公开(公告)号：US20200181170A1

公开(公告)日：2020-06-11

申请号：US16463603

申请日：2017-11-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Prasanna Sivaprakasam ,  Gene M. Dubowchik ,  John E. Macor

IPC: C07D498/18 ,  C07D471/22 ,  C07D498/22

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US09809573B2

公开(公告)日：2017-11-07

申请号：US15033770

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04 ,  C07D213/81 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D401/12 ,  C07D213/81 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US12097242B2

公开(公告)日：2024-09-24

申请号：US17721569

申请日：2022-04-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Gene M. Dubowchik ,  Olafur S. Gudmundsson ,  Xiaojun Han ,  R. Michael Lawrence ,  Dasa Lipovsek ,  Cort S. Madsen ,  Claudio Mapelli ,  Paul E. Morin ,  Michael C. Myers

IPC: A61K38/22 ,  A61K38/18 ,  C07K1/107 ,  C07K14/64 ,  A61K38/00 ,  A61K45/06 ,  A61K47/64 ,  A61P9/00

CPC classification number: A61K38/18 ,  A61K38/2221 ,  C07K1/1077 ,  C07K14/64 ,  A61K38/00 ,  A61K45/06 ,  A61K47/64 ,  A61P9/00

Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

公开(公告)号：US11364281B2

公开(公告)日：2022-06-21

申请号：US17198939

申请日：2021-03-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Gene M. Dubowchik ,  Olafur S. Gudmundsson ,  Xiaojun Han ,  R. Michael Lawrence ,  Dasa Lipovsek ,  Cort S. Madsen ,  Claudio Mapelli ,  Paul E. Morin ,  Michael C. Myers

IPC: A61K38/22 ,  A61K38/18 ,  C07K14/64 ,  C07K1/107 ,  A61K38/00 ,  A61K47/64 ,  A61P9/00 ,  A61K45/06

Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

公开(公告)号：US11053258B2

公开(公告)日：2021-07-06

申请号：US16463603

申请日：2017-11-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Prasanna Sivaprakasam ,  Gene M. Dubowchik ,  John E. Macor

IPC: C07D498/18 ,  C07D471/22 ,  C07D498/22 ,  A61P25/28 ,  A61P25/16 ,  A61P25/14

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US20190315714A1

公开(公告)日：2019-10-17

申请号：US16463467

申请日：2017-11-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Vijay T. Ahuja ,  Guanglin Luo ,  Ling Chen ,  Prasanna Sivaprakasam ,  Gene M. Dubowchik ,  Swannee E. Jacutin-Porte ,  John E. Macor

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14 ,  A61P25/28

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US09718804B2

公开(公告)日：2017-08-01

申请号：US15033813

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Vivekananda M. Vrudhula ,  Senliang Pan ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D213/02 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D471/04

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

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US20160289210A1

公开(公告)日：2016-10-06

申请号：US15033770

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D513/04 ,  C07D487/08 ,  C07D417/12 ,  C07D417/14 ,  C07D409/14 ,  C07D413/14

CPC classification number: C07D401/12 ,  C07D213/81 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract translation: 本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是NR2B受体的配体，拮抗剂，可用于治疗中枢神经系统的各种疾病。

公开(公告)号：US20160272621A1

公开(公告)日：2016-09-22

申请号：US15033813

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Vivekananda M. Vrudhula ,  Senliang Pan ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  C07D413/14 ,  C07D405/14

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

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US20130053570A1

公开(公告)日：2013-02-28

申请号：US13652690

申请日：2012-10-16

Applicant: Bristol-Myers Squibb Company

Inventor： Guanglin Luo ,  Gene M. Dubowchik ,  John E. Macor

IPC: C07D471/04

CPC classification number: C07D401/12 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20

Abstract: The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).

Abstract translation: 本公开内容通常涉及式I的新化合物，其包括药学上可接受的盐，其为CGRP受体拮抗剂。 本公开还涉及用于治疗CGRP相关疾病（包括偏头痛和其他头痛，神经源性血管舒张，神经源性炎症，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘）的药物组合物和方法， 和慢性阻塞性肺疾病（COPD）。