(2R,3R)-3-[[(2S)-1-[4-(diaminomethylideneazaniumyl)butylamino]-4-methyl-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylate

• 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: (2R,3R)-3-[[(2S)-1-[4-(diaminomethylideneazaniumyl)butylamino]-4-methyl-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylate
• 化学式: C15H27N5O5
• 分子量: 357.41
• InChiKey: LTLYEAJONXGNFG-HBNTYKKESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  25
• 可旋转键数：
  11
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  172
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• [EN] CATHEPSIN INHIBITORS<br/>[FR] INHIBITEURS DE LA CATHEPSINE
  申请人：ACADEMISCH ZIEKENHUIS LEIDEN

  公开号：WO2019112426A1

  公开（公告）日：2019-06-13

  This invention relates to compounds that are useful as inhibitors, in particular as inhibitors of Cathepsin K (CatK), and to a method of inhibiting cathepsin activity, comprising administering a compound or formulation comprising a compound according to the invention.

  这项发明涉及一种作为抑制剂有用的化合物，特别是作为Cathepsin K（CatK）的抑制剂，并涉及一种抑制蛋白酶活性的方法，包括给予根据该发明的化合物或配方的化合物。
• SUBSTITUTED 2,4 DIAMINO-QUINOLINE AS NEW MEDICAMENT FOR FIBROSIS, AUTOPHAGY AND CATHEPSINS B (CTSB), L (CTSL) AND D (CTSD) RELATED DISEASES
  申请人：Genoscience Pharma SAS

  公开号：EP3620164A1

  公开（公告）日：2020-03-11

  The present invention relates to novel 2-primary amino-4-secondary amino-quinoline derivatives, their manufacture, pharmaceutical compositions comprising them and their use as medicaments. The active compounds of the present invention can be useful as a medicament in the treatment and/or the decreasing and/or the prevention of fibrosis and/or fibrosis related diseases, or for use as a medicament in the treatment and/or the decreasing and/or the prevention of the autophagy and/or autophagy related diseases and for the inhibition of the autophagy flux, or for use in the inhibition of cathepsins B (CTSB), L (CTSL) and/or D (CTSD) and/or cathepsins B (CTSB), L (CTSL) and/or D (CTSD) related diseases; with the proviso that said compounds are not to be used for the treatment of any forms of cancers.

  本发明涉及新型2-初级氨基-4-次级氨基喹啉衍生物，其制备方法，包含它们的药物组合物以及它们作为药物的用途。本发明的活性化合物可用作药物治疗和/或减少和/或预防纤维化和/或与纤维化相关疾病，或用作药物治疗和/或减少和/或预防自噬和/或与自噬相关疾病以及抑制自噬通量，或用于抑制蛋白酶B（CTSB）、L（CTSL）和/或D（CTSD）和/或与蛋白酶B（CTSB）、L（CTSL）和/或D（CTSD）相关疾病；但所述化合物不得用于治疗任何形式的癌症。
• Mild Chemically Cleavable Linker System
  申请人：Bogyo Matthew S.

  公开号：US20100003735A1

  公开（公告）日：2010-01-07

  A linker system is provided where a small molecule reactive group, e.g., an activity based probe which binds to certain enzymes at the active site, is linked through an aryl diazo linker to an affinity molecule such as biotin. The reactive group may comprise a number of functionalities known to react with a specific target to be studied. This enables the probe to be exposed to analytes, such as proteins and bind specifically to them to form a complex having an affinity molecule allowing immobilization of the bound analyte on an affinity column or other support, e.g. with streptavidin. Then, the linker is cleaved without causing removal of the affinity group or dissociation of the probe from the analyte. The linker is cleaved under mild reducing conditions, e.g., dithionite. The probe is synthesized along with the linker on a solid support.

  提供了一个连接系统，其中一个小分子的反应基团，例如一个能够结合到某些酶的活性基团，通过芳基重氮连接物连接到一种亲和分子，比如生物素。这个反应基团可能包括一些已知能与特定目标反应的官能团。这使得探针能够暴露给待测物，比如蛋白质，并特异性地与它们结合形成一个具有亲和分子的复合物，从而使结合的待测物能够固定在亲和柱或其他支持物上，例如与链球菌素结合。然后，在不导致亲和基团脱落或探针与待测物解离的情况下，断裂连接物。连接物在温和还原条件下被断裂，例如二亚硫酸盐。探针与连接物一起在固体支持物上合成。
• Method For Improved Bioactivation Of Pharmaceuticals
  申请人：Clement Bernd

  公开号：US20120077876A1

  公开（公告）日：2012-03-29

  This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R 1 and R 2 are hydrogen, alkyl, or aryl radicals.

  这项发明涉及一种前药，其包含具有一般式(I)或(II)的部分结构，其中R1和R2为氢、烷基或芳基基团。
• Methods of treating, inhibiting and/or preventing an auditory impairment
  申请人：The Department of Veterans Affairs

  公开号：US10124062B2

  公开（公告）日：2018-11-13

  The present invention provides methods of treating an auditory impairment associated with outer hair cells of the cochlea in a subject. The method may comprise administering to said subject an effective amount of a composition comprising, as an active agent, an oligonucleotide sequence having a portion of a mammalian telomere sequence so as to reduce the auditory impairment thereby treating the auditory impairment in the subject.

  本发明提供了治疗与受试者耳蜗外毛细胞相关的听觉损伤的方法。该方法可包括向所述受试者施用有效量的组合物，该组合物作为活性剂包含具有哺乳动物端粒序列部分的寡核苷酸序列，以减少听觉损伤，从而治疗受试者的听觉损伤。