# US 2017/0247382 A1 · Small molecules targeting androgen receptor nuclear localization and/or level in prostate cancer

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- Number: US 2017/0247382 A1
- Document ID: US20170247382A1
- Status: Published application
- Kind: A1
- Application number: 15/457,774
- Filed: 2017-03-13
- Published: 2017-08-31
- Earliest claimed: 2011-10-12
- Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education
- Applicants: University of Pittsburgh - Of the Commonwealth System of Higher Education
- Inventors: Zhou Wang; Joel Byron Nelson; Minh Bao Nguyen; John S. Lazo; Paul A. Johnston; Peter Wipf
- Web page: https://patentgrep.com/patent/US20170247382A1

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61K 31/4188: condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/4965: Non-condensed pyrazines
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/04: specific for metastasis
- C07D 235/02: condensed with carbocyclic rings or ring systems
- C07D 241/04: having no double bonds between ring members or between ring members and non-ring members
- C07D 261/04: having one double bond between ring members or between a ring member and a non-ring member
- C07D 261/08: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 295/16: acylated on ring nitrogen atoms
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 403/04: directly linked by a ring-member-to-ring-member bond
- 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 417/04: directly linked by a ring-member-to-ring-member bond
- C07D 471/08: Bridged systems
- C07D 487/04: 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

A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group.

## Claims

### Claim 1

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R1 forms a ring structure selected from an optionally substituted single ring that includes four to six C ring atoms, or an optionally substituted polycyclic ring that includes five to ten C ring atoms;
R2 to R6 is each individually H, halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group;
R7 is H, halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group;
R8 is alkyl, hydroxy, alkoxy, hydroxyalkyl, or alkoxyalkyl; and
b is 1.

### Claim 2

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R2, R3, R5, R6 and R7 are each individually H; and R4 is substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, or a seleno-containing group.

### Claim 3

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
R2 to R6 is each individually H, halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group; and
R7 is halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group.

### Claim 4

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R is alkoxy or halogen.

### Claim 5

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R is alkoxy or halogen.

### Claim 6

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R is alkoxy or halogen.

### Claim 7

A compound, or a pharmaceutically acceptable salt of ester thereof, of a structure of:
wherein R4 is H;
at least one of R2, R3, R5 or R6 is halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group; and
R7 is H, halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group.

### Claim 8 (depends on 7)

The compound of claim 7, wherein R5 or R6 is halogen, alkoxy, aryl, substituted aryl, heteroaryl, alkyl, substituted alkyl, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, or a nitro-containing group.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 1.

### Claim 10 (depends on 2)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 2.

### Claim 11 (depends on 3)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 3.

### Claim 12 (depends on 4)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 4.

### Claim 13 (depends on 5)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 5.

### Claim 14 (depends on 6)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 6.

### Claim 15 (depends on 7)

A pharmaceutical composition comprising at least one pharmaceutically acceptable additive, and a compound of claim 7.