David Barnes - Waban MA, US Gregory Raymond Bebernitz - Stow MA, US Scott Louis Cohen - Peabody MA, US Robert Edson Damon - Hopkinton MA, US Robert Francis Day - Watertown MA, US Monish Jain - Belmont MA, US Rajeshri Ganesh Karki - Somerville MA, US Louise Clare Kirman - Swampscott MA, US Tajesh Jayprakash Patel - Medford MA, US Brian Kenneth Raymer - Holliston MA, US Herbert Franz Schuster - Ashland MA, US Wei Zhang - Somerville MA, US
Assignee:
Novartis AG - Basel
International Classification:
A01N 37/18 A61K 31/16 C07C 327/48
US Classification:
514599, 564 74
Abstract:
The present invention provides a compound of formula I;.
1,1,3-Trioxo-1,2,5-Thiadiazolidines And Their Use As Ptp-Ases Inhibitors
David Barnes - Waban MA, US Gary Mark Coppola - Budd Lake NJ, US Robert Edson Damon - Hopkinton MA, US Katsumasa Nakajima - Winchester MA, US Brian Christopher Raudenbush - Beacon Falls CT, US Travis Stams - Stow MA, US Sidney Wolf Topiol - Fair Lawn NJ, US Thalaththani Ralalage Vedananda - Shrewsbury MA, US
Compounds of the formulaare inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
Compounds of the formulaprovide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
Bicyclic Acetyl-Coa Carboxylase Inhibitors And Uses Thereof
David Weninger BARNES - Cambridge MA, US Gregory Raymond BEBERNITZ - Cambridge MA, US Kevin CLAIRMONT - Cambridge MA, US Scott Louis COHEN - Cambridge MA, US Robert Edson DAMON - Cambridge MA, US Robert Francis DAY - Cambridge MA, US Stephanie Kay DODD - Cambridge MA, US Christoph GAUL - Basel, CH Hatice Belgin GULGEZE EFTHYMIOU - Cambridge MA, US Monish JAIN - Cambridge MA, US Rajeshri Ganesh KARKI - Cambridge MA, US Louise Clare KIRMAN - Cambridge MA, US Kai LIN - Cambridge MA, US Justin Yik Ching MAO - Cambridge MA, US Tajesh Jayprakash PATEL - Cambridge MA, US Brian Kenneth RAYMER - Cambridge MA, US Liansheng SU - Cambridge MA, US
The present invention provides compounds of formula (I);or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
Rob Damon (1983-1984), Caleb Howard (1978-1980), Sarah Holtrust (1993-2002), Wendy Kearley (1982-1984), Laura Wills (1987-1989), Catherine Rogers (1983-1985)
With the bankruptcy filing, Helios and Matheson board members Prathap Singh, Gavriel Ralbag, Muralikrishna Gadiyaram and Joseph Fried resigned. In addition, interim CEO Parthasarathy Krishnan, interim CFO Robert Damon resigned.