Merck + Co., Inc.

Arsenio A Pessolano

Philippe L Durette

Tsung-Ying Shen

Robert L Clark

Kathleen M Rupprecht

Robert K Baker

Bruce E Witzel

Ihor E Kopka

Thomas J Lanza, Jr

David A Boulton

Vernon L Moore

Joshua S Boger

Janos Kollonitsch

Francis J Dumont

Nolan H Sigal

New immunosuppressive cyclosporin analogs are disclosed having one or more fluorinated amino acids. These analogs may also have a 'C-9 amino acid' wherein the double bond is replaced by a heteroatom such as sulfur or oxygen.

Immunosuppressive fluorinated cyclosporin analogs

3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.

Derivatives of 3-hydroxyazabenzo(beta)thiophene useful as 5-lipoxygenase

Novel cyclosporin analogs containing a MeAla or MeAbu residue at the 6-position of the cyclic undecapeptide have been synthesized and found unexpectedly to exhibit antagonistic activity toward cyclosporin A binding to its cytosolic protein receptor, cyclophilin, without being immunosuppressive.

Novel 6-position cyclosporin analogs as non-immunosuppressive

3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthioalkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory disease and other leukotriene mediated diseases.

Derivatives of 3-hydroxyazabenzo[b]thiophene useful as 5-lipoxygenase

Derivatives of 3-hydroxyazabenzo(B)thiophene useful as 5-lipoxygenase

2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.

2-benzyl-4-(4-pyridyl)thiazoles and derivatives thereof as

Morpholino pyridyl thiazole compound

1,3-Dihydroimidazo[4,5-b]pyridin-2-ones and corresponding thiones have utility as analgesic, antipyretic and antiinflammatory agents. They are generally prepared by treatment of a 2,3-diaminopyridine with phosgene or thiosphosgene followed by further substitution if desired.

Imidazo pyridine-2-ones and pharmaceutical compositions and methods of

The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.

Anti-inflammatory oxazolo [5,4-b]pyridines

Anti-inflammatory oxazole[4,5-b]pyridines

3H-1,2,3-Triazolo[4,5-b]pyridines substituted in the 3-position have utility as analgesic, anti-inflammatory and anti-pyretic agents. They are prepared by diazotization of a 3-amino-2-(substitute) aminopyridine.

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Arsenio A Pessolano