US 12,264,164 B2
Method of treatment of symptoms of menopause
Mike Trower, Stevenage (GB); Monica Lazaro, St. Petersburg, FL (US); Derek Bush, St. Petersburg, FL (US); David Elder, Hertford (GB); and Mary Kerr, Stevenage (GB)
Assigned to KANDY THERAPEUTICS LIMITED, Berkshire (GB)
Filed by KaNDy Therapeutics Limited, Berkshire (GB)
Filed on Jul. 31, 2023, as Appl. No. 18/228,593.
Application 16/984,961 is a division of application No. 16/351,659, filed on Mar. 13, 2019, granted, now 10,774,091, issued on Sep. 15, 2020.
Application 18/228,593 is a continuation of application No. 18/097,046, filed on Jan. 13, 2023, granted, now 11,767,328.
Application 18/097,046 is a continuation of application No. 16/984,961, filed on Aug. 4, 2020, granted, now 11,591,346, issued on Feb. 28, 2023.
Claims priority of provisional application 62/642,622, filed on Mar. 14, 2018.
Prior Publication US 2023/0382922 A1, Nov. 30, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 498/04 (2006.01); A61K 31/5383 (2006.01); A61P 15/00 (2006.01)
CPC C07D 498/04 (2013.01) [A61K 31/5383 (2013.01); A61P 15/00 (2018.01); C07B 2200/13 (2013.01)] 23 Claims
 
1. A method of treating vasomotor symptoms, insomnia associated with menopause, sleep disturbances associated with menopause, night time awakenings associated with menopause, or any combination thereof, comprising administering to a human in need thereof a pharmaceutically effective dose of 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 (Compound A):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof;
wherein compound A or a pharmaceutically acceptable salt thereof is administered in an oral form so as to reach pharmacokinetic (PK) exposures similar to that achieved when a soft gelatin capsule with a filling comprising:
(a) Compound A or a pharmaceutically acceptable salt thereof;
(b) at least one solubilizer selected from caprylocaproyl polyoxyl-8 glycerides, glycerol monocaprylocaprate, polyoxyl 35 castor oil, and polysorbate 80, or any mixtures thereof; and
(c) at least one antioxidant selected from DL-alpha-tocopherol, butylated hydroxytoluene, and butylated hydroxyanisole, or any mixtures thereof is administered.