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1. 发明授权

US06545037B2 Benzenesulfonamide compounds 失效
标题翻译：苯磺酰胺化合物
公开(公告)号：US06545037B2
公开(公告)日：2003-04-08
申请号：US10097764
申请日：2002-03-14
申请人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号： C07D21132
CPC分类号： C07D207/08 , C07D211/22 , C07D211/32 , C07D211/70 , C07D295/096 , C07D295/192 , C07D401/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： A compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor and pharmaceutical compositions containing the same.
摘要翻译：式（I）化合物：其可用作TXA2和5-HT2受体以及含有该化合物的药物组合物。

2. 发明授权

US06469011B2 Benzenesulfonamide compounds useful as TXA2 and 5-HT2 receptor antagonists 失效
标题翻译：可用作TXA2和5-HT2受体拮抗剂的苯磺酰胺化合物
公开(公告)号：US06469011B2
公开(公告)日：2002-10-22
申请号：US09764576
申请日：2001-01-18
申请人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号： C07D21132
CPC分类号： C07D207/08 , C07D211/22 , C07D211/32 , C07D211/70 , C07D295/096 , C07D295/192 , C07D401/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor antagonist and pharmaceutical compositions containing the same.
摘要翻译：式（I）化合物：其可用作TXA2和5-HT2受体拮抗剂以及含有它们的药物组合物。

3. 发明授权

US6013667A Benzenesulfonylamine compounds, process for preparing them and pharmaceutical compositions 失效
标题翻译：苯磺酰胺化合物，其制备方法和药物组合物
公开(公告)号：US6013667A
公开(公告)日：2000-01-11
申请号：US32587
申请日：1998-02-27
申请人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号： A61K31/18 , A61K31/195 , A61K31/215 , A61P7/02 , A61P9/08 , A61P9/10 , C07C303/40 , C07C311/16 , C07C311/19 , C07C311/21 , C07C381/00 , A61K31/21
CPC分类号： C07C311/19 , C07C311/21 , C07C381/00 , C07C2102/10
摘要： Compounds of formula (I): in which:R.sub.a and R.sub.b, identical or different, represent hydrogen or alkyl or together form a bond,R.sub.C represents hydroxyl optionally substituted alkoxy, or optionally substituted amino,R.sub.1 represents hydrogen or --O--NO.sub.2, --O--NO, or --S--NO,R.sub.2 and R.sub.3, identical or different, represent hydrogen, alkyl, or optionally substituted phenyl,X represents oxygen or --NH--CO--,m represents 0 or 1,n represents an integer such that 0.ltoreq.n.ltoreq.6,p represents 0 or 1,R.sub.4 represents hydrogen, optionally substituted alkyl, optionally substituted phenyl, or a group as defined in the description,R.sub.5 represents hydrogen or alkyl,R.sub.6 represents hydrogen or alkyl,or R.sub.5 and R.sub.6 together form a chain --(CH.sub.2).sub.t -- in which t represents 1 or 2,q represents 0, 1, or 2,r represents an integer such that 0.ltoreq.r.ltoreq.6,R.sub.d and R.sub.e, identical or different, represent hydrogen, halogen, alkyl, alkoxy, hydroxyl, or trihaloalkyl, it being understood that at least one --O--NO.sub.2, O--NO, or S--NO groupis present in R.sub.1, R.sub.4 or R.sub.c ; process of preparing same, pharmaceutical compositions thereof, and their use as TXA.sub.2 -receptor antagonists and NO donors.
摘要翻译：式（I）化合物：其中：R a和R b相同或不同，代表氢或烷基或一起形成键，RC表示羟基任选取代的烷氧基或任选取代的氨基，R 1表示氢或-O-NO 2， O-NO或-S-NO，R 2和R 3相同或不同，表示氢，烷基或任选取代的苯基，X表示氧或-NH-CO-，m表示0或1，n表示整数，使得 0表示0或1，R4表示氢，任选取代的烷基，任选取代的苯基或说明书中定义的基团，R 5表示氢或烷基，R 6表示氢或烷基，或 R5和R6一起形成链 - （CH 2）t-，其中t表示1或2，q表示0,1或2，r表示0以及r和r的整数，相同或不同，代表氢，卤素，烷基，烷氧基，羟基或三卤代烷基，应理解至少有一个-O-NO 2，O-NO或S-NO基团存在于 R1，R4或Rc; 其制备方法，其药物组合物及其作为TXA2受体拮抗剂和NO供体的用途。

4. 发明授权

US06589956B2 Benzenesulphonamide compounds 失效
标题翻译：苯磺酰胺化合物
公开(公告)号：US06589956B2
公开(公告)日：2003-07-08
申请号：US10195031
申请日：2002-07-12
申请人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
发明人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
IPC分类号： A61K31496
CPC分类号： C07D401/06 , C07D209/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： A compound of formula (I): wherein: Ra represents a hydroxy, alkoxy, aryloxy or arylalkyloxy group, A represents a CH group or a nitrogen atom, in which case R1 is as defined in the description, or R1—A together represent an oxygen atom or a group, wherein R3 and R4 are as defined in the description, R2 being a hydrogen atom or an alkyl group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, n is an integer of from 2 to 6 inclusive, m and p are integers of from 0 to 6 inclusive, its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as a TXA2 receptor antagonist and 5-HT2 receptor antagonist.
摘要翻译：式（I）的化合物：其中：R a表示羟基，烷氧基，芳氧基或芳烷氧基，A表示CH基或氮原子，在这种情况下，R1如说明书中所定义，或者R 1 -A一起表示氧原子或基团，其中R 3和R 4如说明书中所定义，R 2为氢原子或烷基，R b和R c可以相同或不同，各自表示氢原子，卤素原子，烷基基团，烷氧基，羟基或三卤代烷基，n为2-6以下的整数，m和p为0〜6的整数，其对映体，非对映异构体及其加成盐与药学上可接受的酸或碱，以及含有它们的药物，其可用作TXA2受体拮抗剂和5-HT2受体拮抗剂。

5. 发明授权

US06541471B1 Benzenesulphonamide compounds 失效
标题翻译：苯磺酰胺化合物
公开(公告)号：US06541471B1
公开(公告)日：2003-04-01
申请号：US10195018
申请日：2002-07-12
申请人： Gilbert Lavielle , Thierry Dubuffet , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
发明人： Gilbert Lavielle , Thierry Dubuffet , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
IPC分类号： A61K315375
CPC分类号： C07D275/06 , C07C311/19 , C07D295/088 , C07D413/04 , C07D417/04
摘要： A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 receptor antagonist and a 5-HT2 receptor antagonist.
摘要翻译：式（I）的化合物：其中：G表示如下基团：其中R1和R2独立地表示氢原子或烷基，环烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基或杂芳基烷基，或R1和R2 与氮原子一起形成杂环烷基，R 3表示氢原子或烷基或任选取代的苯基，R a表示羟基，直链或支链（C 1 -C 6）烷氧基或氨基，R b和R c，可以相同或不同，分别表示氢原子，卤素原子，烷基，烷氧基，羟基或三卤代烷基，m为0〜1的整数，n和q为 0〜6，p和r为1〜6的整数，其对映异构体和非对映异构体及其与药学上可接受的酸或碱的加成盐; 和含有它们的药物，其可用作TXA2受体拮抗剂和5-HT2受体拮抗剂。

6. 发明授权

US07618955B2 Association of an antithrombotic and aspirin 失效
标题翻译：抗凝血和阿司匹林协会
公开(公告)号：US07618955B2
公开(公告)日：2009-11-17
申请号：US10509605
申请日：2003-04-04
申请人： Tony Verbeuren , Gilbert Lavielle , Bernard Cimetiere , Marie-Odile Vallez
发明人： Tony Verbeuren , Gilbert Lavielle , Bernard Cimetiere , Marie-Odile Vallez
IPC分类号： A61K31/60 , A61K31/195
CPC分类号： A61K31/196 , A61K31/616 , A61K2300/00
摘要： The present invention relates to a new combination of an antithrombotic and aspirin and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及抗血栓形成和阿司匹林的新组合以及包含它们的药物组合物。

7. 发明授权

US06509345B2 Camptothecin analogue compounds 失效
标题翻译：喜树碱类似物
公开(公告)号：US06509345B2
公开(公告)日：2003-01-21
申请号：US10010380
申请日：2001-11-05
申请人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , Ghanem Atassi , John Hickman , Bernard Cimetiere
发明人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , Ghanem Atassi , John Hickman , Bernard Cimetiere
IPC分类号： C07D47114
CPC分类号： C07D471/14 , A61K31/4745 , Y02P20/55
摘要： Compound of formula (I): wherein: n is 0, 1 or 2, R1, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NRaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being an integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81 and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group. and medicinal products containing the same are useful for the treatment of cancerous diseases.
摘要翻译：式（I）化合物：其中：n为0,1或2，R1，R2，R3，R4和R5选自氢，卤素，烷基，烯基，炔基，全卤代烷基，环烷基，环烷基烷基，羟基，羟烷基，烷氧基，烷氧基烷基，烷氧基羰基，酰氧基，羧基，硝基，氰基，氨基羰基（任选取代的）和基团（CH 2）p -NR a R b和-OC（O）-NR a R b，其中p，R a和R b如描述或两个相邻基团R 2，R 3，R 4和R 5一起形成基团-O-（CH 2）t O，t为1至3的整数，R 60，R 70n，R 80和R 90表示氢原子，羟基，烷氧基或描述中定义的O-（CO）-X或O-（CO）-NXW基团，R61，R71n，R81和R91表示氢原子，烷基，烯基或炔基，或成对取代一起形成键或环氧乙烷基团，或两个基团一起形成氧代基，并且含有该氧基的药物可用于治疗癌性疾病。

8. 发明授权

US06239129B1 Cyano-indole serotonin-reuptake inhibitor compounds 失效
标题翻译：氰基吲哚5-羟色胺再摄取抑制剂化合物
公开(公告)号：US06239129B1
公开(公告)日：2001-05-29
申请号：US09490909
申请日：2000-01-25
申请人： Gilbert Lavielle , Olivier Muller , Bernard Cimetiere , Mark Millan , Alain Gobert , Jean-Michel Rivet
发明人： Gilbert Lavielle , Olivier Muller , Bernard Cimetiere , Mark Millan , Alain Gobert , Jean-Michel Rivet
IPC分类号： A61K31404
CPC分类号： C07D401/12 , C07D209/08 , C07D403/06 , C07D403/12 , C07D403/14 , C07D513/04
摘要： Compound of formula (I): wherein: R1 and R2 each independently of the other represents hydrogen or alkyl, A represents alkylene, alkenylene or alkynylene, G1 represents wherein R3 and R4 each independently of the other represents hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted aryl or optionally substituted arylalkyl, or G1 represents heterocycloalkyl optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, nitrile, carboxy, alkoxycarbonyl, carbamoyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, and which medicinal products containing the same/are useful as serotonin-reuptake inhibitors.
摘要翻译：式（I）化合物：其中：R 1和R 2各自独立地表示氢或烷基，A表示亚烷基，亚烯基或亚炔基，G 1表示其中R 3和R 4各自独立地表示氢，烷基，环烷基，环烷基烷基，任选地取代的芳基或任选取代的芳基烷基，或G 1表示任选被烷基，环烷基，环烷基烷基，腈，羧基，烷氧基羰基，氨基甲酰基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基取代的杂环烷基， /作为5-羟色胺再摄取抑制剂是有用的。

9. 发明授权

US06699876B2 Camptothecin analogue compounds 失效
标题翻译：喜树碱类似物
公开(公告)号：US06699876B2
公开(公告)日：2004-03-02
申请号：US10300330
申请日：2002-11-20
申请人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , Ghanem Atassi , John Hickman , Bernard Cimetiere
发明人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , Ghanem Atassi , John Hickman , Bernard Cimetiere
IPC分类号： A61K314375
CPC分类号： C07D471/14 , A61K31/4745
摘要： Compound of formula (I): wherein: n is 0, 1 or 2, R1 represents (C3-C11)cycloalkyl or (C3-C11)cycloalkylalkyl, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81, and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group. and medicinal products containing the same are useful for the treatment of cancerous disesases.
摘要翻译：式（I）化合物：其中：n为0,1或2，R1代表（C3-C11）环烷基或（C3-C11）环烷基烷基，R2，R3，R4和R5选自氢，卤素，烷基，烯基，炔基，全卤代烷基，环烷基，环烷基烷基，羟基，羟基烷基，烷氧基，烷氧基烷基，烷氧基羰基，酰氧基，羧基，硝基，氰基，氨基羰基（任选取代的）和基团（CH 2）p-NaRb和-OC（O） -RaRb，其中p，Ra和Rb如说明书中所定义，或两个相邻基团R 2，R 3，R 4和R 5一起形成基团-O-（CH 2）t O，t为1至3的整数，R 60，R 70n R 80和R 90表示如说明书中定义的氢原子，羟基，烷氧基或O-（CO）-X或O-（CO）-NXW基团，R61，R71n，R81和R91表示氢原子，烷基，烯基或炔基，或成对取成一起形成键或环氧乙烷基，或两个基团一起形成氧代基，并且含有该氧基的药物可用于治疗癌性疾病。

10. 发明授权

US08247441B2 Chromene compounds, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：色烯化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08247441B2
公开(公告)日：2012-08-21
申请号：US12804355
申请日：2010-07-20
申请人： Guillaume De Nanteuil , Bernard Cimetiere , Anne Dekeyne , Mark Millan
发明人： Guillaume De Nanteuil , Bernard Cimetiere , Anne Dekeyne , Mark Millan
IPC分类号： A61K31/407 , C07D209/58
CPC分类号： C07D491/04
摘要： The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.
摘要翻译：本发明涉及式（I）化合物：其中R 1和R 2一起形成以下含碳链：其中：R 3表示氢原子或烷基，R 4表示氢原子或烷基，芳基，杂芳基，3 ，4-二氧环戊烯基，烷基羰基，环烷基羰基，杂环烷基羰基，苯甲酰基，芳基磺酰基或杂芳基磺酰基，这些基团任选被取代，或者R3和R4与携带它们的氮原子一起形成5-至8-元环，形成任选地被取代。含有该药物的药物可用于治疗需要D3受体拮抗剂的病症。

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