主权项 |
1. A compound of formula I: or a pharmacologically acceptable salt thereof, wherein: R is an acylamino group or an optionally substituted benzyl-NH— group; R1 and R2 are independently selected from hydrogen, halogen, a C1-C6 alkyl group, a C1-C6 alkoxy group and a —S—C1-C6-alkyl group; n is an integer ranging from 1-5; —Z— is present or absent and represents —O—(CH2)x-, —C—(CH2)x-, —NR′—(CH2)x-, —SO—(CH2)x-, or —SO2—(CH2)x-, where x is 0 or 1 and R′ is hydrogen or a C1-C6 alkyl group, when —Z— is present, y is 1 and when it is absent, y is 2; Y is O—C+ or OR3, where R3 is hydrogen, or an optionally substituted alkyl or aryl group and C+ is a pharmacologically acceptable cation; R4 is hydrogen, a C1-C6 alkyl group, or OR′, where R′ is hydrogen or a C1-C6 alkyl group; R5 is hydrogen, or a C1-C6 alkyl group; and M represents a chemical species which is in the cis or trans position with respect to R1, and which is selected from the group consisting of P, B, BZ, D, E, and F as follows: where: W is O or C(R″) and each R″ for W groups is independently selected from the group consisting of hydrogen, halogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; and R6 and R7 are independently selected from hydrogen, halogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, a 6-10-member-ring heterocyclic aromatic group, a —COR″ group, a —COOR″ group, and a —CON(R″)2 group, wherein each R″ for R6 and R7 groups is independently selected from the group consisting of hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; where: Z2 is O, NR11 or S, where R11 is selected from the group consisting of hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, and a C2-C6 alkynyl group, wherein each group is optionally substituted; each R8 is independently selected from hydrogen, halogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, 6-10-member-ring heterocyclic aromatic group, a C1-C6 alkoxy group, a —S—C1-C6-alkyl group, a —CO—R′ croup, a —CO2R′ croup, a —CO—N(R′)2 group; a —N(R′)2 group, a —NR′—CO—R′ group, and a —NR′CO2—R′ group, wherein each R′ for R8 groups is independently selected from hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; and each R9 is independently selected from hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; each R10 is independently selected from the group consisting of a —CH2—X group, hydrogen, halogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, 6-10-member-ring heterocyclic aromatic group, a C1-C6 alkoxy group, a —S—C1-C6-alkyl group, a —CO—R′ group, a —CO2R′ group, a —CO—N(R′)2 group; a —N(R′)2 group, a —NR′—CO—R′ group, and a —NR′—CO2—R′ group, wherein each R′ for R10 groups is independently selected from hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; R12 is selected from the group consisting of X, hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, a 6-10-member-ring heterocyclic aromatic group, a C1-C6 alkoxy group, a —S—C1-C6-alkyl group, a —CO—R′ group, a —CO2R′ group, a —CO—N(R′)2 group; a —N(R′)2 group, a —NR′—CO—R′ group, and a —NR′—CO2—R′ group, wherein each R′ for R12 groups is independently selected from hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; R13 and R14 are independently selected from the group consisting of X, hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, a 6-10-member-ring heterocyclic aromatic group, a C1-C6 alkoxy group, a —S—C1-C6-alkyl group, a —CO—R′ group, a —CO2R′ group, a —CO—N(R′)2 group; a —N(R′)2 group, a —NR′—CO—R′ group, and a —NR′—CO2—R′ group, wherein each R′ for R13 and R14 groups is independently selected from hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C7-C19 aralkyl group, a 3-7-member-ring cyclic hydrocarbon group, a 3-7-member-ring heterocyclic group, a C6-C10 aromatic group, and a 6-10-member-ring heterocyclic aromatic group, wherein each of said groups is optionally substituted; wherein optional substitution includes substitution with one or more groups selected from a C1-C3 alkyl group, a C6-C12 aryl group, a C1-C3 haloalkyl group, I, Cl, Br, F, —CN, —OH, a C1-C3 alkoxy group, a —O-aryl group, a —O-benzyl group, a -phenoxy group, —SH, a —S—C1-C3-alkyl group, a —S-phenyl group, a —S-benzyl group, —NH2, and a —N(R16)2 group, where each R16 is a C1-C3 alkyl group, a benzyl group or a phenyl group; wherein X is a leaving group; wherein the compound contains one R2 and one M group; and wherein in structures B and Bz at least one R10 is a —CH2—X group, in structure E at least one R10 is a —CH2—X group, or R12 is X and in structure F one of R13 or R14 is X. |