The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001##
In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is: ##STR00001##
R.sub.1 represents ?CH.sub.2O.sup.tBu or ?CH(CH.sub.3)O.sup.tBu, R.sub.3 represents ?CH.sub.2C(O)NHCPh.sub.3, ?CH.sub.2CH.sub.2C(O)NHCPh.sub.3, ?CH.sub.2C(O)O.sup.tBu, or ?CH.sub.2CH.sub.2C(O)O.sup.tBu, and Aaa is an amino acid residue selected from Thr and Ser; wherein the C-terminus thereof is esterified, and wherein the hydroxy moiety of the side chain of Thr or Ser is substituted with tbutyl; the base is triethylamine; and the solvent is tetrahydrofuran.

The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is: ##STR00001##
R.sub.1 represents ?CH.sub.2O.sup.tBu or ?CH(CH.sub.3)O.sup.tBu, R.sub.3 represents ?CH.sub.2C(O)NHCPh.sub.3, ?CH.sub.2CH.sub.2C(O)NHCPh.sub.3, ?CH.sub.2C(O)O.sup.tBu, or ?CH.sub.2CH.sub.2C(O)O.sup.tBu, and Aaa is an amino acid residue selected from Thr and Ser; wherein the C-terminus thereof is esterified, and wherein the hydroxy moiety of the side chain of Thr or Ser is substituted with tbutyl; the base is triethylamine; and the solvent is tetrahydrofuran.

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

Methods of making a compound according to the following scheme: ##STR00001##
wherein: R.sub.1 is a side chain of an amino acid residue selected from Ala, Ser, Thr and Leu; R.sub.2 is a side chain of an amino acid residue selected from Asp, Glu, Gln and Asn; [Aaa] is an amino acid residue selected from Ser, Asp, Ala, Ile, Phe, Trp, Lys, Glu and Thr; R.sub.3 is hydrogen or alkyl; Each of R.sub.4 and R.sub.4 independently is hydrogen or alkyl; Both R.sub.a and R.sub.a are hydrogen; or together are an oxo(O) group; Both R.sub.b and R.sub.b are hydrogen; or together are an oxo (O) group; L is ##STR00002## X is CH.sub.2, O or S; R.sub.5 is hydrogen or alkyl; m is an integer from 1 to 3; and n is an integer from 2 to 20.

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.