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950results about "Isotope introduction to heterocyclic compounds" patented technology
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Method for deuteration of a heterocyclic ring
ActiveUS7517990B2Isotope introduction to heterocyclic compoundsSugar derivativesNickel catalystHydrogen atom
The present invention relates to a method for deuteration of a heterocyclic ring, which comprises subjecting a compound having a heterocyclic ring to sealed refluxing state in a deuterated solvent in the presence of an activated catalyst selected form a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. In accordance with a method of the present invention, a hydrogen atom belonging to a heterocyclic ring of a compound having a heterocyclic ring can be very efficiently deuterated because temperature of deuteration reaction can be maintained at higher than boiling point of the solvent.Further, a method for deuteration of the present invention can be applied widely to deuteration of various compounds having a heterocyclic ring which are liable to decomposition under supercritical conditions or acidic conditions, leading to industrial and efficient deuteration of a compound having a heterocyclic ring.
Owner:FUJIFILM WAKO PURE CHEM CORP
Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors](https://images-eureka.patsnap.com/patent_img/78e0b760-3b4b-4848-b642-2e00beb09f2a/US20070135461A1-20070614-C00001.png "Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors")
![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors](https://images-eureka.patsnap.com/patent_img/78e0b760-3b4b-4848-b642-2e00beb09f2a/US20070135461A1-20070614-C00002.png "Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors")
![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors](https://images-eureka.patsnap.com/patent_img/78e0b760-3b4b-4848-b642-2e00beb09f2a/US20070135461A1-20070614-C00003.png "Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors")
Owner:INCYTE HLDG & INCYTE
HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](https://images-eureka.patsnap.com/patent_img/9ca91ab9-beda-49e3-8a59-55336dec4de6/US20090181959A1-20090716-C00001.png "HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS")
![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](https://images-eureka.patsnap.com/patent_img/9ca91ab9-beda-49e3-8a59-55336dec4de6/US20090181959A1-20090716-C00002.png "HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS")
![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](https://images-eureka.patsnap.com/patent_img/9ca91ab9-beda-49e3-8a59-55336dec4de6/US20090181959A1-20090716-C00003.png "HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS")
Owner:INCYTE HLDG & INCYTE
Modulators of ATP-binding cassette transporters
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Owner:VERTEX PHARMA INC
Gpr120 receptor agonists and uses thereof
InactiveUS20110313003A1Promote insulin secretionLowering blood-glucoseBiocideIsotope introduction to heterocyclic compoundsDiseasePhysiology
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Owner:CYMABAY THERAPEUTICS
Imaging agents for detecting neurological disorders
ActiveUS20100239496A1Isotope introduction to heterocyclic compoundsNervous disorderImaging agentMethod of images
Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and / or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
Owner:ELI LILLY & CO
Deuterated CFTR potentiators
This invention relates to compounds of Formula I:and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
Owner:VERTEX PHARMA EURO
Modulators of ATP-binding cassette transporters
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Owner:VERTEX PHARMA INC
2,6-dioxo-3-deutero-piperdin-3-yl-isoindoline compounds
The present application describes 2-(2′,6′-dioxo-3′-deutero-piperidin-3′-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Owner:DEUTERX
Method for preparation of organofluoro compounds in alcohol solvents
InactiveUS20100113763A1Inhibition formationReduced responseIsotope introduction to heterocyclic compoundsIn-vivo radioactive preparationsAlcoholIsotope
The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound [18F]florbetaben or [18F]AV-45 having <Chemistry Formula 11> and <Chemistry Formula 12>, respectively, by reacting fluorine salt containing radioactive isotope fluorine-18 with alkyl halide or alkyl sulfonate in the presence of alcohol of Chemistry Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.
Owner:FUTURECHEM +1
Opsin-binding ligands, compositions and methods of use
InactiveUS20110003784A1Prevent regenerationPrevent and slow formationBiocideSenses disorderOpsin bindingProtein C
Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
Owner:BIKAM PHARMA
Organic compounds
ActiveUS9745300B2Strong therapeutic activitySide effect can be reduced and minimizedOrganic active ingredientsIsotope introduction to heterocyclic compoundsDisease5-HT3 receptor
The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.
Owner:INTRA CELLULAR THERAPIES INC
Imaging Agents for Detecting Neurological Dysfunction
ActiveUS20120302755A1Isotope introduction to heterocyclic compoundsIn-vivo radioactive preparationsCarbazoleMammal
Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
Owner:ELI LILLY & CO
Compound for organic electronic element, organic electronic element using the same, and an electronic device thereof
ActiveUS20170125689A1Improve in luminescence efficiency and stability and lifespanImprove luminous efficiencyIsotope introduction to heterocyclic compoundsSolid-state devicesElectronic componentOrganic chemistry
Provided are a compound of Formula 1 and an organic electric element including a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode and comprising the compound, the element showing improved luminescent efficiency, stability, and life span.
Owner:DUK SAN NEOLUX
Aryl Substituted Indoles and Their Use as Blockers of Sodium Channels
The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
Owner:PURDUE PHARMA LP
Indole derivatives and use thereof
ActiveUS20150284383A1BiocideIsotope introduction to heterocyclic compoundsMedicinal chemistryBlockade
The Invention provides indole derivatives of Formula I:and pharmaceutically acceptable salts and solvates thereof, wherein R1e, R1f, A, X, Y, Z, and W4 are defined as set forth in the specification. The Invention also provides the use of compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat pain. In certain embodiments, the Compounds of the Invention are effective in treating a disorder responsive to blockade of one or more sodium channels.
Owner:PURDUE PHARMA LP
Organic compounds
ActiveUS20170183350A1To promote metabolismImproves in vitro hepatic microsome stabilityOrganic active ingredientsNervous disorderDisease5-HT3 receptor
The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.
Owner:INTRA CELLULAR THERAPIES INC
Deuterated cftr potentiators
This invention relates to compounds of Formula I:and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
Owner:VERTEX PHARMA EURO
Pyridine Compounds as Sodium Channel Blockers
The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
Owner:PURDUE PHARMA LP
Substituted isoindoline-1,3-dione derivatives
This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
Owner:SUN PHARMA IND INC
Analogs of cocaine
The invention provides a compound of formula (I):wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.
Owner:GEORGETOWN UNIV
Organic compounds
ActiveUS10077267B2Similar biological activityTo promote metabolismOrganic active ingredientsIsotope introduction to heterocyclic compoundsDisease5-HT4 receptor
The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.
Owner:INTRA CELLULAR THERAPIES INC
Method for deuteration or tritiation of heterocyclic ring
ActiveUS20060025596A1Isotope introduction to heterocyclic compoundsSugar derivativesDecompositionPalladium catalyst
The present invention relates to a method for deuteration of a heterocyclic ring, which comprises subjecting a compound having a heterocyclic ring to sealed refluxing state in a deuterated solvent in the presence of an activated catalyst selected form a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. In accordance with a method of the present invention, a hydrogen atom belonging to a heterocyclic ring of a compound having a heterocyclic ring can be very efficiently deuterated because temperature of deuteration reaction can be maintained at higher than boiling point of the solvent. Further, a method for deuteration of the present invention can be applied widely to deuteration of various compounds having a heterocyclic ring which are liable to decomposition under supercritical conditions or acidic conditions, leading to industrial and efficient deuteration of a compound having a heterocyclic ring.
Owner:FUJIFILM WAKO PURE CHEM CORP
Substituted pyridazinone compound
ActiveCN109574995AIsotope introduction to heterocyclic compoundsMetabolism disorderDiseaseThyroid hormones
The invention provides a pharmaceutical composition of a substituted pyridazinone compound, and application thereof. The substituted pyridazinone compound is a compound as shown in formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvent compound, crystalline form, stereoisomer or isotopic variant thereof. The compound, namely a THR-beta agonist, can be used for treating and / or preventing diseases regulated by thyroid hormone analogs.
Owner:SHENZHEN TARGETRX INC
Deuterated baricitinib
ActiveUS9540367B2Organic active ingredientsIsotope introduction to heterocyclic compoundsBiochemistryBaricitinib
Owner:SUN PHARMA IND INC
Pyridine compounds as sodium channel blockers
The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
Owner:PURDUE PHARMA LP
Compounds useful as inhibitors of atr kinase
ActiveUS20150158872A1Organic active ingredientsIsotope introduction to heterocyclic compoundsKinase inhibitionDisease cause
The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I-A or I-B:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC
Analogs of cocaine
InactiveUS20020055521A1BiocideIsotope introduction to heterocyclic compoundsDiseaseTherapy drug addiction
The invention provides a compound of formula (I): wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.
Owner:GEORGETOWN UNIV
Compounds for Treatment of Complement Mediated Disorders
ActiveUS20180022767A1Dampen and inhibit detrimental complement activitySenses disorderNervous disorderDiseaseReperfusion injury
Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
Owner:ACHILLION PHARMA INC
Compositions, methods, and systems for the synthesis and use of imaging agents
ActiveUS20140328756A1Eliminate needIsotope introduction to heterocyclic compoundsRadioactive preparation carriersImaging agentCardiac blood vessel
The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
Owner:LANTHEUS MEDICAL IMAGING INC
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