公开(公告)号：US20200262835A1

公开(公告)日：2020-08-20

申请号：US16784320

申请日：2020-02-07

Applicant: PROXIMAGEN, LLC

Inventor： Max ESPENSEN ,  Lee PATIENT ,  David EVANS ,  Edward SAVORY ,  Iain SIMPSON

IPC: C07D471/04 ,  A61K31/40 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/501 ,  A61K31/506 ,  C07C53/18

Abstract: Compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof, that are inhibitors of SSAO activity: where V, W, X, Y, Z, R1, and R3 are as defined herein.

公开(公告)号：US10428066B2

公开(公告)日：2019-10-01

申请号：US15911935

申请日：2018-03-05

Applicant: PROXIMAGEN, LLC

Inventor： Max Espensen ,  Lee Patient ,  David Evans ,  Iain Simpson ,  Edward Savory

IPC: A61K31/40 ,  C07D471/04 ,  C07C53/18

Abstract: The compounds of formula (I) are inhibitors of SSAO activity wherein V, W, X, Y, Z, R1 and R2 are as defined in the claims.

公开(公告)号：US10421718B2

公开(公告)日：2019-09-24

申请号：US15814600

申请日：2017-11-16

Applicant: THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY

Inventor： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Venkata Velvadapu

IPC: A61K31/195 ,  A61K31/405 ,  A61K31/41 ,  A61K31/42 ,  A61K31/415 ,  A61K31/40 ,  C07D207/327 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/192 ,  A61K31/44 ,  C07C229/56 ,  C07C255/54 ,  C07C255/55 ,  C07C211/27 ,  C07C217/84 ,  C07C233/11 ,  C07C233/64 ,  C07C233/65 ,  C07C235/58 ,  C07C311/08 ,  C07C311/16 ,  C07C311/17 ,  C07C317/14 ,  C07D235/06 ,  C07D403/10 ,  C07D239/26 ,  C07D409/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D209/08 ,  C07D295/155 ,  C07D213/55 ,  C07C53/18 ,  C07C63/66 ,  C07C65/19 ,  C07C65/28 ,  C07C229/64 ,  C07C317/44 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/70 ,  C07D213/64 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D249/06 ,  C07D277/30 ,  C07D307/79 ,  C07D333/54 ,  C07D401/04 ,  C07D401/10

Abstract: Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

公开(公告)号：US10407443B2

公开(公告)日：2019-09-10

申请号：US16041875

申请日：2018-07-23

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Todd Macklin ,  Maria Hopkins ,  Shota Kikuchi

IPC: A61K31/5386 ,  C07D498/08 ,  C07D451/12 ,  C07D471/04 ,  C07D519/00 ,  A61K31/19 ,  C07D221/22 ,  C07C53/40 ,  C07D453/02 ,  C07D471/08 ,  C07C53/18

Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US10407421B2

公开(公告)日：2019-09-10

申请号：US16076781

申请日：2017-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Reynalda Keh Dejesus ,  Haifeng Tang ,  Xianhai Huang ,  Jinlong Jiang ,  Yan Guo ,  Hongwu Wang

IPC: C07D417/14 ,  A61K45/06 ,  C07D471/04 ,  C07C53/18 ,  A61P31/04 ,  A61K31/424 ,  A61K31/431 ,  A61K31/439

Abstract: The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.

公开(公告)号：US10179797B2

公开(公告)日：2019-01-15

申请号：US15774649

申请日：2016-11-23

Applicant: DSM IP ASSETS B.V.

Inventor： Stéphanie Boudon ,  Eileen Jackson ,  Rolf Schuetz ,  Jürgen Herbert Vollhardt ,  Peter Wikstroem ,  Eliane Ursula Wandeler

IPC: A61Q19/08 ,  A61Q19/00 ,  A61K31/675 ,  A61K31/662 ,  A61K31/67 ,  C07C53/18 ,  A61K8/55 ,  C07F9/6553 ,  C07F9/30 ,  C07F9/572

Abstract: This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I).

公开(公告)号：US10125145B2

公开(公告)日：2018-11-13

申请号：US15599239

申请日：2017-05-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: C07D498/08 ,  C07D451/12 ,  C07D471/04 ,  C07D519/00 ,  A61K31/19 ,  A61K31/5386 ,  C07D221/22 ,  C07D453/02 ,  C07C53/40 ,  C07D471/08 ,  C07C53/18

Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20180186808A1

公开(公告)日：2018-07-05

申请号：US15910571

申请日：2018-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Katherine Young ,  David B. Olsen ,  Sheo B. Singh ,  Jing Su ,  Robert R. Wilkening ,  James M. Apgar ,  Dongfang Meng ,  Dann Parker ,  Mihir Mandal ,  Lihu Yang ,  Ronald E. Painter ,  Qun Dang ,  Takao Suzuki

IPC: C07D493/08 ,  C07F7/18 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18

CPC classification number: C07D493/08 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18 ,  C07D519/00 ,  C07F7/1804

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

公开(公告)号：US09981922B2

公开(公告)日：2018-05-29

申请号：US15043121

申请日：2016-02-12

Applicant: Imago Biosciences, Inc.

Inventor： Hugh Y. Rienhoff, Jr. ,  John M. McCall ,  Michael Clare ,  Cassandra Celatka ,  Amy E. Tapper

IPC: C07D249/06 ,  C07C309/30 ,  A61K9/00 ,  A61K31/496 ,  C07D239/26 ,  A61K31/506 ,  C07D295/192 ,  A61K31/495 ,  C07D279/12 ,  A61K31/54 ,  C07D205/04 ,  A61K31/397 ,  C07D295/26 ,  C07D215/54 ,  C07C53/18 ,  C07D231/12 ,  C07D263/32 ,  A61K31/541 ,  C07B59/00 ,  C07D403/12 ,  A61K31/4192 ,  C07D401/12 ,  A61K31/454 ,  C07D249/08 ,  A61K31/4196 ,  C07D211/66 ,  A61K31/445 ,  C07D239/42 ,  C07D491/107 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/5383 ,  C07D471/10 ,  A61K31/435 ,  C07D401/04 ,  A61K31/41 ,  C07D487/04 ,  A61K31/4162 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/551 ,  C07D237/08 ,  A61K31/501 ,  A61K9/16 ,  A61K9/48

CPC classification number: C07D249/06 ,  A61K9/0053 ,  A61K9/1623 ,  A61K9/4858 ,  A61K31/397 ,  A61K31/41 ,  A61K31/4162 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/435 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07B2200/13 ,  C07C53/18 ,  C07C309/30 ,  C07D205/04 ,  C07D211/66 ,  C07D215/54 ,  C07D231/12 ,  C07D237/08 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D263/32 ,  C07D279/12 ,  C07D295/192 ,  C07D295/26 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107 ,  C07D498/08 ,  A61K2300/00

Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

公开(公告)号：US20170360785A1

公开(公告)日：2017-12-21

申请号：US15627851

申请日：2017-06-20

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Dominic REYNOLDS ,  Ming-Hong HAO ,  John WANG ,  Sudeep PRAJAPATI ,  Takashi SATOH ,  Anand SELVARAJ

IPC: A61K31/505 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D239/48 ,  C07C53/18 ,  A61K31/5377 ,  C07D413/12 ,  A61K31/506

Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.