Aliphatic propargylamines as cellular rescue agents
AssigneeUniversity of Saskatchewan
InventorsDavid Durden, Alick Paterson, Bruce Davis, Lillian Dyck, Peter Yu, Xinmin Li, Alan Boulton
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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.
Claims8
A composition for the treatment of a disease in which cell death occurs by apoptosis, which composition comprises an effective amount of a compound having the formula I:
- wherein
- R1=H, CH3
- R2=CH3(CH2)n
- and n represents an integer in the range from 0 to 16, with the provisos that
- (i) if R1 is H, then n is not 4 or less;
- (ii) if R1 is CH3 then n i s not 0;
- and
- (iii) if R1 is CH3 and n is 1 or 4, then the compound of formula (I) is in the form of a substantially pure enantiomer;
- or a pharmaceutically acceptable salt thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant.
A method for the treatment of acute and chronic diseases in which cell death occurs by apoptosis or for the treatment of premature degeneration of cells in mammalian subjects, said method comprising administering to a patient in need thereof an effective amount of a compound having the formula I:
- wherein
- R1=H, CH3;
- R2=CH3(CH2)n;
- and n represents an integer in the range from 0 to 16 provided that if R1 is methyl and R2 is not methyl the compound of formula (I) is in substantially enantiomerically pure form in the R-configuration, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.