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公开(公告)号：US09034866B2
公开(公告)日：2015-05-19
申请号：US13768873
申请日：2013-02-15
申请人： Genentech, Inc.
IPC分类号： C07D498/04 , C07D498/14 , C07D519/00 , C07D513/04 , C07D498/00 , C07D498/12
CPC分类号： C07D498/04 , C07D487/04 , C07D498/00 , C07D498/12 , C07D513/04 , C07D519/00
摘要： The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
摘要翻译： 本发明涉及式I的新化合物：其中A1，A2，A3，A4，A5，A6，R2，R4，R5，R6，R7，R8和下标m和n各自具有本文所述的含义。 式I化合物及其药物组合物可用于治疗观察到NF-kB信号传导的不期望或过度活化的疾病和病症。
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公开(公告)号：US20230271981A1
公开(公告)日：2023-08-31
申请号：US18313703
申请日：2023-05-08
申请人： AMGEN INC.
发明人： BRIAN S. LUCAS , NICK A. PARAS
IPC分类号： C07D513/10 , C07D513/08 , C07D498/00 , C07C59/68 , C07C59/56 , C07C311/11
CPC分类号： C07D513/10 , C07D513/08 , C07D498/00 , C07C59/68 , C07C59/56 , C07C311/11
摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,
and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.-
公开(公告)号：US07247634B2
公开(公告)日：2007-07-24
申请号：US11034195
申请日：2005-01-12
申请人： Zhenkun Ma , Yafei Jin , Jing Li , Charles Z. Ding , Keith P. Minor , Jamie C. Longgood , In Ho Kim , Susan Harran , Keith Combrink , Timothy W. Morris
发明人： Zhenkun Ma , Yafei Jin , Jing Li , Charles Z. Ding , Keith P. Minor , Jamie C. Longgood , In Ho Kim , Susan Harran , Keith Combrink , Timothy W. Morris
IPC分类号： C07D498/08 , A61K31/395 , A61P31/04
CPC分类号： C07D498/00
摘要： Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.
摘要翻译： 本发明要求具有抗微生物活性的利福霉素衍生物，包括抗药性微生物的活性。 本发明的利福霉素衍生物是唯一设计的，因为它们具有通过利福霉素部分的C-3碳与连接基共价连接的利福霉素部分，接头又与治疗部分或抗菌剂/药效基团共价连接。 治疗部分可以是喹诺酮，恶唑烷酮，大环内酯，氨基糖苷，四环素核心或与抗菌剂相关的结构/药效团。
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公开(公告)号：US09850256B2
公开(公告)日：2017-12-26
申请号：US15516290
申请日：2015-10-14
发明人： Sylvaine Cren , Astrid Friedli , Georg Rueedi , Cornelia Zumbrunn
IPC分类号： C07D498/04 , C07D417/14 , C07D498/00 , A61K31/5365 , A61K31/00
CPC分类号： C07D498/04 , A61K31/00 , A61K31/5365 , C07D417/14 , C07D498/00
摘要： The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, U1, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
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公开(公告)号：US5914319A
公开(公告)日：1999-06-22
申请号：US522825
申请日：1995-09-01
IPC分类号： A61K38/00 , A61P7/02 , C07C229/00 , C07D271/06 , C07D271/12 , C07D285/08 , C07D285/14 , C07D417/00 , C07D498/00 , C07D513/00 , C07F9/02 , C07F9/28 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A61K38/00 , C07C229/00 , C07D271/06 , C07D271/12 , C07D285/08 , C07D285/14 , C07D417/00 , C07D498/00 , C07D513/00 , C07F9/02 , C07F9/28 , C07K17/00 , C07K5/00 , C07K7/00
摘要： This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
摘要翻译： 本发明涉及具有式I XY-NH-（CH2）r-GI的凝血酶抑制化合物，其中X，Y，r和G具有描述中定义的值，以及含有这些化合物的药物制剂及其用途的方法 凝血酶抑制剂，凝血抑制剂和血栓栓塞障碍剂。
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公开(公告)号：US11685747B2
公开(公告)日：2023-06-27
申请号：US17075864
申请日：2020-10-21
申请人： AMGEN INC.
发明人： Nick A. Paras
IPC分类号： C07C311/11 , C07D513/10 , C07D513/08 , C07D498/00 , C07C59/68 , C07C59/56
CPC分类号： C07D513/10 , C07C59/56 , C07C59/68 , C07C311/11 , C07D498/00 , C07D513/08
摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,
and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.-
公开(公告)号：US20170305927A1
公开(公告)日：2017-10-26
申请号：US15516290
申请日：2015-10-14
发明人： Sylvaine CREN , Astrid FRIEDLI , Georg RUEEDI , Cornelia ZUMBRUNN
IPC分类号： C07D498/04 , C07D417/14 , A61K31/5365 , C07D498/00 , A61K31/00
CPC分类号： C07D498/04 , A61K31/00 , A61K31/5365 , C07D417/14 , C07D498/00
摘要： The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, Ul, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
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公开(公告)号：US20150166569A1
公开(公告)日：2015-06-18
申请号：US14622446
申请日：2015-02-13
申请人： Genentech, Inc.
IPC分类号： C07D498/04 , C07D513/04 , C07D519/00 , C07D487/04
CPC分类号： C07D498/04 , C07D487/04 , C07D498/00 , C07D498/12 , C07D513/04 , C07D519/00
摘要： The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
摘要翻译： 本发明涉及式I的新化合物：其中A1，A2，A3，A4，A5，A6，R2，R4，R5，R6，R7，R8和下标m和n各自具有本文所述的含义。 式I化合物及其药物组合物可用于治疗观察到NF-kB信号传导的不期望或过度活化的疾病和病症。
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公开(公告)号：US20110171172A1
公开(公告)日：2011-07-14
申请号：US12738540
申请日：2008-10-16
申请人： M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana
发明人： M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana
IPC分类号： A61K38/21 , C07D271/12 , C07D498/10 , A61K31/4184 , A61K31/438 , A61K31/7088 , A61K39/395 , A61P35/00 , A61P35/02 , A61P17/06 , A61P29/00 , A61P19/02 , A61P9/00 , A61P31/10 , A61N5/00
CPC分类号： C07D498/00
摘要： The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
摘要翻译： 本发明涉及下式（I）的化合物（其中R 1，R 2，R 3，p，E，环A和环B如本文所定义）。 本发明还涉及包含这些化合物的组合物（包括药学上可接受的组合物），其单独并与一种或多种另外的治疗剂组合，以及其用于抑制KSP驱动蛋白活性的方法，以及用于治疗相关的细胞增殖性疾病或病症 与KSP驱动组织活动。
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公开(公告)号：US12024529B2
公开(公告)日：2024-07-02
申请号：US18313703
申请日：2023-05-08
申请人： AMGEN INC.
发明人： Robert Farrell
IPC分类号： C07D249/18 , C07C59/56 , C07C59/68 , C07C311/11 , C07D498/00 , C07D513/08 , C07D513/10
CPC分类号： C07D513/10 , C07C59/56 , C07C59/68 , C07C311/11 , C07D249/18 , C07D498/00 , C07D513/08
摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,
and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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