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WO/1994/006426A1 |
The present invention relates to a method of using a bioassay consisting of an electrophysiological method and a cell culture system of dorsal-root ganglion (DRG) neurons to screen and identify opioids with a high potential for use as "l...
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WO/1994/001102A1 |
The design and synthesis of novel aminimide-based molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recogniti...
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WO/1994/000509A1 |
The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recogni...
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WO/1993/021188A1 |
A delta-selective opioid receptor antagonist is provided of formula (I) wherein R1 is (C1-C5)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, aryl, aralkyl, trans(C4-C5)alkenyl, allyl or furan-2-ylalkyl, R2 is H, OH or O2C(C1-C5)...
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WO/1993/020079A1 |
The present invention is directed to novel opiate derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the opiates and opiate metabolites. ...
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WO/1993/015081A1 |
A morphinan derivative represented by general formula (1) or a pharmacologically acceptable acid addition salt thereof, an analgesic and diuretic containing the same as the active ingredient, and a process for producing the same. The inv...
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WO/1993/011761A1 |
Aryltriflates and related compounds having general formula (1) wherein Ar is an aromatic or heteroaromatic system of a compound which has a therapeutic, biological activity when it, in the same position, carries a hydroxy, alkyloxy, halo...
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WO/1993/003051A1 |
Morphine-6-glucuronide or substituted morphine-6-glucuronide of formulae (I) is made by conjugation of a glucuronate ester and/or substituted glucuronate ester with morphine or substituted morphine in the presence of a Lewis acid catalys...
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WO/1992/022330A1 |
A radiolabeled N-substituted-6-iodo-3,14-dihydroxy-4,5alpha-epoxymorphinans
, intermediates for producing the same, and a process for the preparation and methods of detecting opioid receptors. A radioimaging agent of the present inventio...
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WO/1992/020749A1 |
A water-based recording ink comprising water, pigment, a water-soluble homopolymer, and a copolymer having both hydrophobic and hydrophilic parts. This ink can give printed characters excellent in density, lightfasteness and water resist...
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WO/1992/013534A1 |
A biologically active preparation for human or veterinary use for the selective blockade of opioid binding sites of the brain responsible for respiratory depression containing in a biologically active quantity the codeinone derivative of...
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WO/1992/008459A1 |
The invention relates to topical composition for transdermal delivery of morphine. The composition comprises an effective amount of a morphine ester in association with a topical pharmaceutical carrier which gives solutions, suspensions,...
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WO/1991/018605A1 |
A method for treating alcoholism. The alcoholdrinking response of alcoholics is extinguished by having them drink alcoholic beverages while nalmefene, an opiate antagonist, blocks the positive reinforcement effect of ethanol in the brain.
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WO/1991/018606A2 |
Analgesic compositions containing stereoisomerically pure normorphine and norcodeine derivatives or pharmaceutically acceptable acid addition salts thereof are described. Methods of administering the novel compositions to achieve analges...
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WO/1991/007966A1 |
An immunosuppressant having a low toxicity and exhibiting an excellent effect even in the case of oral administration, which is characterized by comprising as an active ingredient a $g(d)-opioid antagonist having a high selectivity for a...
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WO/1991/005768A1 |
Families of antagonist-agonists and opiate narcotics are produced from norhydrocodeinone. In a preferred embodiment, norhydrocodeinone is refluxed with sulfosalicyclic dimethylketal and delta-6-enol ether derivatives and is then converte...
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WO/1989/010348A1 |
It has been found that by using dimethyl formamide as a part of the solvent, the Albertson method for preparing amino acids can be applied to the preparation, in good yield, of long-chain aliphatic amino acids, previously obtainable only...
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WO/1989/000995A1 |
Delta-opioid receptor antagonists are disclosed of formula (I) or (II), wherein R1 is (C1-C5)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, aryl, aralkyl, trans-(C4-C5)alkenyl, allyl or furan-2-ylalkyl, R2 is H, OH or O2CR, whe...
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WO/1988/009603A2 |
The present invention involves compositions and the use thereof for inducing opiate-receptor antagonistic activity in a patient suffering from ischemic or traumatic central nervous system injury by administering to said patient an effect...
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WO/1987/005903A2 |
Stereoisomerically pure forms of normorphine analogs which have superior analgesic and nonaddicting qualities. In addition, a method of separating diastereomeric forms of N-sec-alkyl-substituted analogs utilizes the hydrocarbyl (1-8C) di...
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WO/1987/002586A2 |
Antigen-induced allergic responses are inhibited by administration of opioid antagonists. A preferred antagonist is 6-methylene-6-desoxy-n-cyclopropylmethyl-14-hydroxydihydrono
rmorphine. Oral administration is preferred.
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WO/1987/001703A1 |
A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a long-acting analgesic or opiate abuse treatment agent or appetite suppressant having general formula (I), wherein R is methyl, cyclopropylmethyl...
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WO/1985/000970A1 |
Pharmaceutical compositions having appetite reducing activity. The compositions contain (5alpha,6alpha)-7,8-didehydro-4,5-epoxy-17-(2-propanyl)-morp
hinane-3,6-diol.
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WO/1984/003627A1 |
Compounds the structural formula (I), or their pharmaceutically acceptable salts, wherein X is H or CH3, Z is NH2 or OR6, R1 is a C1-8 alkyl, C3-6-cycloalkylmethyl, or phenyl-C1-2alkyl group, R2 is hydrogen, hydroxy, chloro or fluoro, R3...
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WO/1984/000889A1 |
A topical treatment for relieving pruritis wherein Naloxone, a pharmaceutically acceptable salt of a pharmaceutically acceptable chemical derivative is topically applied in a lotion, solution, cream or ointment.
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WO/1983/003541A1 |
The use of 4-aminopyridine and congeners or derivatives thereof to antagonize drugs which act at or upon central nervous system receptors, especially dopamine receptors, such as butyrophenones and congeners or derivatives thereof. 4-amin...
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WO/1983/003197A1 |
Method for controlling gastrointestinal dysmotility in humans by administration of opioid antagonists.
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WO/1982/004049A1 |
In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically act...
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WO1982000144A1 |
A method of producing morphinan compounds which incorporates double advantages over the prior art, such as the utilization of (Beta), (Alpha)-unsaturated ketones in place of the (Alpha), (Beta)-unsaturated ketones previously used. Additi...
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WO/1981/000409A1 |
N-acyl-dihydro-14-hydroxynormorphones such as N-(cycloalkylcarbonyl)-dihydro-14-hydroxynormorphones which are intermediates useful in the preparation of morphine derivatives that are both narcotic antagonists as well as analagetics. A pr...
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WO/1980/000841A1 |
A process for producing oxymorphone by converting oxycodone utilizing a suitable boron reagent in the presence of a weak Lewis base attenuating agent.
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JP2024508543A |
The invention includes an antagonist of a cell surface opioid receptor, such as a delta opioid receptor, specific to a target cell, an imaging agent, and an immunomodulatory molecule, such as a T cell modulator, coupled to an opioid rece...
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JP2024508542A |
The invention includes an antagonist of a cell surface opioid receptor, such as a delta opioid receptor, specific to a target cell, an imaging agent, and an immunomodulatory molecule, such as a T cell modulator, coupled to an opioid rece...
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JP7421804B2 |
This disclosure relates to crystalline forms of 3-acyl-buprenorphine derivatives and sustained release injectable pharmaceutical compositions for treatment of opioid dependence, pain or depression, including an aqueous suspension of crys...
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JP2024501153A |
The present invention provides a novel, efficient and pot-economical method for converting morphine to noroxymorphone using less toxic and lower cost reagents and solvents compared to those used in the prior art. It also relates to a met...
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JP7397095B2 |
Provided herein are prodrugs of opioid receptor antagonists such as nalmefene and naltrexone, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of behavioral disorders.
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JP2023548356A |
This application is directed to a method for purifying noroxymorphone by preparing and isolating a noroxymorphone bisulfite adduct and regenerating purified noroxymorphone from the noroxymorphone bisulfite adduct. shall be. This applicat...
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JP7369687B2 |
There are provided, prodrugs of opioid and other controlled substance, having enhanced physical and chemical stability to resist tampering and to make long-acting release formulations, and pharmaceutically accepted salts and solvates the...
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JP2023113976A |
To provide a method for producing a morphinan derivative.The invention provides a production method for obtaining a morphinan derivative represented by a general formula (II) in the figure by means of a reduction reaction using a formic ...
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JP2023106478A |
To provide crystalline forms of 3-acyl-buprenorphine derivatives for treatment of opioid dependence, pain or depression.The invention provides a crystalline form of 3-acyl-buprenorphine represented by formula II, which is a buprenorphine...
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JP7307067B2 |
The present invention encompasses improved morphian compositions and methods of use of the improved compositions for modulating neuropathic pain, opioid-induced glial activation, or a combination thereof beyond what is currently known in...
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JP7302904B2 |
Provided is a cost-effective process for preparing naldemedine having high purity with high yields.
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JP7284764B2 |
This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R3, R4 and Z are as defined herein in the disclosure. The invention also relates to the use of such co...
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JP2023518875A |
Compounds, compositions, and methods comprising administering a morphinan family compound to a subject for the treatment or prevention of conditions, conditions and diseases that may benefit from NMDAR modulation. Methods may include adm...
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JP2023028184A |
To provide an agent for treating, improving or preventing various diseases associated with an opioid κ receptor including a pain, having the ability to bind the opioid κ receptor and reduced side effect.The present invention provides a...
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JP7208635B2 |
The present invention relates to a compound as represented by structural formula (I) and a non-toxic, pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH3 or deuterated methyl(CD3); R2 is CH3 or CH2CH3; each of R3, R4 a...
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JP2022160564A |
To provide compounds and their uses, in particular, compounds in the form of prodrugs, that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of a parent drug.The invention provides a co...
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JP2022544564A |
The present invention relates to opiate-derived compositions and antagonists thereof useful in therapeutic areas involving modulation of opioid receptors. 3-hexadienoate modifications of opioids are prepared to improve the binding of opi...
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JP7118888B2 |
The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
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JP2022518461A |
Prodrugs of opioids such as levorphanol or morphine with enhanced physical and chemical stability to withstand tampering and to make long-acting sustained release formulations, and pharmaceutically acceptable thereof. Possible salts and ...
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