公开(公告)号：US20240261416A1

公开(公告)日：2024-08-08

申请号：US18426920

申请日：2024-01-30

申请人： Wisconsin Alumni Research Foundation

发明人： Weiping Tang ,  Haibo Xie ,  Yunxiang Wu ,  Junzhuo Liao ,  Chunrong Li ,  Ira Tandon ,  Hua Tang

IPC分类号： A61K47/55 ,  C07D239/22 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

CPC分类号： A61K47/55 ,  C07D239/22 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

摘要： Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.

公开(公告)号：US20230234950A1

公开(公告)日：2023-07-27

申请号：US18059232

申请日：2022-11-28

申请人： Kymera Therapeutics, Inc.

发明人： Nello MAINOLFI ,  Nan JI ,  Arthur F. KLUGE

IPC分类号： C07D417/04 ,  C07D211/88 ,  C07D239/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D417/04 ,  C07D211/88 ,  C07D239/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

公开(公告)号：US20230227414A1

公开(公告)日：2023-07-20

申请号：US18187211

申请日：2023-03-21

申请人： GlaxoSmithKline LLC

发明人： Kevin J. DUFFY ,  Duke M. FITCH ,  Jian JIN ,  Ronggang LIU ,  Antony N. SHAW ,  Kenneth WIGGALL

IPC分类号： C07D239/60 ,  A61K31/515 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

CPC分类号： C07D239/60 ,  A61K31/515 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

摘要： The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)




which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

公开(公告)号：US11643397B2

公开(公告)日：2023-05-09

申请号：US17383554

申请日：2021-07-23

申请人： GlaxoSmithKline LLC

发明人： Kevin J. Duffy ,  Duke M. Fitch ,  Jian Jin ,  Ronggang Liu ,  Antony N. Shaw ,  Kenneth Wiggall

IPC分类号： C07D239/54 ,  C07D239/60 ,  A61K31/515 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10 ,  C07D239/22

CPC分类号： C07D239/60 ,  A61K31/515 ,  C07D239/22 ,  C07D239/54 ,  C07D239/62 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D417/10

摘要： The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)




which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

公开(公告)号：US20180201604A1

公开(公告)日：2018-07-19

申请号：US15568449

申请日：2016-04-20

申请人： ALLGENESIS BIOTHERAPEUTICS, INC.

发明人： Madhu CHERUKURY ,  Hsiao-Wen LIN ,  Shu Chieh YU ,  Riping PHANG ,  Yesudoss Christu RAJAN ,  Diane Dan-Shya TANG-LIU ,  Andrew D. WHITE ,  Thomas MALONE ,  Richard BERESIS

IPC分类号： C07D403/04 ,  C07D409/04 ,  C07D409/14 ,  C07D405/04 ,  C07D405/14 ,  C07D401/12 ,  C07D401/04 ,  C07D401/06 ,  C07D417/04 ,  C07D417/08 ,  C07D417/14 ,  C07D413/04 ,  C07D413/08 ,  C07D403/10 ,  C07D403/06 ,  C07D471/04 ,  C07D471/14 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D239/22 ,  C07D513/10 ,  A61P25/28

CPC分类号： C07D403/04 ,  A61P25/28 ,  C07D239/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/08 ,  C07D417/04 ,  C07D417/08 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/10

摘要： The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).

公开(公告)号：US20180072685A1

公开(公告)日：2018-03-15

申请号：US15559385

申请日：2016-03-15

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Heiko Schirmer ,  Philipp Rubenbauer ,  Birgit Keil ,  Britta Olenik

IPC分类号： C07D239/22 ,  C07C315/00

CPC分类号： C07D239/22 ,  C07B2200/13 ,  C07C315/00

摘要： The present invention concerns a new and improved method for preparation of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

公开(公告)号：US09815838B2

公开(公告)日：2017-11-14

申请号：US13966546

申请日：2013-08-14

申请人： HYDRA BIOSCIENCES, INC.

发明人： Magdalene M. Moran ,  Christopher Fanger ,  Jayhong A. Chong ,  Colleen Mcnamara ,  Xiaoguang Zhen ,  Josh Mandel-Brehm

IPC分类号： A61K31/522 ,  A61K31/513 ,  C07D473/08 ,  A61K31/505 ,  A61K31/555 ,  C07K14/705 ,  C07D239/22

CPC分类号： C07D473/08 ,  A61K31/505 ,  A61K31/513 ,  A61K31/522 ,  A61K31/555 ,  C07D239/22 ,  C07K14/705

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

公开(公告)号：US09796742B2

公开(公告)日：2017-10-24

申请号：US15228945

申请日：2016-08-04

申请人： Respivert Limited ,  Topivert Pharma Limited

发明人： Matthew Colin Thor Fyfe ,  Michael Knaggs ,  Premji Meghani ,  Stephen Malcolm Thom

IPC分类号： C07F9/6558 ,  C07F9/6568 ,  A61K31/675 ,  A61K31/695 ,  C07D213/68 ,  C07D231/14 ,  C07D239/22 ,  C07F7/08 ,  C07F9/28 ,  C07F9/30 ,  C07F9/6512 ,  C07F9/6503

CPC分类号： C07F9/65583 ,  A61K31/675 ,  A61K31/695 ,  C07D213/68 ,  C07D231/14 ,  C07D239/22 ,  C07F7/0803 ,  C07F9/28 ,  C07F9/304 ,  C07F9/65031 ,  C07F9/6512 ,  C07F9/65685

摘要： There are provided compounds of formula I, wherein R1 to R5, X1, X2, Ar, L, A, A1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

公开(公告)号：US20170273978A1

公开(公告)日：2017-09-28

申请号：US15504134

申请日：2015-08-27

申请人： Codexis, Inc.

发明人： Gjalt W. Huisman ,  Jed Lee Hubbs ,  Xiyun Zhang ,  Robert Osborne

IPC分类号： A61K31/506 ,  C07C59/185 ,  C07D233/54 ,  C07D401/14 ,  C07D239/22

CPC分类号： A61K31/506 ,  C07C59/185 ,  C07D233/54 ,  C07D239/22 ,  C07D401/14

摘要： The present invention provides kinase inhibitor analogs with improved properties, such as improved efficacy, pharmacokinetics, safety, and specificity. In some embodiments, the present invention provides nilotinib analogs that provide therapeutic benefits.

公开(公告)号：US20170267646A1

公开(公告)日：2017-09-21

申请号：US15519886

申请日：2015-11-12

申请人： JIANGSU TASLY DIYI PHARMACEUTICAL CO., LTD.

发明人： Wenzheng Liu ,  Guocheng Wang ,  Qingwei Hou ,  Qiaoping Cui ,  Zhanyuan Zhu ,  Jinping Liu ,  Mingbo Yang ,  Hongguang Meng

IPC分类号： C07D239/08 ,  C07D217/00 ,  A61K31/5395 ,  C07D401/04 ,  C07D239/22

CPC分类号： C07D239/08 ,  A61K31/5395 ,  C07D217/00 ,  C07D239/22 ,  C07D401/04

摘要： Provided is a preparation method for revaprazan hydrochloride, the method comprising: (1) the preparation of 4-hydroxyl-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (2) the preparation of 4-chloro-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (3) the preparation of revaprazan hydrochloride. The method has advantages such as simple operations, high product purity, good yield and suitability for industrial production.