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US 10,300,056 B2Granted
CGRP receptor antagonists
AssigneeHeptares Therapeutics Limited
InventorsJohn Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
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Abstract
The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
Claims19
A method for treating a CGRP-mediated cerebrovascular or vascular disorder in a subject comprising administering to the subject a compound of formula (I)
- or a salt thereof, wherein R1 is H or Q-(C1-C6)alkyl;
- where Q is a bond, C(O) or C(O)O and where the (C1-C6)alkyl can be optionally substituted by N(C1-C3alkyl)2 or CO2H;
- R2 is H or forms a spirocyclic heterocyclic ring with R3;
- R3 forms a spirocyclic heterocyclic ring with R2 or is a heterocyclic ring if R2 is H;
- and R4 is an optionally substituted aryl group which may be monocyclic or fused to a further ring, wherein the disorder is selected from the group consisting migraine without aura, chronic migraine, pure menstrual migraine, menstrually-related migraine, migraine with aura, familial hemiplegic migraine, sporadic hemiplegic migraine, basilar-type migraine, cyclical vomiting, abdominal migraine, benign paroxysmal vertigo of childhood, retinal migraine, status migrainosus, cluster headache, dialysis headache, paroxysmal hemicrania, osteoarthritis, hot flashes associated with menopause or medically induced menopause due to surgery or drug treatment, hemicrania continua, cyclic vomiting syndrome, rosacea and joint pain associated with osteoarthritis or rheumatoid arthritis.
2 more elements
Dependencies are inferred from the claim text.