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1. 发明专利

JP2000128865A NEW DIHYDRO AND TETRAHYDRO-QUINOLINE COMPOUND, THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
公开(公告)号：JP2000128865A
公开(公告)日：2000-05-09
申请号：JP29930399
申请日：1999-10-21
申请人： ADIR
发明人： CASARA PATRICK , DOREY GILBERT , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful for treatment of disorders accompanied by aging, e.g. atherosclerosis or cataract, treatment of cancer, treatment of cognitive impairment and treatment of acute neurodegenerative disorder, e.g. cerebral ischaemia or epilepsy. SOLUTION: This compound is represented by formula I [R1 is H or the like; R2 and R31 are each an alkyl, a (substituted) aryl or the like; R40 is H, a (substituted) alkyl or the like; R41 and R5 are each H or together form a bond; R6 to R9 are each H, OW (W is H, an acyl or the like) or the like, with the proviso that all of R6 to R9 are not H and one or more group thereof are OW and when R2 and R3 are each an alkyl, one group OW exists in the molecule and represents OH, R40 is a group other than H], e.g. 6-ethoxy-1,2- dihydroquinoline-2-spirocyclohexane. The compound of formula I is obtained, e.g. by a method. etc., for obtaining a compound of formula V by cyclizing a compound of formula IV obtained from aniline of formula II and a halogenated acetylide of formula III (G is H or the like; Hal is a halogen).

2. 发明专利

CA2287046C NOUVEAUX COMPOSES DIHYDRO ET TETRAHYDROQUINOLEINIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2287046C
公开(公告)日：2003-12-02
申请号：CA2287046
申请日：1999-10-20
申请人： ADIR
发明人： LESTAGE PIERRE , LOCKHART BRIAN , CASARA PATRICK , DOREY GILBERT
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10 , C07D401/00 , C07D405/00 , C07D409/00 , A61K31/495 , A61K31/535
摘要： Composés de formule générale (I): (see formula I) dans laquelle: .cndot. R1 représente un hydrogène ou . dans lequel A est tel que défini dans la description. .cndot. R2 et R3 représentent indépendamment un alkyle, cycloalkyle, hétérocycloalkyle, aryle éventuellement substitué, hétéroaryle éventuellement substitué, cycloalkylalkyle, hétérocycloalkylalkyle, arylalkyle éventuellement substitué, hétéroarylalkyle éventuellement substitué, aminoalkyle éventuellement substitué, ou bien. R2 et R3 forment ensemble avec l'atome de carbone qui les porte un cycloalkyle ou un hétérocycloalkyle monocyclique substitué ou non. .cndot. R40 représente un hydrogène, ou un groupement choisi parmi alkyle éventuellement substitué, alkényle éventuellment substitué, alkynyle éventuellement substitué, ou un groupement Q ou -V-Q dans lesquels V représente un alkylène, alkénylène, ou alkynylène, et Q représente un cycloalkyle éventuellement substitué, aryle éventuellement substitué, hétérocycloalkyle éventuellement substitué, ou hétéroaryle éventuellement substitué. .cndot. R41 et R5 forment ensemble une liaison. ou représentent chacun un hydrogène, .cndot. R6, R7, R8 et R9 représentent indépendamment un hydrogène, un halogène, un alkyle, cycloalkyle (C3-C8), ou -OW dans lequel W est tel que défini dansla description.

5. 发明专利

FR2784988A1 未知
公开(公告)号：FR2784988A1
公开(公告)日：2000-04-28
申请号：FR9813306
申请日：1998-10-23
申请人： ADIR
发明人： CASARA PATRICK , DOREY GILBERT , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10 , A61K31/438
摘要： Dihydro- and tetrahydro-quinoline derivatives (I) are new. Dihydro- and tetrahydro-quinoline derivatives of formula (I) and their acid or base addition salts are new. R1 = H or a group of formula (i); A = H or -B'NZ1Z2; B' = 1-6C alkylene; Z1, Z2 = H, alkyl, 3-8C cycloalkyl or optionally substituted aryl; or NZ1Z2 = heterocycloalkyl or heteroaryl (optionally substituted); R2, R3 = alkyl, 3-8C cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl or aminoalkyl (optionally substituted on N with 1 or 2 alkyl, cycloalkyl, aryl or arylalkyl); or R2 + R3 = form with C of quinoline, 3-8C cycloalkyl or heterocycloalkyl (optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl); R40 = alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted), H, Q or -V'-Q; V' = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; Q = 3-8C cycloalkyl, aryl, heterocycloalkyl, heteroaryl (all optionally substituted); R5, R41 = H; or R5 + R41 = bond; R6-R9 = H, halo, alkyl, 3-8C cycloalkyl or -OW'; W' = aryl, heteroaryl, arylalkyl, heteroarylalkyl (all optionally substituted), H, alkyl, acyl, 3-8C cycloalkyl or heterocycloalkyl; alkyl = 1-6C; aryl = phenyl, naphthyl or biphenyl; heterocycloalkyl = partially unsaturated 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; heteroaryl = aromatic or partially aromatic 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; substituted aryl, arylalkyl = aryl or arylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted by 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro or OH; substituted alkyl, alkenyl, alkynyl and cycloalkyl = alkyl, alkenyl, alkynyl and cycloalkyl substituted with at least one OH, 1-6C alkoxy, 1-6C alkylthio, amino (optionally substituted with 1 or 2 alkyl), carboxy, nitro, CN, 1-6C alkoxycarbonyl or aminocarbonyl (optionally substituted with 1 or 2 alkyl on N); substituted heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl = heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted with 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro, OH or oxo; and provided that R6-R9 are not all H and at least one of R6-R9 is -OW', that R2 and R3 are alkyl when R6-R9 are H, alkyl, alkoxy, R41 and R5 form a bond, R40 is other than H or alkyl; when (I) has one OH and R40 is other than H; when (I) has one methoxy and R40 is other than hydroxyalkyl; and (I) is other than 7-methoxy-2,2-diphenyl-1,2-dihydroquinoline. An Independent claim is also included for the preparation of (I).

6. 发明专利

ZA9906667B Dihydro-and tetrahydro-quinoline compounds, a process for their preparation and pharmaceutical compositions containing them. 未知
公开(公告)号：ZA9906667B
公开(公告)日：2000-05-02
申请号：ZA9906667
申请日：1999-10-22
申请人： ADIR
发明人： CASARA PATRICK , DOREY GILBERT , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10 , A61K , C07D
CPC分类号： C07D221/20 , C07D215/20 , C07D401/06 , C07D471/10

7. 发明专利

CA2287046A1 NOUVEAUX COMPOSES DIHYDRO ET TETRAHYDROQUINOLEINIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2287046A1
公开(公告)日：2000-04-23
申请号：CA2287046
申请日：1999-10-20
申请人： ADIR
发明人： LESTAGE PIERRE , LOCKHART BRIAN , CASARA PATRICK , DOREY GILBERT
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10 , C07D401/00 , C07D405/00 , C07D409/00 , A61K31/495 , A61K31/535
摘要： Composés de formule générale (I) dans laquelle : ~ R1 représente un hydrogène ou , dans lequel A est tel que défini dans la description. ~ R2 et R3 représentent indépendamment un alkyle, cycloalkyle, hétérocycloalkyle, aryle éventuellement substitué, hétéroaryle éventuellement substitué, cycloalkylalkyle, hétérocycloalkylalkyle, arylalkyle éventuellement substitué, hétéroarylalkyle éventuellement substitué, aminoalkyle éventuellement substitué, ou bien, R2 et R3 forment ensemble avec l'atome de carbone qui les porte un cycloalkyle ou un hétérocycloalkyle monocyclique substitué ou non. ~ R40 représente un hydrogène, ou un groupement choisi parmi alkyle éventuellement substitué, alkényle éventuellement substitué, alkynyle éventuellement substitué, ou un groupement Q ou -V-Q dans lesquels V représente un alkylène, alkénylène, ou alkynylène, et Q représente un cycloalkyle éventuellement substitué, aryle éventuellement substitué, hétérocycloalkyle éventuellement substitué, ou hétéroaryle éventuellement substitué, ~ R41 et R5 forment ensemble une liaison, ou représentent chacun un hydrogène, ~ R6, R7, R8 et R9 représentent indépendamment un hydrogène, un halogène, un alkyle, cycloalkyle (C3-C8), ou -OW dans lequel W est tel que défini dans la description. Médicaments.

8. 发明专利

BR9905587A 未知
公开(公告)号：BR9905587A
公开(公告)日：2001-12-11
申请号：BR9905587
申请日：1999-10-22
申请人： ADIR
发明人： CASARA PATRICK , DOREY GILBERT , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： C07D215/06 , A61K31/47 , A61K31/497 , A61K31/517 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/12 , A61P43/00 , C07D215/20 , C07D221/20 , C07D401/06 , C07D471/10 , C07D215/12 , C07D215/16
摘要： Dihydro- and tetrahydro-quinoline derivatives (I) are new. Dihydro- and tetrahydro-quinoline derivatives of formula (I) and their acid or base addition salts are new. R1 = H or a group of formula (i); A = H or -B'NZ1Z2; B' = 1-6C alkylene; Z1, Z2 = H, alkyl, 3-8C cycloalkyl or optionally substituted aryl; or NZ1Z2 = heterocycloalkyl or heteroaryl (optionally substituted); R2, R3 = alkyl, 3-8C cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl or aminoalkyl (optionally substituted on N with 1 or 2 alkyl, cycloalkyl, aryl or arylalkyl); or R2 + R3 = form with C of quinoline, 3-8C cycloalkyl or heterocycloalkyl (optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl); R40 = alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted), H, Q or -V'-Q; V' = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; Q = 3-8C cycloalkyl, aryl, heterocycloalkyl, heteroaryl (all optionally substituted); R5, R41 = H; or R5 + R41 = bond; R6-R9 = H, halo, alkyl, 3-8C cycloalkyl or -OW'; W' = aryl, heteroaryl, arylalkyl, heteroarylalkyl (all optionally substituted), H, alkyl, acyl, 3-8C cycloalkyl or heterocycloalkyl; alkyl = 1-6C; aryl = phenyl, naphthyl or biphenyl; heterocycloalkyl = partially unsaturated 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; heteroaryl = aromatic or partially aromatic 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; substituted aryl, arylalkyl = aryl or arylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted by 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro or OH; substituted alkyl, alkenyl, alkynyl and cycloalkyl = alkyl, alkenyl, alkynyl and cycloalkyl substituted with at least one OH, 1-6C alkoxy, 1-6C alkylthio, amino (optionally substituted with 1 or 2 alkyl), carboxy, nitro, CN, 1-6C alkoxycarbonyl or aminocarbonyl (optionally substituted with 1 or 2 alkyl on N); substituted heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl = heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted with 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro, OH or oxo; and provided that R6-R9 are not all H and at least one of R6-R9 is -OW', that R2 and R3 are alkyl when R6-R9 are H, alkyl, alkoxy, R41 and R5 form a bond, R40 is other than H or alkyl; when (I) has one OH and R40 is other than H; when (I) has one methoxy and R40 is other than hydroxyalkyl; and (I) is other than 7-methoxy-2,2-diphenyl-1,2-dihydroquinoline. An Independent claim is also included for the preparation of (I).

9. 发明专利

FR2806082A1 New benzocycloheptenyl-alkanoic acid derivatives and analogs are selective vitronectin receptor antagonists useful e.g. for treating cardiovascular or inflammatory diseases or especially cancer 未知
公开(公告)号：FR2806082A1
公开(公告)日：2001-09-14
申请号：FR0002902
申请日：2000-03-07
申请人： ADIR
发明人： CASARA PATRICK , PERRON-SIERRA FRANCOISE , ATASSI GHANEM , TUCKER GORDON , SAINT-DIZIER DOMINIQUE
IPC分类号： C07D233/24 , A61K31/4164 , A61K31/4168 , A61K31/417 , A61K31/4184 , A61K31/426 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/505 , A61K31/55 , A61P9/00 , A61P19/10 , A61P27/02 , A61P29/00 , A61P33/14 , A61P35/00 , A61P43/00 , C07D213/36 , C07D213/74 , C07D223/04 , C07D223/12 , C07D233/48 , C07D233/54 , C07D235/10 , C07D235/14 , C07D235/30 , C07D239/14 , C07D277/18 , C07D277/20 , C07D277/42 , C07D401/12 , C07D403/12 , C07D471/04
摘要： Benzocycloheptenyl-alkanoic acid derivatives (including heterocyclic analogs) (I) are new. Benzocycloheptenyl-alkanoic acid derivatives (including heterocyclic analogs) of formula (I), including their enantiomers, diastereomers and acid or base addition salts are new. G = phenyl or aromatic or partially unsaturated 6-membered heterocyclyl (containing 1 or 2 of N and O as heteroatoms), both optionally substituted by at least one R1-R4; G1, G2 = C or N; T1 = -CH2CH2-, -CH=CH- or =CHCH2-, and T2 = a direct bond, or T1 = -CH2- or =CH-, and T2 = -CH2- or =CH-; R1-R4 = halo, alkyl, perhaloalkyl, CN, NO2, OR7, NR6R6', COOR6, CONR6R6', COR6 or S(O)nR6; n = 0-2; R5 = -(CH2)m-COOR6; R6, R6' = H, alkyl, optionally substituted aryl or optionally substituted aralkyl; R7 = H or alkyl; W = -CH-, -C= or =C-, and A = CO, CH2, =CH- or -CH=, or W = N, and A = CO or CH2; X = CO-X1. CO-NR6-X1, SO2-NR6-X1 or S(O)n-X1; X1 = alkylene; Y = Y1, Y2-Y1 or Y1-Y2-Y1; Y1 = alkylene, alkenylene or alkynylene; Y2 = arylene, heteroarylene, cycloalkylene or heterocycloalkylene; Z = Z1, Z10-NR6 or Z10-NR6-CO; Z10 = alkyl or Z1; Z1 = Z2, Z20-C(=NR6), Z20-NR6 or Z20-NR6-CO; Z20 = alkyl, heteroalkyl or Z2; Z2 = heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused aryl-heteroaryl, fused aryl-heterocycloalkyl, fused heteroaryl-heterocycloalkyl or fused heteroaryl-heteroaryl (all optionally substituted); or fused cycloalkyl-heterocycloalkyl; m = 1-6; alkyl or alkylene moieties have 1-6C; heteroalkyl moieties are alkyl having one C replaced by N, O and/or S; alkenylene or alkynylene moieties have 2-6C and 1-3 double or triple bonds; cycloalkyl or cycloalkylene moieties have 3-8C; heterocycloalkyl moieties are 5-7 membered and contain 1-3 of N, O or S; aryl moieties are phenyl or naphthyl; heteroaryl moieties are mono- or bicyclic, partially or completely unsaturated and 5-11 membered, and contain 1-5 of N, O and/or S; the optional substituents on heterocycloalkyl, aryl or heteroaryl moieties are at least one of halo, alkyl, alkoxy, OH, SH, CN, NH2, mono- or dialkylamino, NO2, COOH, alkoxycarbonyl, CONH2, mono- or dialkylcarbamoyl or (in the case of heteroaryl or heterocycloalkyl) oxo. Independent claims are included for the preparation of (I).

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