Ortho-mcneil Pharmaceutical Corp.

Ortho Pharmaceutical Corporation

Johnson & Johnson Consumer Companies, Inc.

Louis J Fitzpatrick

Kevin Pan

Allen B Reitz

Carlos Plata-Salaman

Boyu Zhao

Magdalena G Eisinger

Virginia L Smith-Swintosky

Daniel H Lee

Pauline J Sanfilippo

Malcolm K Scott

Richard Cordova

Joseph Meschino

Mark J Macielag

John R Carson

Steven J Coats

Dennis J Hlasta

Richard J Carmosin

Michele C Jetter

Stephen S Palmer

Alfonzo D Jordan

Ralph A Rivero

Carolina L Lanter

Ke Pan

The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

1,2,4-thiadiazolium derivatives as melanocortin receptor modulators

The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

1,2,4-thiadiazole derivatives as melanocortin receptor modulators

This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 

Anti-inflammatory compounds

The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Substituted aminoalkylamide derivatives as antagonists of follicle stimulating hormone

This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

4-&lsqb;aryl(piperidin-4-yl)&rsqb;aminobenzamides are delta-opioid receptor agonists/antagonists. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases.

4-&lsqb;aryl(piperidin-4-yl)&rsqb;aminobenzamides

A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.

5-�(heteroaryl)alkyl!-3-oxo-pyrido�1,2-a!benzimidazole-4-carboxamide

Growing community of inventors

Souderton, PA, United States of America

Louis J Fitzpatrick