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1. 发明申请

WO2005000843A3 BENZOTHIAZOLE-4,7-DIONES AND BENZOXAZOLE-4,7-DIONES WITH SUBSTITUENTS IN POSITION 5 OR 6 AND METHOD FOR PRODUCTION THEREOF 审中-公开
标题翻译：苯并噻唑-4,7-二酮和苯并噻唑-4,7-二酮与位置5或6中的取代基及其生产方法
公开(公告)号：WO2005000843A3
公开(公告)日：2005-05-26
申请号：PCT/FR2004001578
申请日：2004-06-24
申请人： SOD CONSEILS RECH APPLIC , GALCERA CONTOUR MARIE-ODILE , LAVERGNE OLIVIER
发明人： GALCERA CONTOUR MARIE-ODILE , LAVERGNE OLIVIER
IPC分类号： A61P3/10 , A61P17/14 , A61P25/28 , A61P31/00 , A61P35/00 , A61P37/00 , C07D277/66 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/423 , A61K31/428 , C07D263/56 , C07D263/57 , C07D277/64 , C07D413/04
CPC分类号： C07D417/04 , C07D277/66 , C07D417/12 , C07D417/14
摘要： The invention relates to a targetted production method for benzothiazole-4,7-dione and benzoxazole-4,7-dione derivatives, mono-substituted in the 5 or 6 position with an amino group, itself optionally substituted. Said derivatives are Cdc25 phosphatase inhibitors and may be used for the production of medicaments for the treatment of cancer. Also disclosed are synthetic intermediates used in the above production. The invention particularly relates to the following benzothiazole-4,7-dione derivatives: 2-(2-chloro-6-fluorophenyl)-5-{[2-(dimethylamino)ethyl]amino }-1,3-benzothiazole-4,7-dione and 2-(2-chloro-6-fluorophenyl)-5-[(2-pyrrolidin-1-ylethyl)amino]-1,3-benzothiazole-4,7-dione.
摘要翻译：本发明涉及苯并噻唑-4,7-二酮和苯并恶唑-4,7-二酮衍生物的靶向制备方法，其在5或6位被单取代，具有氨基，本身任选被取代。所述衍生物是Cdc25磷酸酶抑制剂，可用于制备用于治疗癌症的药物。还公开了在上述生产中使用的合成中间体。本发明特别涉及以下苯并噻唑-4,7-二酮衍生物：2-（2-氯-6-氟苯基）-5 - {[2-（二甲基氨基）乙基]氨基} -1,3-苯并噻唑-4，（2-氯-6-氟苯基）-5 - [（2-吡咯烷-1-基乙基）氨基] -1,3-苯并噻唑-4,7-二酮。

2. 发明专利

PL202393B1 Analogi kamptotecyny, kompozycja farmaceutyczna je zawierająca i zastosowanie 未知
公开(公告)号：PL202393B1
公开(公告)日：2009-06-30
申请号：PL36133400
申请日：2000-02-24
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , BIGG DENNIS , LANCO CHRISTOPHE , ROLLAND ALAIN
IPC分类号： C07D491/22 , A61K31/435 , A61P31/12 , A61P33/00 , A61P35/00

3. 发明专利

NO327260B1 未知
公开(公告)号：NO327260B1
公开(公告)日：2009-05-25
申请号：NO20014117
申请日：2001-08-24
申请人： SOD CONSEILS RECH APPLIC
发明人： ROLLAND ALAIN , LAVERGNE OLIVIER , LANCO CHRISTOPHE , BIGG DENNIS C H
IPC分类号： C07D491/22 , A61K31/435 , A61P31/12 , A61P33/00 , A61P35/00
摘要： Camptothecin analogs (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. Camptothecin analogs of formula (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. R1 = lower alkyl; R2-R5 = H, halo or -OSO2R10; R6 = H, 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl, cycloalkyl- lower alkyl, nitro, halo, -(CH2)m-SiR7R8R9, aryl or aryl-lower alkyl (both optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3); R7-R9 = lower alkyl; R10 = lower alkyl (optionally substituted with at least one halo) or aryl (optionally substituted with at least one lower alkyl); m = 0-6; and provided that R2 is H, when R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3, and/or when one of R3-R5 is -OSO2R10; or that one of R2-R5 is -OSO2R10 and/or R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3 and/or R2 is halo. Independent claims are also included for: (1) the preparation of (III); (2) a compound of formula (M); and (3) the preparation of (M). R'6 = 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl- lower alkyl, -(CH2)m-SiR7R8R9 or aryl-lower alkyl (optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3).

4. 发明专利

DE60221570T2 未知
公开(公告)号：DE60221570T2
公开(公告)日：2008-04-17
申请号：DE60221570
申请日：2002-12-24
申请人： SOD CONSEILS RECH APPLIC
发明人： GALCERA CONTOUR MARIE-ODILE , LAVERGNE OLIVIER , BREZAK PANNETIER MARIE-CHRISTI , PREVOST GREGOIRE
IPC分类号： C07D277/64 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61P17/14 , A61P25/28 , A61P29/00 , A61P31/12 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D263/56 , C07D263/57 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00
摘要： The invention concerns the use as cdc25 phosphatase inhibitors, in particular cdc25-C phosphatase, and CD45 phosphatase, of compounds of general formula (I), wherein: W represents O or S. In accordance with the invention, the compounds of general formula (I) can in particular be used for preparing a medicine for cancer treatment.

5. 发明专利

DE60033447T2 未知
公开(公告)号：DE60033447T2
公开(公告)日：2007-10-31
申请号：DE60033447
申请日：2000-02-24
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , BIGG DENNIS , LANCO CHRISTOPHE , ROLLAND ALAIN
IPC分类号： C07D491/22 , A61K31/435 , A61K31/47 , A61P31/12 , A61P33/00 , A61P35/00
摘要： Camptothecin analogs (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. Camptothecin analogs of formula (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. R1 = lower alkyl; R2-R5 = H, halo or -OSO2R10; R6 = H, 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl, cycloalkyl- lower alkyl, nitro, halo, -(CH2)m-SiR7R8R9, aryl or aryl-lower alkyl (both optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3); R7-R9 = lower alkyl; R10 = lower alkyl (optionally substituted with at least one halo) or aryl (optionally substituted with at least one lower alkyl); m = 0-6; and provided that R2 is H, when R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3, and/or when one of R3-R5 is -OSO2R10; or that one of R2-R5 is -OSO2R10 and/or R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3 and/or R2 is halo. Independent claims are also included for: (1) the preparation of (III); (2) a compound of formula (M); and (3) the preparation of (M). R'6 = 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl- lower alkyl, -(CH2)m-SiR7R8R9 or aryl-lower alkyl (optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3).

6. 发明专利

DE60033447D1 未知
公开(公告)号：DE60033447D1
公开(公告)日：2007-03-29
申请号：DE60033447
申请日：2000-02-24
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , BIGG DENNIS , LANCO CHRISTOPHE , ROLLAND ALAIN
IPC分类号： C07D491/22 , A61K31/435 , A61K31/47 , A61P31/12 , A61P33/00 , A61P35/00
摘要： Camptothecin analogs (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. Camptothecin analogs of formula (I) or 91 compounds (e.g. (5R)-5-ethyl-9-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione or (5R)-5-ethyl-11-fluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7) indolizino(1,2-b)quinoline-3,15-dione) are new. R1 = lower alkyl; R2-R5 = H, halo or -OSO2R10; R6 = H, 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl, cycloalkyl- lower alkyl, nitro, halo, -(CH2)m-SiR7R8R9, aryl or aryl-lower alkyl (both optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3); R7-R9 = lower alkyl; R10 = lower alkyl (optionally substituted with at least one halo) or aryl (optionally substituted with at least one lower alkyl); m = 0-6; and provided that R2 is H, when R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3, and/or when one of R3-R5 is -OSO2R10; or that one of R2-R5 is -OSO2R10 and/or R6 is 7-12C alkyl, -(CH2)m-SiR7R8R9 or aryl substituted with di(lower alkyl)amino or OCF3 and/or R2 is halo. Independent claims are also included for: (1) the preparation of (III); (2) a compound of formula (M); and (3) the preparation of (M). R'6 = 1-12C alkyl (optionally substituted with at least one halo), lower hydroxyalkyl, lower alkoxy- lower alkyl, cycloalkyl- lower alkyl, -(CH2)m-SiR7R8R9 or aryl-lower alkyl (optionally substituted on aryl with lower alkyl, OH, halo, amino, lower alkylamino, di(lower alkyl) amino, CF3 or OCF3).

7. 发明专利

ES2260417T3 DERIVADOS DE MIKANOLIDA, SU PREPARACION Y SUS APLICACIONES TERAPEUTICAS. 未知
公开(公告)号：ES2260417T3
公开(公告)日：2006-11-01
申请号：ES02710969
申请日：2002-01-11
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , LANCO CHRISTOPHE , PREVOST GREGOIRE , TENG BENG POON
IPC分类号： A61K31/34 , A61K31/343 , A61P9/10 , A61P13/08 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07D493/18
摘要： Un compuesto de la **fórmula**, en la que R1 representa un átomo de hidrógeno o un radical SR4 o NR4R5; R2 representa SR6 o NR6R7; R3 representa OH, O(CO)R14, OSiR15R16R17, O(CO)OR18 o O(CO)NHR18; R4 y R6 representan, independientemente, un radical alquilo, un radical cicloalquilo, cicloalquilalquilo, hidroxialquilo o también uno de los radicales arilo o aralquilo opcionalmente sustituidos sobre su grupo arilo con uno o más radicales elegidos entre los radicales alquilo, hidroxi o alcoxi, R5 y R7 representan, independientemente, un átomo de hidrógeno, un radical alquilo, un radical cicloalquilo, cicloalquilalquilo, hidroxialquilo o también uno de los radicales arilo o aralquilo opcionalmente sustituidos sobre su grupo arilo con uno o más radicales elegidos entre los radicales alquilo, hidroxi o alcoxi, o una sal de un compuesto de la fórmula general.

8. 发明专利

AT312105T 未知
公开(公告)号：AT312105T
公开(公告)日：2005-12-15
申请号：AT02077736
申请日：1996-06-21
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , PLA RODAS FRANCESC , POMMIER JACQUES , ULIBARRI GERARD
IPC分类号： A61K31/47 , A61K31/4745 , A61K31/475 , A61K31/496 , A61K31/5377 , A61P31/12 , A61P33/00 , A61P33/02 , A61P35/00 , A61P43/00 , C07D209/00 , C07D213/02 , C07D213/61 , C07D213/64 , C07D213/66 , C07D215/08 , C07D221/00 , C07D313/00 , C07D413/10 , C07D471/14 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/22 , C07D498/14 , C07D215/18
摘要： Camptothecin analogues where the camptothecin hydroxy lactone is: (i) a beta -hydroxy lactone; or (ii) the corresp. beta -hydroxy acid resulting from ring-opening of the aforementioned lactone; or a (iii) deriv. of the beta -hydroxy acid in (ii) or its one of its salts. Also claimed are new industrial prods. of formula (M) and (A). R1 = lower alkyl, lower alkenyl, lower alkynyl, halo(lower alkyl), lower alkoxy(lower alkyl) or lower alkylthio(lower alkyl); R20 = H or halo; R22 = F, Cl, or lower alkoxy; R23 = prim. hydroxy-protecting gp.; and R18, R19 = H, halo, lower alkyl, lower alkoxy or OH.

9. 发明专利

FR2819513B1 未知
公开(公告)号：FR2819513B1
公开(公告)日：2005-06-17
申请号：FR0100397
申请日：2001-01-12
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , LANCO CHRISTOPHE , PREVOST GREGOIRE , TENG BENG POON
IPC分类号： A61P31/12 , A61P33/00 , A61P35/00 , C07D493/18 , C07D493/16 , A61K31/343 , A61K31/4025 , A61K31/4525 , A61K31/5377 , A61K31/695 , C07D493/22 , C07F7/18

10. 发明专利

HK1063793A1 Mikanolide derivatives, their preparation and therapeutic uses 未知
公开(公告)号：HK1063793A1
公开(公告)日：2005-01-14
申请号：HK04106637
申请日：2004-09-03
申请人： SOD CONSEILS RECH APPLIC
发明人： LAVERGNE OLIVIER , LANCO CHRISTOPHE , PREVOST GREGOIRE , TENG BENG POON
IPC分类号： A61P31/12 , A61P33/00 , A61P35/00 , C07D493/18 , C07D , A61K , A61P

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