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38 results about "Proteinase-Activated Receptors" patented technology
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Protease-activated receptors are a subfamily of related G protein-coupled receptors that are activated by cleavage of part of their extracellular domain. They are highly expressed in platelets, and also on endothelial cells, myocytes and neurons.
Compositions and methods comprising proteinase activated receptor antagonists
InactiveUS20060063930A1Minor side effectsAntibacterial agentsSenses disorderAngiogenesis growth factorBiology
Compositions and methods comprising proteinase activated receptor antagonists are provided. More particularly, the present invention relates to the use of proteins, peptides and molecules that bind to proteinase activated receptor 2, and inhibit the processes associated with the activation of that receptor. More specifically, the present invention provides novel compositions and methods for the treatment of disorders and diseases such as those associated with abnormal cellular proliferation, angiogenesis, inflammation and cancer.
Owner:ENTRE MED INC
PAR (Protease Activated Receptor)-1 antagonist as well as preparation method and application of PAR-1 antagonist
InactiveCN104086501AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, a preparation method of the PAR-1 antagonist, a pharmaceutical composition containing the PAR-1 antagonist and an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.
Owner:王佳
PAR (Protease Activated Receptor)-1 antagonist and application thereof
The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, wherein a benzene ring at one side of N-morpholinyl is substituted by ethyoxyl, and a benzene ring at the other side of N-morpholinyl is substituted by dimethoxyl. The invention also relates to an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.
Owner:JILIN BAINIAN HANKE PHARM CO LTD
EGFR and PAR2 Regulation of Intestinal Permeability
InactiveUS20120107329A1Inhibition releaseReduce penetrationOrganic active ingredientsMicrobiological testing/measurementAutoimmune conditionAllergy
The present invention provides methods for diagnosing and treating an immune-mediated disease, e.g., an autoimmune disease, an allergy or an inflammatory disease. Diagnosis is made by detecting a heterozygous or homozygous genotype of haptoglobin 2 or by detecting and quantifying pre-haptoglobin 2 mRNA or protein. After diagnosis, the disease may be treated by decreasing cell permeability leading to increased transepithelial electrical resistance, for example, by administering an antibody directed against single chain zonulin thereby inhibiting epidermal growth factor receptor and inhibiting proteinase-activated receptor 2 (PAR2).
Owner:UNIV OF MARYLAND
Health food or pharmaceutical composition comprising chestnut shell extract
InactiveCN102458156AEasily damagedEnhanced inhibitory effectSugar food ingredientsVitamin food ingredientsPrurigoMedicine
The present invention relates to a health food or pharmaceutical composition for alleviating or suppressing pruritus, comprising chestnut shell extract as an active ingredient. In one example of the present invention, the chestnut shell extract comprised in the health food or pharmaceutical composition of the present invention can suitably be used as the active ingredient of a health food or pharmaceutical composition for alleviating or suppressing pruritus as it has been confirmed that it can exhibit an outstanding effect in alleviating or suppressing pruritus by suppressing the activity of proteinase-activated receptor-2 (PAR-2) which is a source of stimulation in pruritus.
Owner:AMOREPACIFIC CORP
Modulators of protease activated receptors
The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for therapies such as metabolic syndrome, obesity, type II diabetes, fibrosis and cardiovascular diseases, whether they are used alone or in combination with other treatment modalities.
Owner:THE UNIV OF QUEENSLAND
Guinea pig proteinase-activated receptor 4 and its activating peptide
InactiveUS20060141451A1Inhibition of activationPeptide/protein ingredientsReceptors for hormonesHuman plateletGuinea pig
This invention relates to nucleic acid encoding guinea pig PAR 4 and to the protein encoded thereby. The guinea pig DNA and protein are useful for the development of models of human platelet aggregation. The invention further relates to an animal model to assess the role of PAR antagonists in thrombosis.
Owner:ORTHO MCNEIL PHARM INC
PAR (Protease Activated Receptor)-1 antagonist and application thereof
ActiveCN104086500AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseaseEthoxidine
The invention relates to the field of thrombotic disease related drugs and particularly relates to a PAR (Protease Activated Receptor)-1 antagonist with a brand new structure as the specification, wherein the benzene ring at one side of N-morpholinyl is substituted by ethyoxyl. The invention also relates to an application of the PAR-1 antagonist to preparation of drugs for treating thrombotic diseases.
Owner:南京望知星医药科技有限公司
Protease-activated receptor 3 and uses thereof
Disclosed are cDNAs and genomic DNAs encoding protease-activated receptor 3 (PAR3) from mouse and human, and the recombinant polypeptides expressed from such cDNAs. The recombinant receptor polypeptides, receptor fragments and analogs expressed on the surface of cells are used in methods of screening candidate compounds for their ability to act as agonists or antagonists to the effects of interaction between thrombin and PAR3. Agonists are used as therapeutics to treat wounds, thrombosis, atherosclerosis, restenosis, inflammation, and other thrombin-activated disorders. Antagonists are used as therapeutics to control blood coagulation and thereby treating heart attack and stroke. Antagonists mediate inflammatory and proliferative responses to injury as occur in normal wound healing and variety of diseases including atherosclerosis, restenosis, pulmonary inflammation (ARDS) and glomerulosclerosis. Antibodies specific for a protease-activated receptor 3 (or receptor fragment or analog) and their use as a therapeutic are also disclosed.
Owner:RGT UNIV OF CALIFORNIA
Compounds with terminally-substituted phenyl triazole Schiff base structures and applications of compounds
ActiveCN104086493AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-substituted phenyl triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The substituent groups R1 and R2 are defined as the specification.
Owner:蚌埠格识知识产权运营有限公司
EGFR and PAR2 Regulation of Intestinal Permeability
InactiveUS20140363818A1Inhibition releaseReduce penetrationOrganic active ingredientsMicrobiological testing/measurementAutoimmune responsesAutoimmune disease
The present invention provides methods for diagnosing an immune-mediated disease, e.g., an autoimmune disease, an allergy or an inflammatory disease. Diagnosis is made by detecting a heterozygous or homozygous genotype of haptoglobin 2 or by detecting and quantifying pre-haptoglobin 2 mRNA or protein. After diagnosis, the disease may be treated by decreasing cell permeability leading to increased transepithelial electrical resistance, for example, by administering an antibody directed against single chain zonulin thereby inhibiting epidermal growth factor receptor and inhibiting proteinase-activated receptor 2 (PAR2). Also provided is a single step method for determining severity of an immune-mediated disease in a subject by identifying a genotype for haptoglobin 2 in a biological sample from the subject. A homozygous genotype correlates to 2 copies of zonulin and a more severe disease than a heterozygous genotype correlating to 1 copy of zonulin.
Owner:UNIV OF MARYLAND
Cosmetic composition comprising chestnut shell extract
InactiveCN102458356AEnhanced inhibitory effectExcellent palliative effectCosmetic preparationsAntipyreticTraditional medicineBULK ACTIVE INGREDIENT
The present invention relates to a cosmetic composition for alleviating or suppressing pruritus, comprising chestnut shell extract as an active ingredient. According to one embodiment of the present invention, the cosmetic composition containing the chestnut shell extract is suitable for use as an active ingredient in a cosmetic composition for alleviating or suppressing pruritus since it has exhibited proven, superior effects in alleviating or suppressing pruritus by suppressing the activity of proteinase-activated receptor-2 (PAR-2) which is a causative agent for pruritus.
Owner:AMOREPACIFIC CORP
Novel injection composition for beautifying filling
InactiveCN108578775AFilled withAnti-wrinklePharmaceutical delivery mechanismProsthesisFiberWrinkle skin
The invention discloses a novel injection composition for beautifying filling. The injection composition is prepared from, by weight, 12-18 parts of tranexamic acid, 5-12 parts of glutathione, 12-18 parts of vitamin C, 12-18 parts of NK cells, 5-12 parts of platelet-derived growth factors, 8-15 parts of epidermal growth factors, 3-8 parts of fiber binding protein, 2-6 parts of glass adhesion protein, 20-40 parts of protease-activated receptor and 2-7 parts of cross-linking agent. The novel injection composition solves the problems that an existing injection-type product is monotonous in function, only achieves the filling effect, and does not have the functions of oxidation resistance, ageing resistance and whitening. The novel injection composition not only has multiple effects of filling, resisting of wrinkles and ageing and whitening, but also has stable performance, safety and durability.
Owner:白晋
Compounds with terminally-disubstituted triazole Schiff base structure as well as preparation methods and applications of compounds
ActiveCN104086495AGood antithrombotic activityOrganic chemistryBlood disorderDiseasePharmaceutical drug
The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All the substituent groups are defined as the specification.
Owner:JIANGSU BAIJIAN PHARMA TECH CO LTD
Compounds with terminally-disubstituted methyl triazole Schiff base structures as well as preparation methods and applications of compounds
InactiveCN104086494AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseaseMethyl palmoxirate
The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with terminally-disubstituted methyl triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. All substituent groups are defined as the specification.
Owner:吴艺雪
Method for treatment of invasive cells
A method for treating metastatic tumor cells of a subject is disclosed. The method comprises administrating to the subject an antisense molecule comprising a nucleotide sequence which is complementary to an RNA sequence of a protease activated receptor (PAR) protein, or an antibody molecule capable of binding to a PAR protein. A method is also described for the treatment of disorders involving the implantation of a placenta in a female subject comprising administrating to the subject the antisense molecule. Also disclosed is the antisense molecule and a pharmaceutical composition comprising it.
Owner:HADASIT MEDICAL RES SERVICES & DEVMENT
Par3 mimetic peptides and uses thereof
ActiveUS20190119349A1Polypeptide with localisation/targeting motifNervous disorderPeptideStereochemistry
This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 3 (PAR3) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR3 activity.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST +1
Antithrombotic compounds as well as preparation methods and applications of antithrombotic compounds
InactiveCN104086492AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseaseMedicine
The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.
Owner:庞庆国
Substituted and fused 6-membered protease activated receptor 4 (par-4) antagonists
InactiveUS20190119300A1Reduce inflammationReduce edemaOrganic chemistryPeptide/protein ingredientsDiseasePROTEASE-ACTIVATED RECEPTOR 4
Owner:VANDERBILT UNIV
Halogenated tetrazole acetophenone compounds as well as preparation methods and applications of halogenated tetrazole acetophenone compounds
ActiveCN104086502AGood antithrombotic activityOrganic active ingredientsOrganic chemistryTetrazolePharmaceutical drug
The invention relates to the field of thrombotic disease related drugs and particularly relates to novel PAR (Protease Activated Receptor)-1 antagonists with halogenated tetrazole acetophenone structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The group R is defined as the specification.
Owner:珠海优润医药科技有限公司
Antithrombotic compounds as well as preparation methods and applications of antithrombotic compounds
ActiveCN104086496AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.
Owner:济宁华能制药厂有限公司
Triazole Schiff base compounds as well as preparation methods and applications of triazole Schiff base compounds
ActiveCN104086497AGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The compounds have the structures as shown in the specification, wherein all the substituent groups are defined as the specification.
Owner:蚌埠格识知识产权运营有限公司
Guinea pig proteinase-activated receptor 4 and its activating peptide
Owner:ORTHO MCNEIL PHARM INC
Health food or pharmaceutical composition comprising chestnut shell extract
InactiveCN105285986AEasily damagedEnhanced inhibitory effectSugar food ingredientsVitamin food ingredientsMedicineBULK ACTIVE INGREDIENT
Owner:AMOREPACIFIC CORP
Halogenated tetrazolium acetophenone compound, its preparation method and use
ActiveCN104086502BGood antithrombotic activityOrganic active ingredientsOrganic chemistryDiseaseTetrazole
Owner:珠海优润医药科技有限公司
Modulators of protease activated receptors
Owner:THE UNIV OF QUEENSLAND
Inhibitors of protease activated receptor-2
The present invention relates generally to compounds capable of inhibiting Protease Activated Receptor-2 (PAR2), and uses thereof. More specifically, the present invention relates to inhibitors of PAR2, to their preparation, and to their use in the treatment of diseases and disorders mediated by PAR2 signaling.
Owner:TAKEDA PHARMA CO LTD
Protease Activated Receptor-1 (PAR1) Derived Cytoprotective Polypeptides and Related Methods
ActiveUS20150045283A1High activityReduce mortalityNervous disorderCell receptors/surface-antigens/surface-determinantsArginineApoptosis
The present invention provides novel PAR lderived cytoprotective oligopeptides or polypeptides which typically contain at least the first 4 N-terminal residues that are substantially identical to the corresponding N-terminal residues of Met1-Arg46 deleted human PAR 1 sequence. These cytoprotective oligopeptides or polypeptides are capable of activating PAR 1 and promoting PAR 1 cytoprotective signaling activities. The invention also provides engineered cells or transgenic non-human animals which harbor in their genome an altered PAR 1 gene that is resistant to cleavage at Arg41 and / or Arg46 residues. Additionally provided in the invention are methods of screening candidate compounds to identity additional cytoprotective compounds or cytoprotective proteases. The invention further provides therapeutic use or methods of employing a PAR 1 derived cytoprotective oligopeptide or polypeptide to treat conditions associated with tissue injuries or undesired apoptosis.
Owner:THE SCRIPPS RES INST
Terminal double-substituted triazole Schiff base compound, its preparation method and use
ActiveCN104086495BGood antithrombotic activityOrganic chemistryBlood disorderDiseasePharmaceutical drug
Owner:JIANGSU BAIJIAN PHARMA TECH CO LTD
Par2 mimetic peptides and uses thereof
ActiveUS20190117785A1Cell receptors/surface-antigens/surface-determinantsPeptide/protein ingredientsMedicinePeptide
This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 2 (PAR2) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR2 activity.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST +1
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