# US 2019/0169131 A1 · Liver x receptor (lxr) modulators

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- Number: US 2019/0169131 A1
- Document ID: US20190169131A1
- Status: Published application
- Kind: A1
- Application number: 16/269,444
- Filed: 2019-02-06
- Published: 2019-06-06
- Earliest claimed: 2013-09-04
- Assignees: Ralexar Therapeutics, Inc.
- Applicants: Ralexar Therapeutics, Inc.
- Inventors: Raju MOHAN
- Web page: https://patentgrep.com/patent/US20190169131A1

## CPC

- C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- A61K 31/415: 1,2-Diazoles
- A61K 31/4164: 1,3-Diazoles
- A61K 31/422: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 231/14: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D 233/10: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring nitrogen atoms
- C07D 233/64: with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
- C07D 409/04: directly linked by a ring-member-to-ring-member bond
- C07D 413/04: directly linked by a ring-member-to-ring-member bond
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

## Claims

### Claim 1

A compound of Formula (IA):
or a pharmaceutically acceptable salt thereof, wherein:
L1 is a bond, C1-C6alkyl, or C1-C6heteroalkyl;
R1 is —OR9, —N(R9)2, C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, C2-C9heterocycloalkyl, —C(═O)R8, or —C(═O)N(R9)2;
R2 is C1-C6alkyl, C2-C6alkenyl, C3-C8cycloalkyl, or —C1-C6alkyl-C3-C8cycloalkyl;
R3 is hydrogen, halogen, C1-C6alkyl, or C1-C6haloalkyl;
R4 is aryl or heteroaryl; wherein aryl or heteroaryl is substituted with at least one R11;
each R5 is independently halogen, C1-C6alkyl, or C1-C6haloalkyl;
R8 is C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R9 is independently hydrogen, C1-C6alkyl, C1-C6heteroalkyl, C1-C6haloalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R10 is independently hydrogen, C1-C6alkyl, C1-C6heteroalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R11 is independently halogen, nitro, —ORB), —N(R10)2, —CN, —C(═O)R10, —C(═O)OR10, —C(═O)N(R10)2, —NR10C(═O)R10, —NR10SO2R10, —SO2R10, —SO2N(R10)2, —C(═O)OCH2SCH3, optionally substituted C1-C6alkyl, optionally substituted C3 -C8cycloalkyl, optionally substituted C1-C6haloalkyl, optionally substituted C1-C6heteroalkyl, optionally substituted —C1-C6alkyl-aryl, optionally substituted aryl, or optionally substituted heteroaryl; and
n is 0-4.

### Claim 2 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein L1 is a bond.

### Claim 3 (depends on 1, 2)

The compound of any one of claims 1-2, or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C6alkyl.

### Claim 4 (depends on 1, 2)

The compound of any one of claims 1-2, or a pharmaceutically acceptable salt thereof, wherein R1 is C2-C6alkenyl.

### Claim 5 (depends on 1, 2)

The compound of any one of claims 1-2, or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C6haloalkyl.

### Claim 6 (depends on 5)

The compound of claim 5, or a pharmaceutically acceptable salt thereof, wherein R1 is —CF3.

### Claim 7 (depends on 1, 2)

The compound of any one of claims 1-2, or a pharmaceutically acceptable salt thereof, wherein R1 is —C(═O)N(R9)2.

### Claim 8 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein L1 is C1-C6alkyl; and R1 is —OH.

### Claim 9 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein -L1-R1 is —C(═CH2)CH3, isopropyl, —C(═O)NHCH2CF3, —CF3, or —C(CH3)2OH.

### Claim 10 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R2 is C1-C6alkyl.

### Claim 11 (depends on 10)

The compound of claim 10, or a pharmaceutically acceptable salt thereof, wherein R2 is isobutyl.

### Claim 12 (depends on 10)

The compound of claim 10, or a pharmaceutically acceptable salt thereof, wherein R2 is sec-butyl.

### Claim 13 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R2 is C3-C8cycloalkyl.

### Claim 14 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R2 is —C1-C6alkyl-C3-C8cycloalkyl.

### Claim 15 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

The compound of any one of claims 1-9, or a pharmaceutically acceptable salt thereof, wherein R2 is isobutyl, sec-butyl, cyclohexyl, —CH2-cyclohexyl, or —CH2-cyclopropyl.

### Claim 16 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)

The compound of any one of claims 1-15, or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen.

### Claim 17 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)

The compound of any one of claims 1-16, or a pharmaceutically acceptable salt thereof, wherein “optionally substituted” means optionally substituted by 1, 2, 3, or 4 substituents independently selected from halo, cyano, C1-C4 alkyl, C2-C4 alkenyl, hydoxy, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, amino, C1-C4 alkylamino, and di(C1-C4alkyl)amino.

### Claim 18 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)

The compound of any one of claims 1-17, or a pharmaceutically acceptable salt thereof, wherein n is 0.

### Claim 19 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl, which is substituted with at least one R11.

### Claim 20 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)

The compound of any one of claims 1-19, or a pharmaceutically acceptable salt thereof, wherein at least one R11 is —NR10SO2R10, —SO2R10, or —SO2N(R10)2.

### Claim 21 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)

The compound of any one of claims 1-19, or a pharmaceutically acceptable salt thereof, wherein at least one R11 is —SO2R10.

### Claim 22 (depends on 20, 21)

The compound of any one of claims 20-21, or a pharmaceutically acceptable salt thereof, wherein each R10 is independently C1-C6alkyl.

### Claim 23 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is C1-C6alkyl; or R4 is phenyl substituted with two R11, and one R11 is —SO2R10; and one R11 is optionally substituted C 1-C6alkyl.

### Claim 24 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with two R11, wherein one R11 is —SO2CH3 and one R11 is —CH2OH.

### Claim 25 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is C1-C6alkyl.

### Claim 26 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, wherein the compound is a compound of Formula (IB):
wherein:
R11a is —NR10SO2R10, —SOR10), —SO2R10, or —SO2N(R10)2; and
m is 0 or 1;
or a pharmaceutically acceptable salt thereof.

### Claim 27 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The compound of any one of claims 1-18, wherein the compound is a compound of Formula (IC):
wherein m is 0 or 1;
or a pharmaceutically acceptable salt thereof.

### Claim 28 (depends on 1, 27)

The compound of claim 1 or 27, or a pharmaceutically acceptable salt thereof, wherein:
L1 is a bond or C1-C6alkyl;
R1 is —OR9, —C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, or —C(═O)N(R9)2;
R2 is C1-C6alkyl, C3-C8cycloalkyl, or —C1-C6alkyl-C3-C8cycloalkyl;
R3 is hydrogen;
R4 is phenyl substituted with at least one R11;
each R11 is independently —NR10SO2R10, —SOR10), —SO2R10, —SO2N(R10)2, or C1-C6alkyl, wherein said C1-C6alkyl is optionally substituted by 1 hydoxy;
provided that at least one R11 is —NR10SO2R10, —SO2R10, or —SO2N(R10)2 ,
each R10 is independently C1-C6 alkyl; and
each R9 is independently hydrogen or C1-C6haloalkyl; and
n is 0.

### Claim 29 (depends on 1, 27)

The compound of claim 1 or 27, or a pharmaceutically acceptable salt thereof, wherein:
L1 is a bond or C1-C6alkyl;
R1 is —OR9, —C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, or —C(═O)N(R9)2;
R2 is C1-C6alkyl, C3-C8cycloalkyl, or —C1-C6alkyl-C3-C8cycloalkyl;
R3 is hydrogen;
R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is C1-C6alkyl; or
R4 is phenyl substituted with two R11, wherein one R11 is —SO2R10 and one R11 is optionally substituted C1-C6alkyl;
each R9 is independently hydrogen or C1-C6haloalkyl; and
n is 0.

### Claim 30 (depends on 1, 27)

The compound of claim 1 or 27, or a pharmaceutically acceptable salt thereof, wherein:
-L1-R1 is —C(═CH2)CH3, isopropyl, —C(═O)NHCH2CF3, —CF3, or —C(CH3)2OH;
R2 is isobutyl, sec-butyl, cyclohexyl, —CH2-cyclohexyl, or —CH2-cyclopropyl;
R3 is hydrogen;
R4 is phenyl substituted with two R11, wherein one R11 is —SO2CH3 and one R11 is —CH2OH; or R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is CH3; and
n is 0.

### Claim 31 (depends on 1)

The compound of claim 1, selected from:
or a pharmaceutically acceptable salt thereof.

### Claim 32 (depends on 1)

The compound of claim 1, selected from:
or a pharmaceutically acceptable salt thereof.

### Claim 33

A compound of Formula (II):
or a pharmaceutically acceptable salt thereof, wherein:
X is —O—, —S—, or —C(R6)═C(R6)—;
L1 is a bond, C1-C6alkyl, or C1-C6heteroalkyl;
R1 is —OR9, —N(R9)2, C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, C2-C9heterocycloalkyl, —C(═O)R8, or —C(═O)N(R9)2;
R2 is C1-C6alkyl, C2-C6alkenyl, C3-C8cycloalkyl, or —C1-C6alkyl-C3-C8cycloalkyl;
R3 is hydrogen, halogen, C1-C6alkyl, or C1-C6haloalkyl;
R4 is aryl or heteroaryl; wherein aryl or heteroaryl is substituted with at least one R11;
each R5 is independently halogen, C1-C6alkyl, or C1-C6haloalkyl;
each R6 is independently hydrogen, halogen, C1-C6alkyl, or C1-C6haloalkyl;
R8 is C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R9 is independently hydrogen, C1-C6alkyl, C1-C6heteroalkyl, C1-C6haloalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R10 is independently hydrogen, C1-C6alkyl, C1-C6heteroalkyl, —C1-C6alkyl-aryl, aryl, or heteroaryl;
each R11 is independently halogen, nitro, —OR10, —N(R10)2, —CN, —C(═O)R10, —C(═O)OR10, —C(═O)N(R10)2, —NR10C(═O)R10, NR10SO2R10, —SO2R10, —SO2N(R10)2, —C(═O)OCH2SCH3, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C1-C6haloalkyl, optionally substituted C1-C6heteroalkyl, optionally substituted —C1-C6alkyl-aryl, optionally substituted aryl, or optionally substituted heteroaryl; and
n is 0-2.

### Claim 34 (depends on 33)

The compound of claim 33, or a pharmaceutically acceptable salt thereof, wherein X is —S—-.

### Claim 35 (depends on 33)

The compound of claim 33, or a pharmaceutically acceptable salt thereof, wherein X is —CH═CH—.

### Claim 36 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein L1 is a bond; and R1 is C1-C6 alkyl.

### Claim 37 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein L1 is a bond and R1 is C1-C6 haloalkyl.

### Claim 38 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein -L1-R1 is C1-C6alkyl, C1-C6alkyl-OH, or C1-C6haloalkyl.

### Claim 39 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein -L1-R1 is selected from CF3 or —C(CH3)2OH.

### Claim 40 (depends on 35, 36, 37, 38, 39)

The compound of any one of claims 35-39, or a pharmaceutically acceptable salt thereof, wherein R2 is C1-C6 alkyl.

### Claim 41 (depends on 35, 36, 37, 38, 39)

The compound of any one of claims 35-39, or a pharmaceutically acceptable salt thereof, wherein R2 is isobutyl.

### Claim 42 (depends on 35, 36, 37, 38, 39, 40, 41)

The compound of any one of claims 35-41, or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen.

### Claim 43 (depends on 35, 36, 37, 38, 39, 40, 41, 42)

The compound of any one of claims 35-42, or a pharmaceutically acceptable salt thereof, wherein n is 0.

### Claim 44 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl; wherein said phenyl is substituted with at least one R11.

### Claim 45 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43, 44)

The compound of any one of claims 35-44, or a pharmaceutically acceptable salt thereof, wherein at least one R11 is —NR10SO2R10, —SO2R10, or —SO2N(R10)2.

### Claim 46 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43, 44)

The compound of any one of claims 35-44, or a pharmaceutically acceptable salt thereof, wherein at least one R11 is —SO2R10.

### Claim 47 (depends on 45, 46)

The compound of claim 45 or 46, or a pharmaceutically acceptable salt thereof, wherein each R10 is independently C1-C6 alkyl.

### Claim 48 (depends on 45, 46)

The compound of claim 45 or 46, or a pharmaceutically acceptable salt thereof, wherein each R10 is methyl.

### Claim 49 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is C1-C6alkyl; or R4 is phenyl substituted with two R11, and one R11 is —SO2R10 and one R11 is optionally substituted C 1-C6alkyl.

### Claim 50 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with two R11, wherein one R11 is —SO2CH3 and one R11 is —CH2OH.

### Claim 51 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, or a pharmaceutically acceptable salt thereof, wherein R4 is phenyl substituted with one R11, wherein R11 is —SO2R10 and R10 is C1-C6alkyl.

### Claim 52 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51)

The compound of any one of claims 35-51, or a pharmaceutically acceptable salt thereof, wherein “optionally substituted” means optionally substituted by 1, 2, 3, or 4 substituents independently selected from halo, cyano, C1-C4 alkyl, C2-C4 alkenyl, hydoxy, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, amino, C1-C4 alkylamino, and di(C1-C4alkyl)amino.

### Claim 53 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, wherein the compound is a compound of Formula (IIA):
wherein:
R1ia is —NR10SO2R10, —SOR10), —SO2R10, or —SO2N(R10)2; and
m is 0 or 1;
or a pharmaceutically acceptable salt thereof.

### Claim 54 (depends on 35, 36, 37, 38, 39, 40, 41, 42, 43)

The compound of any one of claims 35-43, wherein the compound is a compound of Formula (IIB):
wherein m is 0 or 1;
or a pharmaceutically acceptable salt thereof.

### Claim 55 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein:
X is —CH═CH—;
-L1-R1 is C1-C6alkyl, C1-C6alkyl-OH, or C1-C6haloalkyl;
R2 is C1—C6alkyl;
R3 is hydrogen;
R4 is phenyl; wherein said phenyl is substituted with at least one R11;
each R11 is independently —NR10SO2R10, —SOR10), —SO2R10, —SO2N(R10)2, or C1-C6alkyl, wherein said C1-C6alkyl is optionally substituted by 1 hydoxy;
provided that at least one R11 is —NR10SO2R10, —SOR10, —SO2R10, or —SO2N(R10)2 , each R10 is independently C1-C6 alkyl; and
n is 0.

### Claim 56 (depends on 35)

The compound of claim 35, or a pharmaceutically acceptable salt thereof, wherein:
X is —CH═CH—;
-L1-R1 is C1-C6alkyl, C1-C6alkyl-OH, or C1-C6haloalkyl;
R2 is C1-C6 alkyl;
R3 is hydrogen;
R4 is phenyl; wherein said phenyl is substituted with at least one R11; wherein each R11 is independently —SO2R10, or C1-C6alkyl, wherein said C1-C6alkyl is optionally substituted by 1 hydoxy; provided that at least one R11 is —SO2R10,
each R10 is independently C1-C6 alkyl; and
n is 0.

### Claim 57 (depends on 35)

The compound of claim 35, selected from:
or a pharmaceutically acceptable salt thereof.

### Claim 58 (depends on 34)

The compound of claim 34, selected from:
or a pharmaceutically acceptable salt thereof

### Claim 59

A compound selected from:
or a pharmaceutically acceptable salt thereof.

### Claim 60 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59)

A pharmaceutical composition comprising a compound according to any one of claims 1-59, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 61 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59)

A method of treating a disease, disorder or condition in a mammal that would benefit from LXR modulation comprising administering to the mammal a compound according to any one of claims 1-59, or a pharmaceutically acceptable salt thereof.

### Claim 62 (depends on 61)

The method of claim 61, wherein the disease, disorder or condition in a mammal is increased lipid levels, increased cholesterol levels, low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, sepsis, inflammatory diseases, infectious diseases, skin diseases, colitis, pancreatitis, cholestasis of the liver, fibrosis of the liver, psoriasis, Alzheimer's disease, Parkinson's disease, impaired/improvable cognitive function, HIV, cancer including metastatic cancer and metastatic melanoma, acute macular degeneration, and age related forms of macular degeneration (wet and dry forms).

### Claim 63 (depends on 61)

The method of claim 61, wherein the disease, disorder or condition is cancer.

### Claim 64 (depends on 63)

The method of claim 63, wherein the cancer is malignant melanoma.

### Claim 65 (depends on 63)

The method of claim 63, wherein ApoE levels are reduced in said cancer.

### Claim 66 (depends on 62)

The method of claim 62, further comprising administering a second therapeutic agent.

### Claim 67 (depends on 66)

The method of claim 66, wherein the second therapeutic agent is a BRAF inhibitor.

### Claim 68 (depends on 67)

The method of claim 67, wherein the BRAF inhibitor is selected from PDC-4032, GSK2118436, and PLX-3603.

### Claim 69 (depends on 66)

The method of claim 66, wherein the second therapeutic agent is sunitinib malate, sorafenib tosylate, imatinib mesylate, or nilotinib hydrochloride monohydrate; or a combination thereof.

### Claim 70 (depends on 61, 62, 63, 64, 65, 66, 67, 68, 69)

The method of any one of claims 61-69, wherein the mammal is a human.

### Claim 71 (depends on 61)

The method of claim 61, wherein the disease, disorder or condition is Alzheimer's disease.

### Claim 72 (depends on 61)

The method of claim 61, wherein the disease, disorder or condition is Parkinson's disease.

### Claim 73 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59)

A method of modulating LXR activity comprising contacting LXR, or portion thereof, with a compound according to any one of claims 1-59, or a pharmaceutically acceptable salt thereof.
