US 11,858,932 B2
Methods and compositions for treating polycystic ovary syndrome
Christopher Barnes, South San Francisco, CA (US); David Karpf, South San Francisco, CA (US); and Mustafa Noor, South San Francisco, CA (US)
Assigned to Spruce Biosciences, Inc., South San Francisco, CA (US)
Filed by Spruce Biosciences, Inc., South San Francisco, CA (US)
Filed on Jun. 13, 2023, as Appl. No. 18/209,405.
Application 18/209,405 is a continuation of application No. 18/107,979, filed on Feb. 9, 2023.
Application 18/107,979 is a continuation of application No. PCT/US2021/045780, filed on Aug. 12, 2021.
Claims priority of provisional application 63/064,863, filed on Aug. 12, 2020.
Prior Publication US 2023/0322775 A1, Oct. 12, 2023
Int. Cl. C07D 471/04 (2006.01); A61P 15/08 (2006.01)
CPC C07D 471/04 (2013.01) [A61P 15/08 (2018.01)] 21 Claims
 
1. A method of treating polycystic ovary syndrome with functional adrenal hyperandrogenism (PCOS-FAH) in a subject in need thereof, comprising administering a CRF1 antagonist or pharmaceutically acceptable salt thereof;
wherein said CRF1 antagonist is a compound of Formula (I):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof, wherein:
R1 and R2 are independently ethyl or n-propyl;
R3 is hydrogen, F, Cl, Br, methyl, trifluoromethyl, or methoxy;
R4 is hydrogen, Br, —NRaRb, methoxymethyl, n-butyl, acetamido, pyridin-4-yl,
morpholin-4-yl,

OG Complex Work Unit Chemistry
Ra and Rb are independently hydrogen, C1-C3alkyl, —CH2CH2NH2, —CH2CH2NHC(O)OC(CH3)3, or —CH2CH2NHCH2CH2CH3.