Abstract: The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.

Abstract: The present invention relates to method of modulating TIGIT signaling pathway and PD-1 signaling pathway. The invention also encompasses the use of the compound of formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof for the treatment of diseases or disorders mediated by both TIGIT signaling pathway and PD-1 signaling pathway.

Abstract: The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) In the formula Q is O, R1 is the side chain of Ser, R2 is —CO-Thr, R3 is the side chain of Asn or Glu, and R4, R5 and R6 are each H.

Abstract: The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.

Abstract: 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) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.

Abstract: The present invention provides a method of treating a disease or disorder with at least one SMARCA2/4 degrader, in a subject who are responders to such treatment based on the presence of tumor specific alterations described therein. The present invention also provides the methods for treating prostate cancer in the subjects who are likely to respond to treatment with SMARCA2/4 degraders.

Abstract: The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) inhibitors or as dual inhibitors of TIM-3 and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by TIM-3, PD-1, PD-L1, and/or PD-L2.

Abstract: The present invention relates to 1,2,4-oxadiazole and thiadiazole compounds of formula (1) and their use to inhibit the programmed cell death 1 (PD1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

Abstract: The present invention relates to 1,2,4-oxadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

Abstract: The present disclosure relates to methods comprising administering compounds that inhibit VISTA and PD-1 (e.g., PD-1, PD-L1, or PD-L2) pathways with a compound that inhibits TIM-3 and PD-1 (e.g., PD-1, PD-L1, or PD-L2) pathways. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by VISTA, TIM-3, PD-1, PD-L1, and/or PD-L2.

Abstract: 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) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.

Abstract: The present invention relates to a composition of a CD47-SIRP? blocking agent and one or more anti-cancer agent(s), where the CD47-SIRP? blocking agents are represented by a compound of formula (I). The present invention also relates to a method of treating a cancer in a subject by administering a therapeutically effective amount of a CD47-SIRP? blocking agent represented by formula (I) in combination with one or more anti-cancer agent(s).

Abstract: 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) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.

Abstract: The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as V-domain immunoglobulin suppressor of T-cell activation (VISTA) inhibitors or as dual inhibitors of VISTA and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by VISTA and its ligands, PD-1, PD-L1, and/or PD-L2.

Abstract: The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases oR disorders mediated by CD47.

Abstract: 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) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.

Abstract: The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is: R1 represents ?CH2OtBu or ?CH(CH3)OtBu, R3 represents ?CH2C(O)NHCPh3, ?CH2CH2C(O)NHCPh3, ?CH2C(O)OtBu, or ?CH2CH2C(O)OtBu, 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.

Abstract: The present invention relates to synthetic methods for 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds. The general synthetic scheme is: R1 substituents are —CH2OH, —CH(CH3)OH, —CH2Ph, —CH3, or —CH2C(O)NH2 optionally substituted with alkyl or aralkyl. R3 substituents are —CH2OH, —CH3, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —CH2C(O)NH2, or —CH2C(O)OH, wherein the carboxylic acids and amides are optionally substituted with alkyl or aralkyl.

Abstract: Methods of making a compound according to the following scheme: wherein: R1 is a side chain of an amino acid residue selected from Ala, Ser, Thr and Leu; R2 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; R3 is hydrogen or alkyl; Each of R4 and R4? independently is hydrogen or alkyl; Both Ra and Ra? are hydrogen; or together are an oxo(?O) group; Both Rb and Rb? are hydrogen; or together are an oxo (?O) group; L is X is CH2, O or S; R5 is hydrogen or alkyl; m is an integer from 1 to 3; and n is an integer from 2 to 20.

Abstract: The present invention relates to synthetic methods for 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds. The general synthetic scheme is: R1 substituents are —CH2OH, —CH(CH3)OH, —CH2Ph, —CH3, or —CH2C(O)NH2 optionally substituted with alkyl or aralkyl. R3 substituents are —CH2OH, —CH3, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —CH2C(O)NH2, or —CH2C(O)OH, wherein the carboxylic acids and amides are optionally substituted with alkyl or aralkyl.