Anti-inflammatory piperazinyl-benzyl-tetrazole derivatives and intermediates thereof

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United States of America Patent

PATENT NO 6514975
SERIAL NO

09367322

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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This invention relates to tetrazoles and their pharmaceutically acceptable salts which are selective agonists for the delta opioid receptor, particularly useful in the treatment of inflammatory diseases such as arthritis, psoriasis, asthma, inflammatory bowel disease, disorders or respiratory function, gastrointestinal disorders such as functional bowel disease and functional GI disorders, of formula (I) ##STR1## wherein R.sup.1 is H, C.sub.2 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, (C.sub.3 -C.sub.7 cycloalkyl)-(C.sub.1 -C.sub.4 alkyl), (C.sub.1 -C.sub.4 alkoxy)-(C.sub.1 -C.sub.4 alkyl), carboxy-(C.sub.1 -C.sub.4 alkyl), aryl-(C.sub.1 -C.sub.4 alkyl) or heteroaryl-(C.sub.1 -C.sub.4 alkyl); R.sup.2 and R.sup.3 are each independently H or C.sub.1 -C.sub.4 alkyl; R.sub.4 is selected from (i) H, (ii) a group of the formula R.sup.6 --(CH.sub.2).sub.m --Z--(CH.sub.2).sub.n --, where m is 0, 1, 2 or 3, n is 1, 2 or 3, Z is a direct link or O, and R.sup.6 is --CO.sub.2 H or --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), and (iii) a group of formula (a) ##STR2## where R.sup.7 is H or C.sub.1 -C.sub.4 alkyl; and R.sup.5 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl); with the proviso that when Z is O, m is 1, 2 or 3 and n is 2 or 3.

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Patent Owner(s)

  • PFIZER INC.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Maw, Graham N Sandwich, GB 2 12

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