Femtogenix Limited

Paul Joseph Mark Jackson

David Edwin Thurston

Khondaker Mirazur Rahman

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. 

Cytotoxic agents

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. 

Anti-liferative agents comprising substituted benzo[e]pyrido[1,2-a][1,4]diazepines

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. 

Substituted 6a,7,8,9,10,12-hexahydrobenzo[e]pyrido[1,2-a][1,4]diazepines as anti-proliferative agents

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. PDDs and BPDs may be represented by formula (I): and salts or solvates thereof, wherein R, R-Rand Rare independently selected substituent groups; and either: (i) Rand Rtogether form a double bond; (ii) Ris H and Ris OH; or (iii) Ris H and Ris ORand Ris Calkyl; wherein each of m, n, u and w may be 0 or 1; where (a) the compound is a dimer with each monomer being the same or different and being of formula (I) where one of R, R, Rand Rof the first monomer and one of R', R&#x2032;, Rand R&#x2032;of the second monomer form together a bridge having the formula &#x2014;X-L-X&#x2032;&#x2014; linking the monomers and m+n+u+w=1; or (b) a dimer and one of R, Rand Rof the first monomer and one of R&#x2032;, R&#x2032;and Rof the second monomer form together a bridge having the formula &#x2014;X-L-X&#x2032;&#x2014; linking the monomers and m=n=u=w=o; or (c) one of R, R, Rand Rhas the formula: &#x2014;X-L-X&#x2032;-D or &#x2014;(CH)f-O&#x2014;Rand m+n+u+w=o or 1; or (d) Rhas the formula: &#x2014;X-L-X&#x2032;&#x2014; D or &#x2014;(CH)&#x2014;O&#x2014;and m+n+u+w=1; and X-L-X&#x2032;&#x2014; is a linker group and D has the formula (II) or (III). 

Pyrridinobenzodiazepine and benzopyrridodiazecine compounds

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. (I) and salts or solvates thereof, wherein: the dotted lines indicates the optional presence of a double bond between C1 and C2 or C2 and C3; R-Rare independently selected substituent groups; and either: (i) Rand Rtogether form a double bond; (ii) Ris H and Ris OH; or (iii) Ris H and Ris ORand Ris Calkyl; where Rhas the formula: -X-L-X'-D-X-L-X&#x2032;- is a linker group and D has the formula (II) or (III): or where the compound is a dimer with each monomer being the same or different and being of formula (I) where the Rof the first monomer and R&#x2032;or R&#x2032;of the second monomer, or Rof the first monomer and R&#x2032;of the second monomer, form together a bridge having the formula -X-L-X&#x2032;- linking the monomers. 

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London, United Kingdom

Paul Joseph Mark Jackson