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21. 发明授权

US06569858B2 12,13-(pyranosyl)-indolo[2,3-a]pyrrolo[3,4-c]carbazole and 12,13-(pyranosyl)-furo[3,4-c]indolo[2,3-a]carbazoles 失效
标题翻译： 12,13-（吡喃糖基） - 吲哚并[2,3-a]吡咯并[3,4-c]咔唑和12,13-（吡喃糖基） - 呋喃并[3,4-c]吲哚并[2,3-a] 咔唑
公开(公告)号：US06569858B2
公开(公告)日：2003-05-27
申请号：US10010379
申请日：2001-11-05
申请人： Michelle Prudhomme , Pascale Moreau , Fabrice Anizon , Christelle Marminon , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
发明人： Michelle Prudhomme , Pascale Moreau , Fabrice Anizon , Christelle Marminon , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
IPC分类号： C07D49044
CPC分类号： C07H19/23
摘要： A compound selected from those of formula (I): wherein: R1 and R2, which may be identical or different, represent a group of formula U-V wherein U represents single bond, or alkylene which is optionally substituted and/or unsaturated, and V is as defined in the description, G represents oxygen, or NR3 wherein R3 is as defined in the description, X represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y represents hydrogen, or X+Y represents carbonyl, X1 represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1 represents hydrogen, or X1+Y1 represents carbonyl, R4, R5, and R6 are as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of cancer.
摘要翻译：选自式（I）的化合物：其中：R 1和R 2可以相同或不同，表示其中U表示单键的式UV基团，或任选被取代和/或不饱和的亚烷基，V是 G表示氧或NR 3，其中R3如说明书中所定义，X表示氢，羟基，烷氧基，巯基或烷硫基，Y表示氢，或X + Y表示羰基，X1表示氢，羟基，烷氧基，巯基或烷硫基，Y1表示氢，或X1 + Y1表示羰基，R4，R5和R6如说明书中所定义，其异构体及其药学上可接受的酸或碱加成盐，以及含有它们的药物可用于治疗癌症。

22. 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。

23. 发明授权

US06503919B1 Compounds of 7-oxo-2,3,7,14-tetrahydro-1H-benzo[b]pyrano[3,2-h]acridin carboxylate 失效
标题翻译： 7-氧代-2,3,7,14-四氢-1H-苯并[b]吡喃并[3,2-h]吖啶羧酸酯的化合物
公开(公告)号：US06503919B1
公开(公告)日：2003-01-07
申请号：US09594853
申请日：2000-06-15
申请人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
发明人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
IPC分类号： C07D491052
CPC分类号： C07D491/04
摘要： A compound selected from those of formula (I): wherein: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted amino, R3 and R4 represent hydrogen, or alkyl, R5 and R6 represent —O—CO—U—V wherein U and V are as defined in the description, or Z as defined in the description, it being understood that at least one of the R5 and R6 groups represents —O—CO—U—V, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.
摘要翻译：选自式（I）的化合物：其中：X和Y表示氢，卤素，羟基，巯基，氰基，硝基，烷基，烷氧基，三卤代烷基，任选取代的氨基，亚甲二氧基或亚乙二氧基，，R 2表示氢，羟基，烷基，烷氧基，烷基羰基氧基或任选取代的氨基，R 3和R 4表示氢或烷基，R 5和R 6表示-O-CO-UV，其中U和V如说明书中所定义，或Z 可以理解的是，R 5和R 6基团中的至少一个表示-O-CO-UV，它们的异构体，N-氧化物及其药学上可接受的酸或碱加成盐，以及含有相同的可用于治疗癌症。

24. 发明授权

US06307068B1 Artemisinin derivatives, method for the preparation thereof and pharmaceutical compositions containing the same 失效
标题翻译：青蒿素衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US06307068B1
公开(公告)日：2001-10-23
申请号：US09719767
申请日：2000-12-14
申请人： Ying Li , Feng Shan , Jin Ming Wu , Guangshao Wu , Jian Ding , Jianxian Han , Ghanem Atassi , Pierre Renard
发明人： Ying Li , Feng Shan , Jin Ming Wu , Guangshao Wu , Jian Ding , Jianxian Han , Ghanem Atassi , Pierre Renard
IPC分类号： C07D49318
CPC分类号： C07D493/18 , C07D493/20
摘要： The invention relates to compound of the general formula (I): R—O—A (I) wherein: R represents the radical of formula (II): A is as defined in the description, and medicinal products containing the same which are useful in treating or in preventing cancer.
摘要翻译：本发明涉及通式（I）的化合物：其中：R表示式（II）的基团：A如说明书中所定义，含有该化合物可用于治疗或预防癌症的药物。

25. 发明授权

US6162811A Ellipticine compounds 失效
标题翻译：椭圆形化合物
公开(公告)号：US6162811A
公开(公告)日：2000-12-19
申请号：US999364
申请日：1997-12-29
申请人： Claude Guillonneau , Yves Charton , Emile Bisagni , Ghanem Atassi , Alain Pierre , Nicolas Guilbaud
发明人： Claude Guillonneau , Yves Charton , Emile Bisagni , Ghanem Atassi , Alain Pierre , Nicolas Guilbaud
IPC分类号： A61K31/435 , A61P35/00 , C07D471/04 , A61K31/4745
CPC分类号： C07D471/04
摘要： The compounds of formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and A are as defined in the description, their optical isomers and N-oxides, and pharmaceutically acceptable addition salts thereof with an acid or base, and the use thereof as anti-tumor agents.
摘要翻译：下式的化合物：其中R1，R2，R3，R4，R5，R6，R7，R8和A如说明书中所定义，它们的光学异构体和N-氧化物及其与酸或碱的药学上可接受的加成盐，及其作为抗肿瘤剂的用途。

26. 发明授权

US6063816A Hydroxamic acid compounds 失效
标题翻译：羟肟酸化合物
公开(公告)号：US6063816A
公开(公告)日：2000-05-16
申请号：US370712
申请日：1999-08-09
申请人： Stephen Hanessian , Ghanem Atassi , Gordon Tucker , Daniel-Henri Caignard , Pierre Renard
发明人： Stephen Hanessian , Ghanem Atassi , Gordon Tucker , Daniel-Henri Caignard , Pierre Renard
IPC分类号： C12N9/99 , A61K31/18 , A61K31/185 , A61K31/35 , A61K31/351 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61P43/00 , C07C319/14 , C07C319/20 , C07C323/60 , C07D211/20 , C07D213/34 , C07D309/04 , A01N37/28 , A01K31/19 , A01N43/40 , C07C259/04 , C07D211/32
CPC分类号： C07C323/60
摘要： A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y, or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.
摘要翻译：酰基，环烷基，芳基，氨基羰基烷基或杂环，R 2表示亚烷基，R 3表示如说明书中所定义的X或Y，R 4表示 - 烷基，当R 3表示Y时，环烷基，芳基，芳基烷基，环烷基烷基，杂环亚烷基或杂环，或当R 3表示X或Y时，联芳基，芳基杂芳基或杂芳基芳基，它们的异构体及其药学上可接受的酸或碱加成盐，它们在金属蛋白酶抑制剂治疗癌症中是有用的。

27. 发明授权

US5866587A Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US5866587A
公开(公告)日：1999-02-02
申请号：US842982
申请日：1997-04-25
申请人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
发明人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/42 , C07D217/26 , C07D221/08 , C07D221/10 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D471/04 , C07D209/42 , C07D217/26 , C07D221/10 , C07D491/04 , C07D495/04
摘要： Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.
摘要翻译：式（I）化合物：其中：m，n相同或不同，表示0,1或2，相同或不同的R 1，R 2表示氢，任选取代的烷基，芳基或与其中带有羰基或（C3-C7）环烷基的碳原子形成，R3表示氢，烷基，羟基或芳基，R4表示说明中定义的任何基团，X表示-SO 2 - ， - 或-SO 2 NH-，R 5表示任选取代的烷基，（C 3 -C 7）环烷基，芳基或杂环，A表示芳基环或杂环，其异构体以及其与药学上可接受的酸或碱的加成盐和含有这同样可用作金属蛋白酶抑制剂。

28. 发明授权

US5405948A 1,5-diyne-3-cycloalkene compounds 失效
标题翻译： 1,5-二炔-3-环烯烃化合物
公开(公告)号：US5405948A
公开(公告)日：1995-04-11
申请号：US954004
申请日：1992-09-30
申请人： Jean-Marie Beau , Christophe Crevisy , Ghanem Atassi , Alain Pierre
发明人： Jean-Marie Beau , Christophe Crevisy , Ghanem Atassi , Alain Pierre
IPC分类号： C07C35/205 , C07C69/013 , C07H15/24 , C07C43/20 , C07C67/02
CPC分类号： C07C35/205 , C07C69/013
摘要： A compound of formula (I): selected from 1,5-diyne-3-cyclodecene and undecene compounds. ##STR1## in which: R represents a hydrogen atom, a straight-chain or branched (C.sub.1 -C.sub.6) acyl radical or a glycoside radical,R' represents a hydrogen atom ##STR2## n is 1 or 2, and R.sub.1 and R.sub.2 simultaneously represent two hydrogen atoms or, together with the two carbon atoms and the double bond to which they are attached, form a phenyl ring.
摘要翻译：式（I）化合物：选自1,5-二炔-3-环癸烯和十一碳烯化合物。（I）其中：R表示氢原子，直链或支链（C1-C6）酰基或糖苷基，R'表示氢原子，n为1或2，R1 并且R2同时表示两个氢原子，或者与它们所连接的两个碳原子和双键一起形成苯环。

29. 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。

30. 发明授权

US06627650B2 Indenoindolone compounds 失效
标题翻译：茚并吲哚酮化合物
公开(公告)号：US06627650B2
公开(公告)日：2003-09-30
申请号：US10171191
申请日：2002-06-13
申请人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Ghanem Atassi , John Hickman , Alain Pierre , Stéphane Leonce , Nicolas Guilbaut , Laurence Kraus-Berthier
发明人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Ghanem Atassi , John Hickman , Alain Pierre , Stéphane Leonce , Nicolas Guilbaut , Laurence Kraus-Berthier
IPC分类号： A61K3140
CPC分类号： C07D401/12 , C07D209/94 , C07D405/12 , C07D409/12 , C07D491/04
摘要： A compound of formula (I): wherein: R represents hydrogen, optionally substituted alkyl or alkenyl, R1 to R8, which may be identical or different, each represents hydrogen, optionally substituted alkyl, hydroxy, acyloxy, optionally substituted amino, carboxy, optionally substituted alkoxy, or alkenyloxy, or one of R1 to R8 forms, with another of R1 to R8 that is adjacent, an alkylenedioxy group, X represents oxygen or NR16 wherein R16 represents hydrogen, alkyl, aryl or arylalkyl, R9 represents hydrogen, aryl, heteroaryl, or optionally substituted, saturated or unsaturated alkyl, an isomer thereof, or an addition salt thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as anti-cancer agents.
摘要翻译：式（I）的化合物：其中：R表示氢，任选取代的烷基或烯基，可以相同或不同的R 1至R 8各自表示氢，任选取代的烷基，羟基，酰氧基，任选取代的氨基，羧基，任选地取代的烷氧基或烯氧基，或R 1至R 8中的一个与相邻的R 1至R 8中的另一个相邻，亚烷基二氧基，X表示氧或NR 16，其中R16表示氢，烷基，芳基或芳烷基，R9表示氢，杂芳基或任选取代的饱和或不饱和的烷基，其异构体或其加成盐与药学上可接受的酸或碱的混合物。含有该化合物的药物可用作抗癌剂。

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