Patent ID: 6337394
Filing Date: 2002-01-08
Classification: A61K,A61P,C07D

Abstract:
A compound of formula I, whereinR1 represents H, C(O)R11, SiR12R13R14 or C1-6 alkyl (which latter group is optionally substituted or terminated by one or more substituents selected from OR15 or (CH2)qR16); R12, R13 and R14 independently represent H, phenyl or C1-6 alkyl; R16 represents C1-4 alkyl, phenyl, OH, C(O)OR17 or C(O)N(H)R18; R18 represents H, C1-4 alkyl or CH2C(O)OR19; R15 and R17 independently represent H, C1-6 alkyl or C7-9 alkylphenyl; R11 and R19 independently represent H or C1-4 alkyl; and q represents 0, 1 or 2; R2 and R3 independently represent H, C1-4 alkyl, cyclohexyl or phenyl; Rx represents a structural fragment of formula IIa, IIb or IIc, â€ƒwherein k, l and m independently represent 0, 1, 2, 3 or 4; R4 and R5 independently represent H, Si(Me)3, 1- or 2-naphthyl, a polycyclic hydrocarbyl group, CHR41R42 or C1-4 alkyl (which latter group is optionally substituted by one or more halo substituents), or C3-8 cycloalkyl, phenyl, methylenedioxyphenyl, benzodioxanyl, benzofuranyl, dihydrobenzofuranyl, benzothiazolyl, benzoxazolyl, benzimidazolyl, coumaranonyl, coumarinyl or dihydrocoumarinyl (which latter twelve groups are optionally substituted by one or more of C1-4 alkyl (which latter group is optionally substituted by one or more halo substituents), C1-4 alkoxy, halo, hydroxy, cyano, nitro, SO2NH2, C(O)OH or N(H)R43); R41 and R42 independently represent cyclohexyl or phenyl; R6 and R7 independently represent H, C1-4 alkyl, C3-8 cycloalkyl, phenyl (which latter group is optionally substituted by one or more of C1-4 alkyl (which latter group is optionally substituted by one or more halo substituents), C1-4 alkoxy, halo, hydroxy, cyano, nitro, SO2NH2, C(O)OH or N(H)R44) or together with the carbon atom to which they are attached form a C3-8 cycloalkyl ring; R43 and R44 independently represent H or C(O)R43; and R45 represents H, C1-4 alkyl or C1-4 alkoxy; Y represents CH2, (CH2)2, CH&boxH;CH, (CH2)3, CH2CH&boxH;CH or CH&boxH;CHCH2, which latter three groups are optionally substituted by C1-4 alkyl, methylene, oxo or hydroxy; n represents 0, 1, 2, 3 or 4; and B represents a structural fragment of formula IVa, IVb, IVc or IVd, â€ƒwherein X1, X2, X3 and X4 independently represent CH, N or Nâ€”O; X5 and X6 independently represent a single bond or CH2; one of X7, X8 and X9 represents S, O or NH, and the other two independently represent â€”CH&boxH;, &boxH;CHâ€”, â€”N&boxH;, &boxH;Nâ€”, â€”N(O)&boxH; or &boxH;N(O)â€”; R31 represents, in all cases, one or more optional substituents selected from halo, C1-4 alkyl, C1-4 alkoxy or â€”Oâ€”(CH2)pâ€”C(O)N(R32)(R33); p represents 0, 1, 2, 3 or 4; and R32 and R33 independently represent H, C1-6 alkyl or C3-7 cycloalkyl; wherein, when B represents a structural fragment for formula IVA (in which X1, X2, X3, and X4 all represent CH), a structural fragment of formula or IVB or a structural fragment of formula or IVc, R31 represents one or more substituents selected from halo, C1-4 alkyl, C1-4 alkoxy or â€”O-(CH2)p-C(O)N(R32)(R33); or a pharmaceutically acceptable salt thereof. or a pharmaceutically acceptable salt thereof.