Robert DeVita - Westfield NJ, US Lehua Chang - Ramsey NJ, US MyLe Hoang - Colonia NJ, US JinLong Jiang - Scotch Plains NJ, US Peter Lin - Edison NJ, US Andreas Sailer - Edison NJ, US
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
Robert DeVita - Westfield NJ, US Lehua Chang - Ramsey NJ, US Danny Chaung - Clark NJ, US MyLe Hoang - Colonia NJ, US JinLong Jiang - Scotch Plains NJ, US Peter Lin - Edison NJ, US Andreas Sailer - Edison NJ, US Jonathan Young - Kendall Park NJ, US
International Classification:
A61K031/541 A61K031/5377 A61K031/496 A61K031/4709 C07D417/02 C07D413/02 C 07D 4 3/02
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
Timothy A. Blizzard - Princeton NJ, US Carolyn A. Buser-Doepner - Harleysville PA, US Douglas E. Frantz - Downingtown NJ, US Kelly Hamilton - North Wales PA, US Myle Hoang - Colonia NJ, US Ling Lee - Lansdale PA, US Christopher R. Moyes - Hertfordshire, GB Jerry A. Murry - New York NY, US Arash Soheili - Iselin NJ, US
The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.