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US 11,932,595 B2Granted
VDR-silent vitamin D derivative as inhibitors of SREBP and pharmaceutical use thereof
AssigneeKYOTO UNIVERSITY, NATIONAL UNIVERSITY CORPORATION TOKYO UNIVERSITY OF AGRICULTURE AND TECHNOLOGY, TEIKYO UNIVERSITY and THE UNIVERSITY OF TOKYO
InventorsMotonari Uesugi, Yasushi Takemoto, Kazuo Nagasawa, Atsushi Kittaka, Fumihiro Kawagoe, Hayato Nakagawa
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Abstract
Provided are vitamin D3 derivatives of formula (I), pharmaceutical compositions thereof, and pharmaceutical or medical uses thereof for treating metabolic disease, a liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.
Claims21
A compound of formula (I):
- or a stereoisomer, mixture of stereoisomers, and/or a pharmaceutically acceptable salt thereof,
- wherein
- the double bond from a to b is in the E-configuration or Z-configuration;
- R1 is hydrogen;
- where Ra and Rb together with the carbon to which they are attached form an unsubstituted C5-C7-cycloalkyl group;
- —CH2—S-(heteroaryl);
- —CH2-(1,3-dioxo-isoindolin-2-yl);
- (ortho-carboranyl);
- —CH2—NH-(phenyl);
- or
- R2a, R2b, R3, R3a, R3b, R4, R4a, and R4b are independently selected from hydrogen and halo;
- one of X and Y is CR5 and the other is CH;
- or one of X and Y is CR5 and the other is N;
- R5 is hydrogen;
- C1-C6-alkyl;
- hydroxy-C1-C6-alkyl;
- aryl optionally substituted with 1, 2, or 3 R5a groups;
- or 5- or 6-membered heteroaryl optionally substituted with 1, 2, or 3 R5a groups;
- each R5a is independently hydrogen, alkyl, haloalkyl, or halo;
- and
- wherein each phenyl and heteroaryl group are independently optionally substituted with 1, 2, 3, 4, or 5 groups independently selected from the group consisting of halogen, halo-C1-4 alkyl, —S-(halo-C1-4 alkyl), C1-4 alkoxy, halo-C1-4 alkoxy, nitro, cyano, and C1-4 alkoxycarbonyl;
- and
- provided that the compound is not
- or a stereoisomer, mixture of stereoisomers, and/or a pharmaceutically acceptable salt thereof.
21 more elements
Dependencies are inferred from the claim text.