Patent
Analgesic use of N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester
| العنوان: | Analgesic use of N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester |
|---|---|
| Patent Number: | 5,654,334 |
| تاريخ النشر: | August 05, 1997 |
| Appl. No: | 08/590,409 |
| Application Filed: | January 25, 1996 |
| مستخلص: | N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester and/or its derivatives has been found to have analgesic pain relieving properties. It has been found to be especially effective in relieving pain associated with osteoarthritis and multiple sclerosis. It can be administered by itself or in combination with other analgesics. When given in combination with other analgesics, N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester and/or its derivatives helps to alleviate the detrimental side effects of other analgesic medications by lowering the dosage requirements for pain relief. |
| Inventors: | Edmundson, Allen B. (Oklahoma City, OK); Manion, Carl V. (Oklahoma City, OK) |
| Assignees: | Oklahoma Medical Research Foundation (Oklahoma City, OK) |
| Claim: | We claim |
| Claim: | 1. A method of decreasing pain in a patient comprising administering to said patient in need of such treatment an effective amount of a composition comprising: ##STR1## where R is H or an alkyl containing 1 to 6 carbons to effect a reduction in perceived pain by said patient, wherein an effective amount of said composition is from about 80 milligrams to about 320 milligrams. |
| Claim: | 2. A method of decreasing pain in a patient comprising administering to said patient in need of such treatment an effective amount of a composition comprising: ##STR2## where R is H or an alkyl containing 1 to 6 carbons to effect a reduction in perceived pain by said patient, wherein an effective amount of said composition is about 180 milligrams. |
| Claim: | 3. A method of decreasing the dosage of a first analgesic medication in a patient for pain, comprising administering to said patient in need of such treatment an effective amount of a second compound comprising: ##STR3## where R is H or an alkyl containing 1 to 6 carbons to cause a reduction in perceived pain by said patient. |
| Claim: | 4. The method of claim 3, wherein said first analgesic medication is selected from the group consisting of acetaminophen, phenacetin, aspirin, ibuprofen, phenylbutazone, indomethacin and derivatives, opiates and derivatives, piroxacam, and steroidal and nonsteroidal anti-inflammatory agents. |
| Claim: | 5. The method of claim 3, wherein said effective amount of said second compound is from about 40 milligrams to about 540 milligrams. |
| Claim: | 6. The method of claim 4, wherein said effective amount of said second compound is from about 40 milligrams to about 540 milligrams. |
| Claim: | 7. The method of claim 3, wherein an effective amount of said second compound is that amount required to reduce the effective dosage of said first analgesic medication by about 25% to about 75%. |
| Claim: | 8. The method of claim 4, wherein an effective amount of said second compound is that amount required to reduce the effective dosage of said first analgesic medication by about 25% to about 75%. |
| Claim: | 9. The method of claim 3, wherein an effective amount of said second compound is that amount required to reduce the effective dosage of said first analgesic medication by about 10% to about 90%. |
| Claim: | 10. The method of claim 4, wherein an effective amount of said second compound is that amount required to reduce the effective dosage of said first analgesic medication by about 10% to about 90%. |
| Claim: | 11. A method for treating an osteoarthritis patient for pain, comprising the steps of: administering an effective amount of a composition comprising: ##STR4## where R is CH.sub.3 to effect a reduction in perceived pain by said patient, wherein said composition is the sole active pain-relieving agent administered to said patient. |
| Claim: | 12. A method of treating pain in a patient comprising administering to said patient in need of such treatment an effective pain-reducing amount of an active pain-relieving agent, wherein said active pain-relieving agent consists of a composition of the formula: ##STR5## where R is CH.sub.3. |
| Claim: | 13. The method of claim 12, wherein said effective amount is greater than 40 mg. |
| Claim: | 14. The method of claim 12, wherein said effective amount is from about 80 mg to about 540 mg. |
| Current U.S. Class: | 514/538 |
| Current International Class: | A61K 3124 |
| Patent References Cited: | 3492131 January 1970 Schlatter 4689218 August 1987 Gazzaniga et al. 5053393 October 1991 Tjoeng 5053396 October 1991 Blass 5496856 March 1996 Creppy |
| Other References: | Leon et al., "Safety of Long-term Large Doses of Aspartame", Archives of Internal Medicine, 149, pp. 2318-2324 1989. Douglas, W.W., "Polypeptides-angiotensin, plasma kinins, and other vasoactive agents; prostaglandins," The Pharmacological Basis of Therapeutics, 5th ed., L. S. Goodman and A. Gilman (eds.), MacMillan Publishing Co., Inc., New York, p. 647 (1975). Guiso, et al., "Effect of tyrosine on the potentiation by aspartame and phenylalanine of metrazol-induced convulsions in rats," Fd Chem Toxic 29:855-857 (1991). Insel, Paul, "Analgesic-antipyretic and antiinflammatory agents and drugs employed in the treatment of gout," The Pharmacological Basis of Therapeutics, 9th ed., J. G. Hardman and L.E. Limbird (eds.), McGraw-Hill Companies, Inc., New York, pp. 620-622 (1996). Picot, et al., "The x-ray crystal structure of the membrane protein prostaglandin H.sub.2 synthase-1," Nature 367:243-249 (1991). |
| Primary Examiner: | Henley, III, Raymond |
| Attorney, Agent or Firm: | Sidley & Austin |
| رقم الانضمام: | edspgr.05654334 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |