公开(公告)号：US11787768B2

公开(公告)日：2023-10-17

申请号：US17192683

申请日：2021-03-04

Applicant: St. Jude Children's Research Hospital

Inventor： R. Kip Guy ,  P Jake Slavish ,  William Robert Shadrick ,  Brandon M. Young ,  Vincent A. Boyd ,  Nagakumar Bharatham ,  Jeanine E. Price ,  Anang Shelat

IPC: C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D413/12

CPC classification number: C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D413/12

Abstract: In one aspect, compounds and compositions that modulate a bromodomain and methods of making and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with inhibition of a bromodomain such as, for example, cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US20230183188A1

公开(公告)日：2023-06-15

申请号：US17988575

申请日：2022-11-16

Applicant: Vir Biotechnology, Inc.

Inventor： Roland D. SAITO ,  Winston C. TSE

IPC: C07D239/94 ,  C07D471/04 ,  C07D215/44 ,  C07D215/54 ,  C07D215/233 ,  C07D405/12 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D239/94 ,  C07D471/04 ,  C07D215/44 ,  C07D215/54 ,  C07D215/233 ,  C07D405/12 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

Abstract: The disclosure provides compositions and methods of quinoline, quinazolines, and pyrydylpyridines derivatives for the inhibition of ENPP1 modulators.

公开(公告)号：US20180208584A1

公开(公告)日：2018-07-26

申请号：US15873255

申请日：2018-01-17

Applicant: Sabila Biosciences LLC

Inventor： Tarek Suhayl MANSOUR

IPC: C07D409/12 ,  C07D409/14 ,  A61P35/00 ,  C07D215/44 ,  C07D401/12

CPC classification number: C07D409/12 ,  A61P35/00 ,  C07D215/44 ,  C07D401/12 ,  C07D409/14

Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.

公开(公告)号：US20180085365A1

公开(公告)日：2018-03-29

申请号：US15811712

申请日：2017-11-14

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Michael Jonathan BURY ,  Linda N. CASILLAS ,  Adam Kenneth CHARNLEY ,  Pamela A. HAILE ,  Robert W. MARQUIS, JR. ,  John F. MEHLMANN ,  Joseph J. ROMANO ,  Robert R. SINGHAUS, JR. ,  Gren Z. WANG

IPC: A61K31/4709 ,  A61K31/4706

CPC classification number: A61K31/4709 ,  A61K31/4706 ,  C07D215/44 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.

公开(公告)号：US09464055B2

公开(公告)日：2016-10-11

申请号：US14615575

申请日：2015-02-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Bart DeCorte ,  Mark Macielag ,  Michael Greco ,  Yue-Mei Zhang ,  Christopher Teleha

IPC: C07D215/44 ,  C07D417/14 ,  C07D409/14 ,  C07D417/06 ,  C07D405/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D215/04 ,  C07D215/42 ,  C07D401/04

CPC classification number: C07D215/44 ,  C07D215/04 ,  C07D215/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C09B11/02

Abstract: The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.

公开(公告)号：US20160038641A1

公开(公告)日：2016-02-11

申请号：US14776995

申请日：2014-03-17

Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE

Inventor： John R. CASHMAN ,  Daniel R. RYAN ,  Sigeng CHEN

IPC: A61L27/38 ,  A61L27/54 ,  A61L27/12 ,  A61L27/42 ,  C07D215/44 ,  A61L27/32 ,  A61L27/28 ,  C07D487/04 ,  C07C49/255 ,  C07C225/22 ,  C07C49/248 ,  C07C229/40 ,  G01N33/50 ,  C12Q1/68 ,  A61L27/58

CPC classification number: A61L27/3895 ,  A61K31/12 ,  A61K31/4706 ,  A61K31/519 ,  A61K33/42 ,  A61K35/28 ,  A61K38/18 ,  A61K45/06 ,  A61L27/12 ,  A61L27/28 ,  A61L27/32 ,  A61L27/3834 ,  A61L27/3847 ,  A61L27/425 ,  A61L27/54 ,  A61L27/58 ,  A61L2300/112 ,  A61L2300/412 ,  A61L2300/606 ,  A61L2300/64 ,  A61L2400/18 ,  A61L2420/02 ,  A61L2420/06 ,  A61L2430/02 ,  A61L2430/40 ,  C07C49/248 ,  C07C49/255 ,  C07C225/22 ,  C07C229/40 ,  C07D215/44 ,  C07D487/04 ,  C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/502 ,  G01N33/5044 ,  G01N2333/916 ,  A61K2300/00

Abstract: Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, transdifferentiation, and proliferation of animal cells into the osteoblast blast cell lineage were described. Examples of osteogenic materials that were administered to cells or co-cultured with cells are represented by compounds of Formula II, IV, and VI independently or preferably in combination with a matrix to afford bone cells. Small molecule-stimulated cells were also combined with a matrix, placed with a cellular adhesive or material carrier and implanted to a site in an animal for bone repair. Matrix pretreated with compounds of Formula II, IV, and VI were also used to cause cells to migrate to the matrix that is of use for therapeutic purposes.

Abstract translation: 描述了小分子，基质和分离的细胞的组成，包括制备方法，以及将动物细胞分化，转分化和增殖到成骨细胞胚细胞谱系中的方法。 施用于细胞或与细胞共培养的成骨材料的实例由式II，IV和VI的化合物独立地或优选与基质组合来表示，以提供骨细胞。 小分子刺激的细胞也与基质组合，放置有细胞粘合剂或材料载体，并植入动物的部位用于骨修复。 用式II，IV和VI化合物预处理的基质也用于使细胞迁移到用于治疗目的的基质中。

公开(公告)号：US20160031854A1

公开(公告)日：2016-02-04

申请号：US14800194

申请日：2015-07-15

Applicant: Milan Stojanovic ,  Francine Katz ,  Donald W. Landry

Inventor： Milan Stojanovic ,  Francine Katz ,  Donald W. Landry

IPC: C07D401/12 ,  C07D215/44 ,  C07D233/60

CPC classification number: C07D401/12 ,  C07D215/44 ,  C07D233/60

Abstract: Disclosed herein is an in vitro or in vivo method of activating or reversing inactivation of acetylcholinesterase (AChE) or butyrylcholinesterase (BuchE) using compounds of the present disclosure. Also disclosed is a method of treating a subject exposed to a nerve agent using such compounds. Also disclosed is a method of treating organophosphate poisoning in a subject using such compounds. Also disclosed is a method of modulating neuronal signaling and transmission in a subject using such compounds.

Abstract translation: 本文公开了使用本公开的化合物活化或逆转乙酰胆碱酯酶（AChE）或丁酰胆碱酯酶（BuchE）的灭活的体外或体内方法。 还公开了使用这些化合物治疗暴露于神经药物的受试者的方法。 还公开了使用这种化合物治疗受试者中的有机磷中毒的方法。 还公开了使用这些化合物调节受试者的神经元信号传导和传播的方法。

公开(公告)号：US20150239845A1

公开(公告)日：2015-08-27

申请号：US14615575

申请日：2015-02-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Bart DeCORTE ,  Mark Macielag ,  Michael Greco ,  Yue-Mei Zhang ,  Christopher Teleha

IPC: C07D215/44 ,  C07D401/12 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C07D401/14

CPC classification number: C07D215/44 ,  C07D215/04 ,  C07D215/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C09B11/02

Abstract: The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.

公开(公告)号：US09029395B2

公开(公告)日：2015-05-12

申请号：US14111580

申请日：2012-04-19

Applicant: Dominique Amans ,  Emmanuel Hubert Demont ,  Darren Jason Mitchell ,  Robert J. Watson

Inventor： Dominique Amans ,  Emmanuel Hubert Demont ,  Darren Jason Mitchell ,  Robert J. Watson

IPC: C07D215/44 ,  C07D215/42 ,  C07D401/12

CPC classification number: C07D215/44 ,  C07D215/42 ,  C07D401/12

Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract translation: 四氢喹啉衍生物，含有这些化合物的药物组合物及其在治疗中的应用。

公开(公告)号：US20150057312A1

公开(公告)日：2015-02-26

申请号：US14390771

申请日：2013-04-03

Applicant: HangzhouDeRenYuCheng Biotechnology Ltd

Inventor： Dawei Zhang

IPC: C07D215/44 ,  A61K45/06 ,  A61K31/4706

CPC classification number: C07D215/44 ,  A61K31/4706 ,  A61K45/06 ,  C07D215/48 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention is directed to novel quinolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. The disclosed substituted quinolines include Bruton's tyrosine kinase (Btk) inhibitors.

Abstract translation: 本发明涉及新型喹啉，其衍生物，药学上可接受的盐，溶剂合物和水合物。 本发明的化合物和组合物具有蛋白激酶抑制活性，可用于治疗蛋白激酶介导的疾病和病症。 所公开的取代的喹啉包括Bruton的酪氨酸激酶（Btk）抑制剂。