Patent ID: 7351738
Filing Date: 2008-04-01
Classification: A61P,C07C,C07D

Abstract:
1. A compound of the formula: or pharmaceutically acceptable salts or esters thereof; wherein X is —(C═O)—, —(C═S)—, or —(C═N—Z), wherein Z is R 20 or —OR 20 ; T is NR 20 ; wherein each R 20 is independently H, —CN, C 1 -C 6 alkyl C 2 -C 6 alkenyl, C 1 -C 6 haloalkyl or C 4 -C 7 cycloalkyl, with the proviso that when Z is R 20 or —OR 20 , R 20 is not —CN; wherein R 1 is —(CH 2 ) 1-2 —S(O) 0-2 —(C 1 -C 6 alkyl), or C C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, each of which is optionally substituted with 1, 2, or 3 groups independently selected from halogen, —OH, —SH, —C≡N, —CF 3 , C 1 -C 3 alkoxy, amino, and mono- or dialkylamino, or aryl, heteroaryl, heterocyclyl, —C R and R′ independently are hydrogen, C 1 -C 10 alkyl, C 1 -C 10 alkylaryl or C 1 -C 10 alkylheteroaryl; wherein Rc is (I) —[—(CH (II) —(C(Rc-x)(Rc-y)) wherein each Rc-x and Rc-y is independently chosen from: H C C C —(CH Rc-cycle is aryl, heteroaryl, cycloalkyl or a fused-ring system consisting of no more than three rings where each of the rings is the same or different and is an aryl, heteroaryl, or cycloalkyl ring  wherein Rc-cycle is optionally substituted with up to four substituents independently selected from:  and when there is a saturated carbon atom in Rc-cycle (III) —(CR (IV) —(CR (V) —(CR (VI) —(CR (VII) —(CR (VIII) —(CR (IX) —(CR (X) —(CR (XI) —(CR (XII) —[C(R (XIII) —CH(aryl) (XIV) —CH(heteroaryl) (XVIII) —CH(aryl)(heteroaryl); wherein R N is R′ 100 , —(CRR′) 1-6 R′ 100 , —(CRR′) 0-6 R 100 , —(CRR′) 1-6 —O—R′ 100 , —(CRR′) 1-6 —S—R′ 100 , —(CRR′) 1-6 —C(═O)—R 100 , —(CRR′) 1-6 —SO 2 —R 100 , —(CRR′) 1-6 —NR 100 —R′ 100 or —SO 2 R′ 100 , with the proviso that when R N is —SO 2 R′ 100 , X is not —S(═O) n — or —C(═S)—; wherein R 100 and R′ 100 are independently represent aryl, heteroaryl, -aryl-W-aryl, -aryl-W-heteroaryl, -aryl-W-heterocyclyl, -heteroaryl-W-aryl, -heteroaryl-W-heteroaryl, -heteroaryl-W-heterocyclyl, -heterocyclyl-W-aryl, -heterocyclyl-W-heteroaryl, -heterocyclyl-W-heterocyclyl, —CH [(CH 2 ) 0-2 —O—R 150 ]—(CH 2 ) 0-2 -aryl, —CH [(CH 2 ) 0-2 —O—R 150 ]—(CH 2 ) 0-2 -heterocyclyl or —CH[(CH 2 ) 0-2 —O—R 150 ]—(CH 2 ) 0-2 -heteroaryl, where the ring portions of each are optionally substituted with 1, 2, or 3 groups independently selected from —OR, —NO R 100 is C 1 -C 10 alkyl optionally substituted with 1, 2, or 3 R 115 groups, or R 100 is —(C 1 -C 6 alkyl)—O—C 1 -C 6 alkyl) or —(C 1 -C 6 alkyl)—S—(C 1 -C 6 alkyl), each C 1 -C 6 alkyl is optionally substituted with 1, 2, or 3 R 115 groups, or R 100 is C 3 -C 8 cycloalkyl optionally substituted with 1, 2, or 3 R 115 groups; W is a bond —(CH 2 ) 1-4 —, —O—, —S(O) 0-2 —, —N(R 135 )—, —CR(OH)— or —C(O)—; R 102 and R 102 ′ independently are hydrogen, or C R 105 and R′ 105 independently are —H, —R 110 , —R 120 , C 3 -C 7 cycloalkyl, —(C 1 -C 2 alkyl)-(C 3 -C 7 cycloalkyl), —(C 1 -C 6 alkyl)—O—(C 1 -C 3 alkyl), C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or C 1 -C 6 alkyl chain with one double bond and one triple bond, C 1 -C 6 alkyl optionally substituted with —OH or —NH 2 ; or C 1 -C 6 alkyl optionally substituted with 1, 2, or 3 halogen, or R 105 and R′ 105 together with the atom to which they are attached form a 3 to 7 membered carbocylic ring, where one member is optionally a heteratom selected from —O—, —S(O) 0-2 —, —N(R 135 )—, the ring being optionally substituted with 1, 2 or three R 140 groups; R 115 at each occurrence is independently halogen, —OH, —CO 2 R 102 , —C 1 -C 6 thioalkoxy, —CO 2 -phenyl, —NR 105 R′ 135 , —SO 2 —(C 1 -C 8 alkyl), —C(═O)R 180 , R 180 , —CONR 105 R′ 105 , —SO 2 NR 105 R′ 105 , —NH—CO—(C 1 -C 6 alkyl), —NH—C(═O)—OH, —NH—C(═O)—OR, —NH—C(═O)—O-phenyl, —O—C(═O)—(C 1 -C 6 alkyl), —O—C(═O)-amino, —O—C(═O)-mono- or dialkylamino, —O—C(═O)-phenyl, —O—(C 1 -C 6 alkyl)—CO 2 H, —NH—SO 2 —(C 1 -C 6 alkyl), C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; R 135 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 7 cycloalkyl, —(CH 2 ) 0-2 -(aryl), —(CH 2 ) 0-2 -(heteroaryl), or —(CH 2 ) 0-2 -(heterocyclyl); R 140 is heterocyclyl optionally substituted with 1, 2, 3, or 4 groups independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halogen, hydroxy, cyano, nitro, amino, mono(C 1 -C 6 )alkylamino, di(C 1 -C 6 )alkylamino, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 haloalkyl, C 1 -C 6 haloalkoxy, amino(C 1 -C 6 )alkyl, mono(C 1 -C 6 )alkylamino(C 1 -C 6 )alkyl, di(C 1 -C 6 )alkylamino(C 1 -C 6 )alkyl, and ═O; R 150 is hydrogen, C 3 -C 7 cycloalkyl, —(C 1 -C 2 alkyl)-(C 3 -C 7 cycloalkyl), C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 alkyl with one double bond and one triple bond, —R 110 , —R 120 , or C R 150 ′ is C 3 -C 7 cycloalkyl, —(C 1 -C 3 alkyl)-(C 3 -C 7 cycloalkyl), C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 alkyl with one double bond and one triple bond, —R 110 , —R 120 , or C R R 110 is aryl optionally substituted with 1 or 2 R 125 groups; R 125 at each occurrence is independently halogen, amino, mono- or dialkylamino, —OH, —C≡N, —SO 2 —NH 2 , —SO 2 —NH—C 1 -C 6 alkyl, —SO 2 —N(C 1 -C 6 alkyl) 2 , —SO 2 —(C 1 -C 4 alkyl), —CO—NH 2 , —CO—NH—C 1 -C 6 alkyl, or —CO—N(C 1 -C 6 alkyl) 2 , or C C R 120 is heteroaryl optionally substituted with 1 or 2 R 125 groups; and R 130 is heterocyclyl optionally substituted with 1 or 2 R 125 groups; R 2 is selected from the group consisting of H; C 1 -C 6 alkyl, optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1 -C 3 alkyl, halogen, —OH, —SH, —C≡N, —CF 3 , C 1 -C 3 alkoxy, and —NR 1-a R 1-b ; wherein R 1-a and R 1-b are —H or C 1 -C 6 alkyl; —(CH 2 ) 0-4 -aryl; —(CH 2 ) 0-4 -heteroaryl; C 2 -C 6 alkenyl; C 2 -C 6 alkynyl; —CONR N-2 R N-3 ; —SO 2 NR N-2 R N-3 ; —CO 2 H; and —CO 2 —(C 1 -C 4 alkyl); R 3 is selected from the group consisting of H; C 1 -C 6 alkyl optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1 -C 3 alkyl, halogen, —OH, —SH, —C≡N, —CF 3 , C 1 -C 3 alkoxy, and —NR 1-a R 1-b ; —(CH 2 ) 0-4 -aryl; —(CH 2 ) 0-4 -heteroaryl; C 2 -C 6 alkenyl; C 2 -C 6 alkynyl; —CO—NR N-2 R N-3 ; —SO 2 —NR N-2 R N-3 ; —CO 2 H; and —CO—O—(C 1 -C 4 alkyl); wherein R R