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1. 发明授权

US4501891A Method of forming a solution of papavrine carbanion 失效
标题翻译：形成Papavrine碳阴离子溶液的方法
公开(公告)号：US4501891A
公开(公告)日：1985-02-26
申请号：US348147
申请日：1982-02-11
申请人： Andre Buzas , Gilbert Lavielle
发明人： Andre Buzas , Gilbert Lavielle
IPC分类号： C07D217/20
CPC分类号： C07D217/20
摘要： This invention relates to the new papaverine carbanion of the formula: ##STR1## and to a preparation process of the same comprising reacting on papaverine, in a solvent, a slight excess of a highly basic agent.
摘要翻译：本发明涉及新的具有下式的罂粟碱碳负离子：＆lt; IMAGE＆gt;及其制备方法，包括在罂粟碱，在溶剂中，略微过量的高碱性剂。

2. 发明授权

US4382935A Analgesic drug containing a derivative of benzylpiperazine 失效
标题翻译：含有苄基哌嗪衍生物的止痛药
公开(公告)号：US4382935A
公开(公告)日：1983-05-10
申请号：US229532
申请日：1981-01-29
申请人： Andre Buzas , Jean-Marie Melon , Gilbert Lavielle , Andre Champagnac
发明人： Andre Buzas , Jean-Marie Melon , Gilbert Lavielle , Andre Champagnac
IPC分类号： A61K31/495 , C07D307/82 , C07D405/04
CPC分类号： C07D307/82 , A61K31/495
摘要： The drug contains an active substance consisting of 1-(3'-benzofuryl)-4-benzylpiperazine. In order to prepare the compound, a reaction is carried out with reflux between 3-coumaranone and N-benzylpiperazine in the presence of acetic acid and in an aromatic solvent.
摘要翻译：该药物含有由1-（3'-苯并呋喃基）-4-苄基哌嗪组成的活性物质。为了制备化合物，在乙酸存在下和在芳香族溶剂中，在3-香豆酮与N-苄基哌嗪之间进行反应。

3. 发明授权

US4127666A Disubstituted 2,5-benzamides and pharmaceutical compositions containing the same 失效
标题翻译：二取代的2,5-苯甲酰胺和含有它们的药物组合物
公开(公告)号：US4127666A
公开(公告)日：1978-11-28
申请号：US768893
申请日：1977-02-15
申请人： Andre Buzas , Gilbert Lavielle
发明人： Andre Buzas , Gilbert Lavielle
IPC分类号： C07D207/08 , C07D295/192 , C07D317/58 , A61K31/40 , A61K31/445 , C07D207/02
CPC分类号： C07D207/08 , C07D295/192 , C07D317/58
摘要： The disubstituted 2,5-benzamides correspond to the following general formula: ##STR1## where R is an alkyl group (possessing 1 to 5 carbon atom) or an allyl group, ##STR2## represents one of the following groups: phenylpiperazine, benzylpiperazine, piperonylpiperazine, dimethylaminoethylamino, diethylaminoethylamino, pyrrolidinyl-1 substituted methylamino, morpholine or piperidine, R' is an alkyl possessing 1 to 8 carbon atoms, a phenyl, or substituted phenyl, an alpha-aminomethyl or acrylic group, Y is an oxygen atom, an oxime, oxime ether, oxime ester or imine group.
摘要翻译：二取代的2,5-苯甲酰胺对应于以下通式：其中R是烷基（具有1至5个碳原子）或烯丙基，其中R 1表示以下基团之一：苯基哌嗪，苄基哌嗪，哌啶基哌嗪，二甲基氨基乙基氨基，二乙基氨基乙基氨基，吡咯烷基-1取代的甲基氨基，吗啉或哌啶，R'是具有1至8个碳原子的烷基，苯基或取代的苯基，α-氨基甲基或丙烯酸基，Y是氧原子，肟，肟醚，肟酯或亚胺基。

4. 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。

5. 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。

6. 发明授权

US5472979A 1,2,3,4-tetrahydronaphthalene compounds 失效
标题翻译： 1,2,3,4-四氢萘化合物
公开(公告)号：US5472979A
公开(公告)日：1995-12-05
申请号：US323508
申请日：1994-10-14
申请人： Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人： Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号： A61K31/18 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61P7/02 , A61P9/00 , A61P43/00 , C07C311/02 , C07C311/14 , C07C311/20 , C07C311/29 , C07D213/55 , C07D311/58 , C07D335/06 , A61K31/14
CPC分类号： C07D335/06 , C07C311/20 , C07D213/55 , C07D311/58
摘要： R.sub.1 and R.sub.2 form, with the carbon atoms to which they are attached, cyclopentane or cyclohexane,R.sub.3 represents hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or unsubstituted or substituted amino,R.sub.4 represents alkyl, unsubstituted or substituted phenyl, naphthyl, pyridyl or thienyl, X represents methylene or oxygen or sulfur,its enantiomers and its addition salts with a pharmaceutically acceptable base, and medicinal products containing the same are useful as anti-thrombotic.
摘要翻译：其中：R 1和R 2可以相同或不同，表示氢或卤素，烷基，取代或未取代的苯基，苄基，吡啶基甲基或咪唑基甲基或噻唑基甲基，吡啶基，咪唑基或噻唑基，或者R1 和R 2与它们所连接的碳原子形成环戊烷或环己烷，R 3表示羟基，直链或支链（C 1 -C 6）烷氧基或未取代或取代的氨基，R 4表示烷基，未取代或取代的苯基，萘基，吡啶基或噻吩基，X表示亚甲基或氧或硫，其对映体及其与药学上可接受的碱的加成盐，以及含有它们的药物可用作抗血栓形成。

7. 发明授权

US5278185A Piperidine, Tetrahydropyridine and pyrrolidine compounds 失效
标题翻译：哌啶，四氢吡啶和吡咯烷化合物
公开(公告)号：US5278185A
公开(公告)日：1994-01-11
申请号：US971342
申请日：1992-11-04
申请人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
发明人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/47 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D207/06 , C07D207/08 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D295/13 , C07D295/185 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06
CPC分类号： C07D295/185 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D401/04 , C07D405/04
摘要： The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.4 represents a hydrogen atom, a halogen atom, an alkyl radical having 1 to 6 carbon atoms, or an alkoxy radical having 1 to 6 carbon atoms, and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, and medicaments containing the same.
摘要翻译：本发明涉及式I化合物：其中R 1表示萘基，二氢萘基，四氢萘基，喹啉基或1,4-苯并二恶烷基，A表示单键，双键，亚甲基，式z1的基团：-CH =（z1）或式z2的基团：= CH-（z2）环B表示哌啶基，吡咯烷基或1,2,3,6 并且R 2表示：氢原子，苄基或具有1至6个碳原子的烷基，条件是在这些情况之一中，R 1不同于萘基（y1），二氢萘基（y2）或四氢萘基（y3）基团，B不是哌啶基或具有1-6个碳原子的氨基烷基，具有1至6个碳原子的氰基烷基或式w1的基团：其中其中 n为1-6，R 4表示氢原子，卤素原子，碳原子数1〜6的烷基或烷氧基其具有1至6个碳原子，以及它们与药学上可接受的无机或有机酸的加成盐，以及含有它们的药物。

8. 发明授权

US5250544A New piperidine tetrahydropyridine and pyrrolidine compounds 失效
标题翻译：新的哌啶，四氢吡啶和吡咯烷化合物
公开(公告)号：US5250544A
公开(公告)日：1993-10-05
申请号：US723757
申请日：1991-07-01
申请人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
发明人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/47 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D207/06 , C07D207/08 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D295/13 , C07D295/185 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D211/06
CPC分类号： C07D295/185 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D401/04 , C07D405/04
摘要： The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.4 represents a hydrogen atom, a halogen atom, an alkyl radical having 1 to 6 carbon atoms, or an alkoxy radical having 1 to 6 carbon atoms , and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, and medicaments containing the same.
摘要翻译：本发明涉及式I化合物：其中R 1表示萘基，二氢萘基，四氢萘基，喹啉基或1,4-苯并二恶烷基，A表示单键，双键，亚甲基，式z1的基团：-CH =（z1）或式z2的基团：= CH-（z2）环B表示哌啶基，吡咯烷基或1,2,3,6 并且R 2表示：氢原子，苄基或具有1至6个碳原子的烷基，条件是在这些情况之一中，R 1不同于萘基（y1），二氢萘基（y2）或四氢萘基（y3）基团，B不是哌啶基或具有1-6个碳原子的氨基烷基，具有1至6个碳原子的氰基烷基或式w1的基团：其中其中 n为1-6，R 4表示氢原子，卤素原子，碳原子数1〜6的烷基或烷氧基其具有1至6个碳原子，以及它们与药学上可接受的无机或有机酸的加成盐，以及含有它们的药物。

9. 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。

10. 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。

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