4-(trifluoromethyl)piperidine-1-carbonyl chloride | 862274-38-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-(trifluoromethyl)piperidine-1-carbonyl chloride
• 英文别名: 4-(Trifluoromethyl)piperidine-1-carbonyl chloride
• CAS: 862274-38-2
• 化学式: C₇H₉ClF₃NO
• 分子量: 215.603
• InChiKey: LTABPCGEHHURFG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-氯苯并[D]异恶唑-3-醇 、 4-(trifluoromethyl)piperidine-1-carbonyl chloride 生成 4-trifluoromethyl-piperidine-1-carboxylic acid 6-chloro-benzo[d]isoxazol-3-yl ester
  参考文献：
  名称：

  Azole derivatives in the form of lipase and phospholipase inhibitors

  摘要：

  本发明涉及一般式I所定义的唑类衍生物，以及它们在治疗需要抑制激素敏感性脂肪酶（HSL）的情况下的用途。HSL是脂肪细胞中的一种异构酶，被胰岛素抑制，负责分解脂肪细胞中的脂肪，从而将脂肪成分转移到血液中。因此，抑制这种酶就相当于化合物具有类胰岛素的效果。

  公开号：

  US08921404B2
• 作为产物：
  描述：

  4-(trifluoromethyl)piperidine hydrochloride 、 三光气 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 4-(trifluoromethyl)piperidine-1-carbonyl chloride
  参考文献：
  名称：

  [DE] INDAZOLDERIVATE ALS INHIBITOREN DER HORMON SENSITIVEN LIPASE
  [EN] INDAZOLE DERIVATIVES AS INHIBITORS OF HORMONE-SENSITIVE LIPASES
  [FR] DERIVES D'INDAZOLE UTILISES COMME INHIBITEURS DE LA LIPASE HORMONO-SENSIBLE

  摘要：

  本发明涉及一般式（I）或（II）的吲哚衍生物，其具有描述中所指定的含义，其药用可用盐以及它们作为药物的用途。

  公开号：

  WO2005073199A1

文献信息

• [EN] BENZOXAZEPINES AS INHIBITORS OF MTOR AND METHODS OF THEIR USE AND MANUFACTURE<br/>[FR] BENZOXAZÈPINES COMME INHIBITEURS DE MTOR ET MÉTHODES D'UTILISATION ET DE FABRICATION
  申请人：EXELIXIS INC

  公开号：WO2010138490A1

  公开（公告）日：2010-12-02

  The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula wherein the combination of R1 and R2 are as defined herein, and pharmaceutically acceptable salts thereof.

  这项发明涉及 mTOR 的抑制剂及其药用盐或溶剂，以及它们的使用方法。这些抑制剂通常具有结构式，其中 R1 和 R2 的组合如本文所定义，并且其药用盐。
• [EN] BENZOXAZEPINES AS INHIBITORS OF PI3K/m TOR AND METHODS OF THEIR USE AND MANUFACTURE<br/>[FR] BENZOXAZÉPINES COMME INHIBITEURS DE PI3K/M TOR, MÉTHODES D'UTILISATION ET DE FABRICATION BENZOXAZEPINES AS INHIBITORS OF PI3K/M TOR AND METHODS OF THEIR USE AND MANUFACTURE
  申请人：EXELIXIS INC

  公开号：WO2010138487A1

  公开（公告）日：2010-12-02

  The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK- transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.

  这项发明涉及式(I)的化合物：该发明提供了抑制、调节和/或调节P13K和/或mTOR的化合物，这些化合物在治疗哺乳动物的高增殖性疾病，如癌症，方面非常有用。该发明还提供了制备该化合物的方法，以及在治疗哺乳动物，特别是人类的高增殖性疾病中使用这些化合物的方法，以及含有这些化合物的药物组合物。例如，对PI3fC-α mTOR或两者都具有活性有助于其病理学和/或症状学的癌症包括乳腺癌、套细胞淋巴瘤、肾细胞癌、急性髓细胞白血病、慢性髓细胞白血病、NPM/ALK转化的间变性大细胞淋巴瘤、弥漫性大B细胞淋巴瘤、横纹肌肉瘤、卵巢癌、子宫内膜癌、宫颈癌、非小细胞肺癌、小细胞肺癌、腺癌、结肠癌、直肠癌、胃癌、肝细胞癌、黑色素瘤、胰腺癌、前列腺癌、甲状腺癌、间变性大细胞淋巴瘤、血管瘤、胶质母细胞瘤或头颈癌。
• Indazole derivatives as inhibitors of hormone sensitive lipase
  申请人：Zoller Gerhard

  公开号：US20050197348A1

  公开（公告）日：2005-09-08

  The present invention relates to indazole derivatives of the general formulae I or II having the meanings indicated in the description, to the pharmaceutically useful salts thereof and the use thereof as drugs.

  本发明涉及具有描述中所示含义的一般式I或II的吲唑衍生物，其药用盐以及作为药物的用途。
• Diacyl indazole derivatives as lipase and phospholipase inhibitors
  申请人：Zoller Gerhard

  公开号：US20080287448A1

  公开（公告）日：2008-11-20

  The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.

  该发明涉及一般式(I)或(II)的二酰基吲唑衍生物以及其药用可接受的盐：其中X，R1和R2如本文所定义。该发明还涉及将这些化合物用作药物产品。
• AZOLE DERIVATIVES IN THE FORM OF LIPASE AND PHOSPHOLIPASE INHIBITORS
  申请人：Zoller Gerhard

  公开号：US20080090867A1

  公开（公告）日：2008-04-17

  The invention relates to azole derivatives of the general formula I as defined in the present application as well as to their uses in treatment of conditions that would benefit from their inhibitory effect on hormone sensitive lipase, HSL, an allosteric enzyme in adipocytes which is inhibited by insulin and is responsible for the breakdown of fats in fat cells and thus for transferring fat constituents into the blood stream. Inhibition of this enzyme is therefore equivalent to an insulin-like effect of the compounds of the invention.

  本发明涉及一般式I所定义的唑类衍生物，以及它们在治疗需要其抑制荷尔蒙敏感性脂肪酶（HSL）的条件中的用途。HSL是脂肪细胞中的一种变构酶，受胰岛素抑制，负责分解脂肪细胞中的脂肪，并将脂肪成分转移到血液中。因此，抑制该酶等同于本发明化合物的胰岛素样效应。