Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Ravindra N Guthikonda

Frank P DiNinno

Susan M Schmitt

Burton G Christensen

Shrenik K Shah

William K Hagmann

David B Johnston

Philippe L Durette

Ping Liu

Linus S Lin

Linda L Chang

James Patrick Jewell

Thomas J Lanza, Jr

Hongbo Qi

Helen M Armstrong

Malcolm MacCoss

Ronald W Ratcliffe

Lovji D Cama

Charles G Caldwell

Malcolm Maccoss

Kothandaraman Shankaran

Sander G Mills

William F Hoffman

Thomas N Salzmann

Dong-Ming Shen

Jeffrey John Hale

Dooseop Kim

Christopher L Lynch

Kevin Tyler Chapman

Laura C Meurer

Christopher Alan Willoughby

Jennifer L Loebach

Craig K Esser

Kenny Kin Wong

Stephan K Grant

Renee Chabin

Thomas J Lanza

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Substituted amides

Substituted pyridyoxy amides

The present invention is directed to pyrrolidine compounds of the formula I:

Pyrrolidine modulators of chemokine receptor activity

Substituted 2-aminopyridines as inhibitors of nitric oxide synthase

Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase

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.

Cyclic amidine analogs as inhibitors of nitric oxide synthase

Compounds are disclosed represented by the formula: ##STR1## wherein Y is: ##STR2## or a pharmaceutically acceptable salt or ester thereof. ##STR3## represents an aromatic 6 membered ring; zero or one of T, U, V and W represents N.sup.+ R.sup.y and the remainder of T, U, V and W are independently selected from C and N, such that one of T, U, V and W represents N.sup.+ R.sup.y or N. Pharmaceutical compositions and methods of use are also included.

Carbapenem antibiotics, compositions containing such compounds and

Carbapenems of the formula ##STR1## are useful antibacterial agents.

2-(3-pyridyl)-carbapenem antibacterial agents

Cationic-2-heteroarylphenyl-carbapenem antibacterial agents

MRSA active 2-phenyl-carbapenems

Carbapenems of the formula ##STR1## wherein a suitably substituted aza-9-fluorenone is attached at the 2-position of the carbapenem are useful antibacterial agents.

2-(aza-9-fluorenonyl)carbapenem antibacterial agents

Carbapenem compounds of the formula ##STR1## are useful intermediates for preparing antibacterial agents.

Intermediates for preparing cationic-2-heteroaryl-phenyl-carbapenem

Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.

2-phenyl-carbapenems

Carbapenem intermediates of the formula ##STR1## where: M is a removable protecting group for carboxy, and

Intermediates for preparing 2-heteroarylphenyl-carbapenem antibacterial

Growing community of inventors

Edison, NJ, United States of America

Ravindra N Guthikonda