公开(公告)号：US09938292B2

公开(公告)日：2018-04-10

申请号：US15128064

申请日：2015-03-16

Applicant: GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD

Inventor： Hao Wu ,  Chaofeng Long ,  Jun Lin ,  Xiaoxin Chen ,  Yunhui Li ,  Zhuowei Liu ,  Changqing Wei ,  Lijuan Chen ,  Shuhui Chen

IPC: C07D413/10 ,  C07D413/14 ,  C07D403/10 ,  C07D403/14 ,  C07D498/04 ,  C07D401/10 ,  C07D491/08 ,  C07D487/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D487/10 ,  C07D471/10

CPC classification number: C07D498/04 ,  C07D215/38 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/08

Abstract: Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.

公开(公告)号：US09938243B2

公开(公告)日：2018-04-10

申请号：US15698020

申请日：2017-09-07

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Peter Kumpalume ,  Oliver Schon ,  Christine Patricia Donahue ,  Ghotas Evindar ,  David I. Israel ,  David Paolella ,  Letian Kuai ,  Ninad V. Prabhu

IPC: C07D235/18 ,  A61K31/454 ,  C07D411/14 ,  A61K31/4545 ,  A61K31/4184 ,  C07D401/06 ,  C07D235/24 ,  C07D401/10 ,  C07D417/14

CPC classification number: C07D235/18 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/4545 ,  C07D235/24 ,  C07D401/06 ,  C07D401/10 ,  C07D411/14 ,  C07D417/14

Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.

公开(公告)号：US09931340B2

公开(公告)日：2018-04-03

申请号：US15014336

申请日：2016-02-03

Applicant: TAKEDA PHARMACUETICAL COMPANY LTD.

Inventor： William Farnaby ,  Charlotte Fieldhouse ,  Katherine Hazel ,  Catrina Kerr ,  Natasha Kinsella ,  David Livermore ,  Kevin Merchant ,  David Miller

IPC: A61K31/50 ,  A61K31/501 ,  C07D237/16 ,  C07D401/06

CPC classification number: A61K31/50 ,  A61K31/501 ,  A61K45/06 ,  C07D237/16 ,  C07D237/18 ,  C07D237/22 ,  C07D401/06 ,  C07D401/10 ,  C07D405/06 ,  C07D407/10 ,  C07F7/0812

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy:

公开(公告)号：US09908887B2

公开(公告)日：2018-03-06

申请号：US14654303

申请日：2013-12-20

Applicant: Epizyme, Inc.

Inventor： Kenneth W. Duncan ,  Richard Chesworth ,  Michael John Munchhof ,  Lei Jin

IPC: C07D487/04 ,  A61K31/00 ,  C07D401/14 ,  C07D405/14 ,  C07D217/02 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D217/04 ,  C07D401/10 ,  C07D409/12 ,  C07D413/14

CPC classification number: C07D487/04 ,  C07D217/02 ,  C07D217/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：US20180055054A1

公开(公告)日：2018-03-01

申请号：US15559614

申请日：2016-01-08

Applicant: QINGDAO KINGAGROOT CHEMICAL COMPOUNDS CO., LTD.

Inventor： Lei LIAN ,  Yurong ZHENG ,  Bin HE ,  Xuegang PENG ,  Tao JIN ,  Qi CUI

IPC: A01N43/56 ,  C07D231/20 ,  C07D403/10 ,  C07D403/14 ,  A01N47/06 ,  C07D401/10 ,  C07D401/14 ,  A01N43/60 ,  C07D413/10 ,  A01N43/84 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

CPC classification number: A01N43/56 ,  A01N43/60 ,  A01N43/84 ,  A01N47/06 ,  C07D231/20 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

Abstract: The present invention belongs to the field of pesticides, particularly relates to a pyrazolone compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. The pyrazolone compound is as described in formula I: In the formula, R1R2N represents substituted or unsubstituted 3-8 membered nitrogen-containing heterocyclic group containing 1-3 heteroatoms; or R1 and R2 each represent hydrogen or C1-8 alkyl; R3 represents hydrogen, C1-4 alkyl, alkenyl, alkynyl, unsubstituted C3-6 cycloalkyl or C3-6 cycloalkyl substituted by C1-4 alkyl; R4 represents methyl, ethyl, n-propyl, isopropyl or cyclopropyl; X represents hydrogen, —S(O)nR6, —R7 or substituted or unsubstituted 3-8 membered heterocyclic group containing 1-4 heteroatoms, wherein, n represents 1, 2 or 3, R6 represents substituted or unsubstituted alkyl or aryl, and R7 represents substituted or unsubstituted alkyl, aryl, alkyl acyl or aroyl. The active substance of the invention exhibits good herbicidal effect, and is convenient to use, low in cost and has great commercial value.

公开(公告)号：US09895352B2

公开(公告)日：2018-02-20

申请号：US15357933

申请日：2016-11-21

Applicant: Oncternal Therapeutics, Inc.

Inventor： Jean-Michel Vernier

IPC: A61K31/404 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/4155 ,  C07D209/38 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10 ,  C07D209/34

CPC classification number: A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/5377 ,  C07D209/34 ,  C07D209/38 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10

Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

公开(公告)号：US20180044335A1

公开(公告)日：2018-02-15

申请号：US15554440

申请日：2016-03-04

Applicant: Boehringer Ingelheim International GmbH

Inventor： Laetitia MARTIN ,  Steffen STEURER ,  Xiao-Ling COCKCROFT

IPC: C07D471/04 ,  C07D519/00 ,  C07D237/32 ,  C07D401/06 ,  C07D401/10 ,  C07D217/24

CPC classification number: C07D471/04 ,  C07D213/64 ,  C07D217/24 ,  C07D237/28 ,  C07D237/32 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D471/08 ,  C07D487/08 ,  C07D519/00

Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.

公开(公告)号：US09884878B2

公开(公告)日：2018-02-06

申请号：US14728128

申请日：2015-06-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Genesis M. Bacani ,  Wendy Eccles ,  Anne E. Fitzgerald ,  Steven D. Goldberg ,  Michael D. Hack ,  Natalie A. Hawryluk ,  William M. Jones ,  John M. Keith ,  Paul Krawczuk ,  Alec D. Lebsack ,  Alice Lee-Dutra ,  Jing Liu ,  Kelly J. McClure ,  Steven P. Meduna ,  Daniel J. Pippel ,  Mark D. Rosen ,  Zachary S. Sales

IPC: C07D241/20 ,  A61K31/4965 ,  C07F7/08 ,  C07D241/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D487/04 ,  C07D405/14 ,  C07D413/14 ,  C07D213/73 ,  C07D401/04 ,  C07D235/10 ,  C07D401/10 ,  C07D403/10 ,  C07D237/20 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/08 ,  C07D263/48 ,  C07D491/10 ,  C07D498/04 ,  C07D209/08 ,  C07D277/62 ,  C07D285/12 ,  C07F5/02 ,  C07D403/14 ,  C07D405/12 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10

CPC classification number: C07F7/0812 ,  C07D209/08 ,  C07D213/73 ,  C07D235/10 ,  C07D237/20 ,  C07D241/20 ,  C07D241/26 ,  C07D263/48 ,  C07D277/62 ,  C07D285/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04 ,  C07F5/025 ,  C07F7/08

Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

公开(公告)号：US20180033974A1

公开(公告)日：2018-02-01

申请号：US15437504

申请日：2017-02-21

Applicant: SAMSUNG DISPLAY CO., LTD.

Inventor： Jungsub LEE

IPC: H01L51/00 ,  C07D495/06 ,  C07D401/10 ,  C07D491/06 ,  C09K11/06 ,  C09K11/02

CPC classification number: H01L51/0067 ,  C07D401/10 ,  C07D491/06 ,  C07D495/06 ,  C09K11/025 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1029 ,  C09K2211/185 ,  H01L51/0052 ,  H01L51/0071 ,  H01L51/0072 ,  H01L51/0085 ,  H01L51/5012 ,  H01L51/5016 ,  H01L51/5072 ,  H01L51/5092

Abstract: A polycyclic compound and an organic light-emitting device, the compound being represented by Formula 1:

公开(公告)号：US09873673B2

公开(公告)日：2018-01-23

申请号：US15191943

申请日：2016-06-24

Applicant: Pfizer Inc.

Inventor： Philip A. Carpino ,  Edward L. Conn ,  Robert L. Dow ,  Matthew S. Dowling ,  David Hepworth ,  Daniel Wei-Shung Kung ,  Suvi Orr ,  Benjamin N. Rocke ,  Roger B. Ruggeri ,  Matthew F. Sammons ,  Joseph S. Warmus ,  Yan Zhang

IPC: C07D239/56 ,  A61K31/513 ,  A61K31/352 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/10 ,  C07D487/04 ,  C07D417/04 ,  C07D471/04 ,  A61K31/37 ,  C07D405/06

CPC classification number: C07D239/56 ,  A61K31/352 ,  A61K31/37 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.