Abstract: The invention relates to a compound of formula (I) or formula (II) or pharmaceutically acceptable salts, solvates, tautomers, stereoisomers or mixtures thereof; which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate and in the treatment of proliferative diseases.

Abstract: The invention relates to substituted pyrridinobenzodiazepines (PDDs) of formula (XV) and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.

Abstract: The invention relates to compound of formula (I): A-X1-L-X2-B??(I) and salts, solvates and tautomers thereof, which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate; wherein A is a group selected from: X1 and X2 are independently selected from O, S, NR28, CR28R29, CR28R29O, C(?O), C(?O)NR28, NR28C(?O), C(O)—RA—C(O)—NH, C(O)—RA—NH—C(O), C(O)—NH—RA—C(O), NH—C(O)—RA—C(O), NH—C(O)—RA—C(O)—NH, NH—C(O)—RA—NH—C(O), C(O)—NH—RA—NH—C(O), C(O)—NH—RA—C(O)—NH, O—C(O) and C(O)—O or is absent; L is selected from an amino acid, a peptide chain having from 2 to 12 amino acids, a paraformaldehyde chain —(OCH2)1-24—, a polyethylene glycol chain —(OCH2CH2)1-12— and —(CH2)m—Y6—(CH2)n— wherein Y6 is selected from —(CH2)z— and a group (L1) a group (L1) that is selected from arylene, monocyclic heteroarylene, monocyclic cycloalkylene, monocyclic cycloalkenylene and monocyclic heterocyclylene groups optionally substituted with up to three optional subst

Abstract: The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, —C(?NR?)—NR?R? or —CH2—CH?CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.

Abstract: The invention relates to a compound of formula (I) or formula (II) or pharmaceutically acceptable salts, solvates, tautomers, stereoisomers or mixtures thereof; which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate and in the treatment of proliferative diseases.

Abstract: The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, —C(?NR?)—NR?R? or —CH2—CH?CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infractions, such as drug-resistant bacterial infections.

Abstract: Disclosed are compounds comprising alkylating moieties, such as pyrrolobenzodiazepines (PBDs, comprising three fused 6-7-5-membered rings), C2-substituted PBDs (including C2-endo, C1/C2-endo, and C2/C3-endo PBDs), pyrridinobenzodiazepines (PDDs, comprising three fused 6-7-6-membered rings), indolinobenzodiazapenes (IBDs, comprising four fused 6-7-5-6 membered rings), and tetrahydroisoquinolinebenzodiazapines (QBDs, comprising four fused 6-7-6-6 membered rings), or a pharmaceutically acceptable salt thereof. In particular, the disclosed compounds, or a pharmaceutically acceptable salt thereof, may comprise a guanine alkylating moiety linked to an aromatic group. The disclosed compounds are useful as medicaments, in particular as anti-proliferative agents.

Abstract: The invention relates to a compound of formula (I) or formula (II) or pharmaceutically acceptable salts, solvates, tautomers, stereoisomers or mixtures thereof; which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate and in the treatment of proliferative diseases.

Abstract: The invention relates to compounds comprising a substituted pyrrolo-, indolino- or tetrahydroisoquinoline-benzodiazepines alkylating moiety linked via the A-ring to aromatic groups of formula (Ia), and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.

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, in particular as anti-proliferative agents. PDDs may be represented by formula (I) and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to novel derivatives of formula (I) where R1, R2, R3, R4, R5, X and m are as defined in the specification. These compounds which have therapeutic activity, in particular, as STAT3 inhibitors and so are useful in the treatment of proliferative diseases or conditions such as cancer. Methods for producing these compounds, novel intermediates used in the methods, pharmaceutical compositions containing them and their use in therapy form further aspects of the invention.

Abstract: The invention relates to pyrrolobenzodiazepines compounds (PBDs) and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular, to treat bacterial infections.

Abstract: The invention relates to compounds comprising a substituted pyrrolo-, indolino- or tetrahydroisoquinoline-benzodiazepines alkylating moiety linked via the A-ring to aromatic groups of formula (Ia), and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.

Abstract: The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7- 6-membered rings and to benzopyrridodiazecines (BPDs) comprising three fused 6-8- 6-membered rings and, in particular, to PDD or BPD dimers linked together or PDD and BPD monomers linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents.

Abstract: The invention relates to compound of formula (I): A-X1-L-X2—B?? (I) and salts, solvates and tautomers thereof, which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate; wherein A is a group selected from: X1 and X2 are independently selected from O, S, NR28, CR28R29, CR28R29O, C(?O), C(?O)NR28, NR28C(?O), C(O)—RA—C(O)—NH, C(O)—RA—NH—C(O), C(O)—NH—RA—C(O), NH—C(O)—RA—C(O), NH—C(O)—RA—C(O)—NH, NH—C(O)—RA—NH—C(O), C(O)—NH—RA—NH—C(O), C(O)—NH—RA—C(O)—NH, O—C(O) and C(O)—O or is absent; L is selected from an amino acid, a peptide chain having from 2 to 12 amino acids, a paraformaldehyde chain —(OCH2)1-24—, a polyethylene glycol chain —(OCH2CH2)1-12— and —(CH2)m—Y6—(CH2)n— wherein Y6 is selected from —(CH2)z— and a group (L1) a group (L1) that is selected from arylene, monocyclic heteroarylene, monocyclic cycloalkylene, monocyclic cycloalkenylene and monocyclic heterocyclylene groups optionally substituted with up to three optional subst

Abstract: The invention relates to pyrrolobenzodiazepines compounds (PBDs) and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular, to treat bacterial infections.

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.

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.

Abstract: The invention relates to pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) of formula (I) and in particular to PBD dimers linked through the C1 position, and PBD monomers linked through the C1 position to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.

Abstract: The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7-6-membered rings and to benzopyrridodiazecines (BPDs) comprising three fused 6-8-6-membered rings and, in particular, to PDD or BPD dimers linked together or PDD and BPD monomers linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents.