Allergan, Inc.

Kwok-Yin Tsang

Liming Wang

Xiaoxia Liu

Jayasree Vasudevan

Roshantha A Chandraratna

Yang-Dar Yuan

Richard L Beard

Ling Li

Janet A Takeuchi

Rong Yang

Smita S Bhat

Thong Huy Vu

Roshantha S Chandraratna

The invention provides methods for treating an individual having a retinoid responsive disorder. In one embodiment, a method involves administering to the individual an effective amount of a selective CYP26B inhibitor, the selective CYP26B inhibitor having at least 10-fold selectivity for CYP26B relative to CYP26A. In another embodiment, a method involves administering to the individual an effective amount of a selective CYP26A inhibitor, the selective CYP26A inhibitor having a chemical formula set forth in the specification. The invention further provides screening methods for identifying a selective CYP26A inhibitor or selective CYP26B inhibitor.

Methods for treating retinoid responsive disorders using selective inhibitors of CYP26A and CYP26B

Compounds of the formula where the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.

4-[(8-substituted)-6-chromanoyl]-and 4-[8-substituted)-chroman-6-YL-ethynyl]-benzoic and phenylacetic acids, their esters and salts having cytochrome P450RAI inhibitory activity

4-&lsqb;(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL&rsqb;-BENZOIC AND 2-&lsqb;4-&lsqb;(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL&rsqb;-PHENYL&rsqb;-ACETIC ACID, THEIR ESTERS AND SALTS HAVING CYTOCHROME P450RAI INHIBITORY ACTIVITY

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Irvine, CA, United States of America

Kwok-Yin Tsang