Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Napp Technologies

Ranjit C Desai

Soumya P Sahoo

Hiroo Koyama

Jeffrey P Bergman

Victoria K Lombardo

Julia K Boueres

Richard L Tolman

Lihu Yang

Conrad Santini

Daniel J Miller

Wei Han

Dominick F Gratale

Edward J Metzger

Mohammad Aslam

Daniel A Aguilar

Nicholas Gallegos

Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.

Efficient production of heterologous proteins using mannosyl transferase inhibitors

Efficient production of heterologous proteins using  mannosyl transferase inhibitors

A class of chromane and chromene compounds having the structure shown below and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment and control of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, such as atherosclerosis 

PPAR alpha selective compounds for the treatment of dyslipidemia and other lipid disorders

A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders

Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.

Arylthiazolidinedione derivatives

Arylthiazolidinedione and aryloxazolidinedione derivatives

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.

Arylthiazolidinedione derivitives

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.

A novel process is disclosed for the preparation of dihydropyridine compounds and derivatives thereof, and more particularly felodipine. The process to prepare felodipine involves a two step procedure condensing 2,3-dichlorobenzaldehyde with methyl acetoacetate in the presence of a catalyst system. The resultant benzylidine intermediate is sequentially reacted with ethyl aminocrotonate to provide felodipine. The novelty of the present invention resides in part on (1) a new catalyst system not previously disclosed for the preparation of felodipine, (2) the absence of acid(s), (3) the control of reaction conditions to yield lower amounts of unreacted aldehyde compared to known reactions, (4) a simplified purification process, and (5) formation of negligible quantities of symmetrical diester byproducts.

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Franklin Park, NJ, United States of America

Ranjit C Desai