公开(公告)号：US20240150355A1

公开(公告)日：2024-05-09

申请号：US18540129

申请日：2023-12-14

Applicant: ASTRAZENECA AB ,  CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Maurice Raymond Verschoyle FINLAY ,  Frederick Woolf GOLDBERG ,  Martin Richard HOWARD ,  Attilla Kuan Tsuei TING

IPC: C07D473/32 ,  A61K9/127 ,  A61K31/437 ,  A61K31/502 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/704

CPC classification number: C07D473/32 ,  A61K9/127 ,  A61K31/437 ,  A61K31/502 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/704 ,  A61N5/10

Abstract: The specification generally relates to compounds of Formula (I):




and pharmaceutically acceptable salts thereof, where R1, A1, A2 and A3 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

公开(公告)号：US20230271949A1

公开(公告)日：2023-08-31

申请号：US18056836

申请日：2022-11-18

Applicant: ASCLETIS BIOSCIENCE CO., LTD.

Inventor： Bin Liang ,  Yacheng Yang ,  Peng Wang ,  Bailing Yang ,  Yang Lai ,  Jinzi J. Wu

IPC: C07D405/14 ,  C07D401/10 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04 ,  C07D471/08 ,  C07D471/04 ,  C07D473/32 ,  C07D409/14 ,  C07D413/14 ,  C07D495/04 ,  C07D513/04 ,  C07D498/04

CPC classification number: C07D405/14 ,  C07D401/10 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04 ,  C07D471/08 ,  C07D471/04 ,  C07D473/32 ,  C07D409/14 ,  C07D413/14 ,  C07D495/04 ,  C07D513/04 ,  C07D498/04

Abstract: The present application describes GLP-IR modulating compounds that are useful for treating GLP-IR-mediated diseases or conditions.

公开(公告)号：US20180280398A1

公开(公告)日：2018-10-04

申请号：US16000968

申请日：2018-06-06

Applicant: Celgene Corporation

Inventor： Stacie S. CANAN ,  Natalie Anne HAWRYLUK

IPC: A61K31/52 ,  C07C211/36 ,  C07D473/32 ,  C07C217/02 ,  C07C13/06 ,  G01N33/569 ,  C07D231/02

CPC classification number: A61K31/52 ,  C07C13/06 ,  C07C211/36 ,  C07C217/02 ,  C07D231/02 ,  C07D473/32 ,  G01N33/56905 ,  Y02A50/411

Abstract: Provided herein are Purine Compounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.

公开(公告)号：US09988383B2

公开(公告)日：2018-06-05

申请号：US15100697

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： Victoria Elizabeth Jackson ,  Boris Kroeplien ,  Martin Alexander Lowe ,  John Robert Porter

IPC: C07D473/00 ,  C07D473/32 ,  A61K31/5377

CPC classification number: C07D473/00 ,  A61K31/5377 ,  C07D473/32

Abstract: A series of substituted purine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US20170355712A1

公开(公告)日：2017-12-14

申请号：US15601888

申请日：2017-05-22

Applicant: Epizyme, Inc.

Inventor： John Emmerson Campbell ,  Kenneth William Duncan ,  Megan Alene Foley ,  Darren Martin Harvey ,  Kevin Wayne Kuntz ,  James Edward John Mills ,  Michael John Munchhof

IPC: C07D498/04 ,  C07D405/14 ,  C07D405/12 ,  C07D215/38 ,  C07D487/04 ,  C07D491/044 ,  C07D401/14 ,  C07D401/12 ,  C07D213/74 ,  C07D473/32 ,  C07D239/49 ,  C07D403/14 ,  C07D239/48 ,  C07D413/12 ,  C07D471/04 ,  C07D413/14 ,  C07D403/12 ,  C07D409/14

CPC classification number: C07D498/04 ,  C07D213/74 ,  C07D215/38 ,  C07D231/38 ,  C07D239/48 ,  C07D239/49 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D473/32 ,  C07D487/04 ,  C07D491/044

Abstract: The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US20170348316A1

公开(公告)日：2017-12-07

申请号：US15611108

申请日：2017-06-01

Applicant: Celgene Corporation

Inventor： Stacie S. CANAN ,  Natalie Anne HAWRYLUK

IPC: A61K31/52 ,  C07D473/32 ,  C07C211/36 ,  C07D231/02 ,  C07C13/06 ,  G01N33/569 ,  C07C217/02

CPC classification number: A61K31/52 ,  C07C13/06 ,  C07C211/36 ,  C07C217/02 ,  C07D231/02 ,  C07D473/32 ,  G01N33/56905

Abstract: Provided herein are Purine Comounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.

公开(公告)号：US20170340633A1

公开(公告)日：2017-11-30

申请号：US15589910

申请日：2017-05-08

Applicant: ICOS CORPORATION

Inventor： Chanchal SADHU ,  Ken DICK ,  Jennifer TREIBERG ,  C. Gregory SOWELL ,  Edward A. KESICKI ,  Amy OLIVER

IPC: A61K31/506 ,  C12N9/12 ,  C07D487/04 ,  C07D473/40 ,  C07D473/38 ,  C07D473/34 ,  C07D473/32 ,  C07D473/30 ,  C07D473/24 ,  C07D473/16 ,  C07D473/00 ,  C12N9/99 ,  C07D403/12

CPC classification number: A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

公开(公告)号：US09737541B2

公开(公告)日：2017-08-22

申请号：US15335619

申请日：2016-10-27

Applicant: Signal Pharmaceuticals, LLC

Inventor： Matthew Alexander ,  Sogole Bahmanyar ,  Joshua Hansen ,  Dehua Huang ,  Robert Hubbard ,  Brandon Jeffy ,  Jim Leisten ,  Mehran Moghaddam ,  Raj K. Raheja ,  Heather Raymon ,  Kimberly Schwarz ,  Marianne Sloss ,  Eduardo Torres ,  Tam Minh Tran ,  Shuichan Xu ,  JingJing Zhao ,  John Frederick Boylan

IPC: C07D473/32 ,  A61K31/52 ,  A61K31/5377

CPC classification number: A61K31/52 ,  A61K31/5377 ,  A61P35/00 ,  C07D473/32

Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

公开(公告)号：US09708326B2

公开(公告)日：2017-07-18

申请号：US14770438

申请日：2014-02-20

Applicant: Pharmacyclics LLC

Inventor： Wei Chen ,  Shunqi Yan ,  David J. Loury ,  Leah Lynn Frye ,  Jeremy Robert Greenwood ,  Mee Yoo Shelley ,  Longcheng Wang

IPC: C07D473/32 ,  C07D487/04

CPC classification number: C07D473/32 ,  C07D487/04

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

公开(公告)号：US20170042902A1

公开(公告)日：2017-02-16

申请号：US15335619

申请日：2016-10-27

Applicant: Signal Pharmaceuticals, LLC

Inventor： Matthew Alexander ,  Sogole Bahmanyar ,  Joshua Hansen ,  Dehua Huang ,  Robert Hubbard ,  Brandon Jeffy ,  Jim Leisten ,  Mehran Moghaddam ,  Raj K. Raheja ,  Heather Raymon ,  Kimberly Schwarz ,  Marianne Sloss ,  Eduardo Torres ,  Tam Minh Tran ,  Shuichan Xu ,  JingJing Zhao ,  John Frederick Boylan

IPC: A61K31/52 ,  A61K31/5377

CPC classification number: A61K31/52 ,  A61K31/5377 ,  A61P35/00 ,  C07D473/32

Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

Abstract translation: 本文提供具有以下结构的氨基嘌呤化合物：其中R1，R2和R3如本文所定义，包含有效量的氨基嘌呤化合物的组合物，以及用于治疗或预防癌症的方法，例如黑素瘤。