Pfizer Corporation

Christopher A Lipinski

John L LaMattina

John L La Mattina

Spiro-heteroazolones are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro compounds and a method of treating diabetic complications are also disclosed.

Spiro-heteroazalones for treatment of diabetic complications

Hydroxyacetic acid derivatives for the treatment of diabetic

Spiro-succinimides are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro- compounds and a method of treating diabetic complications are also disclosed.

Spiro-succinimides for treatment of diabetes complications

Sprio-imidazolones for treatment of diabetes complications

A series of 2-guanidino-4-heteroarylthiazoles, wherein the heteroaryl substituent is selected from thiazolyl, triazolyl, imidazolyl, and 2-alkyl, 2-amino and 2-carboxamido derivatives thereof, are disclosed. The novel compounds have activity as antisecretory agents and histamine H.sub.2 antagonists and are useful for the treatment of gastric hyperacidity and peptic ulcers. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of gastric hyperacidity and peptic ulcers. Novel intermediates useful in the preparation of the novel antisecretory compounds are also described.

2-guanidino-4-heteroarylthiazoles

Compounds related to 3',4'-dihydrospiro[imidazolidine-4,1'(2'H)-naphthalene]2,3',5-trione, spiro[chroman-4,4'-imidazolidine]2,2',5'-trione and 1',2'-dihydrospiro[imidazolidine-4,4'-(3'H)-quinoline 2,2'5-trione and reduced products thereof as aldose reductase inhibitors.

Spiro-imidazolidines as aldose reductase inhibitors and their

Spiro-oxazolidones, -thiazolidones and -imidazolidones are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro compounds and a method of treating diabetic complications are also disclosed.

Spiro-3-hetero-azolones for treatment of diabetic complications

2-Guanidino-4-heteroarylthiazoles

Haloacetyl imidazoles

Heretofore unavailable 2-guanidino-4-(2-substituted-amino-4-imidazolyl)thiazoles; a novel process therefor, also advantageous for the preparation of known antiulcer 2-guanidino-4-(2-substituted-amino-4-imidazolyl)thiazoles; intermediate compounds therefor; and a method for treatment of ulcers in mammals therewith.

Antiulcer 2-guanidino-4-(2-substituted-amino-4-imidazolyl)thiazoles and

A series of 2-substituted-4-(4-imidazolyl)pyridines and the pharmaceutically acceptable acid addition salts thereof as histamine H.sub.2 -receptor inhibitors for controlling gastric acidity.

Imidazolylpyridine therapeutic agents

A series of novel 3-amino-5-(4-pyridyl)-1,2,4-triazole derivatives has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as anti-ulcer agents. Preferred member compounds include 3-amino-5-[2-(N-monomethylamino)-4-pyridyl]-1,2,4-triazole, 3-amino-5-[2-(N-monoethylamino)-4-pyridyl]-1,2,4-triazole and 3-amino-5-[2-(N,N-dimethylamino)-4-pyridyl]-1,2,4-triazole. Alternate methods of preparation are provided and the principal synthetic routes leading to the preferred compounds are described in some detail.

Pyridylaminotriazole therapeutic agents

5-M-Tolyloxyuracil, in substantially pure form and also in unit dosage form in a pharmaceutically acceptable diluent. Its use in the treatment of peptic ulcer is claimed.

5-M-Tolyloxyuracil, anti-ulcer agent

The preparation of novel 5-(substituted phenoxy)-4-amino and substituted amino pyrimidines is described. These compounds, possessing anti-secretory and anti-ulcer activity, are effective anti-ulcer agents.

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Waterford, CT, United States of America

Christopher A Lipinski