Class / Patent application number | Description | Number of patent applications / Date published |
530331000 | Tripeptides, e.g., tripeptide thyroliberin (TRH), melanostatin (MIF), etc. | 57 |
20080262200 | 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. | 10-23-2008 |
20090012263 | Process for Production of (1,3-Disubstituted Indolyl)-Urea Derivatives, Intermediates Therefor, and Process for Production of the Intermediates - A process for the production of (1,3-disubstituted indolyl) urea derivatives represented by the general formula (1), characterized by reacting a 1-substituted-aminoindole derivative with a phenyl halocarbonate to form a carbamate derivative, subjecting the carbamate derivative to Mannich reaction with a secondary amine and formaldehyde to form a 3-aminomethylindole derivative represented by the general formula (6), and then reacting the derivative (6) with a peptide derivative; indole derivatives represented by the general formula (6) which are intermediates for the above process; and a process for the production of the indole derivatives. | 01-08-2009 |
20090018311 | METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF - Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided. | 01-15-2009 |
20090048429 | Processes and intermediates - The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof. | 02-19-2009 |
20090069537 | Treatment Of Disease By Inducing Cell Apoptosis - The present invention relates generally to the treatment and prevention of diseases characterized by excess cell proliferation and/or activation. In particular, the present invention provides compositions and methods to suppress the activation and/or proliferation of various cells. In preferred embodiments, the present invention provides compositions and methods to suppress the activation and/or proliferation of mesenchymally derived cells (including, but not limited to hepatic stellate cells), as well as cells with abnormal growth characteristics. In particularly preferred embodiments, the present invention provides compositions and methods to inhibit or eliminate fibrosis. In alternative preferred embodiments, the present invention provides compositions and methods to induce fibrosis. | 03-12-2009 |
20090234098 | METHOD OF PREPARING PEPTIDE - The present invention provides a method of preparing an intermediate for LHRH antagonists, which requires fewer steps than conventional methods and provides the intermediate in high yield and high purity. | 09-17-2009 |
20090299036 | AGENT FOR PREVENTING ARTERIOSCLEROSIS, AGENT FOR SUPPRESSING VASCULAR INTIMAL THICKENING AND AGENT FOR IMPROVING VASCULAR ENDOTHELIAL FUNCTION - There is provided an agent having at least one of an improving effect on vascular endothelial functions and an inhibitory effect on vascular intimal thickening, as well as a prophylactic of arteriosclerosis, which have excellent safety, improve functions associated with the vascular endothelium, have effects of preventing various diseases associated with vascular endothelial functions and of inhibiting vascular intimal thickening, and may be expected to provide prophylactic effect on arteriosclerosis or the like. The agents of the present invention contain, as an active component: (a) Xaa-Pro-Pro, (b) a hydrolysate of animal milk casein containing Xaa-Pro-Pro, or a concentrate thereof, or (c) a fermentation product containing Ile-Pro-Pro and/or Val-Pro-Pro obtained by fermenting a starting material containing milk protein with a bacterial strain of the species | 12-03-2009 |
20090306340 | METHOD FOR PURIFICATION OF OLIGOPEPTIDES - The present invention provides: a method for purifying an oligopeptide, which comprises a step of contacting a solution comprising the oligopeptide and a neutral amino acid with an ion exchange resin in an effective pH range; the method for purifying an oligopeptide, which comprises (a) a step of passing a solution comprising the oligopeptide and the neutral amino acid through a column packed with an ion exchange resin, and (b) a step of eluting the oligopeptide contacted with the ion exchange resin with an eluting solvent; the above method using a weakly acidic cation exchange resin; the above method using a weakly basic anion exchange resin, etc. | 12-10-2009 |
20090318668 | Water-Soluble CC-1065 Analogs and Their Conjugates - This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor. | 12-24-2009 |
20100016550 | Methods for Site-Specific Pegylation - The present invention relates to methods for the chemo-selective pegylation of the cysteine residue having unoxidized sulfhydryl side-chain and free α-amino group in proteins, peptides and other molecules. Similar methods are provided for the chemo-selective pegylation of the homocysteine, selenocysteine, penicillamine, and N-methyl-cysteine residues. | 01-21-2010 |
20100022747 | PROPHYLACTIC AGENT FOR HEART FAILURE - The present invention provides an agent having a suppressive action against the thickening of the heart wall, a prophylactic agent for heart failure containing the above described agent, and functional foods expected to have a prophylactic effect for heart failure. The agent for suppressing heart wall thickening comprises Xaa Pro Pro as an active ingredient. | 01-28-2010 |
20100022748 | PROPHYLACTIC AGENT FOR RENAL FAILURE - The present invention provides an agent having a suppressive action against kidney glomerular disease and renal arteriosclerosis, a prophylactic agent for renal failure containing the above described agent, and functional foods expected to have a prophylactic effect for renal failure. The agent for preventing kidney glomerular disease and renal arteriosclerosis comprises Xaa Pro Pro as an active ingredient. | 01-28-2010 |
20100029904 | Carrier for Separation, Method for Separation of Compound, and Method for Synthesis of Peptide Using the Carrier - A carrier for use for separation purpose and a method for separation of a compound enable a chemical reaction to be performed in a liquid phase, a compound of interest to be separated from the liquid phase after the completion of the reaction readily, the separated compound to be evaluated by structural analysis or the like while the compound is being bound to the carrier, and the compound to be separated from the carrier readily. A carrier for separation is also provided which has a reaction site capable of reacting with other compound(s) on a benzene ring, and a long-chain group having a specified carbon atom(s) at each of the ortho-position and the para-position of the reaction site through an oxygen atom. | 02-04-2010 |
20100056756 | COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase. | 03-04-2010 |
20100099846 | DEPSIPEPTIDE CONTAINING LACTIC ACID RESIDUE - Disclosed are a compound represented by the general formula (I) below and a polymer compound obtained by polymerizing such a compound. R | 04-22-2010 |
20100099847 | CRYSTAL OF GLUTATHIONE AND PROCESS FOR PRODUCTION THEREOF - Disclosed is a crystal of glutathione having an average width of 7 to 40 μm and an average particle diameter of 10 to 60 μm, preferably having an angle of repose of 53 degree or less, more preferably having a crude specific volume of 5.0 cm | 04-22-2010 |
20100105864 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIARRHEA - A compound which is able to activate a calcium receptor can be used as an active ingredient of a prophylactic or therapeutic agent for treating diarrhea. The compound can be a peptide such as γ-Glu-X-Gly (X represents an amino acid or an amino acid derivative), γ-Glu-Val-Y (Y represents an amino acid or an amino acid derivative), γ-Glu-Ala, γ-Glu-Gly, γ-Glu-Cys, γ-Glu-Met, γ-Glu-Thr, γ-Glu-Val, γ-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, γ-Glu-Met(O), γ-Glu-γ-Glu-Val, γ-Glu-Val-NH | 04-29-2010 |
20100145013 | PROCESS FOR PREPARING (1R,2S,5S)-N-[(1S)-3-AMINO-1-(CYCLOBUTYLMETHYL)-2,3-DIOXOPROPYL]-3-[(2S)-- 2-[[[(1,1-DIMETHYLETHYL)AMINO]-CARBONYL]AMINO]-3,3-DIMETHYL-1-OXOBUTYL]-6,- 6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXANE-2-CARBOXAMIDE - The present invention relates also to a process for the preparation of intermediate compounds useful in preparing the compounds of Formula (I) using the process of Scheme (II). | 06-10-2010 |
20100234564 | METHODS AND INTERMEDIATES FOR CHEMICAL SYNTHESIS OF POLYPEPTIDES AND PROTEINS - The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal N-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a β-(methylamino)-thioester intermediate that spontaneously rearranges to form an amide bond. Furthermore, the invention relates to methods of converting N-methyl-thiazolidine to N-methyl-cysteine (SEQ ID NO: 1) of polypeptides and proteins. The invention also relates to methods of synthesizing peptide-thioester from peptide-acid fluoride. | 09-16-2010 |
20100234565 | MOLECULARLY IMPRINTED POLYMERS FOR THE RECOGNITION OF GLUTATHIONE GSH, METHODS FOR PREPARING SAME AND USES THEREOF - The present invention relates to new molecularly imprinted polymers which are suitable for the selective recognition of glutathione GSH and/or of an analog thereof, and in particular which are of use for the treatment of media comprising in particular a mixture of glutathione GSH, and/or of an analog thereof, with GSH adducts. | 09-16-2010 |
20100249373 | SCREENING METHODS - A method of identifying a compound that modulates NCKX-mediated calcium ion exchange across a cell membrane, the method comprising the steps of providing an adherent cell, the cell membrane of which comprises a NCKX polypeptide or a functionally equivalent variant thereof, exposing the cell in suspension to a fluorescent calcium-sensitive dye, thereby causing intracellular uptake of the dye, settling the cell onto a solid support without allowing the cell to adhere to the solid support, exposing the cell to a test compound, exposing the cell to calcium and potassium ions, and measuring fluorescence from the intracellular calcium-sensitive dye after exposure of the cell to the test compound and the calcium and potassium ions, thereby to determine the rate and/or amount of calcium ion exchange across the cell membrane in the presence of the test compound. | 09-30-2010 |
20100249374 | DIPHENYLMETHANE COMPOUND - Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis. | 09-30-2010 |
20100317831 | PROBE COMPOUNDS FOR PROTEIN TYROSINE PHOSPHATASE (PTP) AND PRECURSORS THEREOF - A probe compound for protein tyrosine phosphatases (PTPs), as shown in Formula (I) is provided. | 12-16-2010 |
20110015372 | METHODS AND COMPOSITIONS FOR IMPROVED UPTAKE OF BIOLOGICAL MOLECULES - A “one-step” process for production of peptides and other organic molecules which are both esters and also acetylated forms of the desired molecule. The ester may be a mono-ester, di-ester, or another poly-ester, complexed with a molecule for protecting the organic molecules in the digestive tract. The method allows simple adjustment of the delivery properties of the peptides produced, in particular adjustment or addition of lipiphilic tendencies. A therapeutic or nutrient made by this method comprises acetylated organic molecule esters, in particular an acetylated peptide ester or even an acetylated amino acid ester and demonstrates improved metabolic properties leading to increased efficiency for therapeutic and cosmetic purposes including oral, transdermal, sublingual, buccal, and topical administration. The present disclosure further teaches several specific examples of acetylated esters, including acetyl-glutathione-ester (mGSH), MCAR (carnosine), pyruvate and others modified from base forms by the methods of the present disclosure. | 01-20-2011 |
20110082281 | CASEIN HYDROLYZATE, PROCESS FOR PRODUCING THE SAME AND USE THEREOF - The present invention relates to a casein hydrolysate containing free amino acids and in vivo indigestible peptides having minimally suppressed in vivo enzymatic digestibility, and expected to express functions, such as hypotensive effect, in living organism, and to a method for preparing such a hydrolysate, and use thereof. The casein hydrolysate of the present invention contains free amino acids and peptides, such as in vivo indigestible peptides including Xaa-Pro and Xaa-Pro-Pro, obtained by hydrolyzing animal milk casein to have an average chain length of not longer than 2.1 in terms of the number of amino acid residues, and has ACE inhibitory activity or hypotensive effect. | 04-07-2011 |
20110082282 | PROCESS OF PREPARING CONJUGATES OF ALLIUM ORGANOSULFUR COMPOUNDS WITH AMINO ACIDS, PEPTIDES, AND PROTEINS - Processes using | 04-07-2011 |
20110184147 | ENZYME SUBSTRATE FOR LABELING OF PROTEIN - The present invention provides a substrate of TGase represented by (fluorescent group)-(linker)-(a portion containing a Gln residue capable of recognition by transglutaminase (TGase))-R, wherein the fluorescent group is fluorescein isothiocyanate (FITC), Texas Red (TE) or dansyl (Dns) or a group derived therefrom; the linker is a group represented by —NH—(CH | 07-28-2011 |
20120022229 | COMPOUNDS AND METHODS FOR THE TREATMENT OF CANCER - The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. | 01-26-2012 |
20120065370 | PROCESS FOR THE PREPARATION OF IBODUTANT (MEN15596) AND RELATED INTERMEDIATES - This invention relates to a novel process for synthesising the product ibodutant shown in the figure below, consisting of a small number of high-yield steps involving reagents and solvents with low environmental impact, characterised by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesised by coupling of 6-methyl-2-benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalisations of 4-aminomethylpiperidine (2) | 03-15-2012 |
20120077959 | Asymmetric Cobalt-Catalyzed Cyclopropanation With Succinimidyl Diazoacetate - Cobalt(II) complexes of the D | 03-29-2012 |
20120088903 | CRYSTALLINE TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS - The invention relates to crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. | 04-12-2012 |
20120202970 | Fragment Ligated Inhibitors Selective for the Polo Box Domain of PLK1 - Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs. | 08-09-2012 |
20120329987 | Metal Abstraction Peptide (MAP) Tag and Associated Methods - Compositions comprising a tripeptide having the sequence XC | 12-27-2012 |
20130005945 | FORMING POROUS SCAFFOLD FROM CELLULOSE DERIVATIVES - Scaffold comprises a polymer defining macropores and comprising hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, which is crosslinked through the self-crosslinkable group. The macropores have an average pore size larger than 50 microns and are at least partially interconnected. In one method, bicontinuous emulsion comprising a continuous aqueous phase and a continuous polymer phase is formed. The polymer phase comprises hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, and is crosslinked through the self-crosslinkable group to form a polymer defining at least partially interconnected pores. In another method, phase separation is induced in a solution comprising a polymer precursor and water to form a bicontinuous emulsion comprising a continuous polymer phase and a continuous aqueous phase. The polymer precursor comprises a self-crosslinkable group and is crosslinked through the self-crosslinkable group in the emulsion to form a polymer defining at least partially interconnected macropores. | 01-03-2013 |
20130018172 | Metal Abstraction Peptide and Uses Thereof - Compositions comprising certain tripeptides which are capable of binding a metal in a square planar orientation, a square pyramidal orientation, or both, are disclosed in processes for modulating tagged peptides or proteins. Such compositions and processes may be used for site-specific chiral inversion of amino acids, site-specific peptide cleavage, and protein purification, among other uses. | 01-17-2013 |
20130035470 | CRYSTALLINE OXIDIZED GLUTATHIONE AND PRODUCTION METHOD THEREFOR - Provided is a novel crystal of oxidized glutathione hexahydrate. Crystal of oxidized glutathione hexahydrate is produced by cooling an aqueous solution containing oxidized glutathione to 15° C. or lower to precipitate a crystal of oxidized glutathione hexahydrate. | 02-07-2013 |
20130116407 | CONTROLLED RELEASE FROM MACROMOLECULAR CONJUGATES - The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates. | 05-09-2013 |
20130137852 | NOVEL COMPOUNDS AS DPP-IV INHIBITORS AND PROCESS FOR PREPARATION THEREOF - The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes. | 05-30-2013 |
20130211045 | MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR - The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders. | 08-15-2013 |
20130274439 | ANTIVIRAL COMPOUNDS - The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 10-17-2013 |
20140024803 | 18FDG MULTIMERIC POSITRON EMISSION TOMOGRAPHY IMAGING AGENTS - The present invention discloses | 01-23-2014 |
20140024804 | Crystalline Tripeptide Epoxy Ketone Protease Inhibitors - The invention relates to crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. | 01-23-2014 |
20140073763 | 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. | 03-13-2014 |
20140128571 | AROMATIC COMPOUNDS WITH SULFUR CONTAINING LIGANDS - Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: | 05-08-2014 |
20140275480 | NOVEL PROCESSES FOR PRODUCING SOVAPREVIR - The disclosure includes novel processes for producing Sovaprevir comprising adding | 09-18-2014 |
20140303344 | METHOD FOR THE STEREOSELECTIVE PREPARATION OF AMINO ACID DERIVATIVES - The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C | 10-09-2014 |
20140323690 | ANTIPROLIFERATIVE COMPOUNDS, CONJUGATES THEREOF, METHODS THEREFOR, AND USES THEREOF - Antiproliferative compounds having a structure represented by formula (II), where n, R | 10-30-2014 |
20140329990 | Hydroxyapatite-Targeting Multiarm Polymers and Conjugates Made Therefrom - The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance. | 11-06-2014 |
20140364586 | FUNCTIONALIZING REAGENTS AND THEIR USES - Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group. | 12-11-2014 |
20150031854 | Novel Derivatives of Hemin with Antibacterial and Antiviral Activity - The invention relates to novel hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the novel antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity. | 01-29-2015 |
20150073124 | micro-RNA INHIBITOR - The invention provides a microRNA inhibitor that has two or more sequences complementary to the sequence of microRNA to be the target of inhibition, which two or more complementary sequences are linked via one or more linker residues. | 03-12-2015 |
20150119553 | BIOCONJUGATES OF CYANINE DYES - Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. Bioconjugate cyanine compounds of Formula II are presented: | 04-30-2015 |
20150126708 | RADIOFLUORINATION METHOD - The present invention provides a method of radio fluorination of biological targeting molecules (BTMs) with the radioisotope | 05-07-2015 |
20150315235 | Combinatorial Synthesis of Libraries of Macrocyclic Compounds Useful in Drug Discovery - A library of macrocyclic compounds of the formula (I) | 11-05-2015 |
20150329590 | Cysteine Arylation Directed by a Genetically Encodable Pi-Clamp - Disclosed are methods of single-site-specific cysteine modification on peptide/protein molecules under physiologically relevant conditions. This process features several significant advantages over existing methods of peptide modification, such as specificity towards thiols over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions. Especially important is the specificity observed for thiols appearing in an X-Cys-Pro-X sequence over other thiols or disulfides, where X is Phe, Trp, or Tyr; under the inventive conditions, other cysteines or reactive functional groups on the same peptide/protein chain are not functionalized. | 11-19-2015 |
20150368295 | METHOD FOR PRODUCING PYRAZOLES, NOVEL PYRAZOLES AND APPLICATIONS THEREOF - A method for preparing a pyrazole of formula (I) in which R,R′ and R″ have different meanings, characterised in that it involves reacting a sydnone of formula (II) in which R and R′ have the meanings already indicated, with an alkyne of formula (III) in which R″ has the meaning already indicated, in the presence of copper, to obtain a pyrazole compound of formula (I) that is then isolated and salified if desired. | 12-24-2015 |
20160016993 | PROCESS FOR PREPARING TUBULYSINS - The invention described herein pertains to processes for preparing tubulysins and derivatives thereof. The invention described herein also pertains to processes for preparing tubulysin conjugates. The invention described herein also pertains to processes for preparing intermediates for preparing tubulysin conjugates. In one step, the alpha-thiazolyl alcohol is protected with triethylsilyl chloride in the presence of imidazole in an aprotic solvent. | 01-21-2016 |