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36 results about "COMT inhibitor" patented technology
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A catechol-O-methyltransferase (COMT) inhibitor is a drug that inhibits the enzyme catechol-O-methyltransferase. This enzyme methylates catecholamines such as dopamine, norepinephrine and epinephrine. It also methylates levodopa. COMT inhibitors are indicated for the treatment of Parkinson's disease in combination with levodopa and an aromatic L-amino acid decarboxylase inhibitor (eg. carbidopa or benserazide). The therapeutic benefit of using a COMT inhibitor is based on its ability to prevent the methylation of levodopa to 3-O-methyldopa, thus increasing the bioavailability of levodopa. COMT inhibitors significantly decrease off time in people with Parkinson's disease also taking carbidopa/levodopa.
Methods of treating patients suffering from movement disorders
ActiveUS20060178379A1Reducing and suppressing adverse effectiveness of L-DOPAShorten closing timeBiocideNervous disorderAdenosineDisease patient
Owner:KYOWA HAKKO KIRIN CO LTD
Preparation method of COMT inhibitor 5, 6, 7, 3', 4'-pentamethoxyl isoflavone
InactiveCN101643465AEasy to operateShort reaction timeOrganic active ingredientsOrganic chemistrySulfonyl chlorideFormylation reaction
The invention relates to a preparation method for COMT inhibitor 5, 6, 7, 3', 4'-pentamethoxyl isoflavone, comprising the following steps: mixing 3, 4-dimethoxyphenylacetic acid and oxalyl chloride indichloromethane solution to carry out reflux reaction for 2 to 3 h, and cooling to room temperature; adding 3, 4, 5-trimethoxy sodium phenolate to carry out esterification reaction to carry out Friesrearrangement reaction under the catalysis of Lewis acid boron trifluoride ether; and finally carrying out reaction with DMF with the existence of the Lewis acid boron trifluoride ether; and adding methane sulfonyl chloride to promote Vilsmeier-Haack formylation reaction and subsequent cyclization reaction to obtain light yellow crystals 5, 6, 7, 3', 4'-pentamethoxyl isoflavone. The preparation method has simple and easily available raw materials, simple operation, short reaction time, mild reaction condition, environment protection and high yield of 76 %, and is suitable for industrial production.
Owner:DONGHUA UNIV
Nitrocatechol derivatives as COMT inhibitors
Novel compounds of general formula I are described which have potentially valuable pharmaceutical properties in the treatment of several central and peripheral nervous system dysfunctions.
Owner:BIAL PORTELA & CA SA
New therapy for transthyretin-associated amyloidosis
ActiveUS20140296188A1Acceptable safety profileImprove bioavailabilityBiocideNervous disorderBenzoxazoleGallate
It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of trans-thyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
Owner:SOM INNOVATION BIOTECH
Methods of treating patients suffering from movement disorders
InactiveUS20060148827A1Reducing and suppressing adverse effectiveness of L-DOPAShorten closing timeBiocideNervous disorderAdenosineDisease patient
The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and / or a COMT inhibitor and / or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A2A receptor antagonist singly or together with a dopamine agonist, and / or a COMT inhibitor, and / or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.
Owner:KYOWA HAKKO KIRIN CO LTD
Therapy for transthyretin-associated amyloidosis
ActiveUS9610270B2Acceptable safety profileStrong inhibitory activityNervous disorderKetone active ingredientsBenzoxazoleGallate
It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
Owner:SOM INNOVATION BIOTECH
Pharmaceutical compounds
InactiveUS20090209532A1Improve bioavailabilityProlong the action timeBiocideNervous disorderEnzymeCOMT inhibitor
Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
Owner:ORION CORP
Pharmaceutical compositions comprising levodopa, a dopamine decarboxylase inhibitor and a COMT inhibitor and a method of administration thereof
A pharmaceutical gel composition for intra-intestinal administration is provided and comprises (i) a dopamine replacement agents, (ii) a dopamine decarboxylase inhibitor (DDI), and (iii) a COMT inhibitor.
Owner:LOBSOR PHARM AB
Polypharmacophoric agents
One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.
Owner:MOLECULAR INSIGHT PHARMA
Methods and compositions for the prevention and treatment of genitourinary disorders, including pre-term labor and leiomyomas
InactiveUS20090053207A1Microbiological testing/measurementLibrary screeningCOMT inhibitorUterine disease
The present invention relates to an association between specific polymorphisms of the COMT polypeptide and the development, or risk of developing, preterm labor and uterine diseases and conditions. Disclosed are therapeutic, preventative and diagnostic methods and compositions relating to pre-term labor, uterine diseases and conditions, and ovarian conditions and diseases. In certain embodiments, such methods and compositions involve a COMT inhibitor.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
Methods of treating patients suffering from movement disorders
InactiveUS7727994B2Reducing and suppressing adverse effectiveness of L-DOPAShorten closing timeBiocideNervous disorderDisease patientAdenosine a
Owner:KYOWA HAKKO KIRIN CO LTD
Method of treating postural reflex abnormality caused by parkinson's disease
ActiveUS20140378546A1Raise priorityEffective treatmentBiocideNervous disorderCOMT inhibitorAbnormal postural reflex
The present disclosure relates to a more effective therapeutic agent capable of improving and treating the axial symptoms (particularly freezing of gait symptom) of patients with Parkinson's disease. Such symptoms in patients with Parkinson's disease can be improved and treated by using L-threo-3,4-dihydroxy-phenylserine (DOPS) and a COMT inhibitor in combination together, optionally with an L-DOPA preparation as well. As a result, the axial symptoms difficult to improve with conventional L-DOPA preparations can be treated, and a therapeutic agent and a treatment method are provided for the axial symptoms of patients with Parkinson's disease, particularly those suffering from the disease at a moderate level or higher.
Owner:LUNDBECK NA
New Therapy for Transthyretin-Associated Amyloidosis
ActiveUS20170304243A1Reduce formationInhibition formationNervous disorderKetone active ingredientsBenzoxazoleCOMT inhibitor
It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and / or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
Owner:SOM INNOVATION BIOTECH
Pharmaceutical compounds
Compounds of formula (I), wherein E, G, T, Rd, Re, and Rf are as defined in the disclosure, release levodopa and a COMT inhibitor so that they can be used for the treatment of diseases or conditions, wherein levodopa and inhibition of COMT are indicated to be useful.
Owner:ORION CORPORATION
Polypharmacophoric agents
One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.
Owner:MOLECULAR INSIGHT PHARMA
Catechol O-methyltransferase activity inhibiting compounds
ActiveUS9458128B2Increase concentrationNervous disorderOrganic chemistryCOMT inhibitorMedicinal chemistry
Owner:ORION CORPORATION
COMT (catechol-O-methyltransferase) inhibitor containing hydrazide structure and preparation and application methods thereof
InactiveCN108148010AHas COMT inhibitory effectNervous disorderOrganic chemistryCOMT inhibitorHydrazide
The invention relates to the field of COMT inhibitors, particularly to a COMT inhibitor containing a hydrazide structure, a preparation method of the COMT inhibitor, and application of the COMT inhibitor to preparing schizophrenia treating drugs and the like. The chemical formula of the COMT inhibitor is shown as below, in which R1 is an alkyl selected from C1-C5, R2 is selected from H, an alkyl of C1-C10 or a naphthene of C3-C10.
Owner:FOSHAN SAIWEISI MEDICINE SCI & TECH
Methods of diagnosing leiomyoma by measuring catechol-O-methyltransferase
InactiveUS7960133B2Microbiological testing/measurementLibrary screeningCOMT inhibitorUterine disease
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
Compounds containing hydrazide structure, preparation method and application of compounds
InactiveCN108218796AHas COMT inhibitory effectNervous disorderOrganic chemistryCOMT inhibitorCombinatorial chemistry
The invention relates to the field of COMT (catechol-O-methyltransferase) inhibitors, in particular to compounds containing a hydrazide structure and capable of serving as COMT inhibitors as well as apreparation method and an application of the compounds in preparation of drugs for treating schizophrenia and the like. The compounds have the structure shown in the general formula (I), wherein R isselected from H and C1-C5 alkyl groups.
Owner:FOSHAN SAIWEISI MEDICINE SCI & TECH
Nitrocatechol derivatives as COMT inhibitors
Owner:BIAL PORTELA & CA SA
Process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile
PendingUS20220002232A1Readily availablePreparation from carboxylic acid halidesCarboxylic acid nitrile preparationPhenacylPhenol
The present disclosure relates to a process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile, to use of a compound which is 2-methoxy-5-(4-methylbenzyl)phenol, (3-hydroxy-4-methoxyphenyl)(p-tolyl)methanone, 2-methoxy-5-(4-methylbenzoyl)phenyl 2-chloroacetate, 4-methylbenzoyl chloride, 2-methoxyphenyl 2-chloroacetate or 2-methoxyphenol in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile and to a compound which is 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde dioxime or 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde and use thereof in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile. 4,5-Dihydroxy-2-(4-methylbenzyl)isophthalonitrile is a COMT inhibitor.
Owner:ORION CORPORATION
A method for quantitatively measuring catechol-o-methyltransferase activity and its application
InactiveCN105624268BHigh selectivityReduce testing costsMicrobiological testing/measurementMutantMethyltransferase
A method for quantitatively measuring catechol-O-methyltransferase activity and application thereof belong to the technical field of biomedicine. The method uses 4-acetic acid-7,8-dihydroxycoumarin as the specific probe substrate of COMT enzyme, which can be specifically catalyzed by COMT enzyme to generate 8-methoxy product and display at 520nm Fluorescence signal, the activity of COMT can be quantitatively determined by detecting the change of fluorescence intensity. The invention can not only be used for quantitative evaluation of COMT enzyme activity in biological samples from different sources, but also can be used for rapid screening of COMT inhibitors in vitro and evaluation of their inhibitory ability. The method can be used to quantitatively evaluate the real activity of COMT enzymes in various in vitro biological samples, realize rapid screening of inhibitors and quantitative evaluation of inhibitory ability; it can be used to evaluate the catalytic activity of different species of COMT and COMT mutants with different amino acid sequences , and then evaluate its ability to metabolize catechols. The method of the invention has the advantages of (1) high selectivity, (2) cheap and easy to obtain; (3) high sensitivity and the like.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Specific fluorescent probe for catechol-o-methyltransferase and its application
ActiveCN106467739BHigh selectivityReduce testing costsOrganic chemistryMicrobiological testing/measurementMutantMethyltransferase
A specific fluorescent probe for catechol-O-methyltransferase and its application. The specific probe substrate is 3‑benzothiazole‑7,8‑dihydroxycoumarin (3‑BTD), which can be specifically catalyzed by COMT enzymes to generate 8‑methoxyl products and detect at 520nm A fluorescent signal is displayed at , and the activity of COMT can be quantitatively determined by detecting the change of fluorescence intensity. The probe can not only be used for quantitative evaluation of COMT enzyme activity in biological samples from different sources, but also can be used for rapid screening of COMT inhibitors in vitro and evaluation of their inhibitory ability. This method can be used to quantitatively evaluate the real activity of COMT enzyme in various in vitro biological samples, realize rapid screening of inhibitors and quantitative evaluation of inhibitory ability; it can be used to evaluate the catalytic activity of different species of COMT and COMT mutants with different amino acid sequences , and then evaluate its ability to metabolize catechols. It has the advantages of high sensitivity, high accuracy, strong anti-environmental interference ability, easy high-throughput detection and inhibitor screening.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
COMT inhibitors with terminal olefinic bond and hydrazide structures as well as preparation method and use of COMT inhibitors
InactiveCN107935953AHas COMT inhibitory effectNervous disorderOrganic chemistryCOMT inhibitorCombinatorial chemistry
The invention belongs to the technical field of COMT inhibitors, and in particular relates to COMT inhibitors with terminal olefinic bond and hydrazide structures as well as a preparation method of the COMT inhibitors and application of the COMT inhibitors to preparation of medicines for treating schizophrenia, and the like. The general formula (I) of the COMT inhibitors is described in the description.
Owner:FOSHAN SAIWEISI MEDICINE SCI & TECH
Pharmaceutical compounds
InactiveUS20110086852A2Improve bioavailabilityProlong the action timeBiocideNervous disorderCOMT inhibitorDrug compound
Compounds of formula (I), wherein R1-R4, X, Y and Z are as defined in claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
Owner:ORION CORPORATION
COMT inhibitor comprising terminal olefinic bond and hydrazide structure and application of COMT inhibitor
InactiveCN108129406AHas COMT inhibitory effectNervous disorderOrganic chemistryCOMT inhibitorCombinatorial chemistry
The invention relates to the field of COMT inhibitors, and particularly relates to a COMT inhibitor comprising a terminal olefinic bond and a hydrazide structure, a preparation method of the COMT inhibitor, and application of the COMT inhibitor to preparation of medicines for treating schizophrenia and the like.
Owner:FOSHAN SAIWEISI MEDICINE SCI & TECH
Catechol o-methyltransferase activity inhibiting compounds
ActiveUS20150218124A1Improved levodopa concentrationIncrease concentrationBiocideNervous disorderCOMT inhibitorMedicinal chemistry
Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.
Owner:ORION CORPORATION
First-class phenylmethylamine triazine structural COMT inhibitor, as well as preparation method and application thereof
InactiveCN108191783AHas COMT inhibitory effectNervous disorderOrganic chemistryCOMT inhibitorHalogen
The invention relates to the field of COMT inhibitors, specifically to a first-class phenylmethylamine triazine structural COMT inhibitor as well as a preparation method and application thereof to preparation of drugs for treating schizophrenia. The formula is shown in the description, wherein R is selected from an alkyl group and halogen substituent of H and C1-C5.
Owner:FOSHAN SAIWEISI MEDICINE SCI & TECH
Nitrocatechol derivatives as comt inhibitors
Novel compounds of general formula I are described which have potentially valuable pharmaceutical properties in the treatment of several central and peripheral nervous system dysfunctions.
Owner:BIAL PORTELA & CA SA
Method of treating postural reflex abnormality caused by parkinson's disease
ActiveUS9364453B2Symptoms improvedImprove effectivelyNervous disorderNitrile/isonitrile active ingredientsCOMT inhibitorAbnormal postural reflex
Owner:LUNDBECK NA
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