C07D273/08

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.

COMPOUNDS FOR INHIBITING BACTERIAL GROWTH VIA PHOSPHATIDYLGLYCEROL BINDING
20200261415 · 2020-08-20 ·

Antibacterial small molecule compounds, termed liptins, bind to phosphatidylglycerol in bacterial plasma membranes. The small molecule compounds comprise a three-dimensional complementary binding pocket for phosphatidylglycerol, disrupting membrane function in a bacteriostatic or bactericidal manner. Methods of inhibiting bacterial growth and/or treating Gram-positive or Gram-negative bacterial infection using such compounds are also disclosed.

COMPOUNDS FOR INHIBITING BACTERIAL GROWTH VIA PHOSPHATIDYLGLYCEROL BINDING
20200261415 · 2020-08-20 ·

Antibacterial small molecule compounds, termed liptins, bind to phosphatidylglycerol in bacterial plasma membranes. The small molecule compounds comprise a three-dimensional complementary binding pocket for phosphatidylglycerol, disrupting membrane function in a bacteriostatic or bactericidal manner. Methods of inhibiting bacterial growth and/or treating Gram-positive or Gram-negative bacterial infection using such compounds are also disclosed.

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.

Compounds for inhibiting bacterial growth via phosphatidylglycerol binding

Antibacterial small molecule compounds, termed liptins, bind to phosphatidylglycerol in bacterial plasma membranes. The small molecule compounds comprise a three-dimensional complementary binding pocket for phosphatidylglycerol, disrupting membrane function in a bacteriostatic or bactericidal manner. Methods of inhibiting bacterial growth and/or treating Gram-positive or Gram-negative bacterial infection using such compounds are also disclosed.

Compounds for inhibiting bacterial growth via phosphatidylglycerol binding

Antibacterial small molecule compounds, termed liptins, bind to phosphatidylglycerol in bacterial plasma membranes. The small molecule compounds comprise a three-dimensional complementary binding pocket for phosphatidylglycerol, disrupting membrane function in a bacteriostatic or bactericidal manner. Methods of inhibiting bacterial growth and/or treating Gram-positive or Gram-negative bacterial infection using such compounds are also disclosed.

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.