公开(公告)号：US10577381B2

公开(公告)日：2020-03-03

申请号：US16203108

申请日：2018-11-28

申请人： Rigel Pharmaceuticals, Inc.

发明人： Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

IPC分类号： C07D498/04 ,  C07F9/6574 ,  C07F9/6561 ,  C07F9/6558 ,  A61K31/5383 ,  A61K31/675

摘要： The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

公开(公告)号：US10565015B2

公开(公告)日：2020-02-18

申请号：US16134568

申请日：2018-09-18

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Pavel Nagorny ,  Siyuan Sun ,  Alonso Arguelles

IPC分类号： C07F15/00 ,  C07F9/6571 ,  B01J31/24 ,  C07F9/6561 ,  G06F9/50 ,  G06F11/30 ,  G06F9/48 ,  C07C2/86 ,  C07C67/343 ,  C07D213/30 ,  C07D215/06 ,  C07D493/10

摘要： Provided herein is a compound of formula (I): wherein each R is independently selected from the group consisting of C1-8 alkyl, C1-8 heteroalkyl having 1-4 heteroatoms independently selected from N, O, and S, C3-6 cycloalkyl, 3-10 membered heterocycloalkyl having 1-4 heteroatoms independently selected from N, O, and S, C6-10 aryl, and 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from N, O, and S; each X is independently selected from OH, PAr2, P(O)Ar2, OPAr2, C3-6 cycloalkyl, 3-10 membered heterocycloalkyl having 1-4 heteroatoms independently selected from N, O, and S or each X together form O2PNR′2; Ar is C6-10aryl; and each R′ is independently selected from hydrogen and C1-8 alkyl. Also provided are methods of making and using the compound of formula (I).

公开(公告)号：US10550140B2

公开(公告)日：2020-02-04

申请号：US16164632

申请日：2018-10-18

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Godwin Pais ,  Akihiro Hashimoto ,  Qiuping Wang ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： C07D403/06 ,  C07F9/572 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14 ,  C07D471/04 ,  C07D417/06 ,  C07F9/6561 ,  C07F5/02 ,  C07D417/14 ,  C07F7/08 ,  C07D413/14 ,  C07D487/04 ,  C07D405/14 ,  C07D403/08 ,  C07D413/06 ,  C07F9/6558 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/00 ,  C07D209/14 ,  C07D209/40 ,  C07D405/12 ,  C07D417/12 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  A61K9/00 ,  A61K31/4045 ,  A61K31/444 ,  A61K31/501 ,  A61K31/519 ,  C07D209/12 ,  C07D209/30 ,  C07D209/44 ,  C07D209/88 ,  C07D471/08

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US10544186B2

公开(公告)日：2020-01-28

申请号：US16348234

申请日：2017-11-06

申请人： Merck Patent GmbH

发明人： Nikolai Mykola Ignatyev ,  Walter Frank ,  Peter Barthen ,  Myroslav Vysotsky

IPC分类号： C07D207/404 ,  C07D213/89 ,  C07D249/18 ,  C07D263/08 ,  C07D403/14 ,  C07D471/04 ,  C07F9/535 ,  C07F9/6518 ,  C07F9/6561 ,  C07K1/10 ,  C07D253/08 ,  C07K5/065

摘要： The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.

公开(公告)号：US20200010492A1

公开(公告)日：2020-01-09

申请号：US16490837

申请日：2016-02-28

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Fajun NAN ,  Xin XIE ,  Linhai CHEN ,  Qing ZHANG ,  Yufeng XIAO ,  Hui YANG

IPC分类号： C07F9/09 ,  C07F9/6561 ,  C07F9/6553 ,  C07F9/655

摘要： The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like.

公开(公告)号：US20190388442A1

公开(公告)日：2019-12-26

申请号：US16567092

申请日：2019-09-11

申请人： The Regents of the University of California

发明人： Karl Y. Hostetler ,  James R. Beadle ,  Nadejda Valiaeva

IPC分类号： A61K31/675 ,  C07F9/6561 ,  C07F9/6512 ,  A61K9/00 ,  A61K31/685

摘要： The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.

公开(公告)号：US20190382426A1

公开(公告)日：2019-12-19

申请号：US16451673

申请日：2019-06-25

申请人： Yamasa Corporation

发明人： Hisaki TANAKA ,  Kazuya ISHIGE

IPC分类号： C07F9/6561

摘要： Though 3′,5′-cyclic diadenylic acid was conventionally provided only as a freeze-dried product, a solid material other than a freeze-dried product and a manufacturing method thereof is provided. By a step of adding acid to an aqueous solution of 3′,5′-cyclic diadenylic acid so as to lower pH to 1 to 3, an inclusion compound of 3′,5′-cyclic diadenylic acid can be obtained. Said manufacturing method is an extremely simple and easy method and does not need a special machine or the like.

公开(公告)号：US10508118B2

公开(公告)日：2019-12-17

申请号：US15570119

申请日：2016-04-25

申请人： Xiamen University

发明人： Xianming Deng ,  Zhongji Zhuang ,  Zhou Deng ,  Xiaoxing Huang ,  Yan Liu ,  Ting Zhang ,  Wei Huang ,  Qingyan Xu ,  Zhiyu Hu

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61K31/675 ,  C07F9/6561 ,  A61P35/02

摘要： The present invention relates to a compound of formula I, a stereoisomer, a prodrug, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, and a process for preparing the same, a pharmaceutical composition comprising the same, and use of the compound in the preparation of medicine preventing and treating tumors, wherein the substituents are as defined in the specification.

公开(公告)号：US10478425B2

公开(公告)日：2019-11-19

申请号：US16078875

申请日：2017-02-24

申请人： Shionogi & Co., Ltd.

发明人： Yuusuke Tamura ,  Hiroki Ozasa

IPC分类号： C07D401/10 ,  C07D401/14 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  C07D471/04 ,  C07D519/00 ,  A61P3/10 ,  C07F9/6561

摘要： Provided is a compound which is useful as an AMPK activator. The compound is represented by formula: wherein the symbols are defined in the specification.

公开(公告)号：US10472372B2

公开(公告)日：2019-11-12

申请号：US15753264

申请日：2016-08-17

申请人： Purdue Research Foundation ,  National University Corporation Kumamoto University

发明人： Arun K. Ghosh ,  Hiroaki Mitsuya

IPC分类号： C07D493/04 ,  C07D491/20 ,  C07D498/04 ,  C07F9/6561

摘要： Various embodiments relate to a compound of the formula (I): wherein X, X1, R1—R4 and R7 are defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I), or a pharmaceutical compositions comprising compounds of the formula (I), to a patient in need thereof.