Patent ID: 11858957
Assignee: ANTENGENT THERAPEUTICS LIMITED
Field: Organic fine chemistry (Chemistry)
Classification: CPC C  A | IPC C

Claim 0:
1. A method of treating a disease or disorder selected from cancer, cerebral and cardiac ischemic diseases, fibrosis, immune and inflammatory disorders, inflammatory gut motility disorder, neurological, neurodegenerative and CNS disorders and diseases, depression, Parkinson's disease, and sleep disorders, the method comprising administering to a subject a therapeutically effective amount of a CD73 inhibitor, wherein the CD73 inhibitor comprises a compound having the following formula:, , or a pharmaceutically acceptable salt and/or prodrug thereof, wherein
Y is, Het is an optionally substituted purinyl ring or an optionally substituted 5-methyl-pyrimidin-2,4-dione ring;
R1a is selected from H, halo, hydroxy, cyano, azido, amino, C1-6alkyl, hydroxyC1-6alkyl, amino-C1-6alkyl, —O—C(O)—O—C1-6alkyl, C1-6acyloxy, C1-6alkoxy, C2-6alkenyl, and C2-6alkynyl;
R1b is selected from H, halo, C1-6alkyl, hydroxy-C1-6alkyl, amino-C1-6alkyl, C2-6alkenyl, and C2-6alkynyl;
R2a is selected from halo, hydroxy, cyano, azido, amino, C1-6alkyl, hydroxy-C1-6alkyl, amino-C1-6alkyl, C1-6acyloxy, —O—C(O)—O—C1-6alkyl, C1-6alkoxy, C2-6alkenyl, and C2-6alkynyl;
R2b is C2-6alkynyl;
R3 is selected from H and alkyl;
R4 is selected from H, alkyl, CN, aryl, heteroaryl, —C(O)OR9, —C(O)NR11R12, —S(O)2R10, —P(O)(OR11)(OR12), and —P(O)(OR11)(NR13R14);
R5 is aralkyl or heteroaralkyl, wherein the aralkyl or heteroaralkyl is optionally substituted with one or more substituents selected from halo, haloalkyl, alkyl, alkoxy, carbonyl, aryl, amino, amido, cycloalkyl, heterocyclyl, and heteroaryl;
R6 is selected from —C(O)OR9, —C(O)NR16R17, and —P(O)(OR11)(OR12);
R9 is independently selected from H, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl;
R10 is independently selected from alkyl, alkenyl, alkynyl, amino, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl; and
each R11 and R12 is independently selected from H, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl; or
R11 and R12, together with the nitrogen atom to which they are attached, form a 5- to 7-membered heterocyclyl;
R13 is, independently for each occurrence, H or alkyl;
R14 is, independently for each occurrence, alkyl or aralkyl;
each R15 is independently selected from hydroxy, alkoxy acyloxy and NR13R14;
each R16 and R17 is independently selected from H, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl; or
R16 and R17, together with the nitrogen atom to which they are attached, form a 5- to 7-membered heterocyclyl.