4 results about "Morphine derivatives" patented technology

The present application relates to the field of drug synthesis, in particular to a novel intermediate, a method for preparing the same and application thereof. The structural formula of the novel intermediate provided by the present application is as expressed by formula I:where R is a secondary amine protection group. Based on the possible biogenic pathway of morphine derivatives, the present application realizes the efficient synthesis of morphine derivatives through the strategy of biomimetic synthesis, taking the asymmetric transfer hydrogenation reaction and the intramolecular oxidative dearomatization Heck reaction in the process of preparing the intermediate as the key reactions of total synthesis. Using the novel intermediate provided by the present application to synthesize morphine derivatives has the characteristics of significantly reducing the synthesis steps, improving the yield, reducing the discharge of three wastes and reducing the production cost.

To provide a spirocyclic morphine derivative having κ-opioid receptor agonist activity. 【Solution means】 A compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: TIFF2026086955000362.tif5071 (In the formula, R 1 ~R 5 , R 7 ~R 1 3 represents a hydrogen atom, a C 1-6 alkyl group, etc., R 6 represents a hydrogen atom, a hydroxy group, etc., A represents a heterocycle which may contain at least one heteroatom selected from N, O and S as ring-constituting atoms, etc., W represents a C 1-6 alkylene group, etc., X represents a C 1-6 alkylene group, etc., Y represents a C 1-6 alkylene, etc., Z represents a C 3-7 saturated hydrocarbon ring, etc.).

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.

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.