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JP2009545629A |
The present invention relates to compounds of formula I, synthesis thereof, and methods of using the same.
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JP2009263367A |
To provide a new morphinan compound that can be used as an analgesic of high activity or an opioid antagonist.The morphinan compound is represented by formula (Ia) [wherein: R1 is an alkyl group, an arylalkyl group or the like; X is an o...
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JP4359711B2 |
Remedies for drug addiction which contain as the active ingredient k-opioid receptor agonists typified by the compounds represented by general formula (I). These k-opioid receptor agonists are useful as remedies for drug addiction which ...
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JP4340437B2 |
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is -CH 2 -OH, -CH 2 NH 2 , -NHSO 2 CH 3 , and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction m...
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JP2009534472A |
The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.
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JP2009533443A |
The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to oxycodone in a manner that substantially decreases the potential for overdose. When delivered at the proper dosage the pharmace...
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JP4323547B2 |
A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): wherein R 1 and R 2 are each independently hydrogen, optionally substituted lowe...
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JP4316674B2 |
A novel process for preparing narcotic analgesics such as hydrocodone and hydromorphone using catalytic amounts of homogeneous organometallic complexes is disclosed.
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JP4311369B2 |
Stable medicinal compositions characterized by containing 4,5-epoxymorphinane derivatives and at least one member selected from among water-soluble antioxidants, fat-soluble antioxidants, synergists, saccharides and surfactants.
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JP2009161557A |
To provide a new method for producing narcotic analgesics such as hydrocodone and hydromorphone.Disclosed is a new method for producing narcotic analgesics, for example, hydrocodone and hydromorphone represented by formula (I) using cata...
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JP4292738B2 |
This invention relates to: an indole derivative or a pharmaceutically acceptable salt thereof represented by formula (I): wherein R<1> is, for example, hydrogen or C1-5 alkyl; R<2> is, for example, hydrogen or hydroxy; R<3> is, for examp...
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JP2009522357A |
There is provided a method for the synthesis of norbuprenorphine, and ultimately buprenorphine, utilizing oripavine as the starting material. Conventional methods of producing buprenorphine utilize thebaine as the starting material, requ...
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JPWO2007043518A1 |
Provide treatment and / or prophylaxis for nausea and / or vomiting. Equation (I):(During the ceremony,And R1And R2Are independently hydrogen or lower alkyl, R3Is hydrogen or lower alkoxycarbonyl, R4Is hydrogen or lower alkyl. However, R...
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JP4239592B2 |
Treatment for sepsis involves administration of an opioid kappa receptor agonist. ACTIVITY : Antibacterial; Immunosuppressive; Hypertensive; Anticoagulant; Thrombolytic. In a lipopolysaccharide induced toxemia model in ICR mice, administ...
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JP2009507872A |
This invention relates to a class of 6-amino-morphinan compounds which can be used as highly active analgesics. This invention also relates to their pharmaceutically acceptable salts and easily accessible derivatives (e.g. esters or amid...
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JP2009506080A |
Combination therapies of an opioid receptor agonist and an alpha-2 receptor antagonist in an amount effective to potentiate, but not antagonize, a therapeutic effect of the opioid receptor agonist are provided. Also provided are methods ...
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JP2008546688A |
Novel methods of synthesis of known and novel 14-hydroxyl opiates through 1-halothebaine and derivatives are described.
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JP2008542395A |
The invention provides prophylactic and therapeutic methods for administering a μ-opioid receptor antagonist, e.g., N-methylnaltrexone or a salt thereof, to treat cell barrier diseases and disorders, such as endothelial and epithelial c...
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JP2008538746A |
A method for the catalytic production of hydrocodone derivatives and hydromorphone derivatives, respectively, utilizing a transition metal catalyst of the formula [M(PR4R5R6)nXm]p; wherein M is a Group VIII transition metal; R4, R5 and R...
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JP2008231049A |
To provide an apoptosis-inducing substance which can solve the problem that such diseases as cancer, Alzheimer's disease, BSE, RNA viral infectious diseases (HIV, influenza, hepatitis C, etc.) and allergies have been deemed to be difficu...
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JP2008536934A |
Hydromorphone hydrochloride forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydromorphone hydrochloride.
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JP2008533049A |
Hydrocodone bitartrate forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydrocodone bitartrate.
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JP2008179554A |
To provide a medicine which is useful for preventing or treating various diseases and symptoms related to opioid receptors.A specific pyrrole-condensed morphinan derivative represented by the formula, such as [1-[17-(cyclopropylmethyl)-4...
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JP4117801B2 |
PCT No. PCT/SE95/00503 Sec. 371 Date Aug. 22, 1995 Sec. 102(e) Date Aug. 22, 1995 PCT Filed May 9, 1995 PCT Pub. No. WO95/31463 PCT Pub. Date Nov. 23, 1995New morphinane derivatives of the formula their pharmaceutically acceptable salts,...
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JP4110579B2 |
The present invention provides an indolomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing and preventing cerebral disorders composed of the derivative and salt thereof, which is re...
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JPWO2006064779A1 |
Provided are novel compounds useful as therapeutic and / or prophylactic agents for nausea and / or vomiting. Equation (I):(In the formula, R1Is hydrogen or -CHRARB(Here RAIs lower alkoxycarbonyloxy, etc., RBIs hydrogen or methyl) or a p...
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JP2008515801A |
Dietary supplement compositions containing one or more compounds such as arginine, selenium, calcium, calcium sources, morphine precursors (e.g., reticuline), morphine, and morphine-6beta-glucuronide are provided.
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JP2008512462A |
The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and ...
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JP2008044938A |
To provide a remedy or preventive for urinary frequency or urinary incontinence having improved side actions.The remedy or preventive for urinary frequency or urinary incontinence contains a morphinan derivative having a nitrogen-contain...
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JP4040673B2 |
PCT No. PCT/US95/06097 Sec. 371 Date Nov. 26, 1996 Sec. 102(e) Date Nov. 26, 1996 PCT Filed May 16, 1995 PCT Pub. No. WO95/32973 PCT Pub. Date Dec. 7, 1995A process is described for the synthesis of nalbuphine. The process results in a p...
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JP2008501797A |
A method for extracting at least one alkaloid from opium that includes dissolving opium in a solvent, heating the dissolved opium solution, cooling the dissolved opium solution, adjusting the pH of the dissolved opium solution with at le...
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JP2007537144A |
Expression [M (PR)3R4R5)nXm]p(In the formula, R1Is H, alkyl, aryl or acyl; M is a Group VIII transition metal; R3, R4And R5Is selected from the group consisting of alkyl, aryl, alkoxyl, phenoxyl and combinations thereof; X is a halogen o...
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JP2007537198A |
Morphinane derivatives of the formula their pharmaceutically acceptable salts are provided for use as medicaments for the treatment and/or prevention of disorders associated with the target calcineurin.
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JP4024992B2 |
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JP4016986B2 |
The invention provides a morphinan derivative of the Formula (I): Äwherein R<1> is methyl, cyclopropylmethyl or the like; R<2> and R<3> are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, -C(=O)- or the like; X is...
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JP2007528837A |
A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide as catalyst.
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JP2007526217A |
This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmace...
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JP3948026B2 |
A novel brain cell protective containing a morphinane derivative represented by the compound of formula (1) or a pharmacologically acceptable acid-addition salt thereof as the active ingredient. This compound exhibits an excellent protec...
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JP2007161712A |
To provide a chemical analogue useful in producing a conjugate useful in the development of an antibody recognizing 6-MAM(6-monoacetylmorphine) and 6-MAC(6-monoacetylcodeine) and also useful in an immunoassay for detecting 6-MAM and 6-MA...
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JP2007504150A |
Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X ...
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JP3843456B2 |
A morphinan derivative represented by formula (1) or a pharmacologically acceptable acid-addition salt thereof, and analgesic, diuretic, antitussive and brain cell protective agents each containing the derivative or the salt as the activ...
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JP2006522819A |
Methods for treating constipation are provided. The methods include administration of peripheral opioid antagonists in combination with laxatives and/or stool softeners. Patients treatable by the invention include those refractory to con...
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JPWO2004078177A1 |
The following compoundsIt is related to a drug / substance dependence therapeutic drug containing a compound represented by the above as an active ingredient, and has excellent brain transferability, and recovery from the drug / substanc...
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JP2006131545A |
To obtain a therapeutic agent for neurogenic pains which has an excellent therapeutic effect on neurogenic pains which are intractable disorders.This therapeutic agent for neurogenic pains contains an opioid receptor antagonist (especial...
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JP2006509745A |
A process for the preparation of a quaternary derivative of the morphinan alkaloid, the process comprising contacting a tertiary N-substituted morphinan alkaloid with an alkyl halide in an anhydrous solvent system, wherein the solvent sy...
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JP2006505588A |
An improved process for the preparation of codeine from morphine comprises the steps of a) reacting morphine with a methylating agent in the presence of a hydrocarbon solvent at a temperature of 100 to 215° C. under reflux conditions su...
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JP3743449B2 |
To provide a stable medicine composition which contains a 4,5-epoxymorphinan derivative hardly causing side effects and being useful as an analgesic or a diuretic; and a method for stabilizing the derivative. The stable medicine composit...
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JP2006502190A |
Novel compounds which selectively bind to the delta-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with sele...
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JP2006500326A |
The present invention relates to a class of morphinan compounds and quaternary ammonium salts thereof, substituted in Position 14, which may be used as highly active analgesics or also as opioid antagonists. The present invention also re...
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JPWO2004007503A1 |
The present invention has the general formula (I).[R in the formula1Is R, such as cyclopropylmethyl2And R3Is hydroxy, methoxy, etc., R4And R5Combined with -O-, etc., R6Is hydrogen, Q is substituted or unsubstitutedEtc., X represents NH, ...
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