With An Additional Active Ingredient Patents (Class 514/6.5)
  • Publication number: 20130303446
    Abstract: The invention relates to a pharmaceutical combination comprising the compound of formula I or pharmaceutically acceptable salts thereof in combination with at least one second therapeutic agent 2. The pharmaceutical combination of the invention is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
    Type: Application
    Filed: May 7, 2013
    Publication date: November 14, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Bradford S. HAMILTON, Thomas RAUCH, Manami TSUTSUMI
  • Publication number: 20130296237
    Abstract: The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 7, 2013
    Inventors: Michael B. Kastan, Clay F. Semenkovich, Jochen Schneider
  • Publication number: 20130296236
    Abstract: The present invention refers to a treatment protocol for diabetes type 2 patients.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 7, 2013
    Inventors: Louise SILVESTRE, Elisabeth SOUHAMI, Xiaodan WEI
  • Publication number: 20130295074
    Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.
    Type: Application
    Filed: July 5, 2013
    Publication date: November 7, 2013
    Inventors: Thorsten Degenhardt, Robert Schotzinger, J. Wesley Fox
  • Publication number: 20130280209
    Abstract: The invention relates to use of the natural cytotoxicity receptor NKp46 for preventing and treating diabetes, including type I diabetes (TID) and type 2 diabetes. In particular, the invention provides compositions comprising a fragment of the extracellular region of NKp46 for preventing the onset and progression of diabetes.
    Type: Application
    Filed: April 15, 2013
    Publication date: October 24, 2013
    Inventors: Ofer MANDELBOIM, Angel PORGADOR, Yaakov NAPARSTEK, Chamutal GUR
  • Publication number: 20130281365
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Application
    Filed: July 12, 2013
    Publication date: October 24, 2013
    Inventors: John COLUCCI, Marie-Claire WILSON, Yongxin HAN, Claude DUFRESNE, Michel BELLEY, Cheuk K. LAU, Christopher BAYLY
  • Publication number: 20130281366
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20130274184
    Abstract: The present invention is based on the discovery that certain small molecules can relieve ER stress, leading to increased insulin production in beta cells and improved insulin secretion. Methods of treating a disease or disorder in a subject, wherein the disease or disorder is characterized by intracellular endoplasmic reticulum (ER) stress, by administering to the subject, an effective amount of a compound that is an ER stress reliever, are provided herein.
    Type: Application
    Filed: October 10, 2012
    Publication date: October 17, 2013
    Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, NEW YORK STEM CELL FOUNDATION
    Inventors: NEW YORK STEM CELL FOUNDATION, THE TRUSTEES OF COLUMBIA UNIVERSITY IN
  • Patent number: 8557766
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: October 15, 2013
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • Patent number: 8551528
    Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: October 8, 2013
    Assignee: Mannkind Corporation
    Inventors: Marshall L. Grant, Grayson W. Stowell, Paul Menkin
  • Publication number: 20130252886
    Abstract: The present invention provides methods of treating hyperglycemia and delaying the onset of diabetes, comprising administering to a mammal in need thereof a therapeutically effective amount of a GABA receptor agonist at or near a time of an exogenous insulin administration or a meal.
    Type: Application
    Filed: October 21, 2011
    Publication date: September 26, 2013
    Inventor: Brooke Ligon
  • Publication number: 20130252885
    Abstract: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.
    Type: Application
    Filed: September 22, 2011
    Publication date: September 26, 2013
    Applicant: Advinus Therapeutics Limited
    Inventors: Barawkar Dinesh, Basu Sujay, Ramdas Vidya, Naykodi Minakshi, Patel Meena, Shejul Yogesh, Thorat Sachin, Panmand Anil
  • Publication number: 20130243852
    Abstract: A composition and method for potentiating, sensitizing, and/or amplifying at least one HDAC inhibitor targeting at least one disease in a patient is provided. In one embodiment, the composition is administered to potentiate, sensitize and/or amplify an HDAC inhibitor targeting at least one cancer.
    Type: Application
    Filed: May 9, 2013
    Publication date: September 19, 2013
    Inventor: Robert Sabin
  • Patent number: 8535715
    Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: September 17, 2013
    Assignees: Bristol-Myers Squibb Company, AstraZeneca UK Limited
    Inventors: Admassu Abebe, Kyle Martin, Jatin M. Patel, Divyakant Desai, Peter Timmins
  • Patent number: 8530413
    Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: September 10, 2013
    Assignee: Sanofi
    Inventors: Stefanie Keil, Elisabeth Defossa, Viktoria Dietrich, Siegfried Stengelin, Andreas Herling, Guido Haschke, Thomas Klabunde
  • Publication number: 20130231282
    Abstract: The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists.
    Type: Application
    Filed: May 4, 2012
    Publication date: September 5, 2013
    Inventors: Mark A. Bush, Mary Colleen O'Neill
  • Patent number: 8524669
    Abstract: The invention provides for peptides from the Mucin 1 (MUC1) cytoplasmic domain and methods of use therefor. These peptides can inhibit MUC1 oligomerization, thereby preventing tumor cell growth, inducing tumor cell apoptosis and necrosis of tumor tissue in vivo.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: September 3, 2013
    Assignees: Dana-Farber Cancer Institute, Inc., Genus Oncology, LLC
    Inventors: Donald W. Kufe, Surender Kharbanda
  • Publication number: 20130224118
    Abstract: Disclosed are methods for the treatment of chronic heart failure, comprising administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said chronic heart failure. The chronic heart failure maybe non-ischaemic or ischaemic. Also disclosed is the use of perhexiline in the manufacture of a medicament to treat chronic heart failure, including chronic heart failure of a non-ischaemic origin and chronic heart failure of an ischaemic origin.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 29, 2013
    Applicant: HEART METABOLICS LIMITED
    Inventor: Heart Metabolics Limited
  • Publication number: 20130216625
    Abstract: The present invention relates to the use of a substance with the core structure of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the manufacture of a composition for the treatment of insulin resistance or diseases associated with insulin resistance, preferably in human subject in a daily dosage in a range of from about 5 mg to about 1500 mg. The invention furthermore relates to a method of treating insulin resistance or diseases associated with insulin resistance in a mammal, said method comprises administering to said mamma, preferably a human subject, a substance with the core structure of formula (I), preferably in a daily dosage in a range from about 5 mg to about 1500 mg. The substance is preferably isosteviol or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. Examples of diseases associated with insulin resistance and e.g.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 22, 2013
    Applicant: STEVIA APS
    Inventors: Kjeld Hermansen, Per Bendix Jeppesen
  • Patent number: 8513187
    Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: August 20, 2013
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Wengen Wu
  • Publication number: 20130210721
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
  • Publication number: 20130210719
    Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of heart failure, as well as to a method for treating heart failure, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said heart failure. The invention further relates to a treatment programme for treating heart failure, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating heart failure or the symptoms thereof.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: HEART METABOLICS LIMITED
    Inventor: Heart Metabolics Limited
  • Publication number: 20130210717
    Abstract: Chitosan delivers a plasmid encoding Glucagon-Like Peptide 1 (GLP-1) to cells in a patient for gene therapy of diabetes. Chitosan is optimized for plasmid transfection by modulating three of its physico-chemical properties: degree of deacetylation (DDA), molecular weight (MW), and ratio of amines on chitosan to phosphates on DNA (N:P ratio), Chitosan 92-10-5 (DDA-MW-N:P) is more efficient than chitosans 80-10-10 and 80-80-5 in delivering a plasmid encoding luciferase or GLP-1(7-37) to cells. In the Zucker Diabetic Fatty (ZDF) rat model of diabetes, chitosan-delivered pVax plasmid encoding GLP-1 lowers glucose levels, increases insulin production and reduces weight gain.
    Type: Application
    Filed: May 10, 2011
    Publication date: August 15, 2013
    Applicant: CORPORATION DE L'ECOLE POLYTECHNIQUE DE MONTREAL
    Inventors: Abderrazzak Merzouki, Michael D. Buschmann
  • Publication number: 20130210720
    Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of heart failure, as well as to a method for treating heart failure, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said heart failure. The invention further relates to a treatment programme for treating heart failure, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating heart failure or the symptoms thereof.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: HEART METABOLICS LIMITED
    Inventor: HEART METABOLICS LIMITED
  • Publication number: 20130210718
    Abstract: The invention provides compositions and methods for determining cardiodiabetes status in a subject. The invention also provides compositions and methods for treating a subject experiencing cardiodiabetes.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 15, 2013
    Applicant: IKFE Institut fur Klinische Forschung und Entwicklung GMBH
    Inventor: IKFE Institut fur Klinische Forschung und Entwicklung GMBH
  • Publication number: 20130196898
    Abstract: The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups.
    Type: Application
    Filed: November 26, 2010
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Michael Mark, Hans-Juergen Woerle, Heike Zimdahl-Gelling
  • Publication number: 20130196906
    Abstract: Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.
    Type: Application
    Filed: January 29, 2013
    Publication date: August 1, 2013
    Applicant: CERULEAN PHARMA INC.
    Inventor: Cerulean Pharma Inc.
  • Publication number: 20130184204
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: July 13, 2012
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN
  • Patent number: 8486889
    Abstract: This invention involves compositions and method of using of therapeutic agents for pain relief for the treatment and prevention of disorders associated with endothelial dysfunction, the cause of inflammation, atherosclerosis, cardiovascular disease, diabetes, hypertension, asthma and stroke in mammals comprising anti-inflammatory agents, epinephrine, insulin, anti-viral agents and dietary supplements.
    Type: Grant
    Filed: September 1, 2012
    Date of Patent: July 16, 2013
    Assignee: Advanced Medical Instruments
    Inventor: Edward J Petrus
  • Publication number: 20130178415
    Abstract: A composition in the form of an injectable aqueous solution, the pH of which is between 6.0 and 8.0, including at least (a) a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and (b) a co-polyamino acid bearing carboxylate charges and substituted with hydrophobic radicals. In one embodiment, the compositions also include a prandial insulin and/or a gut hormone.
    Type: Application
    Filed: January 9, 2013
    Publication date: July 11, 2013
    Applicant: ADOCIA
    Inventor: ADOCIA
  • Publication number: 20130172249
    Abstract: The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor.
    Type: Application
    Filed: September 9, 2011
    Publication date: July 4, 2013
    Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITED
    Inventors: Dinesh Barawkar, Sujay Basu, Vidya Ramdas, Venkata Poornapragnacharyulu Palle, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20130171201
    Abstract: Methods of treating an arthritic joint of a subject, including administering a pharmaceutical composition by injection into the arthritic joint, wherein the composition includes an anthocyanin or anthocyanidin, glucose, and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 7, 2012
    Publication date: July 4, 2013
    Inventor: Lanny Johnson
  • Publication number: 20130172248
    Abstract: The invention relates to 3-[4-(phenylaminooxalylamino)phenyl]hex-4-ynoic acids, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3 and R4 are each defined as specified, and to physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: January 4, 2013
    Publication date: July 4, 2013
    Inventors: Elisabeth DEFOSSA, Viktoria DIETRICH, Thomas KLABUNDE, Stefanie KEIL, Siegfried STENGELIN, Guido HASCHKE, Andreas HERLING, Johanna KUHLMANN-GOTTKE, Stefan BARTOSCHEK, Simon GESSLER, Angela DUDDA, Guenter BILLEN, Thomas OLPP, Joerg RIEKE-ZAPP
  • Publication number: 20130165372
    Abstract: Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.
    Type: Application
    Filed: June 29, 2012
    Publication date: June 27, 2013
    Applicant: Rani Therapeutics, LLC
    Inventor: Mir Imran
  • Patent number: 8470773
    Abstract: The present invention relates to compounds of the general formula: wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: June 25, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Michael W. Miller, Andrew W. Stamford, William J. Greenlee
  • Publication number: 20130157940
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: February 7, 2013
    Publication date: June 20, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp
  • Publication number: 20130157941
    Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Sanofi
    Inventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
  • Publication number: 20130157929
    Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain and for treating diabetes and associated metabolic disorders. In particular, the invention provides novel glucagon analogue peptide compounds effective in such methods. The compounds may mediate their effect by having, for example, increased selectivity for the GLP-1 receptor compared to human glucagon.
    Type: Application
    Filed: June 24, 2011
    Publication date: June 20, 2013
    Applicant: ZEALAND PHARMA A/S
    Inventors: Ditte Riber, Eddi Meier
  • Publication number: 20130150292
    Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
    Type: Application
    Filed: September 14, 2012
    Publication date: June 13, 2013
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
  • Publication number: 20130143798
    Abstract: The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
    Type: Application
    Filed: March 28, 2011
    Publication date: June 6, 2013
    Applicant: NOVO NORDISK A/S
    Inventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen
  • Publication number: 20130143793
    Abstract: The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes-related diseases or disorders.
    Type: Application
    Filed: April 27, 2011
    Publication date: June 6, 2013
    Applicant: ZEALAND PHARMA A/S
    Inventors: Trine Skovlund Ryge Neerup, Torben Østerlund, Jakob Lind Tolborg, Keld Fosgerau, Ulrika Mårtensson, Marianne Brorson, Kamilla Rolsted
  • Publication number: 20130143797
    Abstract: The invention provides formulations and methods for ameliorating symptoms associated with metabolic disorders, such as cachexia, hypoglycemia, obesity, diabetes, and the like by administering Zn-?2-glycoproteins or a functional fragment thereof, alone or in combination with additional agents, such as ? adrenergin receptor agonists, ? adrenergin receptor antagonists, and/or glycemic control agents.
    Type: Application
    Filed: June 27, 2011
    Publication date: June 6, 2013
    Inventors: Michael J. Tisdale, Steven Russell
  • Patent number: 8455432
    Abstract: The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitizers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes, syndrome X, hyperglycaemia, vascular disease and kidney disease. The present invention further relates to compounds and agents and compositions thereof for use in the treatment methods.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: June 4, 2013
    Assignee: Verva Pharmaceuticals Ltd.
    Inventors: Gregory Royce Collier, Kenneth Russell Walder, James Alexander Campbell, Juan-Carlos Molero-Navajas, Nicky Konstantopoulos, Guy Yeoman Krippner
  • Patent number: 8450278
    Abstract: Provided are MUC 18 targeting peptides which may be used, e.g., to therapeutically target B-I lymphocytes to reduce the influence of these cells on the metastatic potential of melanoma cells and/or to target cancerous cells, including certain melanoma and leukemia cells. MUC 18 targeting peptides may be comprised in fusion constructs, imaging constructs, and/or therapeutic constructs such as fusion constructs which may be used for diagnosing or treating a cancer.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: May 28, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Fernanda Staquicini, Renata Pasqualini, Wadih Arap
  • Publication number: 20130130974
    Abstract: The present invention relates to process to prepare ?-aminobutyryl compounds having ?-amino acid core structural moieties and optionally having ?-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.
    Type: Application
    Filed: June 3, 2011
    Publication date: May 23, 2013
    Inventors: Damjan Sterk, Matjaz Ustar, Marko Zlicar
  • Publication number: 20130125886
    Abstract: A method for preventing or reducing adverse effects such as profuse sweating, nausea and vomiting, which normally are associated with subcutaneous and intravenous administration of glucagon-like peptide 1 (GLP-1) therapy is provided. In particular, the method comprises the rapid administration of a GLP-1 formulation into the pulmonary circulation such as by inhalation, directly into pulmonary alveolar capillaries using a dry powder drug delivery system.
    Type: Application
    Filed: January 2, 2013
    Publication date: May 23, 2013
    Inventors: Peter Richardson, Robert A. Baughman, Donald Costello
  • Publication number: 20130123172
    Abstract: The present disclosure provides therapeutic methods for prevention and treatment of type-2 diabetes comprising administering to the subject an effective amount of FTY720 or an analog.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 16, 2013
    Applicant: DIAPIN THERAPEUTICS LLC
    Inventor: DIAPIN THERAPEUTICS LLC
  • Patent number: 8436136
    Abstract: A complex comprising at least one heat shock protein (HSP) and at least one peptide selected from the group consisting of R1-QXRAA-R2 with R1=peptide with 1-10 amino acids R2=peptide with 1-10 amino acids X=K or R GFFYTPK (insulin 23-29) SEQ ID No 1 GFFYTPKT (insulin 23-30) SEQ ID No 2 IYPPNANK (DER p1) SEQ ID No 3 GIEYIQHNGVVQESYYR (DER P1) SEQ ID No 4 ASTTTNYT (gp120 of HIV) SEQ ID No 5 DYEYLINVIHAFQYV (PLP 56-70) SEQ ID No 6 EKLIETYFSKNYQDYEYLINVI (PLP 43-64) SEQ ID No 7 KTTICGKGLSATVT (PLP 104-117) SEQ ID No 8 HSLGKWLGHPDKF (PLP 139-151 C140 ô S140) SEQ ID No 9 PRHPIRVELPCRISP (MOG 8-22) SEQ ID No 10 DEGGYTCFFRDHSYQ (MOG 92-106) SEQ ID No 11 Ac-ASQKRPSQRHG (MBP ac1-11) SEQ ID No 12 TGILDSIGRFFSG (MBP 35-47) SEQ ID No 13 VHFFKNIVTPRTP (MBP 89-101) SEQ ID No 14 HCLGKWLGHPDKF (PLP 139-151) SEQ ID No 15 MEVGWYRSPFSRVVHLYRNGK (MOG) SEQ ID No 16 QKRAAYDQYGHAAFE (E. Coli DnaJ) SEQ ID No. 17 QKRAAVDTYCRHNYG (HLA DRB1*0401) SEQ ID No. 18 QRRAAYDQYGHAAFE SEQ ID No. 19 and QRRAAVDTYCRHNYG SEQ ID No. 20.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: May 7, 2013
    Assignee: Biotech Tools S.A.
    Inventors: Frederic Henot, Thierry Legon, Isabelle Galy-Fauroux, Jean Duchateau
  • Publication number: 20130109620
    Abstract: Methods for reducing bone loss in a subject suffering from a condition benefiting from a decrease in insulin resistance, by balaglitazone administration to the subject.
    Type: Application
    Filed: December 17, 2010
    Publication date: May 2, 2013
    Applicants: RHEOSCIENCE A/S, REDDY'S LABORATORIES, LIMITED
    Inventors: Bente Riis, Kim Henriksen, Rajinder Kumar
  • Patent number: 8415297
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber