公开(公告)号：US11919838B2

公开(公告)日：2024-03-05

申请号：US17305537

申请日：2021-07-09

申请人： REATA PHARMACEUTICALS HOLDINGS, LLC

发明人： Eric Anderson ,  Xin Jiang ,  Melean Visnick

IPC分类号： C07C255/47 ,  C07C271/24 ,  C07C275/26 ,  C07C275/34 ,  C07C311/07 ,  C07C311/09 ,  C07C311/10 ,  C07D209/56 ,  C07D211/44 ,  C07D231/12 ,  C07D261/08 ,  C07D261/20 ,  C07D295/195 ,  C07D295/215 ,  C07D307/20 ,  C07D333/34 ,  C07D487/08 ,  C07J63/00

CPC分类号： C07C255/47 ,  C07C271/24 ,  C07C275/26 ,  C07C275/34 ,  C07C311/07 ,  C07C311/09 ,  C07C311/10 ,  C07D209/56 ,  C07D211/44 ,  C07D231/12 ,  C07D261/08 ,  C07D261/20 ,  C07D295/195 ,  C07D295/215 ,  C07D307/20 ,  C07D333/34 ,  C07D487/08 ,  C07J63/008 ,  C07C2603/52

摘要： This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:




wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

公开(公告)号：US11708326B2

公开(公告)日：2023-07-25

申请号：US17106309

申请日：2020-11-30

申请人： CHEMOCENTRYX, INC.

发明人： Christopher Lange ,  Viengkham Malathong ,  Venkat Reddy Mali ,  Jeffrey McMahon ,  Darren J. McMurtrie ,  Sreenivas Punna ,  Howard S. Roth ,  Rajinder Singh ,  Yu Wang ,  Ju Yang ,  Penglie Zhang

IPC分类号： C07D207/12 ,  A61K45/06 ,  C07D401/12 ,  C07D207/267 ,  C07D211/44 ,  C07D403/12 ,  C07D211/38 ,  C07D451/06 ,  C07D205/12 ,  C07F5/02 ,  C07D405/14 ,  C07D401/14 ,  C07D471/10 ,  C07D211/76 ,  A61P37/02 ,  C07D205/04 ,  C07D213/85 ,  C07D295/088 ,  C07D487/10 ,  C07D405/12 ,  A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/40 ,  C07D211/46

CPC分类号： C07D207/12 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4427 ,  A61K31/454 ,  A61K31/4545 ,  A61K45/06 ,  A61P37/02 ,  C07D205/04 ,  C07D205/12 ,  C07D207/267 ,  C07D211/38 ,  C07D211/40 ,  C07D211/44 ,  C07D211/46 ,  C07D211/76 ,  C07D213/85 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/10 ,  C07F5/025

摘要： Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I):




including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US11420933B2

公开(公告)日：2022-08-23

申请号：US17104294

申请日：2020-11-25

申请人： Novartis AG

发明人： Luis Brito ,  Delai Chen ,  Gabriel Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC分类号： C07C229/12 ,  A61K47/18 ,  C07C229/38 ,  C07D205/04 ,  C07D265/30 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D295/088 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D295/15 ,  C07C271/20 ,  C07C219/04 ,  A61K9/127 ,  A61K9/51 ,  A61K31/7105 ,  A61K31/713 ,  A61K39/12 ,  A61K39/39 ,  C07C271/22 ,  C07D211/06 ,  C07D211/34 ,  C07D211/44 ,  A61K39/00

摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US11104654B2

公开(公告)日：2021-08-31

申请号：US16509963

申请日：2019-07-12

申请人： OREGON HEALTH & SCIENCE UNIVERSITY

发明人： Thomas S. Scanlan ,  Andrew Placzek ,  Tapasree Banerji ,  Sky Ferrara ,  James Matthew Meinig

IPC分类号： C07D295/088 ,  C07C219/06 ,  C07C229/36 ,  C07C235/06 ,  C07C237/08 ,  C07C69/736 ,  C07H13/04 ,  A61P25/00 ,  C07C69/708 ,  C07C229/08 ,  C07C237/12 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D211/42 ,  C07D211/44 ,  C07D233/64 ,  C07D309/10

摘要： Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

公开(公告)号：US20210230116A1

公开(公告)日：2021-07-29

申请号：US17090375

申请日：2020-11-05

申请人： 89BIO LTD

发明人： Nadine C. Becknell ,  Reddeppa Reddy Dandu ,  Bruce D. Dorsey ,  Dimitar B. Gotchev ,  Robert L. Hudkins ,  Linda Weinberg ,  Craig A. Zificsak ,  Allison L. Zulli

IPC分类号： C07D211/44 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D495/02 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D409/12 ,  C07D495/04

摘要： Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

公开(公告)号：US20210147356A1

公开(公告)日：2021-05-20

申请号：US17106309

申请日：2020-11-30

申请人： CHEMOCENTRYX, INC.

发明人： Christopher LANGE ,  Viengkham MALATHONG ,  Venkat Reddy MALI ,  Jeffrey McMAHON ,  Darren J. McMURTRIE ,  Sreenivas PUNNA ,  Howard S. ROTH ,  Rajinder SINGH ,  Yu WANG ,  Ju YANG ,  Penglie ZHANG

IPC分类号： C07D207/12 ,  A61K45/06 ,  C07D401/12 ,  C07D207/267 ,  C07D211/44 ,  C07D403/12 ,  C07D211/38 ,  C07D451/06 ,  C07D205/12 ,  C07F5/02 ,  C07D405/14 ,  C07D401/14 ,  C07D471/10 ,  C07D211/76 ,  A61P37/02 ,  C07D205/04 ,  C07D213/85 ,  C07D295/088 ,  C07D487/10 ,  C07D405/12 ,  A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/40 ,  C07D211/46

摘要： Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US10851079B2

公开(公告)日：2020-12-01

申请号：US16079713

申请日：2017-02-27

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Yoshikazu Kawano ,  Hiroshi Shimizu ,  Shunpei Ishikawa ,  Isao Takemura ,  Norimitsu Hariguchi ,  Miki Matsuba ,  Makoto Matsumoto

IPC分类号： C07D401/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D211/44 ,  A61K31/498 ,  A61K31/55 ,  A61K31/554 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/553 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5415 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/536

摘要： The purpose of the present invention is to provide a compound having excellent antibacterial activity against mycobacterium tuberculosis, multidrug-resistant tuberculosis bacteria, and/or non-tuberculous acid-fast bacteria. A compound represented by formula [I]: (in the formula, each symbol is as described in the attached specification), or a salt thereof can be used to diagnose, prevent, and/or treat tuberculosis.

公开(公告)号：US20200181103A1

公开(公告)日：2020-06-11

申请号：US16509963

申请日：2019-07-12

申请人： OREGON HEALTH & SCIENCE UNIVERSITY

发明人： Thomas S. Scanlan ,  Andrew Placzek ,  Tapasree Banerji ,  Sky Ferrara ,  James Matthew Meinig

IPC分类号： C07D295/088 ,  C07D309/10 ,  C07D233/64 ,  C07D211/44 ,  C07D211/42 ,  C07D211/22 ,  C07D207/08 ,  C07D205/04 ,  C07C237/12 ,  C07C229/08 ,  C07C69/708 ,  C07H13/04 ,  C07C69/736 ,  C07C237/08 ,  C07C235/06 ,  C07C229/36 ,  C07C219/06 ,  A61P25/00

摘要： Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

公开(公告)号：US20200157048A1

公开(公告)日：2020-05-21

申请号：US16625922

申请日：2019-03-26

申请人： BIOWAY., INC

发明人： Jong Woo KIM ,  Chi Woo LEE ,  Hak Sung KIM ,  Dirgha Raj JOSHI ,  Sang Hoon KWON

IPC分类号： C07D211/58 ,  C07D241/04 ,  C07D265/30 ,  C07C321/28 ,  C07D211/44 ,  C07D211/42 ,  A61P1/16

摘要： The present application relates to a novel pentadienoyl compound and a pharmaceutical composition including the same. The pentadienoyl compound of the present application may be used to prevent or treat fatty liver and fatty liver-related disease by inhibiting lipogenesis and lipid accumulation in cells and activating lipid metabolism. In addition, the pentadienoyl compound of the present application may increase a SIRT1 expression level in cells or SIRT1 activity, and thus may be used to prevent or treat a SIRT1-mediated disease. In addition, the pentadienoyl compound of the present application may reduce a CK2 expression level in cells or CK2 activity, and thus may be used to prevent or treat a CK2-mediated disease.

公开(公告)号：US10464897B2

公开(公告)日：2019-11-05

申请号：US15577845

申请日：2016-06-03

申请人： Dana-Farber Cancer Institute, Inc.

发明人： James Bradner ,  Michael Erb ,  Jun Qi

IPC分类号： C07D211/44 ,  C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  C07D239/78 ,  C07D471/04 ,  C07D211/58 ,  C07D213/30 ,  A61P35/00

摘要： The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof.