Abstract: This invention provides FSH analogues having increased serum half-life relative to FSH. This invention also provides related compositions and methods for increasing fertility, egg production and spermatogenesis in a subject.
Type:
Grant
Filed:
July 21, 2006
Date of Patent:
October 5, 2010
Assignee:
The Trustees of Columbia University in the City of New York
Abstract: A bisubstrate inhibitor of Src kinases, having a nucleotide or N-heteroaromatic moiety; and a peptide/phosphopeptide, peptidomimetic, or phosphopeptide mimic moiety. The moieties are linked by a rigid or a flexible linker. The nucleotide or N-heteroaromatic moiety is ATP, ATP-mimics, N-heteroaromatics including purine-based derivatives, pyrimidine-based derivatives such as 2,4-diamino-5-substituted pyrimidine derivatives, pyrazole[3,4-d]pyrimidine derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrido[2,3-d]pyrimidine derivatives, amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, thieno- and furo-substituted derivatives, quinazoline derivatives, and quinoline derivatives, and several natural products such as aminogenistein.
Type:
Grant
Filed:
December 1, 2006
Date of Patent:
September 21, 2010
Assignees:
Board of Governers for Higher Education, State of Rhode Island and Providence Plantations
Inventors:
Keykavous Parang, Gongqin Sun, Anil Kumar, Nguyen H. Nam, Yue-Hao Wang, Guofeng Ye
Abstract: The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide.
Type:
Grant
Filed:
April 9, 2003
Date of Patent:
September 14, 2010
Assignee:
Novo Nordisk A/S
Inventors:
Shawn DeFrees, David Zopf, Robert Bayer, David Hakes, Xi Chen
Abstract: The invention concerns the use of a bombesin/gastrin releasing peptide antagonist in the treatment of inflammatory and immune-mediated inflammatory conditions, in particular sepsis, acute lung injury and rheumatoid arthritis as well as for the treatment or prophylaxis of brain disorders, preferably bipolar disorder, and in particular the different forms and/or subforms of bipolar disorder, such as mania, acute mania, severe mania, hypomania, depression, moderate depression, dysthymia, severe depression, episodes of mania and/or depression, psychosis/psychotic symptoms (e.g. hallucinations, delusions), mixed bipolar state, bipolar I disorder, bipolar II disorder and/or rapid-cycling bipolar disorder. In particular, specific nonapeptides with antagonist properties against bombesin or bombesin-like peptides, such as the gastrin releasing peptide, may be used in the treatment of inflammatory and immune-mediated inflammatory conditions as well as brain disorders.
Type:
Grant
Filed:
December 13, 2005
Date of Patent:
September 14, 2010
Assignee:
Bexar Global, Inc.
Inventors:
Gilberto Schwartsmann, Rafael Roesler, Felipe Dal Pizzol, Joao Luciano Quevedo, Flavio Kapczinski
Abstract: The invention provides methods for making peptides from a polypeptide containing at least one copy of the peptide using clostripain to excise the peptide from the polypeptide. The methods enable the use of a single, highly efficient enzymatic cleavage to produce any desired peptide sequence.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
August 24, 2010
Assignee:
NPS Pharmaceuticals, Inc.
Inventors:
Fred W. Wagner, Peng Luan, Yuannan Xia, Daniel Strydom, Jin Seog Seo
Abstract: Agonist polypeptide of a receptor protein has been identified. The agonist can be used to facilitate drug and antigen absorption. Suitable routes of administration include oral, nasal, transdermal, and intravenous. Pharmaceutical formulations may comprise a therapeutic agent or an immunogenic agent in combination with the agonist polypeptide.
Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
Type:
Grant
Filed:
August 18, 2006
Date of Patent:
August 17, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Gerald J. Tanoury, Minzhang Chen, John E. Cochran, Valdas Jurkauskas
Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
August 10, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ny Sin, Brian Lee Venables, Li-Qiang Sun, Sing-Yuen Sit, Yan Chen, Paul Michael Scola
Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Type:
Grant
Filed:
October 11, 2006
Date of Patent:
August 10, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
David J. Carini, Barry L. Johnson, Zhizhen Barbara Zheng, Stanley D'Andrea, Paul Michael Scola
Abstract: Macrocyclic peptides having the general formula: are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Type:
Grant
Filed:
November 14, 2007
Date of Patent:
July 27, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alan Xiangdong Wang, Barbara Zhizhen Zheng, Stanley D'Andrea, Nicholas A. Meanwell, Paul Michael Scola
Abstract: Disclosed herein are polypeptide multilayer films wherein a therapeutic agent is covalently linked to a first layer polypeptide. An advantage of such attachment is that the linked therapeutic agent can be controllably released from the multilayer film into the environment of the film upon the addition of a suitable stimulus. An advantage of the disclosed films and methods is enablement of environmentally-stimulated release under specific conditions.
Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.
Abstract: The present invention relates to platinum complex chemotherapeutic compounds having the generic structure: wherein n is 0 or 1 and, preferably, one of R1, R2, R3 or R8 is a -(linker)-polymer group that may contain up to four additional platinum chelates.
Type:
Grant
Filed:
June 10, 2004
Date of Patent:
July 13, 2010
Assignee:
Access Pharmaceuticals, Inc.
Inventors:
Donald R. Stewart, Paul Sood, K. Bruce Thurmond, David P. Nowotnik, Sergiy V. Shevchuk
Abstract: Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.
Type:
Grant
Filed:
January 19, 2005
Date of Patent:
July 6, 2010
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Montse Llinas-Brunet, Murray Bailey, Punit K. Bhardwaj, Francois Bilodeau, Pasquale Forgione, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Jean Rancourt
Abstract: The present invention relates to the use of erythropoietin for stimulating the physiological mobilization, proliferation and differentiation of endothelial progenitor cells, for stimulating vasculogenesis, for the therapy of diseases associated with a dysfunction of endothelial progenitor cells and for producing pharmaceutical compositions for the treatment of such diseases, and pharmaceutical compositions which comprise erythropoietin and other suitable active ingredients for stimulating endothelial progenitor cells.
Type:
Grant
Filed:
July 25, 2003
Date of Patent:
June 29, 2010
Assignee:
Epoplus GmbH & Co. KG
Inventors:
Ferdinand Hermann Bahlmann, Hermann Haller
Abstract: The use of a collection of compounds of general formula (I), wherein: n is 0 or 1; p represents an integer between 1 and 6; r represents an integer between 1 and 12; R1 and R?1 represent in particular a hydrogen atom; R2 represents an amino acid side chain or an amino acid derivative; R3 represents a group derived from a carboxylic acid, bearing a basic entity; R4 represents in particular an alkyl group containing 1 to 10 carbon atoms; and A represents a hydrogen atom, a protecting group or a tracing group, in particular a fluorophor, a coloring agent or a quencher, for determining, through binding studies, ligands of receptors whose ligand is unknown or whose ligand useful for carrying out specific affinity binding assays is unknown.
Type:
Grant
Filed:
June 15, 2005
Date of Patent:
June 29, 2010
Assignees:
Centre National de la Recherche Scientifique (CNRS), Universite Louis Pasteur
Inventors:
Marcel Francois Louis Hibert, Christel Anne Franchet, Jean-Luc Galzi, Franc Emile Jean Pattus, Fabrice Yves Guillier
Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
Type:
Grant
Filed:
September 6, 2007
Date of Patent:
June 22, 2010
Assignee:
Aeterna Zentaris GmbH
Inventors:
Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
Abstract: Macrocyclic peptides are disclosed having the general formula: wherein R?, R3, R3?, R4, R6, X, Q, and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Type:
Grant
Filed:
November 1, 2006
Date of Patent:
June 22, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Stanley D'Andrea, Zhizhen Barbara Zheng, Jeffrey Allen Campbell, Fiona McPhee, Andrew Charles Good, Paul Michael Scola
Abstract: The invention relates to a method of treatment of collagenous connective tissue removed from a donor for implant into a recipient which is re-habited or re-colonized by host cells without an immune rejection and inflammatory reaction. After removal from the donor the tissue is trimmed and thereafter soaked in a cold stabilizing solution having a temperature range of 4 to 10 degrees centigrade. The tissue is then soaked at a predetermined temperature in a polyglycol, salt, hydrogen peroxide, and phosphate buffer first solution of predetermined quantities and concentrations and of sufficient ionic strength to permit ground substances to dissociate such that the collagen fibers remain stable. The tissue is then soaked in an alcohol and water solution at a predetermined temperature for a sufficient period of time to remove the residue of the first solution.