Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-04-10
1998-06-23
Powers, Fiona T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514321, 514338, 514364, 514374, 514381, 544138, 546199, 5462694, 548131, 548143, 548238, 548252, A61K 3141, C07D491048, C07D49504, C07D48704
Patent
active
057705984
DESCRIPTION:
BRIEF SUMMARY
This is a National Stage application of PCT/GB95/01,599 filed Jul. 6, 1995.
The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention formulations containing them and their use as anti-tumour agents.
Research in the area of cancer chemotherapy has produced a variety of anti-tumour agents which have differing degrees of efficacy. Standard clinically used agents include adriamycin, actinomycin D, methotrexate, 5-fluorouracil, cis-platinum, vincristine and vinblastine. However, these presently available anti-tumour agents are known to have various disadvantages, such as toxicity to healthy cells and resistance to certain tumour types. There thus exists a continuing need to develop new and improved anti-tumour agents. (1980), (2) 203-8, and khim Geterotsikl Soedin (1984), (10) 1366-70 respectively.
Kakhabrishvili et al, khim Geterotsikl Soedin (1985), (3) 355-8 disclose
EP447,703 discloses the synthesis of certain
L.Chunchatprasert et al, J.Chem.Soc., Perkin Trans I, 1779 (1992) disclose
There have now been discovered novel compounds which exhibit anti-tumour cell activity with low toxicity against normal cell lines.
Thus, in a first aspect the present invention provides a compound of the general formula (I) ##STR1## and salts and physiologically functional derivatives thereof, wherein A) is ##STR2## X is O, S, SO, SO.sub.2, CH.sub.2, CO or NR.sup.7, wherein R.sup.7 is H or the following groups which may be optionally substituted: cycoalkyl, cycloalkenyl, alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aroyl, alkylsulphonyl or arylsulphonyl; containing 1 to 4 heteroatoms wherein the 5- or 6- membered ring may be aromatic or non-aromatic. alkynyl, alkoxy, (wherein alkyl, aryl, alkenyl, alkynyl, and alkoxy can be substituted), CHO, COR.sup.8, COOR.sup.8 wherein R.sup.8 is hydrogen or is a C-.sub.1-10 optionally substituted hydrocarbyl group which may contain one or two oxygen atoms; CHO, COR.sup.8, CO.sub.2 R.sup.8, CONHR.sup.8, CONR.sup.8 R.sup.9, alkoxy, halo, cyano, nitro, amino, alkyl amino, dialkyl amino, carboxyl wherein R.sup.9 is alkyl, aryl or aralkyl. following groups which may be optionally substituted: alkyl, aryl, aryloxy, aralkyloxy, alkoxy, aralkyl. R.sup.10 wherein R.sup.10 is optionally substituted alkyl or aryl, or R.sup.6 is alkyl, aralkyl, or aryl wherein alkyl, aralkyl or aryl may be optionally substituted.
Suitably X is O, S, SO, SO.sub.2, CH.sub.2, CO or NR.sup.7 wherein R.sup.7 is suitably H, alkyl, aralkyl, aryl, alkenyl, acyl, alkynyl or optionally substituted sulphonyl;
Suitably R.sup.1 is an optionally substituted five or six-membered heterocyclic ring containing one or two nitrogen atoms and optionally one other heteroatom.
Suitably R.sup.2 is H, alkyl or COOR.sup.8 wherein R.sup.8 is as defined above;
Suitably R.sup.3 and R.sup.4 are independently H, hydroxy, alkyl, haloalkyl, alkoxy, halo, cyano, nitro, amino, alkylamino, dialkylamino or substituted alkyl;,
Suitably R.sup.5 is H, alkyl, substituted alkyl, aryl, aralkyl, nitro, halo, cyano or CHO;
Suitably R.sup.6 is H, alkyl, aralkyl, nitro, halo, CHO or COR.sup.10 wherein R.sup.10 is suitably alkyl or aryl.
Alkyl groups may be straight or branched chain alkyl groups, and may contain 1-10 carbon atoms and suitably 1-6 carbon atoms. Examples of such alkyl groups include methyl, ethyl, t-butyl and the like.
Alkenyl groups may be straight or branched chain alkenyl groups, and may contain 2-10 carbon atoms and suitably 2-6 carbon atoms. Examples of such alkenyl groups include ethenyl, butenyl and the like.
Alkynyl groups may be straight or branched chain alkynyl groups, and may contain 2-10 carbon atoms and suitably 2-6 carbon atoms. Examples of such alkynyl groups include ethynyl, propynyl and the like.
Haloalkyl groups may be straight or branched chain haloalkyl groups and may contain 1-10 carbon atoms and suitably 1-6 carbon atoms. Such groups may contain one or more halo atoms. Examples of haloalkyl groups include trifluoromethyl, and the like.
Acyl gr
REFERENCES:
patent: 5679694 (1997-10-01), Franzmann et al.
Barraclough Paul
Chunchatprasert Laddawan
Debont Pierre P. M.
Hudson Alan T.
Miller David D.
Powers Fiona T.
University College Cardiff Consultants Limited
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