Fluoroergoline analogs
AssigneeMAP Pharmaceuticals, Inc.
InventorsRobert O. Cook, Jian Zhang, Thomas A. Armer
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Abstract
Provided herein are novel fluoroergoline derivatives 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, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.
Claims16
A compound of Formula (I) or (II):
- or ion pairs, polymorphs, salts, hydrates or solvates thereof, wherein:
- R1 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl or (C1-C4) alkyl substituted with one or more fluorine atoms;
- R2 is alkyl, substituted alkyl, acyl, substituted acyl, halo, heteroalkyl, substituted heteroalkyl, —NO2, —N3, —OH, —S(O)kR100, —OR101, —NR102R103, —CONR104R105, —CO2R106 or —OC(O)R107;
- R3 is hydrogen, (C1-C3) alkyl, (C1-C3) substituted alkyl or (C1-C3) alkyl substituted with one or more fluorine atoms;
- R5 is (C1-C4) alkyl or (C1-C4) substituted alkyl;
- R6 is hydrogen, (C1-C4) alkyl, substituted (C1-C4) alkyl, benzyl or substituted benzyl;
- R7 is C1-C4) alkyl, substituted (C1-C4) alkyl, benzyl or substituted benzyl;
- R8 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R108 or —CONR109R110;
- R9 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R111 or —CONR112R113;
- R10 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R114 or —CONR115R116;
- R11 is (C1-C3) alkyl substituted with one or more fluorine atoms;
- R100-R116 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;
- k is 0, 1 or 2;
- and
- n is 0, 1, 2 or 3.
Dependencies are inferred from the claim text.