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51. 发明授权

US4859700A 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds having antihypoxic and nootropic effects 失效
标题翻译：具有抗缺氧和诱导作用的2-（2,3-二氢-2-氧代-3-苯并呋喃基）乙酸化合物
公开(公告)号：US4859700A
公开(公告)日：1989-08-22
申请号：US155352
申请日：1988-02-12
申请人： Gilbert Lavielle , Jean Lepagnol
发明人： Gilbert Lavielle , Jean Lepagnol
IPC分类号： A61K31/34 , A61K31/343 , A61K31/415 , A61P3/00 , A61P25/28 , C07D307/83 , C07D405/06 , C07D405/12 , C07D407/12
CPC分类号： C07D405/12 , C07D307/83 , C07D407/12
摘要： The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.1 (CHZ--COOH)--, in which Z denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms, a hydroxyalkyl radical having 1 to 4 carbon atoms, a 4-imidazolylmethylene radical or a benzyl radical optionally substituted with an alkyl radical having 1 to 4 carbon atoms or with a hydroxyl radical; a radical of general formula A.sub.2 (CH.sub.2 W)- in which W denotes a linear or branches dialkylaminomethylene radical having 3 to 9 carbon atoms, a 2-pyrrolidinyl radical optionally substituted with an alkyl radical having 1 to 4 carbon atoms, a benzyl radical, a 1-isochromanyl radical or a 1-isoquinolyl radical, or form, together with the nitrogen to which they are attached, a 2-carboxy-2-pyrrolidinyl radical, a 4-morpholinyl radical, a piperidino radical optionally substituted with a phenyl radical or with an alkoxyphenyl radical having 7 to 10 carbon atoms, or a 1-piperazinyl radical. Medicinal products.
摘要翻译：本发明涉及通式I的新的2-（2,3-二氢-2-氧代-3-苯并呋喃基）乙酸化合物：其中：R 1表示氢原子，直链或支链烷基具有1至4个碳原子的基团或任选被卤素原子或含有1至4个碳原子的烷氧基或具有1至4个碳原子的烷基的苯基，R 2表示氢或卤素原子，羟基，具有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基，R表示羟基，具有1至4个碳原子的直链或支链烷氧基，苄氧基或通式A的基团（A）其中：X和Y可以相同或不同，各自表示含有1至5个碳原子的直链或支链烷基，通式A1（CHZ-COOH） - 的基团，在其中Z表示氢原子，具有1至4个碳原子的直链或支链烷基，羟烷基具有1至4个碳原子的基团，4-咪唑基亚甲基或任选被具有1至4个碳原子的烷基或羟基自由基取代的苄基; 通式A2（CH2W）的基团，其中W表示具有3至9个碳原子的直链或支链二烷基氨基亚甲基，任选被具有1至4个碳原子的烷基取代的2-吡咯烷基，苄基，或与其连接的氮一起形成2-羧基-2-吡咯烷基，4-吗啉基，任选被苯基取代的哌啶子基或具有7至10个碳原子的烷氧基苯基或1-哌嗪基。药用产品。

52. 发明授权

US06998403B2 Benzoindoline compounds 失效
标题翻译：苯并二氢吲哚化合物
公开(公告)号：US06998403B2
公开(公告)日：2006-02-14
申请号：US10925712
申请日：2004-08-25
申请人： Gilbert Lavielle , Olivier Muller , Mark Millan , Alain Gobert , Benjamin Di Cara
发明人： Gilbert Lavielle , Olivier Muller , Mark Millan , Alain Gobert , Benjamin Di Cara
IPC分类号： A61K31/496 , C07D403/12
CPC分类号： C07D209/60
摘要： A compound of formula (I): wherein: R1 and R2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, and R3 and R4 represent hydrogen, or R1 and R4 represent hydrogen and R2 and R3 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, or R1 and R2 represent hydrogen and R3 and R4 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, addition salts thereof with a pharmaceutically acceptable acid or base, and methods of treating conditions susceptible to α2-AR/5-HT2C antagonists.
摘要翻译：式（I）化合物：化学式id =“CHEM-US-00001”num =“000

53. 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。

54. 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。

55. 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。

56. 发明授权

US06365605B1 Substituted hydrochromenopyrroles 失效
标题翻译：取代的氢色谱
公开(公告)号：US06365605B1
公开(公告)日：2002-04-02
申请号：US09480038
申请日：2000-01-10
申请人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Françoise Lejeune , Mark Millan
发明人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Françoise Lejeune , Mark Millan
IPC分类号： A61K3144
CPC分类号： C07D491/04
摘要： Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl, and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′-Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.
摘要翻译：式（I）的化合物：其中：m为0〜3，n为0〜3，2 <= m + n <= 3，p为1〜6，X表示氰基或-CO-NR 4 R 5， R 5选自氢，直链或支链（C 1 -C 6） - 烷基，（C 3 -C 7） - 环烷基和芳基，R 1和R 2各自独立地表示氢或直链或支链（C 1 -C 6） - 烷基，R 3表示氢，任选取代的苯基，萘基或杂芳基，或芳氧基或芳硫基，或被A'-Cy，A'和Cy取代的芳基或杂芳基如说明书中所定义，和含有它们的可用作D3受体配体的医药产品。

57. 发明授权

US06326377B1 Substituted hydrochromenopyridines 有权
标题翻译：取代的氢氯苯并吡啶
公开(公告)号：US06326377B1
公开(公告)日：2001-12-04
申请号：US09480037
申请日：2000-01-10
申请人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Françoise Lejeune , Mark Millan
发明人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Françoise Lejeune , Mark Millan
IPC分类号： A61K3144
CPC分类号： C07D491/04
摘要： Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl,and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′—Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.
摘要翻译：式（I）的化合物：其中：m为0〜3，n为0〜3，2 <= m + n <= 3，p为1〜6，X表示氰基或-CO-NR 4 R 5， R 5选自氢，直链或支链（C 1 -C 6） - 烷基，（C 3 -C 7） - 环烷基和芳基，R 1和R 2各自独立地表示氢或直链或支链（C 1 -C 6） - 烷基，R 3表示氢，任选取代的苯基，萘基或杂芳基，或芳氧基或芳硫基，或被A'-Cy，A'和Cy取代的芳基或杂芳基如说明书中所定义，和含有它们的可用作D3受体配体的医药产品。

58. 发明授权

US06300340B1 Bisimide compounds 失效
标题翻译：双酰亚胺化合物
公开(公告)号：US06300340B1
公开(公告)日：2001-10-09
申请号：US09616857
申请日：2000-07-14
申请人： Gilbert Lavielle , Patrick Hautefaye , Ghanem Atassi , Alain Pierre , Laurence Kraus-Berthier , Stéphane Leonce
发明人： Gilbert Lavielle , Patrick Hautefaye , Ghanem Atassi , Alain Pierre , Laurence Kraus-Berthier , Stéphane Leonce
IPC分类号： C07D48704
CPC分类号： C07D209/80 , C09B57/08
摘要： A compound of formula (I) in which: m, and n, which may be identical or different, represent 0 or 1, X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C4 to C12 alkylene chain in which one or more —CH2— are optionally replaced by any one of the following atoms or groups: —NR—, —O—, —S—, —SO—, SO2—, or —CONH—, or by a substituted or unsubstituted heterocylcic, A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharamaceutically and acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.
摘要翻译：式（I）化合物，其中m和n可以相同或不同，表示0或1，X和Y可以相同或不同，表示氢或卤素或烷基，三卤代烷基，烷氧基，羟基，氰基，硝基，氨基，烷基氨基或二烷基氨基，Z表示直链或支链的C 4至C 12亚烷基链，其中一个或多个-CH 2 - 任选被以下任何一个原子或基团取代：-NR-，-O - ， - S - ， - SO - ，SO2-或-CONH-，或通过取代或未取代的杂环A形式与苯环的两个相邻碳原子，苯基，萘基或四氢萘基环或杂环，表示在描述中定义的任何一个基团，其光学异构体及其与药物和可接受的酸或碱的加成盐，以及含有该组的药物，其可用作抗癌剂。

59. 发明授权

US6090837A Substituted hydrochromenopyrroles 失效
标题翻译：取代的氢色谱
公开(公告)号：US6090837A
公开(公告)日：2000-07-18
申请号：US103304
申请日：1998-06-23
申请人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Fran.cedilla.oise Lejeune , Mark Millan
发明人： Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Fran.cedilla.oise Lejeune , Mark Millan
IPC分类号： A61K31/40 , A61K31/435 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07B53/00 , C07D491/04 , C07D491/052 , A61K31/407 , A61K31/436 , C07D491/02
CPC分类号： C07D491/04
摘要： Compounds of formula (I): ##STR1## wherein: m is 0 to 3 inclusive,n is 0 to 3 and 2.ltoreq.m+n.ltoreq.3,p is 1 to 6 inclusive,X represents cyano or --CO--NR.sub.4 R.sub.5, R.sub.4 and R.sub.5 being selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, and aryl,R.sub.1 and R.sub.2 each independently represent hydrogen or linear or branched (C.sub.1 -C.sub.6)-alkyl,R.sub.3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A'-Cy, A' and Cy being as defined in the description, andmedicinal products containing the same which are useful as D.sub.3 receptor ligands.
摘要翻译：式（I）的化合物：其中：m为0〜3，n为0〜3，m为2〜3，p为1〜6，X为氰基或-CO-NR 4 R 5， R 4和R 5选自氢，直链或支链（C 1 -C 6） - 烷基，（C 3 -C 7） - 环烷基和芳基，R 1和R 2各自独立地表示氢或直链或支链（C 1 -C 6） - 烷基，R 3 表示氢，任选取代的苯基，萘基或杂芳基，或芳氧基或芳硫基，或被A'-Cy，A'和Cy取代的芳基或杂芳基如说明书中所定义，和含有它们的药物，可用作D3受体配体。

60. 发明授权

US5854273A Bisimide compounds 失效
标题翻译：双酰亚胺化合物
公开(公告)号：US5854273A
公开(公告)日：1998-12-29
申请号：US899289
申请日：1997-07-23
申请人： Gilbert Lavielle , Patrick Hautefaye , Ghanem Atassi , Alain Pierre , Laurence Kraus-Berthier , Stephane Leonce
发明人： Gilbert Lavielle , Patrick Hautefaye , Ghanem Atassi , Alain Pierre , Laurence Kraus-Berthier , Stephane Leonce
IPC分类号： C07D221/10 , A61K31/435 , A61K31/47 , A61K31/473 , A61K31/55 , A61P35/00 , C07D209/80 , C07D401/12 , C07D403/12 , C07D519/00 , A61K31/40 , C07D403/06
CPC分类号： C07D209/80 , C09B57/08
摘要： A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--, A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.
摘要翻译：式（I）化合物其中：X和Y可以相同或不同，表示氢或卤素或烷基，三卤代烷基，烷氧基，羟基，氰基，硝基，氨基，烷基氨基或二烷基氨基 Z表示直链或支链的C 4至C 12亚烷基链，其中一个或多个-CH 2 - 任选被以下原子或基团中的任何一个取代：-NR - ， - O - ， - S - ， - SO-， - SO 2 - 或-CONH-，A形式，其具有苯环的两个相邻碳原子，苯基，萘基或四氢萘基环或杂环，IMAGE表示说明书中定义的任何一个基团，其旋光异构体及其与药学上可接受的酸或碱的加成盐，以及含有该盐的药物，可用作抗癌剂。

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