omega-Formyl histamine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: omega-Formyl histamine
• 英文别名: 2-amino-3-(1H-imidazol-5-yl)propanal
• 化学式: C₆H₉N₃O
• mdl: MFCD19213922
• 分子量: 139.16
• InChiKey: VYOIELONWKIZJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  71.8
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] AMINOPIPERIDINE AMIDES, DERIVATIVES, COMPOSITIONS, AND USES RELATED TO CXCR4 MODULATION<br/>[FR] AMIDES D'AMINOPIPÉRIDINE, DÉRIVÉS, COMPOSITIONS ET UTILISATIONS ASSOCIÉES À LA MODULATION DE CXCR4
  申请人：UNIV EMORY

  公开号：WO2021217143A1

  公开（公告）日：2021-10-28

  This disclosure relates to aminopiperidine amides, derivatives, pharmaceutical compositions, and uses related to CXCR4 modulation. In certain embodiments, the aminopiperidine amides are compounds having formula I, salts, derivatives, and prodrugs thereof wherein, R1, R2, and R3 are further defined herein. In certain embodiments, this disclosure contemplates pharmaceutical compositions comprising compounds disclosed herein. In certain embodiments, this disclosure relates to methods of treating or preventing CXCR4 related diseases or conditions by administering an effective amount of a compound disclosed herein to a subject in need thereof.

  本公开涉及氨基哌啶酰胺、衍生物、制药组合物以及与CXCR4调节相关的用途。在某些实施例中，氨基哌啶酰胺是具有公式I，其盐、衍生物和前药的化合物，其中，R1、R2和R3在此进一步定义。在某些实施例中，本公开考虑了包含所述化合物的制药组合物。在某些实施例中，本公开涉及通过向需要治疗或预防与CXCR4相关的疾病或病况的受试者投与所述化合物的有效量来治疗或预防CXCR4相关疾病或病况的方法。
• COMPOSITIONS IN THE FORM OF AN INJECTABLE AQUEOUS SOLUTION COMPRISING AMYLIN AN AMYLIN RECEPTOR AGONIST OR AN AMYLIN ANALOG, AT LEAST ONE IONIC SPECIES AND AN AMPHOIPHILIC COMPOUNDS CONTAINING HYDRIPHOBIC RADICALS
  申请人：ADOCIA

  公开号：US20210244796A1

  公开（公告）日：2021-08-12

  A composition in the form of an injectable solution includes: amylin, an amylin receptor agonist or an amylin analog; at least one ionic species; and an amphiphilic compound having a hydrophilic skeleton HB, substituted by at least one hydrophobic radical -Hy according to formula (I). A composition further is characterised in that it also has prandial insulin. In one embodiment, the composition also has GLP-1, GLP-1 analogs, and GLP-1 receptor agonists, commonly called GLP-1 RA.

  一种以注射溶液形式的组合物包括：淀粉样蛋白，淀粉样蛋白受体激动剂或淀粉样蛋白类似物；至少一种离子物种；以及具有按照公式（I）的至少一个疏水基团-Hy取代的亲水骨架HB的两性分子化合物。一种组合物还特征在于它还含有餐后胰岛素。在一种实施例中，该组合物还含有GLP-1、GLP-1类似物和GLP-1受体激动剂，通常称为GLP-1RA。
• PH-SENSITIVE POLYMERIC MICELLES FOR DRUG DELIVERY
  申请人：Bae You Han

  公开号：US20090274753A1

  公开（公告）日：2009-11-05

  Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.

  含有聚(L-组氨酸)-聚乙二醇嵌段共聚物和聚(L-乳酸)-聚乙二醇嵌段共聚物的混合胶束是一种pH敏感的药物载体，可以在酸性微环境中释放药物，但不会在血液中释放。由于实体肿瘤的微环境是酸性的，这些混合胶束对于治疗癌症，包括那些表现出多药耐药的癌症，非常有用。针对性配体，例如叶酸，也可以附加到混合胶束上，以增强药物输送到细胞内的效果。公开了使用这种药物治疗恒温动物的方法。
• Histidinol dehydrogenase protein, DNA and muteins and transgenic plants thereof
  申请人：CIBA-GEIGY AG

  公开号：EP0478502A2

  公开（公告）日：1992-04-01

  The present invention comprises cDNA coding for histidinol dehydrogenase from plants, the final step in histidine biosynthesis. The invention also comprises a novel method of purifying histidinol dehydrogenase from plants to essential honogeneity, the purified histidinol dehydrogenase, an assay for identifying inhibitors of histidinol dehydrogenase, an assay to identify mutants of histidinol dehydrogenase that are not inhibited by inhibitors of wild-type histidinol dehydrogenase, the inhibitors so identified as well as herbicide compositions containing them, the non-inhibited mutants of histidinol dehydrogenase, transgenic crop plants containing the non-inhibited mutants of histidinol dehydrogenase, and methods of treating weeds utilizing the application of histidinol dehydrogenase inhibitors to the transgenic crops containing the non-inhibited mutants of histidinol dehydrogenase.

  本发明包括植物组氨醇脱氢酶的 cDNA 编码，这是组氨酸生物合成的最后一步。本发明还包括一种从植物中纯化组氨醇脱氢酶至基本纯度的新方法、纯化的组氨醇脱氢酶、鉴定组氨醇脱氢酶抑制剂的检测方法、鉴定不受野生型组氨醇脱氢酶抑制剂抑制的组氨醇脱氢酶突变体的检测方法、组氨醇脱氢酶的非抑制突变体、含有组氨醇脱氢酶非抑制突变体的转基因作物植株，以及利用向含有组氨醇脱氢酶非抑制突变体的转基因作物施用组氨醇脱氢酶抑制剂来处理杂草的方法。
• MIXTURE OF CARBOXYLIC ACIDS FOR TREATING PATIENTS WITH KIDNEY FAILURE
  申请人：Hernández Miramontes, Jorge Antonio

  公开号：EP3219315A1

  公开（公告）日：2017-09-20

  Currently the treatment for patients with end-stage renal disease (stage V) consists of renal replacement therapy (hemodialysis, peritoneal dialysis or renal transplantation), extraordinarily expensive entailing poor quality of life. Our invention is a mixture of carboxylic acids: citric acid, succinic acid, fumaric acid and malic acid, and any possible combinations thereof. This product is preferably used orally or also intravenously, in the treatment of patients with chronic renal failure, hyperammonemia or human conditions having negative nitrogen balance. This product is beneficial in decreasing the serum values of urea and serum ammonium, while promoting by transamination of the oxalacetate formed via succinate, fumarate and malate, the biosynthesis of non-essential amino acids; by transamination of the alpha ketoglutarate formed via citrate, it generates glutamic acid and related amino acids such as glutamine. This treatment prevents, preserves and even improves kidney function. In other patients it delays deterioration of renal function and the urgent need for renal replacement therapy. In others, it is used as a supplemental renal replacement treatment to improve the patient's quality of life and improve laboratory parameters.

  目前，对终末期肾病（第五期）患者的治疗包括肾脏替代疗法（血液透析、腹膜透析或肾移植），费用极其昂贵，生活质量低下。我们的发明是一种羧酸混合物：柠檬酸、琥珀酸、富马酸和苹果酸及其任何可能的组合。本品最好口服或静脉注射，用于治疗慢性肾功能衰竭、高氨血症或负氮平衡患者。本品有利于降低尿素和血清氨的血清值，同时通过琥珀酸、富马酸和苹果酸形成的草酰乙酸的转氨基作用，促进非必需氨基酸的生物合成；通过柠檬酸形成的α-酮戊二酸的转氨基作用，生成谷氨酸和相关氨基酸，如谷氨酰胺。这种疗法可以预防、保护甚至改善肾功能。在其他患者中，它可以延缓肾功能恶化和对肾脏替代疗法的迫切需要。在其他患者中，它被用作肾替代治疗的补充，以改善患者的生活质量和实验室指标。