IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
|
| 출원번호 |
US-0734993
(2008-12-12)
|
| 등록번호 |
US-8354446
(2013-01-15)
|
| 국제출원번호 |
PCT/US2008/013657
(2008-12-12)
|
| §371/§102 date |
20100607
(20100607)
|
| 국제공개번호 |
WO2009/082437
(2009-07-02)
|
|
발명자
/ 주소 |
|
| 출원인 / 주소 |
- Ligand Pharmaceuticals Incorporated
|
| 인용정보 |
피인용 횟수 :
9 인용 특허 :
135 |
초록
Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
대표청구항
▼
1. A compound of Formula I: wherein: R1 is CF3, F or Cl;R2 is H or methyl; andR3 is H or methyl; or a pharmaceutically acceptable salt or ester thereof. 2. The compound of claim 1 selected from among: the compound wherein R1 is CF3, R2 is H and R3 is H;the compound wherein R1 is CF3, R2 is H and R3
1. A compound of Formula I: wherein: R1 is CF3, F or Cl;R2 is H or methyl; andR3 is H or methyl; or a pharmaceutically acceptable salt or ester thereof. 2. The compound of claim 1 selected from among: the compound wherein R1 is CF3, R2 is H and R3 is H;the compound wherein R1 is CF3, R2 is H and R3 is methyl;the compound wherein R1 is CF3, R2 is methyl and R3 is hydrogen;the compound wherein R1 is F, R2 is H and R3 is H;the compound wherein R1 is F, R2 is H and R3 is methyl;the compound wherein R1 is F, R2 is methyl and R3 is hydrogen;the compound wherein R1 is Cl, R2 is H and R3 is H;the compound wherein R1 is Cl, R2 is H and R3 is methyl; andthe compound wherein R1 is Cl, R2 is methyl and R3 is hydrogen. 3. The A compound of claim 1 selected from among: 4-(2(R)-(1(R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoromethyl)-benzonitrile;4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-trifluoromethyl-benzonitrile;R,R,R-4-(2-(1-Hydroxyl-2,2,2-trifluoroethyl)-5-methylpyrrolidinyl)-2-trifluoromethyl-benzonitrile;4-(2(R)-(1(5)-hydroxyl-2,2,2-trifluoroethyl)-5(R)-methylpyrrolidinyl)-2-trifluoro-methylbenzonitrile;R,R-4-(2-(1-Hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-chlorobenzonitrile;4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-chlorobenzonitrile;R,R,R-4-(2-(1-hydroxyl-2,2,2-trifluoroethyl)-5-methylpyrrolidinyl)-2-chloro-benzonitrile;4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)-5(R)-methylpyrrolidinyl)-2-chloro-benzonitrile;R,R-4-(2-(1-hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-chloro-3-methyl-benzonitrile;4-(2(R)-(1 (5)-hydroxyl-2,2,2-trifluoroethyl)-pyrrolidinyl)-2-chloro-3-methyl-benzonitrile;3-methyl-4-((R)-2-((R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoro-methyl)benzonitrile;3-methyl-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoro-methyl)benzonitrile;3-methyl-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1-yl)-2-(trifluoromethyl)benzonitrile;2-fluoro-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1-yl)-benzonitrile;2-fluoro-3-methyl-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1-yl)benzonitrile;2-fluoro-3-methyl-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-benzonitrile;2-fluoro-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)benzonitrile;2-chloro-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1-yl)-benzonitrile;2-chloro-3-methyl-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1-yl)benzonitrile;2-chloro-3-methyl-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-benzonitrile; and2-chloro-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-benzonitrile; or a pharmaceutically acceptable salt or ester thereof. 4. A pharmaceutical composition, comprising: a compound of claim 1; anda pharmaceutical acceptable carrier. 5. The composition of claim 4, wherein the composition is formulated for oral, rectal, transmucosal, intestinal, enteral, topical, transdermal, intrathecal, intraventricular, intraperitoneal, intranasal, intraocular, parenteral, intravenous, intramuscular, intramedullary or subcutaneous administration.
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