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42 results about "Receptor antagonist activity" patented technology
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Interacts with receptors to reduce the action of another ligand, the agonist. [GOC:ceb, ISBN:0198506732]
Tetrahydroisoquinoline or isochroman compounds
This invention provides the compounds of formula (I): or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X1 is NH; R1, R2, R4 through R6 and R7 through R11 are all hydrogen; R3 is hydroxy; X2 and X3 are methylene; X4 is a bond; and X5 is a carbon atom, and the like. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Owner:ITO FUMITAKA +3
Method of treating mast cell activation-induced diseases with a proteoglycan
InactiveUS6689748B1Decrease in urinaryBiocidePeptide/protein ingredientsInflammatory Bowel DiseasesInterstitial cystitis
The invention provides a method for preventing and treating the harmful biological effects of biochemicals secreted from activated mast cells in the organism of warm blooded animals and more especially human beings, said effects being associated with allergy (including but not limited to allergic conjunctivitis, allergic rhinitis, allergic otitis, asthma, allergic uticaria, food allergy and atopic dermatitis), hyperproliferative diseases such as leukemia and systemic mastocytosis, interstitial cystitis, inflammatory bowel disease, irritable bowel syndrome, osteoporosis and scleroderma. The method consists in administering to said animals and especially to human beings an effective amount of a proteoglycan such as chondroitin sulfate with mast cell secretion inhibitory activity, alone or in combination with one or more synergistic adjuvants such those belonging to the class of flavonoids or compounds with histamine-1 receptor antagonist activity.
Owner:THETA BIOMEDICAL CONSULTING & DEVMENT
Method of treating lower urinary tract disorders
The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.
Owner:EDUSA PHARMA
Protein based tumor necrosis factor-receptor variants for the treatment of TNF related disorders
The invention relates to novel proteins with TNF-receptor antagonist activity and nucleic acids encoding these proteins. The invention further relates to TNF-receptor proteins with reduced immunogenicity and the use of these novel proteins in the treatment of TNF related disorders.
Owner:XENCOR INC
Disintegrin variants and pharmaceutical uses thereof
InactiveUS20080188413A1Treatment and prevention of osteoporosisIncreased formationSenses disorderAntipyreticDiseaseDiabetic retinopathy
Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and / or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and / or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and / or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.
Owner:NAT CHENG KUNG UNIV +1
Method of treating lower urinary tract disorders
The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.
Owner:DYNOGEN PHARM INC
Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as ORL1-receptor antagonists
Owner:PFIZER INC
Methods of decreasing intestinal motility
The invention relates to a method of decreasing intestinal motility in a subject in need of treatment. The method comprises administering to the subject a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of decreasing intestinal motility in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. In certain embodiments, the subject is a subject with a functional bowel disorder, such as IBS, functional abdominal bloating, or functional diarrhea.
Owner:EDUSA PHARMA
Heteroaromatic methyl cyclic amine derivative
ActiveCN104350053AHas OX receptor antagonistic activityOrganic active ingredientsNervous disorderHuntingtons choreaChoreathetosis
A heteroaromatic methyl cyclic amine derivative represented by formula (IA) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.
Owner:TAISHO PHARMACEUTICAL CO LTD
Method of treating functional bowel disorders
The invention relates to a method of treating functional bowel disorders in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating a functional bowel disorder in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. The functional bowel disorders which can be treated according to the method of the invention include IBS, functional abdominal bloating, functional constipation and functional diarrhea.
Owner:DYNOGEN PHARM INC
Disintegrin variants and their use in treating osteoporosis-induced bone loss and angiogenesis-related diseases
InactiveUS7943728B2Avoid problemsIncreased formationSenses disorderPeptide/protein ingredientsDiseaseDiabetic retinopathy
Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and / or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and / or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and / or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.
Owner:NAT CHENG KUNG UNIV +1
Alpha-(aryl-or heteroaryl-methyl)-beta piperidino propanamide compounds as ORL1-receptor antagonists
Owner:PFIZER INC
New alkyl esters of cyclic amino alcohols with muscarinic m3 receptor antagonist activity, useful for treating e.g. chronic bronchial obstruction, asthma and overactive bladder
Owner:ASTRAZENECA AB
Dual-acting benzoimidazole derivative and their use as antihypertensive agents
The invention relates to compounds having the formula: (I) wherein Ar, r, n, X, R2, R2', R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and aprocess and intermediates for preparing such compounds.
Owner:THERAVANCE INC
Alpha-(Aryl-or Heteroaryl-Methyl)-Beta-Piperidino Propanamide Compounds as Orl-1-Receptor Antagonists
This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; —X—Y— represents —CH2O— or the like; and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Owner:PFIZER INC
Dual-acting benzoimidazole antihypertensive agents
InactiveCN101675036AOrganic active ingredientsOrganic chemistryReceptor antagonist activityEnkephalinase
The invention is directed to compounds having the formula: (I) wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Owner:THERAVANCE INC
Compound, muscarine M receptor antagonist, composition and application
The invention discloses a discovery and application of an acting target of hydroxyl cinnamamide compound separated from solanaceae plants, and particularly relates to a discovery of an acting target of hydroxyl cinnamamide compound N1, N8-bis (dihydrocaffeoyl) spermidine (BDCS for short) and application thereof in spasmolysis drug. Unmarked cell target pharmacology technology finds that the compound has high muscarine M receptor antagonistic activity, dose-effect relationship researches show that dose is dependently antagonistic to DMR response signals caused by acetylcholine and BDCS is a muscarine M receptor antagonist. BDCS and one or more than two of pharmaceutically-acceptable salts of BDCS are used as active ingredients of the muscarine M receptor antagonist. Current researches show that muscarine M receptor is related to diseases like spasm, analgesia, sedation and schizophrenia, so that an efficient novel ligand with the acting target being clear can be provided for related diseases.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as ORL1-receptor antagonists
InactiveUS20050277659A1Reduced inhibitory activityInhibitory activityBiocideNervous disorderArylDisease
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Owner:PFIZER INC
Carboxymethyl piperidine derivative
InactiveUS20160289206A1Excellent NK receptor antagonist activityBlock compoundOrganic active ingredientsOrganic chemistryNausea sicknessHydrogen atom
The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.
Owner:KISSEI PHARMA
Branched chain alkyl heteroaromatic ring derivative
InactiveCN104364238AHas OX receptor antagonistic activityOrganic active ingredientsNervous disorderHuntingtons choreaDisease
A branched chain alkyl heteroaromatic ring derivative represented by formula (Ia) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.
Owner:TAISHO PHARMACEUTICAL CO LTD
Indole derivative and pharmacologically acceptable salt thereof
InactiveCN102498097AOrganic active ingredientsOrganic chemistryAntagonismReceptor antagonist activity
Owner:KISSEI PHARMA
Heterocyclic compound
PendingCN112654627AExcellent aryl hydrocarbon receptor antagonist activityPromote productionOrganic chemistryBlood disorderArylReceptor antagonist activity
Provided is a novel heterocyclic compound having an aryl hydrocarbon receptor antagonist activity and useful for the promotion of platelet production, the compound being represented by the general formula [I]: wherein ring A, ring B, R1, R2, R3, R4, n, and X are as defined above, or a salt thereof.
Owner:OTSUKA PHARM CO LTD
Cyclopeptide luteinizing hormone releasing hormone (LHRH) antagonist derivatives and pharmaceutical use thereof
InactiveCN103524599AGood effectImprove stabilityPeptide/protein ingredientsLuteinising hormone-releasing hormoneDiseaseSexual hormones
The invention relates to cyclopeptide derivatives with luteinizing hormone releasing hormone (LHRH) receptor antagonist activity shown in a general formula I in the specification, a preparation method thereof, pharmaceutical compositions containing the cyclopeptide derivatives and use of the cyclopeptide derivatives in treatment of prostatic cancer, endometrial cancer, ovarian cancer, breast cancer and other sex hormone-dependent diseases associated with reproduction, contraception and the like.
Owner:INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
Alpha-(Aryl-or Heteroaryl-Methyl)-Beta-Piperidinopropanoic Acid Compounds as Orl-1-Receptor Antagonists
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 represents aryl or the like; —X—Y— represents —CH2O— or the like, and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Owner:PFIZER INC
Benzocyclic derivative having b2-receptor agonist activity and m3-receptor antagonist activity and medical use thereof
InactiveUS20190185461A1Organic active ingredientsOrganic chemistryMetaboliteReceptor antagonist activity
A compound represented by general formula (I), or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, a cocrystal, or a prodrug thereof, the preparation method thereof, and use thereof in the manufacture of a medicament for treatment of an airway obstructive disease,wherein the substituents are defined as in the specification.
Owner:SICHUAN HAISCO PHARMA CO LTD
Method of treating parkinson's disease with diarylmethylpiperazine compounds exhibiting delta receptor agonist activity
ActiveUS20070066625A1Avoids the dyskinetic side-effectsOrganic active ingredientsNervous disorderSide effectReceptor antagonist activity
Owner:DMK PHARM CORP
Cyclohexyl pyridine derivative
ActiveUS9708266B2Excellent NKReduced inhibitory activityOrganic active ingredientsOrganic chemistryNausea sicknessHydrogen atom
A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
Owner:KISSEI PHARMA
Disubstituted chalcone oximes having RARy retinoid receptor antagonist activity
Compounds of the formula where the variables have the values described in the specification are antagonists of RARγ retinoid receptors.
Owner:ALLERGAN INC
Method of treating Parkinson's Disease with diarylmethylpiperazine compounds exhibiting delta receptor agonist activity
ActiveUS8642599B2Avoids the dyskinetic side-effectsBiocideNervous disorderSide effectReceptor antagonist activity
Owner:DMK PHARM CORP
Carboxymethyl piperidine derivative
InactiveUS10100030B2Excellent NKBlock compoundOrganic active ingredientsOrganic chemistryNausea sicknessHydrogen atom
The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.
Owner:KISSEI PHARMA
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