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US 11,236,079 B2Granted
Morpholine derivates as inhibitors of Vps34
AssigneeNeuropore Therapies, Inc.
InventorsEmily M. Stocking, Wolfgang J. Wrasidlo
Life of this patent
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Abstract
The present disclosure relates to thiazole- or diathiazole-substituted aryl and heteroaryl compounds (I), pharmaceutical compositions containing them, and methods of using them, including treatment of disorders or disease related to regulation of the Vps34/PI3K III signaling pathway.
Claims34
A compound of Formula I:
- wherein
- R1 is C6-C14 aryl, 5- to 10-membered heteroaryl, C3-C6 cycloalkyl, or 4- to 10-membered heterocycloalkyl, wherein the C6-C14 aryl, 5- to 10-membered heteroaryl, C3-C6 cycloalkyl, or 4- to 10-membered heterocycloalkyl of R1 are each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, —CN, —NO2, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C2-C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, C1-C6 haloalkyl, —ORa, —SRa, —S(O)2Ra, —NRbRc, —C(O)Ra, —OC(O)Ra, —C(O)ORa, —C(O)NRbRc, —OC(O)NRbRc, —NRaC(O)Rb, —NRaC(O)ORb, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C3-C6 cycloalkenyl, substituted or unsubstituted C6-C14 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 4- to 10-membered heterocycloalkyl;
- L is —S(O)2—, —O—, —C(O)— or CH2—;
- Y1 is CH or N;
- R2 is a 5-membered heteroaryl or a 5-membered heterocycloalkyl, wherein the 5-membered heteroaryl and 5-membered heterocycloalkyl of R2 are each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, —CN, —NO2, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C2-C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, C1-C6 haloalkyl, —ORd, —SRd, —S(O)2Rd, —NReRf, —C(O)Rd, —OC(O)Rd, —C(O)ORd, —C(O)NReRf, —OC(O)NReRf, —NRdC(O)Re, —NRdC(O)ORe, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C3-C6 cycloalkenyl, substituted or unsubstituted C6-C14 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 4- to 10-membered heterocycloalkyl;
- and
- Ra, Rb, Re, Rd, Re, and Rf are each independently H or C1-4 alkyl;
- wherein when L is —S(O)2— and Y1 is N, R1 is not 4,4-difluoro-piperidin1-yl;
- or a pharmaceutically acceptable salt thereof.
6 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.