# US 2022/0033360 A1 · Ophthalmic compositions and methods for the treatment of skin diseases and eye diseases

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- Number: US 2022/0033360 A1
- Document ID: US20220033360A1
- Status: Published application
- Kind: A1
- Application number: 17/309,434
- Filed: 2019-11-23
- Published: 2022-02-03
- Earliest claimed: 2018-11-26
- Assignees: Cellix Bio Private Limited
- Applicants: Cellix Bio Private Limited
- Inventors: Mahesh Kandula
- Web page: https://patentgrep.com/patent/US20220033360A1

## CPC

- C07D 233/22: Radicals substituted by oxygen atoms
- C07C 53/126: Acids containing more than four carbon atoms
- C07D 213/55: Acids; Esters
- C07D 213/56: Amides
- C07D 339/04: having the hetero atoms in positions 1 and 2, e.g. lipoic acid
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III and formula IV and the methods for the treatment of eye disorders and skin diseases and may be formulated for the topical eye drop, topical paste, ocular solution, device-drug delivery, oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of skin diseases and eye diseases.

## Claims

### Claim 1

A compound of Formula I:
and pharmaceutically acceptable hydrates, solvates, enantiomers, and stereoisomers thereof;
wherein,
RH independently represents
caprylic acid, 1-hydroxy-2-naphthoic acid, 2,2-dichloroacetic acid, 2-hydroxyethanesulfonic acid, 2-oxoglutaric acid, 4-acetamidobenzoic acid, 4-aminosalicylic acid, acetic acid, adipic acid, ascorbic acid, aspartic acid, benzenesulfonic acid, benzoic acid, camphoric acid, camphor-10-sulfonic acid, capric acid (decanoic acid), caproic acid (hexanoic acid), carbonic acid, cinnamic acid, citric acid, cyclamic acid, dodecylsulfuric acid, ethane-1,2-disulfonic acid, ethanesulfonic acid, formic acid, fumaric acid, galactaric acid, gentisic acid, glucoheptonic acid, gluconic acid, glucuronic acid, glutamic acid, glutaric acid, glycerophosphoric acid, glycolic acid, hippuric acid, hydrobromic acid, isobutyric acid, lactic acid, lactobionic acid, lauric acid, maleic acid, malic acid, malonic acid, mandelic acid, methanesulfonic acid, naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, nicotinic acid, nitric acid, oleic acid, oxalic acid, palmitic acid, pamoic acid, phosphoric acid, proprionic acid, pyroglutamic acid, salicylic acid, sebacic acid, stearic acid, succinic acid, sulfuric acid, tartaric acid, thiocyanic acid, toluenesulfonic acid, undecylenic acid, omega 3 fatty acids, alpha linoleic acid, alpha linolenic acid, omega 6 fatty acids, n-acetyl cysteine (nac), furoate, methyl furoate, ethyl furoate, aminocaproic acid, caprilic acid, alpha lipoic acid, R-lipoic acid, myristic acid, myristoleic acid, palmitoleic acid, phospholipids, phosphatidylcholine, elaidic acid, linoleic acid, linolenic acid, menthol, retinoic acid, vitamin A, retinol, linolelaidic acid, arachidonic acid, retinal, isotretinoin, curcumin, tretinoin, α-carotene β-carotene, d2 ergosterol, ergocalciferol, 7-dehydrocholesterol, cholecalciferol, 25-hydroxycholecalciferol, calcitriol (1,25-dihydroxycholecalciferol), calcitroic acid, d4 dihydroergocalciferol, alfacalcidol, dihydrotachysterol, calcipotriol, tacalcitol, paricalcitol, tocopherol, naphthoquinone, phylloquinone (k1), menaquinones (k2), menadione (k3), menadiol (k4), thiamine, acefurtiamine, allithiamine, benfotiamine, fursultiamine, octotiamine, prosultiamine, sulbutiamine, riboflavin, niacin, nicotinamide, pantothenic acid, dexpanthenol, pantethine, pyridoxine, pyridoxal phosphate, pyridoxamine, pyritinol, biotin, folic acid, dihydrofolic acid, folinic acid, levomefolic acid, adenosylcobalamin, cyanocobalamin, hydroxocobalamin, methylcobalamin, choline, dehydroascorbic acid or 1-docosanol.

### Claim at position 2

-4. (canceled)

### Claim 5 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein said pharmaceutical composition is formulated for topical eye drop, topical paste, ocular solution, device-drug delivery, oral admiration, buccal admiration, rectal admiration, topical admiration, transdermal admiration, transmucosal admiration, lozenge, spray, intravenous admiration, oral solution, nasal spray, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection.

### Claim 7 (depends on 6)

The pharmaceutical compositions of claim 6, wherein said pharmaceutical compositions are formulated for the treatment of eye disorders and skin diseases.

### Claim at position 6

-16. (canceled)

### Claim 17 (depends on 1)

A compound of claim 1, wherein said compound is selected from the group consisting of

### Claim 18 (depends on 17)

A pharmaceutical composition comprising a compound of claim 17 and a pharmaceutically acceptable carrier.

### Claim 19 (depends on 18)

The pharmaceutical composition of claim 18, wherein said pharmaceutical composition is formulated for topical eye drop, topical paste, ocular solution, device-drug delivery, oral admiration, buccal admiration, rectal admiration, topical admiration, transdermal admiration, transmucosal admiration, lozenge, spray, intravenous admiration, oral solution, nasal spray, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection.

### Claim 20 (depends on 19)

The pharmaceutical compositions of claim 19, wherein said pharmaceutical compositions are formulated for the treatment of eye disorders and skin diseases.