Alcon, Inc.

Alcon Laboratories, Inc.

Other

Pete Delgado

Raymond E Conrow

William D Dean

Michael S Gaines

Mark R Hellberg

Jon C Nixon

David R Pierce

W Dennis Dean

Methods of making 1-alkylindazoles are described. The methods involve reacting a 2-alkylaminobenzonitrile with a nitrosating agent followed by reduction-cyclization of the resulting nitrosamine to form a 1-alkyl-3-aminoindazole. The 1-alkyl-3-aminoindazole can be deaminated to form a 1-alkylindazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.

1-alkyl-3-aminoindazoles

Methods of making indazoles are described. The methods involved reacting an aromatic aldehyde with a nitrogen source to form a nitroso aromatic aldehyde. The nitroso aromatic aldehyde is reacted with a reducing agent to form an indazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.

Methods of making indazoles

Novel processes useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Process for use in 11-oxa prostaglandin synthesis

Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Compounds for use in 11-oxa prostaglandin synthesis

Processes and novel intermediates for 11-oxa prostaglandin synthesis

Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.

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Fort Worth, TX, United States of America

Pete Delgado