Alcon Laboratories, Inc.

Alcon, Inc.

Alcon Universal Ltd.

Alcon Manufacturing, Ltd.

Raymond E Conrow

Abbot F Clark

William D Dean

Peter G Klimko

Pete Delgado

Paul W Zinke

Michael S Gaines

Michael E Deason

Anura P Dantanarayana

Steven J Sproull

Mark R Hellberg

John Russell Falck

John M Yanni

Daniel A Gamache

Robert D Selliah

Haresh G Bhagat

L Wayne Schneider

Mark T Dupriest

David R Pierce

Daniel Kuzmich

W Dennis Dean

Terri Pasquine

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

Hydroxyeicosatetraenoic acid esters and methods of their use in treating dry eye disorders are disclosed.

Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders

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

Compounds for use in 11-oxa prostaglandin synthesis

Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders are disclosed.

Methods of synthesizing 9-Halo-13,14-dihydroprostaglandins useful in the treatment of glaucoma and ocular hypertension are disclosed. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.

Method of prostaglandin synthesis

Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.

Heteroatom-interrupted analogs of 15-hydroxyeicosatetraenoic acid and methods of use

Processes and novel intermediates for 11-oxa prostaglandin synthesis

HETE salts, the preparation of HETE salts, the preparation of stable and efficacious HETE compositions, HETE compositions and methods of use for treating dry eye are disclosed.

Hydroxyeicosatetraenoate salts, compositions and methods of use in treating dry eye disorders

The present invention is directed to novel methods of prostanoid synthesis. Specifically, the invention is directed to the addition of alpha chains to prostanoids using cis-alkenylstannane intermediates.

Stannane synthesis of prostanoids

Compositions of non-steroidal glucocorticoid antagonists for treating glaucoma or ocular hypertension and methods for their use are disclosed.

Growing community of inventors

Crowley, TX, United States of America

Raymond E Conrow