4-pyranylcarboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡喃
• 英文名称: 4-pyranylcarboxylic acid
• 英文别名: 2H-pyran-4-carboxylic acid
• 化学式: C₆H₆O₃
• mdl: MFCD19231650
• 分子量: 126.112
• InChiKey: MSRAZUGPWHWDHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-pyranylcarboxylic acid 、 二苯基膦叠氮化物 在 三乙胺 、 苯甲醇 作用下， 以 1,4-二氧六环 、 盐酸 、 乙酸乙酯 为溶剂， 以40%的产率得到N-benzyloxycarbonyl-4-aminopyran
  参考文献：
  名称：

  N.sup.6 mono heterocyclic substituted adenosine derivatives

  摘要：

  一种替代N.sup.6-氧杂、硫杂、硫氧杂和氮杂环烷基取代腺苷衍生物，以及一种将该组合物用作A.sub.1心脏腺苷受体的方法。

  公开号：

  US05789416A1

文献信息

• 3- Or 4-monosubstituted phenol derivatives useful as H3 ligands
  申请人：Warner-Lambert Company LLC

  公开号：EP1593679A1

  公开（公告）日：2005-11-09

  The invention relates to 3- or 4-monosubstituted phenol derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

  这项发明涉及3-或4-单取代酚衍生物，以及用于制备、制备中间体、含有和使用这些衍生物的过程。所述的3-或4-单取代酚衍生物是H3配体，在许多疾病、紊乱和状况中非常有用，特别是炎症性、过敏性和呼吸系统疾病、紊乱和状况。
• [EN] NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS UTILISÉS COMME INHIBITEURS DE LA KINASE RÉARRANGÉE AU COURS DE LA TRANSFECTION (RET)
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2016037578A1

  公开（公告）日：2016-03-17

  This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.

  这项发明涉及一种新型化合物，这些化合物是重排转位过程中的抑制剂（RET）激酶，包含它们的药物组合物，它们的制备方法，以及它们在治疗中的使用，单独或结合使用，用于规范胃肠敏感性、蠕动和/或分泌以及/或腹部紊乱或疾病和/或与RET功能障碍相关的疾病或调节RET活性可能具有治疗益处的治疗，包括但不限于所有分类的肠易激综合征（IBS），包括以腹泻为主、以便秘为主或交替排便模式、功能性腹胀、功能性便秘、功能性腹泻、未特指的功能性肠道障碍、功能性腹痛综合征、慢性特发性便秘、功能性食管障碍、功能性胃十二指肠障碍、功能性肛门疼痛、炎症性肠病、非小细胞肺癌、肝细胞癌、结肠癌、髓样甲状腺癌、滤泡性甲状腺癌、间变性甲状腺癌、乳头状甲状腺癌、脑肿瘤、腹腔癌、实体肿瘤、其他肺癌、头颈癌、神经胶质瘤、神经母细胞瘤、冯·希普-林道氏综合征和肾肿瘤、乳腺癌、输卵管癌、卵巢癌、移行细胞癌、前列腺癌、食管和食管胃交界处癌症、胆道癌、腺癌，以及任何具有增加RET激酶活性的恶性肿瘤。
• [EN] (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS<br/>[FR] COMPOSÉS (HÉTÉRO)ARYLE CYCLOPROPYLAMINES EN TANT QU'INHIBITEURS DE LSD1
  申请人：ORYZON GENOMICS SA

  公开号：WO2013057320A1

  公开（公告）日：2013-04-25

  The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

  本发明涉及（杂）芳基环丙胺化合物，特别是如本文所述和定义的公式I的化合物，以及它们在治疗中的用途，例如，在治疗或预防癌症、神经疾病或状况、或病毒感染中的用途。
• [EN] COMPOUNDS AND COMPOSITIONS AS RAF KINASE INHIBITORS<br/>[FR] COMPOSÉS ET COMPOSITIONS COMME INHIBITEURS DE PROTÉINES KINASES
  申请人：NOVARTIS AG

  公开号：WO2016038582A1

  公开（公告）日：2016-03-17

  The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

  本发明提供了如下所述的化合物(I)和(II)，以及其盐，并且提供了这些化合物用于治疗与Raf激酶活性相关的疾病的治疗用途。该发明还提供了包含这些化合物的药物组合物，以及包含这些化合物和治疗协同剂的组合物。
• [EN] ORAL PEPTIDE INHIBITORS OF INTERLEUKIN-23 RECEPTOR AND THEIR USE TO TREAT INFLAMMATORY BOWEL DISEASES<br/>[FR] PEPTIDES INHIBITEURS PAR VOIE ORALE DU RÉCEPTEUR DE L'INTERLEUKINE-23 ET LEUR UTILISATION DANS LE TRAITEMENT DES MALADIES INFLAMMATOIRES DE L'INTESTIN
  申请人：PROTAGONIST THERAPEUTICS INC

  公开号：WO2016011208A1

  公开（公告）日：2016-01-21

  The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel disease. In a first aspect, the present invention provides a peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (Xa). In another aspect, the present invention includes a pharmaceutical composition comprising a peptide inhibitor or a peptide dimer inhibitor of the present invention, and a pharmaceutically acceptable carrier.

  本发明提供了新型的干扰素-23受体肽抑制剂，以及相关的组合物和使用这些肽抑制剂来治疗或预防各种疾病和疾病的方法，包括炎症性肠病。在第一个方面，本发明提供了一种干扰素-23受体的肽抑制剂，或其药用盐或溶剂，其中该肽抑制剂包括式（Xa）的氨基酸序列。在另一个方面，本发明包括一种包含本发明的肽抑制剂或肽二聚体抑制剂的药物组合物，以及药用载体。