3-(3,4-Dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrate

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: 3-(3,4-Dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrate
• 英文别名: 3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid;hydrate
• 化学式: C10H16N2O5
• 分子量: 244.24
• InChiKey: QTAOMKOIBXZKND-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.88
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  117
• 氢给体数：
  6
• 氢受体数：
  7

文献信息

• Synergistic pharmaceutical compositions, their production and use
  申请人：CHINOIN Gyogyszer és Vegyészeti Termékek Gyára RT.

  公开号：EP0146363A2

  公开（公告）日：1985-06-26

  The invention relates to a synergistic pharmaceutical composition, which comprises as an active ingredient a combination of 1-phenylalanine and (-)-deprenyl [(-)-N-(1-phenylisopropyl)-N-methyl-N-propinylamine hydrochloride] and optionally carbidopa [3-(3,4-dihydroxyphenyl)-2-hydrazino-2--methyl-propionic acid monohydrate] or benzerazide [N-(DL--seryl)-N'-(2,3,4-trihydroxybenzyl)-hydrazinel in association with conventional inert, non-toxic solid or liquid pharmaceutical carriers. The invention further relates to the preparation of these compositions and to the use thereof for the treatment of depressive symptoms.

  本发明涉及一种增效药物组合物，其活性成分包括1-苯丙氨酸和(-)-癸烯基[(-)-N-(1-苯基异丙基)-N-甲基-N-丙胺盐酸盐]的组合，以及可选的卡比多巴[3-(3,4-二羟基苯基)-2-肼基-2-甲基丙酸一水合物]或苯泽拉嗪[N-(DL-丝氨酰)-N'-(2,3,4-三羟基苄基)-肼基]与常规惰性、无毒固体或液体药物载体的组合。 本发明还涉及这些组合物的制备及其用于治疗抑郁症状的用途。
• Process for the preparation of tablets or film-coated tablets
  申请人：EGIS GYOGYSZERGYAR

  公开号：EP0497331A2

  公开（公告）日：1992-08-05

  The subject-matter of the invention is a process for the preparation of tablets or film-coated tablets with increased active ingredient release, said tablets comprising as active ingredients a mixture of L-3,4-di-(hydroxy)-phenylalanine and L-alpha-(hydrazino)-alpha-(methyl)-3,4-di-(hydroxy)-phenyl propionic acid, by admixing any of L-3,4-di-(hydroxy)-phenylalanine and L-alpha-(hydrazino)-alpha-(methyl)-3,4-di(hydroxy)-phenyl propionic acid, or both of them, with hydrophilic diluents, and optionally with colouring agents, blending the mixture thus obtained with auxiliary agents conventionally used for the preparation of tablets and optionally with the other active ingredient, moreover with a solution of stearin in an organic solvent, optionally containing auxiliary agents conventionally used for the preparation of tablets, drying and granulating the mixture thus obtained, optionally admixing further auxiliary agents to the dry granulate, compressing it into tablets and, if desired, applying a film-coating onto the surface of the tablets thus obtained. The process according to the invention provides tablets of appropriate quality with rapid active ingredient release.

  本发明的主题是一种制备活性成分释放增加的片剂或薄膜包衣片剂的工艺，所述片剂包括作为活性成分的 L-3,4-二（羟基）-苯丙氨酸和 L-α-（肼基）-α-（甲基）-3、将 L-3,4-二（羟基）-苯丙氨酸和 L-α-（肼基）-α-（甲基）-3,4-二（羟基）-苯 丙酸中的任何一种或两种与亲水性稀释剂混合，并可选择与着色剂混合、将得到的混合物与制备片剂常用的辅助剂混合，也可与其他活性成分混合，还可与硬 脂素在有机溶剂中的溶液混合，其中可选择含有制备片剂常用的辅助剂，将得到 的混合物干燥并造粒，可选择在干燥的颗粒中进一步添加辅助剂，将其压制成片剂， 如果需要，还可在得到的片剂表面进行薄膜包衣。 根据本发明的工艺，片剂质量适当，有效成分释放迅速。
• [EN] ORAL DRUG DELIVERY DEVICE<br/>[FR] ADMINISTRATION DE MÉDICAMENT PAR VOIE ORALE<br/>[ZH] 一种口服给药递送装置
  申请人：SHANGHAI WD PHARMACEUTICAL CO LTD

  公开号：WO2020143843A1

  公开（公告）日：2020-07-16

  本发明公开了一种口服给药递送装置，其包括：一管状构件、一药物容置部件、一装置帽和一湍流产生部件，其中，所述管状构件具有两端开口及内腔，其一端开口为第一开口，另一端开口为第二开口，所述内腔连通所述第一开口和第二开口；所述湍流产生部件包含台阶结构或褶皱部结构，并设置于所述内腔中、介于所述第二开口和所述药物容置部件之间的位置；所述药物容置部件和装置帽的结构及其与管状构件的连接关系如本发明中所述。通过本发明的口服给药递送装置，可在正常的啜吸过程中产生湍流，提供含药物颗粒或多丸与可饮用的液体的充分混合；且该装置可伸缩，减小了尺寸，方便携带。
• COMPOSITIONS AND METHODS FOR PARKINSON'S DISEASE THERAPY
  申请人：Davies Daryl

  公开号：US20180271888A1

  公开（公告）日：2018-09-27

  This disclosure provides methods for the treatment of one or more of: Parkinson's disease (PD); PD symptoms; movement disorders; neurodegenerative diseases linked to changes in dopamine, dopamine signaling, or dopamine expression, in a subject in need thereof comprising administering to the subject an effective amount of an agent that potentiates dopaminergic neurotransmission. Also provided is a method for selecting a candidate agent for the treatment of Parkinson's disease (PD); PD symptoms; and neurodegenerative diseases linked to changes in dopamine, dopamine signaling, or dopamine expression.
• DOPA Formulations for Treatments of Parkinson's Disease
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：US20190054051A1

  公开（公告）日：2019-02-21

  The present disclosure provides compositions and methods for preventing and treating dyskinesia, such as drug-induced dyskinesia in patients of Parkinson's disease. The compositions, preferably in a sustained release formulation, include L-DOPA, carbidopa, and ranitidine wherein the weight ratio of L-DOPA to carbidopa is in the range of about 1:(0.2-0.3), or include L-DOPA, benserazide, and ranitidine, wherein the weight ratio of L-DOPA to benserazide is in the range of about 1:(0.4-0.6).

表征谱图