公开(公告)号：US12084424B2

公开(公告)日：2024-09-10

申请号：US18319630

申请日：2023-05-18

申请人： NOVARTIS AG

发明人： Luigi Franchi ,  Shomir Ghosh ,  Gary Glick ,  Jason Katz ,  Anthony William Opipari, Jr. ,  William Roush ,  Hans Martin Seidel ,  Dong-Ming Shen ,  Shankar Venkatraman ,  David Guenther Winkler

IPC分类号： C07D277/36 ,  C07C307/06 ,  C07D215/36 ,  C07D231/18 ,  C07D239/26 ,  C07D263/46 ,  C07D307/64 ,  C07D307/79 ,  C07D317/62 ,  C07D333/34 ,  C07D487/04 ,  C07C335/42 ,  C07D213/71 ,  C07D231/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D277/36 ,  C07C307/06 ,  C07D215/36 ,  C07D231/18 ,  C07D239/26 ,  C07D263/46 ,  C07D307/64 ,  C07D307/79 ,  C07D317/62 ,  C07D333/34 ,  C07D487/04 ,  C07C335/42 ,  C07D213/71 ,  C07D231/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

摘要： In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:






or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

公开(公告)号：US20220372028A1

公开(公告)日：2022-11-24

申请号：US17221549

申请日：2021-04-02

申请人： The Institute of Cancer Research: Royal Cancer Hospital

发明人： Caroline SPRINGER ,  Richard MARAIS ,  Dan NICULESCU-DUVAZ ,  Leo LEUNG ,  Deborah SMITHEN ,  Cedric CALLENS ,  Haoran TANG

IPC分类号： C07D417/12 ,  C07D333/34 ,  C07D277/36 ,  C07D263/46 ,  C07D409/12 ,  A61P35/00 ,  C07D277/26 ,  C07D333/18 ,  C12Q1/37

摘要： Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

公开(公告)号：US11345671B2

公开(公告)日：2022-05-31

申请号：US16961348

申请日：2019-01-10

申请人： KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION ,  INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY ,  GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY ,  SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION

发明人： Jae Sung Bae ,  Hee Kyung Jin ,  Myung Shik Lee ,  Hye Jin Lim ,  Jin Hee Ahn ,  Haushabhau Shivaji Pagire ,  Min Jae Lee

IPC分类号： C07D263/46

摘要： The present invention relates to a novel phenylsulfonyl oxazole derivative and a use thereof and specifically, to a compound represented by Chemical Formula 1 in the present specification or a pharmaceutically acceptable salt thereof, and to a use thereof for prevention, treatment, or improvement of neurodegenerative disease.

公开(公告)号：US20210230129A1

公开(公告)日：2021-07-29

申请号：US16632850

申请日：2018-07-23

申请人： NOVARTIS INFLAMMASOME RESEARCH, INC.

发明人： Luigi FRANCHI ,  Shomir GHOSH ,  Gary GLICK ,  Jason KATZ ,  Anthony William OPIPARI, Jr. ,  William ROUSH ,  Hans Martin SEIDEL ,  Dong-Ming SHEN ,  Shankar VENKATRAMAN ,  David Guenther WINKLER

IPC分类号： C07D265/30 ,  C07D333/34 ,  C07C381/10 ,  C07D277/36 ,  C07D263/46 ,  C07D231/12 ,  C07D239/26 ,  C07D317/50 ,  C07D215/06 ,  C07D209/26 ,  C07D211/78 ,  C07D239/36 ,  C07D261/08 ,  C07D417/12 ,  C07D409/12 ,  C07D401/12 ,  A61P1/00 ,  A61P11/00 ,  A61P19/08 ,  A61P35/00

摘要： In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured. The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

公开(公告)号：US11059795B2

公开(公告)日：2021-07-13

申请号：US16852810

申请日：2020-04-20

申请人： ESSA Pharma, Inc. ,  The University of British Columbia ,  Provincial Health Services Authority

发明人： Han-Jie Zhou ,  Peter Virsik ,  Raymond John Andersen ,  Marianne Dorothy Sadar

IPC分类号： C07D263/46 ,  A61P35/00 ,  C07D271/113 ,  C07D261/08 ,  C07D263/48 ,  C07D231/38 ,  C07D239/42 ,  C07D233/74 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  C07D307/64 ,  C07D241/20 ,  C07D263/38 ,  C07D233/84 ,  C07D233/88 ,  C07D233/80 ,  C07D233/76

摘要： The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.

公开(公告)号：US10995088B2

公开(公告)日：2021-05-04

申请号：US16908487

申请日：2020-06-22

申请人： The Institute of Cancer Research: Royal Cancer Hospital

发明人： Caroline Springer ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Leo Leung ,  Deborah Smithen ,  Cedric Callens ,  Haoran Tang

IPC分类号： C07D417/12 ,  A61P35/00 ,  C07D263/46 ,  C07D277/46 ,  C07D277/36 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C12Q1/37 ,  C07D277/26

摘要： Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

公开(公告)号：US10975043B2

公开(公告)日：2021-04-13

申请号：US16773720

申请日：2020-01-27

申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED

发明人： Yoshihiro Banno ,  Masahiro Kamaura ,  Kazuaki Takami ,  Koichiro Fukuda ,  Shigekazu Sasaki

IPC分类号： A61K31/4418 ,  A61K31/505 ,  C07D239/34 ,  C07D213/65 ,  C07D213/70 ,  C07D263/46 ,  A61K31/415 ,  A61K31/421 ,  C07D231/12 ,  C07D231/22 ,  C07D263/38 ,  A61P27/02 ,  C07K14/47 ,  C12N15/09

摘要： Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.
A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.

公开(公告)号：US10408820B2

公开(公告)日：2019-09-10

申请号：US14311069

申请日：2014-06-20

申请人： The General Hospital Corporation

发明人： Vineet Gupta ,  M. Amin Arnaout

IPC分类号： G01N33/50 ,  C07C233/81 ,  C07C251/20 ,  C07C311/39 ,  C07D213/85 ,  C07D239/48 ,  C07D249/10 ,  C07D263/46 ,  C07D265/34 ,  C07D277/14 ,  C07D277/36 ,  C07D277/42 ,  C07D277/54 ,  C07D277/72 ,  C07D311/16 ,  C07D333/22 ,  C07D333/68 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/06 ,  C07D498/04 ,  C07D513/18

摘要： The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.

公开(公告)号：US20190177285A1

公开(公告)日：2019-06-13

申请号：US16327478

申请日：2017-08-22

申请人： NORTH CAROLINA STATE UNIVERSITY

发明人： Joshua G. Pierce ,  Jonathan J. Mills

IPC分类号： C07D263/40 ,  A01N43/76 ,  C07D263/46 ,  A61P31/04 ,  A61L31/08 ,  A61L31/16

摘要： Provided herein are oxazolidinone derivatives that can exhibit anti-microbial activity and/or activity as biofilm modulating agents (e.g., activity as biofilm inhibitors and/or activity as biofilm dispersal agents). The compounds can exhibit potent activity anti-microbial activity (e.g., potent activity against Gram-positive positive bacteria including methicillin-resistant Staphylococcus aureus). The compounds can exhibit potent activity against biofilms. In some cases, the compounds can exhibit both anti-microbial activity and biofilm modulation properties.

公开(公告)号：US20110190125A1

公开(公告)日：2011-08-04

申请号：US12989050

申请日：2009-04-15

申请人： Christopher Hugh Rosinger ,  Dieter Feucht ,  Dirk Schmutzler ,  Isolde Haeuser-Hahn ,  Jan Dittgen ,  Arianna Martelletti ,  Hansjorg Dietrich

发明人： Christopher Hugh Rosinger ,  Dieter Feucht ,  Dirk Schmutzler ,  Isolde Haeuser-Hahn ,  Jan Dittgen ,  Arianna Martelletti ,  Hansjorg Dietrich

IPC分类号： A01N25/32 ,  C07D263/46 ,  A01N43/76 ,  C07D263/48 ,  A01P13/00

CPC分类号： C07D263/46 ,  C07D413/12

摘要： The invention relates to 2-(benzylsulfonyl)-oxazole derivatives, chiral 2-(benzylsulfinyl)-oxazole derivatives and 2-(benzylsulfanyl)-oxazole derivatives of general formula (I) and the salts thereof, wherein the individual radicals and indexes have the meaning indicated in the description. Also described are methods for the production thereof as well as the use of said compounds as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.

摘要翻译： 本发明涉及2-（苄基磺酰基） - 恶唑衍生物，通式（I）的手性2-（苄基亚磺酰基） - 恶唑衍生物和2-（苄基硫烷基） - 恶唑衍生物及其盐，其中各基团和指数具有 意义在说明书中指出。 还描述了其生产方法以及所述化合物作为除草剂和植物生长调节剂的用途，特别是作为用于选择性控制植物作物中杂草的除草剂。