Substituted tetrahydroisoquinolines

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United States of America Patent

PATENT NO 7211586
APP PUB NO 20040122047A1
SERIAL NO

10715662

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention is directed to physiologically active compounds of formula (I): ##STR00001## wherein: R.sup.1 represents optionally substituted aryl, optionally substituted heteroaryl, R.sup.3NH--Ar.sup.1--L.sup.2--or R.sup.3--NH--C(.dbd.O)--NH--Ar.sup.2--L.sup.2--; R.sup.3 represents aryl or heteroaryl; Ar.sup.1 represents a saturated, partially saturated or fully unsaturated 8- to 10-membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Ar.sup.2 represents aryldiyl or heteroaryldiyl; L.sup.1 represents a linkage, such as an alkylene linkage; L.sup.2 represents an alkylene chain linkage; R.sup.2 represents hydrogen, halogen, C.sub.1-4alkyl or C.sub.1-4alkoxy; and Y is carboxy or an acid bioisostere; but excluding compounds where an oxygen, nitrogen or sulfur atom is attached directly to a carbon carbon multiple bond of an alkenylene or alkynylene residue; and the corresponding N-oxides and ester prodrugs thereof, and the pharmaceutically acceptable salts and solvates of such compounds, and the N-oxides and ester prodrugs thereof.Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (.alpha.4.beta.1).

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Patent Owner(s)

Patent OwnerAddress
AVENTIS PHARMA LIMITEDWEST MALLING KENT ME19 4AH

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Fenton, Garry Brentwood, GB 36 326
Harris, Neil Victor Tilbury, GB 24 273

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