Entries |
Document | Title | Date |
20080200647 | On-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—[CH | 08-21-2008 |
20080207874 | Peptide 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 |
20080242835 | Ring-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 PG | 10-02-2008 |
20080281075 | ASYMMETRIC 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 NR | 11-13-2008 |
20080287649 | Methods 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 |
20080287650 | High 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 |
20080319162 | Process 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 |
20090062509 | CHELATION 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 |
20090069534 | Hydrochloride 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 |
20090076244 | Beta 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 |
20090088553 | Bis-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 |
20090111969 | MACROCYCLIC 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 |
20090143565 | Methods 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 |
20090149629 | CRFR1 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 |
20090156785 | METHOD 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 |
20090163695 | Process 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 |
20090240027 | INTERMEDIATES 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 |
20090264617 | METHOD 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 |
20090275727 | Peptide 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 |
20090275728 | COMPOUND 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; R | 11-05-2009 |
20090299033 | Methods 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 |
20090326192 | BIOLOGICALLY 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 |
20090326193 | STABILIZING 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 |
20090326194 | PROCESS 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 |
20100022746 | SYNTHESIS 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 |
20100036089 | Methods 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 |
20100069606 | Tubular 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 |
20100137559 | PROCESS 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 |
20100168380 | PROCESS 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 |
20100168381 | CONJUGATES 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 |
20100184946 | Preparation of Fine Particles - A process and device for the precipitation of an organic compound comprising the steps:
| 07-22-2010 |
20100216969 | IMMOBILISATION 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 |
20100216970 | METHODS, 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 |
20100228004 | TEMPLATES 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 |
20100249370 | PROCESS 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 |
20100249371 | PURIFICATION 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 |
20100261871 | CONFORMATIONALLY 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 |
20100273977 | PROCESS 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 |
20100286363 | CYCLIC 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 |
20110046345 | Methods 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 |
20110087002 | Methods 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: D | 04-14-2011 |
20110092669 | SYNTHESIS 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 ISA | 04-21-2011 |
20110144302 | POLYPEPTIDE - 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) EQQX | 06-16-2011 |
20110172391 | PROTEIN 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 |
20110245459 | Processes 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 |
20110257364 | PROCESS 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 |
20110263815 | TRIAZOLE 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 |
20110313130 | BIFUNCTIONAL CHELATING AGENTS - A bifunctional chelating agent of the formula (I): | 12-22-2011 |
20120059146 | METHOD 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 |
20120065366 | CYCLIC 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 |
20120101253 | STRUCTURED 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 |
20120142892 | CONTOXIN 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 |
20120190815 | AZACYCLOHEXAPEPTIDE 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 |
20120202968 | 2-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 |
20120208981 | Method 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 |
20120214967 | CROSS-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 |
20120220752 | TRI-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 VIII | 08-30-2012 |
20120226018 | Process 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)-NH | 09-06-2012 |
20120232247 | PROCESSES 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 |
20120302728 | Actagardine 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 |
20130018171 | PURIFICATION 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 |
20130030149 | PROCESS 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 |
20130109833 | CYCLIC PEPTIDE COMPOUND OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF AND METHOD FOR PRODUCING SAME | 05-02-2013 |
20130116404 | TARGETED NON-INVASIVE IMAGING PROBES OF EGFR EXPRESSING CELLS - A probe for imaging EGFR expressing cells includes an EGFR targeting moiety, a reporter moiety, and a hydrophilic linker that links the EGFR targeting moiety to the reporter moiety. The hydrophilic linker enhances solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells. | 05-09-2013 |
20130123463 | METHODS 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 |
20130144034 | METHOD 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 |
20130165625 | PEPTIDES 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 |
20130197188 | USE 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 |
20130237685 | LINEAR ASSEMBLIES, BRANCHED ASSEMBLIES, MACROCYCLES AND COVALENT BUNDLES OF FUNCTIONALIZED BIS-PEPTIDES - Provided is a macromolecule comprising two or more functionalized bis-peptides connected by one or more linkers, and methods of making thereof. In some embodiments, the functionalized bis-peptides are covalently attached to one or more functionalized bis-peptides to form linear strings of functionalized bis-peptides, macrocycles of functionalized bis-peptides, three-dimensional networks of functionalized bis-peptides, and combinations of any of these. Also provided is a macromolecule comprising two or more bis-peptides connected by one or more linkers, and methods of making thereof. In some embodiments, the bis-peptides comprise non-functionalized bis-peptides, functionalized bis-peptides or a combination of both functionalized and non-functionalized bis-peptides. In some embodiments, the bis-peptides are covalently attached to one or more bis-peptides to form linear strings of bis-peptides, macrocycles of bis-peptides, three-dimensional networks of bis-peptides, and combinations of any of these. | 09-12-2013 |
20130261286 | PROCESS FOR PREPARING CASPOFUNGIN AND NOVEL INTERMEDIATES THEREOF - The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N | 10-03-2013 |
20130274436 | USE OF ANILINE IN THE RADIOSTABILIZATION OF OXIME LIGATION - A method of radiostabilizing an oxime ligation or imine formation reaction using aniline is described. | 10-17-2013 |
20130281657 | MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES - The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol. | 10-24-2013 |
20130296529 | PROCESS FOR PURIFYING CYCLOLIPOPEPTIDE COMPOUNDS OR THE SALTS THEREOF - A method for purifying a cyclic lipopepteide or a salt thereof is provided. The method comprises the steps: (1) extracting a fermentation broth containing a compound of formula I or a salt thereof, to obtain an extract 1 after filtration or centrifugation; (2) diluting or concentrating the extract 1 under vacuum to decrease the content of the organic solvent, to obtain an extract 2; (3) loading the extract 2 onto a macroporous absorption resin; (4) washing the macroporpous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution; and (5) eluting the compound of formula I off from the macroporous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution as an eluant. Compared with the prior art, the purification method has the advantages that fewer organic solvent is used, no silica gel is used, the harm to the environment is less, and the purity of the collected compound of formula I is improved. | 11-07-2013 |
20130317195 | HER2DELTA16 PEPTIDES - The present invention provides cyclic peptides comprising a dimer of peptides, each peptide comprising a sequence corresponding to the HER2 splice variant HER2Delta16, wherein the cyclic peptide is cyclized via a disulfide bond between the peptides and via an amino acid linking the peptides. The invention also provides methods of making antibodies that specifically bind to HER2Delta16 homodimers using said cyclic peptides. | 11-28-2013 |
20140046021 | SELF-MAGNETIC METAL-SALEN COMPLEX COMPOUND - The molecular structures of metal-salen complexes which exerts pharmacological effects are clarified and the metal-salen complexes having such molecular structures and their derivatives are provided. A metal-salen complex compound is characterized in that a metal atom part in each of multiple molecules of the metal-salen complex or its derivative is multimerized via water. | 02-13-2014 |
20140051828 | METHODS FOR PREPARING INTERNALLY CONSTRAINED PEPTIDES AND PEPTIDOMIMETICS - The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, | 02-20-2014 |
20140073761 | CONJUGATES CONTAINING HYDROPHILIC SPACER LINKERS - Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations. | 03-13-2014 |
20140073762 | MULTIPLE STATIONARY PHASE MATRIX AND USES THEREOF - The present invention generally provides a separation matrix comprising at least two stationary phases and a stationary phase comprising at least one chiral modality and at least one achiral modality. Also provided are methods of using the separation matrix or the stationary phase to separate enantiomers of one or more chiral molecules. | 03-13-2014 |
20140100353 | ALDEHYDE ACETAL BASED PROCESSES FOR THE MANUFACTURE OF MACROCYCLIC DEPSIPEPTIDES AND NEW INTERMEDIATES - The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, | 04-10-2014 |
20140114049 | PREPARATION METHOD OF MICAFUNGIN SODIUM - The method of the preparation of micafungin sodium comprises the step of mixing the weak base and the aqueous solution containing micafungin acid (the structure is illustrated by formula I) or the mixed aqueous solution containing the compound of formula I and organic solvent in order to obtain the sodium salt of micafungin (the structure is illustrated by formula II). | 04-24-2014 |
20140142277 | CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS - 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 ISA | 05-22-2014 |
20140148573 | MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS - The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient. | 05-29-2014 |
20140179897 | CRYSTAL STRUCTURES OF DOLASTATIN 16, DOLAMETHYLLEUINE AND DOLAPHENVALINE, AND METHODS FOR PREPARING DOLAMETHYLLEUINE AND DOLAPHENVALINE - The present invention relates to the crystal structures of dolastatin 16, dolamethylleuine and dolaphenvaline. The present invention also relates to processes for preparing dolamethylleuine and dolaphenvaline. The present invention further relates to computer readable medium with crystal structural data and/or information stored thereon. | 06-26-2014 |
20140213757 | CASSETTE FOR RADIOPHARMACEUTICAL SYNTHESIS - The present invention is directed to a modified synthesis cassette ( | 07-31-2014 |
20140243499 | PEPTIDE DERIVATIVES AND USE THEREOF AS CARRIERS FOR MOLECULES IN THE FORM OF CONJUGATES - The invention relates to peptide derivatives (peptides and pseudo-peptides) and use thereof as vectors for molecules of interest. The invention also relates to conjugates containing a peptide derivative of the invention bound to a molecule of interest. The peptides and prodrug conjugates of the invention can be used to vectorise molecules of pharmaceutical or diagnostic interest, such as, for example, therapeutic molecules, imaging or diagnostic agents, or molecular probes, across cell membranes, and notably to promote their transport across the blood-brain barrier (BBB). | 08-28-2014 |
20140243500 | CALIBRATION AND NORMALIZATION SYSTEMS AND METHODS FOR RADIOPHARMACEUTICAL SYNTHESIZERS - The present invention relates to calibration and normalization systems and methods for ensuring the quality of radiopharmaceuticals during the synthesis thereof, such as radiopharmaceuticals used in Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT). | 08-28-2014 |
20140288266 | Synthesis 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 ISA | 09-25-2014 |
20140303343 | CYCLOSPORIN A FORM 2 AND METHOD OF MAKING SAME - Disclosed herein are methods of making cyclosporin A Form 2. | 10-09-2014 |
20140329989 | PREPARATION OF MICAFUNGIN INTERMEDIATES - The present invention relates to the preparation of compounds, in particular to the preparation of compounds of formula (I), which may be used with a compound of formula (VI), or a salt thereof as intermediates for the preparation of antifungal agents, preferably micafungin (MICA) or a salt thereof. | 11-06-2014 |
20140364583 | BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY - β-Hairpin peptidomimetics of the general formula Cyclo(—Xaa | 12-11-2014 |
20150018517 | FLUORESCENT IMAGING AGENTS - Provided is a family of intramolecularly quenched imaging agents for use in both in vivo and in vitro imaging that contain at least one enzymatically cleavable oligopeptide and two fluorophores or a fluorophore and a quencher. When subjected to proteolytic cleavage, at least one fluorophore is unquenched and becomes capable of producing a fluorescent signal upon excitation with light of an appropriate wavelength. Also provided are in vivo and in vitro imaging methods using such imaging agents. | 01-15-2015 |
20150025219 | CYCLIC PENTADEPSIPEPTIDES AND MICROORGANISM OF FUSARIUM STRAIN PRODUCING THE SAME - Disclosed is a | 01-22-2015 |
20150038671 | Efficient Synthesis of CN2097 and RC7 and Their Analogs - Synthesized macrocyclic ligand, CN2097 and analogs, optimized with systemic structure modifications to develop the compounds with lower molecular weights and less peptidic characters. | 02-05-2015 |
20150133630 | Screening Method for Peptide Binding to Target Molecule in PH-Dependent Manner - An object of the present invention is to provide molecules that bind to a target molecule in a pH dependent manner and a screening method for selecting such molecules. Provided is a screening method for selecting peptides that bind to a target molecule at a first pH and do not bind thereto at a second pH, including a step of preparing a peptide library in which each mRNA contains at least one special amino acid that undergoes a pH-dependent change in the charge of the side chain thereof, a step of bringing the peptide library into contact with the target molecule and incubating them under the first pH condition and selecting peptides that bind to the target molecule, and a step of selecting, from the peptides which have bound to the target molecule, peptides that do not bind to the target molecule under the second pH condition. | 05-14-2015 |
20150315243 | METHODS 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. | 11-05-2015 |
20150337013 | NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS - The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against | 11-26-2015 |
20160008495 | Metallocene Compounds and Labeled Molecules Comprising the Same for In Vivo Imaging | 01-14-2016 |
20160068564 | METHOD FOR ISOLATING CASPOFUNGIN - The present invention relates to a method for isolating caspofungin and to a novel crystalline form of caspofungin diacetate thus obtained. | 03-10-2016 |
20160083432 | CRYSTALLINE FORM OF CYCLOSPORIN A, METHODS OF PREPARATION, AND METHODS FOR USE THEREOF - The present invention relates generally to crystalline forms of cyclosporin A and particularly to a newly identified form of cyclosporin A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders. | 03-24-2016 |