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30 results about "NK-1 Receptors" patented technology
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Tachykinin NK1 receptor, often referred to as NK1 receptor, is a member of family 1 (rhodopsin-like) of G protein-coupled receptors and binds to the Gαq protein. NK1 receptor consists of 407 amino acid residues, and it has a molecular weight of 58.000.
Lithium combinations, and uses related thereto
InactiveUS20050233010A1Prevent precipitating manic episodeLessening and preventing riskBiocideNervous disorderPsychoactive drugAdrenergic antagonist
The present invention relates to combinatorial therapies for treating anxiety, depression or psychotic conditions using a lithium salt and a psychoactive drug selected from the group consisting of serotonin reuptake inhibitor, a 5HT2 receptor antagonist, an anticonvulsant, a norepinephrine reuptake inhibitor, an α-adrenoreceptor antagonist, an NK-3 antagonist, an NK-1 receptor antagonist, a PDE4 inhibitor, an Neuropeptide Y5 Receptor Antagonists, a D4 receptor antagonist, a 5HT1A receptor antagonist, a 5HT1D receptor antagonist, a CRF antagonist, a monoamine oxidase inhibitor, a sedative-hypnotic drug, and an atypical antipsychotic.
Owner:NOVEN THERAPEUTICS
Use of NK-1 receptor antagonists in pruritus
The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.
Owner:VYNE THERAPEUTICS INC
Use of nk-1 receptor antagonist serlopitant in pruritus
Owner:VYNE THERAPEUTICS INC
Disulfide conjugated cell toxins and methods of making and using them
The invention pertains to the discovery of novel disulfide linked cell toxins which can ablate NK-1 receptor expressing cells. These toxins are used as pharmaceutical compositions for the ablation of NK1 receptor expressing cells and comprise a substance P (SP)-Pseudomonas exotoxin disulfide linked conjugate. The invention also includes methods of making and using these toxins and pharmaceutical compositions.
Owner:THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SE
Serotonin transporter (sert) inhibitors for the treatment of depression and anxiety
InactiveUS20070232652A1Keep it workingGood effectBiocideNervous disorderANXIETY COMPLEXSerotonin transporter
The present invention relates to trans-derivatives of formulawherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof.The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and / or in the treatment of anxiety.
Owner:F HOFFMANN LA ROCHE INC
Dietary Composition and Method for Preventing, Reducing, Alleviating or Treating Idiopathic Vomiting
ActiveUS20140271943A1Preventing and reducing and alleviating and treating idiopathic vomitingBiocideFodderMedicineNK-1 Receptors
The present invention relates to compositions containing plant materials or extracts with inhibitory effect on a 5-HT3a and / or NK-1 receptor for preventing or treating idiopathic vomiting.
Owner:MARS INC
Tachykinin receptor antagonists
The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
Owner:ELI LILLY & CO
Treatment of corneal neovascularization
There is provided inter alia a compound which is an NK-1 receptor antagonist for use in the treatment or prevention of CNV. There is also provided a compound which is an NK-1 antagonist for use in the treatment of chemical burns of the eye particularly alkali burns of the eye. There is also provided a pharmaceutical composition for topical administration to the eye comprising an NK-1 antagonist and an antibiotic agent.
Owner:IRBM SCI PARK
P substance peptide probe capable of specific recognition of neurokinin-1 receptor protein, and preparation and application thereof
InactiveCN104744568AImprove bindingHigh sensitivityTachykininsPeptide preparation methodsFluorescenceKinin
The invention provides a P substance peptide probe capable of specific recognition of a neurokinin-1 receptor protein. the P substance peptide probe is a polypeptide dimer or a polypeptide polymer, the monomer is formed by a P substance amino acid sequence MLGFFQQPKPR, a bifunctional chelating group, a fluorescence group and a terpyridyl group connected through lysine. The novel peptide probe is used for the preparation of a polypeptide dimer and polypeptide polymer with function of diagnosing multi tumors. The polypeptide dimer and polypeptide polymer marks metal Gd<3+> to a polypeptide molecule by the bifunctional chelating group; the marked P substance peptide probe and the NK-1 receptor protein specifically bind and concentrate to the tumor site in vivo; and magnetic imaging and optical imaging technology are utilized for detection of the neurokinin-1 receptor protein to improve the sensitivity of the detection.
Owner:EAST CHINA UNIV OF SCI & TECH
Composition and method for preventing, reducing, alleviating, or treating idiopathic vomiting
Owner:MARS INC
Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer
Owner:SERVICIO ANDALUZ DE SALUD (SAS)
Novel neurokinin 1 receptor antagonist compounds ii
InactiveCN105579456AOrganic active ingredientsOrganic chemistryNeurokinin-1 Receptor AntagonistsNK1 receptor antagonist
The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.
Owner:LEO PHARMA AS
Serotonin transporter (SERT) inhibitors for the treatment of depression and anxiety
InactiveUS7872022B2High activityDosage of the drug can therefore be reducedBiocideNervous disorderANXIETY COMPLEXSerotonin transporter
Owner:F HOFFMANN LA ROCHE INC
Benzylamine derivative
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.
Owner:ZERIA PHARMA
Antagonizing nk-1 receptors inhibits consumption of substances of abuse
InactiveUS20060205724A1Reduces and block activityGuaranteed detection effectNervous disorderBiological testingNK1 receptor antagonistNK-1 Receptors
This invention pertains to the surprising discovery that administration of one or more NK1 receptor antagonists to a mammal can inhibit self-administration of a substance of abuse (e.g. alcohol). In one embodiment, this invention provides a method of inhibiting or reducing self-administration of a substance of abuse by a mammal. The method involves administering to the mammal an NK1 receptor antagonist in a concentration sufficient to reduce self-administration of a substance of abuse and / or craving for a substance of abuse (e.g. ethanol).
Owner:RGT UNIV OF CALIFORNIA
Serotonin transporter (SERT) inhibitors for the treatment of depression and anxiety
InactiveUS20110105561A1High activityDosage of the drug can therefore be reducedBiocideNervous disorderANXIETY COMPLEXSerotonin transporter
The present invention relates to trans-derivatives of formulawherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof.The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and / or in the treatment of anxiety.
Owner:F HOFFMANN LA ROCHE INC
Benzylamine derivative
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof
Owner:ZERIA PHARMA
Novel neurokinin 1 receptor antagonist compounds ii
InactiveUS20160207930A1High metabolic clearanceImprove securityBiocideOrganic chemistryNeurokinin-1 Receptor AntagonistsHalogen
The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4) hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.
Owner:LEO PHARMA AS
Dietary composition and method for preventing, reducing, alleviating or treating idiopathic vomiting
ActiveUS10441623B2Preventing and reducing and alleviating and treating idiopathic vomitingFodderDigestive systemMedicineNK-1 Receptors
The present invention relates to compositions containing plant materials or extracts with inhibitory effect on a 5-HT3a and / or NK-1 receptor for preventing or treating idiopathic vomiting.
Owner:MARS INC
Substance p polypeptide probe specifically recognizing neurokinin-1 receptor protein and its preparation and application
InactiveCN104744568BImprove bindingHigh sensitivityTachykininsPeptide preparation methodsFluorescenceMetal chelate
The present invention provides a substance P polypeptide probe that specifically recognizes neurokinin-1 receptor protein. The substance P polypeptide probe is a polypeptide dimer or a polypeptide polymer, and its monomer consists of a substance P amino acid sequence MLGFFQQPKPR, A bifunctional chelating group, a fluorescent group and a terpyridine group are connected through lysine. The polypeptide probe is a new type of polypeptide dimer and polypeptide polymer used to prepare various tumor diagnostic functions. The polypeptide dimer and polypeptide polymer label metal Gd3+ to the polypeptide through a bifunctional chelating group Molecularly, the labeled Substance P polypeptide probe in vivo specifically binds to the NK-1 receptor protein and concentrates on the tumor site, and uses magnetic imaging and optical imaging techniques to detect the neurokinin-1 receptor protein to improve detection sensitivity sex.
Owner:EAST CHINA UNIV OF SCI & TECH
NK-1 Receptor Mediated Delivery of Agents to Cells
Provided herein are conjugates including a targeting vehicle coupled to an agent. The targeting vehicle includes a tachykinin receptor ligand and a reactive moiety. Conjugates including a tachykinin receptor ligand attached to an antibody or fragment thereof that is specific for an intracellular target are also provided. Also provided are methods of delivering agents to cells expressing tachykinin receptors, methods of delivering antibodies or fragments thereof to an intracellular extra-endosomal target, and methods of arresting cell growth or introducing cell death of a cancer cell.
Owner:UNIVERSITY OF CHICAGO
Targeted nk1 receptor antagonists and their application in the treatment of chemotherapy-induced nausea and vomiting
ActiveCN109384712BExcellent NK1 receptor antagonist activityExcellent receptor antagonist activityOrganic chemistryDigestive systemNausea sicknessNK1 receptor antagonist
Owner:北京宽厚医药科技有限公司
NK1 receptor antagonist composition
ActiveUS8426386B2Improve securityVarious symptomOrganic active ingredientsCosmetic preparationsNK1 receptor antagonistTherapeutic effect
An NK1 receptor antagonist composition of the present invention uses maltooligosaccharide having an NK1 receptor antagonistic activity as an active ingredient. A suitable amount of the maltooligosaccharide to be blended in the NK1 receptor antagonist composition of the present invention is 0.000001 to 70% by weight. The NK1 receptor antagonist composition of the present invention is prepared for use into various forms of external agents, internal medicines, foods and beverages by blending various materials as the ingredients other than the active ingredient. The NK1 receptor antagonist composition of the present invention has high safety for being used for pharmaceuticals and has satisfactory therapeutic effects.
Owner:LION CORP
Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer
InactiveUS20160317544A1Shrink tumorAvoid developmentOrganic active ingredientsHeavy metal active ingredientsNK1 receptor antagonistNK-1 Receptors
Use of the non-peptide NK1 receptor antagonist, preferably Aprepitant, for the treatment of cancer in predetermined doses. The present invention also describes pharmaceutical compositions comprising said agents, alone or in combination with at least one other active principle, for the treatment of cancer
Owner:SERVICIO ANDALUZ DE SALUD (SAS)
Peptides comprising opioid receptor agonist and nk1 receptor antagonist activities
PendingUS20220024978A1Good analgesic effectHigh activityNervous disorderPeptide/protein ingredientsNK1 receptor antagonistNK-1 Receptors
The present invention relates generally to a compound having both agonist activity at opioid receptor(s) and antagonist activity at NK1 receptor, and methods for producing and using the same. This combination of activities provides several synergistic and / or beneficial effects such as enhanced potency in analgesic effect and reduction or inhibition of tolerance.
Owner:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA
NK-1 Receptor Mediated Delivery of Agents to Cells
Provided herein are conjugates including a targeting vehicle coupled to an agent. The targeting vehicle includes a tachykinin receptor ligand and a reactive moiety. Conjugates including a tachykinin receptor ligand attached to an antibody or fragment thereof that is specific for an intracellular target are also provided. Also provided are methods of delivering agents to cells expressing tachykinin receptors, methods of delivering antibodies or fragments thereof to an intracellular extra-endosomal target, and methods of arresting cell growth or introducing cell death of a cancer cell.
Owner:UNIVERSITY OF CHICAGO
Nk1 receptor antagonist composition
ActiveUS20110039801A1Improve securityVarious symptomBiocideCosmetic preparationsNK1 receptor antagonistTherapeutic effect
An NK1 receptor antagonist composition of the present invention uses maltooligosaccharide having an NK1 receptor antagonistic activity as an active ingredient. A suitable amount of the maltooligosaccharide to be blended in the NK1 receptor antagonist composition of the present invention is 0.000001 to 70% by weight. The NK1 receptor antagonist composition of the present invention is prepared for use into various forms of external agents, internal medicines, foods and beverages by blending various materials as the ingredients other than the active ingredient. The NK1 receptor antagonist composition of the present invention has high safety for being used for pharmaceuticals and has satisfactory therapeutic effects.
Owner:LION CORP
Nk1 receptor antagonist
InactiveCN108368062AExcellent NK
<sub>1</sub>
Receptor antagonist activityExcellent receptor antagonist activityOrganic active ingredientsOrganic chemistryNK1 receptor antagonistNK-1 Receptors
The present invention addresses the problem of providing a novel compound which has NK1 receptor antagonistic activity and which is useful in the prevention and treatment of nausea and vomiting accompanying the administration of antineoplastic agents. The present invention pertains to a compound represented by formula (I) (in the formula, W represents a fluorine atom or the like, ring A representsa cycloalkyl or the like, X1 represents CH or N, R represents a methyl group or the like, Y represents a number from 0 to 2, and U1, U2, and U3 each independently represent a single bond or the like), or a pharmacologically acceptable salt thereof. This compound or pharmacologically acceptable salt thereof has excellent NK1 receptor antagonistic activity and is useful as a prophylactic or therapeutic agent for nausea and vomiting accompanying the administration of antineoplastic agents.
Owner:KISSEI PHARMA
Preparation method of NK1 receptor antagonist
ActiveCN113582982AImprove crystallization efficiencyShort reaction timeOrganic chemistryBulk chemical productionNK1 receptor antagonistNK-1 Receptors
The invention discloses a preparation method of an NK1 receptor antagonist. According to the invention, chiral resolution adopts a mixed solvent, CaCl2 is added for a reaction in an alkaline environment, CaCl2 does not participate in the reaction but needs to be added in advance for better devitrification, water is added for quenching after the reaction is finished, and CaCl2 is dissolved at the same time, so devitrification efficiency is further improved; and then 5-hydroxymethyl-2,4-dihydro-[1,2,4]triazin-3-one is used as a raw material for synthesis of aprepitant under the catalysis of DBU at room temperature.
Owner:SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +2
Method of treatment with tradipitant
Owner:VANDA PHARMA INC +1
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