Compositions and methods for the treatment of moderate to severe pain

Patent metadata

Field	Value
Publication number	US-9321775-B2
Application number	US-201314399183-A
Country	US
Kind code	B2
Filing date	Feb 4, 2013
Priority date	May 10, 2012
Publication date	Apr 26, 2016
Grant date	Apr 26, 2016

Abstract

The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.

First claim

The invention claimed is:

1. A compound of Formula I:

or a pharmaceutically acceptable salt, hydrate, polymorph, solvate, prodrug, enantiomer, or stereoisomer thereof, wherein:
R 1 represents H, D,

R 2 represents null,

a is 2, 3 or 7;
each b is independently 3, 5 or 6;
e is 1, 2 or 6; and
c and d are each independently H, D, —OH, —OD, C 1 -C 6 -alkyl, —NH 2 or —COCH 3 .

2. A compound of Formula II:

or a pharmaceutically acceptable salt, hydrate, polymorph, solvate, prodrug, enantiomer, or stereoisomer thereof, wherein:
R1 represents

R 2 represents

a is 2, 3 or 7;
each b is independently 3, 5 or 6;
e is 1, 2 or 6; and
c and d are each independently H, D, —OH, —OD, C 1 -C 6 -alkyl, —NH 2 or —COCH 3 .

3. A pharmaceutical composition comprising a compound of claim 1 or 2 , and a pharmaceutically acceptable carrier.

4. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition is formulated to treat moderate to severe pain with an effective amount of said pharmaceutical composition by oral administration, delayed release or sustained release, transmucosal administration, syrup, topical administration, parenteral administration, injection, subdermal administration, oral solution, rectal administration, buccal administration or transdermal administration.

5. A method for treating moderate to severe pain, the method comprising administering to a patient in need thereof an effective amount of pharmaceutical composition of claim 3 .

6. The method of claim 5 , wherein moderate to severe pain is selected from pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, and bipolar disorder.

7. The pharmaceutical composition of claim 3 , further comprising a molecular conjugate of bioactive compounds selected from a group consisting of ketorolac and ketoprofen, carboxylic acid compounds selected from a group consisting of R-Lipoic acid, eicosapentaenoic acid, docosahexaenoic acid, acetyl cysteine, salsalate and fumaric acid.

8. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is R-Lipoic acid.

9. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is eicosapentaenoic acid.

10. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is docosahexaenoic acid.

11. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is acetyl cysteine.

12. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is salsalate.

13. The pharmaceutical composition of claim 7 , wherein the carboxylic acid compound is fumaric acid.

14. The pharmaceutical composition of claim 7 , wherein the bioactive compound is ketorolac.

15. The pharmaceutical composition of claim 7 , wherein the bioactive compound is ketoprofen.

Assignees

• Kandula Mahesh
• Cellix Bio Private Ltd

Inventors

• Kandula Mahesh

Classifications

• A61K31/194

  having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid · CPC title

• C07D333/24

  Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals · CPC title

• C07C59/76

  containing keto groups · CPC title

• A61K31/407

  condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title