Selective androgen receptor modulators (SARMS) and uses thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-207/08
A61K-031/401
C07D-498/04
A61K-031/402
A61K-031/5383
A61K-045/06
C07D-207/09
C07D-207/16
출원번호
US-0827228
(2015-08-14)
등록번호
US-9675583
(2017-06-13)
발명자
/ 주소
Zhi, Lin
출원인 / 주소
Ligand Pharmaceuticals Incorporated
대리인 / 주소
Knobbe, Martens, Olson & Bear, LLP
인용정보
피인용 횟수 :
0인용 특허 :
138
초록▼
Provided herein are compounds, such as compounds, of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such
Provided herein are compounds, such as compounds, of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are 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 method of treating a subject having a disease, disorder or condition caused by hyperactivity of an androgen receptor, comprising: administering to the subject a therapeutically effective amount of a compound of formula I; wherein:R1 is CF3, F or Cl;R2 H or methyl; andR3 is H or methyl; or a pha
1. A method of treating a subject having a disease, disorder or condition caused by hyperactivity of an androgen receptor, comprising: administering to the subject a therapeutically effective amount of a compound of formula I; wherein:R1 is CF3, F or Cl;R2 H or methyl; andR3 is H or methyl; or a pharmaceutically acceptable salt or ester thereof;thereby treating the disease, disorder or condition; andwherein the disease, disorder, or condition is selected from among acne, androgenetic alopecia, prostate cancer, hirsutism, hyperandrogenism, male infertility, ovarian hyperandrogenism, and seborrhea. 2. The method of claim 1, wherein R1 is CF3, R2 is H and R3 is H. 3. The method of claim 1, wherein R1 is CF3, R2 is H and R3 is methyl. 4. The method of claim 1, wherein R1 is CF3, R2 is methyl and R3 is hydrogen. 5. The method of claim 1, wherein R1 is F, R2 is H and R3 is H. 6. The method of claim 1, wherein R1 is F, R2 is H and R3 is methyl. 7. The method of claim 1, wherein R1 is F, R2 is methyl and R3 is hydrogen. 8. The method of claim 1, wherein R1 is Cl, R2 is H and R3 is H. 9. The method of claim 1, wherein R1 is Cl, R2 is H and R3 is methyl. 10. The method of claim 1, wherein R1 is Cl, R2 is methyl and R3 is hydrogen. 11. The method of claim 1, wherein the compound of formula I is selected from among: R,R-4-(2-(1-Hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-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(S)2,2,2-trifluoromethyl)-5(R)-methylpyrrolidinyl)-2-trifluoromethyl -benzonitrile;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-chlorobenzonitrile;4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)-5(R)-methylpyrrolidinyl)-2chlorobenzonitrile;R,R-4-(2-(1-hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-chloro-3-methylbenzonitrile;4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)-pyrrolidinyl)-2-chloro-3-methylbenzonitrile;3-methyl-4-((R)-2-((R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoromethyl)-benzonitrile;3-methyl4((R)-2-((S)-2,2,2-trifluoro-1-hydroxethyl)pyrrolidin-1-yl)-2(trilfuoromethyl)-benzonitrile;3-methyl-4-((2R,5R)-2-methyl-5-((S)-2,2,2-trifluoro-1-hydroxyethyl)-pyrrolidin-1yl)-2-(trifluoromethyl)benzonitrile;2-fluoro-4-((2R,5R)-2-methyl-5((S)-2,2,2-trifluoro-1-hydroxethyl)-pyrrolidin-1yl)-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-hydroxyethy)pyrrolidin-1-yl)-benzonitrile;2-fluoro-4-((R)-2-((S)-2,2,2-trifluoro-1-hydroxyehyl)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,3methyl-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 thereof. 12. The method of claim 1, wherein the compound of formula I is 4-(2(R)-(1(S)-hydroxyl-2,2,2-trifluoroethyl)pyrrolidinyl)-2-trifluoromethyl-benzonitrile, or a pharmaceutically acceptable salt thereof.
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