KR900701270A - Treatment of glaucoma and related disorders in human eyes with pyridinylmethyl (sulfinyl or thio) benzimidazole - Google Patents

Abstract

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Description

Treatment of glaucoma and related disorders in human eyes with pyridinylmethyl (sulfinyl or thio) benzimidazole

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Claims (11)

Pressure in the eye of a patient in which the therapeutically effective amount of a compound of formula I and pharmaceutically acceptable salts thereof, in particular alkaline salts such as sodium and potassium salts, is optionally administered in admixture with a pharmaceutically acceptable carrier How to reduce. In the above formula, X is -S- or -SO-, and R ¹ , R ² , R ³ , and R ⁴ are the same or different, and (a) H, (b) 1-8, in particular 1-6 Alkyl groups containing carbon atoms, (c) alkoxy groups containing 1-8, in particular 1-6 carbon atoms, (d) alkoxyalkyl groups containing 1-3 carbon atoms in each alkyl moiety, (e) Alkoxyalkoxy groups containing 1-3 carbon atoms in each alkyl moiety, (f) a halogen atom, (g) -CN, (h) -CF ₃ , (i) -NO ₂ , (j)- COR ¹⁰ , (k) alkylthio groups containing 1-6 carbon atoms in the alkyl moiety, (1) alkylsulfinyl groups containing 1-7 carbon atoms in the alkyl moiety, (m) aryl-thio, -sul Finyl, -sulfonyl, sulfonyloxy oxysulfonyl, -sulfonamido or -aminosulfonyl groups, wherein each aryl group is the same or different and is selected from halogen, CF ³ and (1-5C) alkoxy groups -Substituted by 3 substituents; (n) 1-6 carbon atoms each in the alkyl and alkoxy moieties. An arylalkyl or arylalkoxy group-containing [wherein, the aryl portion by a search which are identical or different, halogen, CF ³ (1-5C) alkyl and (1-5C) 1-3 substituents selected from alkoxy groups optionally substituted) , (o) aryl or aryloxy groups, wherein each aryl group is the same or different, with 1-3 substituents selected from halogen atoms, CF ₃ and (1-5C) alkyl and (1-5C) alkoxy groups Optionally substituted], (P) a haloalkoxy group containing 1-6 carbon atoms and 1-11, in particular 1-6 halogen atoms, or (q) a hydroxyalkyl group containing 1-6 carbon atoms, , (r) R 'and R ₂ , R ₂ and R ³ or R ⁴ together with adjacent carbon atoms in the benzimidazole ring are at least one 5-, 6- or 7-membered ring wherein these rings are saturated or May be unsaturated and may contain 0-3 heteroatoms selected from N, S and 0, each ring 1-10 selected from alkyl groups having 1-3 carbon atoms and halogen, suitably optionally substituted with 1-6 or 1-4 substituents, or 1 with 2 or 4 of these substituents Or forms two oxo groups (C = 0) and when R ¹ and R ² , R ² and R ³ or R ³ and R ⁴ form two rings together with adjacent carbon atoms in the benzimidazole ring, this ring May be condensed with each other. R ⁶ is (a) H, (b) an alkyl group containing 1-8, in particular 1-6, carbon atoms, (c) an alkoxy group containing 1-8, especially 1-6 carbon atoms, or (d) A halogen atom, R ⁸ is (a) H, (b) an alkyl group having 1-8, in particular 1-6 carbon atoms, (c) an alkoxy group containing especially 1-6 carbon atoms, (d) a halogen atom or (e) an arylalkyl group containing 1-4 carbon atoms in the alkyl moiety, R ⁷ is an alkyl group containing ((a) H ₂ , (b) 1-7 carbon atoms, (c) 1-7 Alkoxy groups containing carbon atoms, (d) alkoxyalkyl groups containing 1-3 carbon atoms in each alkyl portion, (e) alkoxyalkoxy groups containing 1-3 carbon atoms in each alkyl portion, (f Aryloxy group, wherein the aryl group is the same or different and is optionally substituted with one or two substituents selected from halogen CF ³ , (1-3C) alkyl and (1-3C) alkoxy), (g) Arylalkyl containing 1-7 carbon atoms in the alkyl, alkoxy moiety Is aryl alkoxy group [wherein, the aryl part being optionally substituted by the same or different and represents halogen, CF ^3, (1-3C) alkyl and (1-3C) 1 or 2 substituents selected from alkoxy groups), (h) alkenyl Alkenyloxy group containing 1-7 carbon atoms in the nile moiety, (i) Alkynyloxy group containing 1-7 carbon atoms in the alkenyl moiety, (j) 1-7 alkyl groups, preferably 1- An alkylthio group containing three carbon atoms, (k) 1-3 in the alkyl moiety, preferably an arylthio or arylalkylthio group containing one carbon atom, (l) 1-7 in the altyl moiety, Preferably, a dialkylamino group containing 1-3 carbon atoms, (m) morpholino group, (n) piperidino group, (0) N-methylpiperazino group, (p) pyrrolidine group or (q) Is a fluoroalkoxy group containing 2-5 carbon atoms and 1-9 fluorine atoms or R ⁶ and R ⁷ , or R ⁷ and R ⁸ together with adjacent carbon atoms in the pyridine ring Or form a six-membered, saturated or unsaturated ring, which rings may optionally contain oxygen, sulfur or alkylated nitrogen atoms. R ¹⁰ is (a) an alkyl group containing 1-6 carbon atoms, (b) an alkoxy group containing 1-6 carbon atoms or (c) an aryl group. A method of reducing eye input in an eye of a patient by administering to said eye a therapeutically effective amount of a compound of formula I as defined in claim 1, optionally with a pharmaceutically acceptable carrier. The method of claim 1, wherein X is —S—. The method of claim 2, wherein X is —S—. The method of claim 1, wherein X is —SO—. The method of claim 2 wherein X is —SO—. The method of claim 1, wherein the method is administered 2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl) -methyl) -sulfinyl) -5-methoxy-1H-benzimidazole How to be. The method of claim 2, wherein X is —SO—. A method of reducing eye input in an eye of a patient, wherein the therapeutically effective amount of a compound of formula I as defined in claim 1 is micro-injected into the eye, optionally with a pharmaceutically acceptable carrier. A compound of formula I as defined in claim 1 for use in the manufacture of a medicament for the treatment of glaucoma. A pharmaceutical composition for the treatment of diseases associated with increased intraocular pressure in the eye, consisting of the compound of formula I as defined in claim 1 as an active ingredient. ※ Note: The disclosure is based on the initial application.