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5 results about "Thebaine" patented technology
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Thebaine (paramorphine), also known as codeine methyl enol ether, is an opiate alkaloid, its name coming from the Greek Θῆβαι, Thēbai (Thebes), an ancient city in Upper Egypt. A minor constituent of opium, thebaine is chemically similar to both morphine and codeine, but has stimulatory rather than depressant effects. At high doses, it causes convulsions similar to strychnine poisoning. The synthetic enantiomer (+)-thebaine does show analgesic effects apparently mediated through opioid receptors, unlike the inactive natural enantiomer (−)-thebaine. While thebaine is not used therapeutically, it is the main alkaloid extracted from Papaver bracteatum (Iranian opium / Persian poppy) and can be converted industrially into a variety of compounds, including oxycodone, oxymorphone, nalbuphine, naloxone, naltrexone, buprenorphine and etorphine. Butorphanol can also be derived from thebaine.
Tetrahydrothebaine derivative as well as preparation method and application thereof
The invention relates to a tetrahydrothebaine derivative as well as a preparation method and application thereof, in particular to a 7alpha-(4 '-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative as shown in a general formula (I) or pharmaceutically acceptable salts thereof and a preparation method of the 7alpha-(4'-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative. And to the use of such derivatives in the preparation of medicaments for the treatment and / or prevention of pain, irritable bowel syndrome, pruritus, addiction, depression. The derivative disclosed by the invention has a remarkable improvement effect in the aspects of agonistic activity of the kappa opioid receptor, subtype selectivity of the kappa opioid receptor and central safety.
Owner:SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES +1
Preparation method of 7alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-bridge ethylidene-6, 7, 8, 14-tetrahydrothebaine
The invention discloses a preparation method of a buprenorphine hydrochloride key intermediate, particularly provides an improved method for preparing 7 alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-diethylidene-6, 7, 8, 14-tetrahydrothebaine, and belongs to the technical field of medical intermediates. The compound is a key intermediate for synthesizing buprenorphine hydrochloride. The solid of the key intermediate is obtained with high yield and high purity through the method, and the method is simple and convenient to operate and suitable for industrial production.
![Preparation method of 7alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-bridge ethylidene-6, 7, 8, 14-tetrahydrothebaine](https://images-eureka.patsnap.com/patent_img/3b8b2969-f148-4cec-81f7-fcba90b092bf/CN121895325A.png "Preparation method of 7alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-bridge ethylidene-6, 7, 8, 14-tetrahydrothebaine")
Owner:CHANGZHOU NO 4 PHARMA FACTORY +1
A fused ring morphine derivative, process for its preparation and use thereof
The application belongs to the field of pharmacy, discloses a fused ring morphine derivative and a preparation method and application thereof, and relates to N-cyclopropylmethyl-4'-substituted aminonalepotem series derivatives with formula (I) and pharmaceutically acceptable salts. The derivative with formula (I) is prepared by reacting thebaine with a substituted phenyl vinyl ketone reagent and through a series of conversion methods. Among them, N-cyclopropylmethyl-(4'-benzoyl amino) nalepotem (SLL-1062) is a typical high selectivity mu opioid receptor antagonist, and can be applied to the research and development in the fields of diagnosis and treatment of opioid and other narcotic analgesic dependence, opioid drug-induced intestinal dysfunction, sedative hypnotics and acute alcohol poisoning, opioid and other narcotic analgesic poisoning and the like.
Owner:FUDAN UNIVERSITY
7a-substituted phenyltetrahydrothebaine derivatives, processes for their preparation and uses thereof
This application relates to a 7α-substituted phenyltetrahydrothebaine derivative, its preparation method, and its uses. Specifically, it relates to a 7α-substituted phenyltetrahydrothebaine derivative as shown in general formula (I) or a pharmaceutically acceptable salt thereof, and its preparation method, and to the use of such derivatives in the preparation of analgesic, anti-anxiety, anti-addiction, and antidepressant drugs. The derivatives of this invention exhibit significantly enhanced agonist activity and subtype selectivity of δ-opioid receptors.
Owner:YANTAI NEW DRUG DEV SHANDONG PROVINCIAL LAB +1
A 7α-substituted piperazine morphine derivative, its preparation method and uses
This application relates to a 7α-substituted piperazine morphine derivative, its preparation method, and its uses. Specifically, it relates to 7α-(N-substituted piperazine)-tetrahydrothebaine derivatives as shown in general formula (I) or pharmaceutically acceptable salts thereof, and their preparation methods. Furthermore, it relates to the use of such derivatives in the preparation of analgesic, anti-irritable bowel syndrome, antipruritic, anti-addictive, and antidepressant drugs. The derivatives described in this invention exhibit significantly enhanced κ-receptor agonist activity and κ-receptor subtype selectivity.
Owner:YANTAI NEW DRUG DEV SHANDONG PROVINCIAL LAB +1