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37results about How to "Effective inhibitor" patented technology
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Compositions useful as inhibitors of protein kinases
InactiveUS20050148603A1Effective inhibitorAvoid cell deathOrganic active ingredientsBiocideDiseaseBiochemistry
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.
Owner:VERTEX PHARMA INC
Bromodomain inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Owner:CONSTELLATION PHARMA INC
Modified oligonucleotides for telomerase inhibition
ActiveUS20050113325A1Superior cellular uptake propertyReduce Toxicity RiskBiocideGenetic material ingredientsTelomeraseLipid moiety
Compounds comprising an oligonucleotide moiety covalently linked to a lipid moiety are disclosed. The oligonucleotide moiety comprises a sequence that is complementary to the RNA component of human telomerase. The compounds inhibit telomerase activity in cells with a high potency and have superior cellular uptake characteristics.
Owner:GERON CORPORATION
Modified oligonucleotides for telomerase inhibition
ActiveUS7494982B2Inhibit telomeraseMaintain good propertiesBiocideSugar derivativesTelomeraseLipid moiety
Owner:GERON CORPORATION
Hcv protease inhibitors and uses thereof
Owner:CELGENE CAR LLC
Tricyclic piperazine derivative
Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.
Owner:SUNOVION PHARMA INC +1
Compositions useful as inhibitors of protein kinases
InactiveUS20070190634A1Effective inhibitorAvoid cell deathOrganic chemistryMetabolism disorderMedicinal chemistryDisease cause
Owner:VERTEX PHARMA INC
Stents capable of controllably releasing histone deacetylase inhibitors
InactiveUS20050065596A1Therapy is simpleAvoid problemsStentsSurgeryPercent Diameter StenosisHDAC inhibitor
A stent device is provided. The stent device includes a stent body and one or more HDAC inhibitor depot(s) provided on or in the stent body, the depot(s) capable of controllably releasing HDAC inhibitor(s). Methods of using the stents in treating and / or preventing restenosis are provided. A delivery system including the stent device and a methods of using the delivery system in treating and / or preventing restenosis are also provided. Kits comprising stents are provided.
Owner:BOSTON SCI SCIMED INC
Modified oligonucleotides for telomerase inhibition
InactiveUS20120329858A1Superior cellular uptake propertyReduce Toxicity RiskOrganic active ingredientsSugar derivativesTelomeraseLipid moiety
Compounds comprising an oligonucleotide moiety covalently linked to a lipid moiety are disclosed. The oligonucleotide moiety comprises a sequence that is complementary to the RNA component of human telomerase. The compounds inhibit telomerase activity in cells with a high potency and have superior cellular uptake characteristics.
Owner:GERON CORPORATION
3-triazolyl-galactoside inhibitors of galectins
Owner:GALECTO BIOTECH
Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
InactiveUS20120184535A1Improve effectivenessInhibitory activityBiocideNervous disorderDiseaseTyrosine
A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine / threonine and tyrosine kinases and a serine / threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine / threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine / threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.
Owner:SELVITA SA
Protease inhibitor compositions for prevention and treatment of skin conditions
InactiveUS20050048105A1Improve barrier propertiesPreventing them from damaging skinCosmetic preparationsBiocideHuman wasteDiaper rash
Treatments for diaper rash that include a protease inhibitor and a polymer with which the inhibitor is delivered. In certain embodiments, the inhibitor may comprises glycine soja protein or dipalmitoyl hydroxyproline. The polymer binds to the skin, creates a non-occlusive barrier, and is substantially resistant to being washed or rubbed off. The invention also relates to methods of preparing such formulations and to methods of treating patients in need of treatments for skin conditions associated with prolonged exposure to enzymes present in human waste.
Owner:SMITH & NEPHEW INC
Macrocyclic compounds as protein kinase inhibitors
ActiveUS20140256717A1Ease of detectabilityEasy to prepareBiocideNervous disorderDiseasePTK Inhibitors
There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A / B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and / or mTOR) is desired and / or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III
Prenylation inhibitors containing dimethylcyclobutane and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.
Owner:DEV PARTNERS
Lipopeptide inhibitors of hiv-1
InactiveUS20120028887A1Avoid fusesGood pharmacologicalBiocidePeptide/protein ingredientsCrystallographyHeptad repeat
The invention provides lipophilic conjugates comprising a short isolated peptide coupled to a hydrophobic moiety, the peptide comprising a sequence derived from the HIV-1 gp41 N-terminal heptad repeat domain, said peptide after conjugation to the hydrophobic moiety possesses anti-fusogenic activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by human and non-human retroviruses, especially HIV.
Owner:YEDA RES & DEV CO LTD
Heterocyclic compounds useful as pdk1 inhibitors
ActiveUS20120208819A1Effective inhibitorInhibitory activityBiocideOrganic chemistryDiseaseCombinatorial chemistry
Owner:MILLENNIUM PHARMA INC +1
Inhibition of cholera toxins by galatooligosaccharides (GOS)
InactiveUS8202842B2Effective in prophylacticEffective inhibitorBiocideSugar derivativesDiseaseMedicine
The invention relates to nutritional and pharmaceutical compositions comprising non-digestible galactooligosaccharides (GOS) and uses thereof. In particular, it relates to the use of GOS species in preventing or treating disease caused by bacterial toxins. Provided is the use of GOS having a polymerization degree of 5 or higher, preferably 6 or higher, for the manufacture of a nutritional or pharmaceutical composition for the treatment or prevention of an acute or chronic disease associated with or caused by the adhesion and / or uptake of a cholera toxin family member. Also provided is a method for providing a GOS fraction capable of inhibiting cholera toxin (Ctx) binding to GM1 and fractions obtainable thereby.
Owner:FRIESLAND BRANDS BV
Small molecule inhibitors of plasmodium falciparum dihydroorotate dehydrogenase
ActiveUS20110130381A1Strong specificityEffective inhibitorBiocideOrganic chemistryANTU toxicityCytotoxicity
Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE +2
Gcn2 inhibitors and uses thereof
ActiveUS20190233411A1Effective inhibitorTargeting/decreasing a protein or lipid kinase activityOrganic active ingredientsNervous disorderMedicinal chemistry
Owner:MERCK PATENT GMBH +1
Macrocyclic compounds as protein kinase inhibitors
ActiveUS20160296528A1Effective inhibitorOrganic active ingredientsNervous disorderDiseasePTK Inhibitors
Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III
Imidazopyrazines for use as kinase inhibitors
ActiveUS20120083492A1Ease of detectabilityEasy to prepareAntibacterial agentsBiocideDiseaseLipid kinases
There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and / or mTOR) is desired and / or required, and particularly in the treatment of cancer or a proliferative disease.
Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III
Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
![Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/e226eab5-eee4-4cae-a6e1-d3cc7b891e63/US20150148337A1-20150528-C00001.PNG "Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof")
![Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/e226eab5-eee4-4cae-a6e1-d3cc7b891e63/US20150148337A1-20150528-C00002.PNG "Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof")
![Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/e226eab5-eee4-4cae-a6e1-d3cc7b891e63/US20150148337A1-20150528-C00003.PNG "Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof")
Owner:CONSTELLATION PHARMA INC
Triazolo [4, 5- B] Pyridin Derivatives
There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and / or PIM-3, and / or Flt3) is desired and / or required, and particularly in the treatment of cancer or a proliferative disease.
![Triazolo [4, 5- B] Pyridin Derivatives](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9516906a-c6f1-42c2-82de-8ec4716318c6/US20130065883A1-20130314-C00001.png "Triazolo [4, 5- B] Pyridin Derivatives")
![Triazolo [4, 5- B] Pyridin Derivatives](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9516906a-c6f1-42c2-82de-8ec4716318c6/US20130065883A1-20130314-C00002.png "Triazolo [4, 5- B] Pyridin Derivatives")
![Triazolo [4, 5- B] Pyridin Derivatives](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9516906a-c6f1-42c2-82de-8ec4716318c6/US20130065883A1-20130314-C00003.png "Triazolo [4, 5- B] Pyridin Derivatives")
Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III
5-aminopyrazole formamide derivative as BTK inhibitor, preparation method and pharmaceutical composition thereof
ActiveCN107382973AEffective inhibitorSecurity inhibitorOrganic active ingredientsSenses disorderStereoisomerismProdrug
The present invention discloses a novel 5-aminopyrazole formamide compound represented by a formula (I), and a stereoisomer, or a pharmaceutically acceptable salt, a solvate or a prodrug thereof, wherein each substituent is defined in the specification. The invention further discloses a preparation method, a pharmaceutical composition and uses of the compound. The formula (I) is defined in the specification.
Owner:SUZHOU SINOVENT PHARMA CO LTD
Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
InactiveUS8604217B2Improve effectivenessInhibitory activityBiocideNervous disorderDiseasePharmacologic action
Owner:SELVITA SA
Methods for treating and/or limiting development of diabetes
InactiveUS8557513B2Effective inhibitorAvoid selectionOrganic active ingredientsMetabolism disorderDiabetes mellitus
Owner:BIOCRINE
Therapeutic agent for interstitial pulmonary disease comprising Anti-hmgb-1 antibody
InactiveUS20100216977A1Increase levelSuppress inflammationImmunoglobulins against cytokines/lymphokines/interferonsAntibody ingredientsInterstitial lung diseaseInterstitial pulmonary disease
An objective of the present invention is to provide effective methods for treating interstitial pulmonary diseases including interstitial pneumonia such as IPF. The present invention suggests that antibodies against HMGB-1 are effective for treating pulmonary fibrosis. Thus, the present invention provides preparations which comprise an anti-HMGB-1 antibody for treating interstitial pulmonary diseases.
Owner:KYUSHU UNIV +2
Nutritional supplement containing alpha-glucosidase and alpha-amylase inhibitors
ActiveUS20050208161A1Inhibits alpha-amylase breakdownEffective inhibitorOrganic active ingredientsBiocideAlgluceraseIntestinal Lipase Inhibitor
A nutritional supplement composition contains inhibitors of alpha-glucosidase and alpha-amylase substantially in the absence of lipase inhibitors. The composition can include touchi extract and phaseolamin as the alpha-glucosidase and alpha-amylase inhibitor, respectively. A method of limiting the absorption of carbohydrates contained in a foodstuff includes administering the nutritional supplement composition prior to consumption of the carbohydrates, and a method promoting weight loss in an individual includes administering the nutritional supplement composition to the individual over a period of days.
Owner:ACCESS BUSINESS GRP INT LLC
Nutritional supplement containing alpha-glucosidase and alpha-amylase inhibitors
ActiveUS7108869B2Effective inhibitorLimit absorptionBiocidePeptide/protein ingredientsCarbohydrate absorptionAmylase inhibitors
A nutritional supplement composition contains inhibitors of alpha-glucosidase and alpha-amylase substantially in the absence of lipase inhibitors. The composition can include touchi extract and phaseolamin as the alpha-glucosidase and alpha-amylase inhibitor, respectively. A method of limiting the absorption of carbohydrates contained in a foodstuff includes administering the nutritional supplement composition prior to consumption of the carbohydrates, and a method of promoting weight loss in an individual includes administering the nutritional supplement composition to the individual over a period of days.
Owner:ACCESS BUSINESS GRP INT LLC
Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
![Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ea1a17dd-7b39-4a7e-bce6-eff1584bfb36/US20150148333A1-20150528-C00001.PNG "Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof")
![Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ea1a17dd-7b39-4a7e-bce6-eff1584bfb36/US20150148333A1-20150528-C00002.PNG "Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof")
![Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ea1a17dd-7b39-4a7e-bce6-eff1584bfb36/US20150148333A1-20150528-C00003.PNG "Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof")
Owner:CONSTELLATION PHARMA INC
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