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301results about "Cyclic peptides" patented technology
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Macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I, II or Ill, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds 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
Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties
The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Methods for preparing internally constrained peptides and peptidomimetics
ActiveUS7202332B2Stable and irreversible bondPeptide preparation methodsCyclic peptide ingredientsBeta sheetHelix
The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet / beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet / beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.
Owner:NEW YORK UNIV
Macrocyclic peptides active against the hepatitis C virus
ActiveUS20050080005A1Avoid virus infectionBiocideTripeptide ingredientsMacrocyclic peptideHcv ns3 protease
Compounds of formula I: wherein D, R4, R3, L0, L1, L2, R2 and Rc are defined herein; or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.
Owner:BOEHRINGER INGELHEIM INT GMBH
Vault agents for chronic kidney disease
InactiveUS20120003201A1Reduce expressionConnective tissue peptidesTripeptide ingredientsAdhesion processRGD peptide
Owner:RGT UNIV OF CALIFORNIA
Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, 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
Deuterated cyclosporine analogs and their use as immunomodulating agents
InactiveUS6605593B1Improve practicalityAltered physicochemical and pharmacokinetic propertyNervous disorderAntipyreticCyclosporinsImmunomodulating Agent
Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
Owner:AURINIA PHARMA
Macrocyclic isoquinoline peptide inhibitors of hepatitis C virus
InactiveUS20060257980A1Inhibit functioningEffective treatmentDigestive systemAntiviralsIsoquinolineCombinatorial chemistry
Macrocyclic isoquinoline peptides are disclosed having the general formula: A compound of formula I: wherein R1 to R9, Q and W are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Owner:BRISTOL MYERS SQUIBB CO
Methods for preparing internally constrained peptides and peptidomimetics
ActiveUS20060014675A1Promote cell deathAvoid interactionPeptide preparation methodsImmunoglobulinsGreek letter betaBeta sheet
The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet / beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet / beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.
Owner:NEW YORK UNIV
Bis-sulfhydryl macrocyclization systems
InactiveUS20090047711A1Good biological propertiesSimple structureApoptosis related proteinsCyclic peptide ingredientsCombinatorial chemistryAmino acid
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
Owner:AILERON THERAPEUTICS INC
Macrocyclic peptides active against the hepatitis C virus
ActiveUS20050192212A1Inhibition of replicationEffective treatmentBiocideAntiviralsMacrocyclic peptideHcv ns3 protease
Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.
Owner:BOEHRINGER INGELHEIM INT GMBH
Bis-Sulfhydryl Macrocyclization Systems
ActiveUS20090088553A1Good biological propertiesSimple structureCell receptors/surface-antigens/surface-determinantsPeptide preparation methodsCombinatorial chemistryAmino acid
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
Owner:AILERON THERAPEUTICS INC
Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, 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
Bis-sulfhydryl macrocyclization systems
ActiveUS20100184628A1Good biological propertiesSimple structureApoptosis related proteinsCyclic peptide ingredientsCombinatorial chemistryAmino acid
Owner:AILERON THERAPEUTICS INC
Macrocyclic isoquinoline peptide inhibitors of Hepatitis C virus
ActiveUS20050090432A1Inhibit functioningEffective treatmentBiocideAntiviralsIsoquinolineCombinatorial chemistry
Macrocyclic isoquinoline peptides are disclosed having the general formula: A compound of formula I: [0001]wherein R1 to R9, Q and W are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Owner:BRISTOL MYERS SQUIBB CO
Process for preparing macrocyclic compounds
Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
Owner:BOEHRINGER INGELHEIM INT GMBH
Macrocyclic ghrelin receptor modulators and methods of using the same
ActiveUS20080194672A1Reduced and dysfunctional gastrointestinal motilityInhibit gastrointestinal motilityAntibacterial agentsOrganic active ingredientsSomatotropic hormonePharmaceutical Substances
The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC
4-amino-4-oxobutanoyl peptides as inhibitors of viral replication
The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula Iand the pharmaceutically salts and hydrates thereof.The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and / or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
Owner:ACHILLION PHARMA INC
Phosphorus-containing hepatitis C serine protease inhibitors
InactiveUS20080039375A1Inhibit serine protease activityInhibitory activityBiocideDipeptide ingredientsSerine protease activitySerine
The present invention relates to phosphorus-derived compounds of Formula I or Formula II, or a pharmaceutically acceptable salt, ester, or prodrug, 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
Stitched polypeptides
ActiveUS8592377B2Improve the immunityImprove permeabilityAntibacterial agentsSenses disorderBiochemistry
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Depeptidized inhibitors of hepatitis C virus NS3 protease
InactiveUS20050164921A1Symptoms improvedModulate activityBiocideAntiviralsDiseaseHcv hepatitis c virus
The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Aza-peptide macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, 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
N-functionalized amides as hepatitis c serine protease inhibitors
InactiveUS20080267917A1Inhibitory activityAntibacterial agentsBiocideHepatitis c viralPharmaceutical medicine
The present invention relates to functionalized amides of Formula I or Formula II, including 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
Macrocyclic modulators of the ghrelin receptor
ActiveUS20060025566A1Promote gastrointestinal motilityModulating activity of receptorDigestive systemCyclic peptide ingredientsInflammationCentral nervous system
Owner:OCERA THERAPEUTICS INC
Depeptidized inhibitors of hepatitis C virus NS3 protease
InactiveUS7253160B2Modulate activityPrevention or ameliorationBiocideDigestive systemMedicinePeptide
The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I, II or Ill, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds 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
Conjugates of rgd peptides and porphyrin or (bacterio) chlorohyll photosynthesizers and their uses
Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and normeoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.
Owner:YEDA RES & DEV CO LTD
Macrocyclic modulators of the ghrelin receptor
ActiveUS7476653B2Promote gastrointestinal motilityModulating activity of receptorDigestive systemPeptide preparation methodsGrowth hormone-releasing peptideInflammation
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC
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