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1. 发明授权

US5296494A Pyrrolidine compounds having thromboxane A.sub.2 receptor antagonistic activity and thromboxane A.sub.2 synthase inhibiting activity 失效
标题翻译：具有血栓烷A2受体拮抗活性和血栓烷A2合酶抑制活性的吡咯烷化合物
公开(公告)号：US5296494A
公开(公告)日：1994-03-22
申请号：US992930
申请日：1992-12-18
申请人： Gilbert Lavielle , Patrick Hautefaye , Michel Laubie , Tony Verbeuren
发明人： Gilbert Lavielle , Patrick Hautefaye , Michel Laubie , Tony Verbeuren
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P43/00 , C07D207/08 , C07D401/04 , C07D401/06 , C07D207/48
CPC分类号： C07D207/08 , C07D401/04 , C07D401/06
摘要： Compounds of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, m, n, and R are as defined in the Specification.Medicinal products containing the same are useful in the treatment or prevention of thrombotic afflictions due to their thromboxane A.sub.2 receptor antagonistic activity and their thromboxane A.sub.2 synthase inhibitory activity.
摘要翻译：式（I）化合物：其中R 1，R 2，R 3，m，n和R如本说明书中所定义。含有它们的药物可用于治疗或预防由于其血栓烷A 2受体拮抗活性及其血栓烷A2合酶抑制活性引起的血栓形成性疾病。

2. 发明授权

US5436343A Alkenecarboxylic acid compounds 失效
标题翻译：烯烃羧酸化合物
公开(公告)号：US5436343A
公开(公告)日：1995-07-25
申请号：US62080
申请日：1993-05-14
申请人： Gilbert Lavielle , Patrick Hautefaye , Michel Laubie , Tony Verbeuren
发明人： Gilbert Lavielle , Patrick Hautefaye , Michel Laubie , Tony Verbeuren
IPC分类号： A61K31/13 , A61K31/135 , A61K31/16 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/34 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/445 , A61P7/02 , A61P9/08 , A61P43/00 , C07C311/19 , C07D211/34 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/96 , C07D213/42 , C07D311/96 , C07D333/20 , C07D211/04
CPC分类号： C07D211/96 , C07C311/19 , C07C2101/08 , C07C2101/14 , C07C2102/08 , C07C2102/10
摘要： Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched (C.sub.1 C.sub.6) alkyl radical, a substituted or unsubstituted phenyl radical, a pyridyl radical or a thienyl radical, or, with the carbon atom to which they are attached, a substituted or unsubstituted (C.sub.4 -C.sub.7) cycloalkyl ring,R.sub.3 representsa substituted or unsubstituted phenylsulfonyl radical,a linear or branched (C.sub.1 -C.sub.6) alkyl radical,an alkylaminocarbonyl radical,or a linear or branched (C.sub.1 -C.sub.6) acyl radical,R.sub.4 represents any one of the radicals:--CH.dbd.CH--(CH.sub.2).sub.p --CO.sub.2 H or --CH.sub.2 --CH.sub.2 --(CH.sub.2)p--CO.sub.2 Hin which p is equal to 0, 1, 2 or 3, n and m, which may be identical or different, represent 0, 1 or 2,their isomers, enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.
摘要翻译：式（I）化合物：其中：R 1和R 2可以相同或不同，表示直链或支链（C 1 -C 6）烷基，取代或未取代的苯基，吡啶基或或与其连接的碳原子一起取代或未取代的（C 4 -C 7）环烷基环，R 3表示取代或未取代的苯基磺酰基，直链或支链（C1-C6）烷基，烷基氨基羰基基团或直链或支链（C1-C6）酰基，R4表示以下基团中的任何一个：-CH = CH-（CH 2）p -CO 2 H或-CH 2 -CH 2 - （CH 2）p -CO 2 H，其中p为等于0,1,2或3，n和m可以相同或不同，表示0,1或2，它们的异构体，对映异构体，非对映异构体和差向异构体以及它们与药学上可接受的酸或碱的加成盐。

3. 发明申请

US20100168149A1 Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them 审中-公开
标题翻译：喜树碱类似物，其制备方法和含有他们的药物组合物
公开(公告)号：US20100168149A1
公开(公告)日：2010-07-01
申请号：US11990065
申请日：2006-08-04
申请人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , John Hickman , Stephane Leonce
发明人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , John Hickman , Stephane Leonce
IPC分类号： A61K31/475 , C07D471/14 , A61P35/00
CPC分类号： C07D471/14
摘要： Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.
摘要翻译：式（I）化合物：其中：R1，R2，R3，R4，R5，R80，R90，R81，R91，Alk和G如说明书中所定义。含有该药物的药物可用于治疗癌症疾病。

4. 发明授权

US6162822A Bisimide compounds 失效
标题翻译：双酰亚胺化合物
公开(公告)号：US6162822A
公开(公告)日：2000-12-19
申请号：US221904
申请日：1998-12-28
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 , A01N43/38 , C07D487/00 , C07D487/02 , C07D491/00 , A61R31/40
CPC分类号： C07D209/80 , C09B57/08
摘要： A compound of formula (I) ##STR1## 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 alky, 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--, 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, ##STR2## and medicinal products containing the same are useful as anticancer agent.
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-，-SO 2 - 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，含有该药物的药物可用作抗癌剂。

5. 发明授权

US5500443A New benzodioxane compounds 失效
标题翻译：新的苯并二恶烷化合物
公开(公告)号：US5500443A
公开(公告)日：1996-03-19
申请号：US392203
申请日：1995-02-22
申请人： Gilbert Lavielle , Patrick Hautefaye , Olivier Muller , Mark Millan , Mauricette Brocco
发明人： Gilbert Lavielle , Patrick Hautefaye , Olivier Muller , Mark Millan , Mauricette Brocco
IPC分类号： C07D319/16 , A61K31/00 , A61K31/335 , A61K31/357 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/453 , A61K31/55 , A61P25/18 , A61P25/22 , C07D319/18 , C07D319/20 , C07D405/12 , C07D405/14 , C07D413/14 , C07D207/04
CPC分类号： C07D405/12 , C07D319/18 , C07D319/20 , C07D405/14 , C07D413/14
摘要： A compound of formula (I): ##STR1## in which: X represents oxygen or methylene,n represents 1, 2 or 3,R.sub.1 represents hydrogen, aminocarbonyl or hydroxymethyl,R.sub.2 represents: ##STR2## in which R.sub.3 and R.sub.4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.
摘要翻译：式（I）的化合物：其中：X表示氧或亚甲基，n表示1,2或3，R1表示氢，氨基羰基或羟甲基，R2表示：其中R3和R4 如本说明书中所定义，其异构体及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用于治疗精神分裂症。

6. 发明申请

US20100168150A1 Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them. 审中-公开
标题翻译：喜树碱类似物，其制备方法和含有他们的药物组合物。
公开(公告)号：US20100168150A1
公开(公告)日：2010-07-01
申请号：US11990104
申请日：2006-08-04
申请人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , John Hickman , Stephane Leonce
发明人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre , John Hickman , Stephane Leonce
IPC分类号： A61K31/475 , C07D471/14 , A61P35/00
CPC分类号： C07D471/14
摘要： Compound of formula (I): wherein: R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk, Alk′, X, X′ and G are as defined in the description. Medicinal products containing the same which are useful in the treatment of cancer diseases.
摘要翻译：式（I）化合物：其中：R1，R2，R3，R4，R5，R80，R90，R81，R91，Alk，Alk'，X，X'和G如说明书中所定义。含有该药物的药物可用于治疗癌症疾病。

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

US5100881A N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases 失效
标题翻译：用于治疗神经疾病的1-氨基乙基磷酸的N-（23-VINCRISTINOYL）和N-（5'-去甲基-23-VINBLASTINOYL）化合物
公开(公告)号：US5100881A
公开(公告)日：1992-03-31
申请号：US561065
申请日：1990-08-01
申请人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre
发明人： Gilbert Lavielle , Patrick Hautefaye , Alain Pierre
IPC分类号： A61K31/675 , A61P35/00 , C07F9/32 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/6561
摘要： The invention relates to the compounds of general formula I: ##STR1## in which: R.sub.1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and which can bear a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidazolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each represents a linear or branched alkyl radical containing from 1 to 6 carbon atoms,n is equal to 1 or 2,R.sub.4 represents a hydrogen atom, a formyl radical or a methyl radical, with the proviso, however, that R.sub.4 is never the methyl radical when n is equal to 2, andeither R.sub.5 and R.sub.6 together form a double bond, or R.sub.5 represents a hydrogen atom and R.sub.6 a hydroxyl radical,in the form of a mixture of diastereoisomers or of pure isomers, their N.sub.b,-oxides and their addition salts with a pharmaceutically acceptable inorganic or organic acid.These compounds are antitumor agents.
摘要翻译：本发明涉及通式I的化合物：其中：R 1表示氢原子，含有1至6个碳原子的直链或支链烷基，含有直链或支链烯基的基团 2至6个碳原子，具有7至10个碳原子的芳基烷基，其可以带有卤素原子作为芳族环上的取代基，羟基或每个含有1至5个碳原子的烷基或烷氧基， 2-吲哚基甲基，4-咪唑基甲基或含有3至11个碳原子的烷氧基羰基甲基，可以相同或不同的R 2和R 3各自表示含有1至6个碳原子的直链或支链烷基，n 等于1或2，R4表示氢原子，甲酰基或甲基，但条件是，当n等于2时，R 4不是甲基，R 5和R 6一起形成双键，或R 5表示氢原子和R6是非对映异构体或纯异构体的混合物形式的羟基，它们的Nb， - 氧化物及其与药学上可接受的无机酸或有机酸的加成盐。这些化合物是抗肿瘤剂。

9. 发明授权

US4946833A N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid useful for treating neoplastic diseases 失效
标题翻译：用于治疗肿瘤疾病的1-氨基甲基膦酸的N-（23-长春碱）基化合物
公开(公告)号：US4946833A
公开(公告)日：1990-08-07
申请号：US276357
申请日：1988-11-23
申请人： Gilbert Lavielle , Patrick Hautefaye , Claude Cudennec
发明人： Gilbert Lavielle , Patrick Hautefaye , Claude Cudennec
IPC分类号： C07D519/04 , A61K31/475 , A61K31/66 , A61P35/00 , A61P35/02 , C07F9/40 , C07F9/6561
CPC分类号： C07F9/6561
摘要： The invention relates to N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkylene radical containing from 1 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and capable of bearing a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidzolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each denote a linear or branched alkyl radical containing from 1 to 4 carbon atoms,in the form of a mixture of diastereoisomers or of pure isomers, their N.sup.b' -oxides and their addition salts with a pharmaceutically acceptable inoranic or organic acid.These compounds are antitumor agents.
摘要翻译：本发明涉及通式I（I）的1-氨基甲基膦酸的N-（23-长春碱）基化合物，其中：R1表示氢原子，含有1至6个碳原子的直链或支链烷基，含有1至6个碳原子的直链或支链亚烷基，具有7至10个碳原子且能够带有卤素原子作为芳族环上的取代基的芳基烷基，羟基或烷基或烷氧基，每个含有 1至5个碳原子，2-吲哚基甲基基团，4-亚氨基甲基基团或含有3至11个碳原子的烷氧羰基甲基基团，可以相同或不同，表示直链或支链烷基， 1至4个碳原子，以非对映异构体或纯异构体的混合物形式，其Nb'氧化物及其与药学上可接受的无机酸或有机酸的加成盐。这些化合物是抗肿瘤剂。

10. 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。

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