	US 7,465,726 B2
	Substituted pyrrolo[2.3-B]pyridines
Saleh Ahmed, Oxford (United Kingdom); Oscar Barba, Oxford (United Kingdom); Jason Bloxham, Oxford (United Kingdom); Graham Dawson, Oxford (United Kingdom); William Gattrell, Oxford (United Kingdom); John Kitchin, Oxford (United Kingdom); Neil Anthony Pegg, Oxford (United Kingdom); Imaad Saba, Oxford (United Kingdom); Shazia Sadiq, Oxford (United Kingdom); Colin Peter Sambrook Smith, Oxford (United Kingdom); Don Smyth, Oxford (United Kingdom); Amo G. Steinig, Farmingdale, N.Y. (US); Robin Wilkes, Oxford (United Kingdom); Bijoy Panicker, Farmingdale, N.Y. (US); Paula Tavares, Farmingdale, N.Y. (US); Matthew Cox, Farmingdale, N.Y. (US); An-Hu Li, Farmingdale, N.Y. (US); Hanqing Dong, Farmingdale, N.Y. (US); Lifu Ma, Farmingdale, N.Y. (US); Kenneth (‘Ken’) Foreman, Farmingdale, N.Y. (US); Qinghua (‘Felix’) Weng, Farmingdale, N.Y. (US); and Kathryn Stolz, Farmingdale, N.Y. (US)
Assigned to OSI Pharmaceuticals, Inc., Melville, N.Y. (US)
Filed on Aug. 01, 2005, as Appl. No. 11/194,158.
Claims priority of provisional application 60/598173, filed on Aug. 02, 2004.
Claims priority of provisional application 60/698516, filed on Jul. 12, 2005.
Prior Publication US 2006/0211678 A1, Sep. 21, 2006
Int. Cl. A61K 31/437 (2006.01); A61K 31/496 (2006.01); A61K 31/5355 (2006.01); A61K 31/541 (2006.01); A61K 31/5513 (2006.01); A61K 31/551 (2006.01); C07D 471/04 (2006.01); C07D 223/04 (2006.01); C07D 243/08 (2006.01); C07D 241/04 (2006.01); C07D 413/10 (2006.01); C07D 413/06 (2006.01); C07D 413/08 (2006.01); C07D 413/12 (2006.01); C07D 413/14 (2006.01); C07D 417/06 (2006.01); C07D 417/14 (2006.01); A61K 31/04 (2006.01); A61K 31/519 (2006.01); C07D 487/04 (2006.01)

U.S. Cl. 514—228.2 [514/253.04; 514/235.5; 514/218; 514/217.04; 514/278; 514/300; 514/265.1; 546/113; 546/15; 546/117; 540/597; 540/575; 544/127; 544/61; 544/280]

14 Claims

1. A compound represented by Formula I:

or a pharmaceutically acceptable salt thereof, wherein

X is C—CN;

Cy is

z is hetaryl, —C_1-6alkyl-O—C_1-6alkyl-, —C_0-6alkyl-(heterocyclyl), —C_0-6alkyl-(hetaryl), —C(O)—C_0-6alkyl, —C(O)—C_0-6alkyl-O—C_0-6alkyl, —C(O)—C_0-6alkyl-O—C_1-6alkyl-O—C_0-6alkyl, —C(O)—C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-(heterocyclyl), —C(O)—C_0-6alkyl-(heterocyclyl)-C(O)—C_0-6alkyl, —C(O)—C_0-6alkyl-(hetaryl), —S(O)₂—C_0-6alkyl, —S(O)₂—N(C_0-6alkyl)(C_0-6alkyl), or —S(O)₂—(hetaryl), wherein any of the alkyl, heterocyclyl, or hetaryl optionally is substituted with 1-6 independent halo, OH, —C_0-6alkyl-O—C_0-6alkyl, —C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-(heterocyclyl), or —C_0-6alkyl;

in which the wavy bond is the point of attachment, and wherein the piperazine or morpholine moieties are optionally substituted with 1-6 independent C_0-6alkyl groups;

Y is —C(C_0-6alkyl)(C_0-6alkyl)-, —N(C_0-6alkyl)-, —N(C_0-6alkyl)-C_1-6alkyl-, O, S, >N—C_2-6alkyl-N—(C_0-6alkyl)(C_0-6alkyl), >N—C_2-6alkyl-O—C_0-6alkyl, >N—C_1-6alkyl-C(O)—NH—C_0-6alkyl, or >N—C_2-6alkyl-N—C(O)—C_1-6alkyl; and

R1 is aryl, hetaryl, or heterocyclyl, optionally substituted with 1-6 independent halo, —CN, —OH, —C_0-6alkyl, —C_3-10cycloalkyl, -haloC_1-6alkyl, —C_2-6alkynyl, —N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-(heterocyclyl), —C_1-6alkyl-C(O)—C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —O—C_0-6alkyl-(heterocyclyl), —C_0-6alkyl-O—C_0-6alkyl, —C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —O—C_0-6alkyl-(hetaryl), —S(O)₂—N(C_0-6alkyl)(C_0-6alkyl), aryl, hetaryl, or heterocyclyl substituents, or substituted with an oxo (═O) using a bond from the aryl, hetaryl, or heterocyclyl ring, wherein any of the substituents optionally is substituted with 1-6 independent halo, CN, OH, —C_0-6alkyl-O—C_0-6alkyl, —C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-N(C_0-6alkyl)(C_0-6alkyl), —C(O)—C_0-6alkyl-(heterocyclyl), or C_0-6alkyl; or a pharmaceutically acceptable salt thereof.