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1. 发明专利

AT252577T 未知
公开(公告)号：AT252577T
公开(公告)日：2003-11-15
申请号：AT98924365
申请日：1998-05-04
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , JEUNESSE JEAN , NEDELEC ALAIN
IPC分类号： A61K31/4245 , A61K31/454 , A61P1/00 , A61P13/00 , A61P25/00 , A61P43/00 , C07D413/04 , C07D413/14 , A61K31/41 , A61K31/445
摘要： Compounds corresponding to the general formula (I)in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula -OCH2O-, -O(CH2)2-, -O(CH2)3-, -O(CH2)2O- or -O(CH2)3O-, X2 represents hydrogen, an amino group or a group of general formula -NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.

2. 发明专利

AT249460T 未知
公开(公告)号：AT249460T
公开(公告)日：2003-09-15
申请号：AT99973291
申请日：1999-12-01
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , NEDELEC ALAIN , GALLI FREDERIC , JEUNESSE JEAN , EVEN LUC
IPC分类号： A61K31/551 , A61P1/00 , A61P3/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , C07D471/08 , C07D221/00 , C07D243/00

3. 发明专利

FR2866885A1 New 1-alkyl-piperidine-4-carbamate derivatives and analogs, are fatty acid amidohydrolase inhibitors useful e.g. for treating pain, cancer or neurodegenerative, cardiovascular, inflammatory or allergic disease 未知
公开(公告)号：FR2866885A1
公开(公告)日：2005-09-02
申请号：FR0401952
申请日：2004-02-26
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , ALMARIO GARCIA ANTONIO , HOORNAERT CHRISTIAN , JEUNESSE JEAN
IPC分类号： C07D205/04 , C07D207/09 , C07D211/26 , C07D211/34 , C07D211/58 , A61K31/4468 , A61P25/00 , A61P31/00 , A61P35/00
摘要： Carbamoylalkyl 1-((hetero)aryl-substituted alkyl)-azetidine, pyrrolidine, piperidine or homopiperidine-carbamates (I) are new. Azetidine, pyrrolidine, piperidine or homopiperidine derivatives of formula (I) and their acid addition salts, hydrates and solvates are new. m : 1-4; n : 1-3; o : 1 or 2; A : one or more of X, Y and/or Z; X : CH 2 (optionally substituted (os) by 1 or 2 of alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl); Y : 2C alkenylene (os by 1 or 2 of alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl) or 2C alkynylene; Z : 3-7C cycloalkylidene or 3-7C cycloalkylene; B : direct bond or 1-6C alkylene; G : direct bond, O, S, CH(OH), CO, SO or SO 2; R 1R 4 (os by one or more groups R 5 and/or R 6); R 4furanyl, pyrrolyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, thiadiazolyl, isothiadiazolyl, oxadiazolyl, triazolyl, tetrazolyl, phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, naphthalenyl, quinolinyl, tetrahydroquinolinyl, isoquinolinyl, tetrahydro-isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl, naphthyridinyl, imidazopyrimidinyl, thienopyrimidinyl, benzofuranyl, dihydrobenzofuranyl, benzothienyl, dihydrobenzothienyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, indolyl, isoindolyl, indazolyl, pyrrolopyridinyl, furopyridinyl, dihydrofuropyridinyl, thienopyridinyl, dihydrothienopyridinyl, imidazopyridinyl, pyrazolopyrimidinyl, pyrazolopyridinyl, oxazolopyridinyl, isoxazolopyridinyl or thiazolopyridinyl; R 5halo, CN, NO 2, alkyl, alkoxy, OH, alkylthio, fluoroalkyl, fluoroalkoxy, fluoroalkylthio, NR 7R 8, NR 7COR 8, NR 7COOR 8, NR 7SO 2R 8, COR 7, COOR 7, CONR 7R 8, SO 2R 7, SO 2NR 7R 8 or 1-3C alkylenedioxy; R 6phenyl, phenoxy, benzyloxy, naphthalenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl (all os by one or more groups R 5); R 7, R 8H or alkyl; or NR 7R 8azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, azepino or piperazino (all os by alkyl or benzyl); R 2H or alkyl; R 3H, alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl; alkyl moieties have 1-6C and cycloalkylene moieties 3-7C unless specified otherwise. Independent claims are included for: (A) the preparation of (I); and (B) oxazolidinedione and carbamate-amide derivative intermediates of formulae (IIa) and (Ia) as new compounds, provided that 3-(1-(phenylmethyl)-4-piperidinyl)-2,4-oxazolidinedione is excluded as (IIa). [Image] ACTIVITY : Analgesic; antimigraine; auditory; antiemetic; anorectic; immunomodulator; neuroleptic; relaxant; tranquilizer; antidepressant; neuroprotective; antiparkinsonian; nootropic; anticonvulsant; cerebroprotective; nephrotropic; cardiant; hypotensive; antiarrythmic; antiarteriosclerotic; vasotropic; cytostatic; immunosuppressive; antipsoriatic; dermatological; antianemic; antiallergic; antiparasitic; virucide; antibacterial; anti-HIV; antiinflammatory; antiarthritic; antirheumatic; osteopathic; antigout; ophthalmological; antitussive; antiasthmatic; antiulcer; antidiarrheic; uropathic. In phenylbenzoquinone-induced writhing tests for analgesic activity in mice, the most active compounds (I) (not specified) inhibited writhing by 35-70% at doses of 1-30 mg/kg p.o. or i.p. MECHANISM OF ACTION : Fatty acid amidohydrolase (FAAH) inhibitor. 2-(Methylamino)-2-oxoethyl ((1-(2-((2,4-dichlorophenyl)-oxy)-ethyl)-piperidin-4-yl)-methyl)-carbamate hydrochloride (I') had IC 50 49 nM for inhibition of FAAH.

4. 发明专利

FR2854633B1 未知
公开(公告)号：FR2854633B1
公开(公告)日：2005-06-24
申请号：FR0305540
申请日：2003-05-07
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , BURNIER PHILIPPE , HOORNAERT CHRISTIAN , JEUNESSE JEAN , PUECH FREDERIC
IPC分类号： A61K31/435 , A61K31/436 , A61K31/44 , A61K31/495 , A61K31/506 , A61P9/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D211/26 , C07D213/38 , C07D295/12 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D403/14 , C07D403/04 , C07D241/04 , A61K31/4365 , A61K31/4355 , A61K31/4409
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3═CHR4CONHR5; R4═H or C1-6-alkyl; R5═H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.

5. 发明专利

FR2854633A1 未知
公开(公告)号：FR2854633A1
公开(公告)日：2004-11-12
申请号：FR0305540
申请日：2003-05-07
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , BURNIER PHILIPPE , HOORNAERT CHRISTIAN , JEUNESSE JEAN , PUECH FREDERIC
IPC分类号： A61K31/435 , A61K31/436 , A61K31/44 , A61K31/495 , A61K31/506 , A61P9/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D211/26 , C07D213/38 , C07D295/12 , C07D295/13 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D403/14 , C07D403/04 , C07D241/04 , A61K31/4365 , A61K31/4355 , A61K31/4409
摘要： Compound corresponding to the general formula (I): in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3═CHR4CONHR5; R4═H or C1-6-alkyl; R5═H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.

6. 发明专利

DE69911241D1 未知
公开(公告)号：DE69911241D1
公开(公告)日：2003-10-16
申请号：DE69911241
申请日：1999-12-01
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , NEDELEC ALAIN , GALLI FREDERIC , JEUNESSE JEAN , EVEN LUC
IPC分类号： A61K31/551 , A61P1/00 , A61P3/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , C07D471/08

7. 发明专利

FR2866885B1 未知
公开(公告)号：FR2866885B1
公开(公告)日：2007-08-31
申请号：FR0401952
申请日：2004-02-26
申请人： SANOFI SYNTHELABO
发明人： ABOUABDELLAH AHMED , ALMARIO GARCIA ANTONIO , HOORNAERT CHRISTIAN , JEUNESSE JEAN
IPC分类号： C07D211/34 , A61K31/4468 , A61P25/00 , A61P31/00 , A61P35/00 , C07D205/04 , C07D207/09 , C07D211/26 , C07D211/58
摘要： Carbamoylalkyl 1-((hetero)aryl-substituted alkyl)-azetidine, pyrrolidine, piperidine or homopiperidine-carbamates (I) are new. Azetidine, pyrrolidine, piperidine or homopiperidine derivatives of formula (I) and their acid addition salts, hydrates and solvates are new. m : 1-4; n : 1-3; o : 1 or 2; A : one or more of X, Y and/or Z; X : CH 2 (optionally substituted (os) by 1 or 2 of alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl); Y : 2C alkenylene (os by 1 or 2 of alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl) or 2C alkynylene; Z : 3-7C cycloalkylidene or 3-7C cycloalkylene; B : direct bond or 1-6C alkylene; G : direct bond, O, S, CH(OH), CO, SO or SO 2; R 1R 4 (os by one or more groups R 5 and/or R 6); R 4furanyl, pyrrolyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, thiadiazolyl, isothiadiazolyl, oxadiazolyl, triazolyl, tetrazolyl, phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, naphthalenyl, quinolinyl, tetrahydroquinolinyl, isoquinolinyl, tetrahydro-isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl, naphthyridinyl, imidazopyrimidinyl, thienopyrimidinyl, benzofuranyl, dihydrobenzofuranyl, benzothienyl, dihydrobenzothienyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, indolyl, isoindolyl, indazolyl, pyrrolopyridinyl, furopyridinyl, dihydrofuropyridinyl, thienopyridinyl, dihydrothienopyridinyl, imidazopyridinyl, pyrazolopyrimidinyl, pyrazolopyridinyl, oxazolopyridinyl, isoxazolopyridinyl or thiazolopyridinyl; R 5halo, CN, NO 2, alkyl, alkoxy, OH, alkylthio, fluoroalkyl, fluoroalkoxy, fluoroalkylthio, NR 7R 8, NR 7COR 8, NR 7COOR 8, NR 7SO 2R 8, COR 7, COOR 7, CONR 7R 8, SO 2R 7, SO 2NR 7R 8 or 1-3C alkylenedioxy; R 6phenyl, phenoxy, benzyloxy, naphthalenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl (all os by one or more groups R 5); R 7, R 8H or alkyl; or NR 7R 8azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, azepino or piperazino (all os by alkyl or benzyl); R 2H or alkyl; R 3H, alkyl, cycloalkyl or cycloalkyl-(1-3C) alkyl; alkyl moieties have 1-6C and cycloalkylene moieties 3-7C unless specified otherwise. Independent claims are included for: (A) the preparation of (I); and (B) oxazolidinedione and carbamate-amide derivative intermediates of formulae (IIa) and (Ia) as new compounds, provided that 3-(1-(phenylmethyl)-4-piperidinyl)-2,4-oxazolidinedione is excluded as (IIa). [Image] ACTIVITY : Analgesic; antimigraine; auditory; antiemetic; anorectic; immunomodulator; neuroleptic; relaxant; tranquilizer; antidepressant; neuroprotective; antiparkinsonian; nootropic; anticonvulsant; cerebroprotective; nephrotropic; cardiant; hypotensive; antiarrythmic; antiarteriosclerotic; vasotropic; cytostatic; immunosuppressive; antipsoriatic; dermatological; antianemic; antiallergic; antiparasitic; virucide; antibacterial; anti-HIV; antiinflammatory; antiarthritic; antirheumatic; osteopathic; antigout; ophthalmological; antitussive; antiasthmatic; antiulcer; antidiarrheic; uropathic. In phenylbenzoquinone-induced writhing tests for analgesic activity in mice, the most active compounds (I) (not specified) inhibited writhing by 35-70% at doses of 1-30 mg/kg p.o. or i.p. MECHANISM OF ACTION : Fatty acid amidohydrolase (FAAH) inhibitor. 2-(Methylamino)-2-oxoethyl ((1-(2-((2,4-dichlorophenyl)-oxy)-ethyl)-piperidin-4-yl)-methyl)-carbamate hydrochloride (I') had IC 50 49 nM for inhibition of FAAH.

8. 发明专利

DE69819147T2 未知
公开(公告)号：DE69819147T2
公开(公告)日：2004-07-29
申请号：DE69819147
申请日：1998-05-04
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , JEUNESSE JEAN , NEDELEC ALAIN
IPC分类号： A61K31/4245 , A61K31/454 , A61P1/00 , A61P13/00 , A61P25/00 , A61P43/00 , C07D413/04 , C07D413/14 , A61K31/41 , A61K31/445
摘要： Compounds corresponding to the general formula (I)in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula -OCH2O-, -O(CH2)2-, -O(CH2)3-, -O(CH2)2O- or -O(CH2)3O-, X2 represents hydrogen, an amino group or a group of general formula -NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.

9. 发明专利

DE69819147D1 未知
公开(公告)号：DE69819147D1
公开(公告)日：2003-11-27
申请号：DE69819147
申请日：1998-05-04
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , JEUNESSE JEAN , NEDELEC ALAIN
IPC分类号： A61K31/4245 , A61K31/454 , A61P1/00 , A61P13/00 , A61P25/00 , A61P43/00 , C07D413/04 , C07D413/14 , A61K31/41 , A61K31/445
摘要： Compounds corresponding to the general formula (I)in which R1 represents hydrogen or an alkyl or cycloalkylmethyl group, X1 represents hydrogen or a halogen or an alkoxy group, or alternatively OR1 and X1 together represent a group of formula -OCH2O-, -O(CH2)2-, -O(CH2)3-, -O(CH2)2O- or -O(CH2)3O-, X2 represents hydrogen, an amino group or a group of general formula -NHCO2R in which R represents an alkyl or phenylalkyl group, X3 represents hydrogen or a halogen, and R2 represents hydrogen or an alkyl, phenylalkyl or [(4-dimethylamino)piperid-1-ylcarbonyl]alkyl group. Therapeutic application.

10. 发明专利

AU1392900A 2,5-diazabicyclo(2.2.1)heptane derivatives, their preparation and therapeutic uses 未知
公开(公告)号：AU1392900A
公开(公告)日：2000-06-26
申请号：AU1392900
申请日：1999-12-01
申请人： SANOFI SYNTHELABO
发明人： LOCHEAD ALISTAIR , JEGHAM SAMIR , NEDELEC ALAIN , JEUNESSE JEAN , GALLI FREDERIC , EVEN LUC
IPC分类号： A61K31/444 , A61K31/501 , A61P1/00 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D487/08 , A61K31/44
摘要： The invention relates to 2,5-diazabicyclo[2.2.1]heptane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.

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