Abstract: 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.
Abstract: A peptide which can adopt a 310-helical conformation in which the side chains of two amino acid residues in the peptide backbone are linked by a group comprising an aromatic 5-membered ring.
Type:
Grant
Filed:
April 22, 2011
Date of Patent:
January 5, 2016
Assignees:
DRUG DISCOVERY LABORATORY AS
Inventors:
Øyvind Jacobsen, Pål Rongved, Jo Klaveness
Abstract: The present invention relates to the use of alpha-1-antitrypsin for the preparation of effective drugs for the treatment of chronic fatigue syndrome. In addition, the present invention relates to the use of plasma or other therapeutic forms with an alpha-1-antitrypsin content sufficient to obtain a dose of 6 mg or more of alpha-1-antitrypsin per kg of body weight at a frequency of between 1 and 31 days.
Type:
Grant
Filed:
June 24, 2010
Date of Patent:
December 8, 2015
Assignee:
Grifols, S.A.
Inventors:
Ana Garcia Quintana, José Alegre Martin
Abstract: The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
Type:
Grant
Filed:
June 29, 2010
Date of Patent:
December 8, 2015
Assignee:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Inventors:
Muriel Caussil-Amblard, Jean Martinez, Julien Tailhades
Abstract: The present invention relates to a method of separating one or more immunoglobulin containing proteins from a liquid. The method includes first contacting the liquid with a separation matrix comprising ligands immobilized to a support; allowing the immunoglobulin containing proteins to adsorb to the matrix by interaction with the ligands; followed by an optional step of washing the matrix containing the immunoglobulin containing proteins adsorbed thereon; and recovering said immunoglobulin containing proteins by contacting the matrix with an eluent which releases the proteins.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
November 17, 2015
Assignee:
GE Healthcare Bio-Sciences AB
Inventors:
Tomas Bjorkman, Bjorn Noren, Gustav Rodrigo, Jelena Vasic, Per-Mikael Aberg
Abstract: There is provided a practical method for preparing lipopeptide compounds, which method is capable of inexpensive mass production without requiring complicated operations. The lipopeptide compound of formula (3): is produced by reacting an ester compound of formula (1): with an ?-amino acid compound of formula (2): in the presence of a base and within a solvent containing a nonpolar organic solvent.
Abstract: The invention relates to a method and a kit for preparing a radiopharmaceutical, the method comprising the steps: elution of a 68Ge/68Ga-Generator using hydrochloric acid as an eluent for obtaining a generator eluate comprising 68Gallium, feeding the generator eluate through a cation exchange cartridge, which collects the 68Gallium, separating the used eluent, eluting the 68Gallium from the cation exchange cartridge using a solution comprising sodium chloride and hydrochloric acid and feeding the resulting eluate into an aqueous precursor mixture comprising at least a labelling precursor thereby forming a reaction solution.
Abstract: The present invention relates to novel tubulin binding molecules of formula (I) and their use for the treatment of cancer and other diseases.
Abstract: The invention relates to bifunctional stapled or stitched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stitched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stitched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stitched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Uses of the inventive bifunctional stapled or stitched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.
Type:
Grant
Filed:
July 13, 2010
Date of Patent:
October 20, 2015
Assignee:
President and Fellows of Harvard College
Inventors:
Gregory L. Verdine, Tom N. Grossmann, Raymond E. Moellering, Tsung-Han Johannes Yeh, Yue Rebecca Yue Liang, Youbean Oak
Abstract: The present invention provides, in part, a chromatographic restricted access media comprising aminopropyl groups derivatized with polysuccinamide that is derivatized with 1-ethylpropylamine and denatured human serum albumin. Methods of purifying polypeptides and complexes thereof are also provided.
Abstract: A process is provided for preparing a conjugate of Formula (I-A) or (I) comprising a polypeptide containing n number of tyrosine units, where n is an integer greater than or equal to 1, dispersed within the amino acid chain having and amino terminus end (A1) and an acid terminus end (A2) of the protein or polypeptide and having a weight average molecular weight equal to or greater than 10,000 Daltons (10 kDa), wherein the conjugate comprises a number m of tyrosine conjugates (modified tyrosine residues) as depicted in Formula (I-A) or (I), where m is at least one and is less than or equal to n: where X, Lg, L and R are as defined herein.
Type:
Grant
Filed:
July 5, 2012
Date of Patent:
October 6, 2015
Assignee:
NOVARTIS AG
Inventors:
Roberto Adamo, Martin Allen, Francesco Berti, Elisa Danieli, Qi-Ying Hu
Abstract: Novel 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) or glycosylamine 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 containing an aziridinyl ring. Optional subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product. Coupling of a peptide thioacid and glycosylamine yields a glycosylated peptide.
Abstract: The present invention relates to a method for preparing a cyclic peptide with antiparasite activity and anticancer activity. The invention also relates to this peptide as an antiparasite agent, for example in the treatment of toxoplasmosis and as an anticancer agent. The invention also relates to the use of this cyclic peptide for treating organs ex vivo before transplantation.
Type:
Grant
Filed:
April 6, 2010
Date of Patent:
September 15, 2015
Assignees:
UNIVERSITE JOSEPH FOURIER (GRENOBLE 1), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, (INSERM) INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE
Abstract: The invention is a novel chemical coupling methodology for the synthesis of a stable polysaccharide-protein conjugates as the immunogenic component for vaccines. A covalent bond is formed between polysaccharide and protein in the dry state in the absence of water and oxygen. A polysaccharide antigen is covalently linked to the protein by activating the polysaccharide with periodate to introduce aldehyde groups into the polysaccharide, lyophilizing an aqueous mixture of a protein and activated polysaccharide, sealing the dry lyophilized mixture in a vessel under vacuum or inert gas and then incubating the sealed vessel at an elevated temperature.
Abstract: Novel template-fixed ?-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are ?-amino acid residues connected from the carbonyl (C?O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these ?-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.
Type:
Grant
Filed:
February 4, 2011
Date of Patent:
August 18, 2015
Assignee:
POLYPHOR AG
Inventors:
Frank Otto Gombert, Alexander Lederer, Ralf Löwe, Daniel Obrecht, Barbara Romagnoli, Johann Zimmermann, Kalpana Patel
Abstract: A solid phase method for synthesizing a peptide containing three or more amino acid residues utilizing both Boc and Fmoc protected amino acids and a chloromethylated polystyrene resin.
Type:
Grant
Filed:
January 4, 2013
Date of Patent:
July 28, 2015
Assignee:
IPSEN MANUFACTURING IRELAND LIMITED
Inventors:
Catherine Fiona Dalton, John Stuart Eynon, Steven Allen Jackson, Gary Alexander Siwruk
Abstract: The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula (II): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.
Type:
Grant
Filed:
October 26, 2011
Date of Patent:
July 28, 2015
Assignee:
Ferring B.V.
Inventors:
Jon Holbech Rasmussen, Jens Fomsgaard, Stefan Hansen, Palle Hedengran Rasmussen, Wolfgang Oliver Wachs
Abstract: The present invention discloses a process for the preparation of a Poly-ubiquitin chain, this process comprising ligating a Ubiquitin thioester Ubm-SR with a Ubiquitin Ubq. Further are disclosed poly-ubiquitin chains prepared according to this process, in particular poly-ubiquitin chains containing at least one unnatural amino acid.
Type:
Grant
Filed:
February 9, 2011
Date of Patent:
July 14, 2015
Assignee:
BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITY