首页> 外国专利> PROFARMACOS 9,11-CYCLOENDOPEROXIDE OF PROSTAGLANDIN ANALOGS FOR THE TREATMENT OF OCULAR HYPERTENSION AND GALUCOMA.

PROFARMACOS 9,11-CYCLOENDOPEROXIDE OF PROSTAGLANDIN ANALOGS FOR THE TREATMENT OF OCULAR HYPERTENSION AND GALUCOMA.

机译:前列腺素类似物的PROFARMACOS 9,11-环戊内酯治疗眼压过高和加仑肉瘤。

摘要

Use of a compound for the manufacture of a medicament for therapeutic application in order to decrease the intraocular pressure in the eye of a mammal, compound having the formula (See formula) in which the dotted lines represent the presence of a bond or the absence of a link, the wavy lines represent the alpha or beta configuration, the black triangles represent the beta configuration and the shaded lines represent the alpha configuration; n is an integer that has values from 1 to 6; m is an integer that has values from 1 to 8; X is NH2, N (R) 2, NHR or OR, where R is hydrogen, R4 or a group - (CO) R4; Y is = O, = S or OH, OR5 or -O (CO) R5 groups, said OH, OR5 or O (CO) R5 groups being attached to the adjacent carbon atom in the alpha or beta configuration; R1 is H, CH3, R7, OR7 or SR7, in which R7 is an aliphatic, aromatic or heteroaromatic ring, heteroaromatic ring having 1 to 3 heteroatoms selected from O, S and N, aliphatic, aromatic or heteroaromatic ring that optionally is substituted with 1 to 3 R8 groups, in which R8 is F, Cl, Br, I, NO2, C1-6 alkyl, 1-6 alkyl substituted with fluorine, COOH, or COOR9 in which R9 is alkyl of 1 at 6 carbon atoms or CH2OCH3; R2 and R3 together represent = O, = S or, independently, are hydrogen or alkyl of 1 to 6 carbon atoms; R4 represents (CH2) rOH, (CH2) rOCOR9 or (CH2) rOR9, where r is an integer that has values from 1 to 6, or R4 represents saturated or unsaturated acyclic hydrocarbons having 1 to 20 carbon atoms , or - (CH2) q R6, in which q is 0-10 and and R6 is an aliphatic, aromatic or heteroaromatic ring, heteroaromatic ring having 1 to 3 heteroatoms selected from O, S and N, aliphatic, aromatic ring or heteroaromatic which is optionally substituted with 1 to 3 R8 groups, where R8 F, Cl, Br, I, NO2, C1-6 alkyl, C1-6 alkyl substituted with fluorine, COOH, COOR9 where R9 is alkyl of 1 to 6 atoms of carbon or CH2OCH3; R5 represents saturated or unsaturated acyclic hydrocarbons having 1 to 20 carbon atoms, or - (CH2) q R6, or a pharmaceutically acceptable salt of said compound.
机译:化合物在制备用于降低哺乳动物的眼内眼压的治疗性用途的药物中的用途,该化合物具有下式(见式)的化合物,其中虚线表示存在键或不存在键链接,波浪线表示alpha或beta配置,黑色三角形表示beta配置,阴影线表示alpha配置; n是一个整数,取值范围是1到6; m是一个整数,取值范围是1到8; X为NH 2,N(R)2,NHR或OR,其中R为氢,R 4或-(CO)R 4基团; Y为= O,= S或OH,OR 5或-O(CO)R 5基团,所述OH,OR 5或O(CO)R 5基团以α或β构型连接至相邻的碳原子; R 1是H,CH 3,R 7,OR 7或SR 7,其中R 7是脂族,芳族或杂芳族环,具有1-3个选自O,S和N的杂原子的杂芳族环,脂族,芳族或杂芳族环,其任选地被取代。 1-3个R8基团,其中R8是F,Cl,Br,I,NO2,C1-6烷基,被氟取代的1-6烷基,COOH或COOR9,其中R9是在6个碳原子上为1的烷基或CH2OCH3 ; R 2和R 3一起表示= O,= S,或独立地是氢或1-6个碳原子的烷基; R4代表(CH2)rOH,(CH2)rOCOR9或(CH2)rOR9,其中r是具有1至6的值的整数,或者R4代表具有1至20个碳原子的饱和或不饱和无环烃,或者-(CH2) q R6,其中q为0-10,并且R6为脂族,芳族或杂芳族环,具有1-3个选自O,S和N的杂原子的杂芳族环,脂族,芳族环或杂芳族,其任选地被1至1个取代3个R 8基团,其中R 8 F,Cl,Br,I,NO 2,C 1-6烷基,被氟取代的C 1-6烷基,COOH,COOR 9,其中R 9为碳或CH 2 OCH 3的1-6个原子的烷基; R5代表具有1至20个碳原子的饱和或不饱和无环烃,或-(CH2)qR6,或所述化合物的药学上可接受的盐。

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