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1. 发明申请

WO2004069803A3 MONO-ACYLATED O-PHENYLENDIAMINES DERIVATIVES AND THEIR USE AGAINST CANCER 审中-公开
标题翻译：单酚O-邻苯二甲酸衍生物及其对癌症的使用
公开(公告)号：WO2004069803A3
公开(公告)日：2004-11-18
申请号：PCT/EP2004001044
申请日：2004-02-05
申请人： HOFFMANN LA ROCHE
发明人： FERTIG GEORG , HERTING FRANK , KUBBIES MANFRED , LIMBERG ANJA , REIFF ULRIKE , WEIDNER MICHAEL
IPC分类号： A61K31/381 , A61K31/44 , C07C233/80 , C07D213/82 , C07D213/90 , C07D333/38
CPC分类号： C07D213/82 , C07C233/80 , C07C2601/02 , C07D333/38
摘要： Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (A) wherein Ar is thiophen-2,5-diyl, pyridine-2,5-diyl, pyridine-5,2-diyl, pyridine-2,6-diyl, pyridine-2,4-diyl or 1,4-phenylene, R , R independently from each other represent hydrogen, C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, C3-12-cycloalkyl, the alkyl, alkenyl, alkynyl and cycloalkyl groups being optionally mono or multiple substituted by hydroxy, halogen, C3-12-cycloalkyl, alkoxy, alkylsulfanyl, acyloxy, alkoxycarbonyl, acyl, C1-6-alkyl-NH-C(O)-, C1-6-alkyl-C(O)NH- or -NR R , or alternatively R is hydrogen, and R is hydroxyl, alkoxy, C2-C12-alkenyloxy or phenoxy, which phenoxy group is optionally substituted with methyl, methoxy, halogen, nitro, cyano, trifluoromethyl, ethenyl or -C(O)-O-CH3, provided that if R is hydroxy, Ar is not thiophen-2,5-diyl; and R and R independently from each other represent hydrogen or C1-6-alkyl, or wherein R and R together with the nitrogen-atom to which they are attached form a ring, which ring is monosubstituted by oxo and which ring may contain a further heteroatom, and pharmaceutically acceptable salts thereof, as well as processes for the manufacturing of these compounds, pharmaceutical compositions containing such compounds and their use in the manufacture of drugs for the treatment of diseases such as cancer.
摘要翻译：本发明的目的是式（A）的新的单酰化邻苯基苯胺衍生物，其中Ar是噻吩-2,5-二基，吡啶-2,5-二基，吡啶-5,2-二基，吡啶-2， 6-二基，吡啶-2,4-二基或1,4-亚苯基，R 1，R 2彼此独立地表示氢，C 1-12 - 烷基，C 2-12 - 烯基，C 2-12 - 炔基，C 3-12 - 环烷基，烷基，烯基，炔基和环烷基任选被羟基，卤素，C 3-12 - 环烷基，烷氧基，烷基硫烷基，酰氧基，烷氧基羰基，酰基，C 1-6 - NH-C（O） - ，C 1-6 - 烷基-C（O）NH-或-NR 3 R 4，或者R 1是氢，R 2是羟基，烷氧基， C 2 -C 12 - 烯氧基或苯氧基，该苯氧基任选被甲基，甲氧基，卤素，硝基，氰基，三氟甲基，乙烯基或-C（O）-O-CH 3取代，条件是如果R 2是羟基，则Ar 不是噻吩-2,5-二基; R 3和R 4彼此独立地表示氢或C 1-6 - 烷基，或其中R 3和R 4与它们所连接的氮原子一起形成环，其中环被氧基单取代，并且该环可以含有另外的杂原子及其药学上可接受的盐，以及制备这些化合物的方法，含有这些化合物的药物组合物及其在制备用于治疗疾病的药物中的用途作为癌症。

2. 发明申请

WO2004076444A3 NOVEL HYDROXYCOUMARANONE DERIVATIVES AS ANTITUMOR AND ANTIMETASTATIC 审中-公开
标题翻译：新型羟基喹诺酮衍生物作为抗肿瘤剂和抗肿瘤药
公开(公告)号：WO2004076444A3
公开(公告)日：2004-10-28
申请号：PCT/EP2004001798
申请日：2004-02-24
申请人： HOFFMANN LA ROCHE , BAUER SABINE , ENDELE RICHARD , FERTIG GEORG , FRIEBE WALTER-GUNAR , KOERNER MATTHIAS , KRELL HANS-WILLI
发明人： BAUER SABINE , ENDELE RICHARD , FERTIG GEORG , FRIEBE WALTER-GUNAR , KOERNER MATTHIAS , KRELL HANS-WILLI
IPC分类号： A61P35/00 , C07D405/12 , C07D451/04 , A61K31/34 , C07D307/83
CPC分类号： C07D451/04 , C07D405/12
摘要： The present invention relates to new compounds of the general formula (I) or (II), their pharmaceutically acceptable salts as well as their enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above mentioned compounds as uPA receptor antagonists and therefore in the control or prevention of corresponding illnesses and disorders as outlined herein; or in the manufacture of corresponding medicaments.
摘要翻译：本发明涉及通式（I）或（II）的新化合物，其药学上可接受的盐以及它们的对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述化合物作为uPA受体拮抗剂的用途，因此用于控制或预防本文概述的相应疾病和病症; 或制造相应的药物。

3. 发明申请

WO2009053038A3 COMBINATION THERAPY OF A TYPE II ANTI-CD20 ANTIBODY WITH A PROTEASOME INHIBITOR 审中-公开
标题翻译：抗抑郁剂类型II抗CD20抗体的联合治疗
公开(公告)号：WO2009053038A3
公开(公告)日：2009-06-25
申请号：PCT/EP2008008919
申请日：2008-10-22
申请人： HOFFMANN LA ROCHE , GLYCART BIOTECHNOLOGY AG , FERTIG GEORG , FRIESS THOMAS , KLEIN CHRISTIAN , UMANA PABLO
发明人： FERTIG GEORG , FRIESS THOMAS , KLEIN CHRISTIAN , UMANA PABLO
IPC分类号： A61P35/00 , A61K31/00 , A61K39/395
CPC分类号： A61K39/39558 , A61K31/69 , A61K47/00 , A61K2039/505 , C07K16/2887 , C07K2317/24 , C07K2317/41 , A61K2300/00
摘要： The present invention is directed to the use an type II anti-CD20 antibody for the manufacture of a medicament for the treatment of cancer, especially of CD20 expressing cancers in combination with a proteasome inhibitor.
摘要翻译：本发明涉及使用II型抗-CD20抗体来制造用于治疗癌症的药物，特别是与蛋白酶体抑制剂组合的CD20表达癌症的药物。

4. 发明申请

WO2004069133A3 N-MONOACYLATED O-PHENYLENEDIAMINES AS ANTI -CANCER AGENTS 审中-公开
标题翻译： N-单硝基邻苯二甲酰胺作为抗体剂
公开(公告)号：WO2004069133A3
公开(公告)日：2004-11-25
申请号：PCT/EP2004001045
申请日：2004-02-05
申请人： HOFFMANN LA ROCHE
发明人： FERTIG GEORG , HERTING FRANK , KUBBIES MANFRED , LIMBERG ANJA , REIFF ULRIKE , WEIDNER MICHAEL
IPC分类号： A61K31/34 , A61K31/38 , A61K31/40 , A61P35/00 , C07D209/42 , C07D307/85 , C07D307/86 , C07D333/70
CPC分类号： C07D333/70 , C07D209/42 , C07D307/85
摘要： Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (I), wherein X represents N, S or O; R represents CH3-(O-CH2CH2)n- or C1-C6-alkyl, which alkyl group is monosubstituted with -CO2H, -OH, R R N-, pyridin-2-yl, pyrrolidin-1-yl, piperidino or morpholino; R , R independently from each other denote C1-C6 alkyl; n is 1, 2, 3 or 4; and pharmaceutically acceptable salts thereof. The present invention also encompasses pharmaceutically acceptable salts or prodrugs of the compounds of formula I as well as the use of these compounds to produce medicaments.
摘要翻译：本发明的目的是式（I）的新的单酰化邻苯基苯胺衍生物，其中X表示N，S或O; R表示CH 3 - （O-CH 2 CH 2）n - 或C 1 -C 6烷基，该烷基被-CO 2 H，-OH，R 1 R 2，吡啶-2-基，吡咯烷-1-基哌啶子基或吗啉代; R 1，R 2彼此独立地表示C 1 -C 6烷基; n为1,2,3或4; 及其药学上可接受的盐。本发明还包括式I化合物的药学上可接受的盐或前药以及这些化合物用于制备药物的用途。

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