- 3-formamido-4-hydroxyl naltrexone deuterated derivative, preparation method thereof and application of 3-formamido-4-hydroxyl naltrexone deuterated derivative in medicine
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The invention relates to a 3-formamido-4-hydroxyl naltrexone deuterated derivative, a preparation method thereof and application of the 3-formamido-4-hydroxyl naltrexone deuterated derivative in medicine. In particular, the present invention relates to a 3-formamido-4-hydroxynaltrexone deuterated derivative represented by a general formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, and application of the 3-formamido-4-hydroxyl naltrexone deuterated derivative as an opioid receptor modulator in the treatment of cough, diarrhea, drug dependence, gastrointestinal tract diseases, allergic bowel syndrome, obesity, respiratory depression, convulsion, pain, allergy, pruritus and other diseases, and central nervous system diseases or/and mental diseases and other related diseases, wherein each substituent in the general formula (I) is as defined in the specification.
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Paragraph 0106; 0117-0120
(2021/08/14)
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- One-Pot Process for Synthesis of Nalbuphine Hydrochloride and Impurity Control Strategy
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An improved kilogram-scale process of synthesis of nalbuphine was developed by investigating the critical parameters. Ten process-related impurities were identified, of which the source and control strategy was elucidated. Moreover, tetramethylammonium triacetoxyborohydride (Me4NBH(OAc)3) was developed to reduce the imine and ketone in one pot. As a result, 6-β-epimer was significantly controlled to only 0.08% in the crude nalbuphine. The improved process was robust at kilogram scale in 60.4% overall yield with 99.95% high-performance liquid chromatography (HPLC) purity.
- Chen, Yibo,Wu, Zenong,Yang, Zhezhou,Zhang, Fuli,Zhang, Tao,Zhao, Weili
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p. 1707 - 1717
(2020/12/01)
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- PROCESS FOR OBTAINING 3,14-DIACETYLOXYMORPHONE FROM ORIPAVINE
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The present invention relates to a new process for obtaining 3,14-diacetyloxymorphone from oripavine, a process to transform the obtained 3,14-diacetyloxymorphone into a noroxymorphone and a process to transform said noroxymorphone into naloxone, naltrexone, nalbuphine, nalfurafine or nalmefene.
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Page/Page column 46
(2018/01/17)
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- COMPOUNDS FOR TREATING PRURITIC CONDITIONS
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The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvates, and/or esters thereof. These compounds are useful for treating itch or a pruritic condition. The present invention also includes compositions comprising the present compounds and methods of treating a pruritic condition. Furthermore, the present invention provides methods for preparing the compounds.
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Paragraph 0120; 0121
(2016/11/14)
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- NOROXYMORPHONE FOR USE AS A MEDICAMENT
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The present invention concerns noroxymorphone and its use in the manufacture of an intrathecally or systemically applicable medicament for the treatment of pain and inflammation. The invention also concerns a composition comprising noroxymorphone. The present invention also relates to a novel method for producing a medicament comprising noroxymorphone. The invention also relates to a method of treating pain in a subject by administering the subject with an analgesically effective amount of noroxymorphone.
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Page/Page column 16
(2008/12/08)
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- Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates
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The invention provides processes for the conversion of normorphinone and its derivatives, which can be synthesized from morphine, to the corresponding 14-hydroxynormorphinone and its derivatives including oxycodone, oxymorphone, noroxymorphone and naltrexone. Noroxymorphone is a key intermediate for the production of important narcotic analgesics and antagonists. The invention also provides certain novel intermediates.
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