C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 260/206
C07D 457/04 (2006.01) A61K 31/44 (2006.01)
Patent
CA 1292223
ABSTRACT OF THE DISCLSOURE The present invention as disclosed provides ergolines of Formula (III): Image wherein R is primary or secondary C1-8 alkyl, C2-4 alkenyl-CH2, C3-8 cycloalkyl or C3-6 cycloalkyl substituted C1-5 primary or secondary alkyl, the total number of carbon atoms in R not to exceed 8; R1 is allyl, H or C1-4 straight-chain alkyl; and R2 is Image wherein n is 0-4 and m is 1 or 2 except that, when n is 0, the ester function may not be attached to the cyclic ether ring alpha to the ring oxygen; (b) Image wherein R3 and R4 can be individually H, CH3 or C2H5; n can be 0, 1 or 2; R5 can be OH, OC1-3 alkyl, chloro, bromo, fluoro, CH3, CF3 or C2H5 when n is 1 or 2; R5 can be phenyl when n is 1; and R5 can be methylenedioxy when n is 2; or (c) monofluoro-, difluoro- or trifluoro- C2-5 alkyl; and pharmaceutically acceptable salts thereof. These compounds of Formula (III), where R1 is other than hydrogen,are useful as central or peripheral serotonin 5HT2 receptor antagonists and thus can be used in treating disease states in which an excess of circulating serotonin is a major contributing cause, eg. hypertension. The compounds of this invention wherein is H are useful as intermediates.
525125
Garbrecht William L.
Marzoni Gifford P.
Whitten Kathleen R.
Eli Lilly And Company
Garbrecht William L.
Gowling Lafleur Henderson Llp
Marzoni Gifford P.
Whitten Kathleen R.
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