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公开(公告)号：WO2013071035A1
公开(公告)日：2013-05-16
申请号：PCT/US2012/064342
申请日：2012-11-09
Applicant: ENSEMBLE THERAPEUTICS , BRISTOL-MYERS SQUIBB COMPANY
Inventor： SEIGAL, Benjamin, Adam , TERRETT, Nicholas , CARTER, Percy, H. , BORZILLERI, Robert, M. , ZHANG, Yong , MILLER, Michael, M.
IPC: C07D249/04 , A61P35/00
CPC classification number: C07D498/22 , A61K38/00 , C07D249/04 , C07D498/16 , C07K5/1008 , C07K7/56 , Y02A50/411 , Y02A50/414
Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.
Abstract translation: 本发明一般涉及大环化合物及其治疗用途。 更具体地说，本发明涉及调节细胞凋亡抑制剂（IAP）活性的大环化合物和/或可用于治疗诸如癌症的医学病症。
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公开(公告)号：WO2019036433A2
公开(公告)日：2019-02-21
申请号：PCT/US2018/046637
申请日：2018-08-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： KRYSTEK, JR., Stanley R. , ZHANG, Yong , VITE, Gregory D. , RAJPAL, Arvind , RAO-NAIK, Chetana , MORIN, Paul E. , SRINIVASAN, Mohan , LIN, Zheng , LAFONT, Virginie , PRITSKER, Alla
IPC: A61K39/395 , C07K16/28 , A61K47/68 , A61K47/65 , A61K47/60
Abstract: A prodrugged antibody has a blocking moiety attached to a Cys on its heavy or light chain via a linker having a cleavable moiety. The blocking moiety inhibits binding of the antibody to its antigen. Cleavage of the cleavable moiety releases the blocking moiety and restores ability of the antibody to bind to its antigen.
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3.发明申请MACROCYCLIC BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, PREPARATION AND USES 审中-公开大分子苯并二唑二聚体，共聚物，制备和用途
公开(公告)号：WO2016209951A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038750
申请日：2016-06-22
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： ZHANG, Yong , BORZILLERI, Robert, M. , TEBBEN, Andrew, J. , STANG, Erik, M. , DONNELL, Andrew, F. , SCHROEDER, Gretchen, M. , PEREZ, Heidi, L. , WEI, Donna, D.
IPC: C07D519/00 , A61K31/5513 , A61K31/5517 , A61P35/00
CPC classification number: C07D498/22 , A61K31/5513 , A61K31/5517 , A61K47/48384 , A61K47/48569 , A61K47/48592 , A61K47/48615 , A61K47/48638 , A61K47/48715 , A61K47/6801 , A61K47/6803 , A61K47/6851 , A61K47/6857 , A61K47/6859 , A61K47/6863 , A61K47/6869 , A61K47/6889 , C07D519/00 , C07K16/30 , C07K16/3023 , C07K16/3046 , C07K16/3069
Abstract: Macrocyclic benzodiazepine dimers having a structure represented by formula (I) where A and B are independently according to formulae (Ia) or (Ib) ]; and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).
Abstract translation: 具有由式（I）表示的结构的大环苯并二氮杂二聚体，其中A和B独立地是根据式（Ia）或（Ib）]; 并且式（I），（Ia）和（Ib）中的其它变量如申请中所定义。 这种二聚体可用作抗癌剂，特别是用作抗体 - 药物偶联物（ADC）中的药物成分时。
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4.发明申请BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING 审中-公开苯并二唑二聚体，其结合物及其制备和使用方法
公开(公告)号：WO2016115191A1
公开(公告)日：2016-07-21
申请号：PCT/US2016/013136
申请日：2016-01-13
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： ZHANG, Yong , MCDONALD, Ivar M. , CHOWDARI, Naidu S. , HUYNH, Tram N. , BORZILLERI, Robert M. , GANGWAR, Sanjeev
IPC: C07D519/00 , C07D487/04 , A61K31/437 , A61P35/00
CPC classification number: C07K5/06052 , A61K47/6843 , A61K47/6849 , C07D487/04 , C07D519/00 , C07K16/18 , C07K16/28 , C07K16/30 , C07K2317/76
Abstract: Benzodiazepine dimers having a structure represented by wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
Abstract translation: 具有由式（I），（Ia）和（Ib）中的变量表示的结构的苯并二氮杂二聚体如本申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。
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公开(公告)号：WO2014074665A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068856
申请日：2013-11-07
Applicant: BRISTOL-MYERS SQUIBB COMPANY , ENSEMBLE THERAPEUTICS
Inventor： BORZILLERI, Robert M. , ZHANG, Yong , MILLER, Michael M. , FRALEY, Andrew W.
IPC: C07K7/06 , C07D249/04 , C07D487/06 , C07D487/16 , C07D498/06 , C07D498/16 , A61P35/00
Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Abstract translation: 公开了利用本发明化合物调节凋亡抑制剂（IAP）的活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病和失调性细胞凋亡障碍的疾病的方法。
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Patent Agency Ranking
公开(公告)号：WO2014011974A1
公开(公告)日：2014-01-16
申请号：PCT/US2013/050247
申请日：2013-07-12
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： PURANDARE, Ashok Vinayak , FINK, Brian E. , JOHNSON, Walter Lewis , HART, Amy C. , HE, Liqi , HUYNH, Tram N. , INGHRIM, Jennifer , MASTALERZ, Harold , SANG, Xiaopeng , TARBY, Christine M. , WAN, Honghe , VACCARO, Wayne , ZHANG, Guifen , ZHAO, Yufen , ZIMMERMANN, Kurt , ZHANG, Yong , CHEN, Libing , CHEN, Bin , TOKARSKI, John S. , GAVAI, Ashvinikumar V.
IPC: C07D487/04 , A61K31/53 , A61P17/08 , A61P19/02 , A61P35/00
CPC classification number: C07D487/04 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/55 , A61K31/551 , A61K31/675 , A61K45/06 , C07D471/10 , C07D487/08 , C07D487/10 , C07D487/22 , C07D498/04 , C07D519/00 , C07F7/1804 , C07F9/65213 , C07F9/6561 , C07F9/65616
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）咪唑三嗪抑制蛋白激酶活性，从而使它们用作抗癌剂。
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公开(公告)号：WO2019046500A1
公开(公告)日：2019-03-07
申请号：PCT/US2018/048666
申请日：2018-08-30
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： DODD, Dharmpal S. , FINK, Brian E. , ZHANG, Yong
Abstract: The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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8.发明申请HETEROARYLENE-BRIDGED BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING 审中-公开异丁烯二苯并二氮杂双环十二烷二酮，其结合物及其制备和使用方法
公开(公告)号：WO2016115201A1
公开(公告)日：2016-07-21
申请号：PCT/US2016/013154
申请日：2016-01-13
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： MCDONALD, Ivar, M. , CHOWDARI, Naidu, S. , JOHNSON, Walter, Lewis , ZHANG, Yong , BORZILLERI, Robert, M. , GANGWAR, Sanjeev
IPC: C07D487/04 , C07D519/00 , A61K31/437 , A61P35/00
CPC classification number: C07D471/04 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07D487/04 , C07D519/00 , C07K5/06052
Abstract: Benzodiazepine dimers having a structure represented by (I) wherein X comprises a heteroaromatic moiety and is as further defined in the application; R 1 is (Ia) or (Ib); and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
Abstract translation: 具有由（I）表示的结构的苯并二氮杂二聚体，其中X包含杂芳族部分并且在本申请中进一步定义; R1是（Ia）或（Ib）; 式（I），（Ia）和（Ib）中的其它变量如本申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。
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公开(公告)号：WO2014074658A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068834
申请日：2013-11-07
Inventor： BORZILLERI, Robert M. , ZHANG, Yong , MILLER, Michael M. , SEIGAL, Benjamin A.
IPC: C07D471/08 , C07D471/18 , C07D498/08 , C07D498/18 , C07D498/22 , A61K31/395 , C07K5/00 , A61P35/00
CPC classification number: C07K7/06 , C07D471/08 , C07D471/18 , C07D498/08 , C07D498/18 , C07D498/22 , C07K7/56
Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Abstract translation: 公开了调节细胞凋亡抑制剂（IAP）的活性的化合物，含有所述化合物的药物组合物以及治疗增殖性疾病和失调性细胞凋亡疾病如癌症的方法，所述化合物利用 发明。
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公开(公告)号：WO2013071039A1
公开(公告)日：2013-05-16
申请号：PCT/US2012/064349
申请日：2012-11-09
Applicant: ENSEMBLE THERAPEUTICS , BRISTOL-MYERS SQUIBB COMPANY
Inventor： SEIGAL, Benjamin Adam , TERRETT, Nicholas , FRALEY, Andrew , CONNORS, William , BRIGGS, Timothy , BORZILLERI, Robert M. , ZHANG, Yong , MATHIEU, Steven , CARTER, Percy H.
Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.
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