PDE IV inhibitors: "bis-compounds"

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United States of America Patent

PATENT NO 5744473
SERIAL NO

08714581

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Abstract

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Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. Also provided is a process of making compounds of Formula I. Compounds of the present invention are represented by Formula I: ##STR1## its pharmaceutically acceptable salts, hydrochloride salts, or prodrug forms thereof, wherein: X.sub.1a, X.sub.1b are independently selected from --NH and --N-lower alkyl; X.sub.2a, X.sub.2b are optionally present and are independently selected from S(O)n, O, CH.sub.2, and NH; P.sub.1a, P.sub.1b, P.sub.2a, P.sub.2b, P.sub.4a, and P.sub.4b are independently selected from N, or CH; R.sub.1a, R.sub.1b, R.sub.2a, R.sub.2b, R.sub.3a and R.sub.3b are independently selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 branched alkyl, C.sub.3 -C.sub.6 cycloalkyl, said alkyl groups being optionally substituted with halogen, aryl or heteroaryl group(s), said aryl and heteroaryl group(s) being optionally substituted with hydroxy, alkoxy, cycloalkoxy, halogen, alkyl, or cycloalkyl; and n is an integer from 0 to 2.

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Patent Owner(s)

Patent OwnerAddress
EURO-CELTIQUE S A2350 LUXEMBOURG

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cavalla, David Cambridge, GB 28 74
Chasin, Mark Manalapan, NJ 116 12920
Hofer, Peter Liestal, CH 56 1088

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