Claims
- 1. Compounds having the structure ##STR6## wherein R represents hydrogen or methyl and wherein R' represents 2-butyl, .alpha.-methylallyl, or 3-pentyl, together with their pharmaceutically acceptable acid addition salts.
- 2. The compound of claim 1 which is N-2-butylnorcodeine.
- 3. The compound of claim 1 which is N-.alpha.-methylallylnorcodeine.
- 4. The compound of claim 1 which is N-3-pentylnorcodeine.
- 5. The compound of claim 1 which is N-2-butylnormorphine.
- 6. The compound of claim 1 which is N-.alpha.-methylallylnormorphine.
- 7. The compound of claim 1 which is N-3-pentylnormorphine.
- 8. A dosage unit for pharmaceutical composition for the amelioration of pain comprising an amount within a range of from about 2 to 1750 mg per dosage unit, therapeutically effective to ameliorate pain, of at least one compound selected from the group consisting of N-2-butylnormorphine, N-.alpha.-methylallylnormorphine, N-3-pentylnormorphine and their pharmaceutically acceptable acid addition salts, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 9. A method having little addiction potential for ameliorating pain in a warm-blooded animal, said method comprising administering to said animal an amount, effective to ameliorate the pain, of at least one compound selected from the group consisting of N-2-butylnormorphine, N-.alpha.-methylallylnormorphine and N-3-pentylnormorphine, together with the salts thereof, said compounds having good antagonist characteristics.
Parent Case Info
This application is a division of application Ser. No. 909,257, filed May 24, 1978, now U.S. Pat. No. 4,218,454, which application is a continuation-in-part of Ser. No. 813,796, filed July 8, 1977, now abandoned.
Government Interests
The invention described herein was made in the course of work under a grant or award from the Department of Health, Education and Welfare.
US Referenced Citations (5)
Non-Patent Literature Citations (5)
Entry |
Clark et al., J. Am. Chem. Soc. v. 75, pp. 4963-4966 (1953). |
Winter et al., Arch. Int. Pharmacodyn, CX No. 2-3, pp. 186-202 (1957). |
Loew et al., Opiates Endog. Opiod. Pept. Proc. Int. Narc. Res. Club Meet, 1976, pp. 399-402, abstract CA, v. 87, 127012g. |
De Graw et al., J. Med. Chem. 21, pp. 415-422 (1978). |
Uyeno et al., Proc. West, Pharmacol. Soc. 1978, 21, pp. 357-360, Chemical Abstracts, vol. 90, 97480a. |
Divisions (1)
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Number |
Date |
Country |
Parent |
909257 |
May 1978 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
813796 |
Jul 1977 |
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