Ortho-condensed systems (C07D493/04)

(e)-2-(4-{ [3-(2,4-dimethoxyphenyl)acrylamido]methyl} -1h-1,2,3-triazole-1-yl)-2-isopropyl-9-(4-methyl piperazine-1-yl)-3,7-dioxo-3,7-dihydro-2h-furo[3,2-g]chromen, having analgesic activity

Invention relates to a low-toxic (E)-2-(4-{[3-(2,4-dimethoxyphenyl)acrylamido]methyl}-1H-1,2,3-triazole-1-yl)-2-isopropyl-9-(4-methyl piperazine-1-yl)-3,7-dioxo-3,7-dihydro-2H-furo[3,2-g]chromen of formula (I) , having the analgesic activity in the test "acetic acid-induced writhing". The said property enables to use this compound in medicine.

Chromone derivatives, method for preparing them and therapeutic uses thereof

Invention refers to new chromone derivatives of general formula

Quinolone compound and pharmaceutical composition

Invention refers to organic chemistry, namely to new quinolin-4-one derivatives of formula (1) or to its pharmaceutically acceptable salt, wherein R1 represents: (1) hydrogen, (2) C1-C6 alkyl, (35) carbamoyl-C1-C6 alkyl optionally containing morpholinyl-C1-C6 alkyl, or (36) phosphonoxy-C1-C6 alkyl optionally containing one or two C1-C6 alkyl groups on a phosphonoxy group; R2 represents: (1) hydrogen or (2) C1-C6 alkyl; R3 represents phenyl, thienyl or furyl, wherein a phenyl ring presented by R3, can be substituted by one C1-C6 alkoxy group; R4 and R5 are bound to form a group presented by any of the following formulas: , , , , , , or a group presented by the following formula: a group optionally containing one or more substitutes specified in a group consisting of C1-C6 alkyl groups and oxogroups; R6 represents hydrogen; and R7 represents C1-C6 alkoxy group. The invention also refers to a pharmaceutical composition based on the compound of formula , to a preventive and/or therapeutic agent based on the compound of formula (1), using the compound of formula (1), a method for preparing the compound of formula , as well as to specific compounds.

Method for making and prescribing sphaelactone derivate and its composites

Invention refers to micheliolide derivatives of formula , a based pharmaceutical composition and using them for treating cancer. In formula (I) R1 represents H, -C(O)R4, wherein R4 represents C1-8alkyl; R2=R3 represents a double bond, or R3 represents H, and R2 represents substituted alkyl having from 1 to 8 carbon atoms, wherein a substitute represents -NR7R8; or its pharmaceutically acceptable salts; and wherein R7 and R8 can be identical or different, and represent C1-8alkyl; X represents oxygen; Y represents a single bond.

Usnic acid derivatives as anti-tumour agents

Invention provides benzylidene furanone derivatives of (+)-usnic acid of formula 6-13 as anti-tumour agents. The compounds exhibit cytotoxic activity with respect to tumour cell lines CEM-13, U-937, MT-4.

Furilidene furanone derivatives of usnic acid as new antituberculosis agents

Invention concerns Mycobacterium tuberculosis growth inhibitors representing (+) and (-)-enantiomers of derivatives of usnic acid containing a furilidene furanone fragment, namely (10R,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4a and (10S,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4b

Method of obtaining pyripyropene derivatives

Invention relates to a method of obtaining pyripyropene derivatives, namely a compound of formula C: , where R represents a linear chain, a branched chain or cyclic C2-6alkylcarbonyl, on condition that, when an alkyl fragment in an alkylcarbonyl group represents a branched chain or a cyclic group, R represents C3-6alkylcarbonyl, including: selective acylation of hydroxyl groups in 1-position and 11-position of a compound B1, represented by formula B1: with an acylating agent in one-three stages in the presence or absence of a base. (i) compound C is obtained by acylation of hydroxyl groups in 1-position and 11-position of the compound B1 in one stage; (ii) method, including obtaining the compound C by acylation in two stages, consisting of stages: acylation of the hydroxyl group in 11-position of the compound B1 with the acylating agent with obtaining the compound B2, represented by formula B2: , where R is determined in formula C; and additional acylation of the hydroxyl group in 1-position of the compound B2; or (iii) method, including obtaining the compound C by acylation in three stages, consisting of stages: acylation of the hydroxyl group in 11-position of the compound B1 with obtaining the compound B2, represented by formula B2: , where R is determined in the formula C; transfer of acyl in 11-position of the compound B2 to hydroxyl in 1-position with obtaining the compound B3, represented by formula B3: , where R is such as determined in the formula C; and acylation of hydroxyl group in 11-position of the compound B3.

Novel (poly)aminoalkylaminoalkylamide, alkyl-urea or alkyl-sulfonamide derivatives of epipodophyllotoxin, method of obtaining thereof and method of application thereof in therapy as anti-cancer medications

Claimed invention relates to novel derivatives of epipodophyllotoxin, substituted in position 4 with possibly substituted chain of (poly)aminoalkylaminoalkylamide, or alkyl-urea, or alkyl-sulphonamide, of formula 1 where R represents hydrogen or C1-4alkyl, A represents CO(CH2)n or CONH(CH2)n, where n equals 2, 3, 4 or 5, R1 represents H or C1-4alkyl, R2 represents (CH2)m-NR3R4, where m equals 2, 3, 4 or 5, R3 represents H or C1-4alkyl, R4 represents H, C1-4alkyl or (CH2)p-NR5R6, where p equals 2, 3, 4 or 5, R5 represents H or C1-4alkyl and R6 represents H, C1-C4alkyl or (CH2)q-NH2, where q equals 2, 3, 4 or 5 or their pharmaceutically acceptable salts, as well as to methods of their obtaining and to their application as anti-cancer medication.

Method of producing pyripyropene derivatives and intermediate products for production thereof

Invention relates to a method of producing a compound C of formula: [1] where R' is a linear, branched or cyclic C2-6 alkyl carbonyl group. In this method, the protective group for the hydroxy group in position 7 used is R1b; where R1b is a formyl group, optionally substituted with a linear C1-4 alkyl carbonyl group, optionally substituted benzyl group, a -SiR3R4R5 group, where R3, R4 and R5 are independently a linear or branched C1-4 alkyl group or a phenyl group, which can be substituted with a halogen atom, a C1-6alkyloxy-C1-6alkyl group, which can be substituted with a halogen atom, C1-6alkylthio-C1-6alkyl group, which can be substituted with a halogen atom, a linear, branched or cyclic C1-6alkyl group, which can be substituted with a halogen atom (in case of branched or cyclic, denotes a C3-4alkyl group), C2-6alkenyl group, which can be substituted with a halogen atom, C2-6alkynyl group, which can be substituted with a halogen atom, or an optionally substituted saturated or unsaturated 5-member or 6-member heterocyclic group. The invention also includes methods of producing intermediate compounds B2a and B2b and the compound of formula 2Bb itself.

Novel compounds with spirochiral carbon base, methods of their obtaining and pharmaceutical compositions which contain such compounds

Invention relates to novel compound with spirochiral carbon base, or its pharmaceutically acceptable salt of general formula 1 , where W represents CO or CHO(C=O)CH3; X represents N3 or OR2; R2 represents hydrogen, linear or branched alkyl C1~C8 or Y represents O; Z represents simple bond or O; R3 represents linear or branched alkyl C1~C8 or alkenyl C2~C8, and M and N represent, each independently, hydrogen, OH or are absent; carbon atom, bound with M or N forms simple bond or double bond with other carbon atoms, and number of double bonds constitutes one or less for each of carbon atoms. Invention relates to method of obtaining and pharmaceutical compositions.

Cinnamic acid compounds (versions), intermediate compounds for their obtaining, based on them pharmaceutical composition, method of inhibiting histone diacetase, method of treating diabetes, method of treating tumour or disease associated with cell proliferation, method of enhancing axon growth and method of treating neurodegenerative diseases and spinal muscular atrophy

Invention relates to novel compounds, represented by the following formula (I) and their pharmaceutically acceptable salts, where values for groups R1, R4-R6, Ra, m, n, Y, X are determined in the invention formula. Said compounds are used as preparations for enhancing growth of axons and prevention of diseases associated with histone diacetases, in particular tumours or diseases associated with cell proliferation.

Intermediate compounds and methods of synthesis of analogues of halichondrin b

Methods are described for synthesis of intermediate compounds used in synthesis of analogues of halichondrin B, in particular, the method to produce substantially diastereomer-pure composition of the compound with the formula including: crystallisation of the specified compound of the formula (I) from the mixture of diastereomers with production of a composition, in which the ratio of the specified compound of the formula (1) to a compound with the opposite stereochemical configuration of chiral centre, indicated with an asterick, makes at least 8:1, where the specified compound of the formula (I) represents: where: z is a single or double link, provided that whenever z is a double link, X2 is C, and Y1 is a hydrogen atom; and provided that when z is a single link, X is CH or O; X1 is O; Y1 is a halogen atom, a hydrogen atom or O-L2, or is absent, when X is O; L1 and L2 independently represent a hydrogen atom or a protective group, or L1 and L2 together are a protective group; or its salt. The invention also includes a whole row of intermediate compounds and a composition of a mixture of separate diastereomers of these compounds.

Solid forms of ortataxel

Present invention refers to solid forms of 1,14-carbonate 13-(N-Boc-β-isobutylserinyl)-14-b-hydroxybaccatineIII (Ortataxel) of formula

Tetrahydropyranochromen gamma-secretase inhibitors

Invention refers to new gamma-secretase inhibitors of formula I: , wherein L1,R1, R2,X,n and Ar have the values specified in the description, their pharmaceutically acceptable salts and solvates, as well as to pharmaceutical compositions based on these compounds for treating Alzheimer's disease and the use of drugs for gamma-secretase and beta-amyloid protein inhibition, and for treating neurodegenerative diseases such as Alzheimer's disease.

Mixture of diesters of dianhydrohexitol derivatives with carboxylic acids of empirical formula c₈h₁₇cooh, methods of producing said diesters and use of said mixtures

Invention relates to a mixture of diesters of formula I with R1-R8=H or an alkyl group with 1-6 carbon atoms, wherein residues R1-R8 may be identical or different, which is characterised by that the mixture contains at least two different diesters I differing in the structure of at least one of the carboxylic acid radicals C8H17COO present, plasticiser properties; the invention also relates to use of said mixtures in paints, inks or coatings, in plastisols, adhesives or adhesive components, in sealants, as plasticisers in plastic or plastic components, as solvents, as lubricant components and as auxiliary materials in metal processing, and a method of producing diesters of isosorbide derivatives of formula I. The invention also describes compositions with PVC or plastisol containing the disclosed mixtures.

Methods of producing hexahydrofuro[2, 3-b] furan-3-ol

Invention relates to a method of producing a compound of formula (V) which can be used in pharmaceutical industry . The method involves reaction of a compound of formula (II) with a compound of formula (III) in the presence of a titanium salt of formula Ti(Hal)n(OR)4-n, where Hal is a halogen radical, n equals 0, 1, 2 or 3, R is an alkyl or arylalkyl, and subsequent reaction of the reaction product with an alcohol of formula (IV), where R1 and R2 denote alkyl or arylalkyl, where the aryl is phenyl or naphthyl.

Docosahexaenoic acid ethers and their application for treatment and prevention of cardiovascular diseases

This invention relates to a compound ether of docosahexanoic acid and an alcohol, its production method and a pharmaceutical composition applied as a medication for prevention and treatment of cardiovascular diseases. The said alcohol is selected from pentanol with formula: and inositol with formula . The compound ether production method consists in transetherification of docosahexanoic acid ethyl ether with one of the said alcohols.

Method of synthesis of anticancer derivatives of (poly)aminoalkylaminoacetamide epipodofillotoxine

Invention refers to a new method for preparing anticancer preparations representing derivatives of (poly)aminoalkylaminoacetamide epipodofillotoxine of formula 1. The method implies a condensation stage of the compounds of formulae 4 and 6 in a polar aprotonic solvent without pre-protection of functional amine groups to produce a compound of formula 1, wherein in formulae 1, 4 and 6 R represents hydrogen atom or -(CH2)c-NH2, 2≤a, b, c≤5.

Carbocyclic and heterocyclic arylsulfones as γ-secretase inhibitors

Claimed invention relates to compounds of formula (I) or to their pharmaceutically acceptable salts, in which X is selected from group, consisting of-C(R1)2-, -O-, -S-, -S(O2)-, -NR1-; each R1 is independently selected from group consisting of H and alkyl; each of R2, R3 and R4 is independently selected from group consisting of (1) H, (2) alkyl, (3) -OR5, (4) alkylene-OR5, (5) -alkylene-R6, (6) -C(O)O-alkyl, (7) - alkylene-C(O)O-alkyl, (8) -alkylene-R8, (9) -NHR5, (10) -N(R5)2, (11) alkenyl, (12) -NH-R8, (13) -NH-CH(C(O)O(C1-C6)alkyl)-alkylene-O-alkyleneR6, (14)-NHCH(C(O)O(C1-C6)aalkyl)-alkylene-OH, (15) -NH-C(O)-alkenyl and (16) -N(C1-C6alkyl)C(O)-alkenyl; or R2 and R3 or R2 and R4 or R3 and R4 together with atoms with which they are bound, form condensed 3-7-member cycloalkyl or heterocycloalkyl ring, which represents non-aromatic monocyclic ring system, which contains in ring from about 5 to about 7 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen or oxygen, and said condensed cycloalkyl or heterocycloalkyl ring is not substituted or is substituted with one or several groups L3 ; and on condition that if X represents -O-, and m equals 1, then, at least, one of R2, R3 or R4 is not H; each R5 is independently selected from group consisting of (1) H, (2) (C1-C6)alkyl, (3) hydroxy-substituted alkyl, (4) R6, (5) R7, (6) -C(O)-(C1-C6)alkyl, (7) -C(O)-(C1-C6)halogenalkyl, (8) -C(O)-R6, (9) -C(O)-R7, (10) -C(O)NH-(C1-C6)alkyl, (11) -C(O)N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (12) -S(O)2-(C1-C6)alkyl, (13) -S(O)2-(C1-C6)halogenalkyl, (14) -S(O)2-R6, (15) -S(O)2-R7, (16) -S(O)2-R8, (17) -alkylene-C(O)-(C1-C6)alkyl, (18) -alkylene-C(O)-(C1-C6)halogen-alkyl, (19) -alkylene-C(O)-R6, (20) -alkylene-C(O)-R7, (21) -alkylene-S(O)2-(C1-C6)alkyl, (22) -alkylene-S(O)2-(C1-C6)halogenalkyl, (23) -alkylene-S(O)2-R6, (24) -alkylene-S(O)2-R7, (25) -alkylene-S(O)2-R8, (26) -alkylene-NHC(O)-(C1-C6)alkyl, (27) -alkylene-NHC(O)-(C1-C6)halogenalkyl, (28) alkylene-NHC(O)-R6, (29) -alkylene-NHC(O)-R7, (30) -alkylene-NHS(O)2-(C1-C6)alkyl, (31) -alkylene-NHS(O)2-(C1-C6)halogenalkyl, (32) -alkylene-NHS(O)2-R6, (33) -alkylene-NHS(O)2-R7, (34) -alkylene-N(alkyl)C(O)-(C1-C6)alkyl, (35) -alkylene-N(alkyl)C(O)-(C1-C6)halogenalkyl, (36) -alkylene-N(alkyl)C(O)-R6, (37) -alkylene-N(alkyl)C(O)-R7, (38) -alkylene-N(alkyl)S(O)2-(C1-Ce)alkyl, (39) -alkylene-N(alkyl)S(O)2-(C1-C6)halogen-alkyl, (40)-alkylene-N(alkyl)S(O)2-R6, (41) -alkylene-N(alkyl)S(O)2-R7, (42) -alkylene-C(O)-NH-(C1-C6)alkyl, (43) -alkylene-C(O)-NHR6, (44) -alkylene-C(O)-NHR7, (45) -alkylene-S(O)2NH-(C1-C6)alkyl, (46) -alkylene-S(O)2NH-R6, (47) -alkylene-S(O)2NH-R7 , (48) -alkylene-C(O)-N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (49) -alkylene-C(O)-N(alkyl)-R6, (50) -alkylene-C(O)-N(alkylene)-R7, (51) -alkylene-S(O)2N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (52) -alkylene-S(O)2N(alkyl)-R6, (53) -alkylene-S(O)2N(alkyl)-R7, (54) -alkylene-OH, (55) -alkylene-OC(O)-NH-alkyl, (56) -alkylene-OC(O)NH-R8, (57) -alkylene-CN, (58) -R8, (59) -alkylene-SH, (60) -alkylene-S(O)2-NH-R8, (61) -alkylene-S(O)2-alkylene-R6, (62) substituted with halogen alkylene, (63) -C(O)OR8, (64) -C(O)O(C1-C6)alkyl, (65) -C(O)R8, (66) -C(O)-alkylene-O-(C1-C6)alkyl, (67) -C(O)NH2, (68) -alkylene-O-(C1-C6)alkyl, (69) -alkylene-R8, (70) -S(O)2-halogen(C1-C6)alkyl, (71) hydroxy-substituted halogen(C1-C6)alkyl, (72) -alkylene-NH2, (73) -alkylene-NH-S(O)2-R8, (74) -alkylene-NH-C(O)-R8, (75) -alkylene-NH-C(O)O-(C1-C6)alkyl, (76) -alkylene-O-C(O)-(C1-C6)alkyl, (77) -alkylene-O-S(O)2-(C1-C6)alkyl, (78) -alkylene-R6 , (79) -alkylene-R7, (80) -alkylene-NH-C(O)NH-(C1-C6)alkyl, (81) -alkylene-N(S(O)2 halogen(C1-C6)alkyl)2, and each -S(O)2 halogen(C1-C6)alkyl fragment is selected independently, (82) -alkylene-N((C1-C6)alkyl)S(O)2-R8 , (83) -alkylene-OC(O)-N(alkyl)2, and each alkyl is selected independently, (84) -alkylene-NH-(C1-C6)alkyl, (85) -C(O)-alkylene-C(O)O-(C1-C6)alkyl, (86) -C(O)-C(O)-O-(C1-C6)alkyl, (87) -C(O)-alkylene-R6, (88) -C(O)-NH-R8, (89) -C(O)-NH-R6, (90) -C(O)-NH-alkylene-R6, (91) -C(O)-alkylene-NH-S(O)2-halogen(C1-C6)alkyl, (92) -C(O)-alkylene-NH-C(O)-O-(C1-C6)alkyl, (93) -C(O)-alkylene-NH2, (94) -C(O)-alkylene-NH-S(O)2-R8, (95) -C(O)-alkylene-NH-S(O)2-(C1-C6)alkyl, (96) -C(O)-alkylene-NH-C(O)-(C1-C6)alkyl, (97) -C(O)-alkylene-N(S(O)2(C1-C6)alkyl)2, and each -S(O)2(C1-C6)alkyl fragment is elected independently, (98) -C(O)-alkylene-NH-C(O)-NH-(C1-C6)alkyl, (99) -alkylene-O-R6, (100) -alkylene-R7, (101) -C(O)OH, (102) -alkylene-N(S(O)2(C1-C6)alkyl)2, (103) -alkylene-C(O)-O-(C1-C6)alkyl, (104) halogenalkyl, (105) halogen, (106) -alkylene-C(O)-NH2, (107) =N-O-(C1-C6)alkyl, (108) =N-O-alkylene-R6, (109) =N-O-alkenyl, (110) -N-O-R6, (111) =N-NH-S(O)2-R6, (112) alkenyl, (113) =R8, (114) -O-C(O)-R9, (115) -O-C(O)-(C1-C6)alkyl, (116)-CN, R6 is selected from group consisting of unsubstituted (C6-C14)aryl, (C6-C14)aryl, substituted with one or several groups L1, unsubstituted (C5-C14)heteroaryl and (C5-C14)heteroaryl, which represents aromatic monocyclic or bicyclic system, which contains in ring from about 5 to about 9 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen, oxygen or sulphur, one or in combination, substituted with one or several groups L1; R7 is selected from group consisting of unsubstituted heterocycloalkyl and heterocycloalkyl which represents non-aromatic monocyclic system, which contains in ring from about 4 to about 6 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen, oxygen substituted with one or several groups L2; R8 is selected from group consisting of unsubstituted cycloalkyl and cycloalkyl substituted with one or several groups L2; A8 is selected from group consisting of (a) unsubstituted aryl, (b) aryl substituted with one or several groups L1; each group L1 is independently selected fron group consisting of halogen, alkyl, -CN, -CF3, -O-(C1-C6)alkyl, -O-(halogen(C1-C6)alkyl), -alkylen-OH (-CH2OH); each group L2 is independently selected from group consisting of (a) -OH, (b) alkyl, (c) alkyl substituted with one or several groups -OH and (d) piperidyl; each group L3 is independently selected from group consisting of -CN, =O, R5 , -OR5 ; =N-R5 and -N(R5)2; n equals 0, 1, 2 or 3; and m equals 0, 1 or 2; and on condition that in composition of substituent -OR5 fragment R5 and oxygen atom, which it is bound with, do not form group -O-O-; and on condition that in composition of substituents -OR5, =N-R5 and -NHR5 R5 are not -CH2OH, -CH2NH2, -CH2NH-alkyl, -CH2NH-aryl or -C(O)OH. Invention also relates to pharmaceutical composition, as well as to application of one or several compounds by one of ii. 1-125.

Synergist for improvement of effectiveness of biological agents against colorado potato beetle

Improvement of effectiveness of insecticidal preparation is achieved through the use in sublethal doses of a mixture of fluorinated usnic acid (FUA) of the formula and II obtained by the reaction of (+)-usnic acid with perfluoropropene as a synergist of such insecticides. The decline of the latent period of the disease and increased mortality rate of larvae of Colorado potato beetle is marked using FUA and entomopathogenic microorganisms of Beauveria bassiana, Metarhizium anisopliae and Bacillus thuringiensis. The mixed composition of FUA at a concentration of 0.03% with a suspension of conidia of the fungus Bauveria bassiana with a titer of 3×106 conidia/ml (in vitro) and 5×106 conidia/ml (in the field) has proved to be the best in all respects.

Method of producing optically active chromene oxide compound

Invention relates to a method of producing an optically active chromene oxide compound of formula or formula where R5, R6, R7, R8, R9, R10 and A are as described in the claim, and the absolute configuration of carbon atoms, denoted by *, denotes (R) or (S), which includes asymmetric epoxidation of a chromene compound of formula or formula with an oxidant in a solvent using optically active titanium complexes of formula formula formula and formula where R1, R2, R3 and R4 are defined in the claim, as a catalyst for asymmetric oxidation of the optically active chromene compound with high enantioselectivity and high chemical output.

Novel condensed pyrrole derivatives

Invention relates to compounds of formula (1) (lb) in which A denotes a benzene ring; Ar denotes naphthalenyl which optionally contains 1-3 substitutes independently selected from a group comprising C1-C6alkyl, C3-C7cycloalkyl, C3-C7cycloalkyl-C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, hydroxy group, C1-C6alkoxy group, halogen, heteroalkyl, heteroalkoxy group, nitro group, cyano group, amino- and mono- or di- C1-C6alkyl-substuted amino group; R1 denotes hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy group, carboxy group, heteroalkyl, hydroxy group optionally substituted with heterocyclylcarbonyl-C1-C6alkyl or R1 denotes N(R')(R")-C1-C6alkyl or N(R')(R")-carbonyl- C1-C6alkyl-, in which R' and R" are independently selected from a group comprising hydrogen, C1-C6alkyl, C3-C7cycloalkyl, C3-C7cycloalkyl-C1-C6alkyl, heteroalkyl, phenyl-C1-C6alkyl; or R1 denotes R'-CO-N(R")-C1-C6alkyl, R'-O-CO-N(R")- C1-C6alkyl- or R'-SO2-N(R")- C1-C6alkyl-, in which R' and R" are independently selected from a group comprising hydrogen, C1-C6alkyl, C3-C7cyclalkyl, C3-C7cycloalkyl- C1-C6alkyl or optionally substituted phenyl; R2, R2' and R2" independently denote hydrogen, halogen, cyano group, C1-C6alkyl, halogenated C1-C6alkyl or C1-C6alkoxy group; n equals 1; and pharmaceutically acceptable salts thereof. The invention also relates to use of compounds in any of claims 1-9, as well as to a pharmaceutical composition.

Antiarrhythmic compound precursors, synthesis processes and methods of application

Invention refers to compounds of formula formula (1) formula (2) or to their hydrate, solvate, salt or tautomer form where R1 independently represents H or halogen; R2 represents H or --R10-NR11R12 where R10 represents C1-C6 alkylene; R11 and R12 independently represent H, C1-C4 alkyl; and R3 independently represents H or halogen. Besides, the invention covers methods of preparing the compounds of the present invention.

Synthesis of protease inhibitor precursor

Invention relates to a compound of formula (I) or stereoisomer thereof, or salt thereof, as well as synthesis method thereof and intermediate compounds of formulae (II) and (III) used in this method.

Methods of producing (3r, 3as, 6ar) hexahydrofuro[2,3-b]furan-3-ol

Invention relates to methods of producing diastereoismerically pure (3R,3aS,6aR)hexahydrofuro[2,3-b]furan-3-ol (6), as well as a novel intermediate compound (3aR,4S,6aS)-4-methoxytetrahydrofuro [3,4-b]furan-2-one (4) for use in said methods. More specifically, the invention relates to a stereo-selective method of producing diastereoisomerically pure (3R,3aS,6aR)hexahydrofuro[2,3-b]furan-3-ol, as well as methods for crystallisation of (3aR,4S,6aS)-4-methoxytetrahydrofuro[3,4-b]furan-2-one and epimerisation of (3aR,4S,6aS)-4-methoxytetrahydrofuro[3,4-b]furan-2-one to (3aR,4S,6aS)-4- methoxytetrahydrofuro[3,4-b]furan-2-one.

Products of oxidative decomposition of atorvastatin calcium

Invention relates to products of oxidative decomposition of atorvastatin calcium, specifically to 4-[6-(4-fluorophenyl)-6-hydroxy-1b-isopropyl-6a-phenyl-1a-phenylcarbamoylhexahydro-1,2-dioxa- 5a-azacyclopropa [a]inden-3-yl]-3-(R)-hydroxybutyric acid, phenylamide 4-(4-fluorophenyl)-2,4-dihydroxy-2-isopropyl-5-phenyl-3,6-dioxabicyclo[3.1.0]hexane-1-carboxylic acid and 4-[1b-(4-fluorophenyl)-6-hydroxy-6-isopropyl-1a-phenyl-6a-phenylcarbamoylhexahydro-1,2-dioxa-5a-azacyclopropa [a]inden-3-yl]-3-(R)-hydroxybutyric acid. The invention also relates synthesis methods thereof, based on oxidation of an atorvastatin salt.

Method and device for preparing compositions rich in episesamin

Sesamin or sesamin-containing composition undergoes epimerisation in such a way that a portion of the sesamin converts to episesamin. Episesamin is crystallised through recrystallisation. The device for producing sesamin has an isomerisation unit which has a mixing reservoir for mixing oil or fat containing sesamin or a sesamin-containing composition with an acid catalyst; a crystallisation unit having a crystallisation reservoir for carrying out recrystallisation; a liquid supply line which connects the mixing reservoir with the crystallisation reservoir.

Method for synthesis of 4beta-amino-4'-demethyl-4-desoxypodophyllotoxin

Invention relates to a method for synthesis of 4β-amino-4'-demetyl-4-desoxypodophyllotoxin of formula (1), involving the following steps: a) reaction of thiourea and 4β-halogenoacetamido-4'-demethyl-4-desoxypodophyllotoxin in a medium of a weak pure acid or mixture of acid, water an organic solvent without using any other solvent at temperature higher than ambient temperature; b) extraction of 4β-amino-4'-demethyl-4- desoxypodophyllotoxin.

Pest control agent

Invention describes compositions for use as a pest control agents containing a compound of formula (I), or a salt of the said compound, acceptable in agriculture or horticulture, as an active ingredient or carrier which is acceptable in agriculture or horticulture: [chemical formula 1] , where Het1 denotes an optionally substituted pyridyl, R1 denotes hydroxyl, optionally substituted C1-6alkylcarbonyloxy, optionally substituted C1-6alkyloxy, or oxo, in the absence of a hydrogen atom in position 13, or the bond between position 5 and position 13 is a double bond in the presence of R1 and a hydrogen atom in position 5, R2 denotes hydroxyl, optionally substituted C1-18alkylcarbonyloxy, benzoyloxy or C1-6alkylsulphonyloxy, R3 denotes a hydrogen atom, hydroxyl, optionally substituted C1-18alkylcarbonyloxy, benzoyloxy, C1-6alkylsulphonyloxy, benzoylsulphonyloxy, imidazolylthiocarbonyloxy, R4 denotes a hydrogen atom, hydroxyl, optionally substituted C1-18alkylcarbonyloxy, C2-6alkenylcarbonyloxy, C2-6alkynylcarbonyloxy, benzoyloxy, C1-6alkylsulphonyloxy, benzoylsulphonyloxy, benzyloxy, C1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy, C1-6alkylthio-C1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy-C1-6alkyloxy, C1-6alkyloxycarbonyloxy, C1-6alkylaminocarbonyloxy, tetrahydropyranyloxy, a saturated or unsaturated five- or six-member heterocyclic carbonyloxy, where the said heterocyclic part is selected from a group comprising pyridyl, thienyl, thiazolylpyrazinyl and imidazolyl, optionally substituted tieno[3,2-b]pyridylcarbonyloxy, 1H-indolylcarbonyloxy, imidazolylthiocarbonyloxy, or oxo, in the absence of a hydrogen atom in position 7, provided that the compound, where Het1 denotes 3-pyridyl, R1 denotes hydroxyl and each of R2, R3 and R4 is acetyloxy, is excluded. Disclosed composition is also used in hemipterous pest control.

Method for synthesis of epothilone derivatives, novel epothilone derivatives, as well as novel intermediate compounds for realising said method and synthesis methods thereof

Invention relates to novel epothilone derivatives of formula (8) , to synthesis method thereof and use thereof to obtain compounds of formula (9) , as well as to novel intermediate compounds for realising said method and synthesis methods thereof. The abbreviation P in said general structural formulae denotes a protective group of a functional hydroxyl selected from silyl protective groups, R2 denotes a 5-member heteroaryl containing N and S as heteroatoms, optionally substituted with C1-C6 alkyl, and R1 denotes methyl.

Dibenzylidene sorbitol (dbs) based compounds, composition and method of using said compounds

Invention relates to novel dibenzylidene sorbitol (DBS) compounds of formula 1: , in which R1 and R2 are independently selected from a group consisting of CH3CH2CH2- and CH3CH2CH2O-; and in which R3 is independently selected from -CH2CH2CH3 and -CH2-CH=CH2 groups. According to one version, this invention pertains to a disubstituted DBS based compound having an allyl or propyl group as a substitute at the first carbon atom in the sorbitol chain. The present invention also relates to compositions containing such DBS based compounds and preparation methods thereof.

Tricyclic compounds of benzopyran as antiarrhythmic agents

Invention relates to benzopyran derivatives of formula or

Method for production of (3r, 3as,6ar)-hexahydrofuro[2,3-b]furan-3-yl(1s,2r)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1- benzyl-2-hydroxypropylurethane

Production of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylurethane is carried out with application of intermediate compound 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(isobutyl)benzenesulfonamide. (3R,3aS,6aR)- hexahydrofuro [2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylurethane is applicable, in particular as inhibitor of HIV protease.

Derivatives of 2-(hereto)aryl-substituted tetrahydroquinolines

There are presented compounds of formula I wherein W, R, R1, R2, R3, R4, R5, R6 and R7 have values specified in cl. 1 of the patent claim, and to method for making these compounds, a based medicinal agent used for treating conditions affected by inhibition, regulation and/or modulation of mitotic motor protein Eg5, to a mixture and application of said compounds for making the medicinal agent.

Method of polyolefin composition nucleation by acetal compounds

Invention concerns method of polyolefin composition nucleation by mixing the composition with compound of the structural formula: , where: n is 0, 1 or 2; Ar1 and Ar2 are independently selected out of group including non-substituted aryl groups and aryl groups substituted by substitutes selected out of group including alkyl groups, alkenyl groups, alkinyl groups, alkoxy groups, carboxy groups and halogens; and R is selected out of group including alkenyl groups, alkyl groups, alkoxy groups, hydroxyalkyl groups and alkylhalide groups. Also invention claims the compound itself, method of its obtaining and moulded or cast polyolefin article including this compound.

Method of obtaining epotilone derivatives

Method ensures carrying out aldole condensation in presence of epoxide mesilate and tosilate, using auxiliary chiral sultamic group as carboxyl- protecting group, as a result, reduction and oxidation stages, requiring extra time, before carrying out final stage of macrolactonisation are excluded. Introduction of epoxidic group at early stages of method allows also excluding stage of epoxilation of more complex intermediate compounds at further stages of process.

New tetracyclic compounds containing heteroatom, used as selective modulators of oestrogen receptors

Invention pertains to new tetracyclic compounds containing a heteroatom. The compounds can be used in treating and/or prevention of disorders, associated with oestrogen depletion, such as hot flash, vaginal dryness, osteopenia and osteoporosis; sensitive cancerous diseases hormone and hyperplasia of the lacteal gland, endometrium, cervix uteri and prostate; endometriosis, uterus fibrosis and osteoarthritis, and as contraceptive agents, used either separately or combined with progestogen or a progestogen antagonist.

Analogs of himbacin, their using and pharmaceutical composition based on thereof possessing property of thrombin receptor antagonist

Invention relates to heterocycle-substituted tricyclic compounds of the formula (I): or their pharmaceutically acceptable salts wherein R means hydrogen atom; R1 and R2 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R3 means hydrogen atom; n1 and n2 = 0-3 independently under condition that they both do not mean 0; Het means pyridyl wherein pyridyl is added to B through cyclic carbon atom and it comprises from 1 to 4 substitutes (W) chosen independently from group comprising -NR4R5, -NHCOR26, -NHSO2R16; R21 means aryl and R21 means heteroaryl wherein heteroaryl represents furyl, thienyl, pyridyl, thiazolyl, pyrrolidinyl, azethidinyl; R4 and R5 mean hydrogen atom or alkyl comprising 1-6 carbon atoms, or R4 and R5 mean in common -(CH2)3-, -(CH2)4-, -(CH2)5- or -(CH2)2NR7-(CH2)2- wherein R7 means hydrogen atom or alkyl comprising 1-6 carbon atoms; R8, R, R10 and R11 mean hydrogen atom; B means -(CH2)n4CR12=CR12a(CH2)n5 wherein n4 and n5 = 0-2 independently; R12 and R12a are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R21 means from 1 to 3 substitutes chosen independently from group comprising hydrogen atom, trifluoromethyl, trifluoromethoxy, halogen atom, cyano, alkyl comprising 1-6 carbon atoms, alkoxy group comprising 1-6 carbon atoms, or -CR29(=NOR28); R22 means -COR23, -S(O)R31, -S(O)2R31 or -COOR27; R23 means cycloalkyl comprising 3-7 carbon atoms, (C3-C7)-cycloalkyl-(C1-C6)-alkyl, cycloalkyl comprising 3-7 carbon atoms containing from 1 to 3 substitutes chosen from group comprising halogen atom, (C1-C3)-alkoxy-(C1-C3)-alkyl, hydroxy group and alkoxy group comprising 1-6 carbon atoms, aryl, aryl-(C2-C6)-alkyl; R27 means alkyl comprising 1-6 carbon atoms, phenyl or benzyl; R28 and R29 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R31 means alkyl comprising 1-6 carbon atoms, halogenalkyl comprising 1-6 carbon atoms, aryl, aryl-(C1-C6)-alkyl. Also, invention relates to pharmaceutical compositions containing these substances and their using for preparing a drug used in treatment of thrombosis, atherosclerosis, restenosis, hypertension, stenocardia, arrhythmia, heart failure and cancer.

Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants)

Invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra 1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

C-glycoside derivatives and their salts

Invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R1-R4 represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R5-R11 represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH2, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH2, -O-lower alkylene-C(=O)-N-(lower alkyl)2, -O-lower alkylene-CH(OH)-CH2(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)2, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)2, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na+-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.

Tetracyclic heterocompounds as estrogen receptor modulating agents

Invention relates to novel tetracyclic heterocompounds of the formula (I): wherein X, Y, Z, R1 - R4, n and m has values given in the invention description and used as selective modulating agents for estrogen receptors. Also, invention relates to a method for synthesis of these compounds and pharmaceutical compositions comprising thereof, and their using in treatment and/or prophylaxis of disorders mediated by one or more estrogen receptors. Proposed compounds are useful in treatment and/or prophylaxis of disorders associated with depleting estrogen and comprising such disorders as rush of blood, vaginal dryness, osteopenia and osteoporosis, hormone-dependent cancer and hyperplasia of breast, endometrium, uterus cervix and prostate, endometriosis, uterus fibroma, osteoarthritis that can be used as contraceptive agents both separately and in combination with progestogen or progestogenous antagonist.

Method for isolating epotilons from reaction mixture and desorption from synthetic resin (variants), using low-polar or nonpolar solvent for realization of method

Invention relates to a method for isolation of epotilons used in medicine in treatment of cancer diseases. Method for desorption of epotilons A, B, D and/or E from synthetic resin is based on using low-polar or nonpolar solvent chosen from the group comprising (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Used aromatic solvent is chosen from the group including naphthalene, benzene or naphthalene and benzene substituted with one or some substitutes chosen from the following group: (lower)-alkyl, (lower)-alkoxy-group, halogen atom, nitro-group and (lower)-alkoxy-(lower)-alkyl wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Solvent is removed to the required level but up to preparing a dry residue preferably. If necessary, residue is dissolved in mixture alcohol/hydrocarbon in the corresponding volume ratio. Alcoholic phase is evaporated until dry and then alcoholic extract is crystallized from mixture alcohol and hydrocarbon. Then formed crystallized product is dissolved in mixture nitrile/water but preferably in mixture acetonitrile/water taken in the ratio = 2:3 (vol./vol.). Formed solution is applied on column (if necessary, after separation for some distillates) for preparative chromatography in reversed phase followed by elution with mixture nitrile/water, removing nitrile and extraction of an aqueous phase with ester. Ester extract is evaporated and formed product is subjected for crystallization. Method for preparing epotilons A, B, D and/or E from resin or reaction mixture involves the following steps: (a) desorption of epotilons with low-polar or nonpolar solvent chosen from the group including (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents being the desorption step can be repeated up to achievement of the more complete desorption; (b) removal of solvent used in desorption from formed solutions by evaporation; (c) optional crystallization of epotilon(s) after desorption and first of all for crystallization of epotilon B by addition of mixture of alcohol with hydrocarbon and the following evaporation of alcoholic phase until dry and crystallization of epotilon B from the corresponding mixture of solvents; (d) (obligatory step) separation of epotilons by method of chromatography in reversed phase and the following dissolving a residue obtained in previous step in suitable solvent, elution with mixture nitrile/water and removing nitrile from epotilon-containing fractions by evaporation. If necessary, water remained with epotilon is extracted with ester followed by evaporation of epotilon-containing ester phase until dry; (e) optional purification by adsorption chromatography method, and final recrystallization of purified epotilon from corresponding solvents or mixture of solvents. If necessary, in this process between each step formed solutions or suspensions are concentrated, and/or liquid or solid components are separated of one another. Separation of epotilons A and B is carried out by chromatography method based on a mobile layer modeling. Invention provides simplifying methods for preparing large amounts of epotilons for satisfying requirement in these agents.

Crystals of taxane derivatives and method for their preparing

Invention relates to a novel crystalline form of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylideneoxy]-5,20-epoxy-1-hydroxytax-11-ene-13-yl-(2R,3S)-3-(tert.-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate that shows the diffraction picture of roentgen rays in powder with characteristic peaks at diffraction angles (θ)= 6.2o, 10.3o, 10.7, 11.4o and 12.0, and a method for its preparing. Method involves carrying out the crystallization step by using organic solvent chosen from group consisting of ketone type solvent, nitrile solvent type and their mixture, or mixture of said solvent and water. Also, invention relates to an antitumor agent based on the prepared crystalline form. Invention provides the stable quality of a medicinal agent based on its lower hygroscopicity.

Method for preparing 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens

Invention relates to a method for synthesis of new compounds, namely, 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens of the formula: (Ia-f): wherein (Ia): R means hydrogen atom (H); R1 means hydrogen atom (H); (Ib): R means bromine atom (Br); R1 means hydrogen atom (H); (Ic): R means chlorine atom (Cl); R1 means hydrogen atom (H); (Id): R means hydrogen atom (H); R1 means bromine atom (Br): (Ie): R means hydrogen atom (H); R1 means chlorine atom (Cl); (If): R means methoxy-group (-OCH3); R1 means hydrogen atom. Method involves formation of condensed tetracyclic system as result of the successive recyclization reactions of furan ring of derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol and the secondary cyclization of formed isochromen ketone in boiling of solution containing derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol of the formula: in ethanol medium in the presence of hydrogen chloride alcoholic solution for 15-40 min. Invention provides synthesis of new derivatives of isochromens possessing the potential anti-inflammatory activity.

Method for preparing derivatives of baccatin iii

Invention relates to a novel method for preparing 14β-hydroxy-1,4-carbonate-desacetylbaccatin III and intermediate substances used in preparing new derivatives of taxane and possessing an antitumor activity. Method involves the following stages: a) protection of hydroxyls at positions 7 and 10 in 10-desacetylbaccatin III wherein R and R1 are taken among hydrogen atom, (C1-C10)-alkyl or aryl, (C1-C10)-alkyl- or aryl-carbonyl, trichloroacetyl, (C1-C4)-trialkylsilyl; preferably, when R and R1 are similar then they represent trichloroacetyl; when they are different then, preferably, R represents trichloroacetyl and R1 represents acetyl; or R represents triethyl or trimethylsilyl and R1 represents acetyl; b) two-stage oxidation to yield a derivative oxidized to carbonyl at position 13 and hydroxylated at position 14; c) carboxylation of vicinal hydroxyls at positions 1 and 14 to yield 1,14-carbonate derivative; d) reduction of carbonyl at position 13; e) removal of protective groups at positions 7 and 10. Also, invention relates to intermediate substances. Invention provides preparing intermediate substances used in synthesis of taxane.

Taxane pentacyclic compound and antitumor agents based on thereof

Invention relates to a new pentacyclic compound derivative of taxane represented by the formula:

Hexahydrofuro[2,3-b]furan-3-yl-n-{3-[(1,3-benzodioxol-5- yl- sulfonyl)(isobu tyl)amino]-1-benzyl-2-hydroxypropyl}carbamate, pharmaceutical composition based on thereof, methods for inhibition and method for treatment

Invention relates to new bis-tetrahydrofuranbenzodioxolyl sulfonamide compounds of the formula (I): , its salts, stereoisomers and racemates that are effective inhibitors of protease activity. Also, invention relates to pharmaceutical preparations, methods for inhibition of retrovirus proteases, in particular, to resistant retrovirus proteases, to many drugs, methods for treatment and prophylaxis of infection or disease associated with retrovirus infection in mammals and to methods for inhibition of retrovirus replication. Invention provides preparing new derivatives of bis-tetrahydrofuranbenzodioxalyl sulfonamides eliciting the valuable pharmaceutical properties.