公开(公告)号：US11998539B2

公开(公告)日：2024-06-04

申请号：US18072490

申请日：2022-11-30

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  Deutsches Krebsforschungszentrum

Inventor： Norbert Schmees ,  Lars Wortmann ,  Dennis Kirchhoff ,  Thi Thanh Uyen Nguyen ,  Nicolas Werbeck ,  Ulf Bömer ,  Kirstin Petersen ,  Christina Kober ,  Christian Lechner ,  Dirk Kosemund ,  Rienk Offringa ,  Mareike Grees ,  Benjamin Bader

IPC: A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20240174653A1

公开(公告)日：2024-05-30

申请号：US18386267

申请日：2023-11-02

Applicant: Boehringer Ingelheim International GmbH

Inventor： Mary Ruth FLACK ,  Julia KAUFMAN ,  Indra SETHY-CORACI

IPC: C07D405/14 ,  A61P11/00 ,  A61P17/00

CPC classification number: C07D405/14 ,  A61P11/00 ,  A61P17/00

Abstract: The present invention relates to methods for treating patients with systemic sclerosis, comprising administering to a patient in need thereof a therapeutically effective amount of a soluble guanylate cyclase (sGC) activator of formula (I),




or a pharmaceutically acceptable salt thereof, where R1-R7 and A are as defined herein.

公开(公告)号：US20240174648A1

公开(公告)日：2024-05-30

申请号：US17771070

申请日：2020-10-10

Applicant: Technoderma Medicines Pte Ltd

Inventor： Li Xing ,  Guanqun Li ,  Xiaolei Wang ,  Yuting Cai ,  Xiang Jiang ,  Xiang Pan ,  Wenhao Zhu ,  Yang Wang ,  Zengquan Wang

IPC: C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: Provided is a small molecule compound, which is characterized in having the structure represented by the following molecular formula: (I), wherein X1 and X2 are selected from carbon or nitrogen; G1 is a carbocyclic ring or heterocyclic ring having aromaticity; any one or more hydrogen atoms on the ring of G1 are substituted by R1; and R1 is selected from nitrogen-containing groups. The small molecule compound of the present invention can be used as a highly effective and specific JAK kinase inhibitor, specifically a Tyk2 inhibitor; and/or a JAK1 inhibitor, and/or a JAK1/Tyk2 or Tyk2/JAK1, Tyk2/Jak2 dual inhibitor.

公开(公告)号：US11993595B2

公开(公告)日：2024-05-28

申请号：US17901390

申请日：2022-09-01

Applicant: Mission Therapeutics Limited

Inventor： Alison Jones ,  Mark Ian Kemp ,  Martin Lee Stockley ,  Karl Richard Gibson ,  Gavin Alistair Whitlock ,  Andrew Madin

IPC: C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

CPC classification number: C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.

公开(公告)号：US11993585B2

公开(公告)日：2024-05-28

申请号：US17342873

申请日：2021-06-09

Applicant: Mitobridge, Inc.

Inventor： Taisuke Takahashi ,  Arthur Kluge ,  Bharat Lagu ,  Nan Ji

IPC: C07D401/14 ,  A61P13/12 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

CPC classification number: C07D401/14 ,  A61P13/12 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula:




The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.

公开(公告)号：US11987573B2

公开(公告)日：2024-05-21

申请号：US17287137

申请日：2019-10-23

Applicant: Step Pharma S.A.S.

Inventor： Abdul Quddus ,  Emma Blackham

IPC: C07D401/14 ,  A61P35/00 ,  C07D405/14

CPC classification number: C07D401/14 ,  A61P35/00 ,  C07D405/14

Abstract: Compounds of formula (I), and related aspects.

公开(公告)号：US11987560B2

公开(公告)日：2024-05-21

申请号：US17356389

申请日：2021-06-23

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D239/47 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/551 ,  C07B59/00 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/10

CPC classification number: C07D239/47 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/551 ,  C07B59/002 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/10 ,  C07B2200/05

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US20240158415A1

公开(公告)日：2024-05-16

申请号：US18303264

申请日：2023-04-19

Applicant: HiberCell, Inc.

Inventor： Johan Lindström ,  Lars Boukharta Persson ,  Jenny Viklund ,  Edward A. Kesicki ,  Eugene R. Hickey ,  Markus K. Dahlgren ,  Aleksey I. Gerasyuto

IPC: C07D498/14 ,  A61P35/00 ,  C07D213/74 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D513/14 ,  C07D519/00 ,  C07F5/02

CPC classification number: C07D498/14 ,  A61P35/00 ,  C07D213/74 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D513/14 ,  C07D519/00 ,  C07F5/02

Abstract: The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: (T) where A, B, R1, X1, X2, and W are described herein.

公开(公告)号：US20240158385A1

公开(公告)日：2024-05-16

申请号：US18275862

申请日：2022-02-08

Applicant: Cerevance, Inc.

Inventor： Roland Werner Burli ,  Kevin Doyle ,  Martin Teall

IPC: C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

CPC classification number: C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, N-oxides, solvates and prodrugs thereof Formula (I) wherein R2, R3, R4, X1, X2, X3 and X4 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly for use in treating disorders associated with KCNK13 activity.

公开(公告)号：US20240158378A1

公开(公告)日：2024-05-16

申请号：US18548489

申请日：2022-02-28

Applicant: Orion Corporation

Inventor： Oskari Karjalainen ,  Mikko Mäkelä ,  Mihaela Pop ,  Anna Shevchenko ,  Eija Tiainen

IPC: C07D405/14 ,  A61K31/454

CPC classification number: C07D405/14 ,  A61K31/454

Abstract: The present invention relates to novel solid forms, particularly crystalline forms, of 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (I). Compound (I) is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.