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1486 results about "Israpafant" patented technology
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Israpafant (Y-24180) is a drug which acts as a selective antagonist for the platelet-activating factor receptor, and was originally developed for the treatment of asthma. Its chemical structure is a thienotriazolodiazepine, closely related to the sedative benzodiazepine derivative etizolam. However israpafant binds far more tightly to the platelet-activating factor receptor, with an IC₅₀ of 0.84nM for inhibiting PAF-induced human platelet aggregation (compared to etizolam's IC₅₀ of 998nM at this target), while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM. Israpafant has been found to inhibit the activation of eosinophil cells, and consequently delays the development of immune responses. It has also been shown to have anti-nephrotoxic properties, and to mobilize calcium transport.
Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase
ActiveUS20140356322A1Organic active ingredientsPeptide/protein ingredientsProtein targetEnhanced degradation
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and / or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:YALE UNIV +2
Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof
The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
Owner:CYTOVIA INC
Compounds and methods for the enhanced degradation of targeted proteins
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:YALE UNIV +1
Inhibitors of Human EZH2, and Methods of Use Thereof
The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
Owner:EPIZYME
Macrocyclic Proline Derived HCV Serine Protease Inhibitors
The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Owner:ENANTA PHARM INC
Methods and compositions for kinase inhibition
The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.
Owner:RGT UNIV OF CALIFORNIA
Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof
InactiveUS6342611B1Organic chemistryMicrobiological testing/measurementScreening proceduresApoptosis
The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
Owner:CYTOVIA INC
4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
Owner:INCYTE HLDG & INCYTE
INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS
Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions / disorders / diseases due to mutations or dysregulation of the Wnt pathway and / or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Owner:BIOSPLICE THERAPEUTICS INC
Acylaminoheteroaryl hepatitis C virus protease inhibitors
InactiveUS20080039470A1Inhibit serine protease activityInhibitory activityBiocideTripeptide ingredientsProteinase activityIsrapafant
The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Owner:ENANTA PHARM INC
Anti-glypican 3 antibody
An antibody capable of binding to a specific region of glypican 3, as well as a humanized antibody created based on that antibody are disclosed. The anti-GPC3 antibody of the invention has a higher ADCC activity and CDC activity compared with those of a conventional antibody. The antibody of the present invention is useful as a cell growth inhibitor, an anticancer agent and an agent for diagnosis of cancers.
Owner:CHUGAI PHARMA CO LTD
Methods for Treating HCV
ActiveUS20130102526A1Improve pharmacokineticsImprove bioavailabilityBiocideDipeptide ingredientsCytochrome P450 InhibitorsShort duration
The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).
Owner:ABBVIE INC
Phosphorus-containing hepatitis C serine protease inhibitors
Owner:ENANTA PHARM INC
Inhibitor which is deactivatable by a reagent produced by a target cell
ActiveUS8809504B2Undesirable effectModulating responseNGF/TNF-superfamilyAntibody ingredientsActive agentWhole body
The invention relates to molecules inhibiting biologically active compounds and further comprising moieties specifically cleavable by a reagent produced by a target cell. The invention relates to inhibitors that bind, inhibit, suppress, neutralize, or decrease activity of a biologically active agent. Inhibitors comprise at least one moiety that bind, inhibit, suppress, neutralize, or decrease activity of a biologically active agent and at least one moiety that can be cleaved specifically by a reagent produced by target cells. The cleavage deactivates the inhibitor. Following cleavage, the active agent is liberated into the local environment. Administration of the inhibitor alone or together with the active agent suppress the compound's activity until it reaches the proximity of a target cell. Targeted specific release enables the agent concentration in specific site to reach levels that have desired therapeutic effects without systemic toxicity.
Owner:VYTACERA BIO LLC
Carboline carboxamide compounds useful as kinase inhibitors
Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
Owner:BRISTOL MYERS SQUIBB CO
Beta sheet breaker peptide analogs that inhibit beta pleated sheet formation in amyloid beta-peptide
The present invention provides peptide analogs and peptide mimetics that inhibit pleated sheet formation in amyloid beta-peptide, pharmaceutical compositions thereof and their therapeutic use. The inhibitory peptides possess activity as inhibitors in the formation of amyloid-like deposits and are useful in the treatment of Alzheimer's Disease.
Owner:AXONYX INC
Cyclic peptide inhibitors of lysine-specific demethylase 1
ActiveUS20150065434A1Inhibit cell growthInhibit cell proliferationPeptide-nucleic acidsDepsipeptidesCyclic peptideIsrapafant
Provided herein are cyclic peptide inhibitors of lysine-specific demethylase 1. These cyclic peptides have the potential to treat cancer, diabetes, cardiovascular disease, and neurological disorders.
Owner:MUSC FOUND FOR RES DEV
2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors
InactiveUS20120277424A1Improve abilitiesPreventing and treating diseaseOrganic active ingredientsBiocideDiseasePTK Inhibitors
![2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/202de86e-704c-43ab-88d8-20d4f38686d1/US20120277424A1-20121101-C00001.png "2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors")
![2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/202de86e-704c-43ab-88d8-20d4f38686d1/US20120277424A1-20121101-C00002.png "2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors")
![2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/202de86e-704c-43ab-88d8-20d4f38686d1/US20120277424A1-20121101-C00003.png "2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors")
Owner:KOREA INST OF SCI & TECH
Hetero-aromatic ring and derivative type tyrosine kinase inhibitor thereof
InactiveCN103664878ABTK kinase inhibition is goodLittle side effectsOrganic active ingredientsOrganic chemistryImmunologic disordersDisease
The invention belongs to the technical field of medicaments, and in particular relates to a hetero-aromatic ring shown by a general formula (I) as well as a derivative type tyrosine kinase inhibitor, a pharmaceutically acceptable salt or a stereoisomer thereof, wherein X, Z, W, R1, R2, R3, L1, L2, a, b, c, d, e, p, q, A and B are as defined in the specification. The invention also relates to preparation methods of these compounds, a pharmaceutical preparation containing these compounds, and important functions of these compounds in preparation of medicaments for treating B cell related leukemia (such as B cell chronic lymphocytic carcinoma and non-hodgkin lymphoma) and autoimmune diseases (such as rheumatoid arthritis, systemic lupus erythematosus and the like).
Owner:KBP BIOSCIENCES CO LTD
Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors
ActiveUS9187489B2Potent ROS kinase enzyme activity inhibitory effectInhibit cell growthOrganic active ingredientsOrganic chemistryPyridazineKinase
![Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/87e6c50b-ff7e-4ff3-866e-b04bf55482cd/US09187489-20151117-C00001.PNG "Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors")
![Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/87e6c50b-ff7e-4ff3-866e-b04bf55482cd/US09187489-20151117-C00002.PNG "Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors")
![Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/87e6c50b-ff7e-4ff3-866e-b04bf55482cd/US09187489-20151117-C00003.PNG "Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors")
Owner:DAIICHI SANKYO CO LTD
Jak1 selective inhibitor and uses thereof
InactiveUS20150118229A1High selectivityLow potencyBiocideSenses disorderInflammatory bowel diseaseDosage schedule
Owner:ABBVIE INC
Method for assay on the effect of vascularization inhibitor
ActiveUS20100092490A1Improve anti-tumor effectBiocideBiological material analysisAngiogenesis growth factorWilms' tumor
The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and / or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and / or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
Owner:EISIA R&D MANAGEMENT CO LTD
Heterocyclic compounds regulating clotting
InactiveUS6180625B1Inhibition formationPreventing initiationOrganic active ingredientsOrganic chemistryFactor VIIaFactor VII
Compounds of formula (I)as factor VII-tissue factor inhibitors as well as novel benzoxazin derivatives are disclosed, wherein R1, R2, R3, X and Y are as defined in the specification. These compounds, and pharmaceutically acceptable salts thereof, have been shown to be inhibitors of factor VIIa-tissue factor activity and have anticoagulant properties. These compounds are useful for treating deficiencies of blood clotting factors or the effects of inhibitors to blood clotting factors. Methods for inhibiting clotting activity are also disclosed.
Owner:NOVO NORDISK AS
Pharmaceutical combination comprising an ibat inhibitor and a bile acid binder
InactiveUS20130236541A1Maximal bile acid binding capacityDecrease needed doseOrganic active ingredientsBiocideDipeptidyl peptidaseAldose reductase inhibitor
The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (I BAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.
Owner:ALBIREO
6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2
ActiveUS20110118241A1Promote degradationImprove survival rateBiocideOrganic chemistryAldosterone Synthase DeficiencyIsrapafant
The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and / or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1).
Owner:ELEXOPHARM
Evodiamine compounds, preparation method thereof and application thereof
InactiveCN102311434AGood antitumor activityOrganic active ingredientsOrganic chemistryEvodiamineDNA underwinding
The invention relates to the technical field of medicines. The content of DNA topoisomerase I (TopoI) in tumor cells is substantially higher the content of the TopoI in normal tissues, and an inhibitor of the TopoI is listed as one of six types of antitumor drugs which are primarily researched by an American NCI (National Cancer Institute). The invention aims to obtain evodiamine derivatives withstrong antitumor activities by modifying the structure of evodiamine. The evodiamine structure of the evodiamine compounds is represented by general formula (I) in the specification. The invention also provides an application of the evodiamine compounds and medicinal salts thereof in preparing topoisomerase inhibitors and antitumor drugs.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
C-17 and C-3 modified triterpenoids with HIV maturation inhibitory activity
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III:These compounds are useful for the treatment of HIV and AIDS.
Owner:VIIV HEALTHCARE UK (NO 5) LTD
Nitric oxide releasing prodrugs of diaryl-2-(5h)-furanones as cyclooxygenase-2 inhibitors
Owner:MERCK FROSST
Novel Compounds
The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
Owner:GLAXO GROUP LTD
Kinase inhibitors
InactiveUS20140057915A1Weak affinityImproved profileBiocideOrganic active ingredientsTyrosineP38 Mitogen Activated Protein Kinase
There are provided compounds of formula I,wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Owner:RESPIVERT +1
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