公开(公告)号：US12017996B2

公开(公告)日：2024-06-25

申请号：US17740364

申请日：2022-05-10

申请人： JIANGSU MEDOLUTION LTD

发明人： Dawei Zhang

IPC分类号： C07D215/54 ,  C07D401/04

CPC分类号： C07D215/54 ,  C07D401/04

摘要： The present disclosure is directed to formulations of novel quinolines and their pharmaceutically acceptable salts, which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this disclosure have a general Formula I






wherein R10 to R14 and X are defined herein.

公开(公告)号：US11999698B2

公开(公告)日：2024-06-04

申请号：US17470980

申请日：2021-09-09

申请人： InflaRx GmbH

发明人： Yong Li ,  Renfeng Guo ,  Niels Christoph Riedemann

IPC分类号： C07D215/54 ,  C07D405/12

CPC分类号： C07D215/54 ,  C07D405/12

摘要： The present invention relates to fused piperidinyl bicyclic, meta-substituted piperidinyl and their related compounds that modulate activities of mammalian C5a receptor by directly binding to the C5a receptor. The invention also relates to pharmaceutical compositions containing such compounds and their use in the treatment of a disease or a disorder involving pathogenic activation of C5a receptors.

公开(公告)号：US20230303586A1

公开(公告)日：2023-09-28

申请号：US18178452

申请日：2023-03-03

申请人： Araxes Pharma LLC

发明人： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

IPC分类号： C07D495/04 ,  C07D239/94 ,  C07D401/12 ,  C07D217/22 ,  C07D215/46 ,  C07D215/54 ,  C07D239/84 ,  C07D487/04 ,  C07D239/95 ,  C07D403/04 ,  C07D241/44 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D495/04 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):





or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：US11713324B2

公开(公告)日：2023-08-01

申请号：US17126581

申请日：2020-12-18

申请人： Neurocrine Biosciences, Inc.

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Richard Lowe ,  Nicole Smith ,  Neil Ashweek ,  Yun-Fei Zhu

IPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D239/36 ,  C07D213/58

CPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:




wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

公开(公告)号：US20180237473A1

公开(公告)日：2018-08-23

申请号：US15509107

申请日：2015-09-08

申请人： LANDSTEINER GENMED, S.L.

发明人： Jesús LLENAS CALVO ,  Miriam ROYO EXPOSITO ,  Elena CARCELLER GONZÁLEZ ,  Unai ELEZCANO DONAIRE ,  Sergio RODRIGUEZ ESCRICH ,  Enrique VAZQUEZ TATAY

IPC分类号： C07K5/06 ,  A61P3/04 ,  A61P3/06

CPC分类号： C07K5/06 ,  A61K38/05 ,  A61P3/04 ,  A61P3/06 ,  C07C237/22 ,  C07C271/22 ,  C07C275/16 ,  C07D211/62 ,  C07D213/81 ,  C07D213/82 ,  C07D215/54 ,  C07D217/02 ,  C07D237/24 ,  C07D239/28 ,  C07D241/24 ,  C07D309/08 ,  C07D317/60 ,  C07K5/0202

摘要： The present invention relates to the use of dipeptidyl ketoamide compounds for preventing accumulation of triglycerides in adipose tissue or for reducing the amount of triglycerides in adipose tissue in a subject in need thereof and to novel dipeptidyl ketoamide compounds.

公开(公告)号：US20180237448A1

公开(公告)日：2018-08-23

申请号：US15548583

申请日：2016-02-03

申请人： COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

发明人： Ekambaram BALARAMAN ,  Siba Prasad MIDYA ,  Garima JAISWAL

IPC分类号： C07D491/056

CPC分类号： C07D491/056 ,  C07D215/04 ,  C07D215/18 ,  C07D215/20 ,  C07D215/54 ,  C07D491/04

摘要： The patent discloses novel quinoline derivatives of formula (I), (Formula should be inserted here) and process for preparing the same. The compounds of formula (I) can be further used for the synthesis of Inhibitors like Kinase Tyrosine Inhibitors.

公开(公告)号：US09809599B2

公开(公告)日：2017-11-07

申请号：US14938005

申请日：2015-11-11

申请人： Hoffmann-La Roche Inc.

发明人： Simona M. Ceccarelli ,  Aurelia Conte ,  Holger Kuehne ,  Bernd Kuhn ,  Werner Neidhart ,  Ulrike Obst Sander ,  Markus Rudolph

IPC分类号： C07D215/00 ,  C07D215/02 ,  C07D215/54 ,  C07D401/04 ,  C07D413/04 ,  C07D491/048 ,  C07D401/14 ,  C07D215/227 ,  C07D413/14

CPC分类号： C07D491/048 ,  C07D215/00 ,  C07D215/02 ,  C07D215/227 ,  C07D215/54 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

公开(公告)号：US09776970B2

公开(公告)日：2017-10-03

申请号：US15120226

申请日：2015-02-20

申请人： Apotex Inc.

发明人： Padiyath Mohammed Akbarali ,  Venkata Ramana Kintali ,  Heggadde Nanjunda Bhatta Shreenivasa Murthy ,  Girisha Meenkere ,  Somanath Bhupal Venkata ,  Raja Ramesh Manda ,  Vishal Amrutlal Sodha ,  Abbulu Kante

IPC分类号： C07D401/12 ,  A61K31/496 ,  C07D215/54 ,  A61K31/4706 ,  A61K9/14

CPC分类号： C07D215/54 ,  A61K9/146 ,  A61K31/4706

摘要： The present subject matter relates to solvates and the amorphous form of bosutinib; the solvates namely being a propylene glycol solvate and an acetonitrile solvate. Also provided are processes for preparing the propylene glycol solvate, the amorphous form and the crystalline acetonitrile solvate of bosutinib; as well as compositions comprising said forms. Bosutinib is a 3-quinolinecarbonitrile kinase inhibitor and is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CMS) with resistance or intolerance to prior therapy.

公开(公告)号：US20170204089A1

公开(公告)日：2017-07-20

申请号：US15328281

申请日：2015-08-03

申请人： DREXEL UNIVERSITY

发明人： Sandhya KORTAGERE ,  Carol M. ARTLETT

IPC分类号： C07D417/14 ,  A61K31/427 ,  C07C237/52 ,  C07D263/56 ,  C07D401/04 ,  A61K31/4439 ,  A61K31/36 ,  A61K45/06 ,  A61K31/167

CPC分类号： C07D417/14 ,  A61K31/167 ,  A61K31/36 ,  A61K31/4162 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/519 ,  A61K38/00 ,  A61K45/06 ,  C07C237/52 ,  C07C317/44 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/90 ,  C07D215/54 ,  C07D249/08 ,  C07D263/56 ,  C07D309/32 ,  C07D317/58 ,  C07D317/66 ,  C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D493/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.

公开(公告)号：US20170020858A1

公开(公告)日：2017-01-26

申请号：US15052385

申请日：2016-02-24

申请人： HYDRA BIOSCIENCES, INC.

发明人： Jayhong A. Chong ,  Christopher Fanger ,  Glenn R. Larsen ,  William C. Lumma, JR. ,  Magdalene M. Moran ,  Amy Ripka ,  Dennis John Underwood ,  Manfred Weigele ,  Xiaoguang Zhen

IPC分类号： A61K31/4709 ,  A61K31/55 ,  A61K31/47 ,  A61K31/427 ,  A61K31/538 ,  A61K9/00 ,  A61K31/498

CPC分类号： A61K31/4709 ,  A61K9/0014 ,  A61K9/0053 ,  A61K31/427 ,  A61K31/47 ,  A61K31/498 ,  A61K31/506 ,  A61K31/538 ,  A61K31/55 ,  C07D215/54 ,  C07D409/04 ,  C07D495/04

摘要： The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.

摘要翻译： 本申请涉及用于治疗与TRPV3相关的疼痛和其它病症的化合物和方法。