Patent ID: 6699856
Filing Date: 2004-03-02
Classification: A61P,C07D

Abstract:
A compound represented by formula I: or a pharmaceutically acceptable salt, ester, N-oxide or hydrate thereof, said ester formed at the carboxy group shown in formula I, wherein:R1 is selected from the group consisting of: OH, C1-6alkyl, HET, Aryl, C1-6alkoxy, NH2, NHC1-6alkyl, N(C1-6alkyl)2, C1-6alkylC(O), C1-6alkylS(O)y, Aryl-S(O)y and Aryl-C(O), the alkyl and alkyl portions of which being optionally substituted with 1-2 members selected from the group consisting of: OH, Aryl1, halo, NH2, NHCH3, N(CH3)2, CO2H, CF3 and C1-4-acyl; Aryl represents a C6-14aromatic 1-3 ring system optionally substituted with 1-3 members selected from OH, C1-6alkyl, OC1-6alkyl, Aryl1, oxadiazolyl, halo, NH2, NHCH3, N(CH3)2, CF3, CO2H and C1-4acyl; Aryl1 represents a C6-14 membered aromatic ring system having 1-3 rings and optionally substituted with 1-3 members selected from the group consisting of: OH, halo, NH2, NHCH3, N(CH3)2, CO2H and C1-4-acyl; HET is selected from the group consisting of: pyridinyl, pyrazinyl, pyrrolyl, furanyl, pyrazolyl, imidazolyl, benzimidazolyl, oxathiazolyl, thiazolyl, benzothiazolyl, oxazolyl, 1,2-diazolyl, 1,2,3- and 1,2,4-triazolyl, 1,2,4- and 1,2,5-oxadiazolyl, 1,2,4- and 1,2,5-thiadiazolyl, tetrazolyl, isoxazolyl, thienyl, azepinyl, pyrrolidinyl, piperidinyl, piperazinyl, said HET being optionally substituted with 1-2 oxo groups and 1-3 groups selected from halo, C1-4alkyl, C1-4alkoxy, CF3 and C1-4acyl; Ra and Rb independently represent a member selected from the group consisting of: H, Aryl, C1-6-alkyl optionally substituted by 1-3 of halo, OR4, SR4 and C5-7cycloalkyl, or in the alternative, Ra and Rb are taken in combination and represent a non-aromatic carbocyclic 4-7 membered ring; R4 is selected from the group consisting of: H, C1-5-alkyl, Aryl and Aryl-C1-4alkyl-optionally substituted with 1-2 groups selected from halo and C1-4alkyl; R5 is H, C1-4alkyl or C1-4acyl; Rc and Rd each independently represents a member selected from the group consisting of: H, C1-6alkyl and Aryl, or in the alternative, Rc and Rd are taken in combination and represent a non-aromatic carbocyclic ring of 3-7 members, n is an integer from 0-6 inclusive; R2 represents H, halo or C1-6alkyl; R3 represents H, C1-6alkyl, Aryl, C1-6alkylSR6, C1-6alkylOR6, C1-6alkylOC(O)R7 or C1-6alkylNR8R9; R6 represents C1-6alkyl, Aryl, or Aryl-C1-6alkyl-, said alkyl and the alkyl portions being optionally substituted with 1-3 members selected from the group consisting of: OH, halo, NH2, NHCH3, N(CH3)2, CO2H, CF3 and C1-4acyl; R7 represents C1-8alkyl or Aryl; R8 and R9 independently represent H, C1-10alkyl, Aryl, â€”C1-6alkylNH2, â€”C1-6alkylNH(C1-6alkyl), â€”C1-6alkylN(C1-6alkyl)2, Aryl-C1-6alkyl-, C1-6alkylOH, or C1-6alkylOC1-6alkyl , or R8 and R9 are taken in combination with the nitrogen atom to which they are attached and represent a 3-10 membered saturated mono- or bi-cyclic ring system optionally containing one additional heteroatom selected from O, S or N or is 1,2,3,4-tetrahydroisoquinolinyl or is 2,3-dyhydro-1H-isoindolyl and optionally substituted with 1-2 oxo groups, and 1-3 groups selected from C1-6alkyl, CO2Rc and C(O)N(Rc)2, said alkyl and alkyl portions being optionally substituted with 1-3 groups selected from halo, C1-3alkyl, hydroxyC1-3alkyl, C1-3alkoxy, C1-3alkoxyC1-3alkyl and Aryl1, and R10 represents H, C1-20alkyl or aryl, with aryl as previously described.