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1. 发明授权

US4975455A New heteroarotinoid compounds 失效
标题翻译：新型类似物类化合物
公开(公告)号：US4975455A
公开(公告)日：1990-12-04
申请号：US336224
申请日：1989-04-11
申请人： Jean-Daniel Brion , Guillaume Le Baut , Patrick Ducrey , Sylvie Piessard-Robert , Claude Cudennec , Genevieve Seurre
发明人： Jean-Daniel Brion , Guillaume Le Baut , Patrick Ducrey , Sylvie Piessard-Robert , Claude Cudennec , Genevieve Seurre
IPC分类号： A61K31/35 , A61K31/352 , A61P35/00 , C07D311/04 , C07D311/58
CPC分类号： C07D311/58
摘要： Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.
摘要翻译：通式（I）的化合物：其中：R表示氢原子，卤素原子或羟基，低级烷基，低级烷氧基，羧基，（低级烷氧基）羰基，（低级芳基烷氧基）羰基，氨基羰基，（低级单或二烷基）氨基羰基或（低级芳基烷基）氨基羰基，被杂环基取代的氨基羰基，或硫代（低级烷基）硫基，磺酰基或（低级烷基）磺酰基，R1，R2，R3 和可以相同或不同的R 4表示任选被一个或多个卤素原子取代的氢原子，卤素原子或低级烷基，低级链烯基，低级烷氧基或低级链烯氧基，它们的异构体，对映体，非对映异构体，以及当R表示羧基时，其与药学上可接受的碱的加成盐，当R含有碱性基团时，其与药学上可接受的酸的加成盐。

2. 发明授权

US4975454A Triene compounds having a chromene structure 失效
标题翻译：具有色烯结构的三烯化合物
公开(公告)号：US4975454A
公开(公告)日：1990-12-04
申请号：US336225
申请日：1989-04-11
申请人： Jean-Daniel Brion , Guillaume Le Baut , Patrick Ducrey , Sylvie Piessard-Robert , Claude Cudennec , Genevieve Seurre
发明人： Jean-Daniel Brion , Guillaume Le Baut , Patrick Ducrey , Sylvie Piessard-Robert , Claude Cudennec , Genevieve Seurre
IPC分类号： A61K31/35 , A61K31/352 , A61P35/00 , C07D311/04 , C07D311/58
CPC分类号： C07D311/58
摘要： Compounds of general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,R.sub.5 denotes a carboxyl, (lower alkyloxy)carbonyl, (lower alkenyloxy)carbonyl or (lower alkynyloxy)-carbonyl,their isomers, stereoisomers and diastereoisomers, and also their addition salts with a pharmaceutically acceptable base.Medicinal products.
摘要翻译：通式（I）的化合物：其中：R1，R2，R3和R4可以相同或不同，表示氢原子，卤原子或低级烷基，低级烯基，低级烷氧基或低级烯氧基 R 5表示羧基，（低级烷氧基）羰基，（低级链烯氧基）羰基或（低级炔氧基） - 羰基，它们的异构体，立体异构体和非对映异构体，以及它们与药学上的加成盐可接受的基数。药用产品。

3. 发明授权

US4567169A Nitrosourea substituted phosphonates and pharmaceutical use 失效
标题翻译：硝基脲取代膦酸盐和药物用途
公开(公告)号：US4567169A
公开(公告)日：1986-01-28
申请号：US547881
申请日：1983-11-02
申请人： Gilbert Lavielle , Claude Cudennec
发明人： Gilbert Lavielle , Claude Cudennec
IPC分类号： A61K31/66 , A61K31/67 , A61K31/675 , A61P31/04 , A61P35/00 , C07C275/68 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/6553 , C07F9/6558 , C07F9/58
CPC分类号： C07F9/3808 , C07F9/4006
摘要： New nitrosourea compounds that can be used as medicaments and correspond to the general formula I ##STR1## in which R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, thienyl, or phenyl which may carry substituents,R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or benzyl which may carry substituents, orR.sub.2 and R.sub.3 together represent --(CH.sub.2).sub.m --, m being 3 or 4.Pharmaceutical compositions; therapeutic administration especially for the treatment of tumours.
摘要翻译：可用作药物并且对应于通式I（I）的新的亚硝基脲化合物，其中R 1是氢，C 1 -C 6烷基或苯基，R 2是氢，C 1 -C 6烷基，噻吩基或苯基，携带取代基，R 3是氢，可以带有取代基的C 1 -C 6烷基或苄基，或者R 2和R 3一起表示 - （CH 2）m - ，m为3或4。特别是用于治疗肿瘤的治疗性给药。

4. 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。

5. 发明授权

US4605647A Oxaazaphosphorine compounds and pharmaceutical compositions 失效
标题翻译：奥氮平磷化合物和药物组合物
公开(公告)号：US4605647A
公开(公告)日：1986-08-12
申请号：US752365
申请日：1985-07-05
申请人： Gilbert Lavielle , Claude Cudennec
发明人： Gilbert Lavielle , Claude Cudennec
IPC分类号： A61K31/675 , A61P35/00 , C07F9/24 , C07F9/6584 , A61K31/66 , C07F9/65
CPC分类号： C07F9/65846
摘要： New oxaazaphosphorine compounds corresponding to the formula: ##STR1## in which R is alkyl, cycloalkyl or alkoxy,phenyl, phenylalkyl, phenoxy or thiophenoxy in which the phenyl ring may be substituted by alkyl or alkoxy or by halogen.mono- or di-alkylamino optionally mono- or di-substituted by halogen, orpyrrolidinyl, piperidyl or morpholinyl or optionally substituted piperazinyl.These compounds may be used for antineoplastic therapy especially in the treatment of tumors.
摘要翻译：对应于下式的新的氮杂磷杂环丁烷化合物：其中R是烷基，环烷基或烷氧基，苯基，苯基烷基，苯氧基或硫代苯氧基，其中苯环可被烷基或烷氧基取代或被卤素取代。任选被卤素或吡咯烷基，哌啶基或吗啉基或任选取代的哌嗪基单取代或二取代的单 - 或二 - 烷基氨基。这些化合物可用于抗肿瘤治疗，特别是用于治疗肿瘤。

6. 发明授权

US5047400A Tripeptide compounds having a nitrogenous polycyclic structure 失效
标题翻译：具有含氮多环结构的三肽化合物
公开(公告)号：US5047400A
公开(公告)日：1991-09-10
申请号：US207710
申请日：1988-06-16
申请人： Michel Vincent , Georges Remond , Bernard Portevin , Claude Cudennec
发明人： Michel Vincent , Georges Remond , Bernard Portevin , Claude Cudennec
IPC分类号： A61K38/00 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/08 , C07K5/09
CPC分类号： C07K5/0815
摘要： The invention relates to the compounds of general formula: ##STR1## in which: X denotes either an oxygen atom, or two hydrogen atoms;Y denotes either a hydrogen atom, or a hydroxyl group;or Y denotes an amino group on condition that X denotes two hydrogen atoms;R denotes a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, optionally substituted with one or more hydroxy, amino, mercapto, methylthio or carboxy groups, or aryl groups such as phenyl, pyridyl or thienyl; ##STR2## denotes a polycyclic nitrogenous structure; their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.
摘要翻译：本发明涉及以下通式的化合物：其中：X表示氧原子或两个氢原子; Y表示氢原子或羟基; 或者Y表示氨基，条件是X表示两个氢原子; R表示氢原子或具有1至6个碳原子的直链或支链烷基，任选被一个或多个羟基，氨基，巯基，甲硫基或羧基取代，或芳基如苯基，吡啶基或噻吩基 ; “IMAGE”表示多环含氮结构; 它们的对映体，差向异构体和非对映异构体，以及它们与药学上可接受的酸或碱的加成盐。

7. 发明授权

US4965250A Peptide compounds having a nitrogenous polycyclic structure 失效
标题翻译：具有含氮多环结构的肽化合物
公开(公告)号：US4965250A
公开(公告)日：1990-10-23
申请号：US148027
申请日：1988-01-25
申请人： Michel Vincent , Georges Remond , Claude Cudennec
发明人： Michel Vincent , Georges Remond , Claude Cudennec
IPC分类号： A61K38/00 , A61P37/04 , C07K1/06 , C07K1/113 , C07K5/08 , C07K5/09 , C07K5/10 , C07K5/117
CPC分类号： C07K5/1024 , C07K5/0815 , Y10S514/885
摘要： Tetrapeptide compounds of general formula: ##STR1## in which R denotes:a hydrogen atom,a straight- or branched-chain alkyl radical containing from 1 to 4 carbon atoms,an aryl radical such as phenyl or a heterocyclic aromatic radical such as thienyl, optionally substituted with a hydroxy, amino, mercapto, methylthio or lower alkyl group,a lower aralkyl radical such as benzyl,R' denotes a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms,X denotes an oxygen atom or an NH group,Y denotes an oxygen or sulfur atom when X denotes an NH group, or Y denotes an NH group when X denotes an oxygen atom,t denotes 0 or 1, ##STR2## denotes a nitrogen-containing polycyclic structure, their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.Medicinal products.
摘要翻译：具有以下通式的四肽化合物：其中R表示氢原子，含有1至4个碳原子的直链或支链烷基，芳基如苯基或杂环芳族基，如噻吩基任选被羟基，氨基，巯基，甲硫基或低级烷基取代，低级芳烷基如苄基，R'表示氢原子或含有1至4个碳原子的直链或支链烷基，X 表示氧原子或NH基，当X表示NH基时，Y表示氧或硫原子，或当X表示氧原子时，Y表示NH基，t表示0或1，表示含氮多环结构，它们的对映异构体，差向异构体和非对映异构体，以及它们与药学上可接受的酸或碱的加成盐。药用产品。

8. 发明授权

US4720484A Peptide compounds having a nitrogenous polycyclic structure 失效
标题翻译：具有含氮多环结构的肽化合物
公开(公告)号：US4720484A
公开(公告)日：1988-01-19
申请号：US933093
申请日：1986-11-20
申请人： Michel Vincent , Georges Remond , Claude Cudennec
发明人： Michel Vincent , Georges Remond , Claude Cudennec
IPC分类号： C07K5/10 , A61K38/00 , A61P35/00 , A61P37/04 , C07D209/42 , C07K5/103 , C07K5/107 , C07K5/11 , C07K5/113 , C07K5/117 , C07K16/00 , A61K37/02
CPC分类号： C07K5/1013 , C07K5/1008 , C07K5/101 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K5/1024
摘要： The invention relates to tetrapeptide derivatives of the general formula ##STR1## in which R represents a hydrogen atom, a straight-chain or branched alkyl radical containing from 1 to 5 carbon atoms, optionally substituted by a hydroxy, amino, mercapto, methylthio, methylsulphoxide, carboxy or guanidino group, or a benzyl or indol-3-ylmethyl radical optionally substituted by a hydroxy group,R.sub.1 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, ##STR2## represents a nitrogenous polycyclic structure, the enantiomers, epimers and diastereoisomers thereof, as well as to the pharmaceutically acceptable acid or base addition salts thereof.
摘要翻译：本发明涉及通式为“IMAGE”的四肽衍生物，其中R表示氢原子，含有1至5个碳原子的直链或支链烷基，任选被羟基，氨基，巯基，甲硫基，甲基亚砜，羧基或胍基，或任选被羟基取代的苄基或吲哚-3-基甲基，R1表示氢原子或含有1至4个碳原子的烷基，表示含氮多环结构，对映异构体，差向异构体和非对映异构体，以及其药学上可接受的酸或碱加成盐。

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