C07C229/22

INDANE-AMINES AS PD-L1 ANTAGONISTS

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

INDANE-AMINES AS PD-L1 ANTAGONISTS

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Compound used as autophagy regulator, and preparation method therefor and uses thereof

It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators. ##STR00001##

a-CARBONYL ALKENYL ESTER PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20230242572 · 2023-08-03 ·

There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

a-CARBONYL ALKENYL ESTER PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20230242572 · 2023-08-03 ·

There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

BENZYLAMINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a benzylamine derivative, a preparation method therefor and use thereof, and in particular, to a benzylamine derivative as represented by general formula (I), or a pharmaceutically acceptable stereoisomer, salt, solvate or prodrug thereof, which has a strong binding capability with human PD-L1, can obviously inhibit the interaction of PD-1/PD-L1, and has significant anti-tumor efficacy in vivo. Therefore, the present invention also relates to a preparation method for the benzylamine derivative and use thereof in preparing a drug for treating PD-1/PD-L1-related diseases.

##STR00001##

BENZYLAMINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a benzylamine derivative, a preparation method therefor and use thereof, and in particular, to a benzylamine derivative as represented by general formula (I), or a pharmaceutically acceptable stereoisomer, salt, solvate or prodrug thereof, which has a strong binding capability with human PD-L1, can obviously inhibit the interaction of PD-1/PD-L1, and has significant anti-tumor efficacy in vivo. Therefore, the present invention also relates to a preparation method for the benzylamine derivative and use thereof in preparing a drug for treating PD-1/PD-L1-related diseases.

##STR00001##

Indane-amines as PD-L1 antagonists

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.