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公开(公告)号：US20210346364A1
公开(公告)日：2021-11-11
申请号：US17385258
申请日：2021-07-26
发明人： John P. CALDWELL , Reynalda DE JESUS , Fa-Xiang DING , Charles J. GIll , Ginny Dai HO , Sookhee N. HA , Sandra J. KOSEOGLU , Marc A. LABROLI , Sang Ho LEE , Christina MADSEN-DUGGAN , Mihir MANDAL , Terry ROEMER , Jing SU , Christopher Michael TAN , Zheng TAN , Haifeng TANG , Hao WANG , Christine YANG , Shu-Wei YANG
IPC分类号： A61K31/4439 , A61P31/04 , A61K31/407 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/431 , A61K31/4375 , A61K31/438 , A61K31/4709 , A61K31/5377 , A61K31/5383 , C07D263/26 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D498/04
摘要： Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.
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公开(公告)号：US20210308090A1
公开(公告)日：2021-10-07
申请号：US17220675
申请日：2021-04-01
IPC分类号： A61K31/337 , A61K31/4155 , A61K31/4375 , A61K31/4545 , A61K31/517 , A61K47/64 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K47/54 , A61K31/519
摘要： Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.
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公开(公告)号：US11090313B2
公开(公告)日：2021-08-17
申请号：US16661660
申请日：2019-10-23
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
IPC分类号： A61K31/58 , A61K31/436 , A61K31/215 , A61K31/352 , A61K31/36 , A61K31/382 , A61K31/404 , A61K31/4164 , A61K31/4166 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/4706 , A61K31/56 , A61K31/353 , A61K31/407 , A61K31/435 , A61K31/473 , A61K31/565 , G01N33/50 , C12Q1/6809
摘要： The invention provides a method for (a) increasing skeletal muscle mass; (b) reducing skeletal muscle atrophy; (c) increasing muscular strength; (d) promoting muscle growth; (e) decreasing muscle wasting; or (f) increasing strength per unit of muscle mass in an animal identified or having been identified to be in need of one or more of (a)-(f), the method comprising administering to the animal an effective amount of a compound of formula: or a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, thereby accomplishing one or more of (a)-(f).
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公开(公告)号：US20210228553A1
公开(公告)日：2021-07-29
申请号：US17099115
申请日：2020-11-16
申请人： BeiGene, Ltd.
发明人： Jing SONG , Lai WANG , Kang LI , Tong ZHANG , Lusong LUO , Min WEI , Zhiyu TANG , Guoliang ZHANG , Changyou ZHOU
IPC分类号： A61K31/4375 , A61P35/00 , C07K16/28
摘要： Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.
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公开(公告)号：US11065258B2
公开(公告)日：2021-07-20
申请号：US16538293
申请日：2019-08-12
发明人： Leonard I. Zon , Alison M. Taylor
IPC分类号： A61K31/553 , A61K31/495 , A61K31/4965 , A61K31/54 , A61K31/5415 , A61K31/145 , A61K31/4184 , A61K31/4375 , A61K31/4418
摘要： The present invention relates generally to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to methods for the use of calmodulin inhibitors and calcium channel blockers for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA).
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公开(公告)号：US20210196693A1
公开(公告)日：2021-07-01
申请号：US17180241
申请日：2021-02-19
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K31/4375 , A61K9/10 , A61K9/00 , A61K47/38
摘要： Provided herein are low impurity compositions comprising a compound represented by Formula (I): which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
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公开(公告)号：US20210196692A1
公开(公告)日：2021-07-01
申请号：US17180234
申请日：2021-02-19
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K31/4375 , A61K9/16 , A61K9/20
摘要： Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
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118.发明申请公开(公告)号：US20210186980A1
公开(公告)日：2021-06-24
申请号：US17171908
申请日：2021-02-09
申请人： KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY , YONSEI UNIVERSITY, UNIVERSITY-INDUSTRY FOUNDATION (UIF)
发明人： Jeong Ho LEE , Jae Seok LIM , Woo-ll KIM , Dong Seok KIM , Hoon Chul KANG , Se Hoon KIM
IPC分类号： A61K31/5377 , A61K31/436 , A61K31/519 , A01K67/027 , C12N15/90 , G01N33/68 , C12Q1/6883 , C12N15/85 , A61K31/501 , A61K31/711 , A61K31/4375 , A61P25/08
摘要： Provided is a use of the prophylaxis, amelioration or therapy of intractable epilepsy, for example, Focal Cortical Dysplasia (FCD).
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公开(公告)号：US11034692B1
公开(公告)日：2021-06-15
申请号：US16542129
申请日：2019-08-15
申请人： Genentech, Inc.
发明人： Bryan Chan , Blake Daniels , Joy Drobnick , Lewis Gazzard , Timothy Heffron , Malcolm Huestis , Jun Liang , Sushant Malhotra , Rohan Mendonca , Naomi Rajapaksa , Michael Siu , Craig Stivala , John Tellis , Weiru Wang , BinQing Wei , Aihe Zhou , Matthew W. Cartwright , Emanuela Gancia , Graham Jones , Michael Lainchbury , Andrew Madin , Eileen Seward , David Favor , Kin Chiu Fong , Andrew Good , Yonghan Hu , Baihua Hu , Aijun Lu
IPC分类号： C07D471/04 , A61K45/06 , A61P35/00 , A61K31/444 , A61K31/4375 , A61K31/506 , C07D519/00 , A61K31/4545 , A61K31/4725 , A61K31/5383 , A61K31/496 , A61K31/5377 , A61K31/5025 , A61K31/551 , A61K31/55
摘要： Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
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公开(公告)号：US20210169876A1
公开(公告)日：2021-06-10
申请号：US17114379
申请日：2020-12-07
申请人： Buck Institute for Research on Aging , Unity Biotechnology, Inc. , Mayo Foundation for Medical Education and Research
发明人： Remi-Martin Laberge , Judith Campisi , Marco Demaria , Nathaniel David , James L. Kirkland , Tamar Tchkonia , Yi Zhu
IPC分类号： A61K31/496 , A61P11/00 , A61P9/10 , A61P27/02 , A61K31/428 , A61K31/495 , A61K31/5377 , C12N15/113 , A61P25/28 , A61K47/68 , A61K31/404 , A61K31/4375 , A61K45/06 , A61K31/4178 , A61K31/728 , C12N5/00 , A61K47/36 , A61K9/00
摘要： Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.
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