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1. 发明申请

WO2010080478A1 COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：化合物和使用方法
公开(公告)号：WO2010080478A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068400
申请日：2009-12-17
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
发明人： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
IPC分类号： A61K31/535
CPC分类号： C07D417/14 , C07D417/12 , C07D487/04
摘要： In one aspect, the present invention provides for a compound of Formula (I) in which, the variables X 1 , X 2a , X 2b , X 2c , R 1 , B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula (I) as well as methods for using compounds of Formula (I) for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
摘要翻译：一方面，本发明提供式（I）的化合物，其中变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。在另一方面，本发明提供包含式（I）化合物的药物组合物以及使用式（I）化合物治疗由表达特征的疾病和病症（例如癌症，血小板增多症等）的方法或过度表达Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

2. 发明申请

WO2008061208A2 ARYLSULFONAMIDE COMPOUNDS 审中-公开
标题翻译：芳基磺酰胺化合物
公开(公告)号：WO2008061208A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/084873
申请日：2007-11-15
申请人： GENENTECH, INC. , WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , BAELL, Jonathan Bayldon , LESSENE, Guillaume Laurent , SLEEBS, Brad Edmund , FAIRBROTHER, Wayne J. , FLYGARE, John A. , KOEHLER, Michael F. T.
发明人： BAELL, Jonathan Bayldon , LESSENE, Guillaume Laurent , SLEEBS, Brad Edmund , FAIRBROTHER, Wayne J. , FLYGARE, John A. , KOEHLER, Michael F. T.
IPC分类号： C07D239/94 , A61K31/517 , A61P43/00
CPC分类号： C07D239/94
摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralising prosurvival Bcl-2 proteins: wherein A 1 , A 2 , B 1, B 2 , B 3 , X, Z, R 1 , R 2 , R 3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译：本发明一般涉及模拟某些肽和蛋白质的生物活性的小分子，含有它们的组合物及其用途。具体而言，本发明涉及模拟仅BH3蛋白的生物学活性并能够结合并中和促存活Bcl-2蛋白的通式（I）的化合物：其中A 1， A 2，B 1，B 2，B 3，X，Z，R 1，B 1，B 2，B 3， R 2，R 3和t如本文所述。本发明还涉及制备模拟肽和蛋白质部分的苯磺酰胺化合物的方法，并涉及这些化合物在调节细胞死亡以及治疗和/或预防与细胞死亡失调相关的疾病或病症中的用途

3. 发明申请

WO2009089502A1 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：WO2009089502A1
公开(公告)日：2009-07-16
申请号：PCT/US2009/030674
申请日：2009-01-09
申请人： GENENTECH, INC. , NDUBAKU, Chudi , FLYGARE, John A. , COHEN, Frederick
发明人： NDUBAKU, Chudi , FLYGARE, John A. , COHEN, Frederick
IPC分类号： C07K5/06 , C07K5/08 , C07K5/062 , C07K5/083 , A61K38/05 , A61K38/06 , A61P35/00
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/0806
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), and G, X 1 , X 2 , R 1 , R 2 , R 3 , R 4 , R 4 ', R 5 , R a , R b , and R c are as described herein.
摘要翻译：本发明提供可用作治疗恶性肿瘤的治疗剂的新型IAP抑制剂，其中化合物具有通式（I），G，X1，X2，R1，R2，R3，R4，R4'，R5，Ra，Rb ，和Rc如本文所述。

4. 发明申请

WO2008134679A1 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：WO2008134679A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061891
申请日：2008-04-29
申请人： GENENTECH, INC. , FLYGARE, John A. , COHEN, Frederick , DESHAYES, Kurt , KOEHLER, Michael F. T. , GAZZARD, Lewis J. , WANG, Lan , NDUBAKU, Chudi
发明人： FLYGARE, John A. , COHEN, Frederick , DESHAYES, Kurt , KOEHLER, Michael F. T. , GAZZARD, Lewis J. , WANG, Lan , NDUBAKU, Chudi
IPC分类号： C07D209/02 , C07D263/06 , C07D513/04
CPC分类号： C07D417/14 , C07D207/16 , C07D519/00
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1 - M - U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3', R4, R4' and R5, are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中具有通式U1-M-U2的化合物，其中M是共价连接U1的R2，R3，R4或R5与R2，R3共价连接的基团，R4或R5组的U2; U1和U2具有通式（I），G，X 1，X 2，R 2，R 3，R 3'，R 4，R 4'和R 5如本文所述。

5. 发明申请

WO2012074757A1 ALANINYL MAYTANSINOL ANTIBODY CONJUGATES 审中-公开
标题翻译： ALANINYL MAYTANSINOL抗体结合
公开(公告)号：WO2012074757A1
公开(公告)日：2012-06-07
申请号：PCT/US2011/061031
申请日：2011-11-16
申请人： GENENTECH, INC. , FLYGARE, John , JUNUTULA, Jagath Reddy , PILLOW, Thomas
发明人： FLYGARE, John , JUNUTULA, Jagath Reddy , PILLOW, Thomas
IPC分类号： C07D491/12 , A61K31/535 , A61K39/00
CPC分类号： C07D491/12
摘要： Linker-drug intermediates of Formula I are conjugated to antibodies to form antibody-drug conjugates where the drug moiety is an N-methylalaninyl-maytansinoid. L is Formula IA; E is Formula IB or Formula IC; n is 2, 3, 4, 5, or 6; m is 2, 3 or 4; and q is 0 or 1.
摘要翻译：式I的接头 - 药物中间体与抗体缀合以形成抗体 - 药物偶联物，其中药物部分是N-甲基丙酰氨基 - 美登木素生物碱。 L是式IA; E为式IB或式IC; n为2,3,4,5或6; m为2,3或4; q为0或1。

6. 发明申请

WO2011130598A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2011130598A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032632
申请日：2011-04-15
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
IPC分类号： A61K47/48 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译：公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。

7. 发明申请

WO2010009124A3 ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS 审中-公开
标题翻译：蒽醌衍生物偶联物，其制备方法及其作为抗微生物化合物的用途
公开(公告)号：WO2010009124A3
公开(公告)日：2010-12-23
申请号：PCT/US2009050537
申请日：2009-07-14
申请人： GENENTECH INC , NERVIANO MEDICAL SCIENCES SRL , BERIA ITALO , CARUSO MICHELE , FLYGARE JOHN A , LUPI VITTORIA , PEREGO RITA , POLAKIS PAUL , POLSON ANDREW , SALSA MATTEO , SPENCER SUSAN D , VALSASINA BARBARA
发明人： BERIA ITALO , CARUSO MICHELE , FLYGARE JOHN A , LUPI VITTORIA , PEREGO RITA , POLAKIS PAUL , POLSON ANDREW , SALSA MATTEO , SPENCER SUSAN D , VALSASINA BARBARA
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： C07K16/2863 , A61K47/64 , A61K47/6809 , C07K2317/76
摘要： The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
摘要翻译：本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。

8. 发明申请

WO2010017035A2 INHIBITORS OF IAP 审中-公开
标题翻译： IAP抑制剂
公开(公告)号：WO2010017035A2
公开(公告)日：2010-02-11
申请号：PCT/US2009/051522
申请日：2009-07-23
申请人： GENENTECH, INC. , DUDLEY, Dannette , FLYGARE, John, A. , NDUBAKU, Chudi
发明人： DUDLEY, Dannette , FLYGARE, John, A. , NDUBAKU, Chudi
IPC分类号： C07D403/12 , C07D403/10 , A61K31/4025 , A61P35/00
CPC分类号： C07D403/12 , C07D207/16 , C07D513/04 , C07K5/0804
摘要： The invention provides novel compounds that are inhibitors of IAPs having the general formula: wherein X 1 , X 2 , X 3 , Y, A, R 1 , R 2 , R 3 , R 4 , R 4' , R 5 , R 5' , R 6 and R 6' are as described herein. The compouds of the invention may be used to induce apoptosis in cells (or sensitise cells to apoptosis) in which IAPs are overexpressed or otherwise implicated in resistance to normal apoptotic processes. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment cancers.
摘要翻译：本发明提供了新型化合物，其为具有以下通式的IAP抑制剂：其中X 1，X 2，X 3， Y，A，R 1，R 2，R 3，R 4，R 4，R 4， 4'，R 5，R 5，R 6和R 6' 如本文所述。本发明的化合物可用于诱导细胞凋亡（或使细胞对细胞凋亡敏感），其中IAP过表达或以其他方式牵涉抗正常细胞凋亡过程。因此，化合物可以以药学上可接受的组合物提供并用于治疗癌症。

9. 发明申请

WO2005094818A1 AZABICYCLO-OCTANE INHIBITORS OF IAP 审中-公开
标题翻译：化学文摘AZABICYCLO-OCTANE抑制剂
公开(公告)号：WO2005094818A1
公开(公告)日：2005-10-13
申请号：PCT/US2005/009328
申请日：2005-03-22
申请人： GENENTECH, INC. , COHEN, Frederick , FAIRBROTHER, Wayne , FLYGARE, John , TSUI, Vickie, Hsiao-Wei , KETELTAS, Stephen, Franz
发明人： COHEN, Frederick , FAIRBROTHER, Wayne , FLYGARE, John , TSUI, Vickie, Hsiao-Wei , KETELTAS, Stephen, Franz
IPC分类号： A61K31/403
CPC分类号： C07K5/06026 , C07K14/4747
摘要： The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X 1 and X 2 are independently O or S; L is a bond or -C(X 3 )-, -C(X 3 )NR 12 , -C(X 3 )O- wherein X 3 is O or S and R 12 is H or R 1 ; R 1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R 2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R 3 is H or alkyl; R 4 and R 4' are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R 5 , and R 5' are each independently H or alkyl; R 6 is H or alkyl; and salts and solvates thereof.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有其中X 1和X 2独立地为O或S的通式（I）; L是键或-C（X3） - ， - C（X3）NR12，-C（X3）O-，其中X3是O或S，R12是H或R1; R 1是烷基，碳环，碳环取代的烷基，杂环或杂环取代的烷基，其中各自任选被卤素，羟基，巯基，羧基，烷基，卤代烷基，烷氧基，烷基磺酰基，氨基，硝基，芳基和杂芳基取代; R2是烷基，环烷基，环烷基烷基，芳基，芳烷基，杂环或杂环基烷基; R3是H或烷基; R 4和R 4'独立地是H，烷基，芳基，芳烷基，环烷基，环烷基烷基，杂芳基或杂芳烷基，其中各自任选被卤素，羟基，巯基，羧基，烷基，烷氧基，氨基和硝基取代; R5和R5'各自独立地为H或烷基; R6是H或烷基; 及其盐和溶剂合物。

10. 发明申请

WO0041531A3 SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：WO0041531A3
公开(公告)日：2001-08-16
申请号：PCT/US0000673
申请日：2000-01-11
申请人： GENENTECH INC , ALIAGAS MARTIN IGNACIO , ARTIS DEAN R , DINA MICHAEL S , FLYGARE JOHN A , GOLDSMITH RICHARD A , MUNROE REGINA A , OLIVERO ALAN G , PASTOR RICHARD , RAWSON THOMAS E , ROBARGE KIRK D , SUTHERLIN DANIEL P , WEESE KENNETH J , ZHOU AIHE , ZHU YAN
发明人： ALIAGAS-MARTIN IGNACIO , ARTIS DEAN R , DINA MICHAEL S , FLYGARE JOHN A , GOLDSMITH RICHARD A , MUNROE REGINA A , OLIVERO ALAN G , PASTOR RICHARD , RAWSON THOMAS E , ROBARGE KIRK D , SUTHERLIN DANIEL P , WEESE KENNETH J , ZHOU AIHE , ZHU YAN
IPC分类号： C07D333/34 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51 , C07C257/16 , C07C311/06 , C07C311/21
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译：具有结构（A）的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。这些化合物可用于预防和/或治疗凝血障碍的方法。

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