Novel methysergide derivatives
AssigneeMAP Pharmaceuticals, Inc.
InventorsLibo Wu, Jian Zhang
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Abstract
Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders or symptoms thereof, such as, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are methods for antagonizing the 5-HT2B receptor without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein such as, for example, are methods of agonizing the 5-HT1A receptor using the compounds and compositions disclosed herein.
Claims20
A compound of Formula (I) or (II):
- or salts, polymorphs, hydrates or solvates thereof, wherein:
- R1 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl, (C1-C4) alkyl substituted with one or more fluorine atoms, (C1-C4) acyl, substituted (C1-C4) acyl, (C1-C4) heteroalkyl or substituted (C1-C4) heteroalkyl;
- R2 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl, (C1-C4) alkyl substituted with one or more fluorine atoms, (C1-C4) acyl, substituted (C1-C4) acyl, halogen, —OH, (C1-C4) heteroalkyl or substituted (C1-C4) heteroalkyl;
- R3 is alkyl, substituted alkyl, acyl, substituted acyl, halo, heteroalkyl, substituted heteroalkyl, —NO2, —N3, —OH, —S(O)kR100, —OR101, —NR102R103, —CONR104R105, —CO2R106 or —O2CR107;
- R4 is hydrogen, (C1-C3) alkyl, (C1-C3) substituted alkyl or (C1-C3) alkyl substituted with one or more fluorine atoms;
- R5 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl, (C1-C4) alkyl substituted with one or more fluorine atoms, (C1-C4) heteroalkyl or substituted (C1-C4) heteroalkyl;
- R6 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl, (C1-C3) alkyl substituted with one or more fluorine atoms, (C1-C4) heteroalkyl or substituted (C1-C4) heteroalkyl;
- n is 0, 1, 2 or 3;
- o is 0, 1, 2, 3 or 4;
- k is 0, 1 or 2;
- and
- R100-R107 are independently hydrogen, alkyl, substituted alkyl, acyl, substituted acyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl;
- provided that both R1 and R2 are not hydrogen and that when R1 is —CH3, n is 0, o is 1, R4 is —CH3, R5 is hydrogen and R6 is hydrogen that R2 is not hydrogen.
Dependencies are inferred from the claim text.