Nobuyoshi Yasuda - Mountainside NJ Michael Palucki - Hillsborough NJ Yi Xiao - Fanwood NJ Frederick W. Hartner - Somerville NJ Lushi Tan - Edison NJ
Assignee:
Merck Co., Inc. - Rahway NJ
International Classification:
C07D21353
US Classification:
546329, 546334, 546335
Abstract:
A novel process is provided for the preparation of optionally protected 2,5-di-(3รข-aminopropyl)-pyridines which are useful in the synthesis of v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
Process For Making Fluorinated 4-Azasteroid Derivatives
Lushi Tan - Edison NJ, US Benjamin T. Dorner - Hoboken NJ, US Wenjie Li - Edison NJ, US Nobuyoshi Yasuda - Mountainside NJ, US Frederick W. Hartner - Somerville NJ, US
Assignee:
Merck & Co., Inc - Rahway NJ
International Classification:
C07D 221/18
US Classification:
546 77
Abstract:
The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
Lushi Tan - Edison NJ, US James Christopher McWilliams - Hoboken NJ, US Frederick W. Hartner - Somerville NJ, US Naoki Yoshikawa - Edison NJ, US Wenji Li - Edison NJ, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
C07D 231/10 C07D 231/12
US Classification:
5483761, 5483771
Abstract:
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
Processes For Preparing Bicyclo [3.1.0] Hexane Derivatives, And Intermediates Thereto
Frederick W. Hartner - Rahway NJ, US Lushi Tan - Rahway NJ, US Nobuyoshi Yasuda - Rahway NJ, US Naoki Yoshikawa - Rahway NJ, US
Assignee:
Taisho Pharmaceutical Co., Ltd - Tokyo
International Classification:
C07D 319/303 C07C 61/00 C07C 69/74
US Classification:
549336, 549546, 562400, 562457, 560116, 5601191
Abstract:
Processes for the preparation of certain [3. 1. 0]hexane derivatives which are useful as mGluR agonists, and intermediates prepared during such processes.
Process For Synthesizing 2-Phenyl-1H-Phenanthro[9,10-D]Imidazole Derivative
Kevin Michael Belyk - Somerset NJ, US Benjamin Dorner - Hoboken NJ, US Frederick Hartner - Branchburg NJ, US Naoki Yoshikawa - Edison NJ, US John Limanto - New Brunswick NJ, US Lushi Tan - Edison NJ, US Enrique Vazquez - South Plainfield NJ, US Joseph Payack - Newbury Park CA, US
International Classification:
C07D 235/02
US Classification:
5483017
Abstract:
The present invention describes an efficient and economical process for the preparation of a 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative that is useful for the large scale production of material for preclinical and clinical use. The process of the present invention represents a convergent approach to generate the 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative in high overall yield. The compound made by the process of the invention is an inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and is therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain.
Process For Solubilizing Polyanoinic Bacterial Polysaccharides In Aprotic Solvents
Ralph Calabria - East Brunswick NJ Frederick W. Hartner - Somerville NJ John T. Sisko - Lansdale PA
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07H 100 C07G 1700 C08B 3700 A61K 3100
US Classification:
514 54
Abstract:
A process for rendering a bacterial polysaccharide soluble in aprotic solvents by exchanging the calcium counterion of a polysaccharide calcium salt for tetra-n-alkylammonium ion by precipitation.
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