Patent ID: 8101770
Filing Date: 2012-01-24
Classification: A61P,C07D

Abstract:
1. A compound of formula I: or a pharmaceutically accepted salt thereof, wherein each R 3 and R 4 is H R 2 is a pyridine ring; R 2 is optionally substituted with J R ; each X 1 and X 2 is independently —C(O)— or NR—, wherein one of X 1 or X 2 is —NR— and the other of X 1 or X 2 is —C(O)—; R is H, unsubstituted C 1-6 aliphatic; R 1 is -T-Q; T is a bond or C 1-3 aliphatic, wherein up to one methylene unit of the chain is optionally and independently replaced by G or G′ wherein G is —NR 5 —, —O—, or —S—; G′ is cyclopropyl, C≡C, or C═C; and T is optionally substituted with OH, C 1-6 aliphatic, or phenyl; each J Q is selected from halogen, C 1-6 alkyl, CN, C 1-4 -haloalkyl, —OR o , —N(R o ) 2 , SCHF 2 , unsubstituted phenyl, benzyl, a 5-7 membered heterocyclyl having 1-2 heteroatoms selected from oxygen or nitrogen, the 5-7 membered heterocyclyl is optionally substituted with pyrrolidinyl or with a C 1-6 alkyl wherein up to three methylene units of the C 1-6 alkyl are optionally and independently replaced by, —NR o —, —O—, or —S—; C 3-6 cycloaliphatic, C 1-6 alkyl-(5-6 membered heterocyclyl having 1-2 heteroatoms selected from oxygen or nitrogen), 5-6 membered heteroaryl having 1-2 nitrogen atoms, CO(phenyl), —SO 2 R o , —SO 2 N(R o ) 2 , or C 1-6 alkyl wherein up to three methylene units are optionally and independently replaced by, —NR o —, —O—, —S—, SO 2 —, or —CO—, in a chemically stable arrangement; each J Q is optionally and independently substituted with R o ; Q is a phenyl ring; Q is optionally substituted with J Q ; R 5 is optionally substituted R, C 6-10 aryl, C 3-10 cycloaliphatic, 5-14 membered heteroaryl, or 5-14 membered heterocyclyl; or two R 5 groups, together with the atom(s) to which they are attached, form an optionally substituted 3-7 membered monocyclic or 8-14 membered bicyclic ring; J R is CN, oxo, halo, 5-8 membered heterocyclyl having 1-2 heteroatoms selected from oxygen or nitrogen, —NR(C 1-4 alkyl)OR o , —NH(5-6 membered heterocyclyl having 1-2 nitrogen atoms), —(C 1-6 alkyl)-OR o , or a C 1-6 alkyl chain wherein up to three methylene units of the chain are independently replaced by, —NR o —, —O—, or —CO— in a chemically stable arrangement; each J R is independently and optionally substituted with R o ; each R o is independently selected from hydrogen, CO 2 (C 1-4 aliphatic)haloC 1-4 aliphatic, optionally substituted C 1-6 aliphatic wherein up to 2 methylene units are optionally replaced by O, N, or S, 5-6 membered heterocyclyl optionally substituted with C 1-3 alkyl; unsubstituted phenyl, unsubstituted —CH 2 (Ph), unsubstituted —CH 2 (5-7 membered heterocyclyl); or, notwithstanding the definition above, two independent occurrences of R o , on the same substituent, taken together with the atom to which each R o group is bound, form an optionally substituted 3-6 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; optional substituents on the aliphatic group of R o or on the ring formed by 2 R o groups are selected from NH 2 , NH(C 1-4 aliphatic), N(C 1-4 aliphatic) 2 , halogen, C 1-4 aliphatic, OH, O(C 1-4 aliphatic), NO 2 , CN, CO 2 H, CO 2 (C 1-4 aliphatic), O(haloC 1-4 aliphatic), and haloC 1-4 aliphatic, wherein each of the foregoing C 1-4 aliphatic groups of R o is unsubstituted; provided that when R 2 is 4-pyridyl, R 3 and R 4 are H, X 1 is —NR—, R is H, and X 2 is —C(O)—, then when T is —CH 2 —, Q is not 3-OH-phenyl, 4-OH-phenyl, 3-NO 2 -phenyl.