1-Benzofuran-7-sulfonyl chloride | 1191030-88-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 1-Benzofuran-7-sulfonyl chloride
• CAS: 1191030-88-2
• 化学式: C₈H₅ClO₃S
• mdl: MFCD16090165
• 分子量: 216.64
• InChiKey: MEOOVUNNRYYGCV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  13
• 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：
  55.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2,6-difluoro-N1-(3-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-yl)pyridin-2-yl)benzene-1,3-diamine 、 1-Benzofuran-7-sulfonyl chloride 、 吡啶 在 盐酸 、 水 、 二氯甲烷 、 sulfuric anhydride magnesium 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 N-(2,4-difluoro-3-(3-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-yl)pyridin-2-ylamino)phenyl)benzofuran-7-sulfonamide
  参考文献：
  名称：

  NOVEL PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYL SULFONAMIDE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION WITH INHIBITORY ACTIVITY AGAINST RAF KINASE, CONTAINING SAME AS ACTIVE INGREDIENT

  摘要：

  本发明提供了一种新型嘌呤基吡啶基氨基-2,4-二氟苯磺酰胺衍生物及其药学上可接受的盐、其制备方法以及含有其作为活性成分的具有抑制Raf激酶活性的制药组合物。本发明的嘌呤基吡啶基氨基-2,4-二氟苯磺酰胺衍生物有效调节B-Raf激酶活性，因此可能有助于预防或治疗由Raf激酶过度活化引起的癌症，特别是各种黑色素瘤、结直肠癌、前列腺癌、甲状腺癌、卵巢癌等。

  公开号：

  US20130317023A1

文献信息

• [EN] 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10<br/>[FR] ANTAGONISTES DE 2-SULFONYLAMINO-4-HÉTÉROARYL BUTYRAMIDE DE CCR10
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009126675A1

  公开（公告）日：2009-10-15

  This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of formula (I) to treat a diseases and disorders that are mediated or sustained through the activity of CCR10.

  本发明涉及一种具有式（I）的化合物及其药学上可接受的盐，其中R1、R2、R4、Ar和Het如本文中所定义。该发明还涉及使用式（I）的化合物治疗通过CCR10活性介导或维持的疾病和紊乱的方法。
• 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10
  申请人：Abeywardane Asitha

  公开号：US20110275800A1

  公开（公告）日：2011-11-10

  This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 4 . Ar and Het are as defined herein. The invention also relates to methods of using the compound of formula (I) to treat a diseases and disorders that are mediated or sustained through the activity of CCR 10 .

  本发明涉及公式(I)的化合物及其药学上可接受的盐，其中R1、R2、R4、Ar和Het的定义如本文所述。本发明还涉及使用公式(I)的化合物治疗通过CCR10活性介导或持续的疾病和障碍的方法。
• NOVEL PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYL SULFONAMIDE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION WITH INHIBITORY ACTIVITY AGAINST RAF KINASE, CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：Shim Eun Kyong

  公开号：US20130317023A1

  公开（公告）日：2013-11-28

  A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.

  本发明提供了一种新型嘌呤基吡啶基氨基-2,4-二氟苯磺酰胺衍生物及其药学上可接受的盐、其制备方法以及含有其作为活性成分的具有抑制Raf激酶活性的制药组合物。本发明的嘌呤基吡啶基氨基-2,4-二氟苯磺酰胺衍生物有效调节B-Raf激酶活性，因此可能有助于预防或治疗由Raf激酶过度活化引起的癌症，特别是各种黑色素瘤、结直肠癌、前列腺癌、甲状腺癌、卵巢癌等。
• PHARMACEUTICAL COMPOSITIONS COMPRISING NITROXYL DONORS
  申请人：CARDIOXYL PHARMACEUTICALS

  公开号：US20150366977A1

  公开（公告）日：2015-12-24

  The present disclosure provides nitroxyl donating pharmaceutical compositions comprising N-substituted hydroxylamine derivatives. The compositions are highly efficacious in treating cardiovascular diseases (e.g., heart failure), have a suitable toxicological profile, and are sufficiently stable for intravenous or oral administration.

  本公开提供了含有N-取代羟胺衍生物的亚硝酰基供体药物组合物。该组合物在治疗心血管疾病（如心力衰竭）方面具有高效性，具有适当的毒理学特性，并且对于静脉或口服给药具有足够的稳定性。
• Pharmaceutical compositions comprising nitroxyl donors
  申请人：Cardioxyl Pharmaceuticals, Inc.

  公开号：US10245249B2

  公开（公告）日：2019-04-02

  The present disclosure provides nitroxyl donating pharmaceutical compositions comprising N-substituted hydroxylamine derivatives. The compositions are highly efficacious in treating cardiovascular diseases (e.g., heart failure), have a suitable toxicological profile, and are sufficiently stable for intravenous or oral administration.

  本公开提供了由 N-取代的羟胺衍生物组成的硝基捐献药物组合物。这些组合物在治疗心血管疾病（如心力衰竭）方面疗效显著，具有合适的毒理学特征，并且足够稳定，可用于静脉注射或口服给药。