ZK-811752(BX471)抑制剂 | 288262-96-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: ZK-811752(BX471)抑制剂
• 中文别名: Bx471盐酸盐；ZK-811752(BX471) 抑制剂
• 英文名称: BX471 hydrochloride
• 英文别名: [5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea;hydrochloride
• CAS: 288262-96-4
• 化学式: C21H25Cl2FN4O3
• 分子量: 471.3
• InChiKey: FRUCNQBAWUHKLS-PFEQFJNWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  87.9
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-chloro-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone 、 (5-Chloro-2-hydroxy-phenyl)-urea 生成 ZK-811752(BX471)抑制剂
  参考文献：
  名称：

  Piperazine derivatives and their use as anti-inflammatory agents

  摘要：

  本发明涉及式(Ia)的酰基哌嗪衍生物，其中R1a、R2、R3、R4、R5和R6在此被定义，它们是作为抗炎药物有用的。本发明还涉及其他酰基哌嗪衍生物、含有该发明化合物的制药组合物，以及使用该化合物治疗人类炎症性疾病的方法。

  公开号：

  US06207665B1

文献信息

• NOVEL SALT 628
  申请人：Briggner Lars-Erik

  公开号：US20100216843A1

  公开（公告）日：2010-08-26

  6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.

  6-甲基-5-(1-甲基-1H-吡唑-5-基)-N-[5-(甲磺酰基)吡啶-2-基]甲基}-2-氧代-1-[3-(三氟甲基)苯基]-1,2-二氢吡啶-3-羧酰胺 4-甲基苯磺酸盐及其一种新的结晶形式，以及制备这种盐和形式的方法，包含这种盐和形式的药物组合物，以及使用这种盐和形式进行治疗的方法。
• Spirocyclic Heterocycles Medicaments Containing Said Compounds, Use Thereof And Method For Their Production
  申请人：Himmelsbach Frank

  公开号：US20110046148A1

  公开（公告）日：2011-02-24

  The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.

  本发明涉及一般式(I)的螺环杂环化合物，其包括其互变异构体、立体异构体、它们的混合物和盐，特别是与无机或有机酸形成的生理上可接受的盐，具有有价值的药理特性，特别是对酪氨酸激酶介导的信号传导具有抑制作用，其用于治疗疾病，特别是肿瘤性疾病以及良性前列腺增生（BPH）、肺部和气道疾病，以及其制备方法。
• Piperazine derivatives and their use as anti-inflammatory agents
  申请人：Schering Aktiengesellschaft

  公开号：US06207665B1

  公开（公告）日：2001-03-27

  This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

  本发明涉及式(Ia)的酰基哌嗪衍生物，其中R1a、R2、R3、R4、R5和R6在此被定义，它们是作为抗炎药物有用的。本发明还涉及其他酰基哌嗪衍生物、含有该发明化合物的制药组合物，以及使用该化合物治疗人类炎症性疾病的方法。
• New Combination 665
  申请人：Cadogan Elaine Bridget

  公开号：US20080242649A1

  公开（公告）日：2008-10-02

  The invention provides a pharmaceutical product comprising a first active ingredient which is N—[2-(Diethylamino)ethyl]-N-(2-[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist which is Aclidinium bromide, Glycopyrrolate, Oxitropium bromide, Pirenzepine, telenzepine, Tiotropium bromide, 3(R)—(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide, 3(R)—1-phenethyl-3-(9H-xanthene-9-carbonyloxy)-1-azoniabicyclo[2.2.2]octane bromide or (3R)—3-[(2S)—2-cyclopentyl-2-hydroxy-2-thien-2-ylacetoxy]-1-(2-phenoxyethyl)-1-azoniabicyclo[2.2.2]actane bromide; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.

  本发明提供了一种药物产品，其中包括第一活性成分，该成分为N-[2-(二乙氨基)乙基]-N-(2-[2-(4-羟基-2-氧代-2,3-二氢-1,3-苯并噻唑-7-基)乙基]氨基}乙基)-3-[2-(1-萘基)乙氧基]丙酰胺或其盐，并且包括第二活性成分，所述第二活性成分选自：非类固醇糖皮质激素受体（GR受体）激动剂；抗氧化剂；CCR1拮抗剂；趋化因子拮抗剂（非CCR1）；皮质类固醇；CRTh2拮抗剂；DP1拮抗剂；组蛋白去乙酰化酶诱导剂；IKK2抑制剂；COX抑制剂；脂氧合酶抑制剂；白三烯受体拮抗剂；MPO抑制剂；Aclidinium溴化物、Glycopyrrolate、Oxitropium溴化物、Pirenzepine、telenzepine、Tiotropium溴化物、3(R)-（2-羟基-2,2-二硫基-2-乙酰氧基）-1-(3-苯氧基丙基)-1-氮杂双环[2.2.2]辛烷溴化物、3(R)-1-苯乙基-3-(9H-黄酮-9-羧酰氧基)-1-氮杂双环[2.2.2]辛烷溴化物或（3R）-3-[(2S)-2-环戊基-2-羟基-2-噻唑基乙氧基]-1-(2-苯氧基乙基)-1-氮杂双环[2.2.2]辛烷溴化物；p38抑制剂；PDE抑制剂；PPARγ激动剂；蛋白酶抑制剂；他汀类药物；血栓素拮抗剂；血管扩张剂；或ENAC阻滞剂（上皮钠通道阻滞剂），以及其在呼吸系统疾病治疗中的应用。
• Combinations of Beta-2-Adrenoceptor Agonistic Benzothiazolone
  申请人：Cadogan Elaine Bridget

  公开号：US20100029732A1

  公开（公告）日：2010-02-04

  The invention provides a pharmaceutical product comprising a first active ingredient which is N-[2-(Diethylamino)ethyl]-N-(2-[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propan amide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor)=Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist which is Aclidinium bromide, Glycopyrrolate, Oxitropium bromide, Pirenzepine, telenzepine, Tiotropium bromide, 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azo-niabicyclo[2.2.2]octane bromide, 3(R)- 1 -phenethyl-3-(9H-xanthene-9-carbonyloxy)-1-azoniabicyclo[2.2.2]octane bromide or (3R)-3-[(2S)-2-cyclopentyl-2-hydroxy-2-thien-2-ylacetoxy]-1-(2-phenoxyethyl)-1-azoniabicyclo[2.2.2]actane bromide; a p38 inhibitor; a PDE inhibitor; a PPARy agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.

  该发明提供了一种药物产品，包括第一活性成分为N-[2-(二乙氨基)乙基]-N-(2-[2-(4-羟基-2-氧代-2,3-二氢-1,3-苯并噻唑-7-基)乙基]氨基}乙基)-3-[2-(1-萘基)乙氧基]丙酰胺或其盐，和第二活性成分从以下中选择：非甾体型糖皮质激素受体（GR受体）=激动剂；抗氧化剂；CCR1拮抗剂；趋化因子拮抗剂（非CCR1）；类固醇；CRTh2拮抗剂；DP1拮抗剂；组蛋白去乙酰化酶诱导剂；IKK2抑制剂；COX抑制剂；脂氧合酶抑制剂；白三烯受体拮抗剂；MPO抑制剂；Aclidinium溴化物，Glycopyrrolate，Oxitropium溴化物，Pirenzepine，telenzepine，Tiotropium溴化物，3(R)-(2-羟基-2,2-二噻吩-2-乙氧基)-1-(3-苯氧基丙基)-1-氮杂双环[2.2.2]辛烷溴化物，3(R)-1-苯乙基-3-(9H-黄酮-9-羰基氧基)-1-氮杂双环[2.2.2]辛烷溴化物或(3R)-3-[(2S)-2-环戊基-2-羟基-2-噻吩-2-乙氧基]-1-(2-苯氧基乙基)-1-氮杂双环[2.2.2]辛烷溴化物；p38抑制剂；PDE抑制剂；PPARy激动剂；蛋白酶抑制剂；他汀类药物；血栓素受体拮抗剂；血管扩张剂；或ENAC阻滞剂（上皮钠通道阻滞剂），以及其在呼吸道疾病治疗中的应用。