	US 7,501,411 B2
	Triazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Martin James Inglis Andrews, Mechelen (Belgium); Paul Edwards, Laval (Canada); Mark Stuart Chambers, Saffron Walden (United Kingdom); Wolfgang Schmidt, Saffron Walden (United Kingdom); Juha Andrew Clase, Mechelen (Belgium); Gregory Bar, Mechelen (Belgium); Kim Louise Hirst, Saffron Walden (United Kingdom); and Angus MacLeod, Saffron Walden (United Kingdom)
Assigned to Galapagos, NV, Mechelen (Belgium)
Filed on May 30, 2007, as Appl. No. 11/809,294.
Claims priority of provisional application 60/932100, filed on May 29, 2007.
Claims priority of provisional application 60/931763, filed on May 25, 2007.
Claims priority of provisional application 60/931844, filed on May 25, 2007.
Claims priority of provisional application 60/931764, filed on May 25, 2007.
Claims priority of provisional application 60/803552, filed on May 31, 2006.
Prior Publication US 2008/0090818 A1, Apr. 17, 2008
Int. Cl. C07D 487/04 (2006.01); A61K 31/4985 (2006.01)

U.S. Cl. 514—233.2 [514/249; 544/118; 544/350]

54 Claims

1. A compound according to formula III:

wherein

R¹is H, or substituted or unsubstituted alkyl;

R⁸is

L is selected from a single bond, alkylene, —O—, —N(R^8e)—, —CO—, —CO₂—, —SO—, —SO₂—, —CON(R^8e)—, —SO₂N(R^8e)—, —N(R^8e)CO—, —N(R^8e)SO₂—, —N(R^8e)CO N(R^8e)—, —N(R^8e)SO₂N(R^8e)—; —O(CR^8e₂)_m1—, or —CON(R^8e)(CR^8e₂)_m1—;

each R^8ais independently selected from hydrogen, substituted or unsubstituted alkyl, alkoxy, cyano, and halo;

R^8dis selected from substituted or unsubstituted heterocycloalkyl;

R^8eis selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted cycloalkyl;

the subscript m1 is 1, 2, 3, or 4; the subscript n is 1, 2, 3, or 4;

and R⁹is independently selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; or a pharmaceutically acceptable salt thereof; and stereoisomers and tautomers thereof.