Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
Type:
Grant
Filed:
February 21, 2014
Date of Patent:
January 19, 2016
Assignee:
Merck Sharp & Dohme Corporation
Inventors:
Seoju Lee, David C. Wylie, Susan Cannon-Carlson
Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
May 6, 2014
Assignee:
Merck Sharp & Dohme Corporation
Inventors:
Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
Type:
Grant
Filed:
August 26, 2011
Date of Patent:
April 15, 2014
Assignee:
Merck Sharp & Dohme Corporation
Inventors:
Seoju Lee, David C. Wylie, Susan Cannon-Carlson
Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.
Type:
Application
Filed:
September 27, 2010
Publication date:
August 9, 2012
Applicant:
Merck Sharp & Dohme Corporation
Inventors:
Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki