Use of steroid compounds in the preparation of a medicament for preventing and / or treating floaters

Abstract

The application of steroid compounds in the preparation of a drug for preventing and / or treating floaters, said steroid compounds have excellent effects of treating, alleviating and preventing floaters, and can greatly reduce and / or cure floaters and improve visual clarity.

Description

[Technical Field]

[0001] The present invention belongs to the technical field of chemical medicine, and relates to the application of steroid compounds in preparing drugs for preventing and / or treating floaters. [Background technology]

[0002] Floaters are generally caused by degeneration of the vitreous body and are a natural aging phenomenon. As the vitreous body "liquefies" with age, some opacities occur. Therefore, the official name for floaters is "vitreous opacity" or "vitreous floaters." They are called floaters because they appear as black dots floating in front of the eye, resembling mosquitoes. Floaters are caused by opaque objects in the vitreous body projected onto the retina. They are more noticeable in bright light or against a white background, and sensitive eyes can even make out their various shapes. In many cases, floaters persist for a long time, remain constant throughout the year, do not affect vision, and examinations reveal no ocular organ damage, so no treatment is necessary and no effective treatment is available.

[0003] Some elderly people may suddenly notice one or two black spots appearing before their eyes without any other symptoms. This is usually due to the detachment of the posterior limiting membrane of the vitreous, and generally poses no significant risk. However, if a large number of black spots suddenly appear, this may indicate rupture of retinal blood vessels or the formation of a retinal tear, which may be a sign of retinal detachment. A more detailed fundus examination is warranted. During choroiditis, many inflammatory cells or exudates can enter the vitreous, which is a common cause of pathological floaters, but they are difficult to detect due to the accompanying visual impairment. Floaters experienced by myopic patients are always associated with liquefied degeneration of the vitreous.

[0004] Floaters are a special and very common eye disease. Although a small number of floaters pose a serious threat to the eyeball, most floaters are benign or are called "physiological floaters" and generally do not require treatment, but still have a serious impact on the mental and physical health of patients. Although some over-the-counter drugs can alleviate symptoms, they have significant side effects. Currently, there are no drugs with a reliable therapeutic effect for this disease. Therefore, a drug for treating floaters with high clinical efficacy and minimal side effects is currently a problem to be solved. Summary of the Invention [Problem to be solved by the invention]

[0005] In view of the shortcomings of the prior art, the object of the present invention is to provide an application of steroid compounds in the preparation of drugs for preventing and / or treating floaters, and the steroid compounds provided by the present invention have excellent effects on treating, alleviating and preventing floaters, and can significantly reduce and / or cure floaters and improve visual clarity. [Means for solving the problem]

[0006] To achieve this goal, the present invention adopts the following technical solutions.

[0007] In a first aspect, the present invention provides the use of a steroid compound having a structure according to Formula I, or which is a stereoisomer, tautomer, oxynitride, solvate, metabolite, pharmaceutically acceptable salt, or prodrug of a compound of Formula I, in the preparation of a medicament for preventing and / or treating floaters. [ka] wherein X is selected from an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, a heteroalkyl group, and a substituted or unsubstituted alkyl group, and the substituent is a hydroxy group, a mercapto group, an amino group, an aryl group, a heteroaryl group, a carboxyl group, R 1 R 2NC(=O)- or R 1 R 2 NC(=NH)-NR 3 -Selected from. R according to the present invention 1 R 2 NC(=O)- or R 1 R 2 NC(=NH)-NR 3 -R included 1 , R 2 are two groups both linked to N. The n Qs are each independently selected from -H, -D, halogen, a hydroxy group, an amino group, a cyano group, a nitro group, a carboxy group, an alkylcarbonyl group, an alkyl group, a halogenated alkyl group, a cycloalkyl group, a heterocyclic group, an aryl group, and a heteroaryl group. An alkylcarbonyl group according to the present invention means RC(=O)-, where R is an alkyl group and it is the carbonyl carbon that is connected to X. n is 0, 1, 2 or 3. R 1 , R 2 and R 3 are each independently selected from -H, -D, or an alkyl group.

[0008] In a preferred technical solution of the present invention, the X is C 6-10 Aryl group, C 2-9 Heteroaryl groups, C 3-8 Cycloalkyl groups, C 2-10 Heterocycloalkyl groups, C 1-6 Heteroalkyl groups, substituted or unsubstituted C 1-6 alkyl groups, 1-6 When the alkyl group has a substituent, the substituent is a hydroxy group, a mercapto group, an amino group, a C 6-10 Aryl group, C 2-9 Heteroaryl group, carboxy group, R 1 R 2 NC(=O)- or R 1 R 2 NC(=NH)-NR 3 -Selected from. R 1 , R2 and R 3 are each independently -H, -D or C 1-6 It is selected from alkyl groups.

[0009] Said C 6-10 may be C6, C7, C8, C9, or C10. 2-9 may be C3, C4, C5, C6, C7, or C8. 3-8 may be C4, C5, C6, or C7. 2-10 may be C3, C4, C5, C6, C7, C8, or C9. 1-6 may be C2, C3, C4, or C5.

[0010] In a preferred technical solution of the present invention, said X is a methyl group, an ethyl group, a propyl group, an isopropyl group, an n-butyl group, an isobutyl group, a tert-butyl group, a hydroxymethyl group, a hydroxyethyl group, a mercaptomethyl group, a mercaptoethyl group, an aminomethyl group, an aminoethyl group, an aminopropyl group, a phenylmethyl group, a phenylethyl group, an imidazolylmethyl group, a carboxymethyl group, a carboxyethyl group, a methylthiomethyl group, a methylthioethyl group, a phenyl group, a naphthyl group, a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohex ... aryl group, tetrahydrofuryl group, dihydrofuryl group, tetrahydrothienyl group, dihydrothienyl group, 1,3-dioxolanyl group, dithiolanyl group, tetrahydropyranyl group, dihydropyranyl group, 2H-pyranyl group, 4H-pyranyl group, tetrahydrothiopyranyl group, piperidinyl group, morpholinyl group, thiomorpholinyl group, piperazinyl group, dioxanyl group, dithianyl group, thioxanyl group, homopiperazinyl group, homopiperidinyl group, oxepanyl group, thiepanyl group, oxaza group, diaza group, thioaza group, indolinyl group, 1,2,3,4- Tetrahydroquinolinyl group, 1,2,3,4-tetrahydroisoquinolinyl group, furanyl group, imidazolyl group, 3-isoxazolyl group, isoxazolyl group, oxazolyl group, pyrrolyl group, pyridyl group, pyrimidyl group, pyridazyl group, thiazolyl group, tetrazolyl group, triazolyl group, 2-thienyl group, 3-thienyl group, pyrazolyl group, isothiazolyl group, 1,2,3-oxadiazolyl group, 1,2,5-oxadiazolyl group, 1,2,4-oxadiazolyl group, 1,2,3-triazolyl group, 1,2,3-thiodiazolyl group, 1,3,4-thio a diazolyl group, a 1,2,5-thiodiazolyl group, a pyrazinyl group, a 1,3,5-triazinyl group, a benzimidazolyl group, a benzofuranyl group, a benzothienyl group, an indolyl group, a purinyl group, a quinolyl group, an isoquinolyl group, an imidazo[1,2-a]pyridyl group, a pyrazolo[1,5-a]pyridyl group, a pyrazolo[1,5-a]pyrimidyl group, an imidazo[1,2-b]pyridazyl group, a [1,2,4]triazolo[4,3-b]pyridazyl group, a [1,2,4]triazolo[1,5-a]pyrimidyl group, a [1,2,4]triazolo[1,5-a]pyridyl group, [ka] , [ka] , [ka] , [ka] , C having HNC(=O)- substituent 1-3 C with alkyl group or HNC(=NH)-NH- substituent 1-3 It is selected from alkyl groups.

[0011] In a preferred technical solution of the present invention, n Qs are each independently -H, -D, halogen, a hydroxyl group, an amino group, a cyano group, a nitro group, a carboxyl group, C 1-6 Alkylcarbonyl group, C 1-6 Alkyl group, C 1-6 Halogenated alkyl groups, C 3-8 Cycloalkyl groups, C 2-9 Heterocyclic group, C 6-10 Aryl group or C 2-9 Heteroaryl groups are selected from the group consisting of:

[0012] Said C 1-6 may be C2, C3, C4, or C5. 3-8 may be C4, C5, C6, or C7. 2-9 may be C3, C4, C5, C6, C7, or C8. 6-10 may be C6, C7, C8, C9, or C10.

[0013] In a preferred technical solution of the present invention, n Qs each independently represent -H, -D, -F, -Cl, -Br, a hydroxyl group, an amino group, a cyano group, a carboxyl group, a formyl group, an acetyl group, a methyl group, an ethyl group, a propyl group, an isopropyl group, an n-butyl group, an isobutyl group, a tert-butyl group, a trifluoromethyl group, a difluoromethyl group, a phenyl group, a naphthyl group, a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group, a tetrahydrofuryl group, a dihydrofuryl group, a tetrahydrothienyl group, a dihydrofuryl group, a di ... Thienyl group, 1,3-dioxolanyl group, dithiolanyl group, tetrahydropyranyl group, dihydropyranyl group, 2H-pyranyl group, 4H-pyranyl group, tetrahydrothiopyranyl group, piperidinyl group, morpholinyl group, thiomorpholinyl group, piperazinyl group, dioxanyl group, dithianyl group, thioxanyl group, homopiperazinyl group, homopiperidinyl group, oxepanyl group, thiepanyl group, oxaza group, diaza group, thioaza group, indolinyl group, 1,2,3,4-tetrahydroquinolinyl group, 1,2,3,4-tetrahydroisoquinolinyl group, Isoquinolinyl group, furanyl group, imidazolyl group, 3-isoxazolyl group, isoxazolyl group, oxazolyl group, pyrrolyl group, pyridyl group, pyrimidyl group, pyridazyl group, thiazolyl group, tetrazolyl group, triazolyl group, 2-thienyl group, 3-thienyl group, pyrazolyl group, isothiazolyl group, 1,2,3-oxadiazolyl group, 1,2,5-oxadiazolyl group, 1,2,4-oxadiazolyl group, 1,2,3-triazolyl group, 1,2,3-thiodiazolyl group, 1,3,4-thiodiazolyl group, 1,2,5-thiodiazolyl group and a quinolyl group, a pyrazinyl group, a 1,3,5-triazinyl group, a benzimidazolyl group, a benzofuranyl group, a benzothienyl group, an indolyl group, a purinyl group, a quinolyl group, an isoquinolyl group, an imidazo[1,2-a]pyridyl group, a pyrazolo[1,5-a]pyridyl group, a pyrazolo[1,5-a]pyrimidyl group, an imidazo[1,2-b]pyridazyl group, a [1,2,4]triazolo[4,3-b]pyridazyl group, a [1,2,4]triazolo[1,5-a]pyrimidyl group, or a [1,2,4]triazolo[1,5-a]pyridyl group.

[0014] In a specific embodiment of the present invention, the compound having the structure represented by formula I is any one selected from the following compounds: [ka] [ka] [ka] [ka] [ka]

[0015] The steroid compounds provided by the present invention can be used therapeutically as raw chemicals or can be provided as the active ingredient in pharmaceutical compositions.

[0016] In a second aspect, the present invention provides the use of a composition comprising a steroid compound according to the first aspect and one or more pharmaceutically acceptable carriers, excipients, diluents, adjuvants or vehicles in the preparation of a medicament for the prevention and / or treatment of floaters.

[0017] Substances that can be used as pharmaceutically acceptable carriers include, but are not limited to, ion exchangers; aluminum; aluminum stearate; lecithin; serum proteins, such as human serum proteins; buffer substances, such as phosphates; glycine; sorbic acid; potassium sorbate; partial glyceride mixtures of saturated vegetable fatty acids; water; salts; electrolytes, such as protamine sulfate; disodium hydrogen phosphate; potassium hydrogen phosphate; sodium chloride; zinc salts; colloidal silicon; magnesium trisilicate; polyvinylpyrrolidone; polyacrylic esters; waxes; polyethylene-polyoxypropylene-block polymers; lanolin; sugars, such as lactose, glucose, and sucrose; starches, such as corn starch and potato starch; cellulose and its derivatives, such as carboxylates. sodium dimethylcellulose, ethylcellulose and cellulose acetate; gum powder; malt; gelatin; talc powder; auxiliary materials such as cocoa butter and suppository waxes; oils such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil and soybean oil; glycols such as propylene glycol and polyethylene glycol; esters such as ethyl oleate and ethyl laurate; agar; buffers such as magnesium hydroxide and aluminum hydroxide; alginic acid; pyrogen-free water; isotonic salts; Ringer's solution; ethanol, phosphate buffer solution, and other non-toxic suitable lubricants such as sodium lauryl sulfate and magnesium stearate, colorants, release agents, coating agents, sweeteners, flavorings and fragrances, preservatives and antioxidants.

[0018] Compared with the prior art, the present invention has the following beneficial effects: The present inventors have found that the steroid compounds provided by the present invention are useful in preventing, treating, curing or alleviating floaters in a patient with minimal to no side effects. DETAILED DESCRIPTION OF THE INVENTION

[0019] The technical solution of the present invention will be further described below through specific embodiments, which should be understood by those skilled in the art that the specific embodiments are merely for understanding the present invention and should not be regarded as specific limitations on the present invention.

[0020] Unless otherwise explained, all scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.

[0021] "Stereoisomers" as used herein refer to compounds that have the same chemical structure but differ in the way the atoms or groups are arranged in space. Stereoisomers include enantiomers, diastereomers, conformational isomers (rotational isomers), geometric isomers (cis / trans) isomers, atropisomers, etc.

[0022] Depending on the selection of starting materials and processes, the compounds of the present invention can exist in the form of one of the possible isomers or a mixture thereof, for example, a racemate or a mixture of diastereomers (depending on the number of asymmetric carbon atoms). Optically active (R)- or (S)-isomers can be prepared using chiral synthesizers or chiral agents or can be resolved using conventional techniques. When the compounds contain one double bond, the substituents can be in the E- or Z-configuration, and when the compounds contain a disubstituted cycloalkyl group, the substituents on the cycloalkyl group can be in the cis- or trans-configuration.

[0023] Any resulting mixture of stereoisomers can be separated into pure or nearly pure geometric isomers, enantiomers, diastereomers, depending on the differences in the physicochemical properties of the components, for example, by chromatography and / or step crystallization methods.

[0024] Unless otherwise indicated, the structural formulae depicted in the present invention include all isomers, e.g., enantiomers, diastereomers, and geometric (or conformational) isomers, e.g., R, S configuration of asymmetric centers, (Z), (E) isomers containing double bonds, and (Z), (E) conformational isomers, and therefore, any single stereochemical isomer of a compound of the present invention or a mixture of its enantiomers, diastereomers, or geometric (or conformational) isomers is within the scope of the present invention.

[0025] The term "prodrug" as used herein refers to a compound that is converted in the body to a compound of Formula I. Such conversion may be mediated by hydrolysis of the prodrug in the blood or enzymatic conversion to the parent structure in the blood or tissue. The prodrug compounds of the present invention may be esters, and in prior art, esters have been used as prodrugs, including phenyl esters, aliphatic esters (C 1-24) esters, acyloxymethyl esters, carbonate esters, carbamates, and amino acid esters. For example, one compound of the present invention contains a hydroxyl group, which can be acylated to obtain a prodrug form of the compound. Other prodrug forms include phosphate esters, for example, these phosphate ester compounds can be obtained by phosphorylating the hydroxy group on the parent molecule. For a complete discussion of prodrugs, see the following references: T. Higuchi and V. Stella, Pro-drugs as Novel Delivery Systems, Vol. 14 of the ACS Symposium Series, Edward B. Roche, ed., Bioreversible Carriers in Drug Design, American Pharmaceutical Association and Pergamon Press, 1987, J. Rautio et al, Prodrugs:Design and Clinical Applications, Nature Review Drug Discovery, 2008, 7, 255-270, and SJ Hecker et al, Prodrugs of Phosphates and Phosphonates, Journal of Medicinal Chemistry, 2008, 51,2328-2345.

[0026] The racemates of the final products or intermediates obtained in known manner can be separated into their optical antipodes by methods well known to those skilled in the art, for example by isolating the diastereomeric salts obtained. Racemic products can also be isolated by chiral chromatography, for example by high performance liquid chromatography (HPLC) using a chiral adsorbent. In particular, enantiomers can be prepared by asymmetric synthesis, see, for example, the following documents: Jacques, et al., Enantiomers, Racemates and Resolutions (Wiley Interscience, New York, 1981); Principles of Asymmetric Synthesis (2nd Ed. Robert E. Gawley, Jeffrey Aube, Elsevier, Oxford, UK, 2012); Eliel, EL Stereochemistry of Carbon Compounds (McGraw-Hill, NY, 1962); Wilen, SH Tables of Resolving Agents and Optical Resolutions p. 268 (EL Eliel, Ed., Univ. of Notre Dame Press, Notre Dame, IN 1972); Chiral Separation Techniques: A Practical Approach (Subramanian, G. Ed., Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, Germany, 2007).

[0027] The term "tautomer" or "tautomeric form" refers to structural isomers that have different energies and are interconvertible via a low energy barrier. When tautomerism is possible (e.g., in solution), a chemical equilibrium of tautomers can be achieved. For example, proton tautomers (also called prototropic tautomers) include interconversions that occur via proton transfer, such as keto-enol isomerization and imine-enamine isomerization. Valence tautomers include interconversions that occur via recombination of some bond electrons. A specific example of keto-enol tautomerism is the interconversion of pentane-2,4-dione and 4-hydroxypent-3-en-2-one tautomers. Another example of tautomerism is phenol-keto tautomerism. One specific example of phenol-keto tautomerism includes the interconversion of pyridin-4-ol and pyridin-4(1H)-one tautomers. Unless otherwise stated, all tautomeric forms of the compounds of the invention are within the scope of the invention.

[0028] The salts according to the present invention are pharmaceutically acceptable salts, and "pharmaceutically acceptable salts" are well known to those skilled in the art, as described in the literature: Berge et al., describe pharmaceutically acceptable salts in detail in J. Pharmacol Sci, 1997, 66, 1-19. Non-limiting examples of pharmaceutically acceptable salts include inorganic acid salts formed by reaction with an amino group, such as hydrochloride, hydrobromide, phosphate, metaphosphate, sulfate, sulfite, nitrate, and perchlorate, and organic acid salts, such as carboxylates, sulfonates, sulfinates, and thiocarboxylates. Specific examples include, but are not limited to, methanesulfonate, ethanesulfonate, formate, acetate, butanedioate, benzoate, succinate, dihydroxynaphthoate, salicylate, and the like. Examples of suitable salts include cilate, galactarate, glucoheptonate, mandelate, 1,2-ethanedisulfonate, 2-naphthalenesulfonate, carbonate, trifluoroacetate, hydroxyacetate, isethionate, oxalate, maleate, tartrate, citrate, succinate, malonate, benzenesulfonate, p-toluenesulfonate, malate, fumarate, lactate, lactose or oxalate, or salts thereof can be obtained by other methods described in the literature, such as ion exchange methods. Other pharmaceutically acceptable salts include adipate, alginate, ascorbate, aspartate, benzenesulfonate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, cyclopentylpropionate, digluconate, dodecyl sulfate, ethanesulfonate, glucoheptonate, glycerophosphate, gluconate, hemisulfate, heptanoate, hexanoate, hydroiodide, 2-hydroxyethanesulfonate, lactobionate, laurate, lauryl sulfate, nicotinate, nitrate, oleate, palmitate, pamoate, pectinate, persulfate, 3-phenylpropionate, picrate, pivalate, propionate, stearate, thiocyanate, undecanoate, pentanoate, etc. Pharmaceutically acceptable salts also include alkali metal, alkaline earth metal, ammonium, and N+ (C 1-4 Also included are salts obtained with appropriate bases, such as salts of alkyl (4). The present invention also contemplates quaternary ammonium salts formed with any compound having an N-containing group. Water- or oil-soluble or dispersible products can be obtained by quaternization. Alkali metal or alkaline earth metal salts include sodium, lithium, potassium, calcium, magnesium, and the like. Pharmaceutically acceptable salts include suitable, non-toxic ammonium, quaternary ammonium salts and amine cations formed from anti-equilibrium ions, e.g., halides, carboxylates, sulfates, phosphates, nitrates, C. 1-8 Further included are sulfonates and aromatic sulfonates.

[0029] Pharmaceutically acceptable salts can be formed with inorganic and organic acids, e.g., acetate, aspartate, benzoate, benzenesulfonate, bromide / hydrobromide, bicarbonate / carbonate, hydrogensulfate / sulfate, camphorsulfonate, chloride / hydrochloride, chlorotheophylline, citrate, ethanedisulfonate, fumarate, glucoheptonate, gluconate, glucuronate, hippurate, hydroiodide / iodide, isethionate, lactate, lactobionate. , lauryl sulfate, malate, maleate, malonate, mandelate, methanesulfonate, methylsulfate, naphthoate, naphthalenesulfonate, nicotinate, nitrate, octadecanoate, oleate, oxalate, palmitate, pamoate, phosphate / hydrogenphosphate / dihydrogenphosphate, polygalacturonate, propionate, stearate, succinate, sulfosalicylate, tartrate, toluenesulfonate and trifluoroacetate.

[0030] Inorganic acids from which salts can be derived include, for example, hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like.

[0031] Organic acids from which salts can be derived include, for example, acetic acid, propionic acid, hydroxyacetic acid, oxalic acid, maleic acid, malonic acid, succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, p-toluenesulfonic acid, sulfosalicylic acid, and the like.

[0032] The term "solvate" as used herein refers to an association formed between one or more solvent molecules and the compound of the present invention. Solvents that form solvates include, but are not limited to, water, isopropanol, ethanol, methanol, dimethyl sulfoxide, ethyl acetate, acetic acid, and aminoethanol. The term "hydrate" refers to an association formed between solvent molecules and water.

[0033] "Pharmaceutical composition" refers to a mixture of one or more compounds described herein, salts, or physiologically / pharmaceutically acceptable salts or prodrugs thereof, with other chemical components, such as physiologically / pharmaceutically acceptable carriers or excipients. The purpose of a pharmaceutical composition is to facilitate administration of a compound to an organism.

[0034] The term "treating" any disease or condition, as used herein, in some embodiments, refers to ameliorating the disease or condition (i.e., alleviating or inhibiting or reducing the progression of the disease or at least one clinical symptom thereof). In some other embodiments, "treatment" refers to alleviating or improving at least one physical parameter, including physical parameters that may not be perceptible to the patient. In some other embodiments, "treatment" refers to modulating the disease or condition physically (e.g., stable perceptible symptoms), physiologically (e.g., stable physical parameters), or both. In some other embodiments, "treatment" refers to preventing or delaying the onset, development, or worsening of the disease or condition.

[0035] The term "alkyl group" as used herein refers to a saturated, linear or branched monovalent hydrocarbon group of 1 to 20 carbon atoms, or 1 to 10 carbon atoms, or 1 to 8 carbon atoms, or 1 to 6 carbon atoms, or 1 to 4 carbon atoms, or 1 to 3 carbon atoms, where the alkyl group may be independently and optionally substituted with one or more substituents as described herein. Examples of alkyl groups include, but are not limited to, methyl (Me, -CH), ethyl (Et, -CHCH), n-propyl (n-Pr, -CHCHCH), isopropyl (i-Pr, -CH(CH)), n-butyl (n-Bu, -CHCHCHCH), isobutyl (i-Bu, -CHCH(CH)), sec-butyl (s-Bu, -CH(CH)CHCH), te, butyl (e-Bu, -CH(CH)CHCH), ... rt-butyl group (t-Bu, -C(CH3)3), n-pentyl group (-CH2CH2CH2CH2CH3), 2-pentyl group (-CH(CH3)CH2CH2CH3), 3-pentyl group (-CH(CH2CH3)2), 2-methyl-2-butyl group (-C(CH3)2CH2CH3), 3-methyl-2-butyl group (-CH(CH3)CH(CH3)2), 3-methyl-1-butyl group (-CH2CH2CH(CH3)2), 2-methyl 1-butyl-2-methyl group (-CH2CH(CH3)CH2CH3), n-hexyl group (-CH2CH2CH2CH2CH2CH2CH3), 2-hexyl group (-CH(CH3)CH2CH2CH2CH2CH3), 3-hexyl group (-CH(CH2CH3)(CH2CH2CH3)), 2-methyl-2-pentyl group (-C(CH3)2CH2CH2CH3), 3-methyl-2-pentyl group (-CH(CH3)CH(CH3)CH2CH3), 4 and the like. Examples of alkyl groups include 2-methyl-2-pentyl (-CH(CH3)CH2CH(CH3)2), 3-methyl-3-pentyl (-C(CH3)(CH2CH3)2), 2-methyl-3-pentyl (-CH(CH2CH3)CH(CH3)2), 2,3-dimethyl-2-butyl (-C(CH3)2CH(CH3)2), 3,3-dimethyl-2-butyl (-CH(CH3)C(CH3)3), n-heptyl, and n-octyl. The term "alkyl group" and its prefix "alkyl," as used herein, are inclusive of both straight and branched saturated carbon chains.The term "alkylene," as used herein, refers to a saturated divalent hydrocarbon group obtained by removing two hydrogen atoms from a straight- or branched-chain saturated hydrocarbon; examples of such groups include, but are not limited to, methylene, ethylidene, isopropylidene, and the like.

[0036] The term "cycloalkyl group" refers to a monovalent or polyvalent, non-aromatic, saturated or partially unsaturated ring, containing no heteroatoms, including monocyclic rings of 3 to 12 carbon atoms or bicyclic rings of 7 to 12 carbon atoms. Bicyclic carbocycles having 7 to 12 atoms may be bicyclic [4,5], [5,5], [5,6], or [6,6] systems, while bicyclic carbocycles having 9 or 10 atoms may be bicyclic [5,6] or [6,6] systems. Suitable cycloaliphatic groups include, but are not limited to, cycloalkyl groups, cycloalkenyl groups, and cycloalkynyl groups. Examples of cycloaliphatic groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopent-1-en-1-yl, cyclopent-2-en-1-yl, cyclopent-3-en-1-yl, cyclohexyl, cyclohex-1-en-1-yl, cyclohex-2-en-1-yl, cyclohex-3-en-1-yl, cyclohexadienyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, and the like. Furthermore, the "alicyclic group", "carbocycle", "carbocyclic group", and "cycloalkyl group" may be substituted or unsubstituted, and the substituents therein may be, but are not limited to, a hydroxy group, an amino group, a halogen atom, a cyano group, an aryl group, a heteroaryl group, an alkoxy group, an alkylamino group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a heterocyclic group, a mercapto group, a nitro group, an aryloxy group, a hydroxy-substituted alkoxy group, a hydroxy-substituted alkyl-C(=O), alkyl-C(=O), alkyl-S(=O), alkyl-S(=O)2-, a hydroxy-substituted alkyl-S(=O), a hydroxy-substituted alkyl-S(=O)2, a carboxyalkoxy group, etc.

[0037] The terms "heterocycle," "heterocyclic group," "heteroalicyclic," or "heterocyclic" are used interchangeably herein and refer to a monocyclic, bicyclic, or tricyclic ring system in which one or more carbon atoms on the ring may be independently optionally replaced with a heteroatom, said heteroatom having the meaning described herein, the ring may be fully saturated or may contain one or more degrees of unsaturation, but is never aromatic, and only one point of attachment is connected to other molecules. One or more hydrogen atoms on the ring may be independently optionally replaced with one or more substituents described herein. In some embodiments, a "heterocycle," "heterocyclic group," "heteroalicyclic," or "heterocyclic" group is a 3-7 membered monocyclic ring (1-6 carbon atoms and 1-3 heteroatoms selected from N, O, P, S, where S or P are optionally replaced with one or more oxygen atoms, e.g., to give groups such as SO, SO, PO, PO; if the ring is three membered, only one heteroatom), or a 7-10 membered bicyclic ring (4-9 carbon atoms and 1-3 heteroatoms selected from N, O, P, S, where S or P are optionally replaced with one or more oxygen atoms, e.g., to give groups such as SO, SO, PO, PO).

[0038] A heterocyclic group may be a carbon atom group or a heteroatom group. The term "heterocyclic group" similarly includes groups formed by combining a heterocyclic group with a saturated or partially unsaturated ring or heterocycle.Examples of heterocycles include, but are not limited to, pyrrolidinyl, tetrahydrofuryl, dihydrofuryl, tetrahydrothienyl, tetrahydropyranyl, dihydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, thiomorpholinyl, thioxanyl, thiazolidinyl, oxazolidinyl, piperazinyl, homopiperazinyl, azetidinyl, oxetanyl, thietanyl, piperidinyl, homopiperidinyl, glycidyl, azacycloheptyl, oxocycloheptyl, Thiocycloheptyl group, 4-methoxy-piperidinyl-1-yl group, 1,2,3,6-tetrahydropyridin-1-yl group, oxazepinyl group, diazazepinyl group, thioazazepinyl group, pyrrolin-1-yl group, 2-pyrrolinyl group, 3-pyrrolinyl group, dihydroindolyl group, 2H-pyranyl group, 4H-pyranyl group, dioxanyl group, 1,3-dioxolanyl group, pyrazolinyl group, dithianyl group, dithiolanyl group, dihydrothienyl group, pyrazolidinyl group, imidazolinyl group, imidazolidinyl group, 1,2,3,4-tetrahydroindolyl group quinolyl group, 1,2,6-thiadiazin-1,1-dioxo-2-yl group, 4-hydroxy-1,4-azaphospholan-4-oxid-1-yl group, 2-hydroxy-1-(piperazin-1-yl)ethanon-4-yl group, 2-hydroxy-1-(5,6-dihydro-1,2,4-triazin-1(4H)-yl)ethanon-4-yl group, 5,6-dihydro-4H-1,2,4-oxadiazin-4-yl group, 2-hydroxy-1-(5,6-dihydropyridin-1(2H)-yl)ethanon-4-yl group, 3-azabicyclo [3.1.0]hexyl, 3-azabicyclo[4.1.0]heptyl, azabicyclo[2.2.2]hexyl, 2-methyl-5,6,7,8-tetrahydro-[1,2,4]triazole[1,5-c]pyrimidin-6-yl, 4,5,6,7-tetrahydroisoxazole[4,3-c]pyridin-5-yl, 3H-indolyl 2-oxo-5-azabicyclo[2.2.1]heptan-5-yl, 2-oxo-5-azabicyclo[2.2.2]octan-5-yl, quinolidinyl, and N-pyridyl urea.Examples of heterocyclic groups further include a 1,1-dioxothiomorpholyl group and a pyrimidinedione group in which two carbon atoms on the ring are replaced with oxygen atoms. The heterocyclic group may be substituted or unsubstituted, and the substituents may be, but are not limited to, oxo (=O), a hydroxy group, an amino group, a halogen atom, a cyano group, a heteroaryl group, an alkoxy group, an alkylamino group, an alkyl group, an alkenyl group, an alkynyl group, a heterocyclic group, a mercapto group, a nitro group, an aryloxy group, a hydroxy-substituted alkoxy group, a hydroxy-substituted alkyl-C(=O), an alkyl-C(=O), an alkyl-S(=O), an alkyl-S(=O)2-, a hydroxy-substituted alkyl-S(=O), a hydroxy-substituted alkyl-S(=O)2, a carboxyalkoxy group, and the like.

[0039] The term "aryl group," whether used alone or as part of an "aralkyl group," "aralkyloxy group," or "aryloxyalkyl group," refers to mono-, bi-, and tri-carbocyclic ring systems with a total of 6 to 14 ring members, provided that at least one ring system is aromatic, each ring system contains 3 to 7 ring members, and only one point of attachment is connected to the remainder of the molecule. The term "aryl" can be used interchangeably with the term "aromatic ring," and for example, aromatic rings can include phenyl, naphthyl, and anthryl. The aryl group may be substituted or unsubstituted, and the substituent may be, but is not limited to, a hydroxy group, an amino group, a halogen atom, a cyano group, an aryl group, a heteroaryl group, an alkoxy group, an alkylamino group, an alkyl group, an alkenyl group, an alkynyl group, a heterocyclic group, a mercapto group, a nitro group, an aryloxy group, a hydroxy-substituted alkoxy group, a hydroxy-substituted alkyl-C(=O), an alkyl-C(=O), an alkyl-S(=O), an alkyl-S(=O)2-, a hydroxy-substituted alkyl-S(=O), a hydroxy-substituted alkyl-S(=O)2, or a carboxyalkoxy group.

[0040] The term "heteroaryl group" refers to monocyclic, bicyclic, and tricyclic ring systems containing a total of 5-14 ring members, provided that at least one ring system is aromatic and at least one ring system contains one or more heteroatoms, which heteroatoms have the meaning described herein, and wherein each ring system contains 3 to 7 ring members and has only one point of attachment connected to the remainder of the molecule. The term "heteroaryl group" can be used interchangeably with the terms "aromatic heterocycle" or "heteroaromatic compound." The heteroaryl group may be substituted or unsubstituted, and the substituent may be, but is not limited to, a hydroxy group, an amino group, a halogen atom, a cyano group, an aryl group, a heteroaryl group, an alkoxy group, an alkylamino group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a heterocyclic group, a mercapto group, a nitro group, an aryloxy group, a hydroxy-substituted alkoxy group, a hydroxy-substituted alkyl-C(=O)-, an alkyl-C(=O)-, an alkyl-S(=O)-, an alkyl-S(=O)2-, a hydroxy-substituted alkyl-S(=O)-, a hydroxy-substituted alkyl-S(=O)2-, or a carboxyalkoxy group.

[0041] In some other embodiments, heteroaryl groups include, but are not limited to, 2-furyl, 3-furyl, N-imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 4-methylisoxazol-5-yl, N-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl group, 2-pyridyl group, 3-pyridyl group, 4-pyridyl group, 2-pyrimidinyl group, 4-pyrimidinyl group, pyrimidin-5-yl group, pyridazinyl group (e.g., 3-pyridazinyl group), 2-thiazolyl group, 4-thiazolyl group, 5-thiazolyl group, tetrazolyl group (e.g., 5-tetrazolyl group), triazolyl group (e.g., 2-triazolyl group and 5-triazolyl group), 2-thienyl group, 3-thienyl group, pyrazolyl group (e.g., 2-pyrazolyl group, etc.), isothiazolyl group, 1,2,3-oxadiazolyl group, 1,2,5-oxadiazolyl group, 1,2,4-oxadiazolyl group, 1,2,3-triazolyl group, 1,2,3-thiodiazolyl group, 1,3,4-thiodiazolyl group, 1,2,5-thiodiazolyl group, 1,3,4-thiadiazol-2-yl group, pyrazinyl group, pyrazin-2-yl group, and 1,3,5-triazinyl group, Bicyclic rings include, but are not limited to, benzimidazolyl, benzofuranyl, benzothienyl, indolyl (e.g., 2-indolyl), purinyl, quinolyl (e.g., 2-quinolyl, 3-quinolyl, 4-quinolyl), and isoquinolyl (e.g., 1-isoquinolyl, 3-isoquinolyl, or 4-isoquinolyl), benzo[d]thiazol-2-yl, and imidazo[1,5-a]pyridin-6-yl.

[0042] The term "heteroatom" refers to one or more O, S, N, P, and Si atoms, including N, S, and P in any oxidation state, in the form of primary, secondary, and tertiary amines and quaternary ammonium salts, or in the form of a hydrogen atom substituted on a nitrogen atom in a heterocycle, such as N (e.g., N in a 3,4-dihydro-2H-pyrrolyl group), NH (e.g., NH in a pyrrolidinyl group), or NR (e.g., NR in an N-substituted pyrrolidinyl group).

[0043] The term "heteroalkyl group" refers to an alkyl chain optionally containing one or more heteroatoms, with the alkyl group and heteroatoms having the meanings described herein. Unless otherwise specified, heteroalkyl groups contain 1-10 carbon atoms; in other embodiments, heteroalkyl groups contain 1-8 carbon atoms; in other embodiments, heteroalkyl groups contain 1-6 carbon atoms; in other embodiments, heteroalkyl groups contain 1-4 carbon atoms; and in other embodiments, heteroalkyl groups contain 1-3 carbon atoms. Examples include, but are not limited to, CHOCH-, CHCHOCH-, CHSCH-, CHSCHCH-, (CH)NCH-, (CH)CHOCH-, CHOCHCH-, CHCHOCHCH-, and the like.

[0044] The term "halogen" means F, Cl, Br or I.

[0045] The term "halogenated" as used herein refers to the substitution of the subsequent group with halogen, and the number of substitutions may be one or more.

[0046] The term "hydroxy-substituted" as used herein means that the subsequent group is substituted with a hydroxy group, and the number of substitutions may be one or more.

[0047] When "substituted" is used between two groups as described herein, the group before it is a substituent group. For example, an "aryl-substituted alkyl group" means that the alkyl group has an aryl substituent, and an "alkoxycarbonyl-substituted alkyl group" means that the alkyl group has an alkoxycarbonyl substituent.

[0048] When a plurality of groups of the present invention are used in combination, the substitution relationship is from left to right, for example, an "arylalkyl group" represents an aryl-substituted alkyl group, and an "alkoxyalkoxy group" represents an alkoxy-substituted alkoxy group.

[0049] Example 1 The present invention provides an eye drop solution comprising the following components: [Table 0]

[0050] The preparation method is as follows. The above ingredients were mixed under aseptic conditions and stirred overnight at 2 to 8°C to obtain a homogeneous mixture, which was then stored in an eye dropper bottle.

[0051] Example 2 This example provides a method of using the eye drops provided by Example 1. The eye drops provided by Example 1 were used every day, 1-2 drops were used 4 times a day.

[0052] Efficacy test Ten patients with floaters were selected to evaluate the clinical efficacy. From the date of definitive diagnosis, the patients used the eye drops provided in Example 1 four times a day, using 1-2 drops each time, and were re-examined on the 15th and 30th days. The therapeutic effects are shown in Table 1 below.

[0053] [Table 1-1] [Table 1-2]

[0054] As can be seen from Table 1, in terms of clinical effects, after about 15 days of administration, the black dots or bands in front of the eyes were obviously shallower, contrast sensitivity was improved, and visual obstructions when observing white backgrounds such as ceilings and walls were reduced; after about 30 days of administration, floaters were basically cured, the floating black dots or bands almost disappeared, there was no visual obstruction when observing white backgrounds such as ceilings and walls, visual qualities such as contrast sensitivity were obviously improved, and there were no other side effects.

[0055] Although the present invention has been described in detail above using general descriptions, specific embodiments and tests, some modifications or improvements can be made based on the present invention, which are obvious to those skilled in the art. Therefore, any modifications or improvements made within the scope of the present invention fall within the scope of protection of the present invention.

Claims

1. A composition for preventing and / or treating floaters, comprising a steroid compound, The steroid compound has a structure represented by Formula I. 【Chemistry 1】 (Wherein, X is C ６ aryl groups, Q is a hydroxy group; n is 1.

2. The composition of claim 1, further comprising one or more of a pharmaceutically acceptable carrier, excipient, diluent, adjuvant or vehicle.

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