首页> 外国专利> PHARMACEUTICAL COMPOSITIONS OF ANTICOLINERGIC AND INHIBITORS OF QUINASE P38 IN THE TREATMENT OF RESPIRATORY DISEASES.

PHARMACEUTICAL COMPOSITIONS OF ANTICOLINERGIC AND INHIBITORS OF QUINASE P38 IN THE TREATMENT OF RESPIRATORY DISEASES.

机译:喹诺酮酶P38的抗药性和抑制剂在治疗呼吸系统疾病中的作用。

摘要

Pharmaceutical compositions characterized in that they contain one or more anticholinergics of the formula A (See formula) in which X- means an anion (counterion), preferably an anion chosen from the group consisting of chloride, bromide, iodide, sulfate, phosphate, methanesulfonate , nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate and p-toluenesulfonate; combined with one or more p38 kinase B inhibitors, optionally in the form of enantiomers, mixtures of enantiomers or in the form of racemates thereof, optionally in the form of solvates or hydrates and optionally together with a pharmaceutically acceptable excipient; characterized in that the inhibitors B of the kinase p38 are chosen from the group of the compounds of the formulas 5, 5a, 6 and 7, in which in the compounds of the formula 5 (See formula) Ar1 is chosen from the group consisting of : pyrrole, pyrrolidine, pyrazole, imidazole, oxazole, thiazole, furan and thiophene; said Ar1 may be substituted by one or more R1, R2 or R3; Ar2 is: phenyl, naphthyl, quinoline, isoquinoline, tetrahydronaphthyl, tetrahydroquinoline, tetrahydroisoquinoline, benzimidazole, benzofuran, indanyl, indenyl or indole, each of which is optionally substituted one to three times by R2 groups; X is: a) a C5-8 cycloalkyl or cycloalkenyl optionally substituted by 0-2 branched or unbranched C 1-4 alkyl groups, C 1-4 alkoxy or C 1-4 alkyl amino; b) phenyl, furan, thiophene, pyrrole, imidazolyl, pyridine, pyrimidine, pyridinone, dihydropyridinone, maleimide, dihydromaleimide, piperidine, piperazine or pyrazine, which independently of each other may optionally be substituted by 0-3 C1-C alkyl groups 4 branched or unbranched, C1-4 alkoxy, hydroxy, nitrile, mono- or di- (C1-3 alkyl) amino, C1-6-S (O) alkyl or halogen.
机译:药物组合物,其特征在于它们包含一种或多种式A的抗胆碱能药(参见式),其中X-表示阴离子(抗衡离子),优选选自氯离子,溴离子,碘离子,硫酸根,磷酸根,甲磺酸根的阴离子,硝酸盐,马来酸盐,乙酸盐,柠檬酸盐,富马酸盐,酒石酸盐,草酸盐,琥珀酸盐,苯甲酸盐和对甲苯磺酸盐;与一种或多种p38激酶B抑制剂组合,任选以对映体形式,对映体混合物或其外消旋体形式,任选以溶剂化物或水合物形式以及任选地与药学上可接受的赋形剂一起;其特征在于激酶p38的抑制剂B选自式5、5a,6和7的化合物,其中在式5(参见式)的化合物中,Ar1选自下组: :吡咯,吡咯烷,吡唑,咪唑,恶唑,噻唑,呋喃和噻吩;所述Ar1可以被一个或多个R1,R2或R3取代; Ar 2是:苯基,萘基,喹啉,异喹啉,四氢萘基,四氢喹啉,四氢异喹啉,苯并咪唑,苯并呋喃,茚满基,茚基或吲哚,它们各自任选被R 2基团取代1-3次; X为:a)任选地被0-2个支链或直链的C 1-4烷基,C 1-4烷氧基或C 1-4烷基氨基取代的C 5-8环烷基或环烯基; b)苯基,呋喃,噻吩,吡咯,咪唑基,吡啶,嘧啶,吡啶酮,二氢吡啶酮,马来酰亚胺,二氢马来酰亚胺,哌啶,哌嗪或吡嗪,它们彼此独立地可以任选地被0-3个C 1 -C 4烷基取代或直链的,C 1-4烷氧基,羟基,腈,单或二(C 1-3烷基)氨基,C 1-6-S(O)烷基或卤素。

著录项

  • 公开/公告号ES2278170T3

    专利类型

  • 公开/公告日2007-08-01

    原文格式PDF

  • 申请/专利权人 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG;

    申请/专利号ES20030738089T

  • 申请日2003-06-26

  • 分类号A61K31/46;C07D231/40;A61K9/12;A61K31/416;A61K31/4178;A61K31/435;A61K31/4418;A61K31/4745;A61K31/517;A61K31/5377;A61K45;A61K47/10;A61K47/26;A61K47/36;A61M15;A61P11;A61P11/02;A61P27/16;A61P37/08;A61P43;C07D401/14;C07D451/06;

  • 国家 ES

  • 入库时间 2022-08-21 20:54:27

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