Abstract: The invention provides compounds of formula (IA) and compounds of formula (IB) and pharmaceutically acceptable salts thereof; wherein A is selected from group (A1) and group (A2): wherein #1 is attached to the carbon atom forming the oxime moiety and wherein group (A1) is optionally substituted by one or two R10 and group (A2) is optionally substituted by one R10, and wherein R1, X, R2 and R10 are as defined in the claims, as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.

Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A1 is —N? or —C(R3)=; A2 is —N? or —CH?; L is —NH—; B1 and B2 are independently —N? or —C(R2b)=; B3 and B4 are independently —C(R2b)=; no more than one R2b on B1, B2, B3 and B4 is other than hydrogen; R1a is hydrogen, halogen, C1-C3alkyl (n-alkyl) optionally substituted with one R4, or R1a is —NH2, —NH(C1-C3alkyl (n-alkyl)), —NH(C(?O)—C1-C2alkyl), —N(C1-C3alkyl (n-alkyl))2, —OC1-C3alkyl (n-alkyl), C1-C3haloalkyl (n-alkyl) or —OC1-C3haloalkyl (n-alkyl); R1b is hydrogen, halogen, C1-C3alkyl (n-alkyl), —OC1-C3alkyl (n-alkyl), —NH2, —NH(C1-C3alkyl (n-alkyl)) or —N(C1-C3alkyl (n-alkyl))2; R1a and R1b may together form a —CH?CH—CH?CH— moiety in which one or two non-adjacent CH are optionally replaced by N; R2a is halogen, C1-C6alkyl, C1-C6haloalkyl, cyclopropyl, cyclobutyl, —OR6, —NHC(?O)—C3-C6cycloalkyl, Cycle Q, —SF5 or group Y (formula (Y)); wherein X is a 3- or 4-membered carbocyclic ring and R8 is halogen, cy

Abstract: The invention provides compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof (I) wherein ring A represents group A-I or A-II (A-I, A-II) A1, A2, A3, A4 represent independently C(R4aa) or N, wherein no more than one of A1, A2, A3, and A4 represents N; A5 represents C(R4b) or N; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a and R4aa and R4b are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.

Abstract: A process for the production of a compound of formula (I) wherein ALINKERB represents a linker moiety of formula (V): A[G1-G2*-G3]B; wherein A and B indicate the orientation of the group of formula (V) in formula (I); G1, G2 and G3 have specific meanings described herein and may be present or absent, with the proviso that at least one of G1 or G3 is present; which linker group may furthermore optionally contain one or more groups of formula (VI); and/or other substituents; and R1 represents hydrogen or a C1-C4-alkyl group; R2 represents hydrogen or a C1-C4-alkyl group; R3 independently at each occurrence, represents hydrogen or a C1-C4-alkyl group; x is 0 or 1; y is 0 or 1; z independently at each occurrence, is 0 or 1; and (—) represents a single bond between a primary, secondary or tertiary carbon atom of the moiety ALINKERB and the adjacent nitrogen atom; in which process (A) a compound of formula (II) is reacted with a compound of formula (III) wherein Pr represents an amino protecting group selected from