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1. 发明授权

US5567707A Acronycine analogues 失效
标题翻译：阿司匹林类似物
公开(公告)号：US5567707A
公开(公告)日：1996-10-22
申请号：US389798
申请日：1995-02-16
申请人： Michel Koch , Fran.cedilla.ois Tillequin , Alexios-Leandros Skaltsounis , Yves Rolland , Alain Pierre , Ghanem Atassi
发明人： Michel Koch , Fran.cedilla.ois Tillequin , Alexios-Leandros Skaltsounis , Yves Rolland , Alain Pierre , Ghanem Atassi
IPC分类号： A61K31/47 , A61P35/00 , C07D491/04 , C07D491/052 , C07D491/14 , C07D491/153
CPC分类号： C07D491/04 , C07D491/14
摘要： Compounds of formula (I): ##STR1## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and Y are defined in the description.Those compounds are used therapeutically in the treatment of cancerous tumours.
摘要翻译：式（I）化合物：其中R 3，R 4，R 5，R 6，X和Y在说明书中定义。那些化合物治疗性地用于癌性肿瘤。

2. 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。

3. 发明授权

US06288073B1 Acronycine derivatives, preparation method and pharmaceutical compositions 失效
标题翻译： Acronycine衍生物，制备方法和药物组合物
公开(公告)号：US06288073B1
公开(公告)日：2001-09-11
申请号：US09581853
申请日：2000-06-19
申请人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
发明人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
IPC分类号： A61K314741
CPC分类号： C07D491/04 , C07D491/14
摘要： A compound selected from those of formula (I): in which: 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 ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, 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，烷基，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，R3和R4表示氢或烷基，A表示-CH = CH-或-CH（R5）-CH（R6） - ，其中R5 和R6如说明书中所定义，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，以及其可用于治疗癌症的药物。

4. 发明授权

US06548515B1 Dihydrofuro[3,4-b]quinolin-1-one compounds 失效
标题翻译：二氢呋喃并[3,4-b]喹啉-1-酮化合物
公开(公告)号：US06548515B1
公开(公告)日：2003-04-15
申请号：US09718917
申请日：2000-11-22
申请人： Henri-Philippe Husson , Sylviane Giorgi-Renault , Christophe Tratrat , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
发明人： Henri-Philippe Husson , Sylviane Giorgi-Renault , Christophe Tratrat , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
IPC分类号： A61K314741
CPC分类号： C07D491/04 , C07D219/06 , C07D221/16 , C07D221/18 , C07D491/14 , C07D495/04
摘要： The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same are useful in the treatment of cancer.
摘要翻译：本发明涉及式（I）的化合物：其中：表示单键或双键，R 0表示氢或羟基或烷氧基，R 1和R 2相同或不同，各自表示氢或卤素或烷基，烷氧基，羟基，多卤代烷基，硝基或任选取代的氨基或其中m表示1≤= m = 4的整数，或与带有带有5至12个环成员的芳族或非芳族单环或双环基团的碳原子一起形成，并且任选地含有1或 2个选自O，S和N的杂原子，R 3表示氢或芳基，杂芳基，环烷基，任选取代的烷基或式COR7基团，其中R7表示芳基，任选取代的烷基，任选取代的氨基或OR 10，其中R 10表示芳基或任选地取代的烷基，X表示氧或硫或-CH 2 - 或-CH 2-CH 2 - ，Ar表示芳基，杂芳基或芳基烷基，其光学异构体，其水合物，溶剂合物，以及其与药学上可接受的酸的加成盐。含有它们的医药产品可用于治疗癌症。

5. 发明授权

US6071945A 8H-thieno-[2,3-b]pyrrolizin-8-one compounds 失效
标题翻译： 8H-噻吩并[2,3-b]吡咯啉-8-酮化合物
公开(公告)号：US6071945A
公开(公告)日：2000-06-06
申请号：US361064
申请日：1999-07-26
申请人： Sylvain Rault , Cecile Enguehard , Jean-Charles Lancelot , Max Robba , Ghanem Atassi , Alain Pierre , Daniel-Henri Caignard , Pierre Renard
发明人： Sylvain Rault , Cecile Enguehard , Jean-Charles Lancelot , Max Robba , Ghanem Atassi , Alain Pierre , Daniel-Henri Caignard , Pierre Renard
IPC分类号： A61K31/00 , A61K31/40 , A61K31/407 , A61P35/00 , C07D495/14
CPC分类号： C07D495/14 , Y02P20/55
摘要： A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents hydrogen, halogen, alkyl, nitro, hydroxy, alkoxy, trihaloalkyl, trihaloalkoxy or optionally substituted amino,R.sub.2 represents optionally substituted aryl or heteroaryl,R.sub.3 represents hydrogen, halogen, alkyl, nitro, hydroxy, alkoxy, trihaloalkyl, trihaloalkoxy or optionally substituted amino,their isomers and addition pharmaceutically-acceptable acid or base 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表示氢，卤素，烷基，硝基，羟基，烷氧基，三卤代烷基，三卤代烷氧基或任选取代的氨基，R 2表示任选取代的芳基或杂芳基，R 3表示氢，硝基，羟基，烷氧基，三卤代烷基，三卤代烷氧基或任选取代的氨基，它们的异构体及其加成药学上可接受的酸或碱盐和含有它们的药物可用于治疗癌症。

6. 发明授权

US5595976A Tetrahydropyran compounds 失效
标题翻译：四氢吡喃化合物
公开(公告)号：US5595976A
公开(公告)日：1997-01-21
申请号：US521189
申请日：1995-08-30
申请人： David Billington , Gilbert Dorey , Pascale Leon , Ghanem Atassi , Alain Pierre , Michael Burbridge , Nicolas Guilbaud
发明人： David Billington , Gilbert Dorey , Pascale Leon , Ghanem Atassi , Alain Pierre , Michael Burbridge , Nicolas Guilbaud
IPC分类号： C07H9/02 , A61K31/70 , A61K31/7028 , A61P9/00 , A61P29/00 , A61P35/00 , C07H9/04 , C07H15/04 , C07H15/10 , C07H15/18 , C07H15/26 , A61K37/00 , C07H3/00
CPC分类号： C07H9/04 , C07H15/04 , C07H15/10 , C07H15/26
摘要： A compound selected from those of formula (I): ##STR1## in which: A either represents --OR.sub.6, and B represents --CH.sub.2 --X,or, together with B and the carbon atom carrying them, forms an oxygen-containing heterocycle selected from oxirane, 2,2-dimethyl[1,3]dioxolane and [1,3]dioxolan-2-one,and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and X are as defined in the description.
摘要翻译：选自式（I）的化合物：其中：A表示-OR6，B表示-CH2-X，或者与B和携带它们的碳原子一起形成氧 - 含有杂环的环氧乙烷，2,2-二甲基[1,3]二氧戊环和[1,3]二氧戊环-2-酮，R1，R2，R3，R4，R5，R6和X如说明书中所定义。

7. 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。

8. 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。

9. 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。

10. 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。

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