公开(公告)号：US20230183197A1

公开(公告)日：2023-06-15

申请号：US17925493

申请日：2020-06-01

Applicant: NeoPhore Limited

Inventor： Julian Blagg ,  Jon Roffey ,  Martin Drysdale ,  Paul Winship ,  David Clark

IPC: C07D295/16 ,  C07D239/26 ,  C07D209/44 ,  C07D207/12 ,  C07D211/42 ,  C07D213/16 ,  C07D471/04 ,  C07D231/12 ,  C07D249/04 ,  C07D401/12 ,  C07D217/04 ,  C07D217/16 ,  C07D265/36 ,  C07D209/08 ,  C07D215/08 ,  C07D405/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/04 ,  A61K45/06

CPC classification number: C07D295/16 ,  C07D239/26 ,  C07D209/44 ,  C07D207/12 ,  C07D211/42 ,  C07D213/16 ,  C07D471/04 ,  C07D231/12 ,  C07D249/04 ,  C07D401/12 ,  C07D217/04 ,  C07D217/16 ,  C07D265/36 ,  C07D209/08 ,  C07D215/08 ,  C07D405/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/04 ,  A61K45/06

Abstract: The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process:




wherein R1, R2, R3, R4, R6 and R10 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 and/or PMS2 activity is implicated.

公开(公告)号：US11603349B2

公开(公告)日：2023-03-14

申请号：US17228041

申请日：2021-04-12

Applicant: Certa Therapeutics Pty Ltd

Inventor： Thomas Miller ,  Nikolaos Papaioannou

IPC: C07D213/06 ,  C07C235/38 ,  C07C255/60 ,  C07D215/08 ,  C07D231/56 ,  C07D233/58 ,  C07D241/42 ,  C07D249/08 ,  C07D257/04 ,  C07D265/34 ,  C07D271/10 ,  C07D305/08 ,  C07D307/06

Abstract: Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

公开(公告)号：US20220324810A1

公开(公告)日：2022-10-13

申请号：US17640287

申请日：2020-09-22

Applicant: Bayer Aktiengesellschaft

Inventor： Christoph SCHOTES ,  Matthias BELLER ,  Kathrin JUNGE ,  Weiping LIU ,  Jacob SCHNEEKOENIG ,  Thomas LEISCHNER

IPC: C07D215/08

Abstract: New iridium catalysts for enantioselective hydrogenation of 4-substituted 1,2-dihydroquinolines The invention relates to a process for preparing optically active 4-substituted 1, 2, 3, 4-tetrahydroquinolines (la, lb) comprising enantioselective hydrogenation of the corresponding 4-substituted 1,2-dihydroquinolines in presence of a chiral iridium (P,N)-ligand catalyst.

公开(公告)号：US11312682B2

公开(公告)日：2022-04-26

申请号：US15748559

申请日：2015-09-01

Applicant: VILNIUS UNIVERSITY

Inventor： Daumantas Matulis ,  Edita Capkauskaite ,  Andrius Zaksauskas ,  Vaida Morkunaite

IPC: C07C311/16 ,  C07D215/08 ,  C07D235/08 ,  C07D233/58 ,  C07D209/08 ,  C07C321/28 ,  C07D265/30 ,  C07C317/40 ,  A61P3/04 ,  A61P25/18 ,  A61P25/08 ,  A61P35/00

Abstract: Disclosed are novel compounds—benzenesulfonamides of general formulas (I) and (II) The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression. Also disclosed are method of treatment using such compounds.

公开(公告)号：US11274090B2

公开(公告)日：2022-03-15

申请号：US16970169

申请日：2019-02-15

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Jonathan E. Wilson ,  Francois Brucelle ,  Julian R. Levell

IPC: C07D401/04 ,  C07D209/08 ,  C07D213/75 ,  C07D215/08 ,  C07D231/12 ,  C07D231/40 ,  C07D237/08 ,  C07D295/135 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04 ,  C07D491/107

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

公开(公告)号：US20210246100A1

公开(公告)日：2021-08-12

申请号：US17228041

申请日：2021-04-12

Applicant: Certa Therapeutics Pty Ltd

Inventor： Thomas Miller ,  Nikolaos Papaioannou

IPC: C07C235/38 ,  C07C255/60 ,  C07D213/06 ,  C07D215/08 ,  C07D231/56 ,  C07D233/58 ,  C07D241/42 ,  C07D249/08 ,  C07D257/04 ,  C07D265/34 ,  C07D271/10 ,  C07D305/08 ,  C07D307/06

Abstract: Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

公开(公告)号：US10723726B2

公开(公告)日：2020-07-28

申请号：US15735560

申请日：2016-06-10

Applicant: GB006, INC.

Inventor： Antonio J. Barbosa

IPC: C07D417/06 ,  A61P35/00 ,  C07D215/08 ,  C07C215/08

Abstract: The present invention provides new salts and crystalline forms of leukadherin LA1 [(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid] according to Formula I. Methods for preparation of the salts and crystalline forms are also described, as well as methods for treating 2 integrin-mediated diseases and conditions using the salts and crystalline forms.

公开(公告)号：US10456394B2

公开(公告)日：2019-10-29

申请号：US15998610

申请日：2017-02-15

Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

Inventor： Alan Kozikowski ,  Sida Shen ,  Joel Bergman ,  Irina Gaisina

IPC: C07D215/08 ,  C07D241/44 ,  C07D279/16 ,  A61K31/498 ,  A61K31/5415 ,  A61K31/47 ,  A61P35/00 ,  A61P37/00 ,  A61P25/28

Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

公开(公告)号：US10301253B2

公开(公告)日：2019-05-28

申请号：US15658219

申请日：2017-07-24

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Brian K. Albrecht ,  James Edmund Audia ,  Alexandre Cote ,  Martin Duplessis ,  Victor S. Gehling ,  Andrew Charles Good ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Christopher G. Nasveschuk ,  Alexander M. Taylor ,  Rishi G. Vaswani

IPC: C07C211/39 ,  C07C211/38 ,  C07C211/17 ,  C07C211/19 ,  A61K31/137 ,  A61K31/136 ,  A61K31/135 ,  A61K31/4465 ,  C07C211/42 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12 ,  C07D211/78 ,  C07D213/38 ,  C07C255/58 ,  C07C217/74 ,  C07C229/50 ,  C07C237/48 ,  A61K31/166 ,  A61K31/196 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/4747 ,  A61K31/495 ,  A61K31/517 ,  A61K45/06 ,  C07C317/36 ,  C07D205/04 ,  C07D205/12 ,  C07D207/06 ,  C07D211/26 ,  C07D211/46 ,  C07D215/08 ,  C07D295/185 ,  C07D305/08 ,  C07D309/04

Abstract: Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

公开(公告)号：US09566284B2

公开(公告)日：2017-02-14

申请号：US14091076

申请日：2013-11-26

Applicant: NONO INC.

Inventor： Xiujun Sun ,  Michael Tymianski ,  Jonathan David Garman

IPC: A61K31/122 ,  A61K31/353 ,  A61K31/551 ,  A61K31/427 ,  A61K31/428 ,  C07D209/08 ,  C07D215/08 ,  C07D215/233 ,  C07D277/36 ,  C07D277/82 ,  C07D311/18 ,  C07D333/38 ,  C07D333/60 ,  C07D339/00 ,  C07D403/06 ,  C07D409/04 ,  C07D409/06 ,  C07D417/04 ,  C40B40/04 ,  G01N33/68 ,  A61K31/381 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496

CPC classification number: A61K31/551 ,  A61K31/122 ,  A61K31/353 ,  A61K31/381 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  C07D209/08 ,  C07D215/08 ,  C07D215/233 ,  C07D277/36 ,  C07D277/82 ,  C07D311/18 ,  C07D333/38 ,  C07D333/60 ,  C07D339/00 ,  C07D403/06 ,  C07D409/04 ,  C07D409/06 ,  C07D417/04 ,  C40B40/04 ,  G01N33/6872 ,  G01N2510/00

Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.

Abstract translation: 本发明涉及使用TRPM7基因和蛋白质活性的调节剂筛选TRPM7基因和蛋白质活性引起的哺乳动物细胞损伤调节剂，调节TRPM7基因的化合物和蛋白质活性的方法以及哺乳动物细胞损伤治疗方法。