tert-butyl 4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine-1-carboxylate | 206989-63-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: tert-butyl 4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine-1-carboxylate
• 英文别名: 4-(5,6,7,8-Tetrahydro-[1,8]naphthyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester；4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine-1-carboxylic acid t-butyl ester
• CAS: 206989-63-1
• 化学式: C₁₈H₂₇N₃O₂
• 分子量: 317.431
• InChiKey: ZVYMXHCYHZCTNG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine-1-carboxylate 在 乙醚 作用下， 以 二氯甲烷 、 ester 、 三氟乙酸 为溶剂， 反应 4.0h， 以to yield 4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine solid的产率得到7-(piperidin-4-yl)-1,2,3,4-tetrahydro-1,8-naphthyridine
  参考文献：
  名称：

  Molecular Crystal of (4-(1,8-Naphthyridin-2-YL)Piperidin-1-YL)Pyrimidine Derivative

  摘要：

  （S）-3-（2,5-二甲基-6-（4-（5,6,7,8-四氢-1,8-萘啶-2-基）哌啶-1-基）嘧啶-4-基氨基）-2-（4-甲氧基苯磺酰胺基）丙酸的分子晶体形式，具有X射线粉末衍射（“XRPD”）谱峰，2θ角度为7.44、14.80、16.64和23.04±0.2°。该分子晶体可以制成药物组合物，用于治疗或控制由病理性血管生成引起的疾病。

  公开号：

  US20110237605A1
• 作为产物：
  描述：

  4-乙酰基哌啶-1-甲酸叔丁酯 在 palladium 10% on activated carbon 、 氢气 、 L-脯氨酸 作用下， 以 乙醇 为溶剂， 生成 tert-butyl 4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidine-1-carboxylate
  参考文献：
  名称：

  INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN

  摘要：

  揭示了αvβ6整合素的小分子抑制剂，以及使用它们治疗多种疾病和症状的方法。

  公开号：

  US20180244648A1

文献信息

• Naphthyridine derivatives, processes for their preparation, their use, and pharmaceutical compositions comprising them
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1065207A1

  公开（公告）日：2001-01-03

  The present invention relates to compounds of the formula I, in which B, G, Z, X, Y, r, s and t have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及公式I的化合物， 其中B、G、Z、X、Y、r、s和t具有索引中指示的含义，它们的生理耐受盐和前药。公式I的化合物是有价值的药理活性化合物。它们是维脱蛋白受体拮抗剂和细胞粘附抑制剂，适用于基于维脱蛋白受体与其配体在细胞-细胞或细胞-基质相互作用过程中的相互作用而导致的疾病的治疗和预防，或者可以通过影响这种相互作用来预防、缓解或治愈。例如，它们可用于通过抑制破骨细胞来抑制骨吸收，从而治疗和预防骨质疏松症，或者用于抑制不良血管生成或血管平滑肌细胞增殖。此外，本发明还涉及公式I化合物的制备方法，它们的用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。
• Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them
  申请人：Aventis Pharma Deutschland GmbH

  公开号：US20040198718A1

  公开（公告）日：2004-10-07

  Naphthyridine compounds of the formula 1 wherein the substituents are defined as in the specification which are vitronectin receptor antagonists and inhibitors of cell adhesion useful for treatment of illnesses based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-materix interaction processes. The compounds are particularly useful for inhibiting bone resorption by osteoclasts and are useful for treating osteoporosis.

  化学式为1的萘啉化合物，其中取代基如规范中所定义，是维特隆连接受体拮抗剂和细胞粘附抑制剂，用于治疗基于细胞-细胞或细胞-基质相互作用过程中维特隆连接受体和其配体相互作用的疾病。这些化合物特别适用于抑制骨吸收细胞破骨细胞并用于治疗骨质疏松症。
• Pyrimidinonesulfamoylureas`
  申请人：——

  公开号：US20030171368A1

  公开（公告）日：2003-09-11

  The disclosure is directed to compounds of the formula (I) 1 wherein the radicals have the meanings described in the disclosure, to the preparation of the compounds and to the use of the compounds to find the integrin receptors.

  本公开涉及式(I)1的化合物，其中基团具有公开说明中所描述的含义，以及制备该化合物和使用该化合物寻找整合素受体的方法。
• Integrin receptor antagonists
  申请人：Merck & Co., Inc.

  公开号：US06358970B1

  公开（公告）日：2002-03-19

  The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

  本发明涉及化合物及其衍生物、它们的合成以及它们作为整合素受体拮抗剂的用途。更具体地说，本发明的化合物是整合素受体αvβ3和/或αvβ5的拮抗剂，可用于抑制骨吸收、治疗和预防骨质疏松症，并抑制血管再狭窄、糖尿病视网膜病变、黄斑变性、血管生成、动脉粥样硬化、炎症、炎性关节炎、病毒性疾病、癌症和转移性肿瘤生长。
• Integrin antagonists
  申请人：Merck & Co., Inc.

  公开号：US05952341A1

  公开（公告）日：1999-09-14

  This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.

  本发明涉及某些新型化合物及其衍生物、它们的合成以及它们作为玻璃蛋白受体拮抗剂的用途。本发明中的玻璃蛋白受体拮抗剂化合物是αvβ3拮抗剂、αvβ5拮抗剂或双重αvβ3/αvβ5拮抗剂，用于抑制骨吸收、治疗和预防骨质疏松症、抑制再狭窄、糖尿病视网膜病变、黄斑变性、血管生成、动脉粥样硬化、炎症和肿瘤生长。