| 主权项 |
1. A compound of the formula I: or stereoisomers, tautoers, prodrug, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: the dotted lines are absent or selected but is not limited from: —C—C—, —C═C—, —C-heterobond, X, X1 and X2 is absent or independently selected but is not limited from: hydrogen, halogen, —C—, —S—, —O—, —NH—, —NR—, —NRR, —NHC(O)—, —NRC(O)—, —NHSO2—, —NRSO2—, —SO2NH—, —SO2NR—, —C(O)—, —C(O)NH—, —C(O)NR—, —C(O)R—, —CO2—, —C(O)H, —C(O)NH2—, —CO2H, —C(NH)NH—, —C(NH)NR—, —C(S)—, —C(S)NH—, —C(S)NR—, —C(S)R—, —C(NH)NH—, —C(NH)NR—, ═CH—, ═CH2, ═CH—O—, ═CH—S—, ═CH—Se—, ═CH—NR—, ═CH—NH—, ═CH—PR—, wherein R is selected but is not limited from: —C1-6 alkyl, —CO2H, —CO2C1-6alkyl, COC1-6alkyl, phenyl, —CH2phenyl, heteroalkyl and heteroaryl; Y is absent or selected but is not limited from: —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, —CHF—, and —CF2—, wherein each CH2 and CHF is unsubstituted or substituted with 1 or 2 substituents selected from Ra; Z is absent or selected but is not limited from: hydrogen, halogen, —C1-6alkyl, —C2-6alkenyl, —C2-6alkynyl, —C3-10cycloalkyl, —C3-10cycloalkenyl, aryl, —C3-10heterocycle, —C3-10heteroaryl, —CN, —CF3, —OH, —OC1-6alkyl, —NH2, —NHC1-6alkyl, —N(C1-6alkyl)2, guanidine, amidine —SC1-6alkyl, —SOC1-6alkyl, —SO2C1-6alkyl, —NHSO2C1-6alkyl, —NHC(O)C1-6alkyl, —SO2NHC1-6alkyl, —C(O)OH, —C(O)OC1-6alkyl, —C(O)NHC1-6alkyl, P(O)(OH)2, P(O)(OR)2, —(CH2)mP(O)(OH)2, —(CH2)mP(O)(OC1-6alkyl)2, —(CH2)mP(O)(NRbC(Rc))2, C3-8 amino acid, C3-10(OH)0-10polyhydroxide; each R1, R2 and R3 is absent or independently selected but is not limited from: hydrogen, halogen, —C1-10alkyl, —C2-6alkenyl, —C2-6lkynyl, —(CH2)pC3-10 cycloalkyl, —(CH2)pC3-7cycloalkylaryl, —(CH2)pC3-7cycloalkylheteroaryl, —(CH2)pC4-10cycloalkenyl, —(CH2)pC4-7 cycloalkenyl-aryl, —(CH2)pC4-7cycloalkenylheteroaryl, —(CH2)pheteroaryl, —C2-6alkenylalkyl, —C2-6alkenylaryl, —C2-6alkenyl-heteroaryl, —C2-6alkenyl-C3-7cycloalkyl, —C2-6alkynylalkyl, —C2-6alkynylaryl, —C2-6alkynyheteroaryl, —C2-6alkynyl-C3-7cycloalkyl, —C2-6alkynyl-C3-7cycloalkenyl, —C2-6alkynyl-C2-7cycloheteroalkyl, —C2-6alkynyl-C2-7cycloheteroalkenyl, —C(O)(CH2)0-3phenyl, —(CH2)pC(O)phenyl, —C(NH) (CH2)0-3phenyl, —(CH2)mP(O)(NRbC(Rc))2, C3-8 amino acid, C3-10(OH)0-10polyhydroxide, aryl, biphenyl, —C3-10heterocycle, —C3-10heteroaryl, —CN, —CF3, —OH, —OC1-6alkyl, —NH2, —NHC1-6alkyl, —N(C1-6alkyl)2, —NHC(O)C1-6alkyl, guanidine, amidine —SC1-6alkyl, —SOC1-6alkyl, —SO2C1-6alkyl, —NHSO2C1-6alkyl, —SO2NHC1-6alkyl, —C(O)OH, —C(O)OC1-6alkyl, —C(O)NHC1-6alkyl, P(O)(OH)2, P(O)(OR)2, —(CH2)mP(O)(OH)2,-(CH2)mP(O)(OC1-6alkyl)2, —(CH2)mP(O)(NRbC(Rc))2, C3-8 amino acid, C3-10(OH)0-10polyhydroxide; wherein each CH2 is unsubstituted or substituted with 1 or 2 substituents selected from: halogen, —CF3, —OH, —NH2, —C1-6alkyl, —OC1-5alkyl, —NHC1-6alkyl and —N(C1-6alkyl)2, each alkyl, alkenyl and alkynyl is unsubstituted or substituted with 1, 2 or 3 substituents selected from: halogen, CF3, —OH, —NH2, —C1-6alkyl, —OC1-6alkyl, —NHC1-6alkyl and —N(C1-6alkyl)2, and each cycloalkyl, cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, phenyl, aryl and heteroaryl is unsubstituted or substituted with 1, 2, 3 or 4 substituents independently selected from Ra; A ring is selected from: —C3-14alkylcycle, —C3-14arylcycle, —C3-14heterocycle and —C3-14heteroaryl; said —C3-14alkylcycle, arylcycle, heterocycle and —C3-14heteroaryl are selected but are not limited from acridinyl, azetidinyl, acridinyl, azocinyl, azepanyl, azepinyl, aziridinyl, azirinyl, azete, benzothiazole, benzofuranyl, benzimidazolyl, benzofuranyl, benzothranyl, benzothiofuranyl, benzthiazolyl, benztetrazolyl, benzisoxazolyl, benzisothiazolyl, benzimidazolinyl, benzopyrazolyl, benzotriazolyl, benzothiophenyl, benzoxazolyl, benz-1H-tetrazolyl, benz-2H-tetrazolyl, benz-3H-tetrazolyl, benz-4H-tetrazolyl, benz-5H-tetrazolyl, benzothienyl, benzofurazanyl, benzodiazepinyl, carbazolyl, carbolinyl, cinnolinyl, carbazolyl, carbolinyl, chromanyl, chromenyl, coumarinyl, decahydroquinolinyl, 4aH-carbazolyl, 1,4-dioxanyl, 2H, 6H-1,5,2-dithiazinyl, dihydrofuro[2,3-b]tetrahydrothran, furazanyl, hexahydroazepinyl, imidazole, imidazolyl, indolinyl, indolazinyl, indazolyl, isoindolyl isoquinolyl, imidazolidinyl, imidazolinyl, indolyl, indolazinyl, indazolyl, 1H-indazolyl, indolenyl, indolinyl, indolizinyl, 3H-indolyl, isobenzofuranyl, isoquinolyl, 1,2-Isoxazole, 1,3-Isoxazole, isoxazolyl, isochromanyl, isoindolinyl, isothiazolyl, isoxazoline, isoquinolinyl, methylenedioxybenzoyl, methylenedioxyphenyl, morpholinyl, naphthpyridinyl, N-oxides oxetanyl, oxadiazolyl, oxazolyl, oxazolinyl, octahydroisoquinolinyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, oxazolidinyl, oxolanyl, oxirenyl, oxete, oxiranyl, oxanyl, oxetanyl, oxepanyl, oxepinyl, oxazolinyl, pyrazole, 2(1H)-pyrimidinone, piperidine, thiiranyl, phenanthridinyl, phenanthrolinyl, phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phthalazinyl, piperidinyl, 2H-pyrrolyl, pyridin-2-one, piperazinyl, piperidonyl, 4-piperizinyl, piperonyl, pteridinyl, purinyl, pyrazinyl, pyrazolidinyl, pyridazine, pyrazolinyl, pyridazinyl, pyridoimidazole, pyridothiazole, pyridyl, pyrimidinyl, pyridopyridinyl, pyrrazolyl, pyrrolinyl, pyrazolyl, pyrrolyl, pyranyl, pyrazine, pyridinyl, pyrrolidinyl, quinazolinyl, quinolyl, quinoxalinyl, 4H-quinolizinyl, quinuclidinyl, quinoxaline-2(1H)-one, quinolinyl, thiadiazolyl, thranyl, 6H-1,2,5-thiadiazinyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazinyl, 1,2,5-thiadiazinyl, 1,3,4-trizzolyl, 1,3,4-thiadiazinyl, thiomorpholinyl, thienyl, thiomorpholinyl, triazolyl, thiirenyl, thietanyl, thiete, thiolanyl, thiophenyl, thianyl, thiopyranyl, thiepanyl, thiepinyl, thiazole, thionaphthenyl, purinyl, 2,4,6-trihydroxypurinyl, 1,2-thiazole, 1,3-thiazole, xanthenyl; wherein A ring includes the above said heteroaryls, as well as dihydro and tetrathydro analogs and is, unsubstituted or optionally substituted with 1, 2 or 3 same or different substituents and each substituent selected but are not limited from: hydrogen, halogen, —OH, —OR, —SH—, —SR—, —O—, —NO2, —NH2, —NH—, —NR—, —NRR, —CF3, —CN, —C(O)—, —NHC(O)—, —NRC(O)—, —C(O)NH—, —C(O)NR—, —NHSO2—, —NRSO2—, —SO2NH—, —SO2NR—, —C(O)R—, —CO2—, —C(NH)NH—, —C(NH)NR—, wherein R is selected from: —C1-6 alkyl, —CH2F, —CHF2, —CF3, —CO2H, —CO2C1-6alkyl, COC1-6alkyl, phenyl, —CH2phenyl, heteroalkyl and heteroaryl oxo, —(CH2)0-3OH, —CN, —NH2, —NH(C1-6alkyl), —N(C1-6alkyl)2, —C1-6alkyl, —OC1-6alkyl, halogen, —CH2F, —CHF2, —CF3, —CO2H, —CO2C1-6alkyl, —C3-7cycloalkyl, phenyl, CH2phenyl, heteroaryl and CH2 heteroaryl; Ra, Rb and Rc are same or different selected but is not limited from hydrogen, halogen, —C—, —S—, —O—, —NH—, —NR—, —NRR, —NHC(O)—, —NRC(O)—, —NHSO2—, —NRSO2—, —SO2NH—, —SO2NR—, —C(O)—, —C(O)NH—, —C(O)NR—, —C(O)R—, —CO2—, —C(O)H, —C(O)NH2—, —CO2H, —C(NH)NH—, —C(NH)NR—, —C(S)—, —C(S)NH—, —C(S)NR—, —C(S)R—, —C(NH)NH—, —C(NH)NR—, wherein R is selected from: —C1 alkyl, —CO2H, —CO2C1-6alkyl, COC1-6alkyl, phenyl, —CH2phenyl, heteroalkyl and heteroaryl; m is 0, 1, 2, 3 or 4; p is 0, 1, 2, or 3; |
