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| Number | Title | Issue Date |
| 8212002 | Synthesis of glatiramer acetate A process of making a polylpeptide or a pharmaceutically acceptable salt thereof comprises reacting a L-lysine protected polypeptide, which comprises L-alanine, L-tyrosine, L-glutamate, and L-lysine that is protected with a protecting group, with a tetraalkylammoniu... | 07/03/2012 |
| 7423117 | Surface-functionalized carrier material and solid phase synthesis method The invention concerns a novel surface-functionalized carrier material with a polymeric surface and at least one linker compound according to the general formula (I), which is covalently bound to the surface. In the formula, P indicates the polymeric surface; R... | 09/09/2008 |
| 7414106 | Synthesis of peptide α-thioesters Disclosed herein is a new method for the solid phase peptide synthesis (SPPS) of C-terminal peptide α thioesters using Fmoc/t-Bu chemistry. This method is based on the use of an aryl hydrazine linker, which is totally stable to conditions required for Fmoc-SPPS. Wh... | 08/19/2008 |
| 7393920 | Microwave-assisted peptide synthesis An instrument and process for accelerating the solid phase synthesis of peptides is disclosed. The method includes the steps of deprotecting a protected first amino acid linked to a solid phase resin by admixing the protected linked acid with a deprotecting solution... | 07/01/2008 |
| 7348310 | Synthetic methods for aplidine and new antitumoral derivatives, methods of making and using them The invention relates to aplidine derivatives of the general formula: which are useful for the treatment of tumors. ... | 03/25/2008 |
| 7247701 | Amino amides, peptides and peptidomimetics Synthetic methods and compounds involving amino amides, peptides and peptidomimetics. Amino amide derivatives are prepared via the one-step three-component reaction of a glyoxamide, an amine, and an organoboron derivative. Conversion of the product to another glyoxa... | 07/24/2007 |
| 7226905 | Process for the preparation of cyclosporin derivatives The invention concerns a novel method for preparing an intermediate polyanion for preparing cyclosporin derivatives by treating a cyclosporin with a hexamethyldisilazane metal salt, optionally in the presence of a metal halide. The treated cyclosporin has one or sev... | 06/05/2007 |
| 7192713 | Stabilized compounds having secondary structure motifs The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involve... | 03/20/2007 |
| 7179918 | HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceuti... | 02/20/2007 |
| 7138489 | Method for producing a modified peptide The present invention is a method for producing a peptide or a protein in which a side chain contains a modified amino acid residue, which comprises chemically producing a peptide fragment containing an amino acid residue having a modified side chain using an weak a... | 11/21/2006 |
| 7122628 | Process for the synthesis of a peptide having a Trp residue A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said pro... | 10/17/2006 |
| 7049399 | Process for the preparation of polypeptide 1 A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutica... | 05/23/2006 |
| 7029846 | Site-specific protein modification Site-specific modified proteins and method for producing site-specific modified proteins using amino acid analogs are disclosed. Methods for labeling proteins at a desired site in the presence of nucleophilic side chains, including lysine and cysteine side chains, a... | 04/18/2006 |
| 7019113 | Reversible modification of membrane interaction An process for the reversible modification of membrane interaction of a compound is described. Modification of membrane interaction can be used to facilitate delivery of molecules to cells in vitro and in vivo. The described modifiers, which are used to reversibly i... | 03/28/2006 |
| 7001982 | Non-natural C-linked carbo-β-peptides with robust secondary structures Nonnatural C-linked carbo-β-peptides with robust secondary structures, which involves the synthesis of a new class of β-peptides called C-linked carbo-β-peptides. The compounds are favorably disposed for the formation of stable helical structures and are useful a... | 02/21/2006 |
| 6953858 | HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical co... | 10/11/2005 |
| 6946542 | Amino amides, peptides and peptidomimetics Synthetic methods and compounds involving amino amides, peptides and peptidomimetics. Amino amide derivatives are prepared via the one-step three-component reaction of a glyoxamide, an amine, and an organoboron derivative. Conversion of the product to another glyoxa... | 09/20/2005 |
| 6897289 | Peptide synthesis procedure in solid phase A procedure for the solid phase peptide synthesis (SPPS), following a linear or convergent strategy, wherein the peptides contain the sequence of general formula (I), wherein n, Y, X and A1 to An have the meanings indicated in the specification... | 05/24/2005 |
| 6770436 | Chemical amplification for the synthesis of patterned arrays Radiation-activated catalysts (RACs), autocatalytic reactions, and protective groups are employed to achieve a highly sensitive, high resolution, radiation directed combinatorial synthesis of pattern arrays of diverse polymers. When irradiated, RACs produce catalyst... | 08/03/2004 |
| 6762280 | High throughput assays for the proteotytic activities of clostridial neurotoxins In this application is described substrates for high-throughput assays of clostridial neurotoxin proteolytic activities. Two types of substrates are described for use in assays for the proteolytic activities of clostridial neurotoxins: (1) modified peptides or prote... | 07/13/2004 |
| 6759511 | Compound used as an amino-protecting group, process for preparing the same, and synthetic method of a peptide using the same The present invention relates to a carbonic acid ester compound of the following formula (1): in which X, Y, and Ar are defined in the specification, which can be easily combined with the amino group of an amino acid or ... | 07/06/2004 |
| 6750312 | Process for the preparation of supports for solid phase synthesis A method for preparing a solid support material for carrying out a chemical reaction, said method comprising the following steps: (i) reacting an amino functionalised solid material with a carboxylic acid having at least two similarly protected amino groups t... | 06/15/2004 |
| 6747009 | Peptidomimetic glutathione analogs The invention relates to peptidomimetic compounds with formula wherein Z═CH2 and Y═CH2, or Z═O and Y═O═O, which are novel analogs of glutathion and are inhibitors of glutathione S-transfer... | 06/08/2004 |
| 6747125 | Peptides intermediates for making GnRH antagonists Peptides which include unnatural amino acids and which either promote or inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists... | 06/08/2004 |
| 6627609 | LHRH antagonists having improved solubility properties The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. Medicaments in which the peptides according to the invention are contained can be used for the treatment of hormone-dependent tumours and hor... | 09/30/2003 |
| 6600016 | Multifunctionalized solid support resins for synthesis of combinatorial libraries and method for using the same Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functi... | 07/29/2003 |
| 6566495 | Very large scale immobilized polymer synthesis A synthetic strategy for the creation of large scale chemical diversity. Solid-phase chemistry, photolabile protecting groups, and photolithography are used to achieve light-directed spatially-addressable parallel chemical synthesis. Binary masking techni... | 05/20/2003 |
| 6562944 | Amide library formation using a "by-product-free" activation/coupling sequence Disclosed is an improved method for preparing an activated carboxylic acid in the form of a pentafluorophenyl ester, an improved method for making a carboxamide from a pentaflourophenyl ester, and a carboxamide and carboxamide library prepared using both ... | 05/13/2003 |
| 6548644 | Site protected protein modification Processes for conjugating proteins with polyethylene glycol are disclosed. The disclosed processes provide modified proteins having little or no decrease in their activity and include the steps of protecting one or more sites on the protein, contacting th... | 04/15/2003 |
| 6504005 | Long-acting drugs and pharmaceutical compositions comprising them Disclosed are conjugates of a polypeptide or oligopeptide with a low molecular weight lipophilic compound, the peptide and lipophilic group being covalently linked to one another either directly or via a connecting element, with the exception of (a) conju... | 01/07/2003 |
| 6492491 | Method of making hypusine peptides The invention relates to novel peptides synthesized according a method utilizing the hypusine reagent: ##STR1## wherein: Q1 Q2 and Q3 may be the same or different and are amino protective groups, provided that Q3 | 12/10/2002 |
| 6458923 | Modified position (7) bradykinin antagonist peptides The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an isoquinoline derivative which converts bradykinin agonists into bradykinin antagonists. The invention further includes the... | 10/01/2002 |
| 6433135 | PEG-LHRH analog conjugates PEG-LHRH analog conjugates, where a PEG moiety is covalently bound to a serine residue of a LHRH analog either directly or via a bifunctional linker molecule, such as an amino acid, and methods for producing these conjugates are provided in the present in... | 08/13/2002 |
| 6426184 | Method and apparatus for chemical and biochemical reactions using photo-generated reagents This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. Specifically, the method and apparatus of the present invention have applications i... | 07/30/2002 |
| 6380358 | Guanidinylation reagents Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.... | 04/30/2002 |
| 6376649 | Methods for the synthesis of - hydroxy-ଲ-amino acid and amide derivatives Methods for the synthesis of -hydroxy-ଲ-amino acid and amide derivatives and -ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehy... | 04/23/2002 |
| 6372717 | Synthetic peptides and their use in cosmetic or dermopharmaceutical compositions The invention concerns the use of peptides of general formula R1-L-Tyr-L-Arg-R2 in which R1=H or a R3-C=0 with R3=a C1 to C20 alkyl chain, linear or branched, saturated or unsaturate, hydroxylated or not, or with R3=an aryl, aryl-alkyl or alkyloxy or aryl... | 04/16/2002 |
| 6288036 | Bradykinin type peptides The substitution of the L-Pro at the 7-position with D-Phe or D-Tic and substitution of the L-Phe at the 8-position with hydroxyproline ethers and thioethers of the peptide hormone bradykinin and other additional substituted analogs of bradykinin converts... | 09/11/2001 |
| 6277958 | Method for preparing peptide thiol ester The present invention provides a method for producing a peptide thiol ester using fluoren-9-ylmethoxycarbonylamino acid (Fmoc-amino acid). The method is for peptide synthesis and involves (1) using and removing the Fmoc group bound as the protective group... | 08/21/2001 |
| 6251625 | Process for preparing peptides and N-carbamoyl-protected peptides The invention concerns a process for the enzymatic preparation of protected di- and oligopeptides and the separation of the protective groups used. The process according to the invention enables peptides to be synthesized simply and economically and the p... | 06/26/2001 |
