IP Library Granted Patent US 9,732,096
Granted Patent B2
US 9,732,096 · App. 15/074,960 · Granted Aug 15, 2017

Buprenorphine dimer and its use in treatment of gastrointestinal disorders

Inventor: Nikhilesh Nihala Singh (Mill Valley, CA)
Assignee: ORPHOMED, INC.
C07D519/00A61K31/137A61K31/167A61K31/485C07C217/64C07C217/70C07C217/74C07C233/16C07C233/25C07C233/43C07D489/00C07D489/02C07D489/08C07D489/12C07C2101/14
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Quick Facts
Patent No.
US 9,732,096
App. No.
15/074,960
Granted
Aug 15, 2017
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 (6)

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

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

3. 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 .

4. 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 .

5. A method in accordance with claim 4 , 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.

6. A method in accordance with claim 4 , wherein the patient is a human and wherein the dose administered is about 10 to about 50 mg daily.

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 May 20, 2016
From: SINGH, NIKHILESH NIHALA
To: ORPHOMED LLC
Reel/Frame 038661/0913 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2016
From: ORPHOMED LLC
To: ORPHOMED, INC.
Reel/Frame 038661/0959 →
Continuity (4)
Continuation 14697174 · Apr 27, 2015
Provisional Application 61985207 · Apr 28, 2014
Provisional Application 62101768 · Jan 9, 2015
Related Publication 20160368932A1 · Dec 22, 2016