公开(公告)号：US20170369509A1

公开(公告)日：2017-12-28

申请号：US15697847

申请日：2017-09-07

申请人： Shionogi & Co., Ltd. ,  ViiV Healthcare Company

发明人： Brian A. JOHNS ,  Takashi KAWASUJI ,  Teruhiko TAISHI ,  Yoshiyuki TAODA

IPC分类号： C07D498/14 ,  C07D498/20 ,  C07D498/04 ,  C07D471/14 ,  A61K31/4985 ,  C07D471/04 ,  A61K45/06 ,  A61K31/5365 ,  C07D498/22 ,  C07D471/22

CPC分类号： C07D498/14 ,  A61K9/0053 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/551 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D498/04 ,  C07D498/20 ,  C07D498/22

摘要： The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

公开(公告)号：US09839687B2

公开(公告)日：2017-12-12

申请号：US14799666

申请日：2015-07-15

申请人： Suzhou M-conj Biotech Co., Ltd ,  Robert Yongxin Zhao

发明人： Robert Yongxin Zhao

IPC分类号： C07D417/14 ,  C07D413/14 ,  C07D407/14 ,  C07D403/14 ,  C07D309/14 ,  C07C237/52 ,  C07C233/20 ,  C07C59/76 ,  A61K39/395 ,  C07K16/28 ,  A61K45/06 ,  A61K47/48 ,  C07D207/46 ,  C07D407/12 ,  C07D413/04 ,  C07D417/12 ,  C07D493/04 ,  C07D498/14 ,  C07D277/56 ,  C07D519/00 ,  A61K39/00

CPC分类号： A61K47/6803 ,  A61K31/337 ,  A61K31/404 ,  A61K31/537 ,  A61K31/5517 ,  A61K38/05 ,  A61K39/395 ,  A61K39/3955 ,  A61K45/06 ,  A61K47/6809 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61K2039/505 ,  C07C59/76 ,  C07C233/20 ,  C07C237/52 ,  C07D207/46 ,  C07D277/56 ,  C07D309/14 ,  C07D403/14 ,  C07D407/12 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  C07D498/14 ,  C07D519/00 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/32 ,  C07K2317/24 ,  G01N33/5014 ,  Y02A50/473

摘要： The present invention relates to novel acetylenedicarboxyl linkers used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

公开(公告)号：US20170342080A1

公开(公告)日：2017-11-30

申请号：US15680688

申请日：2017-08-18

申请人： SIGNAL PHARMACEUTICALS, LLC

发明人： Jan ELSNER ,  Roy L. HARRIS ,  Branden Gingsee LEE ,  Deborah MORTENSEN ,  Garrick K. PACKARD ,  Patrick PAPA ,  Jason PARNES ,  Sophie PERRIN-NINKOVIC ,  Jennifer RIGGS ,  John SAPIENZA ,  Graziella I. SHEVLIN ,  Lida TEHRANI ,  Jingjing ZHAO

IPC分类号： C07D487/04 ,  C07D487/14 ,  C07D487/10 ,  C07D471/14 ,  C07D471/04 ,  C07D498/14 ,  C07D241/20

CPC分类号： C07D487/04 ,  C07D241/20 ,  C07D471/04 ,  C07D471/14 ,  C07D487/10 ,  C07D487/14 ,  C07D498/14

摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

公开(公告)号：US20170275299A1

公开(公告)日：2017-09-28

申请号：US15514326

申请日：2015-09-23

申请人： NORTH CHINA PHARMACEUTICAL NEW DRUG R&D CO., LTD.

发明人： Shuhui CHEN ,  Zhaozhong DING ,  Gangli GONG ,  Xiaobing YAN ,  Wei HUANG ,  Feng GUO ,  Baoling DUAN ,  Renlong GAO ,  Pingfan ZHOU ,  Xinhua LU ,  Guimin DONG

IPC分类号： C07D498/14 ,  C07D265/32

CPC分类号： C07D498/14 ,  C07B2200/13 ,  C07D265/32 ,  C07D498/04

摘要： A preparation method for a high-purity benzoxazoleoxazine ketone compound, a crystal form thereof, and an intermediate compound for preparing a compound of formula (I), and a preparation method therefor.

公开(公告)号：US09771371B2

公开(公告)日：2017-09-26

申请号：US14874524

申请日：2015-10-05

申请人： SIGNAL PHARMACEUTICALS, LLC

发明人： Jan Elsner ,  Roy L. Harris ,  Branden Gingsee Lee ,  Deborah Mortensen ,  Garrick K. Packard ,  Patrick Papa ,  Jason Parnes ,  Sophie Perrin-Ninkovic ,  Jennifer Riggs ,  John Sapienza ,  Graziella I. Shevlin ,  Lida Tehrani ,  Jingjing Zhao

IPC分类号： C07D487/04 ,  C07D498/14 ,  C07D241/20 ,  C07D471/04 ,  C07D471/14 ,  C07D487/10 ,  C07D487/14

CPC分类号： C07D487/04 ,  C07D241/20 ,  C07D471/04 ,  C07D471/14 ,  C07D487/10 ,  C07D487/14 ,  C07D498/14

摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

公开(公告)号：US20170260203A1

公开(公告)日：2017-09-14

申请号：US15598655

申请日：2017-05-18

申请人： Shionogi & Co., Ltd. ,  ViiV Healthcare Company

发明人： Brian A. JOHNS ,  Takashi KAWASUJI ,  Teruhiko TAISHI ,  Yoshiyuki TAODA

IPC分类号： C07D498/14 ,  C07D471/14 ,  C07D498/04 ,  C07D471/22 ,  C07D498/20 ,  C07D498/22 ,  A61K31/4985 ,  A61K31/5365 ,  C07D471/04 ,  A61K45/06

CPC分类号： C07D498/14 ,  A61K9/0053 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/551 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D498/04 ,  C07D498/20 ,  C07D498/22

摘要： The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

公开(公告)号：US20170240564A1

公开(公告)日：2017-08-24

申请号：US15471133

申请日：2017-03-28

申请人： Shionogi & Co., Ltd.

发明人： Yukihito SUMINO ,  Moriyasu MASUI ,  Daisuke YAMADA ,  Fumiya IKARASHI ,  Kazuya OKAMOTO

IPC分类号： C07D498/14 ,  C07D213/80

CPC分类号： C07D498/14 ,  A61K31/5365 ,  C07B2200/13 ,  C07D213/80

摘要： A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].

公开(公告)号：US20170226127A1

公开(公告)日：2017-08-10

申请号：US15424216

申请日：2017-02-03

申请人： Denali Therapeutics Inc.

发明人： Anthony A. Estrada ,  Jianwen A. Feng ,  Brian Fox ,  Colin Philip Leslie ,  Joseph P. Lyssikatos ,  Alfonso Pozzan ,  Zachary K. Sweeney ,  Javier de Vicente Fidalgo

IPC分类号： C07D513/04 ,  C07D413/12 ,  C07D417/12 ,  C07D403/12 ,  C07D498/14 ,  C07D261/18 ,  C07D267/14 ,  C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D495/04 ,  C07D487/04

CPC分类号： C07D513/04 ,  C07D261/18 ,  C07D267/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14

摘要： The present disclosure relates generally to compounds and compositions, and their use as kinase inhibitors.

公开(公告)号：US09707246B2

公开(公告)日：2017-07-18

申请号：US14818539

申请日：2015-08-05

申请人： Shionogi & Co., Ltd. ,  ViiV Healthcare Company

发明人： Brian Alvin Johns ,  Jason Gordon Weatherhead ,  Toshikazu Hakogi ,  Yasunori Aoyama

IPC分类号： C07D498/14 ,  A61K31/675 ,  A61K31/4985 ,  A61K31/5377 ,  C07D211/86 ,  C07D309/40 ,  C07F9/6558

CPC分类号： A61K31/675 ,  A61K31/4985 ,  A61K31/5377 ,  C07D211/86 ,  C07D309/40 ,  C07D498/14 ,  C07F9/65583

摘要： The invention is directed to a method for treatment of viral infections, particularly HIV infection. The method involves administering compounds which are substituted (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-oxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamides of formula (I).

公开(公告)号：US20170145026A1

公开(公告)日：2017-05-25

申请号：US15358761

申请日：2016-11-22

申请人： eFFECTOR Therapeutics, Inc.

发明人： Justin T. ERNST ,  Siegfried H. REICH ,  Paul A. SPRENGELER ,  Chinh Viet TRAN ,  Garrick Kenneth PACKARD ,  Alan X. XIANG ,  Christian NILEWSKI ,  Theo MICHELS

IPC分类号： C07D491/048 ,  C07D491/20 ,  C07D519/00 ,  C07D498/14 ,  C07D491/16 ,  C07D491/153 ,  C07D333/78 ,  C07D307/93

CPC分类号： C07D491/048 ,  C07D307/93 ,  C07D333/78 ,  C07D491/153 ,  C07D491/16 ,  C07D491/20 ,  C07D498/14 ,  C07D519/00

摘要： The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.