C07D273/00

ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS

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

Anthelmintic depsipeptide compounds

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

Anthelmintic depsipeptide compounds

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

CONJUGATED LIPOMERS AND USES THEREOF

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.

CONJUGATED LIPOMERS AND USES THEREOF

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.

Anthelmintic depsipeptide compounds

Cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds are provided that are effective against parasites that harm animals, including humans. The compounds and compositions may be used for combating parasites in or on animals including mammals and birds. Also provided are improved methods for eradicating, controlling and preventing parasite infestation in animals, including birds and mammals.

Anthelmintic depsipeptide compounds

Cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds are provided that are effective against parasites that harm animals, including humans. The compounds and compositions may be used for combating parasites in or on animals including mammals and birds. Also provided are improved methods for eradicating, controlling and preventing parasite infestation in animals, including birds and mammals.

1,2,4-Oxadiazole Derivatives as Immunomodulators

The present invention relates to methods of modulating an immune response mediated by a PD-1 signaling pathway and of treating a cancer or an infectious disease. A subject is administered a compound(s) or a pharmaceutically acceptable salt or pharmaceutically acceptable composition thereof of formula (I)

##STR00001##

In the ring Q is S or O. R.sub.1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R.sub.3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R.sub.2 is hydrogen or CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R.sub.4 and R.sub.5 are independently hydrogen or absent. R.sub.6 is hydrogen, alkyl or acyl.

1,2,4-Oxadiazole Derivatives as Immunomodulators

The present invention relates to methods of modulating an immune response mediated by a PD-1 signaling pathway and of treating a cancer or an infectious disease. A subject is administered a compound(s) or a pharmaceutically acceptable salt or pharmaceutically acceptable composition thereof of formula (I)

##STR00001##

In the ring Q is S or O. R.sub.1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R.sub.3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R.sub.2 is hydrogen or CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R.sub.4 and R.sub.5 are independently hydrogen or absent. R.sub.6 is hydrogen, alkyl or acyl.

1,2,4-oxadiazole derivatives as immunomodulators

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.