30 results about "Morphan" patented technology

The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R1, R2, R3, R4, and R5 are as defined herein. These compounds are useful for treating constipation preferably constipation caused by mu-opioid agonist therapy.

The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, wherein R1, R2a, R2b, R3 and R4 are as defined herein.Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

The present invention relates to an improved process for preparing morphinane analogues of formula (1)wherein the substituents R1, R2, R3, R4, R5 and Y have the same meanings as defined in the specification.

The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis / alkylation reactions for the synthesis of N-alkyl morphinans.

The application is directed to compounds of Formula I-Aand pharmaceutically acceptable salts and solvates thereof, wherein R1a-R3a, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

It is intended to provide a morphinan derivative represented by the following general formula (I): (I) wherein R<1> represents methyl, cyclopropylmethyl, etc.; R<2> and R<3> represent each hydroxy, methoxy, acetoxy, etc.; Y and Z represent each a valence bond, -(C=O)-, etc.; X represents a C2-5 carbon chain constituting a part of the cyclic structure (wherein one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen); (R<4>)k represents an optionally substituted fused benzene ring, carbonyl, etc.; R<9> represents hydrogen, etc.; R<10> and R<11> may be bonded together to form -O-; and R<6> represents hydrogen, etc.The above-described compound is useful as a novel remedy or preventive for urinary frequency or urinary incontinence showing an isolated side effect. Moreover, it is useful in a method for treating or preventing the above diseases and utilization for these diseases.

The invention belongs to the technical field of medicine, and relates to alkaloid compounds and their preparation methods and medical applications, in particular to morphinanes and bisbenzylisoquinoline alkaloids and their preparation methods and their preparation for the prevention or treatment of neurodegenerative diseases, Application in antitumor drugs, the structure of the compound is as follows: wherein, R 1 , R 2 is hydroxyl, C1‑C4 acyl; R 3 is C1‑C4 aldehyde group, R 4 , R 9 is C1‑C4 alkoxy, R 5 for hydrogen, R 6 and R 7 form methylenedioxy, R 8 is C1‑C4 alkyl; R 1 'is C1‑C4 alkyl, R 2 ', R 3 ', R 5 ', R 7 'is C1‑C4 alkoxy, R 4 ' is hydrogen, R 6 ' is a C1-C4 aldehyde group.

The invention provides compounds as represented by Formula I or I′ and pharmaceutically acceptable salts, solvates, and diastereomers thereof: Wherein R1, R2, R2a, R3, and R4 are defined in the disclosure. The invention also provides compounds of Formulae II, III, and A-H, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. In certain embodiments, Compounds of the Invention are useful for treating pain, constipation, and other conditions as delineated in the disclosure. Without wishing to be bound by any theory, it is believed that Compounds of the Invention are effective in treating conditions that are modulated by activity of opioid and / or ORL-1 receptors.

The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ss,bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ss,bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting a,ss-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ss,bicyclic ketone compounds, wherein the ss,bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.

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.

The present invention is directed to Benzomorphan Analog compounds of the Formula I″, Formula IA″, Formula IB″, Formula IC″, or Formula ID″ as shown below; and related Formula I′, Formula IA′, Formula IB′, Formula IC′, or Formula ID′; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 are as defined herein.Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.

The invention describes the process of catalytic O-demethylation of 3-methoxy-morphinane compounds using boron tribromide. Addition of catalysts reduces the reaction time, improves reacting the substrate to give the product in very good purity and yield. The said approach can be used, for example, for the preparation of oxymorphone, naltrexone, naloxone and nalbuphine from their respective O-methyl derivatives.

The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.

The present invention is directed to Benzomorphan Analog compounds of the Formula (I), Formula (IA), Formula (IB), Formula (IC), or Formula (ID) as shown below, wherein R1, R2a, R2b, R3, R4, Z, and G are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

Provided are compounds of the formula:R1; R2, R3; R4; A; X; Y and Z are defined in the present disclosure; pharmaceutically acceptable salts thereof, deuterium forms thereof, isomers thereof, and mixture thereof; and processes for their preparation. The compounds can be used for treating a patient suffering from a condition that is capable of treatment with an agonist and / or antagonist of the opioid receptors and are especially useful a patient suffering from pain, treating a patient in need of an immunosuppressant to prevent rejection in organ transplant and skin graft, in need of an anti-allergic agent, in need of an anti-inflammatory agent, in need of a brain cell protectant, for drug and / or alcohol abuse, to decrease gastric secretion, for diarrhea, for cardiovascular disease, for a respiratory disease, in need of a cough and / or respiratory depressant, for mental illness, for epileptic seizures and other neurologic disorders.