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Publication Number
US-9012640-B2
Publication Date
2015-04-21
Expiration Date
Abstract
Provided herein are novel cabergoline analogs and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B receptor and 5-HT2C receptors the using the compounds and compositions disclosed herein.
Core Innovation
Cabergoline derivatives are disclosed as novel analogs and compositions for treating central nervous system disorders. The disclosure specifies cabergoline-derivative compounds in relation to Formula (I) or Formula (II), including related structures with variable substituents such as R1, R2(n), R5, R7, R8/R9, and R11.
The background problem addressed is cabergoline’s undesirable 5-HT2B agonism, which is associated with fibrosis and was withdrawn. The disclosure describes modified cabergoline-derivative compounds intended to provide dopaminergic D2 receptor agonism and/or antagonism/inhibition of 5-HT receptors, including 5-HT2 receptors.
The compounds are defined with substituent constraints for R1, R5, and R11, where R1 and R11 are alkyl substituted with one or more fluorine atoms and R5 is hydrogen or an alkyl group, as stated. The disclosure also describes formulations that can include salts, prodrugs, solvates, or hydrates, and combinations with a vehicle.
Claims Coverage
The provided claim text contains one independent compound claim and dependent claims that narrow the substituent options, plus one dependent composition claim including a vehicle. The inventive coverage centers on a cabergoline-derivative structure defined by substituent constraints.
Fluorinated alkyl substituent-defined cabergoline-derivative compound
A compound having the structure wherein R1 is hydrogen, (C1-C4) alkyl or (C1-C4) alkyl substituted with one or more fluorine atoms, R5 is hydrogen or (C1-C3) alkyl, and R11 is (C1-C3) alkyl substituted with one or more fluorine atoms.
Specific fluorinated alkyl substituent selections for R1, R5, and R11
A compound having the structure wherein R1 is —CH3 or —CF3, R5 is methyl or allyl, and R11 is —CF3.
Composition including the defined compound and a vehicle
A composition comprising the compound having the structure as defined, together with a vehicle.
The claim coverage focuses on cabergoline-derivative compounds defined by fluorinated alkyl substituent limits, with narrower dependent selections for R1, R5, and R11, and a composition claim that adds a vehicle.
Stated Advantages
Reduced 5-HT2A/5-HT2B activity is intended to reduce cabergoline-associated hallucination/fibrosis side effects.
Addresses cabergoline’s undesirable 5-HT2B agonism associated with fibrosis and its withdrawal.
Provides dopaminergic D2 receptor agonism and/or antagonism/inhibition of 5-HT receptors including 5-HT2 receptors.
Documented Applications
Treatment context for Parkinson’s disease, including possible combination therapy.
Treating central nervous system disorders including Parkinson’s disease and migraine.
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