223645-67-8

Usage

Uses

Used in Ophthalmology:
K115 free base is used as a therapeutic agent for the treatment of glaucoma and ocular hypertension when other treatments are not effective or cannot be administered. It helps in managing intraocular pressure and improving the patient's condition.
Used in Diabetic Retinopathy Clinical Trials:
K115 free base is used as a potential treatment for diabetic retinopathy, as it has shown to promote corneal endothelial cell proliferation, endothelium regeneration, and wound healing. This application is still under investigation and may offer new treatment options for patients suffering from this condition.

Upstream product

• 1011466-10-6 (S)-2-amino-N-(tert-butoxycarbonyl)-N-(3-tert-butyldimethylsilanyloxypropyl)propylamine 
• 194032-33-2 4-fluoro-5-isoquinolinesulfonyl chloride 
• 1360538-91-5 (S)-1-benzyl 4-tert-butyl 2-methyl-1,4-diazepane-1,4-dicarboxylate 
• 1360538-89-1 (S)-2-methyl-1-[(2-nitrophenyl)sulfonyl]-1,4-diazepane 
• 1360538-87-9 (S)-N-{1-[(3-hydroxypropyl)amino]propan-2-yl}-2-nitrobenzenesulfonamide 
• 1360538-86-8 (S)-tert-butyl 4-[(4-fluoroisoquinoline-5-yl)sulfonyl]-3-methyl-1,4-diazepane-1-carboxylate 
• 906820-08-4 4-fluoroisoquinoline-5-sulfonyl chloride hydrochloride 
• 194032-32-1 tert-butyl (S)-3-methyl-1,4-diazepane-1-carboxylate 
• 949109-36-8 tert-butyl (S)-3-methyl-4-[(2-nitrophenyl)sulfonyl]-1,4-diazepane-1-carboxylate 
• 949109-35-7 (S)-tert-butyl 3-hydroxypropyl(2-(2-nitrophenylsulfonylamide)propyl)carbamate 
• 1360538-90-4 (S)-6-benzyloxycarbonylamino-4-(tert-butoxycarbonyl)-4-azaheptyl methanesulfonate 
• 913625-37-3 (S)-6-benzyloxycarbonylamino-4-(tert-butoxycarbonyl)-4-azaheptan-1-ol 
• 223644-14-2 (S)-4-fluoro-N-[1-(3-hydroxypropylamino)propan-2-yl]isoquinoline-5-sulfonamide 
• 223644-02-8 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride 

Downstream Products

• 223644-02-8 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride 

Relevant academic research and scientific papers

Preparation method of 1,4-dioazo-cycloheptane derivative

The invention discloses a preparation method of a 1,4-dioazo-cycloheptane derivative. The preparation method comprises the steps of carrying out multiple coupling on a compound of a formula (VI) and a compound of a formula (V) at -5-0 DEG C in aromatic hydrocarbon or a halogenated hydrocarbon solvent in the presence of alkali, after the coupling, removing hydroxyl protection from the compound of the formula (VI) by virtue of TBAF, carrying out self-cyclization by virtue of a Mitsunobu reaction to obtain a compound of a formula (II), and removing amino protection from the compound of the formula (II) by virtue of a hydrochloric acid ethyl acetate solution, so as to obtain the target compound 1,4-dioazo-cycloheptane derivative. The preparation method has the advantages that synthetic steps are few, the reaction condition of each step is mild, and the operation is simple convenient, so that the production cost is lowered; and more importantly, the yield of the 1,4-dioazo-cycloheptane derivative synthesized by the method is high.

THERAPEUTIC AGENT FOR OCULAR FUNDUS DISEASE

Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (S)-(?)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient.

NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF

The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

AGENT FOR PREVENTION OR TREATMENT OF GLAUCOMA

There is provided an agent for prevention of glaucoma or an agent for prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. An agent for prevention or treatment of glaucoma comprising a Rho kinase inhibitor and a carbonic anhydrase inhibitor in combination.

(S)-(-)-1-(4-FLUOROISOQUINOLIN-5-YL)SULFONYL-2-METHYL-1,4-HOMOPIPERAZINE HYDROCHLORIDE DIHYDRATE

(S)-(-)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate; a process for producing the dihydrate; and a medicinal composition containing the dihydrate. This compound has lower hygroscopicity than anhydrous crystals of (S)-(-)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride and is superior in chemical stability. It is hence useful as a medicine.