imidazo[2,1-b]thiazole-6-carboxylic acid hydrobromide | 725234-39-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并噻唑类
• 英文名称: imidazo[2,1-b]thiazole-6-carboxylic acid hydrobromide
• 英文别名: imidazo[2,1-b][1,3]thiazole-6-carboxylic acid;hydrobromide
• CAS: 725234-39-9
• 化学式: BrH*C₆H₄N₂O₂S
• 分子量: 249.088
• InChiKey: RAVYQOPXHWEAFU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.67
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  82.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-7-((S)-pyrrolidin-3-yloxy)-2,3-dihydro-1H-pyrido[3,4-b][1,4]oxazine 、 imidazo[2,1-b]thiazole-6-carboxylic acid hydrobromide 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 17.08h， 以52%的产率得到imidazo[2,1-b]thiazol-6-yl-{(S)-3-[1-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-2,3-dihydro-1H-pyrido[3,4-b][1,4]oxazin-7-yloxy]-pyrrolidin-1-yl}-methanone
  参考文献：
  名称：

  Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives

  摘要：

  该发明涉及式(I)的二氢苯并噁嗪和二氢吡啶噁嗪化合物，以及其药学上可接受的盐和/或溶剂化合物，其中Y、V、W、U、Q、R1、R5、R7和R30如描述中所定义。这些化合物适用于治疗由PI3K酶活性介导的疾病或疾病。

  公开号：

  US20130165436A1

文献信息

• LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY
  申请人：Bittermann Holger

  公开号：US20130131321A1

  公开（公告）日：2013-05-23

  The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR 1 —C(O)—, and wherein either NR 1 is attached to Ar 1 and —C(O)— is attached to Ar 2 , or —C(O)— is attached to Ar 1 and NR 1 is attached to Ar 2 ; and R 1 is hydrogen or C 1 to C 4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar 1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar 2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C 1 to C 4 alkyl; C 2 to C 4 alkenyl; C 2 to C 4 alkynyl; a halogen; C 1 to C 4 haloalkyl; hydroxyl-substituted C 1 to C 4 alkyl; C 1 to C 4 alkoxy; hydroxyl-substituted C 1 to C 4 alkoxy; C 1 to C 4 alkylamino; C 1 to C 4 alkylthio; and combinations thereof.

  本发明涉及使用具有支持材料和至少一种共价键合到支持材料的配体的替代基矩阵，用于亲和纯化抗体或抗体片段，其中该配体由式(I)表示，其中Sp是一个空间基团；v为0或1；Am是一个酰胺基团-NR1-C（O）-，其中NR1连接到Ar1，-C（O）-连接到Ar2，或-C（O）-连接到Ar1，NR1连接到Ar2；R1是氢或C1到C4烷基，优选氢或甲基，更优选氢；Ar1是二价的5-或6-成员取代或未取代芳香环；Ar2是5-或6-成员的杂环芳香环，它(a)通过单键连接到另一个5-或6-成员的芳香环；或（b）作为多环环系统的一部分与另一个5-或6-成员的芳香环融合；或（c）连接到至少一个取代基，所述取代基选择自C1到C4烷基；C2到C4烯基；C2到C4炔基；卤素；C1到C4卤代烷基；羟基取代的C1到C4烷基；C1到C4烷氧基；羟基取代的C1到C4烷氧基；C1到C4烷基氨基；C1到C4烷基硫基；以及其组合。
• [EN] LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY<br/>[FR] LIGANDS POUR LA PURIFICATION D'ANTICORPS ET DE PROTÉINE DE FUSION À FC PAR CHROMATOGRAPHIE D'AFFINITÉ
  申请人：GRAFFINITY PHARMACEUTICALS GMBH

  公开号：WO2012017021A2

  公开（公告）日：2012-02-09

  The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group -NR1-C(O)-, and wherein either NR1 is attached to Ar1 and C(O)- is attached to Ar2, or -C(O)- is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a halogen; C1 to C4 haloalkyl; hydroxyl-substituted C1 to C4 alkyl; C1 to C4 alkoxy; hydroxyl-substituted C1 to C4 alkoxy; C1 to C4 alkylamino; C1 to C4 alkylthio; and combinations thereof.
• Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives
  申请人：Novartis AG

  公开号：US20130165436A1

  公开（公告）日：2013-06-27

  The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R 1 , R 5 , R 7 and R 30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

  该发明涉及式(I)的二氢苯并噁嗪和二氢吡啶噁嗪化合物，以及其药学上可接受的盐和/或溶剂化合物，其中Y、V、W、U、Q、R1、R5、R7和R30如描述中所定义。这些化合物适用于治疗由PI3K酶活性介导的疾病或疾病。