Stephan K Grant

US Patent:

6514709, Feb 4, 2003

Filed:

Mar 13, 2001

Appl. No.:

09/805285

Inventors:

Stephan K. Grant - East Windsor NJ
Gregory J. Kaczorowski - Edison NJ
Richard E. Middleton - Gillette NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

G01N 3353

US Classification:

435 71, 435 6, 435 4

Abstract:

The present invention provides assays in which intracellular chelators are used to alter the kinetics of signal generation triggered by divalent cations, particularly calcium influx into the cell. The use of an intracellular chelator in the assay can delay and prolong the signal, allowing the signal to be detected by automated instrumentation without the need for simultaneous liquid handling at the time of detection.

US Patent:

56293224, May 13, 1997

Filed:

Jun 6, 1995

Appl. No.:

8/468120

Inventors:

Ravindra N. Guthikonda - Edison NJ
Stephan K. Grant - Robbinsville NJ
Malcolm Maccoss - Freehold NJ
Shrenik K. Shah - Metuchen NJ
Kothandaraman Shankaran - Kendall Park NJ
Charles G. Caldwell - Scotch Plains NJ
Philippe L. Durette - New Providence NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3147
C07D21538

US Classification:

514313

Abstract:

Disclosed herein are compounds of Formula I ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula I are also usful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, mulitple sclerosis, Korsakoff's disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.