1,2,4-Oxadiazole Compounds as Inhibitors of CD47 Signalling Pathways
AssigneeAurigene Oncology Limited
InventorsPottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli, Chennakrishnareddy Gundala
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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.
Claims20
A method of modulating macrophage phagocytic activity towards a cancer cell or tumor cell in an individual comprising administering to said individual an effective amount of a compound of formula (I):
- or a pharmaceutically acceptable salt or an amide or an ester, or a stereoisomer thereof;
- wherein,
- Ra is hydrogen or acyl;
- and R1 represents hydrogen, —(CH2)2CONH2, —(CH2)2COOH, —CH2COOH, —(CH2)3NHC(═NH)NH2, —(CH2)4NH2, —CH2CONH2, —CH(CH3)—CH2—CH3, —CH2-aryl, or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- or Ra and R1 together with the atoms to which they are attached form pyrrolidine ring optionally substituted with oxo group;
- R2 represents hydrogen, —CH2—OH, —(CH2)3NHC(═NH)NH2, —(CH2)2CONH2, —(CH2)2COOH, —CH2-aryl, or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- Rb is hydrogen;
- and R3 represents hydrogen, —CH2-aryl, —(CH2)3NHC(═NH)NH2, —CH2COOH, —CH(CH3)—CH2—CH3, —CH2—CH(CH3)2, —(CH2)2CONH2, —(CH2)2COOH, —(CH2)4NH2 or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- or Rb and R3, together with the atoms to which they are attached form pyrrolidine ring.
A method for treating or delaying progression of diseases or disorders mediated by CD47 in an individual, the method comprising administering to said individual an effective amount of a compound of formula (I):
- or a pharmaceutically acceptable salt or an amide or an ester, or a stereoisomer thereof;
- wherein,
- Ra is hydrogen or acyl;
- and R1 represents hydrogen, —(CH2)2CONH2, —(CH2)2COOH, —CH2COOH, —(CH2)3NHC(═NH)NH2, —(CH2)4NH2, —CH2CONH2, —CH(CH3)—CH2—CH3, —CH2-aryl, or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- or Ra and R1 together with the atoms to which they are attached form pyrrolidine ring optionally substituted with oxo group;
- R2 represents hydrogen, —CH2—OH, —(CH2)3NHC(—NH)NH2, —(CH2)2CONH2, —(CH2)2COOH, —CH2-aryl, or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- Rb is hydrogen;
- and R3 represents hydrogen, —CH2-aryl, —(CH2)3NHC(═NH)NH2, —CH2COOH, —CH(CH3)—CH2—CH3, —CH2—CH(CH3)2, —(CH2)2CONH2, —(CH2)2COOH, —(CH2)4NH2 or —CH2-heteroaryl;
- wherein the said aryl and heteroaryl are unsubstituted;
- or Rb and R3, together with the atoms to which they are attached form pyrrolidine ring.
Dependencies are inferred from the claim text.