1-(3,3,3-trifluoro-propionylamino)-cyclopropanecarboxylic acid 4-[3-chloro-2-(5-methyl-[1,3,4]oxadiazol-2-yl)-indol-1-yl]-benzylamide | 1374455-81-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-(3,3,3-trifluoro-propionylamino)-cyclopropanecarboxylic acid 4-[3-chloro-2-(5-methyl-[1,3,4]oxadiazol-2-yl)-indol-1-yl]-benzylamide
• 英文别名: N-[[4-[3-chloro-2-(5-methyl-1,3,4-oxadiazol-2-yl)indol-1-yl]phenyl]methyl]-1-(3,3,3-trifluoropropanoylamino)cyclopropane-1-carboxamide
• CAS: 1374455-81-8
• 化学式: C₂₅H₂₁ClF₃N₅O₃
• 分子量: 531.922
• InChiKey: CAVZCAIHWDTUHK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  37
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• INDOLE DERIVATIVES
  申请人：Beke Gyula

  公开号：US20130217702A1

  公开（公告）日：2013-08-22

  The present invention relates to the indole derivatives of formula (I), wherein R 1 -R 6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

  本发明涉及式(I)的吲哚衍生物，其中R1-R6和X在权利要求中定义，并且其光学对映体或消旋体和/或盐是布雷金肽B1的选择性拮抗剂，用于制备这些化合物的方法，含有它们的药理学组合物以及它们在治疗或预防疼痛和炎症症状中的用途。
• [EN] INDOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'INDOLE
  申请人：RICHTER GEDEON NYRT

  公开号：WO2012059776A1

  公开（公告）日：2012-05-10

  The present invention relates to the indole derivatives of formula (I), wherein R1- R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

  本发明涉及式(I)的吲哒衍生物，其中R1-R6和X在权利要求中定义，并且其光学对映体或消旋体和/或盐是布雷金肽B1的选择性拮抗剂，用于生产这些化合物的方法，含有它们的药物组合物以及它们在治疗或预防疼痛和炎症状况中的使用。
• [EN] SOLID FORM OF BOSENTAN<br/>[FR] FORME SOLIDE DU BOSENTAN
  申请人：BASF SE

  公开号：WO2013124791A1

  公开（公告）日：2013-08-29

  A novel solid form of bosentan comprises as the active ingredient the N-[6-(2- Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]-4-tert-butyl- benzenesulfonamide] and maleic acidor gentisic acid, especially as cocrystal former. The composition shows improved properties such as dissolution kinetic and hydration stability.

  一种新型的波生坦固体形式，其活性成分为N-[6-(2-羟乙氧基)-5-(2-甲氧基苯氧基)-2-嘧啶-2-基嘧啶-4-基]-4-叔丁基苯磺酰胺]和马来酸或香草酸，尤其是作为共晶形成剂。该组合物显示了改善的性质，如溶解动力学和水合稳定性。
• BOSENTAN SALTS
  申请人：ZHU Jie

  公开号：US20090291974A1

  公开（公告）日：2009-11-26

  Stable acid addition salts of bosentan useful for the purification of bosentan base; the salts are in solid state and the starting acid has a pKa lower than 3.

  稳定的鲍生坦盐酸盐可用于纯化鲍生坦碱；这些盐处于固态，起始酸的pKa值低于3。
• DISINTEGRATING PARTICLE COMPOSITION AND ORALLY RAPIDLY DISINTEGRATING TABLET
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP2465539A1

  公开（公告）日：2012-06-20

  There has been a need for an orally rapidly disintegrating tablet which has a good texture and taste in the oral cavity, such a sufficient hardness as not giving any worry of being chipped or dusted during production or transportation and good disintegrating properties in the oral cavity and can sustain a sufficient hardness even under humid conditions after opening. Disclosed are a disintegrating particle composition which is prepared by dispersing, in the presence of water, mannitol, xylitol, an inorganic excipient, a disintegrating agent and carmellose and drying, and an orally rapidly disintegrating tablet which comprises said disintegrating particle composition, an active substance and a disintegrating agent. The disintegrating tablet has a good texture and taste, an appropriate hardness and good disintegrating properties and can sustain a sufficient hardness under humid conditions.

  人们需要一种口服快速崩解片剂，这种片剂在口腔中具有良好的质地和口感，有足够的硬度，不会担心在生产或运输过程中碎裂或沾上灰尘，在口腔中具有良好的崩解性能，即使在开封后潮湿的条件下也能保持足够的硬度。本发明公开了一种崩解颗粒组合物，其制备方法是在有水存在的情况下，将甘露醇、木糖醇、无机赋形剂、崩解剂和卡麦芽糖分散并干燥；还公开了一种口服快速崩解片剂，其包括所述崩解颗粒组合物、活性物质和崩解剂。该崩解片具有良好的质地和口感、适当的硬度和良好的崩解性能，并能在潮湿条件下保持足够的硬度。