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22. 发明专利

EA007718B1 НОВЫЕ СОЕДИНЕНИЯ ГЕТЕРОЦИКЛИЧЕСКОГО ОКСИМА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ИХ 未知
公开(公告)号：EA007718B1
公开(公告)日：2006-12-29
申请号：EA200400867
申请日：2004-07-27
申请人： SERVIER LAB
发明人： LECLERC VERONIQUE , PAILLOUX SYLVIE , CARATO PASCAL , INTROVIGNE CARINE , LEBERGUE NICOLAS , BERTHELOT PASCAL , DACQUET CARHERINE , BOUTIN JEAN-ALBERT , CAIGNARD DANIEL-HENRI , RENARD PIERRE
IPC分类号： C07D235/26 , C07D277/68 , A61K31/426 , A61K31/427 , A61K31/428 , A61P1/04 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/04 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P35/00 , C07D235/12 , C07D417/06 , C07D417/10 , C07D417/12
摘要： Соединенияформулы (I)вкоторой X представляетсобойатомкислородаилисеры, илигруппуСН, илиR, R, R, R, Rи Rпринимаютзначения, указанныев описании, Апредставляетсобойалкиленовуюцепькаконауказанав описании, Впредставляетсобойалкильнуюгруппуилиалкенильнуюгруппу, замещеннуюгруппойили R, илиВ представляетсобойгруппуили R, D представляетсобойбензольное, пиридиновое, пиразиновое, пиримидиновоеилипиридазиновоеядро. Лекарственныесредства.

24. 发明专利

BRPI0407215A 未知
公开(公告)号：BRPI0407215A
公开(公告)日：2006-01-24
申请号：BRPI0407215
申请日：2004-02-03
申请人： SERVIER LAB
发明人： GALLET SEBASTIEN , BERTHELOT PASCAL , LEBEGUE NICOLAS , FLOUQUET NATHALIE , CARATO PASCAL , HICKMAN JOHN , PIERRE ALAIN , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： A61P35/00 , C07D513/04 , C07D515/04 , A61K31/55
摘要： A compound of formula (I): wherein: represents benzo or pyrido, optionally fused in the 2-3, 3-4 or 4-5 position to a phenyl, (C 4 -C 8 )cycloalkyl or heterocyclic group, which may be optionally substituted, W represents X-Y or Y-X, wherein: X represents and Y represents oxygen or N-R 3 , n represents zero or an integer from 1 to 6, G, R 1 , R 2 and R 3 are as defined in the description, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful for the treatment of cancerous diseases.

25. 发明专利

NO20054092A 未知
公开(公告)号：NO20054092A
公开(公告)日：2005-09-02
申请号：NO20054092
申请日：2005-09-02
申请人： SERVIER LAB
发明人： PIERRE ALAIN , RENARD PIERRE , CARATO PASCAL , PFEIFFER BRUNO , LEBEGUE NICOLAS , BERTHELOT PASCAL , GALLET SEBASTIAN , FLOUQUET NATHALIE , HICKMAN JOHN
IPC分类号： A61P35/00 , C07D513/04 , C07D515/04 , A61K31/55
CPC分类号： C07D513/04 , C07D515/04

26. 发明专利

BRPI0403028A 未知
公开(公告)号：BRPI0403028A
公开(公告)日：2005-06-14
申请号：BRPI0403028
申请日：2004-07-27
申请人： SERVIER LAB
发明人： LECLERC VERONIQUE , PAILLOUX SYLVIE , CARATO PASCAL , INTROVIGNE CARINE , BERTHELOT PASCAL , DACQUET CATHERINE , BOULTIN JEAN ALBERT , CAIGNARD DANIEL HENRI , RENARD PIERRE , LEBEGUE NICOLAS
IPC分类号： C07D235/26 , A61K31/426 , A61K31/427 , A61P1/04 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/04 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P35/00 , C07D235/12 , C07D277/68 , C07D417/10 , C07D417/12 , C07D263/54 , C07D277/62 , A61K31/423 , A61K31/428 , A61P3/00 , A61P5/00
摘要： Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

27. 发明专利

FR2858321A1 未知
公开(公告)号：FR2858321A1
公开(公告)日：2005-02-04
申请号：FR0309214
申请日：2003-07-28
申请人： SERVIER LAB
发明人： LECLERC VERONIQUE , PAILLOUX SYLVIE , CARATO PASCAL , INTROVIGNE CARINE , LEBEGUE NICOLAS , BERTHELOT PASCAL , DACQUET CATHERINE , BOUTIN JEAN ALBERT , CAIGNARD DANIEL HENRI , RENARD PIERRE
IPC分类号： C07D235/26 , A61K31/426 , A61K31/427 , A61P1/04 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/04 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P35/00 , C07D235/12 , C07D277/68 , C07D417/10 , C07D417/12 , A61K31/428
摘要： Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

28. 发明专利

NO20043188L 未知
公开(公告)号：NO20043188L
公开(公告)日：2005-01-31
申请号：NO20043188
申请日：2004-07-27
申请人： SERVIER LAB
发明人： LECLERC VERONIQUE , RENARD PIERRE , CAIGNARD DANIEL-HENRI , CARATO PASCAL , PAILLOUX SYLVIE , INTROVIGNE CARINE , LEBEGUE NICOLAS , BERTHELOT PASCAL , DACQUET CATHRINE , BOUTIN JEAN ALBERT
IPC分类号： C07D235/26 , A61K31/426 , A61K31/427 , A61P1/04 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/04 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P35/00 , C07D235/12 , C07D277/68 , C07D417/10 , C07D417/12 , A61K31/428
摘要： Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

29. 发明专利

MY139278A NEW HETEROCYCLIC OXIME COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：MY139278A
公开(公告)日：2009-09-30
申请号：MYPI20042999
申请日：2004-07-26
申请人： SERVIER LAB
发明人： LECLERC VERONIQUE , RENARD PIERRE , PAILLOUX SYLVIE , CARATO PASCAL , INTROVIGNE CARINE , LEBEGUE NICOLAS , BERTHELOT PASCAL , DACQUET CATHERINE , BOUTIN JEAN ALBERT , CAIGNARD DANIEL-HENRI
IPC分类号： A61K31/428 , C07D235/26 , A61K31/426 , A61K31/427 , A61P1/04 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/04 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P35/00 , C07D235/12 , C07D277/68 , C07D417/10 , C07D417/12
摘要： COMPOUNDS OF FORMULA (I): WHEREIN: X REPRESENTS AN OXYGEN OR SULPHUR ATOM, OR A GROUP CH₂ OR CH, R¹ R² TOGETHER FONN AN OXO OR ARE AS DEFINED IN THE DESCRIPTION,R³, R⁴, R5 ARE HYDROGEN ATOMS, ALKYL GROUPS OR GROUPS AS DEFINED IN THE DESCRIPTION, R6 REPRESENTS AN ALKYL GROUP, AN ARYL GROUP, A CYCLOALKYL GROUP OR A GROUP AS DEFINED IN THE DESCRIPTION, A REPRESENTS AN ALKYLENE CHAIN AS DEFINED IN THE DESCRIPTION, B REPRESENTS AN ALKYL OR ALKENYL GROUP SUBSTITUTED BY A GROUP D REPRESENTS A BENZENE, PYRIDINE, PYRAZINE, PYRIMIDINE OR PYRIDAZINE NUCLEUS,AND THEIR UTILITY IN THE MANUFACTURE OF MEDICAMENTS FOR THE TREATMENT AND/OR PROPHYLAXIS OF HYPERGLYCEMIA AND DYSLIPIDAEMIA. THE FOLLOWING COMPOUND IS PREFERRED.

30. 发明专利

BRPI0607085A2 未知
公开(公告)号：BRPI0607085A2
公开(公告)日：2009-08-04
申请号：BRPI0607085
申请日：2006-01-26
申请人： SERVIER LAB
发明人： HURTEVENT AURELIE , L'HELGOUAL'CH JEAN-MARTIAL , CARATO PASCAL , LEBEGUE NICOLAS , LECLERC VERONIQUE , BERTHELOT PASCAL , DACQUET CATHERINE , CAIGNARD DANIEL HENRI , KTORZA ALAIN
IPC分类号： C07D279/16 , A61K31/538 , A61K31/5415 , A61P3/06 , A61P3/10 , C07D265/36
摘要： Heterocyclic oxime derivatives (I), their enantiomers, diastereomers and their acid or basic addition salts are new. Heterocyclic oxime derivatives of formula (I), their enantiomers, diastereomers and their acid or basic addition salts are new. X : O or S; A : 1-6C alkyl (where CH 2 can be replaced by heteroatom (O or S), NR a or a phenyl or naphthyl group); R aH or 1-6C alkyl; R 1>, R 2>, R, R1 : H, 1-6C ((hetero)aryl)alkyl, 2-6C ((hetero)aryl)alkenyl, 2-6C ((hetero)aryl)alkynyl, (hetero)aryl, 3-8C cycloalkyl-1-6C alkyl or polyhalo-1-6C alkyl; either R 3>, R 4>H, halo, R, OR or NRR1; or -C-R 3>-R 4>-C- : 5-6 membered ring (containing heteroatom (O, S or N); B 1>1-6C alkyl, 2-6C alkenyl (both optionally substituted by -CHR 5>R 6> or R 7>), -CHR 5>R 6> or R 7>; R 5>-C(=Z)-OR, -C(=Z)-NRR1, -N(R)-C(=Z)-R1 or -N(R)-C(=Z)-OR1; Z : O or S; R 6>(hetero)aryl, (hetero)aryl-1-6C alkyl, CN, tetrazole, OR, NRR1, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -N(R)-C(=Z)-R; R 7>CN, tetrazole, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -O-(CH 2) n-C(R 8>R 9>)-COOR; n : 1-6; and R 8>, R 9>H or 1-6C alkyl. Provided that both R 8> and R 9> are not simultaneously H. Provided that: the oxime R 1>-C(=N-OR 2>)- can be the Z or E configuration; the aryl are phenyl, naphthyl or biphenyl, which can be partially hydrogenated; the heteroaryl are 5-10 membered mono or bicylic aromatic, where the bicyclics can partially be hydrogenated, and containing 1-3 heteroatom (O, N or S); the (hetero)aryl are optionally substituted by 1-3 of 1-6C (polyhalo)alkyl, 1-6C alkoxy, OH, carboxy, 1-6C alkoxycarbonyl, 1-6C acyloxy, formyl, 1-6C acyl, aryl, NR bR c, amido, nitro, CN or halo, where R b, R c are H, 1-6C alkyl or (hetero)aryl. Independent claims are included for: (1) the preparations of (I); (2) a composition (X) comprising (I) an antioxidant agent. [Image] ACTIVITY : Antidiabetic; Antilipemic; Analgesic; Antianginal; Cardiant; Vasotropic; Cardiovascular-Gen.; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Osteopathic; Gastrointestinal-Gen.; Antiinflammatory; Antiarteriosclerotic; Anorectic; Anabolic; Eating-Disorders-Gen.; Neuroprotective; Cytostatic; Endocrine-Gen.; Neuroleptic. The antidiabetic and hypolipidemic effect of (I) was tested in female mouse. The results showed that (I) exhibited a very good capacity to reduce the glycemia compared with the effects obtained with Rosiglitazone. MECHANISM OF ACTION : Angiogenesis inhibitor.

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