isoindoline-1-carboxamide | 1095715-76-6

• 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: isoindoline-1-carboxamide
• 英文别名: 2,3-dihydro-1H-isoindole-1-carboxamide
• CAS: 1095715-76-6
• 化学式: C₉H₁₀N₂O
• 分子量: 162.191
• InChiKey: VKYTVITWNRXGGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (R,S)-Boc-1,3-二氢-2H-异吲哚羧酸 在 盐酸 、 氨 、 氯甲酸乙酯 、 三乙胺 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 水 为溶剂， 反应 3.17h， 生成 isoindoline-1-carboxamide
  参考文献：
  名称：

  WO2009/1128

  摘要：

  公开号：

文献信息

• [EN] ISOINDOLINE DERIVATIVES COMPRISING ADDITIONAL HETEROCYCLIC GROUPS AND THEIR USE IN THE TREATMENT OF PAIN DISORDERS<br/>[FR] DÉRIVÉS ISOINDOLINE COMPRENANT DES GROUPES HÉTÉROCYCLIQUES SUPPLÉMENTAIRES ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES DE LA DOULEUR
  申请人：ASTRAZENECA AB

  公开号：WO2009145720A1

  公开（公告）日：2009-12-03

  Compounds of formula I are claimed wherein R1 is hydrogen; C1-3 alkyl, optionally substituted by one or more substituents independently selected from hydroxy, C1-3 alkoxy andfluoro; C1-3 alkoxy, optionally substituted by one or morefluoro; cyano; hydroxy or halo; m is 1,2 or 3; Het is C5-6 heteroaryl substituted by 1 or 2 substituents R2; R2 is C1-4 alkyl; C1-4 haloalkyl;C 1-4 haloalkoxy; halo; C1-4 alkoxy; or C3-7 cycloalkyloxy, optionally substituted by one or morefluoro; D is C5-6 heteroaryl; C3-7 heterocycloalkyl; or C3-7 cycloalkyl; wherein each D may optionally be substituted by one or more X4; X4 is halo; or C1-3 alkyl, optionally substituted by one or morefluoro; C1-3 alkyl-O-C1-3 alkyl, optionally substituted by one or morefluoro; C1-3 alkoxy, optionally substituted by one or morefluoro; cyano; hydroxy; oxo; R3 0(C=O); or R4(C=O); R3 is C1-4 alkyl; C1-4 alkyl-O-C1-4 alkyl; C5-6 cycloalkyl; aryl; or aryl-C1-2 alkyl; R4 is C1-4 alkyl; or C5-6 heteroaryl; L1is C1-4 alkylene; or a bond; and L2 is C1-3 alkylene. Compounds of the invention are useful in therapy, such as pain therapy.

  式I的化合物被要求，其中R1是氢；C1-3烷基，可选地由一个或多个取代基独立选择自羟基、C1-3烷氧基和氟代基；C1-3烷氧基，可选地由一个或多个氟代基取代；氰基；羟基或卤素基；m为1,2或3；Het是C5-6杂环芳基，取代为1或2个取代基R2；R2是C1-4烷基；C1-4卤代烷基；C1-4卤代烷氧基；卤素；C1-4烷氧基；或C3-7环烷氧基，可选地由一个或多个氟代基取代；D是C5-6杂环芳基；C3-7杂环烷基；或C3-7环烷基；其中每个D可选择地被一个或多个X4取代；X4是卤素；或C1-3烷基，可选地由一个或多个氟代基取代；C1-3烷基-O-C1-3烷基，可选地由一个或多个氟代基取代；C1-3烷氧基，可选地由一个或多个氟代基取代；氰基；羟基；氧代基；R3 0(C=O)；或R4(C=O)；R3是C1-4烷基；C1-4烷基-O-C1-4烷基；C5-6环烷基；芳基；或芳基-C1-2烷基；R4是C1-4烷基；或C5-6杂环芳基；L1是C1-4烷基；或一个键；而L2是C1-3烷基。该发明的化合物在治疗中有用，如疼痛治疗。
• NEW COMPOUNDS I/418
  申请人：Bjore Annika

  公开号：US20080015237A1

  公开（公告）日：2008-01-17

  There is provided compounds of formula I, wherein R 1 to R 7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

  提供了式I的化合物， 其中R1至R7在描述中给出了它们的含义，这些化合物在预防和治疗心律失常方面非常有用，特别是房性和室性心律失常。
• [EN] 2,3-DIHYDROISOINDOLE-1-CARBOXAMIDES USEFUL AS ROR-GAMMA MODULATORS<br/>[FR] 2,3-DIHYDROISOINDOLE-1-CARBOXAMIDES UTILES EN TANT QUE MODULATEURS DE ROR-GAMMA
  申请人：ASTRAZENECA AB

  公开号：WO2018229155A1

  公开（公告）日：2018-12-20

  The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an RORγ and/or RORγt mediated disease state.

  本规范提供了化合物的公式(I)或其药用可接受盐；制备这种化合物的方法；以及将这种化合物用于治疗RORγ和/或RORγt介导的疾病状态。
• [EN] AMINE COMPOUNDS<br/>[FR] DERIVES D'INDOLE SERVANT D'ANTAGONISTE DE SOMATOSTATINE
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2004046107A1

  公开（公告）日：2004-06-03

  The present invention provide a compound of the formula (I) wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.

  本发明提供了一种公式(I)的化合物，其中环A代表一个具有可选取代基的芳香环；B、Y和Ya相同或不同，分别代表一个键等；R1和R2相同或不同，每个代表一个氢原子等；R3代表一个氢原子等；R4和R5相同或不同，每个代表一个氢等；R6代表一个可选有取代基的吲哚基团；Z和Za相同或不同，每个代表一个氢原子等；或其盐或前药，具有生长抑素受体结合抑制活性，并且用于预防或治疗与生长抑素相关的疾病。
• 2,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer
  申请人：Bailey Peter John

  公开号：US20080058332A1

  公开（公告）日：2008-03-06

  The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R 1 , R 2 , q, R 3 , r, R 4 , X 1 and Q 1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.

  本发明涉及式(I)的嘧啶衍生物，其中p、R1、R2、q、R3、r、R4、X1和Q1中的每一个具有描述中定义的任何含义；制备它们的过程，含有它们的制药组合物以及它们在制造用于在诸如人类等恒温动物中产生抗增殖效应的药物的制剂中的使用。