US2015203528A1PendingUtilityA1

Treatment of prostate cancer

Assignee: TOKAI PHARMACEUTICALS INCPriority: Aug 7, 2009Filed: Mar 2, 2015Published: Jul 23, 2015
Est. expiryAug 7, 2029(~3.1 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 35/00A61P 17/00A61P 1/14A61P 15/08A61P 17/14A61P 13/08A61K 31/58A61K 9/2095A61K 9/20A61K 31/56A61K 31/4184A61K 9/0053C07J 43/003A61K 9/0019A61K 9/48A61K 2121/00
50
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0
Cited by
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Claims

Abstract

Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. The present invention provides therapies and therapeutic regimens for the treatment of prostate cancer.

Claims

exact text as granted — not AI-modified
1 - 52 . (canceled) 
     
     
         53 . A compound, or a pharmaceutically-acceptable salt thereof, of formula: 
       
         
           
           
               
               
           
         
         wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a crystalline form characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at about 13.1°, and about 14.1°. 
       
     
     
         54 . (canceled) 
     
     
         55 . The compound of  claim 53 , wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form. 
     
     
         56 . The compound of  claim 53 , wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 
     
     
         57 . A compound, or a pharmaceutically-acceptable salt thereof of formula: 
       
         
           
           
               
               
           
         
         wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a crystalline form characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at about 17.2°, about 18.5°, about 19.1°, about 16.2°, and about 29.6°. 
       
     
     
         58 - 62 . (canceled) 
     
     
         63 . The compound of  claim 57 , wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form. 
     
     
         64 . The compound of  claim 57 , wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 
     
     
         65 . A compound, or a pharmaceutically-acceptable salt thereof, of formula: 
       
         
           
           
               
               
           
         
         wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a crystalline form characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at about 12.5°, about 14.8°, and about 25.5°. 
       
     
     
         66 - 68 . (canceled) 
     
     
         69 . The compound of  claim 65 , wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form. 
     
     
         70 . The compound of  claim 65 , wherein the pharmaceutically-acceptable salt thereof is a hydrochloride salt. 
     
     
         71 . A compound, or a pharmaceutically-acceptable salt thereof, of formula: 
       
         
           
           
               
               
           
         
         wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a crystalline form characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at about 14.4°, about 16.1°, about 19.1°, and about 19.3°. 
       
     
     
         72 - 75 . (canceled) 
     
     
         76 . The compound of  claim 71 , wherein the compound, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form. 
     
     
         77 . The compound of  claim 71 , wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 
     
     
         78 . A composition comprising a mixture of:
 i) a first crystalline form of a compound of formula (I):   
       
         
           
           
               
               
           
         
         or a pharmaceutically-acceptable salt thereof, wherein the first crystalline form, is characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at about 14.4°, about 16.1°, about 19.1°, and about 19.3°; and 
         ii) a second crystalline form of the compound of formula (I), or the pharmaceutically-acceptable salt thereof, wherein the second crystalline form is characterized by a powder X-ray diffraction pattern having characteristic peaks expressed in angle 2-theta at: 
         a) about 13.1°, and about 14.1°; 
         b) about 17.2°, about 18.5°, about 19.1°, about 16.2°, and about 29.6°; or 
         c) about 12.5°, about 14.8°, and about 25.5°. 
       
     
     
         79 - 87 . (canceled) 
     
     
         88 . The composition of  claim 78 , wherein the second crystalline form is characterized by a powder X-ray diffraction pattern having characteristic peaks in angle 2-theta at about 13.1° and about 14.1°. 
     
     
         89 . The composition of  claim 78 , wherein the second crystalline form is characterized by a powder X-ray diffraction pattern having characteristic peaks in angle 2-theta at about 17.2°, about 18.5°, about 19.1°, about 16.2°, and about 29.6°. 
     
     
         90 . The composition of  claim 78 , wherein the second crystalline form is characterized by a powder X-ray diffraction pattern having characteristic peaks in angle 2-theta at about 12.5°, about 14.8°, and about 25.5°. 
     
     
         91 . The composition of  claim 78 , wherein the first crystalline form, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form, and the second crystalline form, or the pharmaceutically-acceptable salt thereof, is in a micronized crystalline form. 
     
     
         92 . The composition of  claim 78 , wherein the composition is greater than 80% in the first crystalline form, or the pharmaceutically-acceptable salt thereof. 
     
     
         93 . The compound of  claim 53 , wherein the crystalline form is in a solvent addition form. 
     
     
         94 . The compound of  claim 93 , wherein the solvent is water. 
     
     
         95 . The compound of  claim 93 , wherein the solvent is an alcohol. 
     
     
         96 . The compound of  claim 93 , wherein the solvent is ethanol. 
     
     
         97 . The compound of  claim 93 , wherein the solvent is methanol. 
     
     
         98 . The compound of  claim 57 , wherein the crystalline form is in a solvent addition form. 
     
     
         99 . The compound of  claim 98 , wherein the solvent is water. 
     
     
         100 . The compound of  claim 98 , wherein the solvent is an alcohol. 
     
     
         101 . The compound of  claim 98 , wherein the solvent is ethanol. 
     
     
         102 . The compound of  claim 98 , wherein the solvent is methanol. 
     
     
         103 . The compound of  claim 65 , wherein the crystalline form is in a solvent addition form. 
     
     
         104 . The compound of  claim 103 , wherein the solvent is water. 
     
     
         105 . The compound of  claim 103 , wherein the solvent is an alcohol. 
     
     
         106 . The compound of  claim 103 , wherein the solvent is ethanol. 
     
     
         107 . The compound of  claim 103 , wherein the solvent is methanol. 
     
     
         108 . The compound of  claim 71 , wherein the crystalline form is in a solvent addition form. 
     
     
         109 . The compound of  claim 108 , wherein the solvent is water. 
     
     
         110 . The compound of  claim 108 , wherein the solvent is an alcohol. 
     
     
         111 . The compound of  claim 108 , wherein the solvent is ethanol. 
     
     
         112 . The compound of  claim 108 , wherein the solvent is methanol.

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