IP Library Patent Application 15333654
Patent Application
App. No. 15/333,654

Compositions and Methods Relating to Ionic Salts of Peptides

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Quick Facts
Patent No.
US None
App. No.
15/333,654
Abstract

The present invention relates to compounds of Formula I, compositions containing same, and methods of use.

Claims (32)

1 .- 32 . (canceled)

33 . A compound of Formula I, or an enantiomer, polymorph, solvate, or hydrate thereof, which is a salt of an amino acid moiety and one or two fatty acids, A and B:

wherein

A and B are the same or different, and each of A and B is independently selected from the group consisting of linoleic acid, gamma-linolenic acid (GLA), eicosadienoic acid, dihomo-gamma-linolenic acid (DGLA), arachidonic acid (AA), docosadienoic acid, adrenic acid, docosapentaenoic acid (Osbond acid), tetracosatetraenoic acid, and tetracosapentaenoic acid, 24:5 (n-6).

either A or B, but not both, may be absent,

X 1 and X 2 are each independently selected from (CH 2 ) 3 —R 1 , and (CH 2 ) 4 —R 2 , where R 1 and R 2 are each a basic function which may be the same or different, the basic function being selected from the group consisting of a primary amine, a secondary amine, a tertiary amine, and a guanidine, and

X 3 is H.

34 . The compound of claim 33 , wherein X 1 and X 2 are both (CH 2 ) 4 —R 2 and R 2 is NH 3 +.

35 . The compound of claim 33 , wherein X 1 and X 2 are both (CH 2 ) 3 —R 1 and R 1 is NHC(NH 2 +)NH 2 .

36 . The compound of claim 33 , wherein X 1 is (CH 2 ) 3 —R 1 , R 1 is NHC(NH 2 +)NH 2 , X 2 is (CH 2 ) 4 —R 2 and R 2 is NH 3 +.

37 . The compound of claim 33 , wherein X 1 is (CH 2 ) 4 —R 2 , R 2 is NH 3 +, X 2 is (CH 2 ) 3 —R 1 , and R 1 is NHC(NH 2 +)NH 2 .

38 . A pharmaceutical composition comprising the compound of claim 33 , and a carrier.

39 . The pharmaceutical composition of claim 38 , wherein the composition is a solid oral dosage form.

40 . The pharmaceutical composition of claim 38 , wherein the composition is an intravenous dosage form.

41 . The pharmaceutical composition of claim 38 , wherein the composition is an ophthalmic formulation.

42 . The pharmaceutical composition of claim 38 , wherein the composition is a parenteral dosage form.

43 . A package or kit comprising a unit dosage form of the pharmaceutical composition of claim 38 , at least one container for holding the unit dosage forms, and instructions for use.

44 . The compound of claim 34 , wherein A or B is absent and the remainder is arachidonic acid (AA).

45 . The compound of claim 34 , wherein A and B are both present and are each is arachidonic acid (AA).

46 . The compound of claim 35 , wherein A or B is absent and the remainder is arachidonic acid (AA).

47 . The compound of claim 35 , wherein A and B are both present and are each is arachidonic acid (AA).

48 . The compound of claim 36 , wherein A or B is absent and the remainder is arachidonic acid (AA).

49 . The compound of claim 36 , wherein A and B are both present and are each is arachidonic acid (AA).

50 . The compound of claim 37 , wherein A or B is absent and the remainder is arachidonic acid (AA).

51 . The compound of claim 37 , wherein A and B are both present and are each is arachidonic acid (AA).

52 . A composition comprising a compound of claim 33 .

53 . The composition of claim 52 , wherein the composition is a dietary supplement or nutraceutical additive.

54 . A method for treating a metabolic disease or disorder in a human subject, the method comprising administering to the subject a pharmaceutical composition comprising the compound of claim 33 , wherein the metabolic disease or disorder is selected from the group consisting of hypertriglyceridemia, severe hypertriglyceridemia, hypercholesterolemia, pre-diabetes, fatty liver disease, and obesity.

55 . A method for treating a cardiovascular disease or disorder in a subject, the method comprising administering to the subject a pharmaceutical composition comprising the compound of claim 33 , wherein the cardiovascular disease or disorder is selected from the group consisting of atrial fibrillation, myocardial infarction, and congestive heart failure.

56 . A method for treating an inflammatory disease or disorder in a subject, the method comprising administering to the subject a pharmaceutical composition comprising the compound of claim 33 , wherein the inflammatory disease or disorder is selected from the group consisting of arthritis, irritable bowel syndrome, ophthalmic inflammation disorders, and dry eye syndrome.

57 . A method for treating a gastrointestinal disorder or complication thereof in a subject, the method comprising administering to the subject a pharmaceutical composition comprising the compound of claim 33 , wherein the gastrointestinal disorder or complication thereof is selected from the group consisting of bowel obstruction, short bowel syndrome, Gastroschisis, prolonged diarrhea, high-output fistula, Crohn's disease, ulcerative colitis, colon cancer, familial adenomatous polyposis, parenteral nutrition-associated liver disease, essential fatty acid deficiency, a congenital gastrointestinal anomaly, and necrotizing enterocolitis.

58 . A method for treating a neurological disorder in a subject, the method comprising administering to the subject a pharmaceutical composition comprising the compound of claim 33 , wherein the neurological disorder is selected from the group consisting of Alzheimer's disease, attention deficit hyperactivity disorder (ADHD), depression, traumatic brain injury, spinal cord injury, ischemic stroke, and concussion.

Assignments (1)
SECURITY AGREEMENT Recorded Aug 17, 2018
From: THETIS PHARMACEUTICALS LLC
To: CONNECTICUT INNOVATIONS, INC., AS COLLATERAL AGENT
Reel/Frame 046850/0287 →