Patent ID: 7087626
Filing Date: 2006-08-08
Classification: A61P,C07D

Abstract:
1. A compound of the structure is a four, five, or six membered saturated ring and X is C, O or S with the proviso that the ring is a fully saturated carbon ring wherein X in the ring may be a single substitution of either C, O or S, except X cannot be O when it would be adjacent to carbon of the pyrazolo ring and R1 is pyridine and R2 is a sulfonyl substituted phenyl or thienyl; R1 is unsubstituted or substituted phenyl; unsubstituted or substituted pyridine; unsubstituted or substituted pyridine N-oxide; unsubstituted or substituted quinoline; unsubstituted or substituted quinoline N-oxide; unsubstituted or substituted naphthyridine; unsubstituted or substituted pyrazine; furyl; unsubstituted or substituted thiazolyl; unsubstituted or substituted imidazolyl; unsubstituted or substituted pyrazolyl; or unsubstituted or substituted thiophenyl; wherein the substitution may be one or more of the following: (C R2 is unsubstituted or substituted quinoline; unsubstituted or substituted quinoline N-oxide; unsubstituted or substituted phenyl; unsubstituted or substituted naphthalene; unsubstituted or substituted pyridine; unsubstituted or substituted pyridine N-oxide; unsubstituted or substituted quinazoline; unsubstituted or substituted cinnoline; unsubstituted or substituted benzodioxole; unsubstituted or substituted benzodioxane; unsubstituted or substituted benzothiophene; or unsubstituted or substituted phenanthroline; wherein the substitution may independently be one or more of the following: hydrogen, (C or a group of the formula wherein: X 1 is O, N, S, SO 2 , NR 13 , C(O), or bond; Q 1 is hydrogen, phenyl, 5-(2,2-difluoro-1,3-benzodioxolyl), C(O)Q 5 , or pyridyl when, m and n are independently 0-2, except when one is 0 the other cannot be 0; Q 1 , is OR, NR 11 R 12 , halo, N-morpholino, N-piperazino-N′R 13 , N-imidazolyl, N-pyrazolyl, N-triazolyl, N-(4-piperidinylpiperidine), SO 2 R 14 , SOR 14 , NHSO 2 R 15 , acetamido, N-phthalimido, N-oxazolidino, N-imidazolino, N-benzoxazolidino, N-pyrolidinonyl, N(N′-methylbenzimidazolino), N,N-di(C 1 -C 4 )alkylamino(C 1 -C 4 )alkoxy, N-benzimidazolino; when m and n are independently 0-2, but one or the other of m or n is not 0; Q 5 is hydroxy, methoxy, amino, diethylamino, dimethylamino; R 10 is hydrogen, halo, (C 1 -C 6 )alkyl; R 11 and R 12 are independently hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, arylalkyl, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkylmethyl, 4-(N-methylpiperidinyl), pyridyl, or R 11 and R 10 can be taken together to form a 4, 5, 6, or 7 membered ring, or R 11 and R 12 can be taken together to form a 3, 4, 5, 6, or 7 membered ring; R 13 is hydrogen, (C 1 -C 6 )alkyl, 2-methoxyphenyl, 2-pyridimidinyl; R 14 is 2-pyrimidinyl, N-methyl-2-imidazolyl, 4-chlorophenyl, 2-pyridylmethyl; R 15 is (C 1 -C 6 )alkyl, N-methyl-4-imidazolyl; R 16 is hydrogen, halo, arylalkyl, aryl, or a group of the formula wherein: Q 2 is hydrogen, 4-imidazolyl, or C(O)NR 24 R 25 when o and p are independently 0-2; Q 2 is OR 23 , NR 24 R 25 , or N-morpholino, when o and p are independently 0-2, but one or the other of o or p is not 0; R 20 is hydrogen, or (C 1 -C 6 )alkyl; R 21 is hydrogen, (C 1 -C 6 )alkyl, or R 21 and R 20 can be taken together to form a 4, 5, 6, or 7 membered ring; R 22 is hydrogen, (C 1 -C 6 )alkyl, arylalkyl, aryl, or R 21 and R 22 can be taken together to be a 3, 4, 5, 6, 7 membered ring; R 23 is hydrogen or (C 1 -C 6 )alkyl; R 24 is hydrogen, (C 1 -C 6 )alkyl, or R 24 and R 25 can be taken together to form a 3, 4, 5, 6, or 7 membered ring, or R 24 and R 20 can be taken together to form a 6 or 7 membered ring; R 25 is hydrogen, (C 1 -C 6 )alkyl, or acetyl, or a group of the formula wherein: R 30 is hydrogen, or (C 1 -C 6 )alkyl; R 31 is hydrogen, (C 1 -C 6 )alkyl, 2-pyridyl, pyridylmethyl, amino, or hydroxy, or a group of the formula wherein: R 32 and R 33 are each independently hydrogen, (C 1 -C 6 )alkyl, acetyl, (C 1 -C 4 )alkylsulphonyl, or R 32 and R 33 can be taken together to form a 4, 5, 6, or 7 membered ring, or a group of the formula wherein: X 2 is CH 2 , O, or N; q is 0-3; Q 3 is NR 36 R 37 , or OR 38 , and R 35 is hydrogen, or R 35 and Q 3 can be taken together to form a 5 membered ring; R 36 , R 37 , and R 38 are each independently hydrogen, or (C 1 -C 6 )alkyl, or a group of the formula wherein: X 3 is cyano, carboxamide, N,N-dimethylcarboxamide, N,N-dimethylthiocarboxamide, N,N-dimethylaminomethyl, 4-methylpiperazin-1-yl-methyl or carboxylate, or a group of the formula wherein: Q 6 is NR 41 R 42 ; r is 2-3; R 40 is hydrogen, or (C 1 -C 6 )alkyl; R 41 and R 42 are hydrogen, (C 1 -C 6 )alkyl, or R 41 and R 40 can be taken together to form a 6 or 7 membered ring, or a group of the formula wherein: Q 7 is hydroxy, methoxy, dimethylamino, or N-piperidinyl; with the proviso that when one of R 1 or R 2 is unsubstituted or substituted phenyl, then the other cannot be unsubstituted or substituted phenyl or thiophen-2-yl; and with the proviso that when R 2 is quinolin-4-yl, substitution at the quinoline 7-position cannot include an aryl, heteroaryl, fused aryl, or fused heteroaryl; k is 1-8; R