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1. (WO2017032983) PIPERIDINOBENZODIAZEPINE COMPOUNDS WITH ANTI PROLIFERATIVE ACTIVITY

Pub. No.:    WO/2017/032983    International Application No.:    PCT/GB2016/052565
Publication Date: Fri Mar 03 00:59:59 CET 2017 International Filing Date: Sat Aug 20 01:59:59 CEST 2016
IPC: C07D 403/12
C07D 403/14
C07D 409/12
C07D 409/14
A61K 31/5513
A61P 35/00
Applicants: FEMTOGENIX LIMITED
Inventors: JACKSON, Paul Joseph Mark
THURSTON, David Edwin
RAHMAN, Khondaker Mirazur
Title: PIPERIDINOBENZODIAZEPINE COMPOUNDS WITH ANTI PROLIFERATIVE ACTIVITY
Abstract:
The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7-6-membered rings linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents. PDDs may be represented by formula (I): and salts and solvates thereof, wherein the dotted lines indicates the optional presence of a double bond between one or more of Ci and C2, C2and C3, and C3and C4; R1 and R2 are substituent groups; R3 is selected from H, C1-12 alkyl and CH2Ph; R4is selected from phenyl and C5-9heteroaryl groups optionally substituted, with the proviso that the optionally substituted C5-9heteroaryl is not indolyl; R19is selected from H and (CH2)t-NR20R21; Yiis N or CH; Y2 is N or CH; and wherein at least one of Y1and Y2 is CH; p is o or1; X1 is a connecting group; L is a linker group; X2 is a connecting group or is absent; q is selected from o,1, 2, 3,4,5and 6; A is selected from: for each Ai group one of Y3and Y4is selected from N-R17,S and O; and the other of Y3and Y4is CH; and Y5is selected from CH, N, S and COH; for each A2group one of Y6and Y7is independently selected from N and CH; and the other of Y6and Y7is CH; R13, R14, R17, R2oand R2iare independently selected from H and C1-6alkyl; and either: (i) R5and R6together form a double bond; (ii) R5is H and R6is OH; or (iii) R5is H and R6is OC1-6alkyl; with the proviso that when p is o and A is Ai, then: (a) for at least one Ai group one of Y3and Y4is selected from S and O; or (b) for at least one Ai group Y5is S; or (c) R4is not pyrrolyl, imidazolyl, optionally substituted pyrrolyl or optionally substituted imidazolyl.