Substituted tetrahydroisoquinolines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S146000

Reexamination Certificate

active

10715662

ABSTRACT:
The invention is directed to physiologically active compounds of formula (I):wherein:R1represents optionally substituted aryl, optionally substituted heteroaryl, R3NH—Ar1—L2— or R3—NH—C(═O)—NH—Ar2—L2—; R3represents aryl or heteroaryl; Ar1represents 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; Ar2represents aryldiyl or heteroaryldiyl; L1represents a linkage, such as an alkylene linkage; L2represents an alkylene chain linkage; R2represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; 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 (α4β1).

REFERENCES:
patent: 5236934 (1993-08-01), VanAtten
patent: 6608084 (2003-08-01), Bourzat et al.
Boger, et al., Inverse Electron Demand Diels-Alder reactions of 3-Carbomethoxy-2-pyrones. Controlled Introduction of oxygenated Aromatics: Benzene, Phenol, Catechol, Resorcinol, and Pyrogallol Annulation. Regiospecific Total Synthesis of Sendaverine and a Preparation of 6,7-Benzomorphans., J. Org. Chem.; vol. 49; No. 21; 1984; pp. 4033-4044.

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