KC-11404(KC-11404) - 药物靶点：5-LOX x PAF receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

5-LOX x PAF receptor

作用机制

5-LOX抑制剂(5-脂氧合酶抑制剂)、PAF receptor拮抗剂(血小板活化因子受体拮抗剂)

治疗领域

免疫系统疾病呼吸系统疾病

在研适应症-

非在研适应症

哮喘

原研机构

Horizon Immobilien GmbH

在研机构-

非在研机构

Horizon Immobilien GmbH

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C28H38N4O

InChIKeyGLTHSRFPHHLMIW-UHFFFAOYSA-N

CAS号148490-22-6

关联

100 项与 KC-11404 相关的临床结果

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100 项与 KC-11404 相关的转化医学

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100 项与 KC-11404 相关的专利（医药）

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1

项与 KC-11404 相关的文献（医药）

1995-02-01·Journal of Medicinal Chemistry1区 · 医学

Synthesis, Structure-Activity Relationships, and Pharmacological Evaluation of Pyrrolo[3,2,1-ij]quinoline Derivatives: Potent Histamine and Platelet Activating Factor Antagonism and 5-Lipoxygenase Inhibitory Properties. Potential Therapeutic Application in Asthma

1区 · 医学

Article

作者: Lenoir, Patrick ; Peck, Michael J. ; Jasserand, Daniel ; Cottin, Michel ; Augert, Guy ; Dupassieux, Pierre ; Demonchaux, Patrice ; Paris, Dominique

A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized and evaluated for their in vitro and in vivo activities against histamine, platelet activating factor (PAF), and leukotrienes which are recognized to be of importance in asthma. The structure-activity relationship studies have shown that the optimum moiety on the 1-position of the pyrroloquinoline nucleus is a 2-[4-(4-methyl-2-pyridinyl)-1-piperazinyl]ethyl chain in conjunction with a methyl group on the 2-position for potent antagonism of both histamine and PAF. The introduction of substituents on the 8- and 4-positions was also investigated in order to increase the potency of 5-lipoxygenase inhibition while retaining or improving the activities against histamine and PAF. This series is exemplified by 4-n-butyl-5,6-dihydro-8-hydroxy-2-methyl-1- [2-[4-(4-methyl-2-pyridinyl)-1-piperazinyl]ethyl]-4H-pyrrolo[3,2,1- ij]quinoline (24, KC 11404) which was found to be active against all three of the selected mediators. Compound 24 was found to be orally active in guinea pig models against the histaminic phase of antigen-induced bronchospasm and PAF-induced bronchoconstriction (ED50 = 1.9 and 2.1 mumol/kg, respectively). When tested against the leukotriene-dependent phase of the antigen-induced bronchoconstriction, compound 24 showed the same potency as zileuton.

100 项与 KC-11404 相关的药物交易

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