The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.

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.

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.

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.

Compositions are disclosed herein that include macrocycle derivatives incorporating bridged macrocycles. Also disclosed are methods of producing and using the compositions.

Compositions are disclosed herein that include macrocycle derivatives incorporating bridged macrocycles. Also disclosed are methods of producing and using the compositions.

This invention relates to methods for oligonucleotide synthesis, specifically the synthesis of oligonucleotides that contain a high content of guanine monomers. In more detail, the invention relates to a method for coupling a nucleoside phosphor amidite during the synthesis of an oligonucleotide to a universal support, to a first nucleoside, or to an extending oligonucleotide.

This invention relates to methods for oligonucleotide synthesis, specifically the synthesis of oligonucleotides that contain a high content of guanine monomers. In more detail, the invention relates to a method for coupling a nucleoside phosphor amidite during the synthesis of an oligonucleotide to a universal support, to a first nucleoside, or to an extending oligonucleotide.

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.