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1. 发明申请

WO2011098398A1 SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES 审中-公开
标题翻译：取代的吡咯烷-2-羧酸
公开(公告)号：WO2011098398A1
公开(公告)日：2011-08-18
申请号：PCT/EP2011/051619
申请日：2011-02-04
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , JIANG, Nan , LIU, Jin-Jun , ROSS, Tina Morgan , ZHANG, Jing , ZHANG, Zhuming
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , JIANG, Nan , LIU, Jin-Jun , ROSS, Tina Morgan , ZHANG, Jing , ZHANG, Zhuming
IPC分类号： C07D207/10 , A61K31/40 , A61P35/00
CPC分类号： C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12
摘要： There are provided compounds of the formula (I) wherein X, Y, R 1 , R 2 , R 3 , R 3 , R 4 , R 5 , R 6 and R 7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
摘要翻译：提供式（I）化合物，其中X，Y，R 1，R 2，R 3，R 3，R 4，R 5，R 6和R 7如本文所述，其对映体及其药学上可接受的盐和酯。这些化合物可用作抗癌剂。

2. 发明申请

WO2012116989A1 SUBSTITUTED HETEROARYL 2', 3', 7', 7A' - TETRAHYDROSPIRO-[PYRROLE-3, 6' - PYRROLO [1, 2-C] IMIDAZOLE] - 1', 2 (1H, 5'H) -DIONES AS ANTICANCER AGENTS 审中-公开
标题翻译：取代的杂芳基2'，3'，7'，7A' - 四氢吡喃并[吡咯并[3,6' - 吡咯并[1,2-C]咪唑并] -1'，2（1H，5'H）代理
公开(公告)号：WO2012116989A1
公开(公告)日：2012-09-07
申请号：PCT/EP2012/053369
申请日：2012-02-28
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , JIANG, Nan , LIU, Jin-Jun , ZHANG, Zhuming
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , JIANG, Nan , LIU, Jin-Jun , ZHANG, Zhuming
IPC分类号： C07D471/22 , A61K31/437 , A61P35/00
CPC分类号： C07D471/22
摘要： There are provided compounds of the formula (I), wherein A, B, V, W, R 1 , R 2 , R 3 , R 4 and R 5 are described herein, together with the enantiomers and pharmaceutically acceptable salts and esters thereof, methods of making those compounds, pharmaceutical compositions comprising them, as well as their use as anticancer agents, and which function as inhibitors of the interaction between p53 and MDM2.
摘要翻译：提供式（I）化合物，其中A，B，V，W，R 1，R 2，R 3，R 4和R 5与其对映异构体和药学上可接受的盐和酯一起描述，制备这些化合物的方法，包含它们的药物组合物，以及它们作为抗癌剂的用途，并且其作为p53和MDM2之间相互作用的抑制剂起作用。

3. 发明申请

WO2012022707A1 SUBSTITUTED HETEROARYL SPIROPYRROLIDINE MDM2 ANTAGONISTS 审中-公开
标题翻译：取代的异氟烷螺旋罗丹明MDM2拮抗剂
公开(公告)号：WO2012022707A1
公开(公告)日：2012-02-23
申请号：PCT/EP2011/064015
申请日：2011-08-15
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , KARNACHI, Prabha Saba , LIU, Jin-Jun , SO, Sung-Sau , ZHANG, Jing , ZHANG, Zhuming
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , KARNACHI, Prabha Saba , LIU, Jin-Jun , SO, Sung-Sau , ZHANG, Jing , ZHANG, Zhuming
IPC分类号： C07D471/10 , C07D487/10 , C07D495/10 , A61K31/407 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D471/10 , C07D487/10 , C07D495/10
摘要： There are provided compounds of the general formula (I) wherein A, B, V, W, R 1 , R 2 , R 3 , R 3 , and R 4 , are as described herein, enantiomers and pharmaceutically acceptable salts thereof, as well as methods for making said compounds and pharmaceutical compositions containing them. The present compounds are useful as anticancer agents, in particular as agents in the therapeutic and/or prophylactic treatment of solid tumors such as for example breast, colon, lung and prostate tumors.
摘要翻译：提供通式（I）的化合物，其中A，B，V，W，R 1，R 2，R 3，R 3和R 4如本文所述，其对映体和药学上可接受的盐，以及制备所述化合物和含有它们的药物组合物。本发明化合物可用作抗癌剂，特别是作为治疗和/或预防性治疗实体瘤例如乳腺癌，结肠癌，肺癌和前列腺肿瘤的药物。

4. 发明申请

WO2011067185A1 SPIROINDOLINONE PYRROLIDINES 审中-公开
标题翻译：螺吲哚啉酮吡咯烷酮
公开(公告)号：WO2011067185A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068353
申请日：2010-11-29
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , GRAVES, Bradford James , JIANG, Nan , ZHANG, Jing , ZHANG, Zhuming
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , DING, Qingjie , GRAVES, Bradford James , JIANG, Nan , ZHANG, Jing , ZHANG, Zhuming
IPC分类号： C07D487/10 , A61K31/407 , A61P35/00
CPC分类号： C07D487/10
摘要： There are provided compounds of the formula (I) wherein X, Y and R 1 to R 8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
摘要翻译：提供了式（I）化合物，其中X，Y和R 1至R 8与本文所述的对映异构体，药学上可接受的盐和酯一起描述。这些化合物可用作抗癌剂。

5. 发明申请

WO2013135648A1 SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES 审中-公开
标题翻译：取代的吡咯烷-2-羧酸
公开(公告)号：WO2013135648A1
公开(公告)日：2013-09-19
申请号：PCT/EP2013/054920
申请日：2013-03-12
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , VU, Binh Thanh , ZHAO, Chunlin
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , VU, Binh Thanh , ZHAO, Chunlin , FISHLOCK, Daniel
IPC分类号： C07D207/16 , C07D405/12 , C07D493/04 , C07F9/572 , A61K31/40 , A61K31/4035 , A61P35/00
CPC分类号： C07D403/12 , C07D207/16 , C07D405/12 , C07D493/04 , C07F9/572 , C07F9/5727 , C07H15/26
摘要： There are provided compounds of formula (I) wherein X, Y, Z, R 1 , R 2 , R 3 and R 4 are as described herein, and enantiomers and pharmaceutically acceptable salts and esters thereof; as well as methods for making such compounds, pharmaceutical compositions comprising said compounds, and their use in the treatment of cancer.
摘要翻译：提供式（I）化合物，其中X，Y，Z，R 1，R 2，R 3和R 4如本文所述，及其对映体及其药学上可接受的盐和酯; 以及制备这些化合物的方法，包含所述化合物的药物组合物及其在治疗癌症中的用途。

6. 发明申请

WO2009047161A1 CHIRAL CIS-IMIDAZOLINES 审中-公开
公开(公告)号：WO2009047161A1
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063053
申请日：2008-09-30
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CAI, Jianping , CHU, Xin-Jie , LI, Hongju , LOVEY, Allen John , VU, Binh Thanh , ZHAO, Chunlin
发明人： BARTKOVITZ, David Joseph , CAI, Jianping , CHU, Xin-Jie , LI, Hongju , LOVEY, Allen John , VU, Binh Thanh , ZHAO, Chunlin
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/454 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10
摘要： There are provided compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V 1 , V 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as herein described, processes for obtaining said compounds and pharmaceutical preparations containing them. These compounds are useful as anticancer agents, in particular as agents in the treatment of solid tumors.
摘要翻译：提供式（I）化合物或其药学上可接受的盐，其中X，Y，Z，V1，V2，R 1，R 2，R 3，R 4和R 5如本文所述，获得所述化合物和药物制剂的方法包含它们这些化合物可用作抗癌剂，特别是作为治疗实体瘤的药物。

7. 发明申请

WO2009021869A1 PYRAZOLO[3,4-D]-PYRAMIDINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：吡咯并[3,4-D] - 吡啶衍生物作为抗增殖剂
公开(公告)号：WO2009021869A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/060215
申请日：2008-08-04
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHU, Xin-Jie , LUK, Kin-Chun Thomas
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , LUK, Kin-Chun Thomas
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention is directed to novel pyrazolo[3,4-d]pyrimidine derivatives of the formula (I), and pharmaceutically-acceptable salts and esters thereof, wherein R, Ring A, L, and Ring B are as described herein. These compounds and their pharmaceutically-acceptable salts and esters inhibit Raf kinase and have antiproliferative activity. As such, they are useful in the treatment or control of proliferative disorders such as cancer, in particular solid tumors, more particularly breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.
摘要翻译：本发明涉及式（I）的吡唑并[3,4-d]嘧啶衍生物及其药学上可接受的盐和酯，其中R，环A，L和环B如本文所述。这些化合物及其药学上可接受的盐和酯抑制Raf激酶并具有抗增殖活性。因此，它们可用于治疗或控制增殖性疾病如癌症，特别是实体瘤，更特别是乳腺肿瘤，结肠肿瘤，肺肿瘤，前列腺肿瘤和黑素瘤。还公开了包含这种化合物或其药学上可接受的盐或酯的组合物和单位剂量制剂，以及用于制备这些化合物的方法，以及在治疗中使用这些化合物或其药学上可接受的盐或酯的方法的增殖性疾病。

8. 发明申请

WO2008017594A1 THIENO[3,2-C]PYRIDINE-7-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：噻吩并[3,2-C]吡啶-7-羧酸衍生物
公开(公告)号：WO2008017594A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/057748
申请日：2007-07-27
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHEN, Yi , CHU, Xin-Jie , LUK, Kin-Chun Thomas
发明人： BARTKOVITZ, David Joseph , CHEN, Yi , CHU, Xin-Jie , LUK, Kin-Chun Thomas
IPC分类号： A61K31/4365 , C07D495/04 , A61P35/00
CPC分类号： A61K31/4365 , C07D495/04
摘要： There are provided compounds of the formula (I), wherein R 1 , R 2 , R 3 , X, Y, Q, Ring A and Ring B are as described in the specification.
摘要翻译：提供式（I）化合物，其中R 1，...，R 2，R 3，X，Y， Q，环A和环B如说明书所述。

9. 发明申请

WO2007031428A1 4-AMINO-THIENO[3,2-C]PYRIDINE-7-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译： 4-氨基 - 噻吩并[3,2-C]吡啶-7-羧酸衍生物
公开(公告)号：WO2007031428A1
公开(公告)日：2007-03-22
申请号：PCT/EP2006/065986
申请日：2006-09-05
申请人： F. HOFFMANN-LA ROCHE AG , BARTKOVITZ, David Joseph , CHEN, Yi , CHU, Xin-Jie , LUK, Kin-Chun , ROSSMAN, Pamela Loreen , SO, Sung-Sau
发明人： BARTKOVITZ, David Joseph , CHEN, Yi , CHU, Xin-Jie , LUK, Kin-Chun , ROSSMAN, Pamela Loreen , SO, Sung-Sau
IPC分类号： C07D495/04 , A61K31/435 , A61P35/00
CPC分类号： C07D495/04 , Y02P20/582
摘要： The present invention relates to compounds of the formula (I-A) medicaments containing them and the use of these compounds as pharmaceutically active agents. The compounds exhibit activity as Raf kinase inhibitors and therefore may be useful for the treatment of diseases mediated by said kinases, especially as anticancer agents.
摘要翻译：本发明涉及含有它们的式（I-A）药物的化合物以及这些化合物作为药物活性剂的用途。该化合物表现出作为Raf激酶抑制剂的活性，因此可用于治疗由所述激酶介导的疾病，特别是作为抗癌剂。

10. 发明申请

WO2013178570A1 SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES 审中-公开
标题翻译：取代的吡咯烷-2-羧酸
公开(公告)号：WO2013178570A1
公开(公告)日：2013-12-05
申请号：PCT/EP2013/060834
申请日：2013-05-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTKOVITZ, David Joseph , CHU, Xin-Jie , EHRLICH, George , LIU, Jin-Jun , MICHEL, Hanspeter , VU, Binh Thanh , ZHAO, Chunlin
IPC分类号： A61K31/40 , C07D401/06 , C07D409/04 , C07D207/16
CPC分类号： C07D207/16 , C07D401/12 , C07D405/12 , C07D471/04 , C07F9/5725 , C07H17/02
摘要： There are provided compounds of the formula (I) wherein X, Y, Z, R 1 , R 2 and R 3 are as described herein, enantiomers and pharmaceutically acceptable salts and esters thereof, methods of making those compounds, as well as the use of such compounds as medicaments, especially as anticancer agents.
摘要翻译：提供式（I）化合物，其中X，Y，Z，R 1，R 2和R 3如本文所述，其对映异构体和药学上可接受的盐和酯，制备那些化合物的方法，以及这些化合物的用途作为药物，特别是作为抗癌剂。

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