Vanilloid analogues containing resinferatoxin pharmacophores as potent vanilloid receptor agonists and analgesics, compositions and uses thereof
AssigneesPacific Corporation, Digital Biotech Co., Ltd.
InventorsJeewoo Lee, Uhtaek Oh, Young-Ho Park, Young-Ger Suh, Hyeung-Geun Park, Hee-Doo Kim
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Abstract
The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
Claims12
A compound represented by the following formula (I):
- wherein,
- X is an oxygen or sulfur atom;
- A is —NHCH2— or —CH2—;
- R1 is a substituted or unsubstituted C1-4alkaryl group, or the group of the formula:
- R4CO— wherein R4 is an alkyl group having 1 to 18 carbon atoms, an alkenyl group having 2 to 18 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 10 carbon atoms;
- R2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or a halogen atom;
- R3 is a hydrogen atom, an alkyl grouip having 1 to 4 carbon atoms, an aminoalkyl, a diacid monoester, α-alkyl acid;
- n is an integer of 1 to 2;
- and
- the asterisk mark * indicates a chiral carbon atom, and its pharmaceutically accepatable salts.
A pharmaceutical composition comprising the compound (I) as an active ingredient together with a pharmaceutically acceptable carrier.
A method of alleviating or relieving acute, chronic, inflammatory or neuropathic pains of suppressing inflammation or treating urge incontinence which comprises administering to a subject suffering from such pains, inflammation or incontinence the compound (I) in an amount effective for alleviating or releiving the pains, inflammation or incontinence.
A method of treating bladder hypersensitivity which comprises administering to a subject requiring such treatment the compound (I) in an amount effective for alleviating or relieving the bladder hypersensitivity.
Dependencies are inferred from the claim text.