Claims
- 1. A method for agonizing or antagonizing the ORL1 (opioid receptor-like) receptor of the nociceptin/orphanin FQ ligand ORL1 receptor system, the method comprising administering, to a cell comprising said receptor system, an effective amount of a composition comprising a morphinan compound of formula I:
- 2. A method according to claim 1, wherein R2 denotes a C1-10 alkyl group.
- 3. A method according to claim 1, wherein R2 denotes a C2-10 alkenyl group.
- 4. A method according to claim 1, wherein R3 denotes a C1-10 alkyl group.
- 5. A method according to claim 1, wherein R3 denotes a C2-10 alkenyl group.
- 6. A method according to claim 1, wherein R4 denotes H a C1-10 alkyl group.
- 7. A method according to claim 1, wherein R4 denotes a C2-10 alkenyl group.
- 8. A method according to claim 1, wherein R5 denotes a C1-10 alkyl group.
- 9. A method according to claim 1, wherein R5 denotes a C2-10 alkenyl group.
- 10. A method for antagonizing the ORL1 receptor of the nociceptin/orphanin FQ ligand ORL1 receptor system according to claim 1, wherein the morphinan compound is:
17-allyl-6,7-didehydro-4,5α-epoxy-3,14-dihydroxy-1′-(o-chlorobenzyl)indolo [6,7:2,′3′]-morphinan hydrochloride, 17-allyl-6,7-didehydro-4,5α-epoxy-3-hydroxy-14-(m-chloro-methoxyphenyl) 1′-(m-chlorobenzyl)indolo[6,7:2,′3′]-morphinan hydrochloride, or 17-cyclopropylmethyl-6,7-didehydro-4,5α-epoxy-3-hydroxy-14-(o-chloromethoxyphenyl) 1′-(o-chlorobenzyl)indolo[6,7:2,′3′]-morphinan hydrochloride.
- 11. A method for agonizing the ORL1 receptor of the nociceptin/orphanin FQ ligand ORL1 receptor system according to claim 1, wherein the morphinan compound is:
17-cyclopropylmethyl-6,7-didehydro-4,5α-epoxy-3-hydroxy-14-(methoxynaphthalene) 1′-(p-methylnaphthalene)indolo-[6,7:2,′3′]-morphinan hydrochloride or 17-cyclopropylmethyl-6,7-didehydro-4,5α-epoxy-14-hydroxy-3-benzyloxy-1′-(p-methoxycarbonylmethylphenyl)-indolo [6,7:2,′3′]-morphinan hydrochloride.
- 12. A method for the treatment of at least one condition selected from the group consisting of neuropathic pain, anxiolysis, depression, diuresis, urinary incontinence, hypotension, hypertension, senile dementia, Alzheimer's disease, general cognitive dysfunctions, tinnitus, impaired hearing, epilepsy, obesity, and cachexia, the method comprising administering an effective amount of a compound of formula I:
- 13. A method according to claim 12, wherein the morphinan compound is selected from the group consisting of:
17-allyl-6,7-didehydro-4,5α-epoxy-3,14-dihydroxy-1′-(o-chlorobenzyl)indolo [6,7:2,′3′]-morphinan hydrochloride; 17-allyl-6,7-didehydro-4,5α-epoxy-3-hydroxy-14-(m-chloro-methoxyphenyl) 1′-(m-chlorobenzyl)indolo-[6,7:2,′3′]-morphinan hydrochloride; 17-cyclopropylmethyl-6,7-didehydro-4,5α-epoxy-3-hydroxy-14-(o-chloromethoxyphenyl) 1′-(o-chlorobenzyl) -indolo [6,7:2,′3′]-morphinan hydrochloride; 17-cyclopropylmethyl-6,7-didehydro-4,5cc-epoxy-3-hydroxy-14-(methoxynaphthalene) 1′-(β-methyl-naphthalene)indolo-[6,7:2,′3′]-morphinan hydrochloride; and 17-cyclopropylmethyl-6,7-didehydro-4,5α-epoxy-14-hydroxy-3-benzyloxy-1′-(p-methoxycarbonylmethylphenyl)-indolo [6,7:2,′3′]-morphinan hydrochloride.
Priority Claims (1)
Number |
Date |
Country |
Kind |
199 39 044.4 |
Aug 1999 |
DE |
|
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] The present application is a continuation of international patent application no. PCT/EP00/07585, filed Aug. 4, 2000, designating the United States of America, the entire disclosure of which is incorporated herein by reference. Priority is claimed based on Federal Republic of Germany patent application no. 199 39 044.4, filed Aug. 18, 1999.
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/EP00/07585 |
Aug 2000 |
US |
Child |
10076109 |
Feb 2002 |
US |