RussianPatents.com
|
Thiophenyl and pyrrolyl azepines as serotonin 5ht2c receptor ligands and use thereof. RU patent 2434872. |
|
FIELD: chemistry. SUBSTANCE: invention relates to compounds of formula , where X denotes S; R1 and R2 taken together with atoms to which they are bonded form a 5-member carbocycle, substituted with up to two substitutes selected from alkyl and CF3; R3 is selected from a group consisting of a hydrogen atom and C1-8-alkyl; R3a denotes a hydrogen atom; R4 denotes a hydrogen atom; R4a denotes a hydrogen atom; R5 denotes a hydrogen atom; R5a denotes a hydrogen atom; R6 denotes a hydrogen atom; R6a denotes a hydrogen atom; R7 denotes a hydrogen atom; or pharmaceutically acceptable salts thereof. The invention also relates to compounds of the given formula, compounds selected from the group, as well as a pharmaceutical composition. EFFECT: obtaining novel biologically active compounds which modulate serotonin receptor activity. 6 cl, 19 ex, 1 tbl
|
Uniformly tritium-labelled (r)-(+)-[5-methyl-3-(4-morpholinylmethyl) -2,3-dihydro-[1,4]oxazine[2,3,4-hi]-6-indolyl]-1-naphthalinylmethanone acetate / 2404185 Invention relates to uniformly tritium-labelled (R)-(+)-[5-methyl-3-(4-morpholinylmethyl)-2,3-dihydro-[1,4]oxazine[2,3,4-hi]-6-indolyl]-1-naphthalinylmethanone acetate of formula I: . |
Derivatives (indole-3-yl) heterocyclic compounds as agonists of cannabinoid receptors cb1 / 2376302 Invention is related to new derivatives (indole-3-yl)heterocyclic compounds of formula 1: , where: A represents 5-member aromatic heterocyclic ring, where X1, X2 and X3 are independently selected from N, O, S, CR; R means H, (C1-4)alkyl; or R, when it is available in X2 or X3, may form 5-8-member ring together with R3; R1 means 5-8-member saturated carbocyclic ring, which unnecessarily contains heteroatom O; R2 means H; or R2 is connected to R7 with creation of 6-member ring, which unnecessarily contains heteroatom O, or where mentioned heteroatom is connected to position 7 of indole ring; R3 and R4 independently mean H, (C1-6)alkyl, which is unnecessarily substituted with OH, (C1-4)alkyloxy; or R3 together with R4 and N, with which they are connected, creates 4-8-member ring, which unnecessarily contains additional heteroatom, selected from O and S, and unnecessarily substituted with OH, (C1-4)alkyl, (C1-4)alkyloxy or (C1-4)alkyloxy-(C1-4)alkyl; or R3 together with R5 creates 4-8-member ring, unnecessarily substituted with OH, (C1-4)alkyl, (C1-4)alkyloxy; or R3 together with R, when present in X2 or X3, creates 5-8-member ring; R5 means H; or R5 together with R3 creates 4-8-member ring, unnecessarily substituted with OH, (C1-4)alkyl, (C1-4)alkyloxy; R5' means H; R6 means one substituent selected from H, (C1-4)alkyl, (C1-4)alkyloxy, halogen; R7 means H, (C1-4)alkyl, (C1-4)alkyloxy, halogen; or R7 is connected to R2 with creation of 6-member ring, which unnecessarily contains additional heteroatom O, and where heteroatom is connected to position 7 of indole ring; or its pharmaceutically acceptable salt. Compounds of formula I display activity of agonists to cannabinoid receptor CB1. |
Substituted 6a, 11-dihydro-5h-benzo[4,5][1,3]oxazino[2,3-alpha]isoindol-11-ons-antidots of herbicide of hormonal action of 2,4-dichlorophenoxyacetic acid and method of their obtaining / 2345083 Invention relates to novel biologically active compounds - substituted benzoxazin isoindoles of formula 1: 8,9-dimethoxy-5,5-diphenyl-6a, 11-dihydro-5H-benzo[4,5][1,3]oxazin[2,3-a]isoindol-11-on of formula 1.1; 8,9-dimethoxy-5,5-diethyl-6a, 11-dihydro-5H-benzo[4,5][1,3]oxazin[2,3-a]isoindol-11-on of formula 1.2, protecting sunflower shoots against adverse impact of herbicide of 2,4-dichlorophenoxyacetic acid and method of obtaining them. Method of obtaining 8,9-dimethoxy-5,5-diphenyl-6a, 11-dihydro-5H-benzo[4,5][1,3]oxazin[2,3-a]isoindol-11-on of formula 1.1; 8,9-dimethoxy-5,5-diethyl 6a, 11-dihydro-5H-benzo[4,5][1,3]oxazin[2,3-a]isoindol-11-on of formula 1.2 includes interaction of o-aminophenyldiethyl-(diphenyl)carbinoles wth substituted 2-formyl-4,5-dimethoxybenzoic acids with ratio 1:1. Difference of claimed method from method-analogue lies in single-stage process. |
Derivatives of pyridine and medicinal agent based on thereof possessing selective blocking activity with respect to subspecies of nmda-receptors / 2303037 Invention relates to novel compounds of the formula (IA) or (IB) given in the invention description wherein R1 means hydrogen atom, (C1-C7)-alkyl, -(CH2)n-OH, -(CH2)n-N(R6)2; R2 means (C1-C7)-alkyl, -(CH2)n-N(R6)2, -NR6C(O)C(O)O-(C1-C7)-alkyl, -NR6-(CH2)n-OH, -NR6C(O)-(C1-C7)-alkyl, -NH-benzyl; R3 means hydrogen atom or amine; or R2 and R3 in common with carbon atoms to which they are bound mean the group -N(R6)-CH2-O-CH2-; R4 means hydrogen atom or (C1-C7)-alkyl; R5 means hydrogen atom; R6 means independently of one another hydrogen atom or (C1-C7)-alkyl; R' means hydrogen atom or (C1-C7)-alkyl; n = 0, 1, 2 or 3. Also, invention relates to a medicinal agent possessing the selective blocking activity with respect of subspecies of NMDA-receptors and containing one or more compounds of the formula (IA) or (IB) or their pharmaceutically acceptable acid-additive salt or inert carrier. Invention provides preparing novel compounds possessing the high affinity to NMDA-receptors that can be used as components of a medicinal agent for treatment of diseases mediated by these receptors. |
Novel condensed pyrrole derivatives / 2434853 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. |
Organic compounds / 2430921 Invention relates to an azathiabenzo-azulene derivative of formula I |
Method of producing highly pure prasugrel or acid addition salt thereof / 2424243 Invention relates to a method of producing prasugrel hydrochloride of the formula: |
Novel cysteine protease inhibitors and therapeutic application thereof / 2424234 Invention relates to novel compounds of the formula I |
Pharmaceutical compounds / 2422449 Invention refers to new compounds of formula (I) and to their pharmaceutically acceptable salts exhibiting PI3 kinase inhibitor activity. In the formula (I), A represents a thiophen ring; n=1; R1 represents , where m=1; R30 represents H; R4 And R5 together with N atom whereto attached form a 5- or 6-members N-containing heterocyclic group which includes 0 or 1 additional heteroatom selected from N and O which is unsubstituted or substituted by one or more substitutes selected from C1-6alkyl, C1-6alkoxy, -N(R"')-alk-OR, -alk-OR, -O-alk-OR, -alk-C(O)NR2, -C(O)NR2, -alk-Het, -N(R)-Het, -O-Het, -N(R)-C(O)- alk-OR, -NR-S(O)2R, -N(R)-alk-S(O)2R, -N(R)-alk-OR, -alk-NR'R", -N(R"')-S(O)2R, S(O)2R"', -S(O)2-alk-ORf 5- or 6-members N-containing heterocyclic group, 5- or 6-members N-containing heteroaryl group which includes 0 or 1 additional heteroatom selected from N, O or S, oxo(=O), -SO2NR2, -SO2-alk-NR2 where alk means a C1-6alkylene chain; Het means a 5- or 6-members N-containing heteroaryl group or furan optionally substituted by C1-6alkyl; R means H or C1-6alkyl, or when 2 groups R are bound with N, they together with N atom form a saturated 5- or 6-members N-containing heterocyclic group; each R' and R" means independently H, C1-6alkyl or C1-6alkoxy; R'" represents C1-6alkyl, a 5- or 6-merous saturated N-containing heterocyclic group, or a 5- or 6-merous N-containing heteroaryl group; R2 means where R6 and R7 together with N atom whereto attached form a morpholine group; R3 represents an indazole group. |
Pharmaceutical compounds / 2422448 Invention refers to the new fused pyrimidines of formula (I) and to their pharmaceutically acceptable salts exhibiting P13 kinase inhibitor properties; in formula (I), A represents a thiophen ring; n=1; R1 represents a group of formula , where m=1; R30 represents hydrogen; R4 and R5 together with N atom whereto attached form a 5- or 6-members saturated N-containing heterocyclic group which includes 1 additional heteroatom selected from N which is unsubstituted or substituted by C1-C3alkyl which can be substituted by OH; S(O)2C1-3alkyl; C(O)N(diC1-C3alkyl); N(CH3)2; CON(CH3)-CH2CH2OCH3; N(CH3)-CH2CH2OCH3; -C(O)morpholine or morpholine; R2 is selected from where R6 and R7 together with nitrogen atom whereto attached form a morpholine group which is unsubstituted; and R3 represents an indole group which is unsubstituted. |
Condensed heterocyclic derivative, therapeutic composition which contains it and its application in medicine / 2418803 Invention relates to condensed heterocyclic derivative, represented by formula (I): where ring A represents 5-member monocyclic heteroaryl, containing 1 or 2 heteroatoms, selected from N or S; RA represents lower alkyl group, optionally substituted with hydroxyl group, COW1, COOW1 or CONW2W3, in which W1-W3 independently represent a hydrogen atom or lower alkyl group; m represents integer 0 or 2; ring B represents benzene ring or thiophene ring; RB represents halogen atom, cyano group, lower alkyl group or OW4, in which W4 represents a hydrogen atom or lower alkyl group; n represents integer 0-2; E1 represents an oxygen atom; E2 represents an oxygen atom; U represents a single bond or lower alkelene group; X represents group, represented by Y, -CO-Y, -SO2-Y, -S-L-Y, -O-L-Y, -CO-L-Y, -SO-L-Y, -SO2-L-Y, -S-Z or -O-Z, in which L represents a lower alkylene group optionally substituted with halogen or hydroxy group; Y represents group, represented by Z or -NW7W8, where W7 and W8 independently represent a hydrogen atom, lower alkyl group or Z on condition that W7 and W8 are not simultaneously hydrogen atoms, or W7 and W8 can bind together with adjacent nitrogen atom with formation of cyclic amino group; Z represents cycloalkyl group, optionally condensed with phenyl and optionally substituted with phenyl group, optionally substituted with halogen or alkoxy group; 6-8-member heterocycoalkyl group, which has 1 heteroatom, selected from nitrogen atom or oxygen atom, optionally condensed with phenyl and optionally substituted with phenyl; phenyl group optionally substituted with a substituent, selected from group, consisting of a halogen atom, cyano group, alkyl group, optionally substituted with halogen atom, hydroxy group or alkoxy group, alkoxy group, optionally substituted with halogen atom, hydroxy group, alkoxy group, alkoxy-carbonyl-oxy group or acyloxy group, alkylthio group, carboxy group and alkoxy-carbonyl group; pyridyl; or its pharmaceutically acceptable salt. Invention also relates to pharmaceutical composition possessing antagonistic activity with respect to gonatotropin-releasing hormone, based on the claimed compound. |
Application of thienopyridone derivatives as ampa-activators and pharmaceutic compositions, containing them / 2416409 Invention relates to application of thienopyridone derivatives of formula (I), in which B represents CH, represents , or , R represents H, R1 and R2, independently on each other, represent H, linear or branched (C1-C4)alkyl, (C1-C4)cycloalkyl, halogen or together form group -(CH2)n-, where n=1- 4, R3 and R4, independently on each other, represent H, R6 represents H, X represents -O-, or their pharmaceutically acceptable salts for preparation of pharmaceutical composition. |
Thienopyridines / 2415859 Invention relates to pharmaceutically suitable salts which are given in claim 1. The invention also relates to medicinal agents based on the said compounds, which are HSP90 inhibitors. |
Pyrazole derivatives and use thereof as receptor tyrosine kinase inhibitors / 2413727 Present invention relates to novel pyrazole derivatives of formula (I) or pharmaceutically acceptable salts thereof, having tyrosine kinase Trk inhibiting properties and used for treating or preventing malignant growths accompanied by high level of Trk, to a method of producing said derivatives, use thereof to prepare a medicinal agent, pharmaceutical compositions based on said derivatives, a method of inhibiting Trk activity and a method of obtaining antiproliferative action. where A denotes a single bond or C1-2alkylene; where the said C1-2alkylene can be optionally substituted with one R22; ring C is a phenyl or a 5-6-member heterocyclic ring with 1-2 heteroatoms selected from N or S. Values of R1-R7, R22 and n are given in the formula of invention. |
C-phenyl-1-thioglucitols / 2434862 Invention relates to C-phenyl-1-thioglucitols of formula (I), [formula I] , where X is a hydrogen atom or a C1-6alkyl group, Y is a C1-6alkylene group or -O-(CH2)n- (where n equals a integer from 1 to 5), and Z is -CONHRA or -NHCONHRB (provided that when Z is -NHCONHRB, n is not equal to 1), where RA is a C1-6alkyl group substituted with 1-3 substitutes selected from a group consisting of a hydroxyl group and -CONH2, and RB denotes a hydrogen atom or a C1-6alkyl group substituted with 1-3 substitutes selected from a group consisting of a hydroxyl group and -CONH2, and pharmaceutically acceptable salts thereof or hydrates thereof. The invention also relates to a sodium-dependent glucose transporter 1 (SGLT1) activity inhibitor, a sodium-dependent glucose transporter 1 (SGLT1) and sodium-dependent glucose transporter 2 (SGLT2) activity inhibitor, as well as a prophylactic or therapeutic agent against diabetes. |
Reverse-configuration mimetics and methods relating thereto / 2434017 Invention relates to novel conformationally stable compounds of general formula (I), which imitate the secondary structure of reverse-configuration regions of biologically active peptides and proteins which are reverse-configuration mimetics. The compounds can be used to inhibit or treat disorders modulated by Wnt-signalling pathway, such as cancer, especially colorectal cancer. The invention also relates to a library containing the disclosed compound. In general formula (I), A denotes -(C=O)-, B denotes -(CHR4)-, D denotes -(C=O)-, E denotes -(ZR6)-, G denotes -(XR7)-, Z denotes CH, X denotes a nitrogen atom, W denotes -(C=O)NH-, R1 denotes benzyl; R2 denotes a heterocyclylC1-6alkyl group, including a 9-member condensed bicyclic ring having 2-3 heteroatoms selected from nitrogen, oxygen or sulphur atoms; a substituted hetercyclylC1-6alkyl group, including a 9-member condensed bicyclic ring having 2-3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, an the ring has 1-3 substitutes independently selected from a group comprising halogen, piperidinyl, morpholinyl, C2-6alkenyl, phenyl, hydroxyphenyl, C1-6alkoxycarbonyl, dialkylamino, hydroxypiperidinyl, C1-6alkyl, hydroxyC1-6alkylpiperazinyl, amino, piperidinyl carbonyl; heterocyclyl-C1-6alkyl group having a 9-member condensed bicyclic ring which has one or two nitrogen atoms; and other values given in the claim. R4 denotes a substituted benzyl, having a substitute selected from disodium phosphate, monosodium phosphate, phosphate; R6 denotes hydrogen; R7 denotes: C1-6alkyl; C1-6alkynyl; C2-6alkenyl; substituted benzyl, having one or more substitutes independently selected from halogen and C1-6alkyl. |
Novel polycyclic compounds / 2434006 Pharmaceutical compositions containing at least one compound of formula (IIIa) or (IIIb) or (IVa) or (IVb), where -X- and Y are described in the claims, or pharmaceutically acceptable salts, esters or amides thereof and a pharmaceutically acceptable carrier, which can be used in processes with modulation or E- and P-selectin expression. |
Application of antioxidants for gene modulation / 2433819 Invention relates to field of veterinary. Method includes stage of introduction of food composition, which contains one or several antioxidants, selected from group: vitamin E, vitamin C, lipoic acid, L-carnitine, beta-carotin, selenium, lutein, tocotrienol(s), coenzyme Q10, S- adenosylmethionine, taurine, isoflavone(s) of soya, N-acetylcysteine, glutathione, which are introduced in definite quantities. |
Method of experimental modelling of periodontitis / 2433485 To study etiology and pathogenesis of periodontitis, and in order to define tactics of treating periodontitis in case, when evident symptoms of periodontitis exacerbation are absent carried out is modelling of periodontitis on dogs by introduction in gum around neck of upper and lower incisors of ethanol in concentration 65-75% or corticosteroid medication in amount 0.3-0.4 ml per injection. |
Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1h]-one and zilpaterol / 2433131 Present invention relates to a method for selective synthesis of 6R,7R trans-stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one and 6R,7R trans-stereoisomer of zilpaterol or salts thereof for preparing medicinal agents. The disclosed method of producing 6R,7R trans-stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one involves reaction of 4,5-dihydroimidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or salt thereof with H2 in the presence of a catalyst which contains a complex of at least one phosphine ligand with at least one metal selected from a group comprising rhodium, ruthenium and iridium. The disclosed method for selective synthesis of the 6R,7R trans-stereoisomer of zilpaterol involves reaction of 4,5-dihydroimidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime with H2 in the presence of a catalyst to form 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one and conversion of the latter to zilpaterol. |
Methods and intermediate products / 2433127 Invention relates to a compound of formula I , isomer thereof of formula IA , mixture of isomers thereof IA/C , synthesis method thereof, as well as methods of producing compounds of formula IVA from compounds of formula IA, involving reduction and removal of protection from compounds of formula IA via hydrogenolysis using H2 and a catalytic amount of Pd/C, in the presence of trifluoroacetic acid to obtain a compound of formula VA; further reaction of this compound with Cbz-t-leu-OH, EDC and HOBt to obtain a compound of formula VIA; reaction of compound VIA with H2 and a catalytic amount of Pd/C in the presence of citric acid to obtain an amine and reaction of said amine and 4-amino-3-chlorobenzoic acid in the presence of CDMT and NMM to obtain a compound of formula IVA. |
© 2013-2014 Russian business network RussianPatents.com - Special Russian commercial information project for world wide. Foreign filing in English. |