Morphinan Derivatives with High Oral Bioavailability
The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction.
1 A method of treating a mental illness associated with opioid receptor activity or blockade comprising orally administering a compound of formula:
or a pharmaceutically acceptable salt, ester or prodrug thereof to a subject in need thereof, wherein said compound is administered in a daily dosage of about 1.5 mg/day to about 5 mg/day.
2 . The method according to claim 1 , wherein the mental illness is depression.
3 . The method according to claim 1 , wherein the daily dosage is about 1 mg/day.
4 . The method according to claim 1 , wherein the daily dosage is about 1.5 mg/day.
5 . The method according to claim 1 , wherein the daily dosage is about 2 mg/day.
6 . The method according to claim 1 , wherein the daily dosage is about 3 mg/day.
7 . The method according to claim 2 , wherein the daily dosage is about 1 mg/day.
8 . The method according to claim 2 , wherein the daily dosage is about 1.5 mg/day.
9 . The method according to claim 2 , wherein the daily dosage is about 2 mg/day.
10 . The method according to claim 2 , wherein the daily dosage is about 3 mg/day.
11 . A method of treating a mental illness associated with opioid receptor activity or blockade comprising orally administering a compound of formula:
or a pharmaceutically acceptable salt, ester or prodrug thereof to a subject in need thereof, wherein said compound is administered in a daily dosage of less than 5 mg/day.
12 . The method according to claim 11 , wherein the mental illness is depression.
13 . The method according to claim 11 , wherein the daily dosage is about 1 mg/day.
14 . The method according to claim 11 , wherein the daily dosage is about 1.5 mg/day.
15 . The method according to claim 11 , wherein the daily dosage is about 2 mg/day.
16 . The method according to claim 11 , wherein the daily dosage is about 3 mg/day.
17 . The method according to claim 12 , wherein the daily dosage is about 1 mg/day.
18 . The method according to claim 12 , wherein the daily dosage is about 1.5 mg/day.
19 . The method according to claim 12 , wherein the daily dosage is about 2 mg/day.
20 . The method according to claim 12 , wherein the daily dosage is about 3 mg/day.