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1. 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。

2. 发明申请

WO2008061208A3 ARYLSULFONAMIDE COMPOUNDS 审中-公开
标题翻译：芳香酰胺化合物
公开(公告)号：WO2008061208A3
公开(公告)日：2008-07-03
申请号：PCT/US2007084873
申请日：2007-11-15
申请人： GENENTECH INC , INST MEDICAL W & E HALL , 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学活性的小分子，含有它们的组合物及其用途。特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并且能够结合并中和前病毒Bcl-2蛋白：其中A 1， B 1，B 2，B 3，X 3，Z 1，R 2， R 2，R 3和R 3如本文所述。本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症。

3. 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。

4. 发明申请

WO2010017035A3 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：WO2010017035A3
公开(公告)日：2010-04-15
申请号：PCT/US2009051522
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 , A61K31/4025 , A61P35/00 , C07D403/10
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 X1, X2, X3, Y, A, R1, R2, R3, R4, R4', R5, R5', R6 and R6' 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：本发明提供了具有以下通式的IAP抑制剂的新化合物：其中X1，X2，X3，Y，A，R1，R2，R3，R4，R4'，R5，R5'，R6和R6'如本文所述。本发明的化合物可用于诱导细胞凋亡（或致敏细胞凋亡），其中IAP过表达或以其他方式涉及抗正常凋亡过程。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。

5. 发明专利

JP2012184230A Pyrrolidine inhibitor of iap 审中-公开
标题翻译：吡咯啉抑制剂IAP
公开(公告)号：JP2012184230A
公开(公告)日：2012-09-27
申请号：JP2012064552
申请日：2012-03-21
申请人： Genentech Inc , ジェネンテック, インコーポレイテッド
发明人： COHEN FREDERICK , TSUI VICKIE HSIAO-WEI , LY CUONG , FLYGARE JOHN A
IPC分类号： C07K5/06 , A61K38/00 , A61P35/00 , A61P43/00
CPC分类号： C07D471/04 , C07D417/04 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies.SOLUTION: This invention relates to a compound of formula (I) (wherein A is a 5-membered aromatic heterocycle or the like incorporating 1 to 4 heteroatoms N, O, or S; Q is H, alkyl, a carbocycle, or a heterocycle; Xand Xare each independently O or S; Y is a bond, (CRR), O or S; n is 1 or 2; Ris H; or Rand Rtogether form a 5-8 membered heterocycle; Ris alkyl, a carbocycle or the like; Ris H or alkyl; or Rand Rtogether form a 3-6 heterocycle; R' is H; or Rand R' together form a 3-6 carbocycle; Rand R' are independently H, hydroxyl or the like; Ris H or alkyl; R, and R' are each independently H, alkyl or the like; Ris H, cyano or the like; and Ris H, alkyl or the like). The invention further relates to salts and solvates thereof.
摘要翻译：待解决的问题：提供可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂。解决方案：本发明涉及式（I）化合物（其中A是含有1至4个杂原子N，O或S的5元芳香杂环等; Q是H，烷基，碳环，或杂环; X 1 和X 2 各自独立地为O或S; Y为键（CR 7 R 7 ） n ，O或S; n为1或2; R 1 为H;或者R 1 和R 2 共同形成5 -8元杂环; R 8是苯基，碳环或类似基团; R 3是H或烷基;或R“ SB POS =“POST”> 3 和R 4 一起形成3-6杂环; R 3 是H;或R 3 和R 3 共同形成3-6个碳环; R 4 和R 4 独立地是H，羟基等; R“是H或烷基; R 6 ，R 6 各自独立地为H，烷基等; R 7是H，氰基等; 并且R 8是苯基，烷基等）。本发明还涉及其盐和溶剂化物。版权所有（C）2012，JPO＆INPIT

6. 发明申请

WO2014159981A3 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2014159981A3
公开(公告)日：2015-04-09
申请号：PCT/US2014025564
申请日：2014-03-13
申请人： SPIROGEN SARL , GENENTECH INC
发明人： HOWARD PHILIP WILSON , FLYGARE JOHN A , PILLOW THOMAS , WEI BINQING
IPC分类号： A61K47/48 , A61K31/5517 , C07D487/04
CPC分类号： A61K47/6869 , A61K31/5517 , A61K47/48638 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61P35/00 , C07D487/04 , C07D519/00
摘要： Conjugate compounds of formula (A): wherein: R2 is, where R36a and R36b are independently selected from H, F, C1-4 saturated aikyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester; or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 aikyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 aikyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R' are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR', R and R' together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R16, R17, R19, R20, R21 and R22 are as defined for R6, R7, R9, R10, R11 and R2 respectively; wherein Z is CH or N; wherein T and T' are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X' is 3 to 12 atoms; and X and X' are independently selected from O, S and N(H).
摘要翻译：式（A）的共轭化合物：其中：R 2为，其中R 36a和R 36b独立地选自H，F，C 1-4饱和的烷基，C 2-3链烯基，该烷基和烯基任选被选自C1 -4-烷基酰氨基和C 1-4烷基酯; 或者当R 36a和R 36b之一为H时，另一个选自腈和C 1-4烷基酯; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; Y选自式A1，A2，A3，A4，A5和A6：L是连接到细胞结合剂的连接体; CBA是细胞结合剂; n为0〜48的整数; RA4是C1-6亚烷基; （a）R 10是H，R 11是OH，ORA，其中RA是C 1-4烷基; 或（b）R 10和R 11在与它们结合的氮原子和碳原子之间形成氮 - 碳双键; 或（c）R 10为H且R 11为OSOzM，其中z为2或3，M为单价药学上可接受的阳离子; R和R'各自独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基，并且任选地相对于基团NRR'，R和R'与它们所在的氮原子一起连接形成任选取代的4-，5-，6-或7-元杂环; 其中R16，R17，R19，R20，R21和R22分别如R6，R7，R9，R10，R11和R2所定义; 其中Z是CH或N; 其中T和T'独立地选自单键或C1-9亚烷基，该链可以被一个或多个杂原子间隔。 O，S，N（H），NMe，条件是X和X'之间的最短原子链中的原子数为3至12个原子; X和X'独立地选自O，S和N（H）。

7. 发明申请

WO2015095227A3 PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF 审中-公开
标题翻译：胶原化合物及其抗体药物结合
公开(公告)号：WO2015095227A3
公开(公告)日：2015-12-10
申请号：PCT/US2014070660
申请日：2014-12-16
申请人： GENENTECH INC , UNIV AUCKLAND , LEE HO HUAT , TERCEL MOANA
发明人： LEE HO HUAT , TERCEL MOANA , FLYGARE JOHN A , GUNZNER-TOSTE JANET , PILLOW THOMAS H , SAFINA BRIAN , STABEN LEANNA , VERMA VISHAL , WEI BINQING , ZHAO GUILING
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/48715 , A61K47/6803 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07K16/28 , C07K16/2851 , C07K16/2863 , C07K16/30 , C07K2317/24 , C07K2317/56 , C07K2317/76
摘要： This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
摘要翻译：本发明涉及肽模拟接头及其抗体药物偶联物，含有它们的药物组合物及其在治疗中用于预防或治疗癌症的用途。

8. 发明公开

EP2376085A4 COMPOUNDS AND METHODS OF USE 有权转让
标题翻译：化合物和应用程序
公开(公告)号：EP2376085A4
公开(公告)日：2012-08-15
申请号：EP09837907
申请日：2009-12-17
申请人： GENENTECH INC , INST MEDICAL W & E HALL , ABBOTT LAB
发明人： BAELL JONATHAN BAYLDON , BUI CHINH THIEN , COLMAN PETER , DUDLEY DANETTE A , FAIRBROTHER WAYNE J , FLYGARE JOHN A , LESSENE 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 , CZABOTAR PETER
IPC分类号： A61K31/535 , C07D417/14 , C07D487/04
CPC分类号： C07D417/14 , C07D417/12 , C07D487/04

9. 发明公开

EP2148858A4 INHIBITORS OF IAP 审中-公开
标题翻译： IAP抑制剂
公开(公告)号：EP2148858A4
公开(公告)日：2011-01-26
申请号：EP08747109
申请日：2008-04-29
申请人： GENENTECH INC
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 , A61K31/4025 , A61P35/00 , C07D263/06 , C07D513/04
CPC分类号： C07D417/14 , C07D207/16 , C07D519/00

10. 发明公开

EP2318395A4 INHIBITORS OF IAP 审中-公开
公开(公告)号：EP2318395A4
公开(公告)日：2011-10-26
申请号：EP09805348
申请日：2009-07-23
申请人： GENENTECH INC
发明人： DUDLEY DANNETTE , FLYGARE JOHN A , NDUBAKU CHUDI
IPC分类号： C07K5/08 , A61K31/4025 , A61K38/06 , A61P35/00 , C07D403/10 , C07D403/12
CPC分类号： C07D403/12 , C07D207/16 , C07D513/04 , C07K5/0804

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