US2021236506A1PendingUtilityA1

Novel uses

68
Assignee: KANDY THERAPEUTICS LTDPriority: May 18, 2015Filed: Feb 10, 2021Published: Aug 5, 2021
Est. expiryMay 18, 2035(~8.8 yrs left)· nominal 20-yr term from priority
Inventors:Mike Trower
A61K 45/06A61K 31/5365A61K 31/40A61K 31/5383A61P 15/02A61K 31/436A61P 43/00A61P 5/24A61K 31/444A61P 15/00A61K 9/00A61K 9/0095A61K 31/4436A61P 15/12A61P 5/26A61K 31/4439C07D 498/04
68
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Claims

Abstract

This invention relates to new use of dual NK-1/NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.

Claims

exact text as granted — not AI-modified
1 - 10 . (canceled) 
     
     
         11 . A method of treating vasomotor symptoms in a human in need thereof, comprising administering to the human an effective amount of 2-[3,5-bis(trifluoromethyl)phenyl]-N-{-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide. 
     
     
         12 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate form. 
     
     
         13 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has characteristic 2 theta angles occurring at 4.3±0.1, 7.9±0.1, 9.8±0.1, 10.7±0.1, 10.8±0.1, 13.3±0.1, 14.0±0.1, and 15.1±0.1 degrees. 
     
     
         14 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has d-spacing at 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3, and 5.9 Angstroms. 
     
     
         15 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is orally administered to the human. 
     
     
         16 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is administered to the human in the form of a tablet, powder, lozenge, or capsule. 
     
     
         17 . The method of  claim 11 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino [2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is administered to the human in the form of a gelatine capsule. 
     
     
         18 . A method of treating vasomotor symptoms in a human in need thereof, comprising orally administering to the human a composition comprising 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide. 
     
     
         19 . The method of  claim 18 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate form. 
     
     
         20 . The method of  claim 18 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has characteristic 2 theta angles occurring at 4.3±0.1, 7.9±0.1, 9.8±0.1, 10.7±0.1, 10.8±0.1, 13.3±0.1, 14.0±0.1, and 15.1±0.1 degrees. 
     
     
         21 . The method of  claim 18 , wherein the 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide is in crystalline anhydrate Form 1 and has d-spacing at 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3, and 5.9 Angstroms. 
     
     
         22 . The method of  claim 18 , wherein the composition further comprises at least one pharmaceutically acceptable excipient or carrier. 
     
     
         23 . The method of  claim 18 , wherein the composition is administered to the human in the form of a tablet, powder, lozenge, or capsule. 
     
     
         24 . The method of  claim 18 , wherein the composition is administered to the human in the form of a gelatine capsule.

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