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49 results about "Morphinan derivatives" patented technology
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Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others. ... Small groups are usually found on morphinan derivatives at carbons 3 and 6.
Morphinan-derivatives for treating diabetes and related disorders
ActiveUS20150087669A1Risk of developingDelay progressBiocideMetabolism disorderDiseaseNR1 NMDA receptor
The invention relates to a morphinan-derivative that targets NMDA receptors on pancreatic islets and has the general formula (I)whereinR1 is selected from —OH, —CO2H, —R0, —OR0, —OC(═O)R0, —OC(═O)OR0 or —OC(═O)NHR0; and R2 is selected from —H, —R0, —C(═O)R0, —C(═O)OR0, —C(═O)NHR0 or —C(═NH)—NH—C(═NH)—NH2; wherein R0 is in each case independently selected from —C1-C6-alkyl, -aryl, -heteroaryl, —C1-C6-alkyl-aryl or —C1-C6-alkyl-heteroaryl, in each case independently unsubstituted or substituted;or its physiologically acceptable salt and / or stereoisomer, including mixtures thereof in all ratios, for use in the treatment of a disease or condition, where the disease or condition is insulin-dependent diabetes mellitus, non-insulin-dependent diabetes mellitus, obesity, and / or diabetic nephropathy.
Owner:DEUTE DIABETES FORSCHUNGSGES
6-Carboxy-normorphinan derivatives, synthesis and uses thereof
InactiveUS20080064744A1Prevention and treatment and reduction of severity of symptomReduce secretionBiocideNervous disorderMedicinal chemistryMorphinan derivatives
The present invention relates to compounds of formula I, synthesis thereof, and methods of using the same.
Owner:WYETH LLC
Morphinan derivatives with high oral bioavailability
InactiveUS20100240691A1Improve oral bioavailabilityImprove bioavailabilityBiocideNervous disorderDiseaseAlcohol
The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction.
Owner:ALKERMES PHARMA IRELAND LTD
Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
InactiveUS20060040970A1Efficient processImprovement of side effectsBiocideOrganic chemistryAdditive ingredientMorphine
The invention provides a morphinan derivative of the Formula (I):
(wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(═O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like) or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.
Owner:TORAY IND INC
Preparation of oxymorphone from oripavine
An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1′-dimer side products. The 14-hydroxymorphinone is then reduced, typically by catalytic hydrogenation to form oxymorphone. The inventive method disclosed is further applicable to the production of morphinan derivatives.
Owner:SPECGX LLC
Nitrogen containing morphinan derivatives and the use thereof
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.
Owner:PURDUE PHARMA LP
6,7-unsaturated-7-carbamoyl substituted morphinan derivative
ActiveUS20090203723A1Prevent constipationEliminate side effectsBiocideNervous disorderArylAcyl group
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 R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl,or a pharmaceutically acceptably salt, or a solvate thereof is provided.
Owner:SHIONOGI & CO LTD
Morphinan derivatives for the treatment of drug overdose
The instant application relates to morphinan derivatives of Formula I with sustained effectiveness in treating drug toxicity and overdose:
Owner:ALKERMES PHARMA IRELAND LTD
Morphinan derivative
A morphinan derivative represented by the following general formula (I)
(in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like,
R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like,
X represents O or CH2, and
Y represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
Owner:NIPPON CHEMIPHAR CO LTD
Therapeutic or Prophylactic Agent for Functional Bowel Disorder
InactiveUS20090111843A1Good effectLittle side effectsBiocideOrganic chemistryAdditive ingredientMorphine
A therapeutic or prophylactic agent for functional bowel disorders comprising as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic group or a pharmaceutically acceptable acid addition salt thereof is disclosed. The therapeutic or prophylactic agent for functional bowel disorders comprises as an effective ingredient a morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10).
Owner:TORAY IND INC
Nitrogen Containing Morphinan Derivatives and the Use Thereof
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.
Owner:PURDUE PHARMA LP
Crystals of morphinan derivative and process for producing the same
The present invention is directed to provide 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride including a A-form, B-form or C-form crystal thereof, and a process for producing the same are provided.
Owner:TORAY IND INC
Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
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.
Owner:TORAY IND INC
Analgesic
InactiveUS20070299100A1Highly potent analgesic effectExcellent analgesicBiocideNervous disorderAdditive ingredientMorphine
An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as compound 1:
Owner:TORAY IND INC
Therapeutic or preventive agent for nausea/vomiting
A therapeutic or prophylactic agent for preventing nausea and vomiting is disclosed. The agent includes a morphinan derivative represented by general formula (I): or a pharmacologically acceptable acid addition salt thereof as an active ingredient. The compounds are useful as therapeutic or prophylactic agents for preventing nausea and vomiting caused by μ-agonists represented by, morphine.
Owner:TORAY IND INC
Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has characteristic diffraction peaks at positions of 2θ of 13.6°(±0.2°), 17.2°(±0.2°), 19.1°(±0.2°), 23.2°(±0.2°), and 23.8°(±0.2°) in a powder X-ray diffraction pattern thereof. The present invention also relates to a pharmaceutical composition comprising the above-mentioned X-form crystal of morphinan derivative hydrochloride.
Owner:EVERLIGHT CHEMICAL INDUSTRIAL CORPORATION
Oral preparation comprising specific organic acid, and method for improvement in elution property and chemical stability of oral preparation
InactiveUS20100215750A1Improve solubilityGood chemical stabilityPowder deliveryBiocideOrganic acidSolubility
A chemically stable oral preparation with an excellent dissolution property comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof is disclosed. The oral preparation according to the present invention comprises a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof as an effective ingredient and an organic acid, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C. The method for improving dissolution property and chemical stability of an oral preparation according to the present invention comprises incorporating an organic acid in the oral preparation comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C.
Owner:TORAY IND INC
Preparation of Oxymorphone from Oripavine
An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1′-dimer side products. The 14-hydroxymorphinone is then reduced, typically by catalytic hydrogenation to form oxymorphone. The inventive method disclosed is further applicable to the production of morphinan derivatives.
Owner:SPECGX LLC
8alpha substituted aryl-4,5-epoxy morphinan derivative or its salt, preparation method and application thereof
The invention belongs to the pharmaceutical field and relates to 8alpha substituted aryl-4, 5-epoxy morphinan derivatives shown in formula (I) or salts thereof, a preparation method and the usage of the compound in treating pains. The compound is prepared by Thebaine or analogs thereof reacting with agents containing single substituted ethylenes and by a corresponding transformation method. Test results of in vitro experiments show that the representative compound of the invention shows combining ability and activation ability on mu opioid receptors corresponding to morphine and has high selectivity for the mu opioid receptors but basically has no affinity to other opioid receptor subtypes. The compound of the invention belongs to mu excitant with new structure type and high selectivity and can be further made into pain relievers with strong pain relieving function and low endurance and addiction.
Owner:FUDAN UNIV
Morphinan derivative
ActiveUS10442802B2Good effectSuppression of gastrointestinal motilityOrganic active ingredientsSenses disorderHydrogenMorphine
A morphinan derivative represented by the following general formula (I):(wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.,R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group,Y binds to a carbon atom as a ring-constituting atom of R2,R3, R4, and R5 represent hydrogen; hydroxy, etc.,R6a and R6b represent hydrogen, etc.,R7 and R8 represent hydrogen, etc.,R9 and R10, which are the same or different, represent hydrogen, etc.,X represents O or CH2, andY represents C(═O)),a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.
Owner:NIPPON CHEMIPHAR CO LTD
Stable solid preparation comprising 4,5-epoxymorphinan derivative
ActiveCN101686976AOrganic active ingredientsPowder deliveryLow-substituted hydroxypropylcelluloseMorphine
Disclosed is a stable solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient. Specifically disclosed is a stable solid preparation comprising: a 4,5-epoxymorphinan derivative represented by the general formula (I) or a pharmacologically acceptable acid addition salt thereof as an active ingredient; sodium thiophosphate; a sugar or a sugar alcohol; and a hydroxypropylcellulose having a low degree of substitution in an amount of 1 to 30% by weight per unit weight of the total amount of the active ingredient, sodium thiophosphate and the sugar or the sugar alcohol.
Owner:TORAY IND INC
Morphinan derivatives and preparation methods thereof
InactiveUS8563721B2Simple processDifficult to purifySilicon organic compoundsMorphinanMorphinan derivatives
The present invention relates to morphinan derivatives and preparation methods thereof, especially to ketal hydroxyl protected compounds of morphinan derivatives and preparation method thereof, and to a method for preparing corresponding alkylated morphinan derivatives by using the ketal hydroxyl protected compounds as intermediates, and more especially to a ketal hydroxyl protected compound of methylnaltrexone as intermediate for preparing methylnaltrexone and a method for preparing methylnaltrexone through said intermediate.
Owner:CHONGQING PHARMA RES INST
Remedy for relieving skin troubles comprising morphinan derivative or pharmacologically acceptable acid addition salt thereof as the active ingredient
InactiveCN101848714AGood characterPrevent drynessOrganic active ingredientsCosmetic preparationsMorphinanBULK ACTIVE INGREDIENT
It is intended to provide a therapeutically useful novel drug which exerts a skin moisturizing effect on the skin suffering from functional disorders caused by various factors so as to relieve skin troubles such as dry skin, chapped skin, dullness accompanying horny layer thickening and so on. Namely, a remedy for relieving skin troubles which contains, as the active ingredient, a compound having a specific morphinan skeleton that is typified by a compound (1) represented by the following structural formula (II) or a pharmacologically acceptable acid addition salt thereof.
Owner:TORAY IND INC
Method for therapy of diarrhea-predominant irritable bowel disorders
InactiveUS8058286B2Good effectLittle side effectsBiocideOrganic chemistryIrritable bowelAdditive ingredient
A method for therapy of diarrhea-predominant irritable bowel disorders comprising as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic group or a pharmaceutically acceptable acid addition salt thereof is disclosed. The method for therapy of diarrhea-predominant irritable bowel disorders comprises as an effective ingredient a morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as N-(17-cyclopeopylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10).
Owner:TORAY IND INC
Morphinan derivative
ActiveUS20180057493A1Good effectSuppression of gastrointestinal motilityOrganic active ingredientsSenses disorderHydrogenHeteroatom
A morphinan derivative represented by the following general formula (I):(wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.,R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group,Y binds to a carbon atom as a ring-constituting atom of R2,R3, R4, and R5 represent hydrogen; hydroxy, etc.,R6a and R6b represent hydrogen, etc.,R7 and R8 represent hydrogen, etc.,R9 and R10, which are the same or different, represent hydrogen, etc.,X represents O or CH2, andY represents C(═O)),a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.
Owner:NIPPON CHEMIPHAR CO LTD
Analgesic and methods of treating pain
An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as compound 1:
Owner:TORAY IND INC
Glycyrrhizinates of morphinan derivatives
InactiveUS20130012464A1Overcome limitationsEliminate side effectsBiocideNervous disorderVascular diseaseHepatic Diseases
The present invention provides a pharmaceutically acceptable compound, a pharmaceutical composition comprising the above-mentioned pharmaceutically acceptable compound. The pharmaceutically acceptable compound provided by the present invention is a salt of a basic group-containing morphinan derivative and a carboxyl group-containing glycyrrhizinic acid and has the ability to be used to manufacture medicaments for treating and/or preventing cough, ameliorating pains, treating respiratory system diseases, treating cardiovascular diseases and treating liver diseases.
Owner:STANDARD CHEM & PHARMA
Morphinan Derivatives with High Oral Bioavailability
InactiveUS20150094325A1Improve oral bioavailabilityImprove bioavailabilityBiocideNervous disorderDiseaseAlcohol
The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction.
Owner:ALKERMES PHARMA IRELAND LTD
Morphinan derivative
InactiveUS20210371422A1Superior antidepressive effect effectSuperior effect and anxiolytic effectSenses disorderNervous disorderMorphineMorphinan
A compound represented by the following general formula (I),
- wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, or the like,
- R2 represents a 4- to 7-membered saturated heterocycle containing one or two heteroatoms which may be the same or different and are selected from N, O, and S, and two or more carbon atoms as ring-constituting atoms, the heterocycle may be substituted with a substituent such as an oxo group,
- R2 binds to Y via a carbon atom as a ring-constituting atom of R2,
- R3, R4, and R5, which are the same or different, represent hydrogen; hydroxy; or the like,
- R6a and R6b, which are the same or different, represent hydrogen or the like,
- R7 and R8, which are the same or different, represent hydrogen or the like,
- R9 and R10, which are the same or different, represent hydrogen or the like,
- X represents O or CH2, and
- Y represents C(═O) or the like),
- a tautomer of the compound, a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic, an antidepressant, or the like.
Owner:NIPPON CHEMIPHAR CO LTD
6,7-unsaturated-7-carbamoyl substituted morphinan derivative
ActiveCN101228172BAvoid vomitingEliminate side effectsOrganic active ingredientsNervous disorderAcyl groupMorphine
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 R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptable salt, or a solvate thereof is provided.
Owner:SHIONOGI & CO LTD
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