phenylalanylalanine | 3918-86-3

• 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
• 英文名称: phenylalanylalanine
• 英文别名: Phe-Ala；Ala-Phe；(Phenylalanyl)-alanin；N-phenylalanyl-alanine；Inaktives Phenylalanyl-alanin；N-Phenylalanyl-alanin；Inakt. Phenylalanyl-alanin；2-[(2-Ammonio-3-phenylpropanoyl)amino]propanoate；2-[(2-azaniumyl-3-phenylpropanoyl)amino]propanoate
• CAS: 3918-86-3
• 化学式: C₁₂H₁₆N₂O₃
• 分子量: 236.271
• InChiKey: MIDZLCFIAINOQN-UHFFFAOYSA-N

物化性质

• 沸点：
  506.0±50.0 °C(Predicted)
• 密度：
  1.222±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  phenylalanylalanine 在 水 作用下， 生成 环(丙氨酸-苯丙氨酸)二肽
  参考文献：
  名称：

  One-Year Follow-Up of Medication Management Capacity in Highly Functioning Older Adults

  摘要：

  Background, We tested the hypothesis that impairment in the ability to take medication independently predicts early functional decline.Methods. A 12-month, prospective cohort study was performed at two continuing-care retirement facilities using the Drug Regimen Unassisted Grading Scale (DRUGS). This geriatric screening tool utilizes a stepwise progression of four tasks: (i) identification, (ii) access, (iii) dosage, and (iv) timing.Results, Forty-seven (86%) of the eligible participants completed the 12-month follow-up assessment; three were transferred to skilled nursing facilities. The mean age at study entry was 84.2 i: 5.1 years; 72% of the participants were women, and 68% were college educated. At 12 months there was a decline in the Mini-Mental State Examination (MMSE) score(p = .029), an increase in the timed "Up and Go" test(p = .023), and a decline in the DRUGS score (p = .029). Nine (18%) of the participants resided in assisted- versus independent-living situations compared with three par participants (5%) at study entry (p = .031). Both 12-month DRUGS score and 12-month self-reported medication manage ment capacity were associated with 12-month MMSE (p = .0001 and p = .019, respectively). Baseline DRUGS score was associated with 12-month MMSE and Geriatric Depression Scale scores (p = .0002 and p = .002, respectively). Both baseline DRUGS score and self-reported medication management capacity were also associated with residence in assisted-living communities at 6 months (p = .029 and p = .040, respectively). MMSE was not associated with any of the clinical outcomes.Conclusions. The DRUGS tool may predict functional decline in highly functioning older adults.

  DOI：

  10.1093/gerona/55.10.m550
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 氨 作用下， 生成 phenylalanylalanine
  参考文献：
  名称：

  Fischer,E.; Blank, Justus Liebigs Annalen der Chemie, 1907, vol. 354, p. 4

  摘要：

  DOI：

文献信息

• [EN] NON-LINEAR SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF<br/>[FR] LIEURS AUTO-IMMOLABLES NON LINÉAIRES ET CONJUGUÉS DE CEUX-CI
  申请人：SYNTHON BIOPHARMACEUTICALS BV

  公开号：WO2018069375A1

  公开（公告）日：2018-04-19

  The present invention relates to linker-drug compounds (LDs) and antibody-drug conjugates (ADCs) comprising a non-linear self-immolative linker, which is cleavable or transformable under appropriate conditions and which reduces the hydrophobicity of the antibody-drug conjugate.

  本发明涉及连接子-药物化合物（LDs）和抗体-药物偶联物（ADCs），包括一个非线性自消除连接子，该连接子在适当条件下可被裂解或转化，并减少了抗体-药物偶联物的疏水性。
• Prodrug derivatives of acids using alcohols with homotopic hydroxy groups and methods for their preparation and use
  申请人：deLong A. Mitchell

  公开号：US20070254920A1

  公开（公告）日：2007-11-01

  This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and R b is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.

  这项发明涉及新型同位素前药、药物以及其制备、测试和使用方法。在一个实施例中，同位素前药具有一般公式 其中 是包含羧酸官能团的生物活性基团，而 R b 是通过羧酸官能团与生物活性基团形成酯键的同位对称醇，以及其光学异构体、对映异构体、药用可接受盐、生物水解酰胺、酯、亚酰胺及其组合物。
• Modulators of serotonin receptors
  申请人：Wacker A. Dean

  公开号：US20050080074A1

  公开（公告）日：2005-04-14

  The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.

  本发明提供了血清素受体调节剂，包含这些调节剂的药物组合物以及治疗与血清素受体调节相关的各种疾病、症状和疾患的方法，例如：代谢性疾病，包括但不限于肥胖、糖尿病、糖尿病并发症、动脉粥样硬化、糖耐量受损和血脂异常；中枢神经系统疾病，包括但不限于焦虑、抑郁、强迫症、恐慌症、精神病、精神分裂症、睡眠障碍、性功能障碍和社交恐惧症；头痛；偏头痛；以及使用这些化合物和组合物治疗胃肠道疾病。
• Bismuth-containing compounds, coordination polymers, methods for modulating pharmacokinetic properties of biologically active agents, and methods for treating patients
  申请人：Price John D.

  公开号：US10150792B2

  公开（公告）日：2018-12-11

  Bismuth-containing compounds include bismuth and a biologically active agent coordinated to the bismuth. The biologically active agent includes at least one heteroatom configured for coordination with the bismuth. Coordination polymers include a polymer matrix that contains a bismuth-containing compound. Methods for modulating a pharmacokinetic property of a biologically active agent include coordinating the biologically active agent to bismuth to form a bismuth-containing compound, and administering the bismuth-containing compound orally to a patient. Methods for treating Parkinson's disease, methods for treating hypothyroidism, methods for treating ulcerative colitis, and methods for treating cancer each include administering a bismuth-containing compound to a patient.

  含铋化合物包括铋和与铋配位的生物活性剂。生物活性剂包括至少一个用于与铋配位的杂原子。配位聚合物包括包含含铋化合物的聚合物基质。调节生物活性剂的药代动力学特性的方法包括将生物活性剂与铋配位形成含铋化合物，并将含铋化合物口服给患者。治疗帕金森病的方法，治疗甲状腺功能减退症的方法，治疗溃疡性结肠炎的方法，以及治疗癌症的方法各自包括向患者口服含铋化合物。
• Water-Soluble CC-1065 Analogs and Their Conjugates
  申请人：Beusker Patrick Henry

  公开号：US20090318668A1

  公开（公告）日：2009-12-24

  This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

  这项发明涉及DNA结合烷基化剂CC-1065的新型类似物及其结合物。此外，该发明涉及用于制备上述剂和它们的结合物的中间体。这些结合物设计为在一个或多个激活步骤之后以及/或由结合物控制的速率和时间跨度下释放它们的（多种）荷载，以便选择性地传递和/或可控地释放一个或多个所述的DNA烷基化剂。这些剂、结合物和中间体可用于治疗以不良（细胞）增殖为特征的疾病。例如，这项发明的剂和结合物可用于治疗肿瘤。