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Cyclic peptides

Subclass of:

530 - Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof

530300000 - PEPTIDES OF 3 TO 100 AMINO ACID RESIDUES

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Class / Patent application numberDescriptionNumber of patent applications / Date published
530317000 Cyclic peptides 89
20130030149PROCESS FOR PURIFICATION OF PNEUMOCANDIN - The process described herein discloses purification process of a secondary metabolite produced by fermentation route. The process involves selective removal of impurities at various stages of washings, charcoalization followed by crystallization. The product is closely related to class of echinocandins and is found to be potent antifungal compound & a key ingredient in the synthesis of antifungal drugs.01-31-2013
20090275727Peptide turn mimetics - This invention provides novel compounds useful for the synthesis of peptide mimetics, and describes the use of these compounds for the synthesis of novel reverse turn mimetics. The reverse turn mimetics of the invention have the general structure X wherein the variables are as defined herein.11-05-2009
20090156785METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.06-18-2009
20090299033Methods and Compositions for F-18 Labeling of Proteins, Peptides and Other Molecules - The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.12-03-2009
20130165625PEPTIDES INCORPORATING 3-AMINOADAMANTANE CARBOXYLIC ACIDS ENHANCE SYNAPTIC PLASTICITY AND ACT AS NEUROGENIC AGENTS - The disclosed invention relates to peptides incorporating 3-aminoadamantane-1-carboxylic acids. These peptides are disclosed as surprisingly possessing neurogenic and neurotrophic properties. These pharmacological activities can advantageously be utilized for restoring or maintaining neuronal function in the CNS. In particular, the compounds can be used for treatment and prophylaxis of neurodegenerative diseases, e. g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, as well as in post-acute traumatic brain injury, or cerebral ischemia.06-27-2013
20100036089Methods for the Synthesis of Dicarba Bridges in Organic Compounds - The present invention relates to methods for forming dicarba bridges in organic compounds. This involves the use of a pair of complementary metathesisable groups on the organic compound, and subjecting the compound to cross-metathesis under microwave radiation conditions. In an alternative, the compounds contain a turn-inducing group between the pair of cross-metathesisable groups to facilitate the cross-metathesis.02-11-2010
20120190815AZACYCLOHEXAPEPTIDE OR ITS PHARMACEUTICAL ACCEPTABLE SALT, PREPARING METHOD AND USE THEREOF - The present invention disclosed a novel azacyclohexapeptide or pharmaceutically acceptable salts, preparation methods and uses thereof. The structure of the azacyclohexapeptide is represented by the following formula 4:07-26-2012
20100249370PROCESS FOR THE PRODUCTION OF PRAMLINTIDE - Pramlintide, a peptide having the 37 amino acid sequence KCNTATCATQRLANFLVHSSNNFGPILPPT-NVGSNTY-NH2 is prepared via a convergent three-fragment synthesis strategy from the fragments comprising the amino acid residues 1-12, 13-24 and 25-37, respectively.09-30-2010
20090149629CRFR1 SELECTIVE LIGANDS - CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:06-11-2009
20100121027Cyclic Peptide Compositions for Treatment of Sexual Dysfunction - A cyclic peptide of the structural formula:05-13-2010
20110172391PROTEIN SPLICING USING SHORT TERMINAL SPLIT INTEINS - The invention provides methods of producing functional split inteins having small N-intein and/or small C-intein. Using these split inteins with their protein trans-splicing and cleavage activities, we provide new and more effective methods of manipulating proteins. They include site-specific addition of synthetic peptides at protein's terminal and internal locations, ligation of synthetic and/or expressed polypeptides, controllable cyclization of synthetic and/or expressed polypeptides, and controllable cleavages of recombinant proteins. These methods have numerous utilities including but not limited to protein fluorescence labeling, fixation on microchips, site-specific PEGylation, and linkage with pharmaceutical molecules.07-14-2011
20090143565Methods for the Synthesis of Two or More Dicarba Bridges in Organic Compounds - Described herein are methods for forming two or more dicarba bridges, as well as new compounds containing dicarba bridges.06-04-2009
20090275728COMPOUND HAVING HISTONE DEACETYLASE-INHIBITING ACTIVITY, AND PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUND AS AN ACTIVE INGREDIENT - A novel compound having histone deacetylase-inhibiting activity which is a cyclic tetrapeptide derivative represented by the general formula (1) given below and a pharmaceutical composition comprising such compound as an active ingredient. (In the formula, the cyclic tetrapeptide moiety has a known structure; R11-05-2009
20090088553Bis-Sulfhydryl Macrocyclization Systems - 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.04-02-2009
20080207874Peptide Antibiotics and Methods For Making Same - Novel protected cyclopeptide intermediates are prepared from polymyxin B are used to synthesize new peptide antibiotics. Intermediates are readily derivatized and deprotected to provide new families of antibiotics, which have potent anti-bacterial activity against gram-negative bacteria; but also are useful and potent against gram-positive bacteria.08-28-2008
20080281075ASYMMETRIC SYNTHESIS OF PEPTIDES - The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR11-13-2008
20080287649Methods for the synthesis of cyclic peptides - Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.11-20-2008
20090264617METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.10-22-2009
20090163695Process for the preparation of bicyclic peptide compounds - The present invention relates to a new process carried out entirely in solution, for the preparation in high yields of high purity bicyclic peptide compounds of formula (I), useful as intermediates for preparing compounds with pharmacological activity.06-25-2009
20090326194PROCESS FOR PREPARING MACROCYCLIC COMPOUNDS - Disclosed is a process for preparing a macrocyclic compound of the formula (I) wherein a hydroxyl-substituted macrocyclic compound of formula (3) is reacted with a sulfonyl-substituted compound of formula QUIN:12-31-2009
20090326193STABILIZING ALKYLGLYCOSIDE COMPOSITIONS AND METHODS THEREOF - The present invention relates to alkylglycoside-containing compositions and methods for preventing loss of a parathyroid hormone (PTH) analog or octreotide via denaturation due to adherence upon contact with glass.12-31-2009
20090326192BIOLOGICALLY ACTIVE PEPTIDOMIMETIC MACROCYCLES - The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.12-31-2009
20110144302POLYPEPTIDE - The invention provides an immunoglobulin G Fc region binding polypeptide, which polypeptide comprises an immunoglobulin G Fc region binding motif, BM, consisting of an amino acid sequence selected from: i) EQQX06-16-2011
20090240027INTERMEDIATES FOR MACROCYCLIC COMPOUNDS - The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates:09-24-2009
20100261871CONFORMATIONALLY CONSTRAINED PEPTIDE MIMETICS - Conformationally constrained peptide mimetics in which a hydrogen bond interaction is replaced with a covalent hydrogen bond mimic are provided. Also provided are various methods of making these peptide mimetics.10-14-2010
20100184946Preparation of Fine Particles - A process and device for the precipitation of an organic compound comprising the steps: 07-22-2010
20090076244Beta Helical Peptide Structures Stable in Aqueous and non-Aqueous Media and Methods for preparing same - Disclosed is a method of making peptide structures that are stable in aqueous and non-aqueous media where a first linear peptide chain comprising alternating 03-19-2009
20100137559PROCESS FOR PRODUCTION OF CYCLIC PEPTIDES - The invention relates to methods for the preparation of polypeptides. The polypeptides are prepared in high purity of at least about 98.5%, and preferably at least about 99% by HPLC.06-03-2010
20120142892CONTOXIN ANALOGUES AND METHODS FOR SYNTHESIS OF INTRAMOLECULAR DICARBA BRIDGE-CONTAINING PEPTIDES - According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.06-07-2012
20090111969MACROCYCLIC COMPOUNDS AS INHIBITORS OF VIRAL REPLICATION - The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.04-30-2009
20100228004TEMPLATES FOR NUCLEATION AND PROPAGATION OF PEPTIDE SECONDARY STRUCTURE - Compounds having the Formula I and pharmaceutically acceptable salts thereof are provided in which the variables are described herein.09-09-2010
20100216969IMMOBILISATION OF POLYPEPTIDES BY IRRADIATION - The present invention relates generally to methods and carriers for cross-linking or immobilising biomolecules such as polypeptides. In particular, the present invention relates to methods and carriers useful for coupling a polypeptide to a carrier via at least one disulphide bond. The carrier coupled to the biomolecules has applications in the fields of e.g. molecular biology, biochemistry, pharmacology, and medical diagnostic technology.08-26-2010
20110245459Processes for Intermediates for Macrocyclic Compounds - The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates:10-06-2011
20100069606Tubular nanostructure targeted to cell membrane - Devices, compositions, and methods are described which provide a tubular nanostructure targeted to a lipid bilayer membrane. The targeted tubular nanostructure can have a surface region configured to pass through a lipid bilayer membrane of a cell, a hydrophobic surface region flanked by two hydrophilic surface regions configured to form a pore in a lipid bilayer membrane of a cellular organelle, and at least one ligand configured to bind one or more cognates on the lipid bilayer membrane of the cellular organelle. The target cell can be, for example, a tumor cell, an infected cell, or a diseased cell in a subject. The tubular nanostructure can form a pore in the lipid bilayer membrane of the cellular organelle, e.g., mitochondria, which can permit transit or translocation of at least one compound across the membrane and cause cell death of the target cell.03-18-2010
201202029682-Amino-3-methyl-hex-5-enoic acid and its use in the prodction of peptides such as bacitracins - The present invention concerns 2-amino-3-methyl-hex-5-enoic acid, its use for the production of peptides such as bacitracins and a method for producing it.08-09-2012
20080242835Ring-Closing Metathesis Process for the Preparation of Macrocyclic Peptides - Disclosed is a process for preparing a compound of formula (I) by protecting the secondary amide nitrogen atom in the compound of formula (III) to obtain (IV) wherein PG10-02-2008
20120302728Actagardine Derivatives, and Pharmaceutical Use Thereof - Described are lantibiotic-based compounds, pharmaceutical compositions comprising the same and use of the compounds and said compositions, for the treatment of microbial infection, for example 11-29-2012
20110257364PROCESS FOR PURIFYING GLYCOPEPTIDE PHOSPHONATE DERIVATIVES - Disclosed are methods of purifying glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups that are useful as antibacterial agents. The methods include contacting a solution of the glycopeptide derivatives with a polystyrene-containing resin, eluting the resin with an aqueous solution, and isolating the purified glycopeptide derivative.10-20-2011
20100168380PROCESS FOR SYNTHESIZING CYCLIC PEPTIDE COMPOUND - The objective is to provide a novel process for synthesizing a cyclic peptide compound. It is also an objective to provide a novel cyclic peptide compound. The novel process for synthesizing a cyclic peptide compound comprises the steps of: (1) translationally synthesizing a non-cyclic peptide compound having in a molecule a functional group 1 and a functional group 2, which are a pair of functional groups capable of reacting to form a bond, and (2) cyclizing the non-cyclic peptide compound by the reaction of the functional groups 1 and 2 to form a bond. The novel cyclic peptide compound can be synthesized by the process.07-01-2010
20100168381CONJUGATES OF MEMBRANE TRANSLOCATING AGENTS AND PHARMACEUTICALLY ACTIVE AGENTS - Membrane translocation peptides, compositions comprising them, chimeric molecules comprising them, and methods of using them to achieve transmembrane transport of various agents.07-01-2010
20110087002Methods for Cyclizing Synthetic Polymers - The invention provides methods and compositions for production of a cyclic polymer in a cell free system. In general, the methods of the invention involve ligating first and second recombinant intein domains to a linear synthetic polymer to form a compound containing the structure: D04-14-2011
20110263815TRIAZOLE MACROCYCLE SYSTEMS - 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.10-27-2011
20100022746SYNTHESIS OF A RADIOFLUORINATED PEPTIDE USING PHOTOLABILE PROTECTING GROUPS - The present invention encompasses a method of preparing a radiofluorinated compound by adding a photolabile protecting group, R, to an aminoxy group of a peptide based compound wherein the peptide based compound reacts with a light of a specified wavelength in an automated radiosynthesis apparatus to form a radiofluorinated compound. The present invention further relates to a photolabile peptide based compound.01-28-2010
20090069534Hydrochloride salts of a glycopeptide phosphonate derivative - Disclosed are hydrochloride salts of telavancin having a chloride ion content of from about 2.4 wt. % to about 4.8 wt. %. The disclosed salts have improved stability during storage at ambient temperatures compared to other hydrochloride salts. Also disclosed are processes for preparing such salts.03-12-2009
20080287650High purity peptides - The invention relates to methods for the preparation of highly purified peptides. The peptides are prepared in high optical purity of at least about 98.5%, and preferably at least about 99%. Specifically, Nesiritide (SEQ. ID NO. 1) having a purity of at least 99% as measured by HPLC and containing about 0.05% to about 0.5% [D-His]-Nesiritide (SEQ. ID NO. 1) as measured by chiral GC/MS.11-20-2008
20100249371PURIFICATION PROCESS FOR LIPOPEPTIDES - The present invention provides simple, cost effective, rapid, and scalable at industrial scale and provide high purity and yield of Echinocandin-type compounds at low cost as compared to prior art. Moreover the process allows for the removal of impurities by using economical salt-adsorbent complex and provide highly purified Echinocandin type compounds which is highly improved in terms of purity and sufficient for further processing to obtain an active pharmaceutical ingredient such as, the antifungals caspogungin, anidulafungin, and micafungin.09-30-2010
20080319162Process and Intermediates for the Synthesis of Caspofungin - The present invention relates to novel processes for preparing certain aza cyclohexapeptide compounds, e.g. caspofungin, novel intermediates used in said processes and a process for preparing said intermediates. In particular, the intermediates have formula (II), wherein X is amino or substituted amino and contains a cyano/nitrile functionality.12-25-2008
20110092669SYNTHESIS OF CYCLOSPORIN ANALOGS - The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISA04-21-2011
20120208981Method for purification of colistin and purified colistin components - The present invention concerns a method of purifying colistin using reverse phase chromatography, wherein loading a column with colistin base in acetic acid and high ethanol concentration and eluting with low ethanol concentration is performed.08-16-2012
20120059146METHOD FOR THE PREPARATION OF CYCLOPEPTIDES - The present invention relates to a method for preparing cyclopeptides by means of protection with a substituted boronic acid. The present invention also discloses novel boronate esters of cyclopeptides of general formula (8).03-08-2012
20120065366CYCLIC AMINO ACID MOLECULES AND METHODS OF PREPARING THE SAME - Macrocyclization of amino acids or linear peptides upon reaction with amphoteric amino aldehydes and isocyanides is provided.03-15-2012
20120232247PROCESSES FOR PREPARING PROTEASE INHIBITORS OF HEPATITIS C VIRUS - The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.09-13-2012
20120214967CROSS-LINKED GLYCOPEPTIDE-CEPHALOSPORIN ANTIBIOTICS - This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.08-23-2012
20100216970METHODS, COMPOSITIONS, AND APPARATUSES FOR FORMING MACROCYCLIC COMPOUNDS - This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation. More preferably, the macrocyclic compound spontaneous precipitates from the reaction medium and therefore can be easily recovered by simple filtration.08-26-2010
20100273977PROCESS FOR THE PREPARATION OF ECHINOCANDIN DERIVATIVES - A subject of the invention is a process for the preparation of the compounds of formula (I):10-28-2010
20120220752TRI-AMINO RELEASING FULVATE - A free amino acid and/or amino ion-releasing molecule useful for a wide variety of medical and cosmetic applications. The chemical name of the new molecule nino-gl ino-parabenzoate, sometimes referred to herein as TAFA. Its chemical structure is graphically depicted according to structure VIII08-30-2012
20120226018Process for the Synthesis of Ac-Arg-Cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2 - The present invention relates to a novel process for the synthesis of the melanocortin analog, Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH09-06-2012
20110046345Methods for preparing linked peptide rings and peptide nanotubes obtained thereby - Peptide nanotube polymers and methods of making such are disclosed. The peptide nanotube polymers comprise of alternating monomers of the first peptide ring and monomers of the second peptide ring covalently bonded to one another via a linker, and can be functionalized. The described peptide nanotube polymers can enjoy the combined properties of healing and toughness, self-reporting, and tunability and actuation.02-24-2011
20090062509CHELATION OF METALS TO THIOL GROUPS USING IN SITU REDUCTION OF DISULFIDE-CONTAINING COMPOUNDS BY PHOSPHINES - A method is disclosed for the syntheses of thiol-containing radiopharmaceuticals without the need for purification starting from chelators containing disulfide bonds. This is done by providing a method that reduces disulfide bonds on a precursor molecule or a precursor compound in the presence of phosphine compounds, thus freeing thiols for metal complexation.03-05-2009
20120101253STRUCTURED POLYCYCLIC PEPTIDE - The invention relates to a peptide ligand comprising a polypeptide linked to a molecular scaffold at n attachment points, wherein said polypeptide is cyclised and forms n separate loops subtended between said n attachment points on the molecular scaffold, wherein n is greater than or equal to 2.04-26-2012
20130018171PURIFICATION OF CASPOFUNGIN INTERMEDIATESAANM De Pater; Robertus MattheusAACI DelftAACO NLAAGP De Pater; Robertus Mattheus Delft NL - The present invention relates to a method for the purification of cyclopeptides of general formula (3) by means of a silicate.01-17-2013
20130123463METHODS FOR THE SYNTHESIS OF TWO OR MORE DICARBA BRIDGES IN ORGANIC COMPOUNDS - Described herein are methods for forming two or more dicarba bridges, as well as new compounds containing dicarba bridges.05-16-2013
20130144034METHOD FOR THE PRODUCTION OF A COMPOUND OF INTEREST - The present invention relates to a method for the production of a compound of interest by microbial fermentation, wherein the microbial host cell used has been modified in its genome such that it results in a deficiency in the production of at least one non-ribosomal peptide synthase. The present invention further relates to a microbial host cell that has been modified in its genome such that it results in a deficiency in the production of at least one non-ribosomal peptide synthase. The invention further relates to a compound of interest.06-06-2013
20080200647On-Resin Peptide Cyclization - Method of peptide synthesis, comprising the steps of a. synthesizing a peptide linked to a solid phase which peptide comprises at least one cysteine, homo- or nor-cysteine residue, which cysteine is protected in its side chain by a S-tert.butyl-sulphenyl group b. either coupling N-terminally a further amino acid having a 3,3′-dithio-(1-carboxy-propyl)-propionyl-radical on its Nα or deprotecting the Nα of the N-terminal amino acid and reacting the free Nα with 3,3′-dithio-propionic acid imide to yield the corresponding Nα-3,3′-dithio-(1-carboxy-propyl)-propionamide or deprotecting the Nα of the N-terminal amino acid and reacting the free Nα with a compound of formula IV R7-S—S—[CH08-21-2008
20100286363CYCLIC HEPTAPEPTIDE AND USE OF THE SAME - A novel cyclic heptapeptide that is useful as a preadipocyte differentiation-inhibitory agent or an adipocyte fat accumulation-inhibitory agent, and the use of such agents, are provided. A novel cyclic heptapeptide represented by the following formula is provided.11-11-2010
20110313130BIFUNCTIONAL CHELATING AGENTS - A bifunctional chelating agent of the formula (I):12-22-2011
20130197188USE OF URODILATIN FOR PREPARING A MEDICAMENT FOR THE TREATMENT OF CARDIOVASCULAR, RENAL, PULMONARY AND NEURONAL SYNDROMES WHILE AVOIDING A REBOUND - Use of urodilatin for preparing a medicament for the treatment of cardiovascular, renal, pulmonary and neuronal syndromes while avoiding a rebound, wherein said medicament for the delivery of urodilatin is suitable in a first quantity for a first period of at least 48 hours, followed by delivery over a second period of at least 12 hours with successive reduction of said first quantity continuously or gradually to 0 ng/kg/min.08-01-2013
530318000 The cyclisation occurring through the 4-amino radical of 2,4-diamino butanoic acid 1
530319000 Polymyxin; related peptides 1
20090253894METHOD OF POLYMYXIN B RECOVERY FROM FERMENTATION BROTH - The invention is related to the method of polymyxine B recovery from fermentation broth for the purpose of pure substance recovery. The invention mentioned above is obtained by using the method of polymyxine B recovery from fermentation broth according invention, which abstract is characterized by, that the filtrate is obtained from fermentation broth, its pH and color is adjusted and purified on non-ionogenic synthetic adsorbents of polystyrene type with specific surface 500 till 1000 m10-08-2009
530321000 Containing only normal peptide links in the ring, i.e., homodetic cyclic peptides 21
20130030150Purification Method of Azacyclohexapeptide or Its Salt - A purification method of the compound represented by formula 1 is provided, which includes the following steps: (1) loading crude compound 1 on macroporous adsorbent resin, (2) washing the macroporous adsorbent resin with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water, (3) eluting with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water. The purified compound represented by formula 1 is obtained.01-31-2013
20090306339Preparation of Fine Particles - A process for the precipitation of an organic compound comprising mixing simultaneously introduced streams of a solution and a precipitation agent in a chamber using a mechanical stirrer in the presence of an amphiphilic polymer. The process may be operated in a continuous manner and is particularly useful for providing low solubility organic compounds (e.g. pharmaceuticals) in readily dispersible, nano-sized particulate form up to manufacturing scale.12-10-2009
20090093613Treatment of tinnitus - The invention relates to the use of substances which are at least partly blocking one ionotropic acetylcholine receptor of the inner ear and/or a calcium-activated potassium channel functionally associated with said acetylcholine receptor of the inner ear for the manufacturing of a pharmaceutical composition or medicament for the treatment of tinnitus.04-09-2009
20090326195Process for the manufacture of peptides - A process for manufacturing a cyclic peptide which comprises providing a cyclic peptide bonded to a Merrifield-type resin and cleaving the cyclic peptide from the Merrifield type resin by transesterification.12-31-2009
20120190816ASYMMETRIC SYNTHESIS OF PEPTIDES - The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR07-26-2012
20120142893SEPARATION AND/OR PURIFICATION OF B0 FROM C0 - The present invention concerns a method for separation of the antifungal cyclic hexapeptides Pneumocandin B06-07-2012
20110230638METHODS FOR DETECTION OF CYCLOSPORIN A - Methods and reagents are disclosed for determining the presence and/or amount of cyclosporin A in a medium suspected of containing cyclosporin A. In the method a combination is provided in a medium. The combination comprises (i) the sample, (ii) a first member of a signal producing system (sps) associated with a first support wherein the first sps member is capable of activating a second member of the sps and wherein the first support is associated with a first member of a specific binding pair, and (iii) the second sps member associated with a second support wherein the second sps member is activatable by the first sps member. The second support comprises either (I) cyclosporin C or cyclosporin A and the combination further comprises a conjugate of an antibody for cyclosporin A and a second member of the specific binding pair or (II) antibody for cyclosporin A and the combination further comprises a conjugate of cyclosporin A and a second member of the specific binding pair. The combination is subjected to conditions for binding of cyclosporin A to the antibody for cyclosporin A. The first sps member is activated and the amount of signal generated by the second sps member is detected. The amount of signal is related to the presence and/or amount of cyclosporin A in the sample.09-22-2011
20130131311AZIRIDINE MEDIATED NATIVE CHEMICAL LIGATION - Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.05-23-2013
20110118437Process for the Synthesis of Cyclic Heptapeptide - The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.05-19-2011
20100190957SPECIFIC THERAPY AND MEDICAMENT USING INTEGRIN LIGANDS FOR TREATING CANCER - The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agents or therapy forms that have synergistic efficacy when administered consecutively with said ligands, such as chemotherapeutic agents and or radiation therapy. The therapy results in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone, concurrently or not in the dosage regime of the present invention.07-29-2010
20120283410ATTACHMENT OF BIOLOGICAL TARGETING GROUPS USING METAL FREE CLICK CHEMISTRY - The present invention relates to the field of polymer chemistry and more particularly to click-functionalized targeting compounds and methods for using the same.11-08-2012
20110166320SOMATOSTATIN ANALOGUES - The invention provides cyclo[{4-(NH07-07-2011
20130225791MICROREACTOR AND METHOD FOR PREPARING A RADIOLABELED COMPLEX OR A BIOMOLECULE CONJUGATE - A microreactor for preparing a radiolabeled complex or a biomolecule conjugate comprises a microchannel for fluid flow, where the microchannel comprises a mixing portion comprising one or more passive mixing elements, and a reservoir for incubating a mixed fluid. The reservoir is in fluid communication with the microchannel and is disposed downstream of the mixing portion. A method of preparing a radiolabeled complex includes flowing a radiometal solution comprising a metallic radionuclide through a downstream mixing portion of a microchannel, where the downstream mixing portion includes one or more passive mixing elements, and flowing a ligand solution comprising a bifunctional chelator through the downstream mixing portion. The ligand solution and the radiometal solution are passively mixed while in the downstream mixing portion to initiate a chelation reaction between the metallic radionuclide and the bifunctional chelator. The chelation reaction is completed to form a radiolabeled complex.08-29-2013
20120065367Radioactively Labeled Substance - Provided are: a radiolabeled drug, which is efficiently accumulated in a target and has high in vivo stability; and diagnosis and treatment each using the radiolabeled drug. Specifically provided are: a radiolabeled drug showing increased accumulation in a target site, which comprises a complex composed of a ligand that is bound to a compound capable of binding to a target molecule and forms a polycoordinated complex with a metal (e.g., technetium or rhenium) and a radionuclide of the metal; the radiolabeled drug for diagnosis or treatment; a ligand for preparing the radiolabeled drug; a kit that comprises a drug comprising the ligand and a drug comprising a radionuclide of a metal, as separate package units; and a method of increasing accumulation of a radiolabeled drug in a target site, comprising using the above-mentioned radiolabeled drug.03-15-2012
20120214968Preparation of phalloidin and its derivatives - The present invention relates to novel phalloidin derivatives and their fluorescent dye conjugates. These new compounds may be used in studies of actin dynamics in living systems. The present invention also relates to methods for preparing such compounds. The synthesis routes combine solid-phase and solution phase peptide synthesis, and has great advantage for efficient preparation of a diverse library of the phalloidin derivatives, especially for the synthesis of phalloidin.08-23-2012
20100298528Cystine knot molecules - The present invention relates generally to a molecular framework having a cyclic structure. More particularly, the present invention provides cyclic proteins and derivatives thereof in which particular turns and other elements of the molecular structure are held in defined orientations with respect to each other. The cyclic proteins of the present invention provide a molecular framework for the introduction of particular amino acids or heterologous amino acid sequences to facilitate the presentation of biological activities associated with these heterologous amino acid sequences. The molecular framework of the present invention may be naturally cyclic or may be a cyclized derivative of a linear molecular or may be a linear derivative of a cyclized molecule. The present invention contemplates the use of the molecular framework with or without particular amino acids inserted or substituted thereon for the treatment of or prophylaxis of disease conditions in animals, mammals (including humans) and plants.11-25-2010
20120253007Synthesis of Cyclosporin H - A method of preparing purified cyclosporin H includes dissolving cyclosporin A in a first organic solvent and heating the first organic solvent in the presence of an acid catalyst; adding a base to the first organic solvent; recrystallizing cyclosporin H in a second solvent; and purifying the recrystallized cyclosporin H via chromatography to obtain purified cyclosporin H, while excluding recrystallizing the cyclosporin H in the presence of ether. In a further aspect, the method includes, after adding the base and before the recrystallizing, mixing the first organic solvent with a solvent more polar than the first organic solvent, separating the first organic solvent, and drying the first organic solvent. Cyclosporin H prepared as described herein was found to be biologically active, unlike that prepared using a previously-described method.10-04-2012
20130231457PREPARATION METHOD FOR CASPOFUNGIN09-05-2013
20110275784ASYMMETRIC SYNTHESIS OF PEPTIDES - The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR11-10-2011
20130184433METHOD FOR ISOLATING A CYCLOHEXAPEPTIDE - The present invention relates to a method for isolating acyclohexapeptide and to a novel crystalline form of caspofungin diacetate thus obtained.07-18-2013
20130197189Method For Synthesizing A Cyclic Multivalent Peptide Using A Thiol-Mediated Reaction - A method has been developed for the formation of multivalent cyclic peptides. This procedure exploits on-resin peptide cyclization using a photoinitiated thiol-ene click reaction and subsequent clustering using thiol-yne photochemistry. Both reactions utilize the sulfhydrl group on natural cysteine amino acids to participate in the thiol-mediated reactions.08-01-2013

Patent applications in class Cyclic peptides

Patent applications in all subclasses Cyclic peptides