Merrell Dow Pharmaceuticals

The Dow Chemical Company

Aventis Pharma Limited

Shyam Sunder

Norton P Peet

Gary A Flynn

Robert J Cregge

Thomas L Fevig

Patrick W Shum

Anna P Vinogradoff

John K Daniel

The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.

Aminoacetylmercapto derivatives useful as inhibitors of enkephalinase

This invention is directed to a group of compounds which are acyl derivatives of amino substituted triazolopyridazines. They are prepared by the reaction of an aminotriazolopyridazine or an aminotriazolophthalazine with an appropriate acid chloride. These compounds possess bronchodilating and antiallergenic activity.

Substituted triazolopyridazines, pharmaceutical compositions and use

The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.

Substituted imidazo(2,1-b)quinazolin-5(3H)-ones and related tricyclic

3-(1H-Tetrazol-5-yl)thieno[2,3-d]pyrimidin-4(3H)-ones useful as antiallergic agents are described herein. The compounds are prepared by cyclization of an appropriate substituted amidine using an alkali metal base. The reaction is carried out in an appropriate inert solvent.

3-(1H-tetrazol-5-yl)thieno[2,3-d]pyrimidin-4(3H)-ones

2-(Formylamino)-N-(1H-tetrazol-5-yl)benzamide and its pharmaceutically acceptable salts are useful as antiallergic agents. The compounds are prepared by the reaction of 2-amino-N-(1H-tetrazol-5-yl)benzamide with formic acetic anhydride.

2-(Formylamino)-N-(1H-tetrazol-5-yl)benzamide and use as anti-allergics

3,6,7,8-Substituted-s-triazolo-pyridazine compounds such as 7,8-dimethyl-6-morpholino-3-methyl-s-triazolo[4,3-b]pyridazine or 7,8-dimethyl-6-(1-pyrrolidinyl)-3-(isopropyl)-s-triazolo-[4,3-b]pyridazine are prepared by the reaction of a carboxylic acid with a substituted 3-hydrazino-6-halo-pyridazine followed by the reaction of the resulting 6-halotriazolopyridazine with a corresponding base. The compounds have pharmacological activity as bronchodilators.

3,6,7,8-Substituted-s-triazolo[4,3-b]pyridazines as bronchodilators

Alkoxycarbonyl and oxalyl derivatives of amino-N-(1H-tetrazol-5-yl)benzamides are described herein. The compounds involved are useful as antiallergic agents. These compounds can be prepared by the reaction of an amino-N-(1H-tetrazol-5-yl)benzamide with an appropriate acid chloride.

Carbamates and oxalamides of amino-N-(1H-tetrazol-5-yl)benzamides

Substituted tetrahydrotetrazolo[5,1-a]phthalazine compounds such as 6-methylamino-7,8,9,10-tetrahydrotetrazolo[5,1-a]phthalazine are prepared by reacting a 6-halo-7,8,9,10-tetrahydrotetrazolo[5,1-a]phthalazine with an appropriate amine. The compounds are useful as bronchodilators.

Substituted tetrahydrotetrazolo[5,1-a]phthalazines

3-(1H-tetrazol-5-yl)-4(3H)-quinazolinones useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate 2-amino-N-(1H-tetrazol-5-yl)benzamide with an appropriate ortho ester.

3-(1H-Tetrazol-5-yl)-4(3H)-quinazolinones

A series of 2-chloro-3-phenoxypyrazines and 2-chloro-6-phenoxypyrazines exhibiting antiviral activity are disclosed. Methods of using the disclosed compounds as antiviral agents are also described as well as pharmaceutically-acceptable compositions.

2-Chloro-3-phenoxypyrazines and 2-chloro-6-phenoxypyrazines possessing

Novel N-(2-hydroxyethyl)cycloalkylaminocarboxamides are described. The compounds are pharmacodynamically active and serve as intermediates for the preparation of corresponding 2-amino-2-oxazolines which are active pharmacodynamically.

Substituted N-(2-hydroxyethyl)morpholino carboxamides

Novel 2-cycloalkylamino-2-oxazolines and their salts are described which are biologically active. Member compounds exhibit useful activity as CNS-depressants, CNS-stimulants, platelet aggregation inhibitors, fungicides, and herbicides.

2-Cycloalkyl-amino-2-oxazolines

Novel N-(2-hydroxyethyl)heteroiminocarboxamides are described. The compounds are pharmacodynamically active and serve as intermediates for the preparation of corresponding 2-amino-2-oxazolines which are active pharmacodynamically.

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Indianapolis, IN, United States of America

Shyam Sunder