Claims
- 1. 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.
- 2. A compound of claim 1, whereinR1 is benzyl group or the group of formula: R4CO— wherein R4 is an alkyl group having 1 to 18 carbon atoms, phenyl group, or phenyl group substituted with one or more C1-4alkyl groups; R2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 4 carbon atoms or a halogen atom; and R3 is a hydrogen atom, an alkyl group having having 1 to 4 carbon atoms, —(CH2)nNH2—, —CO(CH2)nCO2H or —(CH2)nCO2H (wherein, n is 1 or 2).
- 3. A compound of claim 1, wherein X is oxygen atom and A is —CH2—.
- 4. A compound of claim 1, wherein X is sulfur atom and A is —NHCH2—.
- 5. A compound of claim 1, wherein R3 is a hydrogen atom, methyoxymethyl group, —CH2CH2NH2, —COCH2CH2CO2H or —CH2CO2H.
- 6. A compound of claim 1, wherein R2 is selected from the group of consisting of a hydrogen atom, t-butyl, 3,4-(dimethyl) and chloro atom.
- 7. A compound of claim 1, wherein R4 is selected from the group of consisting of t-butyl, i-propyl, pentyl, heptadecyl, phenyl and 3,4-(dimethyl)phenyl group.
- 8. A compound of claim 1, which is one selected from the group of consisting of2,2-dimethyl propionic acid 2-({2-[4-(2-aminoethoxy)-3-methoxyphenyl]acetylamino}methyl)-3-(3,4-dimethylphenyl)propyl ester; 2,2-dimethyl propionic acid 2-({2-[4-(2-aminoethoxy)-3-methoxyphenyl]acetylamino}methyl)-3-(4-tert-butylphenyl)propyl ester; 2,2-dimethyl propionic acid 2-benzyl 3-[3-(4-hydroxy-3-methoxybenzyl)thioureido]propyl ester; 2-methyl propionic acid 2-benzyl 3-[3-(4-hydroxy-3-methoxybenzyl)thioureido]propyl ester; 2,2-dimethyl propionic acid 2-(3,4-dimethylbenzyl)-3-[3-(4-hydroxy-3-methoxybenzyl)thioureido]propyl ester; and 2,2-dimethyl propionic acid 2-(4-tert-butylbenzyl)-3-[3-(4-hydroxy-3-methoxybenzyl)thioureido]propyl ester.
- 9. A pharmaceutical composition comprising the compound (I) as an active ingredient together with a pharmaceutically acceptable carrier.
- 10. A pharmaceutical composition of claim 9, which comprises the compound (I) as an active ingredient in an amount effective to alleviate or relieve acute, chronic, inflammatory or neuropathic pains, suppress inflammation, or treat urge incontinence together with a pharmaceutically acceptable carrier.
- 11. 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.
- 12. 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.
Priority Claims (1)
Number |
Date |
Country |
Kind |
99-5751 |
Feb 1999 |
KR |
|
CROSS REFERENCE TO RELATED APPLICATION
This application is a 371 of International Application PCT/KR00/00137, with an international filing date of Feb. 21, 2000, designating the United States of America.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/KR00/00137 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO00/50387 |
8/31/2000 |
WO |
A |
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5431914 |
Adekunie et al. |
Jul 1995 |
A |
Non-Patent Literature Citations (4)
Entry |
Analogues of Capsaicin with Agonist Activity as Novel Analgesic Agents; Structure-Activity Studies. 2. The amide Bond “B-Region” Walpole et al, J. Med. Chem. vol. 36 pp 2373-2380 (1993).* |
Analogues of Capsaicin with Agonist Activity as Novel Analgesic Agents; Structure-Activity Studies. 3. The Hydrophobic Side-Chain “C-Region” Walpole et al, J. Med. Chem. vol. 36 pp 2381-2389 (1993).* |
“Analogues of Capsaicin with Agonist Activity as Novel Analgesic Agents; Structure-Activity Studies. 4. Potent, Orally Active Analgesics” Wriggleworth et al, J. Med. Chem. vol. 39 pp 4942-4951 (1996).* |
“3-Acyloxy-2-phenylalkylpropyl Amides and Esters of Homovanillic Acid as Novel Vanilloid Receptor Agonists” Lee et al, Biorganic and Medicinal Chemistry Letters vol. 9 pp 2909-2914 (1999). |