US2019381041A1PendingUtilityA1

Compositions and methods for treating myelofibrosis

56
Assignee: IMPACT BIOMEDICINES INCPriority: Nov 7, 2010Filed: Aug 23, 2019Published: Dec 19, 2019
Est. expiryNov 7, 2030(~4.3 yrs left)· nominal 20-yr term from priority
A61P 7/00A61P 35/00A61P 19/08A61K 9/4866A61K 9/0053A61K 31/506A61K 2121/00A61K 9/48A61K 9/4858
56
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Claims

Abstract

Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or a hydrate thereof.

Claims

exact text as granted — not AI-modified
1 - 69 . (canceled) 
     
     
         70 . A unit dosage form for ingestion to the stomach, the unit dosage form comprising:
 (i) a compound:   
       
         
           
           
               
               
           
         
         
           or a pharmaceutically acceptable salt or hydrate thereof; 
         
         (ii) a microcrystalline cellulose, wherein the weight ratio of the compound to the microcrystalline cellulose is about 1:1.5 to about 1:9; and 
         (iii) about 0.5% to about 5% w/w of sodium stearyl fumarate. 
       
     
     
         71 . The unit dosage form of  claim 70 , wherein the weight ratio of the compound to the microcrystalline cellulose is about 1:1.5 to about 1:2. 
     
     
         72 . The unit dosage form of  claim 70 , wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 
     
     
         73 . The unit dosage form of  claim 70 , wherein the unit dosage form comprises about 0.5% to about 2% w/w of sodium stearyl fumarate. 
     
     
         74 . The unit dosage form of  claim 73 , wherein the unit dosage form comprises about 1% w/w of sodium stearyl fumarate. 
     
     
         75 . The unit dosage form of  claim 70 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         76 . The unit dosage form of  claim 71 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:2. 
       
     
     
         77 . The unit dosage form of  claim 72 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         78 . The unit dosage form of  claim 73 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         79 . The unit dosage form of  claim 74 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         80 . A unit dosage form for ingestion to the stomach, the unit dosage form comprising:
 (i) a compound:   
       
         
           
           
               
               
           
         
         
           or a pharmaceutically acceptable salt or hydrate thereof; 
         
         (ii) a microcrystalline cellulose, wherein the weight ratio of the compound to the microcrystalline cellulose is 1:1.5 to 1:9; and 
         (iii) one or more lubricants. 
       
     
     
         81 . The unit dosage form of  claim 80 , wherein the one or more lubricants comprises sodium stearyl fumarate. 
     
     
         82 . The unit dosage form of  claim 80 , wherein the weight ratio of the compound to the microcrystalline cellulose is 1:1.5 to 1:2. 
     
     
         83 . The unit dosage form of  claim 80 , wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 
     
     
         84 . The unit dosage form of  claim 80 , wherein the unit dosage form comprises about 0.5% to about 5% w/w of the one or more lubricants. 
     
     
         85 . The unit dosage form of  claim 84 , wherein the unit dosage form comprises about 0.5% to about 2% w/w of the one or more lubricants. 
     
     
         86 . The unit dosage form of  claim 85 , wherein the unit dosage form comprises about 1% w/w of the one or more lubricants. 
     
     
         87 . The unit dosage form of  claim 80 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         88 . The unit dosage form of  claim 81 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         89 . The unit dosage form of  claim 82 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:2. 
       
     
     
         90 . The unit dosage form of  claim 83 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         91 . The unit dosage form of  claim 84 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         92 . The unit dosage form of  claim 85 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         93 . The unit dosage form of  claim 86 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the weight ratio of 
 
       
         
           
           
               
               
           
         
         to the microcrystalline cellulose is about 1:1.5 to about 1:9. 
       
     
     
         94 . A unit dosage form for ingestion to the stomach, the unit dosage form comprising:
 (i) a compound:   
       
         
           
           
               
               
           
         
         
           or a pharmaceutically acceptable salt or hydrate thereof; 
         
         (ii) one or more fillers and/or diluents; and 
         (iii) about 0.5% to about 5% w/w of sodium stearyl fumarate. 
       
     
     
         95 . The unit dosage form of  claim 94 , wherein the one or more fillers and/or diluents comprises a microcrystalline cellulose. 
     
     
         96 . The unit dosage form of  claim 95 , wherein the microcrystalline cellulose is silicified microcrystalline cellulose. 
     
     
         97 . The unit dosage form of  claim 94 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
     
     
         98 . The unit dosage form of  claim 95 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
     
     
         99 . The unit dosage form of  claim 96 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
     
     
         100 . A unit dosage form for ingestion to the stomach, the unit dosage form comprising:
 (i) a compound:   
       
         
           
           
               
               
           
         
         
           or a pharmaceutically acceptable salt or hydrate thereof; 
         
         (ii) one or more fillers and/or diluents, wherein the ratio of the weight of the compound to the total weight of the one or more fillers and/or diluents is about 1:1.5 to about 1:9; and 
         (iii) about 0.5% to about 5% w/w of a lubricant. 
       
     
     
         101 . The unit dosage form of  claim 100 , wherein the compound is in the form of a dihydrochloride monohydrate: 
       
         
           
           
               
               
           
         
       
       and
 the ratio of the weight of 
 
       
         
           
           
               
               
           
         
         to the total weight of the one or more fillers and/or diluents is about 1:1.5 to about 1:9. 
       
     
     
         102 . The unit dosage form of  claim 100 , wherein the ratio of the weight of the compound to the total weight of the one or more fillers and/or diluents is about 1:1.5 to about 1:2. 
     
     
         103 . The unit dosage form of  claim 100 , wherein the unit dosage form comprises about 0.5% to about 2% w/w of the lubricant. 
     
     
         104 . The unit dosage form of  claim 103 , wherein the unit dosage form comprises about 1% w/w of the lubricant.

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