主权项 |
1. A compound having the structure of Formula I-R or I-S or a pharmaceutically acceptable salt, ester, prodrug, homolog, hydrate or solvate thereof:wherein
X is —NR′R″ or —OR′″; Y is —CN, —Cl, or —CF3; R′ is H, C1-4 alkyl, n-hydroxy C1-4 alkyl, —SO2—R1, or —CO—R1; R″ is H, —SO2—R3, C1-4 alkyl optionally substituted with 1 or more R2, or a ring moiety optionally substituted with R4 wherein such ring moiety is piperidinyl, cyclohexyl, morpholinyl, thiazolyl, pyrazolyl, pyrrolidinyl, imidazolyl, or phenyl; or R′ and R″ taken together with the nitrogen atom to which they are bound form a 4, 5, or 6 membered saturated heterocyclic ring containing 0 or 1 additional heteroatoms where such additional heteroatom is O or N wherein such heterocycle is optionally singly or multiply substituted with substituents independently selected from the group consisting of —OH, oxo, —NH2, n-hydroxy-C1-4 alkyl, —COOH, —(CH2)m—COOH, —(CH2)m—COOR1, —N(R1R1), and —(CH2)m—CO—N(R5R5); R′″ is H, C1-4 alkyl, or —CO—R1; each R1 is independently C1-4 alkyl or H; each R2 is independently H, halo, OH, oxo, ═NH, NH2, —COOH, F, —NHR1, —N(R5R5),—SO2—R1, —SO2—N(R5R5), —N(R1)—SO2—R1, —COOR1, —OCO—R1, —CO—N(R5R5), —N(R1)—COR1, C1-3 alkyl, C1-3 alkoxy, and a ring moiety optionally substituted with R4 wherein such ring moiety is piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, pyrazolyl, imidazolyl, benzimidazolyl, azetidinyl, cyclobutinyl, or phenyl; each R3 is independently R2, C1-4 alkyl, C3-6 cycloalkyl, or C1-4 alkyl optionally substituted with 1 or more R2; each R4 is independently halo, OH, —NH2, —NHR1, —N(R1R1), —COOH, —COOR1, —NHCO—R1, each R5 is independently C1-4 alkyl or H, or two R5 taken together with the nitrogen atom to which they are bound form a 4, 5, or 6 membered saturated heterocyclic ring containing 0 or 1 additional heteroatoms where such additional heteroatom is O or N wherein such heterocycle is optionally substituted with —OH, —NH2, —N(R1R1), n-hydroxy C1-4 alkyl, —(CH2)m—COOH, —(CH2)m—COOR1; and each m is independently 0, 1, 2, or 3. |