公开(公告)号：US20230027752A1

公开(公告)日：2023-01-26

申请号：US17755780

申请日：2020-11-02

申请人： Fudan University

发明人： Wei Fu

IPC分类号： C07D211/96 ,  A61P25/04 ,  C07C317/28 ,  C07C311/20 ,  C07D409/12 ,  C07D401/06

摘要： The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.

公开(公告)号：US20220363639A1

公开(公告)日：2022-11-17

申请号：US17263590

申请日：2019-07-31

申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA ,  VAL-CHUM, LIMITED PARTNERSHIP

发明人： Melissa Carey GRENIER ,  Amos B. SMITH, III ,  Andres FINZI ,  Shilei DING ,  Jean-Philippe CHAPLEAU

IPC分类号： C07D211/96 ,  C07D207/48 ,  C07D403/12 ,  C07D401/12 ,  C07D265/30 ,  C07D413/12 ,  C07D241/04 ,  C07D211/60 ,  C07D309/08 ,  C07D211/56 ,  C07D215/54 ,  A61P31/18

摘要： Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R1-R7, X, X′, Y, Y′, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

公开(公告)号：US11485725B2

公开(公告)日：2022-11-01

申请号：US16766538

申请日：2018-11-14

申请人： Auransa Inc.

发明人： Andrew Asher Protter ,  Michael John Green ,  Hak Jin Chang ,  Son Minh Pham ,  Sarvajit Chakravarty ,  Gregory R. Luedtke ,  Pek Yee Lum

IPC分类号： C07D401/06 ,  C07D401/14 ,  C07D211/86 ,  C07D211/96 ,  C07D413/06 ,  C07D491/056 ,  C07D405/06 ,  C07D405/14 ,  C07D401/12 ,  C07D401/04 ,  C07D403/06 ,  C07D223/10

摘要： The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer.

公开(公告)号：US20220306630A1

公开(公告)日：2022-09-29

申请号：US17632909

申请日：2020-08-05

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Lalgudi S. Harikrishnan ,  Peter Kinam Park ,  Zheming Ruan ,  Donna D. Wei ,  Daniel O'Malley ,  Honghe Wan ,  Ashok Vinayak Purandare ,  Brian E. Fink

IPC分类号： C07D471/10 ,  C07C317/18 ,  C07D213/73 ,  C07D213/71 ,  C07C255/60 ,  C07D213/82 ,  C07D231/12 ,  C07D231/18 ,  C07D263/24 ,  C07D213/56 ,  C07D401/12 ,  C07C311/16 ,  C07D213/69 ,  C07D233/61 ,  C07D211/34 ,  C07D235/18 ,  C07D213/58 ,  C07D211/96 ,  C07D295/26

摘要： The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20220265595A1

公开(公告)日：2022-08-25

申请号：US17606884

申请日：2020-04-30

申请人： Sitryx Therapeutics Limited

发明人： Michael Liam COOKE ,  David COUSIN ,  Matthew Colin Thor FYFE ,  Barry John TEOBALD ,  Stephen Malcolm THOM ,  Thomas Michael WAUGH

IPC分类号： A61K31/225 ,  C07C255/14 ,  C07C317/18 ,  C07C69/593 ,  C07D305/08 ,  C07D207/27 ,  C07C233/05 ,  C07D207/273 ,  C07C311/03 ,  C07C219/08 ,  C07D307/20 ,  C07D309/12 ,  C07D211/96 ,  C07D295/08 ,  C07D331/04 ,  C07D205/04 ,  C07D295/088 ,  C07D207/277 ,  C07D257/04 ,  C07D519/00 ,  C07D451/10 ,  A61K31/275 ,  A61K31/337 ,  A61K31/4015 ,  A61K31/341 ,  A61K31/351 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/38 ,  A61K31/397 ,  A61K31/495 ,  A61K31/54 ,  A61K31/41 ,  A61K31/46

摘要： The invention relates to compounds of formula (IW-1) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response: wherein RA, RB, RC and RD are as defined herein.

公开(公告)号：US20220177422A1

公开(公告)日：2022-06-09

申请号：US17594086

申请日：2020-04-02

申请人： The University of Chicago ,  The United States of America,as Represented by the Secretary, Department of Health and Human Servic ,  President and Fellows of Harvard College ,  IIT Research Institute ,  Beth Israel Deaconess Medical Center, Inc. ,  REGENTS OF THE UNIVERSITY OF MINNESOTA ,  THE TRUSTEES OF PURDUE UNIVERSITY

发明人： Julian SOLWAY ,  Nickolai DULIN ,  Diane Luci ,  David MALONEY ,  Chan Young PARK ,  Jeffrey FREDBERG ,  David MCCORMICK ,  Ramaswamy KRISHNAN

IPC分类号： C07C311/46 ,  C07D207/48 ,  C07D211/96 ,  C07D277/52 ,  C07D295/26 ,  A61P11/00

摘要： Disclosed herein is a class of molecules termed remodilins that are effective in treating asthma, pulmonary fibrosis, and associated disorders. The molecules ameliorate asthma and pulmonary fibrosis symptoms by various mechanisms, including inhibiting airway smooth muscle contractile protein accumulation, reducing airway constrictor hyperresponsiveness, inhibiting bronchial fibroblast transformation into myofibroblasts, and/or treating or preventing airway or pulmonary fibrosis.

公开(公告)号：US20220169605A1

公开(公告)日：2022-06-02

申请号：US17422500

申请日：2020-01-13

申请人： Cadila Healthcare Ltd.

发明人： Rajiv Sharma ,  Sameer Agarwal

IPC分类号： C07D207/48 ,  C07D207/08 ,  C07D211/24 ,  C07D211/96 ,  C07D403/06 ,  C07D405/06 ,  C07D401/04 ,  C07D405/04 ,  C07D417/06 ,  C07D409/12 ,  C07D409/06 ,  C07D417/04 ,  C07D205/04 ,  C07D403/04 ,  C07D409/04

摘要： The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions in which interleukin 1β activity is implicated.

公开(公告)号：US20220153698A1

公开(公告)日：2022-05-19

申请号：US17434139

申请日：2020-02-20

申请人： ADEKA CORPORATION ,  TOKYO INSTITUTE OF TECHNOLOGY

发明人： Hideyuki OTSUKA ,  Daisuke AOKI ,  Daisuke SAWAMOTO ,  Atsushi KOBAYASHI ,  Satoyuki CHIKAOKA

IPC分类号： C07D211/96 ,  C08K5/43 ,  C09D7/63 ,  C09J11/06 ,  H01M4/62

摘要： Provided is a compound, which is represented by the following general formula (1): where X1 and X2 each independently represent an acrylic group or a methacrylic group, R1 to R8 each independently represent a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, and “n” represents an integer of from 1 to 10.

公开(公告)号：US20210338658A1

公开(公告)日：2021-11-04

申请号：US17234272

申请日：2021-04-19

申请人： The Johns Hopkins University

发明人： David Sullivan ,  Nick Kaludov ,  Martin Martinov

IPC分类号： A61K31/4709 ,  A61K31/5377 ,  C07D498/04 ,  C07D211/96 ,  C07D213/80 ,  C07D249/12 ,  A61K31/706 ,  A61K31/635 ,  A61K31/4706 ,  A61K31/65 ,  A61K31/505 ,  A61K31/4453 ,  A61K31/4196 ,  A61K31/122 ,  A61P31/00 ,  A61P33/06 ,  A61K45/06

摘要： A novel quantum-based computational process for drug discovery and design was used to identify potential novel liver-stage anti-malarial therapeutic molecules. The approach combined the latest big-data advances in high-throughput bioassay development with fundamental scientific knowledge to generate new pharmaceutical leads. Several molecules with no previous association with anti-parasitical activity were identified. These molecules and there use in prevention and/or treatment of Plasmodium infections are provided.

公开(公告)号：US20210317114A1

公开(公告)日：2021-10-14

申请号：US17206542

申请日：2021-03-19

申请人： TRUSTEES OF BOSTON UNIVERSITY ,  MASSACHUSETTS INSTITUTE OF TECHNOLOGY

发明人： Arturo VEGAS ,  Sean QUINNELL ,  Daniel SHEEHY ,  Kelly TAN ,  Luke CEO ,  Stephen Thomas NESTOR ,  Angela Nicole KOEHLER ,  Becky LEIFER ,  Shelby DOYLE

IPC分类号： C07D417/14 ,  C07D213/85 ,  C07D401/10 ,  C07D401/04 ,  C07D409/04 ,  C07D405/04 ,  C07D401/14 ,  C07D471/04 ,  C07D403/12 ,  C07D207/09 ,  C07D495/04 ,  C07D211/96 ,  C07D417/06 ,  C07D403/06 ,  A61K45/06 ,  C07K16/28

摘要： The technology described herein is directed to IL-4 and/or IL-13 inhibitors and uses thereof.