IP Library Granted Patent US 9,321,780
Granted Patent B2
US 9,321,780 · App. 14/697,174 · Granted Apr 26, 2016

Buprenorphine dimer and its use in treatment of gastrointestinal disorders

Inventor: Nikhilesh Nihala Singh (Mill Valley, CA)
Assignee: OrphoMed, Inc.
C07D489/02A61K31/137A61K31/167A61K31/485C07C217/64C07C217/70C07C233/16C07C233/25C07C233/43C07D489/00C07D489/08C07C2101/14
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,321,780
App. No.
14/697,174
Granted
Apr 26, 2016
Kind
B2
Abstract

The present invention provides a buprenorphine dimer compound, wherein the two buprenorphine portions are linked via an ethylene spacer, wherein the spacer is bonded to the two opioid molecules via an ether bond. Pharmaceutical compositions comprising such a buprenorphine dimer drug are also disclosed, and the use of such compounds in the treatment of gastrointestinal hyperalgesia generally and in particular diarrhea-predominant irritable bowel syndrome.

Claims (11)

1. A buprenorphine dimer compound having Formula (I):

or a pharmaceutically acceptable salt or solvate thereof.

2. The buprenorphine dimer compound of claim 1 , wherein the compound is in the form of a pharmaceutically acceptable salt.

3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and a buprenorphine dimer compound of claim 1 .

4. A method of treating or managing gastrointestinal hyperalgesia wherein

the method comprises administering to a patient in need thereof a therapeutically effective amount of a buprenorphine dimer compound of claim 1 .

5. A method of treating IBS-D in a patient in need thereof, said method comprising administering to said patient a therapeutically effective amount of a buprenorphine dimer compound of claim 1 .

6. A method in accordance with claim 5 , wherein the patient is a human and wherein the dose administered is about 0.1 mg/kg of the patient's body weight to about 7.2 mg/kg of the patient's body weight.

7. A method in accordance with claim 5 , wherein the patient is a human and wherein the dose administered is about 10 to about 50 mg daily.

8. A citric acid salt of the compound of claim 1 .

9. A method according to claim 5 , wherein the compound is administered as a citric acid salt.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 11, 2023
From: ORPHOMED, INC.
To: DIMERX, INC.
Reel/Frame 063610/0911 →
SECURITY INTEREST Recorded Jun 11, 2021
From: ORPHOMED, INC.
To: COMERICA BANK
Reel/Frame 056508/0376 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2016
From: ORPHOMED LLC
To: ORPHOMED, INC.
Reel/Frame 037930/0971 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 23, 2015
From: SINGH, NIKHILESH NIHALA
To: ORPHOMED LLC
Reel/Frame 036168/0347 →
Continuity (4)
Provisional Application 61985207 · Apr 28, 2014
Provisional Application 62101768 · Jan 9, 2015
Provisional Application 62176883 · Jan 9, 2015
Related Publication 20150307504A1 · Oct 29, 2015