首页> 外国专利> USE OF PDGF RECEPTOR THYROSINE KINASE INHIBITORS IN THE TREATMENT OF DIABETIC NEFROPATIA.

USE OF PDGF RECEPTOR THYROSINE KINASE INHIBITORS IN THE TREATMENT OF DIABETIC NEFROPATIA.

机译:PDGF受体酪氨酸激酶抑制剂在糖尿病性肾病治疗中的应用。

摘要

Use of a PDGF receptor tyrosine kinase inhibitor of formula I, wherein R1 is 4-pyrazinyl; 1-methyl-1H-pyrrolyl; amino- or amino-C1-7-substituted phenyl, wherein the amino group in each case is free, alkylated or acylated; 1 H-indolyl or 1H-imidazolyl attached to a five-membered ring of carbon atoms; or unsubstituted or substituted C1-7-pyridyl alkyl attached to a ring of a carbon atom and unsubstituted or substituted on the nitrogen atom by an oxygen; R2 and R3 are each independently of the other hydrogen or C1-7 alkyl; one or two of the radicals R4, R5, R6, R7 and R8 are each nitro, fluoro-substituted C1-7 alkoxy or a radical of the formula II -N (R9) -C (= X) - (Y) nR10 (II), wherein R9 is hydrogen or C1-7 alkyl, X is oxo, thio, imino, N-C1-7-imino alkyl, hydroximino or O-C1-7-hydroxyino alkyl, Y is oxygen or the NH group , n is 0 or 1 and R10 is an aliphatic radical having at least 5 carbon atoms, or an aromatic, aromatic-aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or heterocyclic-aliphatic radical, and the remaining radicals R4, R5, R6, R7 and R8 are each independently of the other hydrogen, C1-7 alkyl which is unsubstituted or substituted by a free or alkylated amino, piperazinyl, piperidinyl, pyrrolidinyl or by a morpholinyl, or C1-7 alkanoyl, trifluoromethyl, hydroxy free, etherified or esterified, free amino, alkylated or acylated or free or esterified carboxy, or a salt of said compounds having at least one salt forming group, for the preparation ation of a medication for the treatment of diabetic nephropathy.
机译:式I的PDGF受体酪氨酸激酶抑制剂的用途,其中R 1为4-吡嗪基; 1-甲基-1H-吡咯基;氨基-或氨基-C1-7-取代的苯基,其中氨基分别是游离的,烷基化的或酰化的; 1个H-吲哚基或1H-咪唑基连接到碳原子的五元环上;连接在碳原子环上的未取代或取代的C 1-7-吡啶基烷基,在氮原子上未被氧取代或取代。 R2和R3各自独立于另一个氢或C1-7烷基; R4,R5,R6,R7和R8中的一个或两个分别为硝基,氟取代的C1-7烷氧基或式II -N(R9)-C(= X)-(Y)nR10( II),其中R9是氢或C1-7烷基,X是氧代,硫代,亚氨基,N-C1-7-亚氨基烷基,氢氧氨基或O-C1-7-羟基代烷基,Y是氧或NH基,n R 10为0或1,并且R 10为具有至少5个碳原子的脂族基团,或为芳族,芳族脂族,脂环族,脂环族脂族,杂环或杂环脂族基团,且其余基团R4,R5,R6,R7和R8各自独立于其他氢,未被取代或被游离或烷基化的氨基,哌嗪基,哌啶基,吡咯烷基或吗啉基或C1-7烷酰基,三氟甲基,无羟基,醚化或酯化的未取代或取代的C1-7烷基,用于制备药物的游离氨基,烷基化或酰化或游离或酯化的羧基,或具有至少一个成盐基团的所述化合物的盐r糖尿病肾病的治疗。

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