# US 2017/0290830 A1 · Small molecule regulators of steroid receptor coactivators and methods of use thereof

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- Number: US 2017/0290830 A1
- Document ID: US20170290830A1
- Status: Published application
- Kind: A1
- Application number: 15/480,731
- Filed: 2017-04-06
- Published: 2017-10-12
- Earliest claimed: 2016-04-08
- Assignees: Baylor College of Medicine
- Applicants: Baylor College of Medicine
- Inventors: Bert W. O'Malley; David Michael Lonard; Jin Wang; Jianming Xu; Jianwei Chen
- Web page: https://patentgrep.com/patent/US20170290830A1

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- A61K 31/426: 1,3-Thiazoles
- A61K 31/4402: only substituted in position 2, e.g. pheniramine, bisacodyl
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- 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 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 401/14: containing three or more hetero rings
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07D 498/04: Ortho-condensed systems
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a cell.

## Claims

### Claim 1

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2 and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl,
wherein when X is a pyridine or a pyrimidine, (1) the pyridine or the pyrimidine is substituted, (2) at least one of R4, R5, R6, and R7 is other than hydrogen, or (3) R1 is other than hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted cycloalkyl.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound has the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
Y1 is CRR, NR, O, or S; and
Y2 is CR or N,
wherein each R is hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl.

### Claim 3 (depends on 2)

The compound of claim 2, wherein each R is hydrogen or substituted or unsubstituted alkyl.

### Claim 4 (depends on 1)

The compound of claim 1, wherein the compound has the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
Y1 and Y2 are each independently selected from CR and N, wherein R is hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl; and
R10 and R12 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl,
wherein at least one of R4, R5, R6, R7, R10, R12, and R is other than hydrogen.

### Claim 5 (depends on 4)

The compound of claim 4, wherein R, R10, and R12 are each independently selected from hydrogen and halogen.

### Claim 6 (depends on 1)

The compound of claim 1, wherein the compound is selected from the group consisting of

### Claim 7 (depends on 1)

A tautomer of the compound of claim 1.

### Claim 8 (depends on 7)

The tautomer of claim 7, wherein the tautomer has the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2 and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl,
wherein when X is a pyridine or a pyrimidine, (1) the pyridine or the pyrimidine is substituted, (2) at least one of R4, R5, R6, and R7 is other than hydrogen, or (3) R1 is other than hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted cycloalkyl.

### Claim 9

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2 is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

### Claim 10

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2 is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

### Claim 11

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; and
R1, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.

### Claim 12

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R5, and R6 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2, R3, and R4 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.

### Claim 13

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R5, and R6 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R3 and R4 are each independently selected from hydrogen, cyano, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.

### Claim 14

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R2 and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.

### Claim 15

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R3 is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

### Claim 16

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R3 is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

### Claim 17

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R2, and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl; and
R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.

### Claim 18

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R2, and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl; and
R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.

### Claim 19

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R1, R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R3 is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl.

### Claim 20

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R2 and R3 are each independently selected from hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl; and
R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.

### Claim 21

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
X is a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
R3 is hydrogen, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl; and
R4, R5, R6, and R7 are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.

### Claim 22 (depends on 1)

The compound of claim 1, wherein the compound is isotopically substituted with a stable isotope.

### Claim 23 (depends on 22)

The compound of claim 22, wherein the stable isotope is selected from the group consisting of deuterium, 13C, 15N, and 18O.

### Claim 24 (depends on 1)

A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

### Claim 25 (depends on 1)

A kit comprising a compound of claim 1.

### Claim 26 (depends on 1)

A method of treating or preventing a steroid receptor coactivator-related disease in a subject, comprising:
administering to the subject an effective amount of a compound of claim 1.

### Claim 27 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator-related disease is cancer.

### Claim 28 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator-related disease is a metabolic disorder.

### Claim 29 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator-related disease is human immunodeficiency virus.

### Claim 30 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator-related disease is a neurodegenerative disorder.

### Claim 31 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator-related disease is an inflammatory disease.

### Claim 32 (depends on 26)

The method of claim 26, wherein the steroid receptor coactivator is SRC-1, SRC-2, or SRC-3.

### Claim 33 (depends on 26)

The method of claim 26, further comprising administering a second compound or composition.

### Claim 34 (depends on 33)

The method of claim 33, wherein the second compound or composition is a chemotherapeutic agent.

### Claim 35 (depends on 1)

A method of regulating a steroid receptor coactivator protein in a cell, comprising:
contacting a cell with an effective amount of a compound of claim 1.

### Claim 36 (depends on 35)

The method of claim 35, wherein the steroid receptor coactivator protein is SRC-1, SRC-2, or SRC-3.

### Claim 37 (depends on 35)

The method of claim 35, wherein the contacting is performed in vitro or in vivo.

### Claim 38

A method of treating a metabolic disorder, human immunodeficiency virus, a neurodegenerative disorder, or an inflammatory disease in a subject, comprising:
administering to the subject an effective amount of a compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
Y1 and Y2 are each independently selected from CH and N; and
R1, R2, and R3 are each independently selected from hydrogen and substituted or unsubstituted alkyl,
wherein at least one of Y1 and Y2 is N.

### Claim 39 (depends on 38)

The method of claim 38, wherein the compound is selected from the group consisting of:

### Claim 40

A method of regulating a steroid receptor coactivator protein in a cell, comprising:
contacting a cell with an effective amount of a compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
Y1 and Y2 are each independently selected from CH and N; and
R1, R2, and R3 are each independently selected from hydrogen and substituted or unsubstituted alkyl,
wherein at least one of Y1 and Y2 is N.

### Claim 41 (depends on 40)

The method of claim 40, wherein the steroid receptor coactivator protein is SRC-1, SRC-2, or SRC-3.

### Claim 42 (depends on 40)

The method of claim 40, wherein the contacting is performed in vitro or in vivo.

### Claim 43

A compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
is a single bond or a double bond;
X and Y are each independently selected from the group consisting of substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heterocycloalkenyl, substituted or unsubstituted heterocycloalkynyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted alkynyl;
A1 is B, CR, CRR′, N, NR, O, or S;
A2 is BR, CRR′, NR, O, or S;
R and R′ are each independently selected from hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl; and
R1 is hydrogen, halogen, cyano, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl,
wherein if X is pyridine, is a double bond, A1 is N, A2 is NH, and R1 is methyl, then Y is not unsubstituted benzimidazole or N-methyl-benzimidazole.

### Claim 44 (depends on 43)

A method of treating or preventing a steroid receptor coactivator-related disease in a subject, comprising:
administering to the subject an effective amount of a compound of claim 43.