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758results about "Tripeptides" patented technology
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Cross-linkers and their uses
ActiveUS20090274713A1Good water solubilityHigh sensitivityOrganic active ingredientsTripeptide ingredientsCell bindingCross-link
Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
Owner:IMMUNOGEN INC
Elongated and multiple spacers in activatible prodrugs
InactiveUS7223837B2Improved kineticsFacilitate enzymatic cleavageAntibacterial agentsOrganic active ingredientsTumor cellsChemistry
This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k—(X)l—A—Z, wherein: V is a specifier; (W)k—(X)l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.
Owner:BYONDIS BV
Peptides as NS3-serine protease inhibitors of hepatitis C virus
InactiveUS7012066B2Organic active ingredientsDigestive systemSerine Protease InhibitorsHepatitis C virus
The present invention discloses novel 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 compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:DENDREON PHARMA INC +1
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
Methods for identifying RNA binding compounds
Owner:RUTGERS THE STATE UNIV
Inhibitors of IAP
Owner:GENENTECH INC
Substituted cycloalkyl P1′ hepatitis C virus inhibitors
InactiveUS6878722B2Inhibit functioningEffective treatmentBiocideDipeptide ingredientsHepacivirusVirology
The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.
Owner:BRISTOL MYERS SQUIBB CO
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
Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases
The present invention relates to compounds of formula I:or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
Owner:VERTEX PHARMA INC
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
Hepatitis C inhibitor tri-peptides
ActiveUS7091184B2Better pharmacokinetic profileNot significant inhibitory activityBiocideDipeptide ingredientsHcv ns3 proteaseHepatitis C
Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or —CH2—C(CH3)3 or —CH2-cyclopentyl; R3 is t-butyl or cyclohexyl and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.
Owner:BOEHRINGER INGELHEIM INT GMBH
Inhibitors of IAP
Owner:GENENTECH INC
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
Formulation of boronic acid compounds
The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.
Owner:US DEPT OF HEALTH & HUMAN SERVICES
Compounds for enzyme inhibition
ActiveUS20050245435A1Inhibiting and reducing HIV infectionAffecting levelBiocideNervous disorderEnzyme inhibitionAziridine
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Owner:ONYX THERAPEUTICS
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
Compositions containing mixtures of tetrapeptides and tripeptides
ActiveUS6974799B2Reducing visible sign of agingImprove stateCosmetic preparationsToilet preparationsPersonal careTetrapeptide
Pharmaceutical, personal care and cosmetic compositions containing a tripeptide and a tetrapeptide are useful for treating visible signs of aging including wrinkles, stretch marks and dark circles.
Owner:SEDERMA SA
Fullerene nanotube compositions
InactiveUS20080063585A1High yieldModerate temperatureMaterial nanotechnologyFullerenesFullereneNanotube
This invention relates generally to a fullerene nanotube composition. The fullerene nanotubes may be in the form of a felt, such as a bucky paper. Optionally, the fullerene nanotubes may be derivatized with one or more functional groups. Devices employing the fullerene nanotubes of this invention are also disclosed.
Owner:RICE UNIV
Triazole Macrocycle Systems
InactiveUS20080262200A1Simple structureExhibit biological activityPeptide-nucleic acidsTumor rejection antigen precursorsCombinatorial 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
3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel 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 compounds as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Peptide nucleic acids
InactiveUS6395474B1Remove complicationsAvoid less flexibilityPeptide/protein ingredientsGenetic material ingredientsPeptide backboneRNA
Owner:BUCHARDT OLE +3
Macrocyclic inhibitors of hepatitis C virus NS3-serine protease
InactiveUS20050119168A1HCV infectionImprove overall utilizationBiocideAntiviralsDiseaseStructural formula
The present invention discloses novel 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. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z′, L′, M′, R1, X and D are defined herein.
Owner:MERCK SHARP & DOHME CORP
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 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
Psma binding ligand-linker conjugates and methods for using
Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
Owner:PURDUE RES FOUND INC
Quinoxalinyl tripeptide hepatitis C virus 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
Hepatitis C virus inhibitors
ActiveUS7132504B2Inhibit functioningEffective treatmentBiocidePeptide/protein ingredientsBiochemistryVirus
Owner:BRISTOL MYERS SQUIBB CO
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
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