Method of using diketopiperazines and composition containing them

A method of inhibiting inflammation comprising administering to an animal in need thereof an effective amount of a compound of the formula:

• 7
• wherein:
• R1 is —CH2COR3, or —CH2CH2COR3;
• R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threorine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and omithine;
• R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4;
• and
• each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl;
• or
• a physiologically-acceptable salt thereof.

A method of inhibiting aggregation of platelets comprising contacting the platelets with an effective amount of a compound of the formula:

• 8
• wherein:
• R1 is —CH2COR3, or —CH2CH2COR3;
• R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and omithine;
• R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4;
• and
• each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl;
• or
• a physiologically-acceptable salt thereof.

A method of inhibiting the production, release or both of interleukin 8 by cells comprising contacting the cells with an effective amount of a compound of the formula:

• 9
• wherein:
• R1 is —CH2COR3, or —CH2CH2COR3;
• R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and ornithine;
• R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4;
• and
• each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl;
• or
• a physiologically-acceptable salt thereof.

A method of inhibiting the effects of platelet activating factor (PAF) comprising contacting the PAF with an effective amount of a compound of the formula:

• 10
• wherein:
• R1 is —CH2COR3, or —CH2CH2COR3;
• R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and ornithine;
• R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4;
• and
• each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl;
• or
• a physiologically-acceptable salt thereof.

A pharmaceutical composition comprising a pharmaceutically-acceptable carrier and a compound of the formula:

• 11
• wherein:
• R1 is —CH2COR3, or —CH2CH2COR3;
• R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and ornithine;
• R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4;
• and
• each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl, or
• a physiologically-acceptable salt thereof.