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81. 发明专利

NO20033131L 未知
公开(公告)号：NO20033131L
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
摘要： The present invention relates to the use of 2-amino-4-pyridylmethyl thiazoline derivatives of formula (I) wherein either R1=R2=Cl or (C1-C4)alkyl, or hydroxy; or (C1-C4)alkoxy or at least one of R1 or R2 is a hydrogen and the other is a (C1-C4)alkyl, hydroxy, (C1-C4)alkoxy or chlorine or pharmaceutically acceptable salts thereof as inhibitors of inducible NO-synthase.

82. 发明专利

NO20033130A 未知
公开(公告)号：NO20033130A
公开(公告)日：2003-08-27
申请号：NO20033130
申请日：2003-07-08
申请人： AVENTIS PHARMA SA
发明人： BACQUE ERIC , BIGOT ANTONY , CARRY JEAN-CHRISTOPHE , MIGNANI SERGE
IPC分类号： A61K31/427 , A61K31/4439 , A61P25/16 , C07D239/26 , C07D277/28 , C07D333/20 , C07D413/06 , C07D417/06
CPC分类号： C07D239/26 , C07D277/28 , C07D333/20 , C07D413/06 , C07D417/06

83. 发明专利

AT243683T 未知
公开(公告)号：AT243683T
公开(公告)日：2003-07-15
申请号：AT98939677
申请日：1998-07-15
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 , A61K31/497 , A61P3/10 , C07D241/12 , C07D405/14
摘要： Disclosed are polyhydroxybutylpyrazines of the general formulaIncluding their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.

84. 发明专利

NO20033130D0 未知
公开(公告)号：NO20033130D0
公开(公告)日：2003-07-08
申请号：NO20033130
申请日：2003-07-08
申请人： AVENTIS PHARMA SA
发明人： BACQUE ERIC , BIGOT ANTONY , CARRY JEAN-CHRISTOPHE , MIGNANI SERGE
IPC分类号： A61K31/427 , A61K31/4439 , A61P25/16 , C07D239/26 , C07D277/28 , C07D333/20 , C07D413/06 , C07D417/06 , C07D
摘要： The present invention relates to the use of 2-amino-4-heteroarylethyl-thiazoline derivatives of formula (I)in which Het represents a thienyl, pyrimidyl, pyridyl or thiazolyl radical or pharmaceutically acceptable salts thereof as inhibitors of inducible NO-synthase.

85. 发明专利

DE69908367D1 未知
公开(公告)号：DE69908367D1
公开(公告)日：2003-07-03
申请号：DE69908367
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.

86. 发明专利

CA2465877A1 DERIVES DE 2-AMINO-4-PYRIDYLMETHYL-THIAZOLINE ET LEUR UTILISATION COMME INHIBITEURS DE NO-SYNTHASE INDUCTIBLE 未知
公开(公告)号：CA2465877A1
公开(公告)日：2003-05-15
申请号：CA2465877
申请日：2002-11-07
申请人： AVENTIS PHARMA SA
发明人： BACQUE ERIC , BIGOT ANTONY , TABART MICHEL , RONAN BAPTISTE , CARRY JEAN-CHRISTOPHE , MIGNANI SERGE
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
摘要： La présente invention concerne l'utilisation de dérivés 2-amino-4- pyridylméthyl thiazoline de formule (I) dans laquelle soit R1 = R2 = Cl, ou alkyle(C1-C4), ou hydroxy ; ou alcoxy (C1-C4)soit au moins un des deux R1, R 2 est hydrogène et l'autre est un radical alkyle (C1-C4), un hydroxy, un alcox y (C1-C4) ou un chlore ou leurs sels pharmaceutiquement acceptables comme inhibiteurs de NO-synthase inductible.

87. 发明专利

BR0111986A 未知
公开(公告)号：BR0111986A
公开(公告)日：2003-04-01
申请号：BR0111986
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 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 , A61K31/497 , C07D213/38 , C07D213/40 , C07D333/20 , C07D241/12 , C07D213/70 , C07D213/89 , C07C335/06 , C07C215/00 , C07C229/00 , C07C233/00 , C07C271/00 , C07C333/00
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.

88. 发明专利

PT948527E 未知
公开(公告)号：PT948527E
公开(公告)日：2002-11-29
申请号：PT97952998
申请日：1997-12-23
申请人： AVENTIS PHARMA SA
发明人： BARRIERE JEAN-CLAUDE , MIGNANI SERGE , LECONTE JEAN-PIERRE , BASHIARDES GEORGES , CARRY JEAN-CHRISTOPHE , EVERS MICHEL , FILOCHE BRUNO
IPC分类号： A61K38/00 , A61P31/14 , C07K7/64 , A61K38/13
摘要： A cyclosporin compound of the formula (I): wherein Alk and R are as defined herein, or a pharmaceutically acceptable salt thereof, which derivatives are is useful in the treatment and/or prophylaxis of retrovirus infections.

89. 发明专利

CZ290896B6 Polyhydroxybutyl pyrazines, process of their preparation and medicaments containing thereof 未知
公开(公告)号：CZ290896B6
公开(公告)日：2002-11-13
申请号：CZ2000121
申请日：1998-07-15
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 , A61K31/497 , A61P3/10 , C07D241/12 , C07D405/14
摘要： In the present invention there are disclosed medicaments containing as an active component at least one compound of the general formula I, wherein either (A) Ri9 and Ri10 are the same and each represents {-CHi2OH} and either Ri3 represents methylene, Ri4 represents {-CHOH-} and one of Ri1, Ri2, Ri5 and Ri6 represents carbonyl, methylene, {-CHF-}, {-CH(NHRi7)-} , or {-CH(ORi8)-} and the others represent the group {-CHOH-}, or Ri2 and Ri5 represent {-CHOH-}, Ri3 represents methylene and Ri1, Ri4 and Ri6 are the same and each represents carbonyl, methylene, {-CHF-}, {-CH(NHRi7)-} or {-CH(ORi8)-} , or Ri1 and Ri6 are {-CHOH-}, Ri3 represents methylene and Ri2, Ri4 and Ri5 are the same and each represents carbonyl, methylene, {-CHF-}, {-CH(NHRi7)-} or {-CH(ORi8)-}, or Ri1, Ri4, Ri5 and Ri6 represent each {-CHOH-}, and -Ri2-Ri3- are {-CH=CH-}, or (B) Ri1, Ri2, Ri4, Ri5 and Ri6 are {-CHOH-}, Ri3 represents methylene, Ri9 represents {-CHi2F} or {-CHi2OH}, Ri10 represents {-CHi2F} or {-CHi2OH}, with the proviso that Ri9 and Ri10 are not both {-CHi2OH}, or stereoisomers thereof or salts of these compounds, further novel compounds of the general formula I as well as a process for their preparation.

90. 发明专利

CZ2002940A3 Quinolylpropyl piperidine derivatives, process of their preparation and their use 未知
公开(公告)号：CZ2002940A3
公开(公告)日：2002-07-17
申请号：CZ2002940
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.

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