Morphine hydrochloride hydrate | 6055-06-7

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: Morphine hydrochloride hydrate
• 英文别名: (4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;hydrate;hydrochloride
• CAS: 6055-06-7
• 化学式: C17H22ClNO4
• 分子量: 339.8
• InChiKey: RTLFRZCGRLMVRK-ZGZIUUKVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  23
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  53.9
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• CRYSTAL OF SALT OF NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：US20180148409A1

  公开（公告）日：2018-05-31

  Disclosed herein are a crystal comprising a compound, which has μ-opioid receptor antagonistic action, few side effects, and high safety, and having high purity and excellent physical properties (stability, solubility, etc.), and a method for producing the crystal. The crystal is a crystal of a salt comprising: a compound represented by a formula (I) [wherein R 2 is a hydrogen atom or a halogen atom, and R 1 is a group selected from the group consisting of and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, and oxalic acid, or a hydrate thereof.

  本文披露了一种晶体，其中包含一种化合物，具有μ-阿片受体拮抗作用，副作用少，安全性高，纯度高，具有优异的物理性质（稳定性、溶解性等），以及一种制备该晶体的方法。该晶体是一种包含盐的晶体，该盐包含以下化合物：由式（I）表示的化合物[其中R2是氢原子或卤原子，R1是从所选组中选择的群，以及从盐酸、溴酸和草酸中选择的酸或其水合物。
• ORALLY DISINTEGRATING TABLET
  申请人：Sanwa Kagaku Kenkyusho Co., Ltd

  公开号：EP3023109A1

  公开（公告）日：2016-05-25

  Disclosed is an orally disintegrating tablet including: (a) an active ingredient; (b) a starch with an amylose content of 20% by mass to 30% by mass and a degree of gelatinization of less than 10%; and (c) at least one inorganic excipient selected from the group consisting of magnesium silicate, calcium silicate, and synthetic hydrotalcite. The orally disintegrating tablet is a single-layer tablet or a dry-coated tablet having an inner core and an outer layer. The orally disintegrating tablet as a single-layer tablet or the outer layer of the orally disintegrating tablet as a dry-coated tablet has a crystalline cellulose content of 0% by mass to 5% by mass.

  本发明公开了一种口腔崩解片剂，包括：(a)活性成分；(b)淀粉含量为 20% 至 30%，糊化度低于 10%的淀粉；以及(c)至少一种无机赋形剂，该赋形剂选自硅酸镁、硅酸钙和合成水滑石组成的组。口腔崩解片是具有内核和外层的单层片剂或干包衣片剂。作为单层片剂的口腔崩解片或作为干包衣片剂的口腔崩解片的外层的结晶纤维素含量为 0%（质量分数）至 5%（质量分数）。
• NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：EP3072884A1

  公开（公告）日：2016-09-28

  The object of the present invention is to provide a compound having an antagonistic action against µ-opioid receptors, which causes less side effects and thus is highly safe. A compound represented by the general formula (I), or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and each represents a hydrogen atom or a halogen atom, provided that R1 and R2 are not simultaneously halogen atoms, R3 represents a C1-C3 alkyl group or a vinyl group, and R4 represents the formula (II): wherein R5 represents a hydroxy group or a C1-C3 alkoxy group, and R6 and R7 are the same or different, and each represents a hydrogen atom or a halogen atom; or the formula (III): wherein Ring A represents a halogen atom(s)-substituted C5-C7 cycloalkyl group which is optionally substituted by a C1-C3 alkoxy group, or a halogen atom(s)-substituted 5- to 7-membered saturated heterocyclic group.

  本发明的目的是提供一种对μ-阿片受体具有拮抗作用的化合物，该化合物的副作用较小，因此安全性高。 通式(I)代表的化合物或其药理学上可接受的盐： 其中 R1 和 R2 相同或不同，各自代表氢原子或卤素原子，但 R1 和 R2 不能同时代表卤素原子、 R3 代表 C1-C3 烷基或乙烯基，以及 R4 代表式 (II)： 其中 R5 代表羟基或 C1-C3 烷氧基，R6 和 R7 相同或不同，且各自代表氢原子或卤素原子； 或式 (III)： 其中环 A 代表任选被 C1-C3 烷氧基取代的卤原子取代的 C5-C7 环烷基或卤原子取代的 5-7 元饱和杂环基。
• Therapeutic or prophylactic agent for biliary diseases
  申请人：Kobayashi Ryosuke

  公开号：US10131672B2

  公开（公告）日：2018-11-20

  A therapeutic or prophylactic agent for biliary tract diseases includes as an effective component a specific compound having a morphinan skeleton represented by Compound 1, or a pharmaceutically acceptable acid addition salt thereof:

  胆道疾病的治疗剂或预防剂包括作为有效成分的具有化合物 1 所代表的吗啡烷骨架的特定化合物或其药学上可接受的酸加成盐：
• Crystal of salt of novel 3-azabicyclo[3.1.0]hexane derivative and pharmaceutical use thereof
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：US10392345B2

  公开（公告）日：2019-08-27

  Disclosed herein are a crystal comprising a compound, which has μ-opioid receptor antagonistic action, few side effects, and high safety, and having high purity and excellent physical properties (stability, solubility, etc.), and a method for producing the crystal. The crystal is a crystal of a salt comprising: a compound represented by a formula (I) [wherein R2 is a hydrogen atom or a halogen atom, and R1 is a group selected from the group consisting of and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, and oxalic acid, or a hydrate thereof.

  本文公开了一种由化合物组成的晶体，该化合物具有μ-阿片受体拮抗作用，副作用小，安全性高，纯度高，物理性质（稳定性、溶解性等）优良。 该晶体是一种盐的晶体，包括：由式（I）代表的化合物 [其中 R2 是氢原子或卤素原子，R1 是选自以下组别的基团 和一种选自盐酸、氢溴酸和草酸或其水合物的酸。