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12. 发明专利

PT869952E 未知
公开(公告)号：PT869952E
公开(公告)日：2002-02-28
申请号：PT96941108
申请日：1996-12-04
申请人： SANOFI SYNTHELABO
发明人： SEVRIN MIREILLE , EVANNO YANNICK , FROST JONATHAN , LARDENOIS PATRICK , GEORGE PASCAL , DARGAZANLI GIHAD
IPC分类号： A61K31/00 , A61K31/335 , A61K31/357 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P9/00 , A61P25/00 , C07D319/06 , C07D405/12
摘要： PCT No. PCT/FR96/01926 Sec. 371 Date Jun. 8, 1998 Sec. 102(e) Date Jun. 8, 1998 PCT Filed Dec. 4, 1996 PCT Pub. No. WO97/20836 PCT Pub. Date Jun. 12, 1997Compounds of general formula (I) in which R1 represents a hydrogen atom or a (C1-C4)alkyl, (C3-C6)cycloalkylmethyl or phenyl-(C1-C3)alkyl group optionally substituted on the phenyl ring with one or more atoms or groups chosen from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R2 represents a hydroxyl or alkoxy group or a group of general formula NR3R4 in which R3 and R4 each represent a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridyl group, or alternatively R3 and R4 form, together with the nitrogen atom, a pyrrolidine or piptzidine ring, and n represents the number 1, 2 or 3. Application in therapy.

13. 发明专利

BG103271A DERIVATIVES OF N-(BENZOTHIAZOL-2-YL) PIPERIDINE-1-ETHANEAMINES, METHOD FOR THEIR PREPARATION AND APPLICATION AS THERAPEUTICAL MEANS 未知
公开(公告)号：BG103271A
公开(公告)日：2000-05-31
申请号：BG10327199
申请日：1999-03-22
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , GEORGE PASCAL , LARDENOIS PATRICK , FROST JONATHAN , SCHOEMAKER JOHANNES , RENONES MARIA-CARMEN , MAGAT PASCALE
IPC分类号： A61K31/425 , A61K31/454 , A61P25/00 , C07D417/12
摘要： The invention relates to compounds with the general formula where n has the value of 0, 1,2 or 3, R1 means hydrogen or halogen, of methyl group, or methoxygroup, R2 is hydrogen or methyl group, R3 means hydrogen or one or two halogen atoms. 4 claims

14. 发明专利

CZ430699A3 Derivatives of 5-naphthalen-1-yl-1,3-dioxan, process of their preparation and their therapeutical use 未知
公开(公告)号：CZ430699A3
公开(公告)日：2000-04-12
申请号：CZ430699
申请日：1998-06-03
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , LARDENOIS PATRICK , FROST JONATHAN , GEORGE PASCAL
IPC分类号： A61K31/357 , A61P25/00 , C07D319/06 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12

15. 发明专利

NO995966L 未知
公开(公告)号：NO995966L
公开(公告)日：2000-02-04
申请号：NO995966
申请日：1999-12-03
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , LARDENOIS PATRICK , FROST JONATHAN , GEORGE PASCAL
IPC分类号： A61K31/357 , A61K31/382 , A61K31/4025 , A61K31/427 , A61K31/4433 , A61K31/4725 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/06 , A61P43/00 , C07D319/06 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D
摘要： The invention concerns compounds of formula (I) in which: R1 represents an alkyl group; V represents a hydrogen atom or a linear or branched alkyl, cycloalkyl, cycloalkylmethyl, phenylalkyl group optionally substituted on a phenyl ring, carboxymethyl, alkoxycarbonylmethyl, carbamoylmethyl optionally substituted on the nitrogen; W represents a carboxymethyl, alkoxycarbonylmethyl, carbamoylmethyl group optionally substituted on the nitrogen, a cyclic group with 4 to 7 apices and optionally containing an oxygen or sulphur atom, or a pyridinylmethyl, 1-methylpyrrolymethyl, furanyl-methyl, thienylmethyl or 1,3-thiazolylmethyl group, or V and W together, and with the nitrogen atom, form a pyrrolidinyl, piperidinyl, or 1,2,3,4-tetrahydroisoquinolinyl group. The invention is applicable in therapy.

16. 发明专利

NO995966A 未知
公开(公告)号：NO995966A
公开(公告)日：2000-02-04
申请号：NO995966
申请日：1999-12-03
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , LARDENOIS PATRICK , FROST JONATHAN , GEORGE PASCAL
IPC分类号： A61K31/357 , A61K31/382 , A61K31/4025 , A61K31/427 , A61K31/4433 , A61K31/4725 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/06 , A61P43/00 , C07D319/06 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D
CPC分类号： C07D405/06 , C07D319/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12

17. 发明专利

FR2861070B1 未知
公开(公告)号：FR2861070B1
公开(公告)日：2006-01-06
申请号：FR0312143
申请日：2003-10-17
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , ESTENNE BOUHTOU GENEVIEVE , MEDAISKO FLORENCE , RAKOTOARISOA NATHALIE
IPC分类号： C07D207/09 , A61K31/401 , A61K31/55 , A61P25/00 , C07D223/04
摘要： N-heterocyclylmethyl-benzamide derivatives (I) and their acid addition salts are new. N-heterocyclylmethyl-benzamide derivatives of formula (I) and their acid addition salts are new. [Image] n : 1-3; R 1hydrogen, 1-7C alkyl (optionally substituted by one or more fluoro), 3-7C cycloalkyl (Cy), Cy(1-3C)alkyl, phenyl(1-3C)alkyl (optionally substituted by 1 or 2 methoxy), or 2-4C alkenyl or alkynyl; X : hydrogen or one or more of halo, trifluoromethyl, 1-6C alkyl or alkoxy; R 2hydrogen or one or more of halo, trifluoromethyl, 1-6C alkyl or alkoxy, Cy, phenyl, cyano, acetyl, benzoyl, 1-6C alkylthio, 1-6C alkylsulfonyl, carboxy, 1-6C alkoxycarbonyl, NR 3R 4, SO 2NR 3R 4 or CONR 3R 4; R 3 and R 4hydrogen, 1-6C alkyl or Cy; and R 3 + R 4a pyrrolidino, piperidino or morpholino ring. ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Antialcoholic; Endocrine-Gen.; Eating Disorders-Gen.; Antimigraine; Spasmolytic; Analgesic; Antiparkinsonian; Anticonvulsant; Neuroprotective; Neuroleptic; Hypnotic. No details of tests for these activities are given. MECHANISM OF ACTION : Glycine transporters glyt1 and glyt2 inhibitor. IC 5 0 0.01-10 MicroM for glyt1 and 0.1-10 MicroM for glyt2.

18. 发明专利

FR2861070A1 New N-heterocyclylmethyl-benzamide derivatives, useful for treating e.g. dementia and Parkinson's disease, are inhibitors of glycine transporters 未知
公开(公告)号：FR2861070A1
公开(公告)日：2005-04-22
申请号：FR0312143
申请日：2003-10-17
申请人： SANOFI SYNTHELABO
发明人： DARGAZANLI GIHAD , ESTENNE BOUHTOU GENEVIEVE , MEDAISKO FLORENCE , RAKOTOARISOA NATHALIE
IPC分类号： A61P25/00 , C07D207/09 , C07D223/04 , A61K31/401 , A61K31/55
摘要： N-heterocyclylmethyl-benzamide derivatives (I) and their acid addition salts are new. N-heterocyclylmethyl-benzamide derivatives of formula (I) and their acid addition salts are new. [Image] n : 1-3; R 1hydrogen, 1-7C alkyl (optionally substituted by one or more fluoro), 3-7C cycloalkyl (Cy), Cy(1-3C)alkyl, phenyl(1-3C)alkyl (optionally substituted by 1 or 2 methoxy), or 2-4C alkenyl or alkynyl; X : hydrogen or one or more of halo, trifluoromethyl, 1-6C alkyl or alkoxy; R 2hydrogen or one or more of halo, trifluoromethyl, 1-6C alkyl or alkoxy, Cy, phenyl, cyano, acetyl, benzoyl, 1-6C alkylthio, 1-6C alkylsulfonyl, carboxy, 1-6C alkoxycarbonyl, NR 3R 4, SO 2NR 3R 4 or CONR 3R 4; R 3 and R 4hydrogen, 1-6C alkyl or Cy; and R 3 + R 4a pyrrolidino, piperidino or morpholino ring. ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Antialcoholic; Endocrine-Gen.; Eating Disorders-Gen.; Antimigraine; Spasmolytic; Analgesic; Antiparkinsonian; Anticonvulsant; Neuroprotective; Neuroleptic; Hypnotic. No details of tests for these activities are given. MECHANISM OF ACTION : Glycine transporters glyt1 and glyt2 inhibitor. IC 5 0 0.01-10 MicroM for glyt1 and 0.1-10 MicroM for glyt2.

19. 发明专利

AU2003274292A1 DERIVATIVES OF DIOXANE-2-ALKYL CARBAMATES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS 未知
公开(公告)号：AU2003274292A1
公开(公告)日：2004-03-19
申请号：AU2003274292
申请日：2003-08-27
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , BAS MICHELE , DARGAZANLI GIHAD , HOORNAERT CHRISTIAN , LI ADRIEN TAK , MEDAISKO FLORENCE
IPC分类号： A61K31/335 , A61K31/357 , A61K31/4178 , A61K31/4184 , A61K31/4433 , A61P1/00 , A61P1/12 , A61P9/00 , A61P11/00 , A61P13/02 , A61P13/12 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/08 , C07D319/06 , C07D405/06 , C07D405/12 , C07D413/06
摘要： 1,3-Dioxanylalkylcarbamate derivatives (I) are new. 1,3-Dioxanylalkylcarbamate derivatives of formula (I) and their salts, hydrates and solvates are new. [Image] R 1phenyl or naphthyl optionally substituted with halo, OH, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3, OCF 3, benzyloxy, 3-6C cycloalkoxy or (3-6C)cycloalkyl(1-3C)alkoxy; R 2CHR 3CONHR 4, CH 2CF 3, imidazol-2-ylmethyl, benzimidazol-2-ylmethyl, or phenyl optionally substituted with halo, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3 or OCF 3; R 3H or Me; R 4H, 1-3C alkyl, 3-5C cycloalkyl or 4-pyridylmethyl; n : 1-3. Independent claims are also included for: (1) two processes for preparing compounds (I); (2) intermediates of formula (Ia) and (VI). [Image] R 5Me or Et. ACTIVITY : Analgesic; Antimigraine; Antiarthritic; Antiemetic; Neuroleptic; Neuroprotective; Antidepressant; Nootropic; Antiparkinsonian; Hypotensive; Antiarrhythmic; Cardiant; Anticonvulsant; Nephrotropic; Cytostatic; Immunosuppressive; Antipsoriatic; Antiallergic; Antiparasitic; Virucide; Anti-HIV; Antibacterial; Antiinflammatory; Osteopathic; Ophthalmological; Uropathic. MECHANISM OF ACTION : Fatty acid amino hydrolase (FAAH) inhibitor. The most active compounds (unspecified) have IC50 values of 0.005-1 mu M in the FAAH assay described in Life Sciences, 56, 1999 (1995).

20. 发明专利

FR2843964A1 未知
公开(公告)号：FR2843964A1
公开(公告)日：2004-03-05
申请号：FR0210707
申请日：2002-08-29
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , BAS MICHELE , DARGAZANLI GIHAD , HOORNAERT CHRISTIAN , LI ADRIEN TAK , MEDAISKO FLORENCE
IPC分类号： A61K31/335 , A61K31/357 , A61K31/4178 , A61K31/4184 , A61K31/4433 , A61P1/00 , A61P1/12 , A61P9/00 , A61P11/00 , A61P13/02 , A61P13/12 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/08 , C07D319/06 , C07D405/06 , C07D405/12 , C07D413/06 , A61K31/4409
摘要： 1,3-Dioxanylalkylcarbamate derivatives (I) are new. 1,3-Dioxanylalkylcarbamate derivatives of formula (I) and their salts, hydrates and solvates are new. [Image] R 1phenyl or naphthyl optionally substituted with halo, OH, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3, OCF 3, benzyloxy, 3-6C cycloalkoxy or (3-6C)cycloalkyl(1-3C)alkoxy; R 2CHR 3CONHR 4, CH 2CF 3, imidazol-2-ylmethyl, benzimidazol-2-ylmethyl, or phenyl optionally substituted with halo, CN, NO 2, 1-3C alkyl. 1-3C alkoxy, CF 3 or OCF 3; R 3H or Me; R 4H, 1-3C alkyl, 3-5C cycloalkyl or 4-pyridylmethyl; n : 1-3. Independent claims are also included for: (1) two processes for preparing compounds (I); (2) intermediates of formula (Ia) and (VI). [Image] R 5Me or Et. ACTIVITY : Analgesic; Antimigraine; Antiarthritic; Antiemetic; Neuroleptic; Neuroprotective; Antidepressant; Nootropic; Antiparkinsonian; Hypotensive; Antiarrhythmic; Cardiant; Anticonvulsant; Nephrotropic; Cytostatic; Immunosuppressive; Antipsoriatic; Antiallergic; Antiparasitic; Virucide; Anti-HIV; Antibacterial; Antiinflammatory; Osteopathic; Ophthalmological; Uropathic. MECHANISM OF ACTION : Fatty acid amino hydrolase (FAAH) inhibitor. The most active compounds (unspecified) have IC50 values of 0.005-1 mu M in the FAAH assay described in Life Sciences, 56, 1999 (1995).

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