Estradiol prodrugs and methods of use thereof
AssigneesUniversity of Maryland, Baltimore, The United States Government as represented by the Department of Veterans Affairs, The United States of America, as represented by the Secretary, Department of Health and Human Servic
InventorsTodd Gould, Istvan Merchenthaler, Polymnia Georgiou, Patrick Joseph Morris
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Abstract
Estradiol compounds and methods of using the same for treating diseases and conditions including depressive disorder, an anxiety disorder, post-traumatic stress disorder (PTSD), drug addiction, schizophrenia, Alzheimer's dementia, Parkinson's disease, stroke, traumatic brain injury (TBI), amyotrophic lateral sclerosis (ALS), complex regional pain syndrome (CRPS), chronic pain, neuropathic pain, anhedonia, fatigue, andropause-induced symptoms, and orchiectomy-induced symptoms are provided.
Claims28
A compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, cocrystal, or prodrug thereof:
- wherein in formula (I):
- L1 and L2 are each a linker comprising independently one or more of a bond, —C(O)—, —O—, —S—, —NRa—, —CRa2—, —C(O)O—, —C(O)S—, —C(O)NRa—, —C(O)NRaSO2—, disubstituted alkyl, disubstituted heteroalkyl, disubstituted alkenyl, disubstituted alkynyl, disubstituted cycloalkyl, disubstituted heterocycloalkyl, disubstituted aryl, disubstituted arylalkyl, disubstituted heteroaryl, and disubstituted heteroarylalkyl;
- Ra is independently selected at each occurrence from hydrogen, optionally substituted alkyl, optionally substituted fluoroalkyl, optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycloalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl;
- R1 is selected from optionally substituted alkyl, optionally substituted fluoroalkyl, optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycloalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl;
- R2 is selected from hydrogen, optionally substituted alkyl, optionally substituted fluoroalkyl, optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycloalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl;
- R3 is selected from hydrogen and optionally substituted alkynyl;
- and
- R4 is selected from hydrogen and optionally substituted alkyl.
Dependencies are inferred from the claim text.