New platinum complexes obtained by reacting platinum compound and amine compound, useful as anticancer agent

摘要

Platinum complexes (I) are new. Platinum complexes of formula (R1-Pt(R2)(X)(-O-(CH 2) n-O-W1-Z)(L1)-L2) (I) are new. X : halo; either R1 : R1aNH 2or 2-picoline directly related to the platinum by its nitrogen atom; and R2 : R2aNH 2, where R1 and R2 are cis configuration relative to platinum; or R1 and R2 together with the platinum atom : 5-7 membered ring of formula (A); R1a, R2a : H, 1-6C alkyl, 1-6C alkenyl or 3-8C cycloalkyl; either L1, L2 : halo, where L1 and L2 is in cis position with respect to the platinum; or L1 and L2 together with the platinum : 5-7 membered ring of formula (B), (both the ring (A) and/or (B) are optionally substituted with at least one 4C alkyl, optionally fused by two carbon atoms together with 4-8C cycloalkyl or saturated 4-8C mono or bicyclic heterocycloalkyl, and optionally spiro-substituted with 4-8C cycloalkyl or saturated 4-8C mono or bicyclic heterocycloalkyl); V1 : CH 2, C(O) or P(O)OH; Y1 : a bond or (CR1R2) 1-2; R1, R2 : H or 1-4C alkyl; W1 : single bond, -C(O)-(CH 2) m-NH-C(O)- or -C(O)-(CH 2) mC(O)-NH-group attached to (CH 2) nby the group C(O); n, m : 2-4; and Z : a fragment of a targeting agent attached to W1 may to be recognized by a tumor cell and such that ZH is a bile acid or a polyunsaturated fatty acid (when W1 represents a single bond) and Z-COOH or NH 2is antibody, a peptide, a sugar, a hormone, vitamin, folic acid, biotin, an endogenous or synthetic ligand of a receptor overexpressed on the surface of a tumor cell. An independent claim is included for use of (I) as precursor of platinum compound of formula (R1-Pt(R2)(X)(-O-(CH 2) n-OH)(L1)-L2) (II) and platinum complex of formula (R1-Pt(R2)(L1)-L2) (III). [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.