公开(公告)号：US20190119245A1

公开(公告)日：2019-04-25

申请号：US15886192

申请日：2018-02-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qingjie Liu ,  Scott Hunter Watterson ,  John E. Macor ,  Khehyong Ngu ,  Saleem Ahmad

IPC: C07D401/10 ,  A61P37/00 ,  C07D403/12 ,  C07D209/08 ,  C07D209/18 ,  C07D487/10 ,  C07D487/04 ,  C07D471/04 ,  C07D417/04 ,  C07D413/04 ,  C07D403/10 ,  C07D403/04 ,  C07D401/12 ,  C07D401/06 ,  C07D401/04 ,  A61P29/00

CPC classification number: C07D401/10 ,  A61P29/00 ,  A61P37/00 ,  C07D209/08 ,  C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US20190112279A1

公开(公告)日：2019-04-18

申请号：US16218108

申请日：2018-12-12

Applicant: FORMA Therapeutics, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR. ,  David S. Millan ,  Matthew W. Martin ,  Kenneth W. Bair

IPC: C07D267/14 ,  C07D413/04 ,  C07D267/12 ,  C07D413/06 ,  C07D401/06 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D243/14 ,  C07D291/08 ,  C07D498/08 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D495/10 ,  C07D491/107 ,  C07D413/08 ,  C07D493/08 ,  C07D413/12

CPC classification number: C07D267/14 ,  C07D243/14 ,  C07D267/12 ,  C07D291/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/107 ,  C07D493/08 ,  C07D495/10 ,  C07D498/04 ,  C07D498/08

Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20190077790A1

公开(公告)日：2019-03-14

申请号：US16080323

申请日：2016-04-03

Applicant: Boehringer Ingelheim International GmbH

Inventor： Frank HIMMELSBACH ,  Andreas BLUM ,  Stefan PETERS

IPC: C07D403/04 ,  C07D401/04 ,  C07D295/116 ,  C07D295/096 ,  C07D205/04 ,  C07D471/04 ,  C07D211/34 ,  C07D211/26 ,  C07D211/70 ,  C07D417/04 ,  C07D413/04 ,  C07D451/02 ,  C07D471/20

CPC classification number: C07D403/04 ,  A61P1/16 ,  C07D205/04 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/26 ,  C07D211/28 ,  C07D211/34 ,  C07D211/52 ,  C07D211/58 ,  C07D211/62 ,  C07D211/64 ,  C07D211/70 ,  C07D211/96 ,  C07D213/72 ,  C07D213/82 ,  C07D213/85 ,  C07D237/20 ,  C07D239/42 ,  C07D239/47 ,  C07D241/04 ,  C07D241/08 ,  C07D241/20 ,  C07D251/42 ,  C07D277/38 ,  C07D295/096 ,  C07D295/116 ,  C07D295/155 ,  C07D309/14 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D451/02 ,  C07D471/04 ,  C07D471/20

Abstract: The invention relates to new benzonitrile derivatives of the formula (I) wherein R1 to R3 and A are as defined in the description and Claims, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

公开(公告)号：US20190062321A1

公开(公告)日：2019-02-28

申请号：US16049482

申请日：2018-07-30

Applicant: CHDI Foundation, Inc.

Inventor： Celia Dominguez ,  Ignacio Muñoz-Sanjuán ,  Roland W. Bürli ,  Christopher A. Luckhurst ,  Daniel R. Allen ,  Gilles Raphy ,  Perla Breccia ,  Alan F. Haughan ,  Grant Wishart ,  Samantha J. Hughes ,  Rebecca E. Jarvis ,  Huw D. Vater ,  Stephen D. Penrose ,  Michael Wall ,  Andrew J. Stott ,  Elizabeth A. Saville-Stones

IPC: C07D417/04 ,  C07D275/04 ,  C07D231/56 ,  C07C259/08 ,  C07D277/60 ,  C07D231/54 ,  C07D239/74 ,  C07D239/70 ,  C07D403/04 ,  C07D401/04 ,  C07D239/88

CPC classification number: C07D417/04 ,  C07C259/08 ,  C07D231/54 ,  C07D231/56 ,  C07D239/70 ,  C07D239/74 ,  C07D239/88 ,  C07D275/04 ,  C07D277/60 ,  C07D401/04 ,  C07D403/04

Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, or pharmaceutically acceptable salts thereof, compositions thereof, and methods of their use.

公开(公告)号：US20190062288A1

公开(公告)日：2019-02-28

申请号：US16173871

申请日：2018-10-29

Applicant: FORMA Therapeutics, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR. ,  David S. Millan ,  Matthew W. Martin

IPC: C07D267/14 ,  C07D413/04 ,  C07D267/12 ,  C07D413/06 ,  C07D401/06 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D243/14 ,  C07D291/08 ,  C07D498/08 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D495/10 ,  C07D491/107 ,  C07D413/08 ,  C07D493/08 ,  C07D413/12

CPC classification number: C07D267/14 ,  C07D243/14 ,  C07D267/12 ,  C07D291/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/107 ,  C07D493/08 ,  C07D495/10 ,  C07D498/04 ,  C07D498/08

Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20190047961A1

公开(公告)日：2019-02-14

申请号：US16059075

申请日：2018-08-09

Applicant: Janssen Pharmaceutica NV

Inventor： Xuqing Zhang ,  Mark J. Macielag

IPC: C07D213/64 ,  C07D413/04 ,  C07D417/04 ,  A61P3/10

CPC classification number: C07D213/64 ,  A61P3/10 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.

公开(公告)号：US20190038578A1

公开(公告)日：2019-02-07

申请号：US16153706

申请日：2018-10-06

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Zhiyuan Zhang ,  Xiaodong Wang ,  Yaning Su ,  Hanying Ruan ,  Yan Ren

IPC: A61K31/165 ,  C07D417/04 ,  C07D263/22 ,  C07D207/12 ,  C07D205/04 ,  C07D263/04 ,  C07D205/08 ,  C07D261/02 ,  C07D207/06 ,  C07D231/02 ,  C07D241/04 ,  C07D207/08 ,  C07D231/08 ,  C07D233/38 ,  C07D207/20 ,  C07D211/16 ,  C07D207/24 ,  C07D405/04 ,  C07C233/01 ,  C07D265/30 ,  C07C235/38 ,  C07D231/04 ,  C07D211/70 ,  C07D207/333 ,  C07D207/27 ,  C07D203/18 ,  C07D409/04 ,  A61K31/167 ,  A61K31/10 ,  C07D211/82

CPC classification number: A61K31/165 ,  A61K31/10 ,  A61K31/167 ,  C07C233/01 ,  C07C235/38 ,  C07D203/18 ,  C07D205/04 ,  C07D205/08 ,  C07D207/06 ,  C07D207/08 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D207/27 ,  C07D207/333 ,  C07D211/16 ,  C07D211/70 ,  C07D211/82 ,  C07D231/02 ,  C07D231/04 ,  C07D231/08 ,  C07D233/38 ,  C07D241/04 ,  C07D261/02 ,  C07D263/04 ,  C07D263/22 ,  C07D265/30 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04

Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US20190023657A1

公开(公告)日：2019-01-24

申请号：US16138369

申请日：2018-09-21

Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.

Inventor： Fumihiko SAITOH ,  Hiroshi NAGASUE

IPC: C07D213/75 ,  A61K45/06 ,  A61K31/4418 ,  C07D401/04 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  C07D213/84 ,  C07D405/04 ,  A61K31/4433 ,  C07D405/14 ,  C07D213/81 ,  C07D413/12 ,  C07D417/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P9/00 ,  A61P9/06 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/04 ,  A61P11/06 ,  A61P13/02 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P19/02 ,  A61P19/10 ,  A61P21/00 ,  A61P21/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P29/02 ,  A61P31/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07B2200/07 ,  C07C215/44 ,  C07C271/24 ,  C07C2602/10 ,  C07D213/81 ,  C07D213/84 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound represented by formula (I):

公开(公告)号：US20190016670A1

公开(公告)日：2019-01-17

申请号：US16133297

申请日：2018-09-17

Applicant: Ming-Yu Ngai ,  Katarzyna N. Hojczyk

Inventor： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

IPC: C07C233/25 ,  C07D209/08 ,  C07J43/00 ,  C07D473/40 ,  C07D239/91 ,  C07D239/47 ,  C07D405/04 ,  C07D347/00 ,  C07D213/76 ,  C07D213/75 ,  C07C255/60 ,  C07C233/54 ,  C07C233/80 ,  C07C231/12 ,  C07C233/33 ,  C07C233/81 ,  C07D263/57 ,  C07D215/40 ,  C07D401/04 ,  C07D417/04 ,  C07D471/04 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C273/18 ,  C07C231/14 ,  C07C253/30 ,  C07C275/64 ,  C07C271/38 ,  C07C255/58 ,  C07C275/34

CPC classification number: C07C233/25 ,  C07C231/12 ,  C07C231/14 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C253/30 ,  C07C255/58 ,  C07C255/60 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C271/38 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/34 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D215/40 ,  C07D239/47 ,  C07D239/91 ,  C07D263/57 ,  C07D347/00 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/40 ,  C07J43/003 ,  C07C275/64

Abstract: The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without subsutitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl); —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

公开(公告)号：US20190002453A1

公开(公告)日：2019-01-03

申请号：US16131275

申请日：2018-09-14

Applicant: Midwestern University

Inventor： Mark Jon Olsen ,  John Michael Thomas

IPC: C07D417/04 ,  C12Q1/26 ,  C07D409/04 ,  C07D405/12 ,  A61P35/00 ,  C07D307/32 ,  C07D307/66 ,  C07D405/04

CPC classification number: C07D417/04 ,  A61P35/00 ,  C07D307/32 ,  C07D307/66 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C12Q1/26

Abstract: The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.