The University of Edinburgh

University of Warwick

Other

Peter John Sadler

Abraha Habtemariam

Haimei Chen

Duncan Jodrell

Robert Edward Morris

Ying Fu

Philippe Muller

Joan Josep Soldevila

Ana Maria Pizarro

Zhe Liu

Philippe Müller

The present invention relates to the use of certain osmium containing complexes such as cytotoxic agents particularly for the treatment of cancer. There is also provided novel osmium containing complexes, as well as pharmaceutical formulations comprising such complexes.

Osmium (II) arene imino anti-cancer complexes

The present invention relates to novel iridium and/or rhodium containing complexes for use as a cytotoxic, such as an anti-cancer agent. There is also provided a method of preparing said compounds.

Iridium/rhodium anti-cancer compounds

Osmium (II) arene azo anti-cancer complexes

The present invention provides a compound of formula (I): Pt(N)XXYY, wherein Xand Xare the same or different and each one is a group NRRRwherein R, Rand Rare the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or Xand Xtogether represent a group RRNRNRRwherein Rand Rhave the same meaning as before, and Rrepresents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or Ror two or more of R, R, Rand Rand the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Yand Yare the same or different or when cis together represent a divalent moiety Y, wherein at least one of Yand Y, or Y, is a substantially labile ligand in the analogous Pt(II) complex without the azide groups, whilst being substantially resistant, in vivo, to hydrolysis and physiological reducing agents. One or more of R, R, Rand R, may further represent a covalently bonded link to at least one further complex of formula (I) to form a dimer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type.

Photoreactive compounds and compositions

Ruthenium (II) compounds of formula (I) are useful in the treatment and/or prevention of cancer 

Ruthenium compounds

The present invention provides a compound of formula (I): Pt(N)XXYY, wherein Xand Xare the same or different and each one is a group NRRRwherein R, Rand Rare the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or Xand Xtogether represent a group RRNRNRRwherein Rand Rhave the same meaning as before, and Rrepresents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or Ror two or more of R, R, Rand Rand the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Yand Yare the same or different or when cis together represent a divalent moiety Y, wherein at least one of Yand Y, or Y, is a substantially labile ligand in the analogous Pt(II) complex without the azide groups, while being substantially resistant, in vivo, to hydrolysis and physiological reducing agents. One or more of R, R, Rand R, may further represent a covalently bonded link to at least one further complex of formula (I) to form a dimer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type.

Ruthenium (II) compounds of the formula:wherein: Ris &#x2014;COCH; R, R, R, Rand Rindependently represent H, alkyl, cylcoalkyl, &#x2014;COR', aryl or alkylaryl, which latter two groups are optionally substituted on the aromatic ring; R&#x2032; represents alkyl, cylcoalkyl, aryl or alkaryl; X is halo, HO, (R&#x2032;)(R&#x2033;)SO, R&#x2032;COor (R&#x2032;)(R&#x2033;)C&#x2550;O, where R&#x2033; represents alkyl, cylcoalkyl, aryl or alkaryl; Y is a counterion; m is 0 or 1; q is 1, 2 or 3; C&#x2032; is Cto Calkylene, optionally substituted in or on the alkylene chain, bound to two A groups; p is 0 or 1 and r is 1 when p is 0 and r is 2 when p is 1; and A and B are: each independently R&#x2014;CN, where R&#x2033; represents alkyl or cycloalkyl; or B is halo and A is 4-substitued pyridine; or p is 0, A is NRRand B is NRRwherein R, R, Rand Rindependently represent H, or alkyl, and A and B are linked by an alkylene chain, optionally substituted in or on the alkylene chain; or p is 1, A is NRand B is NRR, wherein R, Rand Rare as previously defined, and A and B are linked by an alkylene chain, optionally substituted are described.

Half-sandwich ruthenium (II) compounds comprising nitrogen containing ligands for treatment of cancer

Compounds which may be used in the treatment and/or prevention of cancer have the formula (I): wherein Rand Rtogether with the ring to which they are bound represent a saturated or unsaturated carbocyclic or heterocyclic group

Ruthenium (II) compounds for use in the therapy of cancer

Compounds which may be used in the treatment and/or prevention of cancer have the formula (I) wherein: R , R , R , R , R and R independently represents H, alkyl, &mdash;CO R&prime;, aryl or akylaryl, which latter two groups are optionally substituted on the aromatic ring; R&prime; represent alkyl, aryl or alkaryl; X is halo, H O, (R&prime;)(R&Prime;)SO, R&prime;CO &mdash; or (R&prime;)(R&Prime;)C&boxH;O, where R&Prime; represents alkyl, aryl or alkaryl; Y is a counterion; m is 0 or 1; q is 1, 2 or 3; C&prime; is C to C alkylene, optionally substituted in or on the alkylene chain, bound to two A groups; p is 0 or 1 and r is 1 when p is 0 and r is 2 when p is 1; and A and B are: each independently N-donor nitrile ligands; or B is halo and A is an N-donor pyridine ligand, optionally substituted at one or more of the carbon atoms of the pyridine ring; or p is 0, A is NR R and B is NR R , wherein R , R , R and R independently represent H or alkyl, and A and B are linked by an alkylene chain, optionally substituted in or on the alkylene chain, or p is 1, A is NR and B is NR R , wherein R , R and R are as previously defined, and A and B are linked by an alkylene chain, optionally substituted.

Growing community of inventors

Penicuik, United Kingdom

Peter John Sadler