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1. 发明授权

EP3082872B1 PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF 有权
公开(公告)号：EP3082872B1
公开(公告)日：2020-12-09
申请号：EP14821453.9
申请日：2014-12-16
申请人： Genentech, Inc. , Medimmune Limited
发明人： FLYGARE, John , GUNZNER-TOSTE, Janet , PILLOW, Thomas , SAFINA, Brian , VERMA, Vishal , WEI, Binqing , ZHAO, Guiling , STABEN, Leanna , HOWARD, Philip, Wilson , MASTERSON, Luke
IPC分类号： A61K47/68 , A61K31/5517 , A61P35/00 , A61P35/02

2. 发明公开

EP2968596A2 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 有权
标题翻译：吡咯并苯并二氮杂及其偶联物
公开(公告)号：EP2968596A2
公开(公告)日：2016-01-20
申请号：EP14761432.5
申请日：2014-03-13
申请人： MEDIMMUNE LIMITED , 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 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61P35/00 , C07D487/04 , C07D487/16 , 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 alkyl, 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 alkyl 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 alkyl; 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）的偶联化合物：其中：R 2是，其中：R 36a和R 36b独立地选自H，F，C 1-4饱和烷基，C 2-3烯基，其中烷基和烯基任选被选自C 1-4烷基酰胺基和C 1-4烷基酯的基团; 或者当R 36a和R 36b中的一个是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是与细胞结合剂连接的接头; CBA是细胞结合剂; n是在0至48范围内选择的整数; R A4是C 1-6亚烷基; （a）R 10为H，且R 11为OH，OR A，其中R A为C 1-4烷基; 或（b）R 10和R 11在它们所键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OSO zM，其中z为2或3且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，并且任选地与基团NRR'，R和R'一起与氮原子一起形成它们连接形成任选取代的4-，5-，6-或7-元杂环; 其中R 16，R 17，R 19，R 20，R 21和R 22分别与R 6，R 7，R 9，R 10，R 11和R 2的定义相同; 其中Z是CH或N; 其中T和T'独立地选自单键或C 1-9亚烷基，该链可被一个或多个杂原子例如 O，S，N（H），NMe，条件是在X和X'之间的最短原子链中的原子数是3至12个原子; X和X'独立地选自O，S和N（H）。

3. 发明公开

EP3700901A1 (4-HYDROXYPYRROLIDIN-2-YL)-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：EP3700901A1
公开(公告)日：2020-09-02
申请号：EP18799977.6
申请日：2018-10-23
申请人： Genentech, Inc.
发明人： BLAQUIERE, Nicole , DRAGOVICH, Peter , GAZZARD, Lewis J. , PILLOW, Thomas , STABEN, Steven T. , WEI, Binqing , XIN, Jianfeng
IPC分类号： C07D401/14 , C07D413/14 , A61K31/55 , C07D403/04 , C07D417/14 , C07D471/18 , A61P35/00 , A61P37/00

4. 发明授权

EP2968596B1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 有权
公开(公告)号：EP2968596B1
公开(公告)日：2019-03-06
申请号：EP14761432.5
申请日：2014-03-13
申请人： MEDIMMUNE LIMITED , Genentech, Inc.
发明人： HOWARD, Philip, Wilson , FLYGARE, John, A. , PILLOW, Thomas , WEI, Binqing
IPC分类号： A61K47/68 , C07D487/04 , C07D487/16 , C07D519/00 , A61K31/5517 , A61P35/00

5. 发明公开

EP3082874A2 PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF 审中-公开
标题翻译：肽制剂化合物和抗体 - 药物偶联物
公开(公告)号：EP3082874A2
公开(公告)日：2016-10-26
申请号：EP14824686.1
申请日：2014-12-16
申请人： Genentech, Inc.
发明人： FLYGARE, John , GUNZNER-TOSTE, Janet , PILLOW, Thomas , SAFINA, Brian , VERMA, Vishal , WEI, Binqing , ZHAO, Guiling , STABEN, Leanna
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/6803 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6889 , C07K16/28 , C07K16/2851 , 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：本发明涉及拟肽连接体和其抗体药物偶联物，含有它们的药物组合物，以及它们在治疗癌症的预防或治疗中的用途。

6. 发明公开

EP3082872A1 PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF 有权
标题翻译：肽制剂化合物和抗体 - 药物偶联物
公开(公告)号：EP3082872A1
公开(公告)日：2016-10-26
申请号：EP14821453.9
申请日：2014-12-16
申请人： Genentech, Inc. , Medimmune Limited
发明人： FLYGARE, John , GUNZNER-TOSTE, Janet , PILLOW, Thomas , SAFINA, Brian , VERMA, Vishal , WEI, Binqing , ZHAO, Guiling , STABEN, Leanna , HOWARD, Philip, Wilson , MASTERSON, Luke
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/48569 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6867 , A61K47/6869 , A61K47/6889 , C07K16/2851 , C07K16/30 , C07K16/3061 , C07K16/3069 , C07K16/3092 , C07K2317/24 , C07K2317/51 , C07K2317/515 , C07K2317/56
摘要： This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.
摘要翻译：本发明涉及拟肽连接体和其抗体药物缀合物，含有它们的药物组合物，以及它们在预防癌症治疗的疗法中的用途。

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