公开(公告)号：US20230093404A1

公开(公告)日：2023-03-23

申请号：US17794661

申请日：2021-01-22

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Qingjie Liu ,  T.G. Murali Dhar

IPC分类号： C07D221/16 ,  C07D409/12

摘要： There are described RORγ modulators of the formula (I), or stereoisomers, pharmaceutically acceptable salts thereof, wherein all substituents are defined herein.

公开(公告)号：US11352370B2

公开(公告)日：2022-06-07

申请号：US16927517

申请日：2020-07-13

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

发明人： Said M. Sebti ,  Yangmei Li ,  Richard A. Houghten

IPC分类号： C07D221/16 ,  C07D401/04 ,  C07D401/14 ,  A61K31/429 ,  A61P35/00 ,  C07D513/04

摘要： Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.

公开(公告)号：US11236074B2

公开(公告)日：2022-02-01

申请号：US15562725

申请日：2016-04-06

申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

发明人： Todd Ridky ,  Christopher Natale

IPC分类号： A61K8/49 ,  C07D405/04 ,  C07D491/048 ,  A61P17/06 ,  A61P17/18 ,  A61P17/14 ,  A61P17/00 ,  A61P17/16 ,  C07D221/16 ,  A61Q19/02 ,  A61Q17/04

摘要： The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR).

公开(公告)号：US10421764B2

公开(公告)日：2019-09-24

申请号：US15568931

申请日：2016-04-25

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

发明人： Said M. Sebti ,  Yangmei Li ,  Richard A. Houghten

IPC分类号： C07D221/16 ,  C07D401/04 ,  C07D401/14 ,  C07D513/04 ,  A61K31/429 ,  A61P35/00

摘要： Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.

公开(公告)号：US20170217984A1

公开(公告)日：2017-08-03

申请号：US15328112

申请日：2015-07-23

申请人： Northeastern University ,  University of Florida Research Foundation, Inc.

发明人： Ganeshsingh A. THAKUR ,  Abhijit R. KULKARNI ,  Roger Lee PAPKE

IPC分类号： C07D495/04 ,  C07D401/04 ,  C07D491/048 ,  C07D405/04 ,  C07D409/10 ,  C07D401/12 ,  C07D401/10 ,  C07D417/04 ,  C07D409/14 ,  C07D221/16 ,  C07D409/04

CPC分类号： C07D495/04 ,  C07D221/16 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D417/04 ,  C07D491/048

摘要： Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.

公开(公告)号：US09718845B2

公开(公告)日：2017-08-01

申请号：US15225261

申请日：2016-08-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： David K. Leahy ,  Yu Fan ,  Collin Chan ,  Lopa V. Desai ,  Sunil S. Patel ,  Masano Sugiyama

IPC分类号： C07D221/06 ,  C07D221/16 ,  C07F7/18 ,  C07D221/04 ,  C07D471/04

CPC分类号： C07F7/1804 ,  C07D221/04 ,  C07D471/04

摘要： The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.

公开(公告)号：US09663470B2

公开(公告)日：2017-05-30

申请号：US15079544

申请日：2016-03-24

申请人： Vitae Pharmaceuticals, Inc./Boehringer-Ingelheim

发明人： Matthias Eckhardt ,  Frank Himmelsbach ,  Linghang Zhuang ,  Stefan Peters ,  Herbert Nar

IPC分类号： C07D221/06 ,  C07D221/10 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04 ,  C07D221/16 ,  C07D401/04 ,  C07D405/04

CPC分类号： C07D221/10 ,  C07D221/06 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

公开(公告)号：US09453022B2

公开(公告)日：2016-09-27

申请号：US14378089

申请日：2013-02-13

申请人： CHILDREN'S HOSPITAL MEDICAL CENTER

发明人： Yi Zheng ,  Prakash Jagtap ,  Emily E. Bosco ,  Jaroslaw Meller ,  Marie-Dominique Filippi

IPC分类号： C07D491/052 ,  C07D498/04 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D409/04 ,  C07D401/04 ,  A61K31/473 ,  A61K31/4738 ,  A61K31/5365 ,  A61K31/5377 ,  C07D221/16 ,  C07D491/04 ,  C07D215/06 ,  C07D491/048

CPC分类号： C07D498/04 ,  A61K31/473 ,  A61K31/4738 ,  A61K31/5365 ,  A61K31/5377 ,  C07D215/06 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D221/12 ,  C07D221/16 ,  C07D401/04 ,  C07D409/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052

摘要： Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods recited thereto.

摘要翻译： 本文提供了p67phox蛋白的抑制剂，以及其中所述的药物组合物和方法。

公开(公告)号：US09334284B2

公开(公告)日：2016-05-10

申请号：US14378089

申请日：2013-02-13

申请人： CHILDREN'S HOSPITAL MEDICAL CENTER

发明人： Yi Zheng ,  Prakash Jagtap ,  Emily E. Bosco ,  Jaroslaw Meller ,  Marie-Dominique Filippi

IPC分类号： C07D491/052 ,  C07D498/04 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D409/04 ,  C07D401/04 ,  A61K31/473 ,  A61K31/4738 ,  A61K31/5365 ,  A61K31/5377 ,  C07D221/16 ,  C07D491/04 ,  C07D215/06 ,  C07D491/048

摘要： Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods recited thereto.

公开(公告)号：US20160031899A1

公开(公告)日：2016-02-04

申请号：US14772731

申请日：2014-02-27

申请人： AQUINOX PHARMACEUTICALS (Canada) INC.

发明人： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC分类号： C07D493/10 ,  C07D211/58 ,  C07C255/30 ,  C07D213/75 ,  C07C275/22 ,  C07C335/10 ,  C07D231/54 ,  C07D215/227 ,  C07D221/16 ,  C07C215/38 ,  C07D307/52 ,  C07D333/20 ,  C07D213/38 ,  C07D277/28 ,  C07D231/56 ,  C07D261/20 ,  C07D277/64 ,  C07C35/21 ,  C07C35/23 ,  C07D307/42 ,  C07C233/23 ,  C07D213/82

CPC分类号： C07D493/10 ,  A61K31/416 ,  C07C35/21 ,  C07C35/23 ,  C07C215/26 ,  C07C215/38 ,  C07C233/23 ,  C07C255/30 ,  C07C275/22 ,  C07C335/10 ,  C07C2601/14 ,  C07C2602/24 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/82 ,  C07D215/227 ,  C07D221/16 ,  C07D221/18 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D307/42 ,  C07D307/52 ,  C07D333/16 ,  C07D333/20

摘要： Compounds of formula (II): wherein A, R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

摘要翻译： 本文描述了其中A，R 1，R 2，R 5和R 13或其立体异构体，对映异构体或互变异构体或其混合物或其药学上可接受的盐或溶剂化物的式（II）化合物，以及其它 化合物。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，病症或病症。 还公开了包含本发明化合物的组合物，以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。