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US 6,645,955 B1Granted
3,6-dihydroxy-24-amidyl steroid derivatives
AssigneeArch Development Corporation
InventorsShutsung Liao, Ching Song
Life of this patent
Estimating the term…
Abstract
Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.
Claims13
A compound of the following formula:
- wherein
- each of R1, R2, R4, R4′, R5, R7, R8, R9, R11, R12, R14, R15, R16, and R17′, independently, is hydrogen;
- each of R3 and R6, independently, is hydroxy;
- each of R10 and R13, independently, is alkyl, haloalkyl, or hydroxyalkyl;
- R17 is —X—Y—Z, in which
- X is alkyl or alkenyl;
- Y is —CO—NH— or —CO—N(alkyl)-;
- and
- Z is alkynyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, heteroaryl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, halo, oxo, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, or alkylthio;
- is straight chain C1-C8 alkyl, alkenyl, or cycloalkyl, which is substituted with hydroxy, alkoxy, halo, oxo, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, or alkylthio;
- or is —CH(A)—B with A being an amino acid side chain containing an aromatic moiety, and B being hydrogen, —NRaRb, or —COORc wherein each of Ra, Rb, and Rc, independently, is hydrogen or alkyl;
- and
- n is 0;
- or a salt thereof.
11 more elements
A pharmaceutical composition for treating a UR- or a LXR-mediated disorder, said composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound of the following formula:
- wherein
- each of R1, R2, R4, R4′, R5, R7, R8, R9, R11, R12, R14, R15, R16, and R17′, independently, is hydrogen;
- each of R3 and R6, independently, is hydroxy;
- each of R10 and R13, independently, is alkyl, haloalkyl, or hydroxyalkyl;
- R17 is —X—Y—Z, in which
- X is alkyl or alkenyl;
- Y is —CO—NH— or —CO—N(alkyl)-;
- and
- Z is alkynyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, heteroaryl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, halo, oxo, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, or alkylthio;
- is straight chain C1-C8 alkyl, alkenyl, or cycloalkyl, which is substituted with hydroxy, alkoxy, halo, oxo, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, or alkylthio;
- or is —CH(A)—B with A being an amino acid side chain containing an aromatic moiety, and B being hydrogen, —NRaRb, or —COORc wherein each of Ra, Rb, and Rc, independently, is hydrogen or alkyl;
- and
- n is 0;
- or a salt thereof.
11 more elements
Dependencies are inferred from the claim text.