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US 12,679,849 B2Granted
Macrocyclic compounds as STING agonists
AssigneeLupin Limited
InventorsNavnath Popat Karche, Moloy Banerjee, Pradeep Rangrao Patil, Vinod Popatrao Vyavahare, Deepak Sahebrao Walke, Vaibhav Madhukar Kalhapure, Vidya Ramdas, Venkata P. Palle, Rajender Kumar Kamboj
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Abstract
Disclosed are the macrocyclic compounds having the general Formula (I) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.
Claims10
A compound of Formula (Ia), its stereoisomer, or its pharmaceutically acceptable salt,
- wherein,
- R2 is independently selected from hydrogen, optionally substituted C1-C6 alkyl, and optionally substituted C3-C5 monocyclic cycloalkyl;
- ring A is independently selected from optionally substituted heterocyclyl, and optionally substituted heteroaryl;
- m is selected from 0, or 1;
- n is selected from 0, 1, or 2;
- when ‘alkyl’ is substituted, it is substituted with 1 to 4 substituents independently selected from halogen, alkyl, perhaloalkyl, cycloalkyl, heterocyclyl, —N(R4)2, and —OR4;
- when ‘carbocycle’ or ‘cycloalkyl’ is substituted, it is substituted with 1 to 4 substituents independently selected from halogen, alkyl, perhaloalkyl, —N(R4)2, and —OR4;
- when ‘heterocycle’ or ‘heterocyclyl’ is substituted, it is substituted with 1 to 4 substituents independently selected from oxo (═O), halogen, cyano, alkyl, perhaloalkyl, —OR4, —C(═O)OH, —OP(O)(OR4)2, —P(O)(OR4)2, —P(O)(OR4)R4a, —SO2R4a, —SO2NH2, —C(═O)N(H)R4, —C(═O)N(alkyl)R4, —N(H)C(═O)R4a, —N(H)R4, and —N(alkyl)R4;
- when the ‘heteroaryl’ group is substituted, it is substituted with 1 to 4 substituents selected from halogen, cyano, alkyl, perhaloalkyl, —O-alkyl, —O-perhaloalkyl, —N(alkyl)alkyl, —N(H)R4, —SO2-alkyl, —N(alkyl)C(═O)alkyl, —N(H)C(═O)alkyl, —C(═O)N(alkyl)alkyl, —C(═O)N(H)alkyl, —C(═O)NH2, —SO2N(alkyl)alkyl, —SO2N(H)alkyl, —SO2NH2, —C(═O)OH, —OP(O)(OR4)2, —P(O)(OR4)2, and —P(O)(OR4)R4a;
- each R4 is independently selected from hydrogen, alkyl, and cycloalkyl;
- and
- each R4a is independently selected from alkyl, and cycloalkyl.
9 more elements
Dependencies are inferred from the claim text.