公开(公告)号：US20180244606A1

公开(公告)日：2018-08-30

申请号：US15758709

申请日：2016-09-16

申请人： Metacrine, Inc.

发明人： Nicholas D. SMITH ,  Steven P. GOVEK ,  Johnny Y. NAGASAWA

IPC分类号： C07C233/54 ,  A61K45/06 ,  A61K31/216 ,  C07C271/28 ,  A61K31/27 ,  C07C255/57 ,  A61K31/277 ,  C07D309/08 ,  A61K31/351 ,  A61K31/337 ,  C07D305/08 ,  C07D335/02 ,  A61K31/382 ,  C07D205/04 ,  A61K31/397 ,  C07D265/30 ,  A61K31/5375 ,  C07C323/50 ,  C07C317/44 ,  C07D211/94 ,  A61K31/45 ,  C07C235/04 ,  C07C235/40 ,  C07D211/06 ,  A61K31/4453 ,  C07C235/82 ,  C07D231/12 ,  A61K31/415 ,  C07D213/40 ,  A61K31/4406 ,  C07D261/08 ,  A61K31/42 ,  C07D295/135 ,  A61K31/402 ,  C07D231/56 ,  A61K31/416 ,  A61K31/404 ,  C07D209/04 ,  C07D317/58 ,  A61K31/36 ,  C07D295/26 ,  C07D295/195 ,  C07D277/28 ,  A61K31/426 ,  A61K31/4184 ,  C07D235/08 ,  C07D249/18 ,  A61K31/4192 ,  C07D239/42 ,  A61K31/505 ,  C07D241/20 ,  A61K31/4965 ,  C07D237/20 ,  A61K31/50 ,  A61P1/16

CPC分类号： C07C233/54 ,  A61K31/16 ,  A61K31/216 ,  A61K31/27 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/36 ,  A61K31/382 ,  A61K31/397 ,  A61K31/402 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/4453 ,  A61K31/45 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5375 ,  A61K45/06 ,  A61P1/16 ,  C07C233/63 ,  C07C233/65 ,  C07C233/81 ,  C07C233/87 ,  C07C235/04 ,  C07C235/16 ,  C07C235/40 ,  C07C235/56 ,  C07C235/64 ,  C07C235/82 ,  C07C237/24 ,  C07C255/57 ,  C07C255/60 ,  C07C271/24 ,  C07C271/28 ,  C07C311/07 ,  C07C311/08 ,  C07C317/32 ,  C07C317/44 ,  C07C323/50 ,  C07C323/61 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/16 ,  C07C2602/42 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/04 ,  C07D211/06 ,  C07D211/62 ,  C07D211/76 ,  C07D211/94 ,  C07D211/96 ,  C07D213/40 ,  C07D231/12 ,  C07D231/56 ,  C07D235/04 ,  C07D235/08 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D249/18 ,  C07D261/08 ,  C07D265/30 ,  C07D277/28 ,  C07D295/088 ,  C07D295/135 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D309/08 ,  C07D317/58 ,  C07D319/12 ,  C07D335/02 ,  A61K2300/00

摘要： Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

公开(公告)号：US10039844B2

公开(公告)日：2018-08-07

申请号：US14956431

申请日：2015-12-02

申请人： The Board of Trustees of the Leland Stanford Junior University

发明人： Timothy Witney ,  Michelle L. James ,  Sanjiv S. Gambhir

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07D295/26 ,  G01N33/574 ,  G01N33/60

摘要： A novel pyruvate kinase M2 (PKM2)-specific activator, [11C]DASA-23 and derivatives thereof, and methods for their rapid synthesis are provided. The probes are particularly useful in methods for the non-invasive positron emission tomography (PET) detection and imaging of PKM2 expression in subcutaneous and orthotopic tumors. [11C]DASA-23 cell uptake correlates with PKM2 protein expression in cultured tumor cells and orthotopic tumors are delineated from the surrounding normal brain tissue in vivo.

公开(公告)号：US09994537B2

公开(公告)日：2018-06-12

申请号：US15672165

申请日：2017-08-08

申请人： Abide Therapeutics, Inc.

发明人： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Olivia D. Weber ,  Dong-Hui Wang

IPC分类号： C07D295/205 ,  C07D207/08 ,  C07D471/10 ,  C07D417/04 ,  C07D403/04 ,  C07D401/04 ,  C07D295/26 ,  C07D265/30 ,  C07D207/12 ,  C07D211/38 ,  C07D211/58 ,  C07D207/14 ,  C07D211/14 ,  C07D498/08 ,  C07D211/62 ,  C07D487/04 ,  C07D207/16

CPC分类号： C07D295/205 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/14 ,  C07D211/38 ,  C07D211/58 ,  C07D211/62 ,  C07D265/30 ,  C07D295/26 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/10 ,  C07D487/04 ,  C07D498/08

摘要： Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

公开(公告)号：US09975864B2

公开(公告)日：2018-05-22

申请号：US15100361

申请日：2014-12-02

申请人： Mylan Laboratories Ltd.

发明人： Lakshmana Rao Vadali ,  Rameshbabu Konda ,  Ramesh Dandala

IPC分类号： C07D295/26 ,  C07D203/24 ,  C07D417/12

CPC分类号： C07D295/26 ,  C07B2200/13 ,  C07D203/24 ,  C07D417/12

摘要： The present disclosure provides crystalline piperidine sulfamoyl intermediates of formula 8 and 9. The present disclosure also relates to an improved process for the preparation of cobicistat using compounds of formulae 8 and 9.

公开(公告)号：US20180043040A1

公开(公告)日：2018-02-15

申请号：US15674701

申请日：2017-08-11

申请人： The Board of Trustees of the Leland Stanford Junior University

发明人： Corinne Gaye Beinat ,  Israt Shamima Alam ,  Michelle L. James ,  Sanjiv S. Gambhir ,  Ananth Srinivasan

IPC分类号： A61K51/04 ,  C07B59/00 ,  C07D295/26

摘要： The present disclosure provides a positron emission tomography (PET)-detectable 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) probe that can selectively bind to the pyruvate kinase variant M2 (PKM2) found in cancer cells, such as of human glioma. Given the importance of PKM2 in the regulation of tumor metabolism, there is an on-going need to non-invasively measure its expression through the development of PKM2-specific radiopharmaceuticals. Precursors useful for the synthesis of the radiolabeled [18F]DASA-23-PKM2-specific probe and related compounds, and their methods of synthesis, are provided. Since the half-life of the 18F isotope is approximately 110 min, it is advantageous for a practitioner to attach the radionuclide to the precursor shortly before administration. Therefore, a precursor compound suitable for receiving the radionuclide and capable of specifically binding to the PKM2 variant can be provided.

公开(公告)号：US20170320818A1

公开(公告)日：2017-11-09

申请号：US15656769

申请日：2017-07-21

申请人： DREXEL UNIVERSITY ,  BARUCH S. BLUMBERG INSTITUTE

发明人： JU-TAO GUO ,  XIAODONG XU ,  TIMOTHY M. BLOCK

IPC分类号： C07C311/46 ,  A61K31/167 ,  C07D295/26 ,  C07D281/16 ,  C07D223/04 ,  C07D213/40 ,  C07D211/96 ,  C07D307/52 ,  A61K31/18 ,  A61K31/341 ,  A61K31/4406 ,  A61K31/4453 ,  A61K31/553 ,  A61K31/55 ,  A61K31/54 ,  A61K31/5375 ,  C07D307/68 ,  A61K31/44 ,  A61K31/541 ,  A61K31/445 ,  A61K31/5377

摘要： The present invention provides sulfamoylbenzamide derivatives, and pharmaceutical compositions thereof. In certain embodiments, the compounds and pharmaceutical compositions of the invention inhibit pregenomic RNA encapsidation. In other embodiments, the compounds and pharmaceutical compositions of the invention are useful for treating Hepatitis B virus (HBV) infection.

公开(公告)号：US20170233354A1

公开(公告)日：2017-08-17

申请号：US15500174

申请日：2015-07-30

申请人： INSERM (INSTITUT NATIONAL DE SANTÉ ET DE LA RECHERCHE MÉDICALE) ,  UNIVERSITE DE MONTPELLIER ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITÉ DE STRASBOURG

发明人： Jean VALMIER ,  Jean-Philippe LEYRIS ,  Didier ROGNAN ,  Martine SCHMITT

IPC分类号： C07D295/26 ,  C07D249/08 ,  C07D233/64 ,  A61K31/18 ,  C07D257/04 ,  C07C311/20 ,  A61K31/4453 ,  A61K31/454 ,  C07D209/08 ,  C07D235/04

CPC分类号： C07D295/26 ,  A61K31/18 ,  A61K31/4453 ,  A61K31/454 ,  C07C311/20 ,  C07D209/08 ,  C07D233/64 ,  C07D235/04 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/57

摘要： The invention pertains to novel FLT3 receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.

公开(公告)号：US09707230B2

公开(公告)日：2017-07-18

申请号：US15076258

申请日：2016-03-21

申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services

发明人： Craig J. Thomas ,  Douglas S. Auld ,  James Inglese ,  Amanda P. Skoumbourdis ,  Jian-Kang Jiang ,  Matthew B. Boxer

IPC分类号： A61K31/496 ,  C07D495/14 ,  A61K31/5025 ,  A61K31/445 ,  A61K31/495 ,  C07D295/26 ,  C07D319/18

CPC分类号： A61K31/496 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5025 ,  C07D295/26 ,  C07D319/18 ,  C07D495/14

摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,

公开(公告)号：US09689841B2

公开(公告)日：2017-06-27

申请号：US14241358

申请日：2012-08-27

申请人： Gyula Vigh ,  Ming-Chien Li

发明人： Gyula Vigh ,  Ming-Chien Li

IPC分类号： C07C311/32 ,  G01N27/447 ,  C09K11/06 ,  C07C311/42 ,  C07D233/64 ,  C07D295/088 ,  C07D295/13 ,  C07D295/26 ,  C07C311/37 ,  G01N33/58

CPC分类号： G01N27/44795 ,  C07C311/32 ,  C07C311/37 ,  C07C311/42 ,  C07C2603/50 ,  C07D233/64 ,  C07D295/088 ,  C07D295/13 ,  C07D295/26 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1033 ,  C09K2211/1044 ,  G01N27/447 ,  G01N33/582 ,  Y10T436/143333

摘要： UV-Absorbing and fluorescent pl markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.

公开(公告)号：US20170166542A1

公开(公告)日：2017-06-15

申请号：US15372778

申请日：2016-12-08

申请人： Commissariat a l'Energie Atomique et aux Energies Alternatives

发明人： Niklas von Wolff ,  Joëlle Char ,  Thibault Cantat

IPC分类号： C07D295/26 ,  C07C315/04 ,  C07D213/71

CPC分类号： C07D295/26 ,  C07C315/04 ,  C07D213/71 ,  C07D265/30 ,  C07C317/14 ,  C07C317/22

摘要： A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.