[(1R)-3-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-3-[3-[2-(phenylmethoxycarbonylamino)ethoxy]phenyl]piperazin-1-yl]-3-oxo-1-phenylpropyl]carbamic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: [(1R)-3-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-3-[3-[2-(phenylmethoxycarbonylamino)ethoxy]phenyl]piperazin-1-yl]-3-oxo-1-phenylpropyl]carbamic acid
• 化学式: C₄₀H₄₃N₇O₈
• 分子量: 749.8
• InChiKey: PUGBMSXZIRELSE-GWLFDFPQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  55
• 可旋转键数：
  15
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  191
• 氢给体数：
  4
• 氢受体数：
  12

文献信息

• [EN] 2-(1H-INDOL-4-YLMETHYL)-3H-IMIDAZO[4,5-B]PYRIDINE-6-CARBONITRILE DERIVATIVES AS COMPLEMENT FACTOR B INHIBITORS USEFUL FOR THE TREATMENT OF OPHTHALMIC DISEASES<br/>[FR] DÉRIVÉS DE 2-(1H-INDOL-4-YLMÉTHYL)-3H-IMIDAZO[4,5-B]PYRIDINE-6-CARBONITRILE COMME INHIBITEURS DU FACTEUR B DU COMPLÉMENT UTILES POUR LE TRAITEMENT DE MALADIES OPHTALMIQUES
  申请人：NOVARTIS AG

  公开号：WO2014143638A1

  公开（公告）日：2014-09-18

  The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.

  本发明提供了一种化合物的公式（I）：其中X为N或CH，Y为NH，O或S，制造这些化合物的方法，以及它们作为因子B抑制剂用于治疗与补体替代途径激活相关的疾病和疾病的用途，如年龄相关性黄斑变性、糖尿病性视网膜病变和相关眼科疾病。本发明还提供了药物组合和药理活性剂的配方。
• [EN] 2-BENZYL-BENZIMIDAZOLE COMPLEMENT FACTOR B INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DU FACTEUR B DU COMPLÉMENT À BASE DE 2-BENZYL-BENZIMIDAZOLE ET LEURS UTILISATIONS
  申请人：NOVARTIS AG

  公开号：WO2015066241A1

  公开（公告）日：2015-05-07

  The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  本发明提供了一种具有化学式（I）的化合物，一种制造本发明化合物的方法以及其治疗用途。本发明还提供了一种药理活性剂的组合和制药组合物。
• [EN] PIPERIDINYL INDOLE DERIVATIVES AND THEIR USE AS COMPLEMENT FACTOR B INHIBITORS<br/>[FR] DÉRIVÉS DE PIPÉRIDINYL-INDOLE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DU FACTEUR B DU COMPLÉMENT
  申请人：NOVARTIS AG

  公开号：WO2015009616A1

  公开（公告）日：2015-01-22

  The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitors of the complement alternative pathway, in particular of Factor B. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  本发明提供了一种公式I的化合物：（I）一种制造本发明化合物的方法，以及其作为补体替代途径抑制剂的治疗用途，特别是对因子B的抑制。本发明还提供了一种药理活性剂的组合和一种药物组合。
• Complement pathway modulators and uses thereof
  申请人：ADAMS Christopher Michael

  公开号：US20150250767A1

  公开（公告）日：2015-09-10

  The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  本发明提供了一种I式化合物，一种制造本发明化合物的方法以及其治疗用途。本发明还提供了一种药理活性剂的组合和一种药物组合物。
• Complement Factor B inhibitors and uses there of
  申请人：ADAMS Christopher Michael

  公开号：US20160024079A1

  公开（公告）日：2016-01-28

  The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.

  本发明提供了一个式子为(I)的化合物：其中X是N或CH，Y是NH，O或S，制造这些化合物的方法，以及它们作为因子B抑制剂治疗与补体替代途径激活相关的疾病和病症的用途，例如老年性黄斑变性，糖尿病视网膜病变和相关眼科疾病。本发明还提供了药物组合和药理活性剂的组合。