IP Library Granted Patent US 8,227,627
Granted Patent B2
US 8,227,627 · App. 12/326,036 · Granted Jul 24, 2012

Prodrugs of tetrahydrocannabinol, compositions comprising prodrugs of tetrahydrocannabinol and methods of using the same

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Quick Facts
Patent No.
US 8,227,627
App. No.
12/326,036
Granted
Jul 24, 2012
Kind
B2
Abstract

Described herein are Δ 9 -THC prodrugs, methods of making Δ 9 -THC prodrugs, formulations comprising Δ 9 -THC prodrugs and methods of using Δ 9 -THC. One embodiment described herein relates to the transdermal administration of a Δ 9 -THC prodrug for treating and preventing diseases and/or disorders.

Claims (34)

1. A compound having the formula:

wherein R 1 is an oxygenated ester selected from the group consisting of a pegylated ester, a hydroxylated ester, a branched hydroxylated ester, and an oxalic acid mixed pegylated ester.

2. The compound from claim 1 selected from the group consisting of:

3. A pharmaceutical composition comprising:

(a) a compound as described in claim 1 ; and

(b) a pharmaceutically acceptable excipient.

4. A pharmaceutical composition comprising:

a) a compound selected from the group consisting of:

and

b) a pharmaceutical excipient.

5. A method of treating a medical condition in a mammal comprising the step of administering a compound as described in claim 1 , wherein the medical condition is selected from the group consisting of: anorexia, nausea, emesis, pain, wasting syndrome, HIV-wasting, chemotherapy induced nausea and vomiting, alcohol use disorders, anti-tumor, amyotrophic lateral sclerosis, glioblastoma multiforme, glioma, increased intraocular pressure, glaucoma, cannabis use disorders, Tourette's syndrome, dystonia, multiple sclerosis, inflammatory bowel disorders, arthritis, dermatitis, Rheumatoid arthritis, systemic lupus erythematosus, anti-inflammatory, anti-convulsant, anti-psychotic, anti-oxidant, neuroprotective, anti-cancer, immunomodulatory effects, peripheral neuropathic pain, neuropathic pain associated with post-herpetic neuralgia, diabetic neuropathy, shingles, burns, actinic keratosis, oral cavity sores and ulcers, post-episiotomy pain, psoriasis, pruritis, contact dermatitis, eczema, bullous dermatitis herpetiformis, exfoliative dermatitis, mycosis fungoides, pemphigus, severe erythema multiforme (e.g., Stevens-Johnson syndrome), seborrheic dermatitis, ankylosing spondylitis, psoriatic arthritis, Reiter's syndrome, gout, chondrocalcinosis, joint pain secondary to dysmenorrhea, fibromyalgia, musculoskeletal pain, neuropathic-postoperative complications, polymyositis, acute nonspecific tenosynovitis, bursitis, epicondylitis, post-traumatic osteoarthritis, synovitis, and juvenile rheumatoid arthritis.

6. The method of claim 5 wherein the compound is administered by a route selected from the group consisting of: transdermal, topical, oral, buccal, sublingual, intra venous, intra muscular, vaginal, rectal, ocular, nasal and follicular.

7. A method of treating a medical condition in a mammal comprising the steps of administering a compound selected from the group consisting of:

and

wherein the medical condition is selected from the group consisting of: anorexia, nausea, emesis, pain, wasting syndrome, HIV-wasting, chemotherapy induced nausea and vomiting, alcohol use disorders, anti-tumor, amyotrophic lateral sclerosis, glioblastoma multiforme, glioma, increased intraocular pressure, glaucoma, cannabis use disorders, Tourette's syndrome, dystonia, multiple sclerosis, inflammatory bowel disorders, arthritis, dermatitis, Rheumatoid arthritis, systemic lupus erythematosus, anti-inflammatory, anti-convulsant, anti-psychotic, anti-oxidant, neuroprotective, anti-cancer, immunomodulatory effects, peripheral neuropathic pain, neuropathic pain associated with post-herpetic neuralgia, diabetic neuropathy, shingles, burns, actinic keratosis, oral cavity sores and ulcers, post-episiotomy pain, psoriasis, pruritis, contact dermatitis, eczema, bullous dermatitis herpetiformis, exfoliative dermatitis, mycosis fungoides, pemphigus, severe erythema multiforme (e.g., Stevens-Johnson syndrome), seborrheic dermatitis, ankylosing spondylitis, psoriatic arthritis, Reiter's syndrome, gout, chondrocalcinosis, joint pain secondary to dysmenorrhea, fibromyalgia, musculoskeletal pain, neuropathic-postoperative complications, polymyositis, acute nonspecific tenosynovitis, bursitis, epicondylitis, post-traumatic osteoarthritis, synovitis, and juvenile rheumatoid arthritis.

8. The method of claim 7 wherein the compound is administered by a route selected from the group consisting of: transdermal, topical, oral, buccal, sublingual, intra venous, intra muscular, vaginal, rectal, ocular, nasal and follicular.

9. A method of administering a compound to a mammal comprising the steps of:

(a) combining a compound of claim 1 with a pharmaceutical excipient to form a pharmaceutical composition;

(b) creating a dosage form suitable for administration to a mammal from the pharmaceutical composition; and

(c) administering the dosage form to a mammal.

10. The method of claim 9 wherein the pharmaceutical composition is administered by a route selected from the group consisting of: transdermal, topical, oral, buccal, sublingual, intra venous, intra muscular, vaginal, rectal, ocular, nasal and follicular.

11. A method of administering a compound to a mammal comprising the steps of:

(a) combining the compound selected from the group consisting of:

with a pharmaceutical excipient to form a pharmaceutical composition;

(b) creating a dosage form suitable for administration to a mammal from the pharmaceutical composition; and

(c) administering the dosage form to a mammal.

12. The method of claim 11 wherein the pharmaceutical composition is administered by a route selected from the group consisting of: transdermal, topical, oral, buccal, sublingual, intra venous, intra muscular, vaginal, rectal, ocular, nasal and follicular.

13. The compound of claim 2 , which is

14. The compound of claim 2 , which is

15. The compound of claim 2 , which is

16. The compound of claim 2 , which is

17. The compound of claim 2 , which is

18. The compound of claim 2 , which is

19. The compound of claim 2 , which is

Assignments (5)
SUPPLEMENTAL CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 18, 2026
From: HARMONY BIOSCIENCES MANAGEMENT, INC. (F/K/A ZYNERBA PHARMACEUTICALS, INC.)
To: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
Reel/Frame 075642/0639 →
CHANGE OF NAME Recorded Dec 11, 2014
From: ALLTRANZ INC.
To: ZYNERBA PHARMACEUTICALS, INC.
Reel/Frame 034477/0690 →
RELEASE OF SECURITY INTEREST Recorded Sep 25, 2014
From: KENTUCKY ECONOMIC DEVELOPMENT FINNCE AUTHORITY
To: ZYNERBA PHARMACEUTICALS, INC.
Reel/Frame 033816/0866 →
CONDITIONAL ASSIGNMENT Recorded Jan 13, 2014
From: ALLTRANZ, INC.
To: KENTUCKY ECONOMIC DEVELOPMENT FINANCE AUTHORITY
Reel/Frame 031950/0443 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 7, 2009
From: STINCHCOMB, AUDRA LYNN; GOLINSKI, MIROSLAW JERZY; HAMMELL, DANA CARMEL; HOWARD, JEFFREY LYNN
To: ALLTRANZ INC.
Reel/Frame 022652/0563 →