available chiral columns. Enantiomer, which is then used in the method according to scheme a, is a (S,S)-alcohol (IV), such as enantiomer will give the desired (S,S)-substituted compound I or X. (S,S)-Alcohol (IV) is transformed into the corresponding epoxide (V) by means known to specialists in this field of technology. The stereochemistry of the centre (S)to(IV) in the formation of the epoxide (V) is retained. The preferred method is the interaction with a base, such as hydroxide ion formed from sodium hydroxide, potassium hydroxide, lithium hydroxide and other similar reasons. Reaction conditions include the use of solvents of alcohols With1-C6; preferred is ethanol. You can also use regular co-solvent, such as, for example, ethyl acetate. The reaction is carried out at temperatures ranging from-45ºC to the boiling point of the used alcohol; the preferred temperature intervals are between-20ºC and 40ºC. An alternative, and preferred, method of production of the epoxide (V)when R1represents 3,5-diferensial presented in figure D. the First stage of the method is to protect the free amino group (S)-amino acids (A) group, protective for amino - protecting group, previously described for obtaining (S)-Conn is Noah amino acids (II). In the alternative method (S)-protected amino acid (A) is transformed into the corresponding (S)-protected ester (XVII) one of a number of ways. One method involves the use of lithium hydroxide. Using lithium hydroxide (S)-protected amino acid (a) and lithium hydroxide are mixed and cooled to a temperature of from about -20 to about 10ºC. Then add metymirumi agent selected from the group consisting of dimethylsulfate, under the conditions and metallifere. Preferably, meteorous agent was dimethylsulfate. Followed by heating to a temperature of from about -20 to about 50ºC. On the other hand, (S)-protected amino acid (A) enter into contact with a weak base, such as bicarbonate or preferably carbonate. Then add metymirumi agent. Heating is not necessary, but it can be used to facilitate interaction. Carbonate method known to specialists in this field of technology. In the case of (S)-protected ester (XVII)in which Z1is not the stands, the specialist in the art, knowing the chemical structure is known how to obtain the necessary connections from known starting materials. In one known method (S)-protected amino acid (A) enter into contact with an activating agent such as DCC, followed by adding suitable the alcohol Z 1-HE. This method works when Z1is a (C1-C4)-alkyl (optionally substituted), -CH2-CH=CH2or phenyl (optionally substituted). Scheme E illustrates an alternative method of obtaining of ester (II). In the method of scheme E aldehyde (XX), well-known specialists in the field of technology, enter into interaction with the connection phosphorus (XXI), where X3represents an easily removable group, and get olefin (XXII). Phosphorus compounds (XXI) are known to specialists in this field of technology. Preferably, X1was a (C1-C3)-alkyl; preferably, X1represented With1-alkyl. The aldehyde (XX) and phosphate (XXI) are combined in an organic solvent and then cooled to 0ºC. Add a base, such as DBU or TMG, and the contents of the reaction mixture is heated to about 20 ░ to 25 ░ C and stirred until then, until the reaction is complete. Once the reaction is complete, it is preferable to divide the E - and Z-olefin isomers (XXII). The separation is carried out by methods known to experts in the art such as chromatography on silica gel. Then the olefin (XXII) hydronaut using a suitable hydrogenation catalyst and get the desired ester (II). Some hydrogenation reactions will give racemize the cue ester (II). The desired stereochemistry of ester (II) is (S)-and therefore it is preferable to use the Z-olefin (XXII) with a hydrogenation catalyst. Preferably, the hydrogenation catalyst was represented by a compound of the formula [Rh(diene)L]+X-, where Rh is a rhodium; where the diene is cyclooctadiene and norbornadiene; where L represents the DIPMAP, MeDuPhos, EtDuPhos, Bintan, f-Bintan, IU-KetalPhos, IU-f-KetalPhos, BINAP, DIOP, BPPFA, BPPM, CHIRAPHOS, PROPHOS, NORPHOS, CYCLOPHOS, BDPP, DEGPHOS, PNNP, and where X-is a ClO4-BF4-, CF3-SO3-, Cl-, Br-PF6-and SbF6-. Preferably, the hydrogenation catalyst was or DIPMAP or EtDuPhos. Suitable solvents are polar solvents, such as alcohols, preferably alcohols With1-C5and THF, preferably methanol, ethanol, isopropanol and THF. Chiral hydrogenation is carried out in a temperature range from about -20 to about the temperature of education phlegmy. Preferably, the interaction was carried out in the temperature range from about 0 to about room temperature (25ºC). Chiral hydrogenation is carried out at a pressure of from about one atmosphere to about 100 f/d2; preferably, the chiral hydrogenation of implementing Talos at a pressure of from about 10 f/d 2up to about 40 f/d2. Then (S)-protected ester (II) is transformed into the corresponding (S)-protected ketone (III) interaction with a slight excess of the compound of the formula CH2ClX2where X2is a-Br and-I, one of two different ways. In the same way do not use exogenous nucleophiles. This method requires (1) the presence of three or more equivalents of a strong base with pKbmore than about 30, and then (2) adding acid. The other method requires (1) the presence of from about 2 to about 2.5 equivalents of a strong base with pKbmore than about 30, (2) introducing into contact with the mixture from step (1) with from about 1 to about 1.5 equivalents of exogenous nucleophile and (3) the addition of an acid. Suitable strong bases are bases that have pKbmore than about 30. Preferably, the strong base is selected from the group consisting of LDA, LiHMDS and KHMDS; rather, a strong reason was that the LDA. Suitable acids are acids with pKandless than about 10. Preferably, the acid is selected from the group consisting of acetic, sulfuric, chloroethanol, citric, phosphoric, and benzoic acids; preferably, the acid represented acetic acid. The preferred solvent is THF. Usaimage the dance can be performed in the temperature range from about-80ºC until about-50ºC; it is preferable to carry out the interaction in the temperature range from about-75ºC to about-65ºC. Suitable nucleophiles are alkality, ability, alkyl - and arylesterase Grignard reagents. Preferably, the nucleophile selected from the group consisting of finelite, n-utility, methylacrylamide, methylacrylamide, phenylmagnesium, formanilide; preferably, the nucleophile was n-utility. Then (S)-protected ketone (III) is reduced to the corresponding (S)-alcohol (IV) by methods known to experts in the art for recovery of the ketone to the corresponding secondary alcohol. Means and reaction conditions for recovery (S)-protected compound (III) to the corresponding alcohol (IV) include, for example, sodium borohydride, lithium borohydride, borane, hydride diisobutylaluminum, zinc borohydride and alumoweld lithium. Sodium borohydride is the preferred reducing agent. The restoration carried out over a period of time from about 1 hour to about 3 days at temperatures ranging from about-78ºC to the temperature increased up to the boiling point of the used solvent. Preferably restoration at a temperature of from about to about 70ºC 0ºC. If using borane, it can be used in the form of sets the KSA, for example, a complex of borane-metilsulfate, complex, borane-piperidine or a complex of borane-tetrahydrofuran. Preferred combinations necessary reducing agents and reaction conditions known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989. Recovery of (S)-protected compound (III) to the corresponding alcohol (IV) gives the second chiral center. Recovery of (S)-protected compound (III) gives a mixture of diastereomers according to the second centre (S, R/S)-alcohol (IV). Then this diastereomers the mixture is separated by methods known to experts in the field of technology, such as selective recrystallization at low temperatures or chromatographic separation, the most preferred recrystallization or the use of commercially available chiral columns. The diastereoisomer, which is then used in the method according to scheme a, is a (S,S)-alcohol (IV), such as stereochemistry will give the desired epoxide (V). The alcohol (IV) is transformed into the corresponding epoxide (V) by means known to specialists in this field of technology. The stereochemistry of the centre (S)to(IV) in the formation of the epoxide (V) is retained. The preferred method is the interaction with the base, such as hydroxide ion formed from sodium hydroxide, potassium hydroxide, lithium hydroxide and other similar reasons. Reaction conditions include the use as solvents alcohols With1-C6; preferred is ethanol. You can also use regular co-solvent, such as, for example, ethyl acetate. The reaction is carried out at temperatures ranging from about-45ºC to the boiling point of the used alcohol; the preferred temperature intervals are between about -20 and about 40ºC. Then the epoxide (V) enter into interaction with the appropriately substituted C-terminal amine Rc-NH2(VI) by methods known to experts in the field of technology, which opens the epoxide with the formation of the desired corresponding enantiomerically pure (S,R)-protected alcohol (VII). Substituted C-terminal amine Rc-NH2(VI) this invention are commercially available or known to experts in the art and can be easily obtained from known compounds. Preferably, Rcwas substituted in position 3 or the provisions of 3.5, when he represents phenyl. Suitable reaction conditions for opening the epoxide (V) include the reaction takes place in a wide range of conventional and inert solvents. Preferred are alcohols With1-C6and the most preferable isopropyl alcohol. The reaction can be conducted at temperatures to replysize from 20-25 ° C to the boiling point of the used alcohol. The preferred temperature range for the reaction is from 50ºC to the boiling point of the used alcohol. When the substituted C-terminal amine (VI) is 1-amino-3,5-CIS-dimethylcyclopropanecarboxylate, it is preferably prepared as follows. It dimethyl-5-isophthalate in acetic acid and methanol in a thick-walled flask add the rhodium in the aluminum oxide. The contents of the flask is saturated with hydrogen at a pressure of 55 f/d2and shaken for one week. The mixture is then filtered through a thick layer of celite, celite is washed three times with methanol, the solvents are removed under reduced pressure (when heated) and get the concentrate. The concentrate is treated with ether and again filtered and receive the desired C-terminal amine (VI). When the substituted C-terminal amine (VI) is 1-amino-3,5-CIS-dimethoxytoluene, it preferably receive, following the General procedure described above and making non-critical changes, but based on 3,5-dimethoxyaniline. When the substituted C-terminal amine (VI) contains aminomethyl group, where the substituent in the methyl group is an aryl group, such as, for example, NH2-CH2is aryl, it is not available, and it is obtained preferably as follows. A suitable starting material is a (relevant about what atom substituted) arylalkyl connection. The first stage is the bromination of alkyl substituent methods known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, R. Then alkylhalogenide enter into interaction with azide and get aryl(alkyl)azide. Finally, the azide is reduced to the corresponding amine (VI) in the system hydrogen/catalyst and receive a C-terminal amine (VI) of the formula NH2-CH2-Rc-aryl. Scheme reveals an alternative way of obtaining enantiomerically pure (S,R)-protected alcohol (VII) of (S)-protected compound (III). In this way, (S)-protected compound (III) is first introduced in the interaction with the appropriately substituted C-terminal amine Rc-NH2(VI) using the preferred conditions described above, and receive the corresponding (S)-protected ketone (XI), which is then restored using the preferred conditions described above, and receive the corresponding (S,R)-protected alcohol (VII). The scheme discloses another alternative method of obtaining enantiomerically pure (S,R)-protected alcohol (VII), but this time of the epoxide (V). In the method according to the scheme With the epoxide (V) enter into interaction with azide and receive the corresponding enantiomerically pure (S,R)-protected azide (XII). Conditions azidopirimidinov disclosure EP is xida well-known specialists in the field of technology see, for example, J. March, Advanced Organic Chemistry, 3rdEdition, John Wiley & Sons Publishers, 1985, p.380. Then (S,R)-protected azide (XII) is reduced to the corresponding amine (XIII) by methods known to experts in this field of technology. The preferred conditions of the recovery (S,R)-protected azide (XII) in the presence of N-protective tert-butoxycarbonyl groups include catalytic hydrogenation, the terms of which are well-known specialists in this field of technology. Alternative terms of recovery, which can be used to avoid removal of the protective group from the N-protected by other protective groups than tert-butoxycarbonyl, known to experts in the art, see, for example, R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, R. Finally, (S,R)-amine (XIII) is converted into the corresponding protected alcohol (VII) by alkylation of the nitrogen compound of the formula RWith-X3. X3is a corresponding delete the group, such as-Cl, -Br, -I, -O-mesilate, -O-tosylate, -O-triflate etc., and other groups. X3may also be an aldehyde; an appropriate combination of (XIII) by means of known procedures reductive amination gives protected (S,R)-alcohol (VII). In the formation of compounds of formula (I) - protected alcohol (VII) enter into interaction with accordingly Zam is on aminoaldehydes agent (IX), such as, for example, anhydride, allalone or acid of the formula (RN)2O or RNX or RNOH, respectively, by methods known to experts in the art, and receive the corresponding (S,R)-substituted amine (IA). Conditions of acylation of the nitrogen to the interaction of alcohol (VII) with aminoaldehydes agent (IX) to obtain the corresponding compounds (IA) are known to experts in the art and can be found, for example, in R.C. Larock, Comprehensive Organic Transformations, VCH Publishers, 1989, SS. 981, 979 and 972. From (S,R)-protected amine (IA) remove the protective group with formation of the corresponding compounds (I) by methods known to experts in the art to remove aminosidine group. Suitable means for removing aminosidine group depends on the nature of the protective group. Experts in the art, knowing the specific nature of the protective group, you know, what is the preferred reagent to remove it. For example, it is preferable to remove the preferred protective group BOC, dissolving (S,R)-protected amine (IA) in a mixture triperoxonane acid/dichloromethane (1:1). After removal of the solvents removed under reduced pressure and get the corresponding (S,R)-amine (I) (in the form of a corresponding salt, i.e. salt triperoxonane acid), which is used without further purification. But what if appropriate (S,R)-amine (I) can be cleaned advanced methods, well-known experts in the art, such as, for example, recrystallization. Further, if desired nosoleva form, this form can also be obtained by methods known to experts in the art, such as, for example, to obtain the free base amine by treatment of the salt in a moderately alkaline medium. Other conditions of removal of the protective group BOC and terms of remove other protective groups can be found in T.W. Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991, p.309. Chemically suitable salts are triptorelin and salt containing the anion of a mineral acid such as chloride, sulfate, phosphate; preferred is triptorelin. In the formation of compounds of formula (X) alcohol (VII) also protects as described above, with the formation of desasosiego connection (XB). Then the compound (XB) enter into interaction with an appropriately substituted aminoaldehydes compound (IX) with the formation of compound (HA), as described above for compound (IA). Removing the protective groups from the compound (HA) to form compounds (X) are as described in the case of the conversion of compounds (IA) to the compound (I). Removing the protective groups of the amines is carried out, if necessary, by methods known to experts in this field of technology. Aminosidine group of renowned experts in the Noah engineering. See, for example, "Protective Groups in Organic Chemistry", John Wiley and Sons, New York, N.Y., 1981, Chapter 7; "Protective Groups in Organic Chemistry", Plenum Press, New York, N.Y., 1973, Chapter 2. When aminosidine group is no longer needed, it is removed by methods known to experts in this field of technology. By definition, aminosidine group should easily be removed. Many different methodologies known to experts in the art; see, for example, also Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991. Suitable aminosidine groups are tert-butoxycarbonyl, benzyloxycarbonyl, formyl, trityl, phthalimido, trichloroacetyl, chloroacetyl, bromoacetyl, iodoacetyl, 4-phenylbenzoxazole, 2-methylbenzyloxycarbonyl, 4-ethoxybenzothiazole, 4-forantimicrobial, 4-chlorobenzenesulfonyl, 3-chlorobenzylidene, 2-chlorobenzenesulfonyl, 2,4-dichlorobenzenesulfonyl, 4-bromobenzyloxycarbonyl, 3-bromobenzyloxycarbonyl, 4-nitrobenzenesulfonyl, 4-cyanobenzeneboronic, 2-(4-xenil)isopropoxycarbonyl, 1,1-diffenret-1-jocstarbunny, 1,1-diphenylprop-1-jocstarbunny, 2-phenylprop-2-jocstarbunny, 2-(p-toluyl)prop-2-jocstarbunny, cyclopentanecarbonyl, 1-methylcyclopentadienyl, cyclohexyloxycarbonyl, 1-methylcyclohexanecarboxylic, 2-methylcyclohexanecarboxylic, 2-(4-toluensulfonyl)etoxycarbonyl, 2-(methylsulphonyl)is oxycarbonyl, 2-(triphenylphosphino)etoxycarbonyl, fluorenylmethoxycarbonyl, 2-(trimethylsilyl)etoxycarbonyl, allyloxycarbonyl, 1-(trimethylsilylmethyl)prop-1-relaxerror, 5-benzisothiazolinone, 4-acetoxybenzoic, 2,2,2-trichlorocyanuric, 2-ethinyl-2-propoxycarbonyl, cyclopropanecarbonyl, 4-(decyloxy)benzyloxycarbonyl, isobornylacitate, 1-piperidinylcarbonyl, 9-fluorenylmethoxycarbonyl, -CH-CH=CH2and phenyl-C(=N -). Preferably, the protective group represented tert-butoxycarbonyl (VOS) and/or benzyloxycarbonyl (CBZ), it is preferable that the protective group represented tert-butoxycarbonyl. Specialist in the art will know the appropriate ways of introducing tert-butoxycarbonyl or benzyloxycarbonyl protective group and may additionally be accessed as a guide to the Green and P.G.M. Wuts, "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991. Compounds according to the invention can be geometric or optical isomers, and tautomers. Thus, the invention includes all tautomers and pure geometric isomers such as E - and Z-geometric isomers, and mixtures thereof. In addition, the invention includes the pure enantiomers and diastereoisomers, and also mixtures thereof, including racemic mixtures. Single geometric isomer, enantiomer is or diastereomers can be obtained or highlight ways, well-known experts in the art, including chiral chromatography; obtaining diastereomers, separating the diastereomers and converting the diastereoisomers of enantiomers using chiral decomposing agent and other methods. Compounds of the invention with the planned stereochemistry can log in mixtures, including racemic mixtures, with other enantiomers, diastereomers, geometric isomers or tautomers. In a preferred aspect of compounds of the invention with the stereochemistry of (S, R, R), (S, S, S) or (S, R, S) in such mixtures are present in more than 50%. Preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 80%. Preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 90%. More preferred compounds of the invention with the planned stereochemistry of these compounds are present in more than 99%. The invention encompasses pharmaceutically acceptable salts of compounds of formula (AA), (I) and (X). Pharmaceutically acceptable salts are preferred over the corresponding amines of formula (AA), (I) or (X), as they give compounds which are more water soluble, stable and/or more crystalline. Pharmaceutically who ielemia salt is any salt, which retains the activity of the parent compound and does not produce any harmful or unwanted actions of the entity to which it is administered and in the context in which it is injected. Pharmaceutically acceptable salts include salts of both inorganic and organic acids. Preferred pharmaceutically acceptable salts are acid salts, acetic, aspartic, benzosulfimide, benzoic acid, bicarbonate, bisulfate, bitartrate, butyric acid, calcium salt of ethylenediaminetetraacetic acid, acid Kamilova, coal, chlorbenzene, lemon, ethylenediaminetetraacetic, agisilaou, Astroboy, asilinae, silovoi, formic, fumaric, gluceptate, gluconic, glutamic, picolylamine, examinados, hexylresorcinol, geranamine, Hydrobromic, chloroethanol, iodomethane, hydroxynaphthoic, italianboy, lactic, lactobionic, maleic, malic, malonic, almond, methansulfonate, metolazone, metallernas, mucus, Mukanova, natsiavas, nitric, oxalic, p-micrometeorology, pambou, Pantothenic, phosphoric, disubstituted phosphate, monosubstituted phosphate, phthalic acid, polygalacturonases, propionic, salicylic, stearic, succinic, sulfamic, sulfanilic, sulfonic, sulfuric, tannic, the wine, tolovaj, toloo the sulfonic. About other acceptable salts, see Int. J. Pharm., 33, 201-217 (1986)and J. Pharm. Sci., 66(1), 1 (1977). The invention relates to compounds, compositions, kits and methods for inhibiting the enzymatic activity of beta-secretase and production of peptide A-beta. Inhibition of the enzymatic activity of beta-secretase stops or reduces the production of A-beta from the RDA and reduces or eliminates the formation of beta-amyloid deposits in the brain. The methods of the invention Compounds according to the invention and their pharmaceutically acceptable salts are suitable for the treatment of humans or animals suffering from a condition characterized by a pathological form of beta-amyloid peptide, such as beta-amyloid plaques, and to promote the prevention or delay the emergence of such a state. Used in this description, the term "treatment" means that the compounds of the invention can be used for people with at least a presumptive diagnosis of the disease. Compounds of the invention will delay or slow the progression of the disease, whereby the individual provides much greater life expectancy. The term "prevention" means that the compounds of the invention are suitable, when you enter the patient has no diagnosis possible presence of disease at the time of introduction, but whose natural the public to expect the development of the disease or increased risk of disease. Compounds according to the invention will slow the progression of symptoms of the disease, to delay the appearance of the disease or even prevent the individual from developing the disease. Prevention also includes the introduction of compounds of the invention to those individuals suspected of predisposition to disease because of age, family history, genetic or chromosomal abnormalities, and/or because of the presence of one or more biological markers of disease, such as a known genetic mutation of APP or cleavage products of APP in the tissues or fluids of the brain. In the treatment or prevention of the above diseases, the compounds of the invention are administered in therapeutically effective amounts. therapeutically effective amount will greatly vary depending on the specific compound and the method of administration, which is known to specialists in this field of technology. When treating a patient who has diagnosed with any of the above conditions, the doctor may prescribe a compound of the invention immediately and continue the introduction of the unlimited, as required. In the treatment of patients who are not diagnosed with Alzheimer's disease, but which, considered to be facing a significant risk of developing Alzheimer's disease, the physician should preferably start the treatment when the patient COI is melting the first early symptoms, prior Alzheimer's disease, such as problems with memory and cognition associated with aging. In addition, there are some patients for whom it is possible to determine that they are in danger of developing Alzheimer's disease through the detection of a genetic marker, such as AREA, or other biological indicators that predict Alzheimer's disease. In such situations, even if the patient has no symptoms of the disease, the introduction of the compounds of the invention can be started before the onset of symptoms, and the treatment can be continued indefinitely to prevent or delay onset of the disease. Dosage forms and number Compounds according to the invention can be administered orally, parenterally (IV, IM, depo-IM, SQ, and depo-SQ), sublingual, intranasally (inhalation), vnutriobolochechnoe, topically or rectally. Pharmaceutical form known to the person skilled in the art are suitable for delivery of the compounds according to the invention. Provide compositions containing therapeutically effective amounts of compounds according to the invention. The connection is preferably introduced into suitable pharmaceutical preparations such as tablets, capsules or elixirs for oral administration or in sterile solutions or suspensions for parenteral administration. Typically, the compounds described above, putting the t into pharmaceutical compositions using techniques and procedures, well known in the art. About 1-500 mg of the compound or mixture of compounds according to the invention or their physiologically acceptable salts or esters combined with a physiologically acceptable excipient, carrier, excipient, binder, preservative, stabilizer, flavorants, etc. in a unit dosage form by methods accepted pharmaceutical practice. The amount of active substance in these compositions or preparations is such that you are getting the right dosage at the specified interval. The composition is preferably prepared in the form of a unit dosage form, each dosage containing from about 2 to about 100 mg, preferably from about 10 to about 30 mg, of the active ingredient. The term "unit dosage form" refers to physically discrete units suitable as single doses to humans and other mammals, each unit contains a preset amount of the active substance is calculated in order to obtain the desired therapeutic effect, in combination with a suitable pharmaceutical excipient. In order to obtain compositions, one or more compounds according to the invention is mixed with a suitable pharmaceutically acceptable carrier. After mixing or addition of the compound(s) obtained mixture may be a p is the target, suspension, emulsion or similar form. Liposomal suspensions can also be suitable as pharmaceutically acceptable carriers. They can be obtained according to methods known to experts in this field of technology. The shape of the resulting mixture depends upon a number of factors, including the intended route of administration and the solubility of the compounds in the selected carrier or filler. The effective concentration is the concentration that is sufficient to attenuate or reduce at least one symptom of a disease, disorder or condition which is treatable and can be determined empirically. Pharmaceutical carriers or excipients suitable for administration of the compounds described herein include any such carriers known to experts in the art as suitable for a particular method of administration. In addition, the active substance can also be mixed with other active materials that do not weaken the desired action, or with substances that Supplement the desired action, or have a different action. Compounds can be introduced into the composition as the sole pharmaceutically active ingredient in the composition or can be combined with other active ingredients. When the connection detect low solubility, can be used in the th methods of solubilization. Such methods are known and include the use of co-solvents, such as dimethylsulfoxide (DMSO), using surfactants, such as tween®, and dissolution in aqueous solution bicarbonate sodium, and other ways. Derivative compounds, such as salts or prodrugs can also be used to obtain effective pharmaceutical compositions. The concentration of the compound is effective for delivery after the introduction of a number that weakens or reduces the intensity of at least one symptom of the disorder, which enter the connection. Typically, the compositions have for a single dose. Compounds of the invention can be introduced into the drug with carriers that protect them against rapid removal from the body, such as the composition with the gradual release of, or coated. Such media include compositions for controlled release, such as microencapsulation delivery systems, and others. Active connection include pharmaceutically acceptable carrier in a quantity sufficient for the manifestation of therapeutically useful effect in the absence of undesirable side effects on the patient treated. therapeutically effective concentration may be determined empirically testing the connection on the well-known m the sensible systems in vitro and in vivo for the disorder, from where they treat. Compounds and compositions of the invention can be enclosed in packaging one or more techniques. Packed compounds and compositions can be provided in sets, for example, contains elements that can be connected for use. For example, the connection-inhibitor in liofilizovannyh form and a suitable diluent can be provided in the form of separate components to merge before use. The set can include a connection-inhibitor and another therapeutic agent for joint injection. The inhibitor and the second therapeutic agent can be provided in the form of individual components. The set can include several packages, with each package contains one or more standard doses of the compounds of the invention. Packing is preferably adapted for the desired method of administration, including tablets, soft capsules, capsules, delayed release, etc. for oral administration; products of prolonged action, pre-filled syringes, ampoules, vials, etc. for parenteral administration; and labels, patches, creams, etc. for local injection. The concentration of the active compounds in the composition of the medicinal product will depend on the speed of absorption, inactivation and excretion of the active connection scheme application Lakers the governmental funds and the input quantity, as well as other factors known to specialists in this field of technology. The active ingredient can be injected once or divided into several smaller doses for insertion through a certain period of time. It should be borne in mind that the precise dosage and duration of treatment depends on the disease that is treatable and can be determined empirically using known testing protocols or by extrapolation of the test results in vivo or in vitro. It should be noted that the concentration and size of doses may also vary due to the severity of the condition with a partial withdrawal symptoms. It should also be borne in mind that for any particular subject, specific patterns of use of the medicinal product must be adjusted over time according to individual needs and professional assessment of the person making the introduction of, or control over the introduction of the compositions, and that the intervals of the concentrations mentioned in this description are only examples and are not intended to limit the scope or the practical application of the inventive compositions. If it is desirable oral administration, the connection should be provided in a composition that protects it from the active medium in the stomach. For example, it is possible to obtain a composition with intersolubility coating which retains its entirety the guard in the stomach and releases the active compound in the gut. It is also possible to obtain compositions in combination with antacid agent or the other ingredient. Oral compositions generally will contain an inert diluent or edible carrier and can be compressed into tablets or enclosed in gelatin capsules. For purposes of oral administration for the treatment of active compound or compounds can be combined with excipients and used in the form of tablets, capsules or lozenges. Pharmaceutically compatible binding agents, and adjuvants may be included as part of the composition. Tablets, pills, capsules, lozenges and the like can contain any of the following ingredients, or compounds of a similar nature: a binder such as tragacanth resin, Arabian gum, corn starch or gelatin, or a similar substance; excipients, such as microcrystalline cellulose, starch or lactose; disintegrant, such as alginic acid, corn starch, or the like; a lubricant such as magnesium stearate or the like; glidants, such as colloidal silicon dioxide, or the like; sweeteners such as sucrose or saccharin; and flavorant, such as peppermint, methyl salicylate or fruit substance. When the unit dosage form is a capsule, it may contain, in addition to the substances of the above type, a liquid is osiel, such as fatty oil. In addition, the standard dosage forms can contain various other materials which modify the physical form of the dosage form, for example, coatings of sugar and other intersolubility substances. Connections can also be entered as a component of an elixir, suspension, syrup, wafer, chewing gum or the like. A syrup may contain, in addition to the active compounds, sucrose as a sweetener and certain preservatives, dyes and tinted substance and flavorant. The active substance can also be mixed with other active materials that do not weaken the desired action, or with substances that Supplement the desired action. Solutions or suspensions used for parenteral, intradermal, subcutaneous, or topical application can include any of the following components: a sterile diluent such as water for injection, saline solution, fixed oil, a naturally occurring vegetable oil such as sesame oil, coconut oil, peanut oil, cottonseed oil and the like, or synthetic fatty filler, such as etiloleat and the like, polyethylene glycol, glycerine, propylene glycol or other synthetic solvent; antimicrobial agents, such as benzyl alcohol and methylparaben; antioxidants, such as ascorbic acid and sodium bisulfite; hepatoblastoma agents such as ethylenediaminetetraacetic acid (edtc); buffering agents such as acetates, citrates and phosphates; and agents to achieve isotonicity, such as sodium chloride and dextrose. Parenteral preparations can be enclosed in ampoules, syringes disposable or vessels in multiple doses, made of glass, plastic or other suitable material. Optionally, you can include buffering agents, preservatives, antioxidants, etc. For intravenous administration, suitable carriers are saline, phosphate buffered saline (SFR) and solutions containing thickening agents and soljubilizatory, such as glucose, polyethylene glycol, polypropyleneglycol and mixtures thereof. Liposomal suspensions containing darinaparsin liposomes, may also be suitable as pharmaceutically acceptable carriers. They can be obtained according to known methods, for example as described in U.S. patent No. 4522811. The active compounds can be introduced into the drug with carriers that protect the compound against rapid removal from the body, such as the composition with the gradual release of, or coated. Such media include compositions for controlled release, such as implants and microencapsulation system dostavka the other, and biodegradable, biocompatible polymers, such as collagen, a copolymer of ethylene and vinyl acetate, polyanhydrides, polyglycolic acid, complex poliorcetes, polylactic acid and other Methods of obtaining such compositions are well-known specialists in this field of technology. The compound of the invention can be administered orally, parenterally (IV, IM, depo-IM, SQ, and depo-SQ), sublingual, intranasally (inhalation), vnutriobolochechnoe, topically or rectally. Pharmaceutical form known to experts in the art and are suitable for delivery of the compounds of the invention. The compound of the invention can enter interline or parenteral. When administered orally, the compounds of the invention can be introduced in the form of conventional pharmaceutical forms for oral administration are well known to the specialists in this field of technology. Such dosage forms include tablets and capsules) and liquid dosage forms such as solutions, suspensions and elixirs. When using solid dosage forms, preferably so that they are type forms with delayed release, so that compounds of the invention need to enter only once or twice a day. Oral dosage form is administered to the patient 1, 2, 3 or 4 times a day. Preferably, the connection izobreteny is introduced or three or fewer times, preferably only once or twice a day. Therefore, it is preferable that the compounds of the invention were administered in oral dosage form. Preferably, whatever dosage form is not used, it was created so that the compounds of the invention are protected from the acidic environment of the stomach. Specialists in the art of well-known tablets intersolubility coating. In addition, specialists in the art is also well-known capsules, filled with small spheres coated to protect it from the acidic environment of the stomach. When administered orally enter the amount therapeutically effective for inhibiting beta-secretase activity, for inhibiting the production of A-beta, for inhibiting the deposition of A-beta, or for treating or preventing AD is from about 0.1 mg/day to about 1000 mg/day. Preferably, the oral dosage ranged from about 1 mg/day to about 100 mg/day. Preferably, the oral dosage ranged from about 5 mg/day to about 50 mg/day. It should be borne in mind that although the patient may start with one dose, the dose may change over time, so how does the patient's condition. Compounds according to the invention can also be advantageously Dostal shall be composed of nanocrystalline dispersion. The receipt of such compositions is described, for example, in U.S. patent No. 5145684. Nanocrystalline dispersion of HIV protease inhibitors and method of use are described in U.S. patent No. 6045829. Nanocrystalline compositions generally provide greater bioavailability of the compounds of the medicinal product. Compounds according to the invention it is possible to enter parenterally, for example, IV, IM, depo-IM, SQ, or depo-SQ method. When parenteral administration should deliver a therapeutically effective amount of about 0.5 mg/day to about 100 mg/day, preferably from about 5 mg/day to about 50 mg/day. When using the composition-depot injections once a month or once every two weeks, the dose should be from about 0.5 mg/day to about 50 mg/day or a monthly dose of about 15 mg to about 1500 mg Partly due to forgetfulness of patients with Alzheimer's disease it is preferable that a parenteral dosage form had the form of a depot composition. Compounds according to the invention it is possible to enter the hyoid. When the hyoid reception compounds of the invention should be given one to four times a day in amounts described above for IM injection. Compounds according to the invention it is possible to enter the route. To receive such a manner appropriate drug Faure who s have the form of a nasal spray or dry powder, what is known by the experts in this field of technology. The dosage of the compounds according to the invention for intranasal represents the number described above for IM injection. Compounds according to the invention it is possible to enter vnutriobolochechnoe. To receive in this way a suitable dosage form can be a parenteral dosage form, well-known specialists in this field of technology. The dosage of the compounds of the invention for vnutriobolochechnoe introduction represents the number described above for IM injection. Compounds according to the invention can be entered locally. To receive in this way a suitable dosage form can be a cream, ointment or sticker. Due to the insertion amount of the compounds of the invention, it is preferable sticker. The local introduction of the dosage is from about 0.5 mg/day to about 200 mg/day. Because the amount that can deliver the label is limited, you can use two or more labels. The number and size of the labels are not important, and it is important that delivered therapeutically effective amount of the compounds according to the invention, as is well known to specialists in this field of technology. Compounds according to the invention it is possible to enter rectal use suppository, how people know this is the field of technology. With the introduction of using the suppository therapeutically effective amount is from about 0.5 mg to about 500 mg Compounds according to the invention can be entered with the help of implants, as is well known to specialists in this field of technology. With the introduction with implant therapeutically effective amount is the amount described above for the introduction of the depot. Specific compounds according to the invention and the desired dosage form specialist in the art will be able to learn how to obtain and enter the appropriate dosage form. Compounds according to the invention is used in the same way, the same introduction methods using the same pharmaceutical dosage forms and schemes of a medicament which is described above, for prevention or treatment of patients with MCI (mild cognitive impairment) and preventing or delaying the appearance of Alzheimer's disease in those people with MCI may evolve to AD, for treating and preventing down syndrome, for treating humans with hereditary cerebral hemorrhage with amyloidosis (Dutch-Type, for treating cerebral amyloid angiopathy and preventing its potential consequences, i.e. single or repeated lobes hemorrhages, for treating other degeneratively, including dementia of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, and Alzheimer's disease-type diffusion Taurus Levi. Compounds according to the invention can be used in combination with each other or with other therapeutic agents or methods used to treat or prevent conditions listed above. To such means or methods include acetylcholinesterase inhibitors such as taken (tetrahydroaminoacridine, marketed as COGNEX®), donepezil hydrochloride (marketed as Aricept®) and rivastigmine (marketed as Exelon®); inhibitors of gamma-secretase; anti-inflammatory agents, such as inhibitors of cyclooxygenase II; antioxidants, such as vitamin E and ginkolide; immunological methods, such as, for example, immunization with peptide A-beta or antibodies against peptide A-beta; statins and acting directly or indirectly neurotropic agents such as Cerebrolysin®, AIT-082 (Emilieu, 2000, Arch. Neurol., 57:454) and other neurotropic tools, which will appear in the future. In addition, the compounds of formula (AA), (I) or (X) can also be used with inhibitors of P-glycoprotein (P-gp). Inhibitors of P-gp and the use of such compounds is swesty specialists in this field of technology. See, for example, Cancer Research, 53, 4595-4602 (1993), Clin. Cancer Res., 2, 7-12 (1996), Cancer Research, 56, 4171-4179 (1996), international publication WO 99/64001 and WO 01/10387. Importantly, the level of inhibitor of P-gp in the blood is such that it exerts its effect by inhibition of P-gp at lower levels in the blood brain compounds of formula (A). To this end, the inhibitor of P-gp and the compounds of formula (A) can be entered simultaneously in the same or different routes of administration or at different times. It is not the time of introduction, and the presence of an effective level of inhibitor of P-gp in the blood. Suitable inhibitors of P-gp are cyclosporin a, verapamil, tamoxifen, quinidine, vitamin E TGPS, ritonavir, acetate megestrol, progesterone, rapamycin, 10,11-metasedimentary, phenothiazines, acridine derivatives, such as GF120918, FK506, VX-710, LY335979, PSC-833, GF-102,918 and other steroids. It should be borne in mind that they will find other means having the same function and, therefore, reaching the same result; such compounds are also considered suitable. Inhibitors of P-gp can be administered orally, parenterally (IV, IM, depo-IM, SQ, or depo-SQ), topical, sublingual, rectal, intranasal, vnutriobolochechnoe and with implant. A therapeutically effective amount of the inhibitors of P-gp is from about 0.1 to about 300 mg/kg/day, preferably from about 0.1 to about 150mg/kg daily. It should be borne in mind that although the patient can start taking one dose, you may need to change this dose over time, as changing the patient's condition. When orally administered inhibitors of P-gp can be entered in the usual pharmaceutical forms for oral administration, known to specialists in this field of technology. Such dosage forms include conventional solid and liquid dosage forms - tablets and capsules) and liquid dosage forms such as solutions, suspensions and elixirs. When using solid dosage forms, preferably, they represented a type of delayed release, in order to introduce the P-gp was required only once or twice a day. Oral dosage form is administered to the patient one to four times per day. Preferably, the inhibitors of P-gp was administered three or fewer times per day, preferably once or twice per day. Therefore, preferably, the inhibitors of P-gp was administered in solid dosage form, and also preferably, the solid dosage form was a form of delayed release, allowing the reception once or twice a day. Preferably, whenever the dosage form is not used, it was created so that inhibitors of P-gp was defending himself from what Isla environment of the stomach. Specialists in the art of well-known tablets intersolubility coating. In addition, specialists in the art is also well-known capsules, filled with small spheres coated to protect it from the acidic environment of the stomach. In addition, inhibitors of P-gp can be entered parenteral. When parenteral they can be administered IV, IM, depo-IM, SQ, or depo-SQ method. Inhibitors of P-gp you can enter the hyoid. When the hyoid receiving inhibitors of P-gp should be given one to four times per day in the same amount as for IM injection. Inhibitors of P-gp you can enter the route. To receive this way is suitable dosage forms have the form of a nasal spray or dry powder, which is known to specialists in this field of technology. Dosage of inhibitors of P-gp for intranasal same as for IM injection. Inhibitors of P-gp can be entered vnutriobolochechnoe. To receive in this way a suitable dosage form can be a parenteral dosage form, well-known specialists in this field of technology. Inhibitors of P-gp can be entered locally. To receive in this way a suitable dosage form can be a cream, ointment or sticker. Because of the necessary input number of inhibitors of P-gp is preferable NAC the side. However, the amount that can deliver sticker, limited. So you may need two or more labels. The number and size of the labels are not important, and it is important that delivered therapeutically effective amount of the inhibitors of P-gp, as is well known to specialists in this field of technology. Inhibitors of P-gp can be entered by using a suppository, as is well known to specialists in this field of technology. Inhibitors of P-gp can be entered with the help of implants, as is well known to specialists in this field of technology. There is nothing new in no relation to the method of administration, neither in terms of dosage forms for administration of inhibitors of P-gp. Using a specific inhibitor of P-gp and the desired dosage form specialist in the art will be able to learn how to obtain and enter an appropriate dosage form for an inhibitor of P-gp. For specialists in the art should be obvious that the exact dosage and frequency of injection will depend on the particular input connection of the invention, a specific condition, which are treated, the severity of the condition, which are treated, age, weight, General physical condition of the particular patient, and other medications that can take an individual that is well known to physicians prescribing treatment is, who are specialists in this field of technology. Inhibition of cleavage of APP Compounds of the invention inhibit cleavage of APP between Met595 and Asp596 numbered on the isoforms ARR, or its mutant, or in the corresponding website the other isoforms, such as AR or AR, or its mutant (sometimes referred to as the "site beta secretase"). Without going into any theory, under the inhibition of beta-secretase activity understand the inhibition of the production of beta-amyloid peptide (A-beta). Inhibitory activity demonstrated in the analysis of a series of tests on inhibition, in which cleavage of the substrate by the RDA in the presence of the enzyme beta-secretase analyze in the presence of inhibitory compounds in the environment, is usually sufficient to obtain cleavage site cleavage of beta-secretases. The decrease in the cleavage of APP at the site of cleavage of beta-secretases compared with untreated or inaktivirovannye control correlates with inhibitory activity. System tests that can be used to demonstrate the efficacy of compounds for inhibitors of the invention are known. Typical system analyses are described, for example, in U.S. patent No. 5942400 and 5744346, as well as in the examples below. The enzymatic activity of beta-secretase and the production of A-beta can analizirovat the in vivo or in vitro using natural substrates, the mutated and/or synthetic RDAs, natural, mutated, and/or synthetic enzyme and test compound. In the analysis it is possible to use primary or secondary cells expressing native, mutant, and/or synthetic RDAs and the enzyme, animal models expressing native RDAs and the enzyme, or you can use transgenic animal models expressing the substrate and the enzyme. The detection of the enzymatic activity can be performed by analysis of one or more cleavage products, for example, by immunoassay, fluorometric or chromogenic analysis, HPLC or other methods of detection. Connection-inhibitors are defined as compounds with the ability to reduce the amount of cleavage product of beta-secretases compared with the control, where the cleavage in the reaction system, mediated beta-secretases observed and measured in the absence of compounds inhibitors. Beta secretase Various forms of the enzyme beta-secretase known and available and suitable for analysis of enzyme activity and inhibition of enzyme activity. Such forms include native, recombinant and synthetic forms of the enzyme. Human beta-secretase known as an enzyme that breaks down beta-site of APP (VASYA), Asp2 and Melepsin 2, and characterized, n is the sample, in U.S. patent No. 5744346 and published patent applications PCT WO 98/22597, Wo 00/03819, WO 01/23533 and WO 00/17369, as well as in literary publications (Hussain et al., 1999, Mol. Cell. Neurosci., 14:419-427; Vassar et al., 1999, Science 286:735-741; Yan et al., 1999, Nature, 402:533-537; Sinha et al., 1999, Nature, 40:537-540; and Lin et al., 2000, PNAS USA, 97:1456-1460). Synthetic forms of the enzyme have also been described (WO 98/22597 and WO 00/17369). Beta secretase can be extracted and separated into a pure form of the fabric of the human brain and can be obtained in the cells, for example mammalian cells expressing recombinant enzyme. Preferred subjected to rearrangement compounds are effective for inhibiting the enzymatic activity of beta-secretase to about 50% at a concentration of less than about 50 microns, preferably in a concentration of 1 μm or less, and most preferably at a concentration of 10 nm or less. The substrate RDAs In the analyses that demonstrate inhibition mediated beta-secretases cleavage of APP, you can use any of the known forms of ADR, including "normal" isotype of 695 amino acids described by Kang et al., 1987, Nature, 325:733-6, of 770 amino acids described by Kitaguchi et al., 1981, Nature, 31:530-532, and options such as the Swedish mutation (CM-1NL) (APP-SW), the London mutation (V7176F) and others. See, for example, U.S. patent No. 5766846 and Hardy, 1992, Nature Genet., 1:233-234, for an overall view of the known variants of mutations. Other prigodin the mi substrates are modifying dibasic amino acids ARR-ACS, disclosed, for example, in WO 00/17369, fragments of APP and synthetic peptides containing the site of cleavage of beta-secretases, wild type (WT) or mutated form, for example, SW, described, for example, in U.S. patent No. 5942400 and WO 00/03819. The substrate ARR contains the site cleavage of APP by beta secretases (KM-DA or NL-DA), such as the full peptide of APP or variant, fragment of APP, recombinant or synthetic APP or fused peptide. Preferably fused peptide includes the site of cleavage of beta-secretases, fused with a peptide containing a group suitable for enzymatic analysis, for example, have properties to effect the separation and/or detection. Suitable group may be antigenic epitope for binding of the antibody, a label or other detected group, substrate for binding, etc. Antibodies Characteristic cleavage products of APP may be determined by immunoassay using various antibodies, as described, for example, in Pirtilla et al., 1999, Neuro. Lett., 249:21-4, and in U.S. patent No. 5612486. Antibodies suitable for detection of a-beta, are, for example, monoclonal antibodies E (Senetek, St. Louis, MO), which specifically recognize an epitope on amino acids 1-16 of peptide A-beta; antibodies 162 and 164 (New York State Institute for Basic Research, Staten Island, NY), which is specific for human A-beta 1-40 and 1-42, respectively; and antibodies that recognize the region of the junction be the a-amyloid peptide - the site between residues 16 and 17, described in U.S. patent No. 5593846. Antibodies induced against a synthetic peptide residues 591-596 RDAs, and antibodies SW192 induced against 590-596 Swedish mutation, also suitable immunoanalyzer RDAs and fission products, as described in U.S. patent No. 5604102 and 5721130. System analysis Analyses to determine the cleavage of APP at the site of cleavage of beta-secretases well known in the art. Examples of analyses are described, for example, in U.S. patent No. 5744346 and 5942400, and are described below in the examples. Cell-free tests Examples of analyses that can be used to demonstrate the inhibitory activity of the compounds of the invention are described, for example, in WO 00/17369, WO 00/03819 and in U.S. patent No. 5942400 and 5744346. Such analyses can be performed by incubation in the absence of cells or in the presence of cells, using cells expressing beta-secretase, and substrate RDAs, with the site of cleavage of beta-secretases. The substrate of APP that contains the site of cleavage of beta-secretases, for example, the full RDA or variant, fragment of APP, or the substrate recombinant or synthetic APP containing the amino acid sequence of KM-DA or NL-DA, incubated in the presence of the enzyme beta-secretase, its fragment or variant synthetic or recombinant polypeptide region is giving beta secretase activity and effective for cleavage site cleavage of beta-secretases RDAs, the incubation conditions suitable for splitting activity of the enzyme. Suitable substrates include optional derivatives, which can be a fused proteins or peptides containing peptide substrate, and modification suitable to facilitate purification or detection of the peptide or products of the cleavage of beta-secretases. Suitable modifications are inserting a known epitope for binding of antibodies; attaching a label or detectable group, joining binding substrate, etc. Suitable incubation conditions for cell-free in vitro assays are, for example, incubation of a mixture of approximately 200 nm - 10 μm substrate, approximately 10-200 PM enzyme, and approximately 0.1 nm - 10 μm compound inhibitor in aqueous solution at a pH of about 4-7, at approximately 37º during the period of time from about 10 minutes to 3 hours. Such conditions of incubation are only examples, and may require changes to specific components of the analysis and/or need of the measuring system. Optimization of incubation conditions for specific components of the analysis should take account of the used enzyme beta-secretase and its pH optimum, any additional enzyme and/or markers that can be used in the analysis, and similar factors. This optimization is usual the case and does not require additional experiments. In one suitable analyses using fused peptide containing maltose binding protein (MBP)fused to a C-terminal amino acids of APP-SW. MBP-part captured on the substrate for the analysis of immobilized antibodies against MBP. Incubation of immobilized fused protein in the presence of beta-secretase leads to cleavage of the substrate at the site of cleavage of beta-secretases. Analysis of digestive activity can be performed, for example, by immunoassay products of cleavage. In one such analysis discover a unique epitope at the carboxy-end of the cleaved fused protein, for example, using antibodies SW192. This analysis is described, for example, in U.S. patent No. 5942400. Cell analysis Many analyses based cells can be used to analyze beta-secretase activity and/or processing of APP with the release of A-beta. The contact substrate RDAs with the enzyme beta-secretases in the cell in the presence or in the absence of the compound inhibitor of the invention can be used to demonstrate the inhibitory activity of compounds against beta-secretase. Preferably the analysis in the presence of a suitable connection inhibitor gives the inhibition of the enzymatic activity of at least about 30%, most preferably at least about 50%, when compared with control, not p is delavska inhibition. In one embodiment using cells naturally expressing beta-secretase. On the other hand, cells modify for the expression of recombinant beta-secretase or synthetic version of the enzyme, as described above. The substrate RDAs can be added to the culture medium, and preferably to Express in cells. Cells naturally expressing the RDA, variant or mutant form of APP, or cells that have been transformed for the expression of isoforms of APP, mutant or variant ARR, recombinant or synthetic APP, fragment of APP or synthetic peptide of APP or fused protein containing the site cleavage of APP by beta secretases, can be used, provided that downregulation of APP is allowed to contact with the enzyme and can be analyzed enzymatic splitting activity. Line of human cells that naturally produce A-beta from the RDA, provide a suitable tool for the analysis of the inhibitory activity of the compounds of the invention. The production and release of A-beta and/or other fission products into the culture medium can be measured, for example, immunoassay methods, such as Western blotting or enzyme immunoassay (EIA), such as ELISA. Cells expressing the substrate RDAs and active beta-secretase, can be incubated in the presence of the connection is in inhibitor to demonstrate the inhibition of the enzymatic activity when compared with control. The activity of beta-secretase can be measured by analysis of one or more products of the cleavage of the substrate by the RDA. For example, it can be expected that inhibition of beta-secretase activity against substrate RDAs will reduce the release of specific cleavage products of APP, called beta-secretases, such as A-beta. Although both neural and aneuretinae cells produce and release A-beta, the levels of endogenous beta-secretase activity are low and often barely detectable EIA. Therefore, it is preferable to use types of cells, known as cell-enhancing beta-secretshow activity, enhancing the processing of APP to A-beta and/or enhancing production of A-beta. For example, transfection of cells form the Swedish mutant of APP (APP-SW), ARR-ACS or the RDA-SW-KK, provides cells with enhanced beta-secretase activity and producing amount of A-beta, which can be easily measured. In such analyses, for example, cells expressing the RDA and beta secretase, incubated in culture medium under conditions suitable for the beta secretase enzymatic activity in her cleavage site on the substrate by the RDA. When exposed to cell connection-inhibiting amount of A-beta, released on Wednesday, and/or the number of fragments CTF99 of APP in cell lysates compared to control. Prod the points of cleavage of APP can be analysed for example, using immune reactions with specific antibodies described above. The preferred cells for the analysis of beta-secretase activity are the primary neural cells human primary neural cells of transgenic animals, where the transgene is RDAs, and other cells, such as cells of the resistant cell line 293 expressing the RDA, such as the RDA-SW. Anility in vivo: animal models Various animal models can be used to analyze beta-secretase activity and/or processing of APP with the release of A-beta, described above. For example, to demonstrate the inhibitory activity of the compounds of the invention can be used transgenic animals expressing the substrate RDAs and the enzyme beta-secretase. Some transgenic animal models are described, for example, in U.S. patents№№ 5877399, 5612486, 5387742, 5720936, 5850003, 5877015 and 5811633, and Ganes et al., 1995, Nature, 373:523. Preferred animals, showing the properties that are associated with the pathophysiology of AD. Introduction compounds are inhibitors of the invention the transgenic mice described herein, is an alternative way to demonstrate inhibitory activity of compounds. Also preferably, the introduction of compounds in pharmaceutically effective carrier and method of administration, which delivers to the target tissue suitable treatment the number. Inhibition mediated beta-secretases cleavage of APP at the site of cleavage of beta-secretases and the release of A-beta can be analyzed on animals, by measuring the cleavage fragments in body fluids of animals, such as cerebral fluid, or tissues. The preferred analysis of brain tissue to deposition of a-beta or plaques. Upon contact of the substrate RDAs with the enzyme beta-secretases in the presence of the compound is an inhibitor of the invention and under conditions sufficient to create opportunities mediated by enzyme cleavage of APP and/or release of a-beta from the substrate, the compounds of the invention are effective to reduce mediated beta-secretases cleavage of APP at the site of cleavage of beta-secretases and/or effective to reduce the released amounts of A-beta. When this contact is the introduction of compounds inhibitors of the invention to an animal model, such as described above, the compounds are effective to reduce sediment And-beta in the brain tissue of the animal and to reduce the number and/or size of beta-amyloid plaques. When this introduction is carried out to a person, the compounds are effective for inhibiting or slowing the disease, characterized by increased amounts of A-beta, to slow down the progression of AD and/or to prevent the Oia began the development of AD in patients at risk of such disease. Unless otherwise stated, terms used in this description have the same values, which usually gives the person skilled in the art to which it pertains to this invention. All patents and publications cited in this specification, are included as references. Definitions Definitions and explanations below are for terms used throughout this document, including the description and the claims. It should be noted that as used in this description and the attached claims the signs of the singular number include the corresponding plural forms, if the content does not indicate clearly otherwise. So, for example, reference to a composition containing "a compound"includes a mixture of two or more compounds. It should also be noted that the term "or" is used generally in its sense including "and/or"unless the content is not clearly indicates otherwise. The symbol "-" in General represents a bond between two atoms in the chain. So, CH3-About- CH2-CH(R1)-CH3represents the connection of 2-substituted 1-methoxypropan. In addition, the symbol "-" represents the place of connection of the Deputy to the connection. So, for example, aryl((C1-C6)-alkyl)- shows alkylaryl the group, such as benzyl, attached to the connection in the alkyl part. When you specify several deputies, acceding to the structure, it should be borne in mind that the substituents may be the same or different. So, for example, Rm, optionally substituted by 1, 2 or 3 groups Rqindicates that Rmsubstituted by 1, 2 or 3 groups Rqwhere the group Rqmay be the same or different. Amyloid protein precursor of the RDA is defined as any peptide RDAs, including options for RDAs, mutation and isoforms, for example, described in U.S. patent No. 5766846. Amyloid beta-peptide A-beta is defined as any peptide, the resulting mediated beta-secretases cleavage of APP, including the peptides of 39, 40, 41, 42 and 43 amino acids, and capacity from the site of cleavage of beta-secretases to amino acids 39, 40, 41, 42 or 43. Beta secretase (VASE, Asp2, Melepsin 2) represents aspirinplease, which mediates cleavage of APP by aminobenzo A-beta. Human beta-secretase described, for example, in WO 00/17369. The term "pharmaceutically acceptable" refers to those properties and/or substances which are acceptable to the patient from a pharmacological/Toxicological point of view and for a pharmacist / chemist from a physical/chemical point of view when considering the composition, structure, ostoich the stability and acceptance by the patient. "Therapeutically effective amount" is defined as an amount effective to reduce or ameliorate at least one symptom of the disease, which is treated, or to reduce or delay the appearance of one or more clinical markers or symptoms of the disease. The terms "alkyl" and "(1-C6)-alkyl" in the present invention denotes an alkyl group with a linear or branched chain with 1-6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, pentyl, 2-pentyl, isopentyl, neopentyl, hexyl, 2-hexyl, 3-hexyl, and 3-methylpentyl. It should be borne in mind that in cases where the alkyl chain substituent (e.g. alkyl, alkoxy or Alchemilla group) shorter or longer chain of 6 atoms of carbon, it will also be specified in the second "S", as, for example, "(1-C10indicates a maximum of 10 carbon atoms. The terms "alkoxy" and "(1-C6)-alkoxy" in the present invention denotes an alkyl group with a linear or branched chain with 1-6 carbon atoms, attached through at least one divalent oxygen atom, such as, for example, methoxy, ethoxy, propoxy, isopropoxy, n-butoxy, sec-butoxy, tert-butoxy, pentox, isopentane, neopentane, hexose and 3 methylpentane. The term "ha is oven" in the present invention are denoted by fluorine, bromine, chlorine and iodine. The terms "alkenyl" and "(2-C6)-alkenyl" refers to linear or branched hydrocarbon radical with 2-6 carbon atoms and one to three double bonds and includes, for example, ethynyl, propenyl, 1-but-3-enyl, 1-Penta-3-enyl, 1-Gex-5-enyl and similar groups. The terms "quinil" and "(2-C6)-quinil" refers to linear or branched hydrocarbon radical with 2-6 carbon atoms and one or two triple bonds and includes ethinyl, PROPYNYL, butynyl, pentyn-2-yl and the like groups. Used in this description, the term "cycloalkyl" refers to saturated carbocyclic radicals from three to twelve carbon atoms. Cycloalkyl may be single-core or multi-core condensed system. Examples of such radicals are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl. Cycloalkyl group herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such cycloalkyl groups can be optionally substituted (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6)-alkyne is scrap, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl or di(C1-C6)alkylamino(C1-C6)-alkyl. The term "aryl" refers to aromatic carbocyclic group of from one cycle (e.g., phenyl), multiple cycles (e.g., biphenyl) or multiple condensed nuclei, of which at least one is aromatic (e.g., 1,2,3,4-tetrahydronaphthyl, naphthyl), which optionally is mono-, di - or tizamidine. Preferred aryl groups of the present invention are phenyl, 1-naphthyl, 2-naphthyl, indanyl, indenyl, dihydronaphtho, tetralinyl or 6,7,8,9-tetrahydro-5H-benzo[a]cyclopentyl. Aryl groups herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such aryl groups can be optionally substituted, for example, (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1 -C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl, di(C1-C6)alkylamino(C1-C6)-alkyl, -COOH, -C(=O)O((C1-C6)-alkyl), -C(=O)NH2, -C(=O)N(mono - or di((C1-C6)-alkyl), -S-((C1-C6)-alkyl), -SO2-((C1-C6)-alkyl), -O-C(=O)((C1-C6)-alkyl), -NH-C(=O)-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-C(=O)-((C1-C6)-alkyl), -NH-SO2-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-SO2-((C1-C6)-alkyl), -NH-C(=O)NH2, -NH-C(=O)N(mono - or di-(C1-C6)-alkyl), -NH((C1-C6)-alkyl)-C(=O)-NH2or-NH((C1-C6)-alkyl)-C(=O)-N-(mono - or di-(C1-C6)-alkyl). The term "heteroaryl" refers to a system of one or more aromatic cyclic 5-, 6 - or 7-membered cycles, including the condensed-cyclic systems of 9-11 atoms containing at least one and up to four heteroatoms selected from nitrogen atoms, oxygen or sulfur. Preferred heteroaryl groups of the present invention are pyridinyl, pyrimidinyl, chinoline, benzothiazyl, indolyl, indolinyl, pyridazinyl, pyrazinyl, isoindolyl, ethanolic, hintline, honokalani, phthalazine, imidazolyl, isoxazolyl, pyrazolyl, oxazol is l, thiazolyl, indolizinyl, indazoles, benzothiazoles, benzimidazoles, benzofuranyl, furanyl, thienyl, pyrrolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, oxazolopyridine, imidazopyridines, isothiazolin, naphthyridine, cinnoline, carbazolyl, beta-carbolines, isopropanol, bromanil, tetrahydroisoquinoline, isoindolines, isobenzofuranyl, isobenzofurandione, isobenzofuranyl, benzoxazolyl, pyridopyrimidines, bettererererer, betterregulation, purinol, benzodioxolyl, triazinyl, phenoxazines, phenothiazines, pteridinyl, benzothiazolyl, imidazopyridines, imidazothiazoles, dihydroergotoxine, benzisoxazole, benzoxazine, dihydromethysticin, benzopyranyl, benzothiophene, coumarinyl, isocoumarins, chromones, chromanones, pyridinyl-N-oxide, tetrahydroquinoline, dihydroquinoline, dihydroquinoline, dihydroisoquinoline, dihydrocoumarin, dihydroisocoumarin, isoindolines, benzodioxane, benzoxazolinone, pyrrolyl-N-oxide, pyrimidinyl-N-oxide, pyridazinyl-N-oxide, pyrazinyl-N-oxide, chinoline-N-oxide, indolyl-N-oxide, indolyl-N-oxide, ethanolic-N-oxide, hintline-N-oxide, honokalani-N-oxide, phthalazine-N-oxide, imidazolyl-N-oxide, isoxazolyl-N-oxide, oxazolyl-N-oxide, thiazolyl-N-oxide, indolizinyl-N-oxide, indazolin-N-oxide, benzothiazolyl-N-oxide, gasoline is idazole-N-oxide, pyrrolyl-N-oxide, oxadiazolyl-N-oxide, thiadiazolyl-N-oxide, triazolyl-N-oxide, tetrazolyl-N-oxide, benzothiophene-S-oxide, benzothiophene-S,S-dioxide. Heteroaryl groups herein are unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such heteroaryl groups can be optionally substituted (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl or di(C1-C6)alkylamino(C1-C6)-alkyl, -COOH, -C(=O)O((C1-C6)-alkyl), -C(=O)NH2, -C(=O)N(mono - or di((C1-C6)-alkyl), -S-((C1-C6)-alkyl), -SO2-((C1-C6)-alkyl), -O-C(=O)((C1-C6)-alkyl), -NH-C(=O)-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-C(=O)-((C1-C6)-alkyl), -NH-SO2-((C1-C6)-alkyl), -N((C1-C6)-alkyl)-SO2-((C1-C6)-alkyl), -NH-C(=O)NH2, -NH-C(=O)N(mono - or di-(C1-C6 )-alkyl), -NH((C1-C6)-alkyl)-C(=O)-NH2or-NH((C1-C6)-alkyl)-C(=O)-N-(mono - or di-(C1-C6)-alkyl). The terms "heterocycle", "heteroseksualci" or "heterocyclyl" refers to a system of one or more of 3, 4, 5, 6 - or 7-membered cycles, including the condensed-cyclic systems of 9-11 atoms containing at least one and up to four heteroatoms selected from nitrogen atoms, oxygen or sulfur. Preferred heterocycles of the present invention are morpholinyl, thiomorpholine, thiomorpholine-S-oxide, thiomorpholine-S,S-dioxide, piperazinil, homopiperazine, pyrrolidinyl, pyrrolyl, tetrahydropyranyl, piperidinyl, tetrahydrofuranyl, tetrahydrothieno, homopiperazine, homomorpholine, homotaurine, homotaurine-S,S-dioxide, oxazolidinones, dihydropyrazolo, dihydropyrrole, dihydropyrazine, dihydropyridines, dihydropyrimidines, dihydrofuran, dihydropyran, azepane, diazepan, tetrahydrothieno-S-oxide, tetrahydrothieno-S,S-dioxide and homotaurine-S-oxide. Heterocyclyl group in this description may be unsubstituted or, as specified, substituted in one or more substitutable positions of different groups. For example, such heterocyclyl groups can be optionally substituted (C1-C6)alkyl, (C1-C6)-alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino, (C2-C6-alkenyl, (C2-C6-quinil, (C1-C6-halogenation, (C1-C6)-halogenoalkane, amino(C1-C6)alkyl, mono(C1-C6)alkylamino(C1-C6)-alkyl, di(C1-C6)alkylamino(C1-C6)-alkyl or =O. All patents and publications cited in this specification, are included as references. Patterns are named using the Name Pro IUPAC Naming Software, version 5.09, available from Advanced Chemical Development, Inc., 90 Adelaide Srteet West, Toronto, Ontario, M5H 3V9, Canada. The present invention can be better understood by referring to the following examples. These examples are intended to be typical examples of specific embodiments of the invention and are not intended to limit the scope of the invention. Chemical examples The following detailed examples describe how you can get a variety of compounds and/or to perform various methods of the invention, and such examples should be considered only as a clarification in any way as limitations of the preceding disclosure. Specialists in the art will immediately recognize the corresponding change is to the procedures in respect of reagents, and conditions of interactions and methods. Preparative example 1 tert-Butyl(1S)-3-bromo-1-(3,5-diferensial)-2-oxopropionate (III) To (2S)-[(tert-butoxycarbonyl)amino]-3-(3,5-differenl)propanoic acid (II, 15 g, 50 mmol) in THF (100 ml) is added N-methylmorpholine (of 5.83 ml, 53 mmol, of 1.05 equiv.) and the reaction mixture was cooled to-78ºC. Quickly add isobutylparaben (6,87 ml, 53 mmol, of 1.05 EQ.). Then the cooling bath removed and the mixture is stirred for 1 hour. The reaction mixture was checked by TLC in order to ensure the full realization of the reaction, and the mixture is then filtered, washed with dry THF (50 ml) and stored cold in the flask to the filtrate at -20 ºc. At bath with a mixture of ice and salt is placed 500-ml measuring cylinder containing ether (200 ml) and aqueous solution of potassium hydroxide (40%, 60 ml). Gradually under stirring was added 1-methyl-3-nitro-1-nitrosoguanidine (5.6 g, 106 mmol, 2.1 EQ.) and keep the temperature below zero degrees. The mixture becomes yellow, and bubbling continued for 10 minutes. Stirring is stopped and, without mixing the two layers, the upper diazolidinyl layer is transferred by pipette with the whole tip into the mixture with the mixed anhydride under stirring at-20ºC. The reaction is controlled by TLC (ethyl acetate/hexane, 50/50; Rf=0,69). Then after 1 hour the mixture barbotine is nitrogen. The solvent is removed under reduced pressure (when heated) and the mixture is treated with ether and water. The phases are separated, the organic phase is washed with bicarbonate solution and brine, dried over anhydrous sodium sulfate, filter and remove the solvent under reduced pressure (when heated). The residue is dissolved in ether (100 ml), at -20 ░ C add Hydrobromic acid (48%, 15 ml, 135 mmol, 2.7 equiv.) the cooling bath is removed and the mixture is stirred for another half an hour. The reaction mixture was checked by TLC (ethyl acetate/hexane, 50/50; Rf=0,88). The mixture is treated with ether and water, washed with bicarbonate solution and brine, dried over anhydrous sodium sulfate, filter and remove the solvent. The residue is recrystallized from ethanol and get called in the header connection. TLC (ethyl acetate/hexane, 50/50; Rf=0,88); MS (MH+)=379,3. Preparative example 2 tert-Butyl(1S,2S)-3-bromo-1-(3,5-diferensial)-2-hydroxypropionate (IV) To tert-butyl(1S)-3-bromo-1-(3,5-diferensial)-2-oxopropionate (III preparative example 1, 12 g of 31.75 mmol), dissolved in absolute alcohol (500 ml)at-78ºC add sodium borohydride (1,32 g, is 34.9 mmol, 1.1 EQ.). The reaction mixture is stirred for 30 minutes and control TLC (ethyl acetate/hexane, 20/80; Rf=0,2). The mixture was quenched with water (10 ml) and remove the solvent to the ear under reduced pressure with heating (not exceeding 30ºC). The solid is treated with dichloromethane and water and the organic portion washed with brine and dried over anhydrous sodium sulfate. The solvent is removed under reduced pressure and get called in the header connection. TLC (ethyl acetate/hexane, 20/80; Rf=0,2); MS (MH+)=381,2. Preparative example 3 tert-Butyl(1S)-2-(3,5-diferensial)-1-[(2S)-oxiranyl]ethylcarbamate (V) tert-Butyl(1S,2S)-3-bromo-1-(3,5-diferensial)-2-hydroxypropionate (IV preparative example 2) is dissolved in absolute alcohol (150 ml) and ethyl acetate (100 ml), at -20 ░ C add potassium hydroxide (2.3 g, is 34.9 mmol, 1.1 EQ.) in absolute alcohol (85%, 5 ml). Then the cooling bath removed and the mixture is stirred for 30 minutes. Reaction control TLC (ethyl acetate/hexane, 20/80). When the reaction is complete, the reaction mixture is diluted with dichloromethane and extragere, the extract washed with water and brine, dried over anhydrous sodium sulfate and remove the solvent under reduced pressure. The crude substance is purified flash chromatography on silica gel and get called in the header connection. TLC (ethyl acetate/hexane, 20/80; Rf=0,2), Rf=0,3; MS (MH+)=300,4. Preparative example 4 tert-Butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propellernet
tert-Butyl(1S)-2-(5-diferensial)-1-[(2S)-oxiranyl]ethylcarbamate (preparative example 3, 8.5 g, 28.4 mmol) is mixed with isopropanol (145 ml). In a reaction flask is charged with 3-(trifluoromethyl)benzylamine. The reaction mixture is refluxed for 3 hours, analysis by HPLC indicates complete disappearance of the epoxide. The reaction mixture was concentrated under reduced pressure and the residue treated with ethyl acetate and hydrochloric acid. The organic phase is separated and washed with hydrochloric acid, bicarbonate solution and brine and then dried over sodium sulfate. Concentration under reduced pressure and recrystallization from hexane to give the named header connection. MS (MH+) 475. Preparative example 5 tert-Butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-{(tert-Butylochka)carbonyl-3-{(trifluoromethyl)benzyl}amino}propellernet
To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propylgallate (preparative example 4, 6.2 g, of 13.1 mmol) in THF (70 ml) at 0ºC add di-tert-butylpyrocatechol (6.3 g, of 28.9 mmol). The reaction mixture is stirred at 20 to 25 ° C for 18 hours. The reaction mixture was diluted with diethyl ether and washed with a solution of bicarbonate, 0.5 m citric acid and brine, then dried over sodium sulfate and concentrate and get called in the header connection. MS (MNa+) 597. Ven is an operational example 6 3-Iodine-5-(methoxycarbonyl)benzoic acid
To commercially available 3-amino-5-(methoxycarbonyl)benzoic acid (5,19 g, 26,59 mmol) in 2n hydrochloric acid (156 ml) under ice cooling and stirring, a solution of sodium nitrite (1.84 g, 26,67 mmol) in water (10,8 ml). Then the resulting mixture under ice cooling and stirring, added dropwise to a solution of potassium iodide (8,84 g, 53,25 mmol) in water (26,2 ml). After stirring for 30 minutes the reaction mixture was diluted with water and extracted with ethyl acetate. The organic layer was washed with 5% aqueous sodium thiosulfate solution and a saturated solution of sodium chloride, dried (sodium sulfate) and concentrated under reduced pressure. Purification column flash chromatography (silica, hexane/ethyl acetate/acetic acid 50:50:2) gives named the title compound (4,48 g, yield 55%) as not quite white solid. ESI-MS (m/z 305 [M+H]+. Preparative example 7 3-[(Dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid
To a solution of oxazole (4.0 g, 58 mmol) in tetrahydrofuran (100 ml) at-70ºC add n-utility (1.6 m solution in hexane, 40 ml, 64 mmol). After 30 minutes add zinc chloride (1M solution in diethyl ether, 166 ml, 166 mmol)and the reaction mixture is heated to 0ºC in those which begins 1 hour. To this mixture is added 3-iodine-5-(methoxycarbonyl)benzoic acid (preparative example 6, with 21.4 g, 55 mmol) and tetrakis(triphenylphosphine)palladium(0) (2.7 g, 2.34 mmol). The reaction mixture is refluxed for 1 hour. The reaction mixture was diluted with ethyl acetate (300 ml) and washed with water and saturated sodium chloride solution. The organic layer is dried (sodium sulfate) and concentrated under reduced pressure. Purification on a layer of silica gel (10-33% ethyl acetate/hexane) gives oxazol (17,7 g, 97%) as a pale yellow solid.1H NMR (300 MHz, CDC13) δ 8,73 (t, J=2 Hz, 1H), 8,24 (t, J=2 Hz, 1H), 8,11 (t, J=2 Hz, 1H), to 7.77 (d, J=1 Hz, 1H), 7,28 (d, J=1 Hz, 1H), of 3.97 (s, 3H), 3,49 (m, 2H), 3,19 (m, 2H), 1,71 (m, 2H), 1.57 in (m, 2H), 1,01 (m, 3H), 0.76 to (m, 3H). To a solution of ester from step 1 (17,7 g, 53.6 mmol) in tetrahydrofuran (50 ml), methanol (25 ml) and water (25 ml) add monohydrate of lithium hydroxide (6,92 g, 165 mmol). The reaction mixture was stirred at room temperature for 2 hours and then concentrated under reduced pressure. The residue is treated with water (100 ml) and diethyl ether (100 ml). The aqueous layer was acidified to pH 4-5 with hydrochloric acid and extracted with ethyl acetate (3×200 ml). The combined organic layers washed with a saturated solution of sodium chloride, dried (sodium sulfate) and concentrated under reduced pressure to half its original volume. Received fallen in about the of ADOC substance is collected by filtration and washed with hexane and get named in the title compound (15.5 g, 91%) as not quite white solid. MP 131-133º;1H NMR (300 MHz, CD3OD) δ 8,72 (s, 1H), they were 8.22 (s, 1H), 8,10 (s, 1H), of 8.06 (d, J=1 Hz, 1H), was 7.36 (d, J=1 Hz, 1H), 3,52 (m, 2H), 3,25 (m, 2H), 1,76 (m, 2H), 1,62 (m, 2H), 1,02 (m, 3H), 0.76 to (m, 3H); APCI MS m/z 317 [M+H]+. Preparative example 8 The dihydrochloride of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate
To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-{(tert-Butylochka)carbonyl-3-{(trifluoromethyl)benzyl}amino}propylgallate (preparative example 5, 594 mg, 1.0 mmol) in DMF (2 ml) is added 3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid (preparative example 7, 316 mg, 1.0 mmol), hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (210 mg, 1.1 mmol) and 4-(dimethylamino)pyridine (146 mg, 1.2 mmol). After ~36 hours, the reaction mixture was diluted with ethyl acetate and washed with bicarbonate solution (2×) and brine (4×), then dried over sodium sulfate, filtered and concentrated under reduced pressure. The concentrate is purified flash chromatography on silica gel using the solvent ethyl acetate/hexane gradient (from 20/80 to 50/50) and receive (1R,2S)-2-[(tert-butoxycarbonyl)amino]-1-({(tert-butoxycarbonyl)[3-(trifluoromethyl)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-(1-oxazol-2-yl)benzoate, MC (MNa+) 895. (1R,2S)-2-[(tert-Butoxycarbonyl)amino]-1-({(tert-butoxycarbonyl)[3-(trifluoromethyl)benzyl]amino}methyl)-3-(3,5-differenl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (482 mg, 0.55 mmol) dissolved in a mixture of hydrogen chloride/dioxane (4n, 3 ml) and stirred for 1 hour at 20-25ºC. Then the solvent is removed under reduced pressure and get called in the header connection. MS (MN+) 673. Preparative example 9 Hydrochloride N~1~-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N~3~,N~3~-dipropyl-N~1~-[3-(trifluoromethyl)benzyl]isophthalamide
To a solution of tert-butyl(1S,2R)-1-(3,5-diferensial)-2-hydroxy-3-[(3-(trifluoromethyl)benzyl)amino]propylgallate (preparative example 4, 393 mg, 0.83 mmol) in DMF (2 ml) is added 3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoic acid (preparative example 7, 262 mg, 0.83 mmol), hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (175 mg, of 0.91 mmol) and 4-(dimethylamino)pyridine (122 mg, 1.0 mmol). After ~18 hours the reaction mixture was diluted with ethyl acetate and washed with bicarbonate solution (2×) and brine (4×), then dried over sodium sulfate, filtered and concentrated under reduced pressure. The concentrate is purified flash chromatography on silica gel using a solvent ethylacetate/hexane gradient (from 50/5 to 70/30) and get tert-butyl(1S,2R)-1-(3,5-diferensial)-3-{[3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoyl][3-(trifluoromethyl)benzyl]amino}-2-hydroxypropionate. MC (MH+) 773. tert-Butyl(1S,2R)-1-(3,5-diferensial)-3-{[3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoyl][3-(trifluoromethyl)benzyl]amino}-2-hydroxypropionate (226 mg, 0.29 mmol) dissolved in a mixture of hydrogen chloride/dioxane (4n, 2 ml) and stirred for 20 minutes at 20-25º. Then the solvent is removed under reduced pressure and the crude substance is purified HPLC with reversed phase using a gradient of solvent a acetonitrile/water with 0.5% triperoxonane acid. The obtained Sol triperoxonane acid is converted into the hydrochloride by treatment with HCl in methanol (1,25M, 5 ml). Concentration under reduced pressure gives the named header connection. MS (MN+) 673. The following compounds get essentially according to the procedures described in the diagrams, charts, examples and formulation examples given in this description. 1033N-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N',N'-diethyl-N-(3-active compounds)-5-methylisophthalic1-(3-{[[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl](3-active compounds)amino]carbonyl}-5-methylbenzoyl)-L-prolinamide(1R,2S)-2-Amino-1-[(benzylamino)methyl]-3-(2-thienyl)propyl-3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoateHydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[(3-active compounds)amino]methyl}propyl-3-(4-methyl-1,3-oxazol-2-yl)benzoateN-[(2R,3S)-3-Amino-4-(3,5-differenl)-2-hydroxybutyl]-N-(3-active compounds)-N'-(2-methoxy-5-were)succinamictr>
Examples of rearrangement The following examples illustrate the migration of the acyl group, which occurs in the compounds of the invention. These examples are provided only for purposes of explanation and not intended to limit the scope of the invention. The General procedure The compound of formula (I) or (X) (5 mg) dissolved in DMSO-d6(500 ál) and add or buffer solution, pH 4 (500 μl, bufonidae substance hydroptila potassium), or buffer solution, pH 7 (500 μl, bufferer the abuser substance sodium phosphate and potassium). The sample was then heated to 40 ºC. Check O-acyl or N-acyl migration to the N-end, watching the change in chemical shift for the aromatic fluorine using19F-NMR. (Shifts of fluorine atoms associated with the desired migration, confirmed by comparison with authentic analogue.) The sample analyzing method19F-NMR approximately at time 0, 1,5, 3, 24, 48 and 144 hours. The number of On-allstargame prodrugs, N-allstargame prodrugs and the desired product migration in each moment of time estimated by integration of the corresponding NMR signals. Example 1 A specific example of the NMR
Hydrochloride N~1~-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N-~3~,N~3~-dipropyl-N~1~-[3-(trifluoromethyl)benzyl]isophthalamide (preparative example 7, 5 mg) is dissolved in DMSO-d6(500 ál) and add buffer solution, pH 4 (500 μl, bufonidae substance hydroptila potassium). The sample was then heated to 40 ºC. Check N-acyl migration of N-acyl N-end, watching the change in chemical shift for the aromatic fluorine using19F-NMR. (Shifts of fluorine atoms to the desired product migration in the presence of buffer is confirmed by comparison with authentic product migration, N1-((1S,2R)-1-(3,5-differenl)-2-hydroxy-3-{[3-(trifluoromethyl)is ensil]amino}propyl)-5-(1,3-oxazol-2-yl)-N 3N3-dipropylacetamide.) These NMR collect at time 0, 1, 3, 25, 48, 96 and 144 hours. The amount of N-allstargame prodrugs and the desired product migration present in each moment of time, estimated by integration of the corresponding NMR signals. The lack of migration to On-allstargame prodrugs see using this method and podverzhdayut by comparison with authentic connection. The following examples illustrate the migration in a solution of acyl groups of the compounds of formulas (I) and (X), the observed method19F-NMR spectroscopy. The results are collected, as described above in example 1. Example 2 Rearrangement of (1R,2S)-2-amino-3-(3,5-differenl)-1-({[1-(3-ethynylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (22)
Table 1-2 shows the relative concentrations of prodrugs 22 and its rearrangement product as a function of time and the change of the pH value.
Example 3 Regrouping dihydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-({[1-(3-ethylphenyl)cyclopropyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (17)
Table 3-4 shows the relative concentrations of prodrugs 17 and its rearrangement product as a function of time and the change of the pH value.
Example 4 Regrouping hydrochloride N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-N(u)1(d)-(3-active compounds)-5-(1,3-oxazol-2-yl)-N3N3-dipropylacetamide (19)
Table 5-6 shows the relative concentrations of prodrugs 19 and its rearrangement product as a function of time and the change of the pH value.
Example 5 Regrouping hydrochloride N1-[(2R,3S)-3-amino-4-(3,5-differenl)-2-hydroxybutyl]-5-(1,3-oxazol-2-yl)-N3N3-dipropyl-N1-[3-(trifluoromethyl)benzyl]isophthalamide (20)
Table 7-8 shows the relative concentrations of prodrugs 20 and prod the KTA its rearrangement as a function of time and the change of the pH value.
Example 6 Regrouping dihydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-{[1-(3-active compounds)amino]methyl}propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-is)benzoate (16)
Table 9-10 shows the relative concentrations of prodrugs 16 and its rearrangement product as a function of time and the change of the pH value.
Example 7 Regrouping dihydrochloride (1R,2S)-2-amino-3-(3,5-differenl)-1-({[3-(trifluoromethyl)benzyl]amino}methyl)propyl-3-[(dipropylamino)carbonyl]-5-(1,3-oxazol-2-yl)benzoate (18)
Table 11-12 shows the relative concentrations of prodrugs 18 and its rearrangement product as a function of time and the change of the pH value. 43
Biological examples An example of a Analysis of enzyme inhibition Undergone a rearrangement of compounds of the invention examined for inhibitory activity using the assay with MBP-C125. In this analysis, determine the relative inhibition by compounds cleavage of beta-secretases on the model substrate RDAs MBP-C125W when compared to untreated control. Detailed description of the parameters of the analysis can be found, for example, in U.S. patent No. 5942400. Briefly, the substrate is a fused peptide formed maltesewatertaxis protein (MBP) and carboxykinase 125 amino acids of the Swedish mutation of APP-SW. The enzyme beta-secretase obtained from brain tissue of a person, as described in Sinha et al., 1999, Nature, 40:537-540, or get recombinante as reprezentirovannoe enzyme (amino acids 1-501), and can be obtained, for example, from 293 cells expressing recombinant cDNA, as described in WO 00/47618. Enzyme inhibition analyze, for example, by immunoassay products of cleavage by the enzyme. As an example, in ELISA using immobilized antibodies against MBP, which osajda the t on pre-sensitised and blocked 96-well tablets strong binding, followed by incubation with the diluted supernatant for the enzymatic reaction, incubation with specific reporter antibody, for example, biotinylating reporter antibodies against SW192, and additional incubation with conjugate streptavidin/alkaline phosphatase. In the analysis of the cleavage of intact fused protein MBP-C125SW leads to a shortened aminoanisole fragment, exposing a new positive for antibodies SW192 epitope on carboxilic. The detection carried out by the signal of the fluorescent substance on the splitting of the phosphatase. ELISA detects only after splitting Leu 596 site mutations 751 substrate ARR-SW. Specific analytical procedure Solutions of compounds diluted by serial dilutions of 1:1 for the concentration curve by six points (two wells per concentration) in the same row 96-well plate on the test connection. Each of the test compounds dissolved in DMSO to obtain the original 10 mm solution. The original solution was serially diluted DMSO to the final concentration of the compound 200 μm at the highest point 6-point curve cultivation. Ten (10) microliters each dilution added to each of the two holes in the row With the corresponding wells with a V-shaped bottom, in which pre-add 190 ál of 52 mm NaOAc, 7,9% DMSO, pH 4.5. Tablet with diluted NaOAc connection centrifuged for sedimentation and 20 ál/l the GCC is transferred into the respective tablet with flat-bottomed holes, in which add 30 ál chilled on ice, the mixture of the enzyme-substrate (2,5 µl of substrate MBP-C125SW, of 0.03 μl of enzyme and 24.5 μl chilled on ice 0,09% TH 30 μl). The final reaction mixture c 200 microns connection at the highest point of the curve contains 5% DMSO, 20 mm NaOAc, 0,06% D at pH 4.5. Heating the tablet to 37º starts enzymatic reaction. After 90 minutes at 37º add 200 ál/well of cold diluent to stop the reaction and 20 μl/well is transferred into the corresponding sensitized with antibodies against MBP tablet for ELISA for immobilization containing 80 μl/well of diluent. The reaction mixture is incubated overnight at 4ºC and ELISA spend the next day after 2-hour incubation with antibodies against 192SW, and then conjugate streptavidin-AP and a fluorescent substance. The signal read on fluorimetry to read the tablets. The relative inhibitory effect of the compounds determined by calculating the concentration of a compound that shows a fifty percent weakening of the detected signal (IC50compared with the signal products of the enzymatic reaction in the control wells. In this analysis, the preferred compounds of the invention show an IC50less than 50 microns. The example In Cell-free analysis of inhibition using subs the rata synthetic RDAs For the analysis of beta-secretase activity in the presence or in the absence of compounds inhibitors according to the invention using the synthetic substrate RDAs, which can split a beta secretases contains Biotin at the N-end and has the ability to fluoresce due to joining Oregon green to Cys-residue. Suitable substrates are Biotin-SEVNL-DAEFRC[Oregon green]KK [SEQ ID NO: 1]; Biotin-SEVKM-DAEFRC[Oregon green]KK [SEQ ID NO: 2]; Biotin-GLNIKTEEISEISY-EVEFRC[Oregon green]KK [SEQ ID NO: 3]; Biotin-ADRGLTTRPGSGLTNIKTEEISEVNL-DAEFRC[Oregon green]KK [SEQ ID NO: 4]; Biotin-FVNQHLCoxGSHLVEALY-LVCoxGERGFFYTPKAC[Oregon green]KK [SEQ ID NO: 5]. The enzyme (0.1 nm) and test compound (0.001 to 100 μm) incubated in pre-blocked with a low affinity tablets with holes with tinted bottom (384-well) when 37º within 30 minutes. The reaction is initiated by adding 150 mm substrate to a final volume of 30 μl per well. End conditions analysis: 0,001-100 ám connections-inhibitor; 0,1M sodium acetate (pH 4.5); 150 nm of the substrate; 0.1 nm soluble beta-secretase; 0.001% of tween-20 and 2% DMSO. Mixture for analysis incubated for 3 hours at 37º and the reaction being removed by adding a saturating concentration of streptavidin purified immunosorption method. After incubation with streptavidin at room temperature for 15 minutes to measure the polarization of fluorescence,for example, using LJL Acqurest (suc. 485 nm/Emiss. 530 nm). The activity of the enzyme beta-secretase detects the change of the polarization of fluorescence that occur when the substrate is cleaved by the enzyme. Incubation in the presence or in the absence of a connection-inhibitor shows specific inhibition of cleavage by the enzyme beta-secretases its synthetic substrate ARR. In this analysis, the preferred compounds of the invention show an IC50less than 50 microns. Example With Inhibition of beta-secretase: analysis R-R SW Synthetic substrates containing site cleavage of APP by beta secretases, used for the analysis of beta-secretase activity using the methods described, for example, in published PCT application WO 00/47618. The substrate R-R SW represents a peptide sequence (Biotin)CGGADRGLTTRPGSGLTNIKTEEISEVNLDAEF [SEQ ID: 6]. Standard R-P1 has the sequence (Biotin)CGGADRGLTTRPGSGLTNIKTEEISEVNL [SEQ ID: 7]. Briefly, in this analysis of synthetic substrates with attached Biotin incubated at a concentration of from about 0 to about 200 microns. When the test compounds are inhibitors preferred substrate concentration of about 1.0 μm. Test compounds, dissolved in DMSO, is added to the reaction mixture to the final concentration of DMSO 5%. A control sample is also contain DMSO at a final concentration of 5%. The concentration of the enzyme beta-secretase change in the reaction mixture and after dilution receive product concentration in the linear range of the assays, ELISA from about 125 to about 2000 PM. The reaction mixture also contains 20 mm sodium acetate, pH 4.5, and 0.06% Triton X100, and incubated at 37º for about 1-3 hours. Then the samples are diluted with buffer for analysis (for example, 145,4 nm sodium chloride, 9,51 mm phosphate, 7,7 mm of sodium azide, 0.05% of Triton H, 6 g/l bovine serum albumin, pH 7.4) in order to quench the reaction, and then diluted further for immunoassay products of cleavage. Cleavage products can be analyzed using ELISA method. Diluted samples and standards are incubated in analytical tablets, sensitized by the immobilized antibody, e.g SW192, for about 24 hours at 4ºC. After washing in TTBS buffer (150 mm sodium chloride, 25 mm Tris, 0.05% tween-20, pH 7.5) samples incubated with conjugate streptavidin-AP according to the manufacturer's instructions. After one-hour incubation at room temperature the samples are washed in TTBS and incubated with substrate solution And fluorescent substances (31,2 g/l 2-amino-2-methyl-1-propanol, 30 mg/l, pH of 9.5). Interaction with conjugate streptavidin-alkaline phosphatase creates opportunities for detection using fluorescence is. Compounds that are effective inhibitors of beta-secretase activity show reduced cleavage of the substrate compared to control. Example D Analyses using substrates of synthetic oligopeptides Synthetic oligopeptides, including the famous site of cleavage of beta-secretases and, optionally, detected labels, such as fluorescent or chromogenic groups. Examples of such peptides, as well as their receipt and detection methods are described in U.S. patent No. 5942400 included in this description by reference. Cleavage products can be detected using high performance liquid chromatography or methods of fluorescence detection or generation of Chromogens that are appropriate for the detected peptide according to methods well known in the art. For example, one such peptide has the sequence SEVNL-DAEF [SEQ ID NO: 8], and the cleavage site is between residues 5 and 6. Another preferred substrate has the sequence ADRGLTTRPGSGLTNIKTEEISEVNL-DAEF [SEQ ID NO: 9], and the cleavage site is between residues 26 and 27. Such synthetic substrates incubated in the presence of beta-secretase under conditions sufficient to produce mediated beta-secretases cleavage of the substrate. The comparison result is tov cleavage in the presence of compounds of the inhibitor with the results for the control gives a measure of the inhibitory activity of the compounds. Example E Inhibition of beta-secretase activity: cellular analysis In analyzing the inhibition of beta-secretase activity using cell line cells of the kidney of a human embryo Necr ADS, inventory No. CRL-1573), transfected AR containing naturally occurring double mutation Lys651Met52 on Asn651Leu652 (numbering for ARR), commonly called the Swedish mutation and, as shown, overproducers A-beta (Citron et al., 1992, Nature, 360:672-674), described in U.S. patent No. 5604102. Cells incubated in the presence/absence of connection inhibitor (dissolved in DMSO) at the desired concentration, usually up to 10 mcg/ml At the end of the treatment period, air-conditioned environment to analyze beta-secretshow activity, for example, by analyzing the cleavage fragments. A-Beta can be analyzed by immunoassay using specific antibodies for detection. The enzymatic activity measured in the presence and in the absence of compounds for inhibitors to demonstrate specific inhibition of cleavage of the substrate by the RDA-mediated beta-secretases. Example F Inhibition of beta-secretase in animal models of AD To test the inhibition of beta-secretase activity can be used in various animal models. Examples of animal models suitable for the zebrette, are, but not limited to, mouse, Guinea pig, dog and other animals. Used animals can be models of wild-type, tracename or models with missing genes. In addition, model animals-mammals can Express the mutation in the RDA, such as ARR-SW, and the like described in this description. Examples of transgenic models mammals that are not relevant to humans, are described in U.S. patent No. 5604102, 5912410 and 5811633. Mouse PDAPP prepared as described by Games et al., 1995, Nature, 373:523-527, suitable for the analysis of in vivo suppression of the release of A-beta in the presence of the alleged connections inhibitors. As described in U.S. patent No. 6191166, 4-month-old PDAPP mice administered the compound in a composition with a carrier, such as corn oil. Mice injected dose of the compound (1-30 mg/ml, preferably 1-10 mg/ml). After some time, for example 3 to 10 hours, animals kill and remove the brain for analysis. Transgenic animals injected a certain amount of coupling inhibitor in combination with a carrier suitable for the chosen route of administration. Control animals not treated, treated with media or treated with an inactive connection. The introduction can be sharp, i.e. in a single dose or in multiple doses per day, or can be constant, i.e. the dose is repeated every day in t is the significance of a few days. Starting from time 0, selected from animals get the brain tissue or cerebral fluid and examined for the presence of peptides cleavage of APP, including A-beta, for example, by immunoassay using specific antibodies for detection of a-beta. At the end of the test period the animals killed and the brain tissue or cerebral fluid examined for the presence of A-beta and/or beta-amyloid plaques. The fabric also examined for necrosis. It is expected that the compounds administered to the animals-inhibitors of the invention will show a low content of A-beta in the brain tissue or cerebral fluids and reduced the number or size of beta-amyloid plaques compared with these values in untreated control animals. Example G Inhibition of the production of A-beta in patients with human Patients suffering from Alzheimer's disease (AD)demonstrate an increased amount of a-beta in the brain. Sick AD impose a certain number of connections-inhibitor in combination with a carrier suitable for the chosen route of administration. The introduction is repeated daily throughout the test period. Starting from day 0, conduct cognitive tests and tests on the memory, for example, once a month. It is expected that patients receiving connection-inhibitors, will show deceleration is whether stabilization of the disease, analyzed the changes compared with patients not receiving treatment, one or more of the following diseases: the presence of A-beta in the CSF or plasma; the volume of the brain or hippocampus; deposition of a-beta in the brain; amyloid plaque in the brain and indicators of cognitive function and memory function. Example N Preventing the production of A-beta in patients with risk of disease AD Patients predisposed to AD or in the status of the risk of developing AD, identify, or on the basis of knowledge of hereditary characteristics, such as having the Swedish mutation, and/or by monitoring diagnostic parameters. Patients identified as predisposed to AD or in the status of the risk of developing AD, enter a number of connections inhibitor in combination with a carrier suitable for the chosen route of administration. The introduction is repeated daily throughout the test period. Starting from day 0, conduct cognitive tests and tests on the memory, for example, once a month. It is expected that patients receiving connection-inhibitors, will demonstrate slowing or stabilization of disease progression analyzed for changes compared with patients not receiving treatment, one or more of the following diseases: the presence of A-beta in the CSF or m is the AZM; the volume of the brain or hippocampus; amyloid plaque in the brain and indicators of cognitive function and memory function. The invention is described with reference to various specific and preferred embodiments and techniques. However, it should be borne in mind that many changes and modifications can be done within the essence and scope of the invention. Scheme And
Scheme
Scheme
Scheme D
Scheme E
The invention is described with reference to various specific and preferred embodiments and techniques. However, it should be borne in mind that many changes and modifications can be done within the essence and scope of the invention. 1. The compound of the formula 2. The compound according to claim 1, where RNrepresents hydrogen. 3. The compound according to claim 1, where RN' represents hydrogen. 4. The compound according to claim 2, where 5. The compound according to claim 3, 6. The method of obtaining the compounds of formula (Y) 7. The method according to claim 6, where the aqueous medium have a pH from about 2 to about 10. 8. The method according to claim 7, where the aqueous medium have a pH from about 3 to about 7. 9. The use of compounds according to claim 1 or its salt to obtain drugs having inhibitory activity against enzyme beta-secretase. 10. The use of compounds according to claim 1 or its salt to obtain drugs for treating or preventing Alzheimer's disease. 11. Pharmaceutical composition having inhibitory activity against enzyme beta-secretase containing an effective amount of a compound according to any one of claims 1 to 5, in combination with a physiologically acceptable carrier or excipient.
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