US2015166599A1PendingUtilityA1

Treatment of prostate cancer

Assignee: TOKAI PHARMACEUTICALS INCPriority: Aug 7, 2009Filed: Mar 2, 2015Published: Jun 18, 2015
Est. expiryAug 7, 2029(~3.1 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 35/00A61P 15/08A61P 13/08A61P 1/14A61P 17/00A61P 17/14A61K 9/0019A61K 9/20A61K 31/58A61K 31/4184A61K 2121/00C07J 43/003A61K 9/0053A61K 9/2095A61K 9/48A61K 31/56
50
PatentIndex Score
0
Cited by
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0
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 method of making a crystalline form of compound (I): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically-acceptable salt thereof, the method comprising:
 a) dissolving an initial form of compound (I), or the pharmaceutically-acceptable salt thereof, in a solvent; 
 b) allowing the solvent to evaporate to obtain the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof; and 
 c) collecting the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, wherein the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, is 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 method of  claim 53 , wherein the initial form is a crystalline form. 
     
     
         56 . The method of  claim 53 , wherein the initial form is an amorphous form. 
     
     
         57 . The method of  claim 56 , wherein the amorphous form is dissolved in an aqueous solvent to form a mixture. 
     
     
         58 . The method of  claim 57 , wherein the mixture is subjected to a series of heat-cool cycles. 
     
     
         59 . The method of  claim 58 , wherein a heat-cool cycle lasts 8 hours. 
     
     
         60 . The method of  claim 58 , wherein a heat-cool cycle ranges from room temperature to 50° C. 
     
     
         61 . The method of  claim 53 , wherein the collected crystalline form is dehydrated to about below 40% relative humidity. 
     
     
         62 . The method of  claim 61 , wherein the dehydration is performed using gravimetric vapor sorption. 
     
     
         63 . A method of making a crystalline form of compound (I): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically-acceptable salt thereof, the method comprising:
 a) dissolving an initial form of compound (I), or the pharmaceutically-acceptable salt thereof, in a solvent; 
 b) allowing the solvent to evaporate to obtain the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof; and 
 c) collecting the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, wherein the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, is 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°. 
 
     
     
         64 - 68 . (canceled) 
     
     
         69 . The method of  claim 63 , wherein the initial form is a crystalline form. 
     
     
         70 . The method of  claim 63 , wherein the initial form is an amorphous form. 
     
     
         71 . The method of  claim 70 , wherein the amorphous form is dissolved in an aqueous solvent to form a mixture. 
     
     
         72 . The method of  claim 71 , wherein the mixture is subjected to a series of heat-cool cycles. 
     
     
         73 . The method of  claim 72 , wherein a heat-cool cycle lasts for 8 hours. 
     
     
         74 . The method of  claim 72 , wherein a heat-cool cycle ranges from room temperature to 50° C. 
     
     
         75 . A method of making a crystalline form of compound (I): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically-acceptable salt thereof, the method comprising:
 a) dissolving an initial form of compound (I), or the pharmaceutically-acceptable salt thereof, in a solvent; 
 b) allowing the solvent to evaporate to obtain the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof; and 
 c) collecting the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, wherein the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, is 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°. 
 
     
     
         76 - 78 . (canceled) 
     
     
         79 . The method of  claim 75 , wherein the initial form is a crystalline form. 
     
     
         80 . The method of  claim 75 , wherein the initial form is an amorphous form. 
     
     
         81 . The method of  claim 80 , wherein the amorphous form of compound (I) is dissolved in an aqueous solvent to form a mixture. 
     
     
         82 . The method of  claim 81 , wherein the mixture is subjected to a series of heat-cool cycles. 
     
     
         83 . The method of  claim 82 , wherein a heat-cool cycle lasts for 8 hours. 
     
     
         84 . The method of  claim 82 , wherein a heat-cool cycle ranges from room temperature to 50° C. 
     
     
         85 . The method of  claim 75 , wherein the collected crystalline form is dehydrated to about below 50% relative humidity. 
     
     
         86 . The method of  claim 85 , wherein the dehydration is performed using gravimetric vapor sorption. 
     
     
         87 . A method of making a crystalline form of compound (I): 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically-acceptable salt thereof, the method comprising:
 a) dissolving an initial form of compound (I), or the pharmaceutically-acceptable salt thereof, in a solvent; 
 b) allowing the solvent to evaporate to obtain the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof; and 
 c) collecting the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, wherein the crystalline form of compound (I), or the pharmaceutically-acceptable salt thereof, 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°. 
 
     
     
         88 - 91 . (canceled) 
     
     
         92 . The method of  claim 87 , wherein the initial form is a crystalline form. 
     
     
         93 . The method of  claim 87 , wherein the initial form is an amorphous form. 
     
     
         94 . The method of  claim 87 , wherein the initial form is dissolved in an organic solvent to form a mixture. 
     
     
         95 . The method of  claim 94 , wherein the organic solvent is cumene. 
     
     
         96 . The method of  claim 94 , wherein the mixture is subjected to a series of heat-cool cycles. 
     
     
         97 . The method of  claim 96 , wherein a heat-cool cycle lasts for 8 hours. 
     
     
         98 . The method of  claim 96 , wherein a heat-cool cycle ranges from room temperature to 50° C. 
     
     
         99 . The method of  claim 53 , further comprising formulating the collected crystalline form into a pharmaceutical formulation. 
     
     
         100 . The method of  claim 99 , wherein the pharmaceutical formulation further comprises a pharmaceutically-acceptable excipient. 
     
     
         101 . The method of  claim 99 , wherein the pharmaceutical formulation is formulated as a tablet. 
     
     
         102 . The method of  claim 99 , wherein the pharmaceutical formulation is for oral delivery. 
     
     
         103 . The method of  claim 63 , further comprising formulating the collected crystalline form into a pharmaceutical formulation. 
     
     
         104 . The method of  claim 103 , wherein the pharmaceutical formulation further comprises a pharmaceutically-acceptable excipient. 
     
     
         105 . The method of  claim 103 , wherein the pharmaceutical formulation is formulated as a tablet. 
     
     
         106 . The method of  claim 103 , wherein the pharmaceutical formulation is for oral delivery. 
     
     
         107 . The method of  claim 75 , further comprising formulating the collected crystalline form into a pharmaceutical formulation. 
     
     
         108 . The method of  claim 107 , wherein the pharmaceutical formulation further comprises a pharmaceutically-acceptable excipient. 
     
     
         109 . The method of  claim 107 , wherein the pharmaceutical formulation is formulated as a tablet. 
     
     
         110 . The method of  claim 107 , wherein the pharmaceutical formulation is for oral delivery. 
     
     
         111 . The method of  claim 87 , further comprising formulating the collected crystalline form into a pharmaceutical formulation. 
     
     
         112 . The method of  claim 111 , wherein the pharmaceutical formulation further comprises a pharmaceutically-acceptable excipient. 
     
     
         113 . The method of  claim 111 , wherein the pharmaceutical formulation is formulated as a tablet. 
     
     
         114 . The method of  claim 111 , wherein the pharmaceutical formulation is for oral delivery.

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