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31. 发明专利

DK1097145T3 未知
公开(公告)号：DK1097145T3
公开(公告)日：2003-09-15
申请号：DK99929482
申请日：1999-07-13
申请人： AVENTIS PHARMA SA
发明人： BASHIARDES GEORGES , CARRY JEAN-CHRISTOPHE , EVERS MICHEL , FILOCHE BRUNO , MIGNANI SERGE
IPC分类号： A61K31/495 , A61K31/4965 , A61P3/10 , A61P43/00 , C07D241/12
摘要： The invention concerns medicines containing as active principle at least a compound of formula (I):wherein either R2 represents a -CH2-(CHOH)2-CH3 chain and R3 represents a hydrogen atom or R2 represents a hydrogen atom and R3 represents a -CH2-(CHOH)2-CH3 chain or one of its stereoisomers or one of its salts, the novel compounds of formula (I), their stereoisomers, their salts and their preparation.

32. 发明专利

ZA200202073B Quinolyl propyl piperidine derivatives and their use as antibacterial agents. 未知
公开(公告)号：ZA200202073B
公开(公告)日：2003-08-27
申请号：ZA200202073
申请日：2002-03-13
申请人： AVENTIS PHARMA SA
发明人： MALLERON JEAN-LUC , TABART MICHEL , CARRY JEAN-CHRISTOPHE , EVERS MICHEL , AHMAD YOUSSEF EL , MIGNANI SERGE , VIVIANI FABRICE , CHEVE MICHEL
IPC分类号： A61K31/47 , A61K31/4709 , A61P31/00 , A61P31/04 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14 , C07D , A61K , A61P
摘要： 1-Substituted 4-(3-(6-alkoxy-4-quinolinyl)-propyl)-piperidine derivatives (I) are new. Quinolinylpropyl-piperidine derivatives of formula (I), in the form of diastereomers or their mixtures, and their salts are new. [Image] R 1H, halo or OH; R' 1H; or may also be halo if R 1= halo; R 0H; or R 0+ R 1bond, in which case R' 1= H; R 2COOH, CH 2COOH, CH 2CH 2COOH or CH 2OH; R 3(i) 1-6C alkyl substituted by 1-3 groups selected from OH, halo, oxo, COOH, alkoxycarbonyl, alkoxy, alkylthio, Ph', SPh' or Ph'-alkylthio, cycloalkyl, cycloalkylthio, Het and -S-Het; (ii) propargyl substituted by Ph', cycloalkyl or Het; (iii) cinnamyl or (iv) 4-phenylbuten-3-yl; provided that if R 3CH 2OH, then R 3= (i) 1-6C alkyl substituted by SPh', cycloalkylthio or -S-Het; or (ii) propargyl substituted by Ph', cycloalkyl or Het; R 41-6C alkyl, (2-6C) alkenyl-CH 2O- or (2-6C) alkynyl-CH 2O-; Ph' : phenyl (optionally substituted by 1-3 of halo, OH, alkyl, alkoxy, CF 3, OCF 3, COOH, alkoxycarbonyl, CN or NH 2); Het : 5- or 6-membered aromatic heterocycle containing 1-4 of N, O and S as heteroatom(s) (optionally substituted by 1-3 of halo, OH, alkyl, alkoxy, CF 3, OCF 3, oxo, COOH, alkoxycarbonyl, CN or NH 2); unless specified otherwise alkyl moieties have 1-3C and cycloalkyl moieties 3-7C. An independent claim is included for the preparation for (I). ACTIVITY : Antibacterial. (I) are effective in vitro against methicillin-resistant Staphylococcus aureusAS5155 at 0.03-4 Microg/ml, Streptococcus pneumoniaeIP53146 at 0.12-8 Microg/ml, Enterococcus faeciumat 0.5-64 Microg/ml and Moxarella catharrhalisIPA152 at 0.25-32 Microg/ml; and in vivo against Staphylococcus aureusIP8203 in mice at 10-150 mg/kg s.c. (CD 50) or (in some cases) 20-150 mg/kg p.o. (No specific results for individual compounds are given). MECHANISM OF ACTION : None given.

33. 发明专利

NO20033131A 未知
公开(公告)号：NO20033131A
公开(公告)日：2003-08-27
申请号：NO20033131
申请日：2003-07-08
申请人： AVENTIS PHARMA SA
发明人： BACQUE ERIC , BIGOT ANTONY , CARRY JEAN-CHRISTOPHE , MIGNANI SERGE , RONAN BAPTISTE , TABART MICHEL
IPC分类号： A61K31/4439 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D213/40 , C07D213/55 , C07D213/64 , C07D213/89 , C07D417/06 , C07F7/18
CPC分类号： C07D213/40 , C07D213/55 , C07D213/64 , C07D213/89 , C07D417/06 , C07F7/1856

34. 发明专利

NO20033129L 未知
公开(公告)号：NO20033129L
公开(公告)日：2003-08-27
申请号：NO20033129
申请日：2003-07-08
申请人： AVENTIS PHARMA SA
发明人： BIGOT ANTONY , CARRY JEAN-CHRISTOPHE , MIGNANI SERGE
IPC分类号： C07D295/12 , A61K31/497 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D277/18 , C07D295/13 , C07D295/15 , C07D413/02 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH 2 ) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO 2 , CH 2 or CHPh; or Y is a carbonyl (C-O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.

35. 发明专利

NO20032187L 未知
公开(公告)号：NO20032187L
公开(公告)日：2003-06-26
申请号：NO20032187
申请日：2003-05-14
申请人： AVENTIS PHARMA SA
发明人： BACQUE ERIC , CARRY JEAN-CHRISTOPHE , EL-AHMAD YOUSSEF , EVERS MICHEL , HUBERT PHILIPPE , MALLERON JEAN-LUC , MIGNANI SERGE , PANTEL GUY , TABART MICHEL , VIVIANI FABRICE
IPC分类号： A61K31/4709 , A61P31/00 , A61P31/04 , C07D215/20 , C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14 , A61K31/47
摘要： 1,4-Disubstituted 4-(quinolin-4-yl-alkyl)-piperidine derivatives (I) are new. Piperidine derivatives of formula (I), their enantiomers, diastereomers and mixtures, syn- or anti-isomers and salts, are new. [Image] X 1- X 5CR or N, provided that only one may be N; R, R 1H, halo, alkyl, cycloalkyl, Ph, SPh, Het, -S-Het, OH, alkoxy, OCF 3, alkylthio, SCF 3, cycloalkoxy, cycloalkylthio, CN, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NR aR b, CONR aR b, CH 2T, OPh, heterocyclyloxy, benzyloxy or heterocyclylmethoxy; or R 1may also be 1-6C perfluoroalkyl, 1-6C perfluoroalkoxy or 1-6C perfluoroalkylthio; or R in the X 5position may also be COCF 3; Het : mono- or bicyclic aromatic heterocyclyl; R a, R bH, alkyl, cycloalkyl, phenyl or Het; or NR aR b5- or 6-membered heterocyclyl, optionally containing another O, S, SO, SO 2or NQ heteroatom; Q : H, Ph or Het; T : F, OH, alkoxy, alkylthio, cycloalkoxy, cycloalkylthio, Het, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NR aR bor CONR aR b; R 2COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CN, COOH, SO 3H, CONR' aR' b, CH 2OH, -U-V, CF 2R c, CMe 2-R c, COR c, CH(OH)R c, -C(cycloalkyl)-R cor -CH=CH-R c; R' a, R' bas R a, R b, except that one of R' a, R' bmay also be OH, alkoxy or cycloalkoxy; or NR' aR' bheterocycle as defined for NR aR b; U : 1-2C alkylene; V : COOH, alkoxycarbonyl, cycloalkoxycarbonyl, CN, SO 3H or CONR' aR' b; R cCOOH, alkoxycarbonyl, cycloalkoxycarbonyl or CONR' aR' b; R 3Ph, Het or alkyl (optionally substituted by R' 3); R' 3halo, OH, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, mono- or dialkylamino, cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylsulfinyl, cycloalkylsulfonyl, mono- or dicycloalkylamino, N-alkyl-N-cycloalkylamino, acyl, cycloalkylcarbonyl, Ph, OPh, SPh, SOPh, SO 2Ph, NHPh, NPh 2, N-alkyl-N-phenylamino, N-cycloalkyl-N-phenylamino, phenylalkoxy, phenylalkylthio, phenylalkylsulfinyl, phenylalkylsulfonyl, phenylalkylamino, N-alkyl-N-phenylalkylamino, N-cycloalkyl-N-phenylalkylamino, benzoyl, -O-Het, -S-Het, -SO-Het, -SO 2-Het, -NH-Het, N-alkyl-N-(Het)-amino, N-cycloalkyl-N-(Het)-amino, -CO-Het, Het-alkoxy, Het-alkylthio, Het-alkylsulfinyl, Het-alkylsulfonyl, Het-alkylamino, N-alkyl-N-(Het-alkyl)-amino, N-cycloalkyl-N-(Het-alkyl)-amino, COOH, alkoxycarbonyl, NR' aR' b, CONR' aR' b, -C(R'' b)=C(R' c)-R'' a, -CC-R d, -CF 2-phenyl or -CF 2-Het; R'' aPh, phenylalkyl, Het, Het-alkyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl, phenylsulfonylalkyl, phenylaminoalkyl, N-alkyl-N-phenylaminoalkyl, Het-O-alkyl, Het-S-alkyl, Het-SO-alkyl, Het-SO 2-alkyl, Het-NH-alkyl, N-alkyl-N-(Het)-amino, -S-Het, -SO-Het, -SO 2-Het, SPh, SOPh or SO 2Ph; R'' b, R' cH, alkyl or cycloalkyl; R dalkyl, Ph, phenylalkyl, phenoxyalkyl, phenylthioalkyl, N-alkyl-N-phenylaminoalkyl, Het, Het-alkyl, Het-O-alkyl, Het-S-alkyl, Het-NH-alkyl or N-alkyl-N-(Het)-aminoalkyl; Y : -CH(R e)-, CF 2, CO C(=NOH), alkoxyiminomethylene, cycloalkoxyiminomethylene or 3-6C cycloalkylidene; R eH, F, OH, alkoxy, cycloalkoxy, COOH, alkoxycarbonyl, cycloalkoxycarbonyl, NQ aQ bor CONQ aQ b; Q a, Q bas R' a, R' b; or one is H and the other is alkoxycarbonyl, acyl, cycloalkoxycarbonyl, -CO-Ph or -CO-Het; and n : 0-4; phenyl and heterocyclyl moieties are optionally substituted by 1-4 of halo, OH, alkyl, alkoxy, alkoxyalkyl, haloalkyl, CF 3, OCF 3SCF 3, COOH, alkoxycarbony, CN, alkylamino, NR' aR' b, Ph, hydroxyalkyl, alkylthioalkyl, alkylsulfonylalkyl or alkylsulfonylalkyl; alkyl or acyl moieties have 1-10C (unless specified otherwise); cycloalkyl moieties have 3-6C. An independent claim is included for the preparation of (I). ACTIVITY : Antibacterial. (I) show activity in vitro against methicillin-resistant Staphylococcus aureusAS5155 at 0.03-4 Microg/ml, Streptococcus pneumoniae6254-01 at 0.03-8 Microg/ml and Moraxella catarrhalisIPA 152 at 0.12-64 Microg/ml, and in vivo against Staphylococcus aureusIP8203 infections in mice at 18-150 mg/ml s.c. (DC 50). No specific results for individual compounds are given in the source material. MECHANISM OF ACTION : None given.

36. 发明专利

SK3632002A3 Piperidine quinolyl propyl derivatives, preparation method and compositions containing same 未知
公开(公告)号：SK3632002A3
公开(公告)日：2003-04-01
申请号：SK3632002
申请日：2000-09-14
申请人： AVENTIS PHARMA SA
发明人： MALLERON JEAN-LUC , TABART MICHEL , CARRY JEAN-CHRISTOPHE , EVERS MICHEL , EL AHMAD YOUSSEF , MIGNANI SERGE , VIVIANI FABRICE , CHEVE MICHEL
IPC分类号： A61K31/47 , A61K31/4709 , A61P31/00 , A61P31/04 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： 1-Substituted 4-(3-(6-alkoxy-4-quinolinyl)-propyl)-piperidine derivatives (I) are new. Quinolinylpropyl-piperidine derivatives of formula (I), in the form of diastereomers or their mixtures, and their salts are new. [Image] R 1H, halo or OH; R' 1H; or may also be halo if R 1= halo; R 0H; or R 0+ R 1bond, in which case R' 1= H; R 2COOH, CH 2COOH, CH 2CH 2COOH or CH 2OH; R 3(i) 1-6C alkyl substituted by 1-3 groups selected from OH, halo, oxo, COOH, alkoxycarbonyl, alkoxy, alkylthio, Ph', SPh' or Ph'-alkylthio, cycloalkyl, cycloalkylthio, Het and -S-Het; (ii) propargyl substituted by Ph', cycloalkyl or Het; (iii) cinnamyl or (iv) 4-phenylbuten-3-yl; provided that if R 3CH 2OH, then R 3= (i) 1-6C alkyl substituted by SPh', cycloalkylthio or -S-Het; or (ii) propargyl substituted by Ph', cycloalkyl or Het; R 41-6C alkyl, (2-6C) alkenyl-CH 2O- or (2-6C) alkynyl-CH 2O-; Ph' : phenyl (optionally substituted by 1-3 of halo, OH, alkyl, alkoxy, CF 3, OCF 3, COOH, alkoxycarbonyl, CN or NH 2); Het : 5- or 6-membered aromatic heterocycle containing 1-4 of N, O and S as heteroatom(s) (optionally substituted by 1-3 of halo, OH, alkyl, alkoxy, CF 3, OCF 3, oxo, COOH, alkoxycarbonyl, CN or NH 2); unless specified otherwise alkyl moieties have 1-3C and cycloalkyl moieties 3-7C. An independent claim is included for the preparation for (I). ACTIVITY : Antibacterial. (I) are effective in vitro against methicillin-resistant Staphylococcus aureusAS5155 at 0.03-4 Microg/ml, Streptococcus pneumoniaeIP53146 at 0.12-8 Microg/ml, Enterococcus faeciumat 0.5-64 Microg/ml and Moxarella catharrhalisIPA152 at 0.25-32 Microg/ml; and in vivo against Staphylococcus aureusIP8203 in mice at 10-150 mg/kg s.c. (CD 50) or (in some cases) 20-150 mg/kg p.o. (No specific results for individual compounds are given). MECHANISM OF ACTION : None given.

37. 发明专利

NO20025885L 未知
公开(公告)号：NO20025885L
公开(公告)日：2003-01-29
申请号：NO20025885
申请日：2002-12-06
申请人： AVENTIS PHARMA SA
发明人： CARRY JEAN-CHRISTOPHE , DAMOUR DOMINIQUE , GUYON CLAUDE , MIGNANI SERGE , BACQUE ERIC , BIGOT ANTONY
IPC分类号： A61K31/426 , A61P1/04 , A61P3/10 , A61P9/04 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P31/04 , A61P35/00 , A61P39/02 , A61P43/00 , C07D277/18 , A61K31/427 , A61P1/00 , A61P29/00
摘要： The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (I) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (I) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved abnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2).

38. 发明专利

NO20025884L 未知
公开(公告)号：NO20025884L
公开(公告)日：2003-01-29
申请号：NO20025884
申请日：2002-12-06
申请人： AVENTIS PHARMA SA
发明人： CARRY JEAN-CHRISTOPHE , DAMOUR DOMINIQUE , GUYON CLAUDE , MIGNANI SERGE , BIGOT ANTONY , BACQUE ERIC , TABART MICHEL
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/444 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P35/00 , C07C335/08 , C07D277/18 , C07D277/28 , C07D417/06 , C07D417/12
摘要： The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, -CH-R3, -CH2-S-R4 or phenyl radical substituted by a nitro or NH-C(=NH)CH3 radical; or R1 is an alkyl radical and R2 is a hydrogen atom; R3 is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R4 represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.

39. 发明专利

AP2002002708A0 2-Aminothiazoline derivatives and their use as no-synthase inhibitors. 未知
公开(公告)号：AP2002002708A0
公开(公告)日：2002-12-31
申请号：AP2002002708
申请日：2001-06-07
申请人： AVENTIS PHARMA SA
发明人： CARRY JEAN-CHRISTOPHE , DAMOUR DOMINIQUE , GUYON CLAUDE , MIGNANI SERGE , BIGOT ANTHONY , BACQUE ERIC , TABART MICHAEL
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/444 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P35/00 , C07C335/08 , C07D277/18 , C07D277/28 , C07D417/06 , C07D417/12
摘要： The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, -CH-R3, -CH2-S-R4 or phenyl radical substituted by a nitro or NH-C(=NH)CH3 radical; or R1 is an alkyl radical and R2 is a hydrogen atom; R3 is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R4 represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.

40. 发明专利

AP2002002707A0 4, 5-Dihydro-Thiazo-2-Ylamine Derivatives and their Use as NO-Synthase Inhibitors. 未知
公开(公告)号：AP2002002707A0
公开(公告)日：2002-12-31
申请号：AP2002002707
申请日：2001-06-07
申请人： AVENTIS PHARMA SA
发明人： DAMOUR DOMINIQUE , GUYON CLAUDE , MIGNANI SERGE , BIGOT ANTHONY , BACQUE ERIC , CARRY JEAN-CHRISTOPHE
IPC分类号： A61K31/426 , A61P1/04 , A61P3/10 , A61P9/04 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P31/04 , A61P35/00 , A61P39/02 , A61P43/00 , C07D277/18
摘要： The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (1) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (1) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved arbnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2)

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