BMS-317180(BMS-317180) - 药物靶点：GHSR_在研适应症：恶病质_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

GHSR

作用机制

GHSR激动剂(促生长激素释放激素受体激动剂)

治疗领域

其他疾病

在研适应症

恶病质

非在研适应症-

原研机构

Bristol-Myers Squibb Pharma Research Labs LLC

在研机构

Bristol-Myers Squibb Pharma Research Labs LLC

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C21H33N7O5

InChIKeyKJXOYJXMFGXDRR-QGZVFWFLSA-N

CAS号295337-71-2

关联

100 项与 BMS-317180 相关的临床结果

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100 项与 BMS-317180 相关的转化医学

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100 项与 BMS-317180 相关的专利（医药）

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2

项与 BMS-317180 相关的文献（医药）

2009-06-05·The Journal of Organic Chemistry2区 · 化学

Process Research and Development for a Tetrazole-Based Growth Hormone Secretagogue (GHS) Pharmaceutical Development Candidate

2区 · 化学

Article

作者: Davulcu, Akin H. ; Katipally, Kishta ; Parsons, Rodney L. ; Littke, Adam ; Xu, Zhongmin ; Doubleday, Wendel ; Lai, Chiajen J. ; Li, Jun ; Gleeson, Margaret ; Schwinden, Mark ; McLeod, Douglas D. ; McConlogue, Cary W.

BMS-317180 (1) is a potent, orally active agonist of the human growth hormone secretagogue (GHS) receptor. This manuscript details the process research and development efforts that enabled the synthesis of the phosphate salt of 1 on a multi-kilogram scale. Key considerations in the development of this process focused on safe execution and the requirement for telescoped synthetic transformations (i.e., without isolation of intermediate products) to contend with a lack of suitably crystalline products.

2008-03-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Design and synthesis of tetrazole-based growth hormone secretagogue: The SAR studies of the O-benzyl serine side chain

4区 · 医学

Article

作者: Mujing Yan ; Blake Beehler ; Brian J. Murphy ; Shiwei Tao ; Ramakrishna Seethala ; David Gordon ; Paul Sleph ; Steve Swartz ; Jeffrey A. Robl ; James J. Li ; Kenneth E. Dickinson ; Andres A. Hernandez ; Dorothy Slusarchyk ; Gary Grover ; Joseph A. Tino ; Hongjian Zhang ; Leah Giupponi ; William G. Humphreys ; Christa Musial ; William R. Ewing ; Haixia Wang ; Jun Li ; Neil Flynn ; Stephanie Y. Chen

The structure-activity relationship of the O-benzyl serine side chain was investigated based on the tetrazole-based growth hormone secretagogue BMS-317180 (2). The ortho position of the benzyl moiety was found to be favorable for introduction of substituents. A series of ortho-substituted compounds were synthesized with improved in-vitro and in-vivo activity. Among them, the biphenyl compound 2p shows twofold improvement in potency compared to its parent compound BMS-317180 (2).

100 项与 BMS-317180 相关的药物交易

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