Abstract: Novel compounds of formula (I) are described wherein: R1=(CH2)mCH3 where m is 0 or an integer in the range from 1 to 16, or an alkenyl, alkynyl, alkoxy, alkylthio, or alkyl sulfinyl group having from 2 to 17 carbon atoms; R2=H, CH3 or CH2CH3; R3=H or CH3; R4H or CH3; R5=lower alkyl having from 1 to 5 carbon atoms; n is an integer in the range from 1 to 3, and X is carboxyl (COOH) or carbalkoxy (COOR5), cyano (C?N), phosphonic acid (PO3H2), phosphonate ester (PO3[R5]2) or 5-tetrazole, and pharmaceutically acceptable salts thereof. Preferably, the compounds are optically pure enantiomers of the R— or S—configuration in which R3=R4=R5=H, R2=CH3 and R1 is a saturated aliphatic chain of one to five carbon atoms.

Abstract: Antineoplastic drug modulators are described. The specific modulators referred to are propargylamines which can enhance the cytotoxic effects of antineoplastic drugs on cancer cells while protecting normal cells from damage. The propargylamine modulators can be used to increase the selectivity and effectiveness of conventional antineoplastic drugs, to reduce the unwanted side-effects of cancer chemotherapy, to improve effectiveness of cancer chemotherapy, to improve treatment of cancers for which treatment is otherwise ineffective, to improve therapy of cancers otherwise unresponsive or poorly responsive due to drug-resistance and/or toxicity limited treatment regimens and to render effective chemotherapy for previously untreatable cancers.

Abstract: The present invention relates to the use of a group of propargylamines of the general formula (I) wherein R1 is hydrogen or CH3 and R2 is (CH2)nCH3 and n is an integer from 0 to 16, and salts thereof, as cellular rescue agents in the treatment and prevention of diseases in which cell death occurs by apoptosis. Some of the compounds of formula I are novel. The invention is also directed to the use of these compounds in the treatment of these diseases, as well as to processes for the preparation of the compounds.

Abstract: The present invention relates to the use of a group of propargylamines of the general formula (I) ##STR1## wherein R.sup.1 is hydrogen or CH.sub.3 and R.sup.2 is (CH.sub.2).sub.n CH.sub.3 and n is an integer from 0 to 16, and salts thereof, as cellular rescue agents in the treatment and prevention of diseases in which cell death occurs by apoptosis. Some of the compounds of formula I are novel. The invention is also directed to the use of these compounds in the treatment of these diseases, as well as to processes for the preparation of the compounds.