公开(公告)号：US6124330A

公开(公告)日：2000-09-26

申请号：US214080

申请日：1999-04-29

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： C07D473/34 ,  A61K31/00 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/498 ,  A61K31/50 ,  A61K31/501 ,  A61K31/502 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/529 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P17/00 ,  A61P17/06 ,  A61P35/00 ,  A61P43/00 ,  C07D277/22 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04 ,  C07D521/00 ,  A61K31/426 ,  C07D277/60 ,  C07D417/10

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： PCT No.PCT / EP97 / 03248 Sec。 371日期1999年4月29日第 102（e）1999年4月29日PCT 1997年6月19日PCT公布。 公开号WO97 / 49704 PCT 日期1997年12月31日本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐及其立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US07205312B2

公开(公告)日：2007-04-17

申请号：US10979362

申请日：2004-11-02

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： A61K31/44 ,  C07D415/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及式的化合物

公开(公告)号：US07378433B2

公开(公告)日：2008-05-27

申请号：US11639043

申请日：2006-12-13

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： A61K31/425 ,  C07D257/04

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6 - 烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8链烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US06833375B2

公开(公告)日：2004-12-21

申请号：US10238686

申请日：2002-09-10

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： C07D41710

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US06486187B1

公开(公告)日：2002-11-26

申请号：US09624966

申请日：2000-07-25

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： A61K31422

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US5922734A

公开(公告)日：1999-07-13

申请号：US860239

申请日：1997-06-16

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Gerard Charles Sanz

IPC分类号： C07D401/06 ,  A61K8/14 ,  A61K8/49 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： This invention is concerned with the compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof,wherein: R.sup.1 is hydrogen, amino or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halo or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-4 alkyl; Y is 0 or S, and --X.sup.1 .dbd.X.sup.2 --is a bivalent radical having the formula --N.dbd.CH--(a-1) or --CH.dbd.N--(a-2);compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.

摘要翻译： PCT No.PCT / EP95 / 05173 Sec。 371日期：1997年6月16日 102（e）日期1996年6月16日PCT 1995年12月21日PCT PCT。 WO96 / 20200 PCT出版物 日期：1996年7月4日本发明涉及药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中：R1是氢，氨基或C1-4烷基; R2是氢，卤素或C1-4烷基; R3是氢，卤素或C1-4烷基; Y为0或S，-X1 = X2-为具有式-N = CH-（a-1）或-CH = N-（a-2）的二价基团。 含有它们的组合物，以及制备这些化合物的方法。 它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

公开(公告)号：US07115630B2

公开(公告)日：2006-10-03

申请号：US10381987

申请日：2001-09-25

申请人： Dominique Jean-Pierre Mabire ,  Marc Gaston Venet ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Anne Simone Josephine Lesage

发明人： Dominique Jean-Pierre Mabire ,  Marc Gaston Venet ,  Sophie Coupa ,  Alain Philippe Poncelet ,  Anne Simone Josephine Lesage

IPC分类号： C07D215/17 ,  C07D215/20 ,  A61K31/47

CPC分类号： C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D221/10 ,  C07D221/12 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D417/04 ,  C07D453/06 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07F7/0812

摘要： The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula —Z4—CH2—CH2—CH2— or —Z4—CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

公开(公告)号：US20110124673A1

公开(公告)日：2011-05-26

申请号：US12950345

申请日：2010-11-19

申请人： Dominique Jean-Pierre Mabire ,  Jerôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

发明人： Dominique Jean-Pierre Mabire ,  Jerôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

IPC分类号： A61K31/473 ,  C07D405/14 ,  C07D401/12 ,  C07D221/12 ,  A61P35/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/02 ,  A61P29/00 ,  A61P19/02 ,  A61P3/10 ,  A61P9/10

CPC分类号： C07D215/227 ,  C07D241/44 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/12

摘要： The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.

摘要翻译： 本发明提供式（I）化合物和式（VII-a）化合物以及包含所述化合物及其用作PARP抑制剂的药物组合物，其中n，R1，R2，R3，R4，R5，R6，R7， Re，Rd和X定义含义。

公开(公告)号：US07879857B2

公开(公告)日：2011-02-01

申请号：US10596086

申请日：2004-11-18

申请人： Dominique Jean-Pierre Mabire ,  Jérôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

发明人： Dominique Jean-Pierre Mabire ,  Jérôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

IPC分类号： C07D241/44 ,  C07D215/227 ,  A61K31/498 ,  A61K31/4704 ,  A61P25/28

CPC分类号： C04B35/632 ,  C07D241/44 ,  C07D401/12 ,  C07D407/06 ,  C07D409/14

摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4 and X have defined meanings.

摘要翻译： 本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，R1，R2，R3，R4和X具有定义的含义。

公开(公告)号：US08524714B2

公开(公告)日：2013-09-03

申请号：US13047402

申请日：2011-03-14

申请人： Dominique Jean-Pierre Mabire ,  Jerome Emile Georges Guillemont ,  Jacobus Alphonsus Josephus van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

发明人： Dominique Jean-Pierre Mabire ,  Jerome Emile Georges Guillemont ,  Jacobus Alphonsus Josephus van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

IPC分类号： A61K31/498 ,  C07D401/06

CPC分类号： C07D403/06 ,  C07D241/44 ,  C07D401/06

摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4, R5, R6 and X have defined meanings.

摘要翻译： 本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，R1，R2，R3，R4，R5，R6和X具有定义的含义。