摘要:
The present invention relates to genetically modified plants of the species Papaver bracteatum wherein the type or amount of one or more alkaloids produced by the plants has been modified. Specifically, the genetically modified plants have an increased expression of one or more of thebaine 6-O-demethylase, codeine O- demethylase and/or codeinone reductase relative to wild type P. bracteatum such that the genetically modified poppy plants produce an increased quantity of an alkaloid selected from codeine, oripavine and/or morphine relative to a wild type P. bracteatum. Also provided are progeny plants having the genetically modified poppy plants described above as a parent; mutant or derivative plants of the aforementioned plants; reproductive material derived from, straw produced from, straw concentrate produced from, latex derived from, or one or more isolated cells derived from, the aforementioned plants. Methods for producing an alkaloid from the aforementioned plants are also provided, together with nucleic acid and amino acid sequence variants of the 6-O-demethylase and codeine O-demethylase genes.
摘要:
The present disclosure generally relates to a process for converting a fused, tricyclic compound to a fused, tetracyclic compound that includes a furan ring therein. More particularly, the present disclosure related to a process for preparing a hydrocodone compound, or a compound structurally related thereto, and in particular (+)-hydrocodone, by subjecting a structurally corresponding sinomeπine starting compound to a super acid-assisted furan ring closure reaction. Formula I, II. Examples of super acids useful in the processes described herein include, but are not limited to, trifluoromethanesulfonic acid (CF 3 SO 3 H), tetrafluoroboric acid (HBF 4 ), fluorophosphoric acid (HPF 6 ), fluorosulfuric acid (FSO 3 H). and fiuoroantimonic acid (HSbF 8 ), fluorophosphoric acid (FP(O)(OH) 2 ) as well as combinations thereof.
摘要:
The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates.
摘要:
Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided. The intermediates are morphinane derivatives of formula (10) wherein X is a F or Cl and R is selected from the group consisting of an H, alkyl, aryl, acyl, formyl, COR”, CONHR”, COOR, Bn(benzyl), alkyl(methyl), and sulfonamide SO2CH2COPh.
摘要:
The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I . The approach disclosed herein is the modification of D ring by- substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound.
摘要:
This invention relates to a tamper-resistant transdermal-delivery device comprising an opioid, or a pharmaceutically acceptable salt thereof, and an acyl opiod antagonist, or a pharmaceutically acceptable salt thereof. The transdermal-delivery device allows an analgesically effective amount of the opioid, or a pharmaceutically acceptable salt thereof, to be transdermally administered to a patient. The invention further relates to methods for treating or preventing pain in a patient comprising contacting the skin of a patient in need thereof with the transdermal-delivery device of the invention for an amount of time sufficient to treat or prevent pain. The invention further relates to acyl opioid antagonists.
摘要:
The present invention concerns the use of compound of formula (I) or (II) and their pharmaceutically acceptable salts in the preparation of a pharmaceutical composition useful namely in an anti-malarial prophylactic or curative treatment. The invention also concerns the new compounds and the pharmaceutical compositions comprising the same.
摘要:
The invention relates to sinomenine and compounds thereof and also to compounds of formula (I), wherein R1 represents an alkyl group; R2 represents a hydrogen atom or an alkylcarbonyl group, an haloalkylcarbonyl group or an arylcarbonyl; Y represents a group (II), (III) or (IV); R3 ,R4, R’4, R5, R’5 and R6 are as defined in the description; and X represents a halogen atom. Medicaments.