N-4-哌啶基甘氨酸 | 782494-21-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: N-4-哌啶基甘氨酸
• 英文名称: N-4-Piperidinyl-glycine
• 英文别名: 2-(piperidin-4-ylamino)acetic acid
• CAS: 782494-21-7
• 化学式: C₇H₁₄N₂O₂
• mdl: MFCD10565767
• 分子量: 158.2
• InChiKey: GMYSPKJLZSKGSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.8
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.857
• 拓扑面积：
  61.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
  申请人：Goble D. Stephen

  公开号：US20070238723A1

  公开（公告）日：2007-10-11

  Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

  环戊基化合物通过酰胺基团与苯并噁唑基团相连，利用苯并噁唑环的环氮原子，并进一步用杂环基团取代，这些化合物由式I表示： 用于调节CCR-2趋化因子受体，以预防或治疗炎症和免疫调节性疾病和疾病，过敏性疾病，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及类风湿性关节炎和动脉粥样硬化等自身免疫病理病变；以及包含这些化合物的药物组合物和这些化合物和组合物的使用。
• Inhibitors of the blood-clotting factor xa, production thereof and use of the same
  申请人：Sturzebecher Jorg

  公开号：US20050119190A1

  公开（公告）日：2005-06-02

  The invention relates to novel inhibitors of clotting factor Xa, the preparation and use thereof for therapy, prophylaxis and diagnosis of cardiovascular disorders and thromboembolic events.

  本发明涉及一种新型凝血因子Xa抑制剂，其制备和用途用于治疗、预防和诊断心血管疾病和血栓栓塞事件。
• Serine protease inhibitors
  申请人：Lively Elizabeth Sarah

  公开号：US20050267173A1

  公开（公告）日：2005-12-01

  Compounds of formula (I) where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.

  式(I)的化合物，其中R5，R6a，每个X，L，Cy和Lp的定义如规范所述，是一种抑制组胺酶的试剂，可用作抗炎剂。
• Synthesis of enantiomerically enriched 4-piperidinylglycine
  申请人：——

  公开号：US20020133014A1

  公开（公告）日：2002-09-19

  A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I), 1 said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X − is an anion wherein X is independently a halogen; and “*” designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.

  一种制备对映富集的4-哌啶基甘氨酸(I)的方法，该方法包括(a)将N-保护的甘氨酸酯与4-哌酮结合形成双脱水氨基酸酯；(b)在(R,R)-BPE-Rh、(S,S)-BPE-Rh、(R,R)-DuPHOS-Rh、(S,S)-DuPHOS-Rh或其组合物中选择一个铑催化剂，在氢气存在下还原双脱水氨基酸酯，形成保护化合物；(c)从保护化合物中去除保护基，从而形成式(I)的4-哌啶基甘氨酸，其中X-是一个阴离子，其中X独立地是卤素；“*”表示具有(R)-或(S)-构型的不对称碳。该发明的方法产生对映富集的(R)-4-哌啶基甘氨酸或(S)-4-哌啶基甘氨酸。
• APELIN POLYPEPTIDES
  申请人：Amgen, Inc

  公开号：EP3674314A2

  公开（公告）日：2020-07-01

  The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.

  本发明提供了相对于原生凋亡素-13 多肽具有更高的稳定性、循环半衰期和/或效力的修饰凋亡素多肽。本发明还公开了包含经修饰的凋亡磷多肽的组合物以及使用该多肽治疗心脏疾病（如心力衰竭）的方法。