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1. 发明专利

JP2001072679A NEW BETA-CARBOLINE COMPOUND, ITS PREPARATION, AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效
公开(公告)号：JP2001072679A
公开(公告)日：2001-03-21
申请号：JP2000218942
申请日：2000-07-19
申请人： ADIR
发明人： GOLDSTEIN SOLO , POISSONNET GUILLAUME , PARMENTIER JEAN-GILLES , BRION JEAN-DANIEL , MILLAN MARK , DEKEYNE ANNE , BOUTIN JEAN
IPC分类号： A61K31/437 , A61P1/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07B61/00 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To obtain a new beta-carboline compound which is a strong ligand for a 5-HT2 receptor that is one of the family of 5-hydroxytryptamine (5-HT) receptors and is useful for treating depression, psychosis, somnipathy, aggressive lesion, and so on. SOLUTION: A compound of formula I [the dotted line is a single bound or a double bond (for giving an aromatic property to a ring which has the dotted line); R1 is H. COR8 (R8 H, an aryl or the like) or the like; R2 is cyano, CO2R8 or the like; R3 and R4 together form a 3 to 10C cycloalkyl; R5 is H, a 1 to 6C alkyl or the like; Ra to Rd are each H, a halogen, OH or the like], for example, cyclopentyl 1-(6-chloro-2,3,4,9-tetrahydro-1H-β-carbolin-1-yl) cyclobutanecarboxylate. The compound of formula I is produced, for example, by reacting a compound of formula II with a compound of formula III and then treating the obtained compound of formula IV in the presence of phosphorus oxychloride in a solvent (for example, toluene) to obtain a compound of formula V.

2. 发明专利

NZ505903A Beta-carboline compounds (derivatives of harmaline) and composition to treat depression, psychosis, schizophrenia and migraine 未知
公开(公告)号：NZ505903A
公开(公告)日：2001-08-31
申请号：NZ50590300
申请日：2000-07-21
申请人： ADIR
发明人： GOLDSTEIN SOLO , POISSONNET GUILLAUME , PARMENTIER JEAN-GILLES , BRION JEAN-DANIEL , MILLAN MARK , DEKEYNE ANNE , BOUTIN JEAN
IPC分类号： A61K31/437 , A61P1/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07B61/00 , C07D471/04
摘要： A process for the preparation of b-carboline related compounds for the formula as shown. The b -carboline related compounds are useful for treating symptoms of depression, psychosis, schizophrenia, phobia, anxiety, panic attacks, sleep disorders, appetite disorders, impulsive and aggressive disorders, sexual disorders, migraine. The compounds are potent selective ligands of 5-HT2 receptors, in particular 5-HT2c and 5HT2B antagonists. Wherein; R1 represents hydrogen, linear or branched C1-6alkyl, -R6-aryl, R6-cycloalkyl, R6-heterocycle, -COOR7, -COOR8, CONH-R8; wherein R6 is a linear or branched C1-6alkylene group, R7 is a linear or branched C1-6alkyl, aryl, cycloalkyl, heterocycle, -R6-cycloalkyl group or -R6-heterocycle, and R8 is hydrogen, a linear or branched C1-6alkyl, aryl, cycloalkyl, heterocycle, -R6-aryl, -R6-cycloalkyl or -R6-heterocycle; R2 represents -CN, -COOR8, -CONHR8, mono-C1-6alkylamino-C1-6alkylaminocarbonyl, di-C1-6alkylamino-C1-6alkylaminocarbonyl, -NR8R9, -NHCOOR7, -COR8 or R3 and R4 together form C3-10cycloalkyl group; R5 represents hydrogen, linear or branched C1-6alkyl group or an aryl-C1-6alkyl group in which the alkyl moiety may be linear or branched; Ra, Rb, Rc and Rd, which may be-identical or different, each represents, independently of the others, a group selected from hydrogen, halogen, linear or branched C1-6alkyl, hydroxy, linear or branched C1-6alkoxy, linear or branched trihalo-C1-6alkyl, linear or branched trihalo-C1-6alkoxy, nitro, cyano, amino, linear or branched C1-6alkylamino, di-C1-6alkylamino in which each alkyl moiety may be linear or branched, aryl, aryl-C1-6alkyl in which the alkyl moiety may be linear or branched, carboxy, linear or branched C1-6alkylcarbonyloxy, linear or branched C1-6acyl, aryloxy, and aryl-C1-6alkoxy in which the alkoxy moiety may be linear or branched.

3. 发明专利

NZ270132A EBURNANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：NZ270132A
公开(公告)日：1995-09-26
申请号：NZ27013294
申请日：1994-12-13
申请人： ADIR
发明人： BRION JEAN-DANIEL , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE , PUJOL JEAN-FRANCOIS , SCHMITT PASCAL , POTIER PIERRE , THAL CLAUDE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , C07D487/06 , A61K31/40
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

4. 发明专利

DK0658557T3 未知
公开(公告)号：DK0658557T3
公开(公告)日：1999-05-31
申请号：DK94402862
申请日：1994-12-13
申请人： ADIR
发明人： BRION JEAN-DANIEL , THAL CLAUDE , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE , PUJOL JEAN-FRAN OIS , SCHMITT PASCAL , POTIER PIERRE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , A61K31/495
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

5. 发明专利

ES2123739T3 未知
公开(公告)号：ES2123739T3
公开(公告)日：1999-01-16
申请号：ES94402862
申请日：1994-12-13
申请人： ADIR
发明人： BRION JEAN-DANIEL , THAL CLAUDE , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , A61K31/495
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

6. 发明专利

FR2713644B1 未知
公开(公告)号：FR2713644B1
公开(公告)日：1996-02-09
申请号：FR9314944
申请日：1993-12-14
申请人： ADIR
发明人： BRION JEAN-DANIEL , THAL CLAUDE , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE , PUJOL JEAN-FRANCOIS , SCHMITT PASCAL , POTIER PIERRE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , C07D491/22 , C07D455/00 , A61K31/505 , A61K31/445
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

7. 发明专利

ZA949973B Eburnane analogues a process for the preparation thereof and pharmaceutical compositions containing them 未知
公开(公告)号：ZA949973B
公开(公告)日：1995-08-22
申请号：ZA949973
申请日：1994-12-14
申请人： ADIR
发明人： BRION JEAN-DANIEL , THAL CLAUDE , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE , PUJOL JEAN-FRANCOIS , SCHMITT PASCAL , POTIER PIERRE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , A61K , C07D
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

8. 发明专利

ZA200003702B Beta-carboline compounds, a process for their preparation and pharmaceutical compositions containing them. 未知
公开(公告)号：ZA200003702B
公开(公告)日：2001-05-21
申请号：ZA200003702
申请日：2000-07-21
申请人： ADIR
发明人： GOLDSTEIN SOLO , POISSONNET GUILLAUME , PARMENTIER JEAN-GILLES , BRION JEAN-DANIEL , MILLAN MARK , DEKEYNE ANNE , BOUTIN JEAN
IPC分类号： A61K31/437 , A61P1/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07B61/00 , C07D471/04 , A61K , C07D
摘要： 1-( beta -Carbolin-1-yl)-cycloalkanecarboxylic acid derivatives (I) are new. beta -Carboline derivatives of formula (I), and their isomers and acid or base addition salts, are new. dotted lines = optional bonds; R1 = H, alkyl, -R6-Q, -COOR7, -COR8 or -CONHR8; or is absent if the N of NR1 carries an intracyclic double bond; R6 = 1-6C alkylene; Q = cycloalkyl, aryl or heterocyclyl; R7 = alkyl, Q or -R6-Q; R8 = H or as R7; R2 = CN, COOR8, CONHR8, mono- or dialkylaminoalkylaminocarbonyl, NR8R9, NHCOOR7 or COR6; R9 = as R8; R3 + R4 = group completing 3-10C cycloalkyl; R5 = H, alkyl or arylalkyl; Ra-Rd = H, halo, alkyl, OH, alkoxy, trihaloalkyl, trihaloalkoxy, NO2, CN, NH2, mono- or dialkylamino, aryl, arylalkyl, alkoxycarbonyl, 1-6C acyl, aryloxy or arylalkoxy; cycloalkyl moiety = 3-10C mono- or bicyclic, saturated or mono- or polyunsaturated (but not aromatic) group (optionally substituted by one or more of halo, OH, alkyl and alkoxy); aryl moiety = phenyl, naphthyl, tetrahydronaphthyl, dihydronaphthyl, indenyl or indanyl group (optionally substituted by one or more of halo, OH, CN, NO2, alkyl, alkoxy, NH2, mono- or dialkylamino, aryloxy, arylalkoxy, trihaloalkyl, 1-6C acyl, alkoxycarbonyl, alkylaminocarbonyl and oxo); heterocyclyl moiety = 5-12 membered mono- or bicyclic, saturated or unsaturated, aromatic or non-aromatic group containing 1-3 of N, O and S as heteroatom(s) (optionally substituted by one or more of halo, OH, alkyl, alkoxy, NO2, oxo, NH2, and mono- or dialkylamino); alkyl moieties have 1-6C. An Independent claim is included for the preparation of (I).

9. 发明专利

CA2314473A1 NOUVEAUX DERIVES DE B-CARBOLINE, LEUR PROCEDE DE PREPARATIONET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2314473A1
公开(公告)日：2001-01-23
申请号：CA2314473
申请日：2000-07-20
申请人： ADIR
发明人： DEKEYNE ANNE , MILLAN MARK , BOUTIN JEAN , POISSONNET GUILLAUME , PARMENTIER JEAN-GILLES , GOLDSTEIN SOLO , BRION JEAN-DANIEL
IPC分类号： A61K31/437 , A61P1/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07B61/00 , C07D471/04 , A61P1/14 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/517
摘要： -71- L'invention concerne de nouveaux composés répondant à la formule (I): (voir formule I) dans laquelle ~ représente une liaison simple ou double conférant optionellement un caractère aromatique au cycle qui les porte; R1 représente (a) un atome d'hydrogène, (b) un groupement alkyle, (c) un groupement -R6-aryle ou -R6-cycloalkyle ou -R6- hétérocycle dans lequel R6 représente un groupement alkylène, (d) un groupement -CO2R7 dans lequel R7 représente un groupement alkyle, un groupement aryle, un groupement cycloalkyle, un hétérocycle ou un groupement -R6-aryle, -R6-cycloalkyle ou -R6-hétérocycle dans lequel R6 est tel que défini précédemment, (e) un groupement -COR8 dans lequel R8 représente un atome d'hydrogène, un groupement alkyle, un groupement aryle, un groupement cycloalkyle, un hétérocycle ou un groupement -R6-aryle, -R6-cycloalkyle ou -R6-hétérocycle dans lequel R6 est tel que défini précédemment, ou (f) un groupement -CONHR8 dans lequel R8 est tel que défini précédemment, ou R1 n'existe pas lorsque l'atome d'azote qui le porte, porte déjà une double liaison intracyclique; R 2 représente (a) un groupement cyano, (b) un groupement -CO2R8 dans lequel R8 est tel que défini précédemment, (c) un groupement -CONHR8 dans lequel R8 est tel que défini précédemment, (d) un groupement monoalkylaminoalkylaminocarbonyle ou dialkyl-aminoaminoalkylaminocarbonyle, (e) un groupement -NR8R9 dans lequel R8 est tel que défini précédemment et R9 représente un groupement R8 défini précédemment, ( f) un -72- groupement -NH-CO2R7 dans lequel R7 est tel que défini précédemment, ou (g) un groupement -COR8 dans lequel R8 est tel que défini précédemment; R3 et R4 forment ensemble, avec l'atome de carbone qui les porte, un cycloalkyle; R5 représen te un atome d'hydrogène ou un groupement alkyle ou arylalkyle; Ra, Rb, Rc et Rd, identiques ou différents, représentent indépendamment l'un de l'autre un atome d'hydrogène ou d'halogène, ou un groupement alkyle, hydroxy, alkoxy, trihalogénoalkyle, trihalo-génoalkoxy, nitro, cyano, amino, alkylamino, dialkylamino, aryle, arylalkyle, carboxy, alkylcarbonyloxy, acyle, aryloxy ou arylalkoxy; leurs isomères ainsi que leu rs sels d'addition à un acide ou à une base pharmaceutiquement acceptable. Les composés selon l'invention sont utiles à titre de médicaments pour le traitement de la dépression, de la psychose, de ls schizophrénie, de la phobie, de l'anxiété, des attaques de panique, des troubles du sommeil, des troubles de l'appétit, des troubles impulsifs et agressifs, des troubles sexuels ou de la migraine.

10. 发明专利

DE69412980D1 未知
公开(公告)号：DE69412980D1
公开(公告)日：1998-10-08
申请号：DE69412980
申请日：1994-12-13
申请人： ADIR
发明人： BRION JEAN-DANIEL , THAL CLAUDE , DEMUYNCK LUC , PARMENTIER JEAN-GILLES , LEPAGNOL JEAN , LESTAGE PIERRE , PUJOL JEAN-FRANCOIS , SCHMITT PASCAL , POTIER PIERRE
IPC分类号： C07D471/06 , A61K31/435 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D461/00 , C07D471/22 , A61K31/495
摘要： Compounds of general formula (I): in which A represents a divalent radical chosen from and R1, R2, R3, R4, R5, R6, R7, R8, R9 and Z are as defined in the description. Medicaments.

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