1-Methyl-1,2-dihydropyridin-1-ium-3-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-Methyl-1,2-dihydropyridin-1-ium-3-carboxylate
• 英文别名: 1-methyl-1,2-dihydropyridin-1-ium-3-carboxylate
• 化学式: C7H9NO2
• mdl: MFCD19230658
• 分子量: 139.15
• InChiKey: YCABHAGDPZAUBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  烟酸 、 碘甲烷 、 1-Methyl-1,2-dihydropyridin-1-ium-3-carboxylate 在 water ethanol 作用下， 以 乙醇 为溶剂， 生成 3-Carboxy-1-methylpyridiniumiodid
  参考文献：
  名称：

  METHODS AND COMPOSITIONS FOR DIABETES TREATMENT AND PREVENTION

  摘要：

  本发明涉及用于预防或治疗糖尿病的方法和组合物。该发明特别公开了根据式(I)的化合物，用于预防和治疗II型或I型糖尿病。

  公开号：

  US20110288014A1

文献信息

• Use of Quaternary Pyridinium Compounds for Vasoprotection and/or Hepatoprotection
  申请人：MARCINEK Andrzej

  公开号：US20080221172A1

  公开（公告）日：2008-09-11

  The invention relates to a method for the treatment or prevention of diseases or conditions associated with vascular endothelium dysfunction or liver injury comprising the administration to a patient in a need of such treatment or prevention of a therapeutically or prophylactically effective amount of a compound selected from the group consisting of: wherein R represents hydrogen atom, CH 3 , OH, pyridyl (C 5 H 4 N), 1-methylpyridyl (C 5 H 4 N—CH 3 ) or pyridyl substituted with hydroxy group ((OH)C 5 H 3 N), and X represents a physiologically acceptable counterion.

  该发明涉及一种治疗或预防与血管内皮功能障碍或肝损伤相关的疾病或病况的方法，包括向需要此类治疗或预防的患者施用所述治疗或预防有效量的化合物，所述化合物选自以下组合：其中R代表氢原子、CH3、OH、吡啶基（C5H4N）、1-甲基吡啶基（ - ）或带有羟基取代的吡啶基（（OH）C5H3N），X代表生理上可接受的对离子。
• Novel Drugs for Dementia
  申请人：Ternansky Robert

  公开号：US20080227806A1

  公开（公告）日：2008-09-18

  The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.

  本发明涉及一种含有化学递送系统（CDS）基团和半胱氨酸蛋白酶抑制剂基团的前药化合物。CDS基团将前药定位于大脑或中枢神经系统。半胱氨酸蛋白酶抑制剂在从前药中释放后抑制半胱氨酸蛋白酶。半胱氨酸蛋白酶抑制剂对治疗痴呆症、阿尔茨海默病和血管性痴呆症有效。定位于大脑或中枢神经系统在治疗这些疾病和症状方面具有显著的优势。首选的CDS前药是将二氢三角线CDS基团与环氧丙酰肽半胱氨酸蛋白酶抑制剂基团耦合。
• COMPOSITIONS AND METHODS FOR TREATING BETA-AMYLOID RELATED DISEASES
  申请人：TERNANSKY Robert J.

  公开号：US20110105603A1

  公开（公告）日：2011-05-05

  In alternative embodiments the invention provides compositions and methods for ameliorating diseases and conditions having a beta-amyloid component, including Alzheimer's disease (AD), Vascular Dementia (VD), dementia, pre-dementia, Cognitive Dysfunction Syndrome (CDS) and loss of cognition in humans and in non-human animal. In alternative embodiment the invention provides analogs of AB-007 and its acid form E64c (loxistatin), their preparation, and pharmaceutical compositions thereof and methods of making and using same. In alternative embodiments compositions of the invention are deuterated analogs of AB-007 (or E64d) and E64c (or loxistatin). In alternative embodiments compositions of the invention are metabolically blocked forms as compared to AB-007 and loxistatin. In alternative embodiments compositions of the invention are used to ameliorate (including treat, slow, reverse or prevent) a disease or condition which can be ameliorated by partial or complete inhibition of a cysteine protease, e.g., AD, VD, CDS. The invention also provides alternative dosage forms and formulations for AB-007 and loxistatin, and for compounds of this invention, which can be used e.g., to treat AD, VD and CDS, in humans and in non-human animals.

  在另一种实施方案中，本发明提供了用于改善具有β-淀粉样成分的疾病和病况的组合物和方法，包括阿尔茨海默病（AD），血管性痴呆（VD），痴呆，前痴呆，认知功能障碍综合征（CDS）和人类和非人类动物的认知丧失。在另一种实施方案中，本发明提供了AB-007的类似物及其酸性形式E64c（loxistatin），它们的制备，以及其制备和使用的药物组合物和方法。在另一种实施方案中，本发明的组合物是AB-007（或E64d）和E64c（或loxistatin）的氘代类似物。在另一种实施方案中，本发明的组合物是与AB-007和loxistatin相比代谢阻滞的形式。在另一种实施方案中，本发明的组合物用于改善（包括治疗，减缓，逆转或预防）可以通过部分或完全抑制半胱氨酸蛋白酶（例如AD，VD，CDS）改善的疾病或病况。本发明还提供了AB-007和loxistatin的另一种剂型和配方，以及本发明化合物的剂型和配方，可用于治疗人类和非人类动物的AD，VD和CDS等疾病和病况。
• Brain-specific drug delivery
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0221588A2

  公开（公告）日：1987-05-13

  The invention provides compounds adapted for the site-specific/sustained delivery of a centrally acting drug species to the brain having the formula [D-DHC] and the non-toxic pharmaceutically acceptable salts thereof, wherein [D] is a centrally acting drug species which is an antiviral agent, an antiinflammatory steroid, a narcotic or an estrogen and which contains at least two reactive hydroxyl functional groups, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine=pyridinium salt redox carrier comprising at least one dihydropyridine ring system of the formula wherein R is lower alkyl or benzyl and the dotted line indicates the presence of a double bond in either the 2 or 3 position of the dihydropyridine ring, a ring carbon atom of each dihydropyridine ring system being connected via a bridging group to a reactive hydroxyl functional group in the centrally acting drug species. The corresponding quaternary derivatives are also described.

  本发明提供了适用于向大脑定点/持续递送中枢作用药物的化合物，其具有式[D-DHC]及其无毒的药学上可接受的盐，其中[D]是中枢作用药物，它是一种抗病毒剂、一种抗炎类固醇、一种麻醉剂或一种雌激素，并含有至少两个活性羟基官能团，而[DHC]是还原的、可生物氧化的、可透过血脑屏障的脂质形式的二氢吡咯、DHC]是二氢吡啶=吡啶鎓盐氧化还原载体的还原型、可生物氧化、可穿透血脑屏障的类脂形式，该载体包含至少一个式中的二氢吡啶环系统。 其中 R 为低级烷基或苄基，虚线表示在二氢吡啶环的 2 位或 3 位存在双键，每个二氢吡啶环系统的环碳原子通过桥基与中心作用药物种类中的活性羟基官能团相连。还描述了相应的季衍生物。
• FOOD COMPOSITION COMPRISING MAGNESIUM METAL PARTICLES
  申请人：Miljkovic, Dusan

  公开号：EP2896302A2

  公开（公告）日：2015-07-22

  The invention relates to food compositions comprising a plurality of zero-valent, non-ionic, and non-oxidized magnesium metal particles and a food substance. The food compositions may further comprise a carrier, and wherein the magnesium metal particles are comingled with the carrier.

  本发明涉及由多种零价、非离子、非氧化金属镁颗粒和食品物质组成的食品组合物。食品组合物还可进一步包含载体，其中金属镁颗粒与载体混合。