| 主权项 |
1. A compound of Formula I,wherein:
‘—’ is either a single bond or absent; ring A represents monocyclic or polycyclic C3-20 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl or 3-14 membered heterocyclyl ring; ring B represents monocyclic or polycyclic C3-20 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl or 3-14 membered heterocyclyl ring; U, V and W are independently selected from —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, —OH, —CN, —N3, —NO2, —OCONH2, —F, —Cl, —Br, —I, —COOH, —CONH2, —CONHNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCOOH, —SH, —SO3H, —CH(═NOH), —CORa, —OR9, —COORa, —CONRaRb, —NRaRb, —NRaSO2Rb, —NRaCONRbRc, —NRaCORb, —NRaCOORb, —OCORa, —OCOORa, —OCONRaRb, —SRa, —S(O)Ra, —S(O)2Ra, —SO2NRaRb, —CRa (═NORb), —NHP(O) RaRb; wherein the said C1-12 alkyl, C2-12 alkenyl and C2-12 alkynyl, may be substituted with substituents selected from R11; provided that atleast two out of U, V and W represent —OR9; Z represents —(CH2)nORa, —ORa, —OCORa, —OCOORa, —OCONRaRb, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, —CN, —OCONH2, —CHO, —COOH, —CONH2, —CONHNH2, —NH2, —NHCOOH, —CH2OH, —OH, —SH, —SO3H, —CH(═NOH), —CH(═NCN), —CORa, —COORa, —CONRaRb, —NRaRb, —NRaSO2Rb, —NRaCONRbRc, —NRaNRbRc, —NRaCORb, —NRaCOORb, —SRa, —S(O)Ra, —S(O)2Ra, —SO2NRaRb or —CRa (═NORb); wherein the said C1-12 alkyl, C2-12 alkenyl and C2-12 alkynyl, may be substituted with substituents selected from R11; R1, R2, R3 and R4 are independently selected from —H, C1-12 alkyl , C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCONH2, —F, —Cl, —Br, —I, —CHO, —COOH, —CONH2, —NH2, —NHCONH2, —NHCHO, —NHCOOH, —OH, —ORa, —SH, —SO3H; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R11; R5 represents —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl or 5-10 membered heteroaryl; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R11; R6 represents —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —NH2, —NHCONH2, —NHCHO, —OH, —SH, —NRaRb, —NRaCONRbRc, —NRaCORb, —ORa or —SRa; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R11; E represents O, S, SO, SO2, NR10 or a single bond; G represents C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl or 5-10 membered heteroaryl; each of which may be substituted with substituents selected from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH), —CH(═NCN), —CORa, —CSRa, —COORa, —CSORa, —COSRa, —CONRaRb, —CSNRaRb, —COCORa, —CONRaNRbRc, —CSNRaNRbRc, —CSNRaRb, —NRaRb, —NRaSO2Rb, —NRaCONRbRc, —NRaCSNRbRc, —NRa(C═NRb)NRcRd, —NRaNRbRc, —NRaCORb, —NRaCSRb, —NRaCOORb, —NRaCSORb, —ORa, —OCORa, —OCOORa, —OCONRaRb, —OCSRa, —OCSORa, —ONO2, —OCSNRaRb, —SRa, —S(O)Ra, —S(O)2Ra, —SO2NRaRb, —CRa(═NORb), —CRa (═NCOORb), —CRa(═NSORb), —CRa(═NSO2Rb), —C(═NRa)—NRbRc, —C(═NORa)—NRbRc, —CRa(═NCN), —NCRa, —P(O)RaRb, —P(O)ORaORb, —P(O)RaORb, —P(O)NRaORb, —P(O)NRaRb, —OP(O)RaRb, —NHP(O)RaRb; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH), —CH(═NCN); When E is a single bond or Nitrogen, then E and R6 can be joined together to farm a saturated or unsaturated C3-10 cycloalkyl or 3-10 membered heterocyclyl ring, which may further be fused to one or more C3-10 cycloalkyl, 3-10 membered heterocyclyl, C5-10 aryl or 5-10 membered heteroaryl ring. The ring thus formed may further be substituted with substituents selected from R12; G and R6 can be joined together to form a saturated or unsaturated C3-10 cycloalkyl or 3-10 membered heterocyclyl ring, which may further be fused to one or more C3-10 cycloalkyl, 3-10 membered heterocyclyl, C5-10 aryl or 5-10 membered heteroaryl ring. The ring thus formed may further be substituted with substituents selected from R12; R7 represents —H, —OH or —OR9; R8 represents —H, —CHO, —COOH, —CONH2, —OH, —CH(═NOH), —CORa, —COORa, —CONRaRb, —CRa (═NORb), —ORa, or —(CH2)nORa; or R7 and R8 can be joined together to form a saturated or unsaturated ring, in which one or more methylene groups or methyne groups can be replaced with O, S, NRa or oxo; the ring thus formed may be substituted with substituents selected from R12; or R8 and Z can be joined together to form a saturated or unsaturated ring, in which one or more methylene groups or methyne groups can be replaced with O, S, NRa or oxo; the ring thus formed may be substituted with substituents selected from R12; R9 represents —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CHO, —CONH2, —CORa, —CONRaRb, —S(O)2Ra, —SO2NRaRb, —P(O)RaRb, —P(O)ORaORb, —P(O)RaORb, —P(O)NRaORb or —P(O)NRaRb; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CHO, —CONH2, —CORa, —CONRaRb, —S(O)2Ra, —SO2NRaRb, —P(O)RaRb, —P(O)ORaORb, —P(O)RaORb, —P(O)NRaORb, —P(O)NRaRb; further wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R13; R10 represents —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CRa(═NORb), —S(O)Ra, —S(O)2Ra, —S(O)2NRaRb, —(CH2)nS(O)Ra, —(CH2)nS(O)2Ra, —P(O)RaRb, —CORa, —CSRa, —COORa, —CSORa, —COSRa, —CSSRa, —CONRaRb or —CSNRaRb; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —NO2, NH2; further wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R13; R11 represents C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH), —CH(═NCN), —CORa, —CSRa, —COORa, —CSORa, —COSRa, —CONRaRb, —CSNRaRb, —COCORa, —CONRaNRbRc, —CSNRaNRbRc, —CSNRaRb, —NRaRb, —NRaSO2Rb, —NRaCONRbRc, —NRaCSNRbRc, —NRa(C═NRb)NRcRd, —NRaNRbRc, —NRaCORb, —NRaCSRb, —NRaCOORb, —NRaCSORb, —ORa, —OCORa, —OCOORa, —OCONRaRb, —OCSRa, —OCSORa, —ONO2, —OCSNRaRb, —SRa, —S(O)Ra, —S(O)2Ra, —SO2NRaRb, —CRa(═NORb), —CRa (═NCOORb), —CRa(═NSORb), —CRa(═NSO2Rb), —C(═NRa)—NRbRc, —C(═NORa)—NRbRc, —CRa(═NCN), —NCRa, —P(O)RaRb, —P(O)ORaORb, —P(O)RaORb, —P(O)NRaORb, —P(O)NRaRb, —OP(O)RaRb or —NHP(O)RaRb; wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R13; R12 represents C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH) or —CH(═NCN); wherein the said C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl and 5-10 membered heteroaryl, may be substituted with substituents selected from R13; R13 represents C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH) or —CH(═NCN); Ra, Rb, Rc and Rd are independently selected from —H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10 aryl, C3-20 cycloalkyl, 3-14 membered heterocyclyl, 5-10 membered heteroaryl, —CN, —COCN, —N3, —NO2, —OCN, —NCO, —SCN, —NCS, —OCONH2, —ONO2, —F, —Cl, —Br, —I, —CO—, —CS—, —CHO, —CHS, —COOH, —COSH, —CONH2, —CONHNH2, —CSNHNH2, —CSNH2, —NH2, —NHCONH2, —NHCSNH2, —NH(C═NH)NH2, —NHNH2, —NHCHO, —NHCHS, —NHCOOH, —NHCSOH, —OH, —SH, —SO3H, —CH(═NOH), —CH(═NCN); each of which may be substituted with substituents selected from R13; or Ra and Rb when attached to the same atom, can be joined together to form a monocyclic or polycyclic ring, in which one or more methylene groups or methyne groups can be replaced with O, S, SO, SO2, NRa, PRa, P(═O)Ra or oxo; the ring thus formed may be substituted with substituents selected from R12; or Rb and Rc when attached to the same atom, can be joined together to form a monocyclic or polycyclic ring, in which one or more methylene groups or methyne groups can be replaced with O, S, SO, SO2, NRa, PRa, P(═O)Ra or oxo; the ring thus formed may be substituted with substituents selected from R12; or Rc and Rd when attached to the same atom, can be joined together to form a monocyclic or polycyclic ring, in which one or more methylene groups or methyne groups can be replaced with O, S, SO, SO2, NRa, PRa, P(═O)Ra or oxo; the ring thus formed may be substituted with substituents selected from R12; n represents 1, 2, 3, 4 or 5; their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. |
