With An Additional Active Ingredient Patents (Class 514/6.5)
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Patent number: 8410049Abstract: Improved methods and kits for treating the long-term complication of diabetes that reduce the risk of the patient developing hypoglycemia during C-peptide therapy. The use of such methods and kits, can also maintain good glycemic control, and avoid excessive weight gain that may otherwise be associated with excessive insulin administration or caloric intake during C-peptide therapy.Type: GrantFiled: March 4, 2010Date of Patent: April 2, 2013Assignee: CebixInventors: John Wahren, Karin Ekberg, James Callaway
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Publication number: 20130079278Abstract: The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present 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: ApplicationFiled: September 21, 2012Publication date: March 28, 2013Applicant: NOVO NORDISK A/SInventor: Novo Nordisk A/S
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Publication number: 20130079279Abstract: Subject of the present invention is A pharmaceutical composition comprising (a) desPro36Exendin-4(1-39)-Lys6-NH2 or/and a pharmaceutically acceptable salt thereof, and (b) insulin glargine or/and a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 27, 2011Publication date: March 28, 2013Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Reinhard Becker, Gerrit Hauck
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Publication number: 20130065826Abstract: A composition in the form of an injectable aqueous solution, the pH of which is between 6.0 and 8.0, includes at least a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and a dextran substituted by radicals carrying carboxylate charges and hydrophobic radicals. Single-dose formulations at a pH of between 7 and 7.8 includes a basal insulin whose isoelectric point is between 5.8 and 8.5 and a prandial insulin.Type: ApplicationFiled: August 9, 2012Publication date: March 14, 2013Applicant: ADOCIAInventors: Olivier SOULA, Gérard SOULA, Jeff TONNAR
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Publication number: 20130058969Abstract: Vaccines for conferring immunity in mammals to infective pathogens are provided, as well as vectors and methods for plastid transformation of plants to produce protective antigens and vaccines for oral delivery. The vaccines are operative by parenteral administration as well. The invention also extends to the transformed plants, plant parts, and seeds and progeny thereof. The invention is applicable to monocot and dicot plants.Type: ApplicationFiled: July 26, 2012Publication date: March 7, 2013Inventor: Henry Daniell
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Publication number: 20130059777Abstract: Compositions and methods are provided for decreasing blood glucose levels in an animal, comprising administering to said animal an antisense inhibitor of glucose-6-phosphatase translocase expression alone or in combination with at least one glucose-lowering drug. Also provided are compositions and methods for treating diabetes and other metabolic disorders.Type: ApplicationFiled: July 30, 2012Publication date: March 7, 2013Applicant: Isis Pharmaceuticals, Inc.Inventors: Sanjay Bhanot, Kenneth W. Dobie
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Publication number: 20130053309Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.Type: ApplicationFiled: October 11, 2012Publication date: February 28, 2013Inventor: Kelly Sullivan Kraft
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Publication number: 20130053308Abstract: New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine Aza receptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine Aza receptor.Type: ApplicationFiled: March 29, 2011Publication date: February 28, 2013Inventors: Juan Alberto Camacho Gomez, Julio Cesar Castro-Palomino Laria
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Publication number: 20130035285Abstract: The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, 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: ApplicationFiled: March 28, 2011Publication date: February 7, 2013Applicant: Novo Nordisk A/SInventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen, Jacob Kofoed, Kirsten Dahl
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Publication number: 20130022610Abstract: Methods for treating abnormal glycosylated hemoglobin (HbA1c) levels in a patient in need thereof, wherein the provided methods comprise administering to a patient in need a therapeutically effective amount of an Interleukin-1? modulator. Also, the invention provides compositions comprising at least one lipid modifying agent and an IL-1? modulator.Type: ApplicationFiled: July 19, 2012Publication date: January 24, 2013Inventors: Mannching Sherry Ku, Chih-Kuang Chen, Wei-Shu Lu, Chih-Ming Chen, I-Yin Lin
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Publication number: 20130017993Abstract: This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Gregory Raymond BEBERNITZ, Mark G. BOCK, Dumbala Srinivas REDDY, Atul Kashinath HAJARE, Vinod VYAVAHARE, Sandeep Bhausaheb BHOSALE, Suresh Eknath KURHADE, Videsh SALUNKHE, Nadim S. SHAIKH, Debnath BHUNIYA, P. Venkata PALLE, Lili FENG, Jessica LIANG
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Publication number: 20130012434Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
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Publication number: 20130011379Abstract: 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: ApplicationFiled: April 13, 2012Publication date: January 10, 2013Applicant: NEPHROGENEX, INC.Inventors: Thorsten Degenhardt, Robert Schotzinger, Wesley J. Fox
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Publication number: 20130011361Abstract: The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: October 1, 2010Publication date: January 10, 2013Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20130005649Abstract: The present invention refers to a pharmaceutical combination for use in glycemic control in diabetes type 2 patients.Type: ApplicationFiled: May 9, 2012Publication date: January 3, 2013Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Elisabeth NIEMÖELLER, Louise SILVESTRE, Gabor BOKA, Patrick MIOSSEC
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Publication number: 20130005650Abstract: Methods and compositions are provided comprising acriflavine for inhibiting and treating diseases and disorders associated with pathogenic proteins causing neurodegenerative diseases and amyloid diseases, such as protease resistant prion proteins (PrPSc) and those associated with transmissible spongiform encephalopathies (TSEs), Alzheimer's disease, amyloidosis, and the like.Type: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Inventor: Peter K. Chiang
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Publication number: 20120322727Abstract: In one embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In yet another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. The pharmaceutical compositions of the invention may be used to treat or prevent a neurodegenerative disorder such as Alzheimer's disease, stroke, Parkinson's disease, multiple sclerosis, spinal cord injuries, and/or traumatic brain injuries and the like, in addition to other systemic and local diseases.Type: ApplicationFiled: June 15, 2012Publication date: December 20, 2012Inventors: Yaser A. Abdel Maksoud, Mustafa A. Maher
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Publication number: 20120294936Abstract: The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.Type: ApplicationFiled: November 12, 2010Publication date: November 22, 2012Applicants: ASTRAZENECA UK LIMITED, BRISTOL-MYERS SQUIBB COMPANYInventors: Admassu Abebe, Kyle Martin, Jatin M. Patel, Peter Timmins
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Publication number: 20120296403Abstract: The disclosure relates to treating muscle wasting-associated disorders in a patient, using a therapeutically effective amount of an antagonist of Fbxo40, wherein the antagonist reduces the expression, level or activity of Fbxo40. The Fbxo40 antagonist increases muscle mass, or prevents, limits or reduces muscle mass loss, in the patient. The Fbxo40 antagonist can be a low molecular weight (LMW) compound, a protein, an antibody, or an inhibitory nucleic acid, such as a siRNA. The disclosure also relates to methods of screening for antagonists of Fbxo40, and methods of diagnosing or monitoring levels of muscle mass maintenance, loss or increase.Type: ApplicationFiled: February 8, 2011Publication date: November 22, 2012Applicant: NOVARTIS AGInventors: David Glass, Jun Shi
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Publication number: 20120295846Abstract: A liquid composition comprising a GLP-1 agonist or/and a pharmacologically tolerable salt thereof, an insulin or/and a pharmacologically tolerable salt thereof, and, optionally, at least one pharmaceutically acceptable excipient, wherein the composition comprises methionine, as add-on therapy with metformin where appropriate.Type: ApplicationFiled: November 11, 2010Publication date: November 22, 2012Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Annika Hagendorf, Gerrit Hauck, Werner Mueller, Isabell Schoettle, Verena Siefke-Henzler, Katrin Tertsch
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Publication number: 20120283179Abstract: A liquid composition comprising a GLP-1 agonist or/and a pharmacologically tolerable salt thereof and, optionally, at least one pharmaceutically acceptable excipient, wherein the composition comprises methionine, as add-on therapy with metformin and/or with long-acting insulin/insulin derivates where appropriate.Type: ApplicationFiled: November 11, 2010Publication date: November 8, 2012Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Anette Brunner-Schwarz, Werner Mueller, Verena Siefke-Henzler
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Publication number: 20120283169Abstract: The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor and an insulin which 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.Type: ApplicationFiled: November 2, 2011Publication date: November 8, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Rolf GREMPLER, Odd-Eric JOHANSEN, Thomas KLEIN, Gerd LUIPPOLD, Michael MARK
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Publication number: 20120282227Abstract: Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time.Type: ApplicationFiled: June 9, 2010Publication date: November 8, 2012Inventor: Laurence M. Katz
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Publication number: 20120282184Abstract: A method for the prevention or treatment of a condition selected from type 2 diabetes, obesity and metabolic syndrome comprising activating a GITRL pathway. Methods for screening for substances to treat these conditions, diagnosing or predicting these conditions and selecting and monitoring therapies.Type: ApplicationFiled: October 29, 2010Publication date: November 8, 2012Applicant: ISIS INNOVATION LTDInventors: Herman Waldmann, Kathleen Nolan, Lynn Poulton
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Publication number: 20120283181Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.Type: ApplicationFiled: July 11, 2012Publication date: November 8, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
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Publication number: 20120282336Abstract: 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: ApplicationFiled: November 12, 2010Publication date: November 8, 2012Applicants: ASTRAZENECA UK LIMITED, BRISTOL-MYERS SQUIBB COMPANYInventors: Admassu Abebe, Kyle Martin, Jatin M. Patel, Divyakant Desai, Peter Timmins
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Publication number: 20120277150Abstract: [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: ApplicationFiled: April 11, 2012Publication date: November 1, 2012Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Munetaka OHKOUCHI
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Publication number: 20120277149Abstract: The invention relates to a pharmaceutical composition comprising 1.a and/or 1.b according to claim 1 in combination with at least one second therapeutic agent 2 which 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: ApplicationFiled: October 31, 2011Publication date: November 1, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bradford S. Hamilton, Thomas Rauch, Manami Tsutsumi
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Publication number: 20120270778Abstract: The present invention provides C-peptide compositions that permit the noninvasive or non-injectable administration of C-peptide via nasal or pulmonary routes, as well as methods for treating disease.Type: ApplicationFiled: December 16, 2010Publication date: October 25, 2012Inventor: Edward T. Maggio
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Publication number: 20120269882Abstract: Methods and composition for the treatment of systemic inflammation, such as bacterial or viral sepsis, are described. Methods of treating systemic inflammation comprise delivery of insulin to the brain, for example by intracranial or intranasal administration. Insulin delivery systems and brain-targeted insulin compositions and polypeptides are also provided.Type: ApplicationFiled: May 19, 2010Publication date: October 25, 2012Applicant: MOUNT SINAI SCHOOL OF MEDICINE Office of Technology & Business DevelopmentInventor: Christoph Buettner
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Publication number: 20120258913Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.Type: ApplicationFiled: June 12, 2012Publication date: October 11, 2012Inventors: Sumihiro NOMURA, Eiji KAWANISHI, Kiichiro UETA
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Publication number: 20120252725Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as amino-transferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.Type: ApplicationFiled: November 26, 2010Publication date: October 4, 2012Inventors: Raphaël Darteil, Rémy Hanf, Dean Hum
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Publication number: 20120252724Abstract: The invention relates to an aqueous pharmaceutical formulation having insulin, an insulin analog, or an insulin derivative, and methionine; and to the production thereof, to the use thereof for treating diabetes mellitus, and to a medication for treating diabetes mellitus.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Applicant: SANOFI-AVENTISInventors: Isabell Schoettle, Annika Hagendorf, Christiane Fuerst, Gerrit Hauck, Verena Siefke-Henzler, Walter Kamm, Julia Schnieders
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Publication number: 20120241356Abstract: The invention relates to a method for producing an aqueous, pharmaceutical formulation comprising an insulin, an insulin analog, or an insulin derivative, wherein the ready-made formulation takes place directly by dissolving the insulin, the insulin analog, or the insulin derivative as a solid in a suitable solvent mixture.Type: ApplicationFiled: July 2, 2010Publication date: September 27, 2012Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Anja Pfenninger, Norbert Tennagels, Christiane Fuerst
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Publication number: 20120245085Abstract: If albumin is added to a pharmaceutical formulation containing acylated insulin described in WO 2009/022005 and WO 2009/022013, the acylated insulin can be kept in solution after subcutaneous injection.Type: ApplicationFiled: November 1, 2010Publication date: September 27, 2012Applicant: Novo Nordisk A/SInventors: Helle Naver, Svend Havelund, Peter Madsen
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Publication number: 20120225812Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides process of preparation of compounds of formula (I).Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Applicant: Advinus Therapeutics LimitedInventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Ventaka Poornapragnacharyulu Palle
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Publication number: 20120214736Abstract: The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK1 protein.Type: ApplicationFiled: December 9, 2011Publication date: August 23, 2012Applicant: Isis Pharmaceuticals, Inc.Inventors: Xing-Xian Yu, Sanjay Bhanot
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Publication number: 20120196801Abstract: The main active ingredients of the formula are papaverin, bendazol, and insulin. The drug may be produced in soft, liquid medicinal form or as an aerosol.Type: ApplicationFiled: February 1, 2011Publication date: August 2, 2012Inventors: Artur Martynov, Boris S. Farber, Sonya Sophya Farber
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Publication number: 20120195959Abstract: The present invention provides a use of an insulin for manufacture of a medicament for treating or preventing a disorder or disease of a central nervous system of an adult individual, wherein the disorder or disease is associated with tissue shrinkage or atrophy. Also provided are methods of treating such disorder or disease using a pharmaceutically effective amount of an insulin or composition that enhances the activity of endogenous insulin.Type: ApplicationFiled: November 30, 2011Publication date: August 2, 2012Inventor: Douglas N. Ishii
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Publication number: 20120183616Abstract: The present invention relates to a pharmaceutical composition comprising an insulin compound in a concentration that is sufficient to maintain a therapeutically effective level of the insulin compound in blood plasma for at least 3 days characterized by having a pharmacokinetic profile in vivo with substantially no burst of the insulin compound. The present invention further relates to the use of an insulin compound for preparing said pharmaceutical composition as well as a kit of parts comprising said pharmaceutical composition.Type: ApplicationFiled: July 30, 2010Publication date: July 19, 2012Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Kennett Sprogoe, Felix Cleemann, Ulrich Hersel, Silvia Kaden-Vagt, Torben Lessmann, Harald Rau, Thomas Wegge
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Publication number: 20120184489Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.Type: ApplicationFiled: July 30, 2010Publication date: July 19, 2012Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Harald Rau, Felix Cleeman, Ulrich Hersel, Silvia Kaden-Vagt, Torben Lessman
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Publication number: 20120178681Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
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Publication number: 20120178680Abstract: This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: NOVARTIS AGInventors: Gregory Raymond BEBERNITZ, Mark G. BOCK, Dumbala Srinivas REDDY, Atul Kashinath HAJARE, Vinod VYAVAHARE, Sandeep Bhausaheb BHOSALE, Suresh Eknath KURHADE, Videsh SALUNKHE, Nadim S. SHAIKH, Debnath BHUNIYA, P. Venkata PALLE, Lili FENG, Jessica LIANG
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Publication number: 20120178676Abstract: The present invention relates to modified forms of C-peptide, and methods for their use. In one aspect, the modified forms of C-peptide comprise PEGylated C-peptide derivatives comprising at least one PEG group attached to the N-terminus, which exhibit superior pharmacokinetic and biological activity in vivo.Type: ApplicationFiled: May 17, 2011Publication date: July 12, 2012Applicant: CEBIX, INC.Inventors: Sheri Barrack, James Callaway, Michelle Mazzoni
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Publication number: 20120178678Abstract: The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: either —(C?O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, or —(C?O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.Type: ApplicationFiled: August 5, 2010Publication date: July 12, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Elisabeth Dupont-Passelaigue, Samuel Mialhe, Jean-Pierre Rieu, Didier Junquero, Karine Valeille
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Publication number: 20120178670Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes and associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.Type: ApplicationFiled: June 24, 2010Publication date: July 12, 2012Applicant: Zealand Pharma A/SInventors: Ditte Riber, Eddi Meier, Jens Rosengren Daugaard, Marie Skovgaard, Jakob Lind Tolborg, Gita Kampen, Camilla Ærteberg Bæk
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Publication number: 20120178679Abstract: 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: ApplicationFiled: March 13, 2012Publication date: July 12, 2012Applicant: KANEQ PHARMA INC.Inventors: John COLUCCI, Marie-Claire WILSON, Yongxin HAN, Claude DUFRESNE, Michel BELLEY, Cheuk K. LAU, Christopher BAYLY
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Publication number: 20120178677Abstract: 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: ApplicationFiled: March 1, 2010Publication date: July 12, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai, Wengen Wu
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Publication number: 20120164120Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.Type: ApplicationFiled: December 23, 2011Publication date: June 28, 2012Applicant: FOOD INDUSTRY RESEARCH AND DEVELOPMENT INSTITUTEInventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
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Publication number: 20120165251Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a DPP-4 inhibitor and a long-acting insulin. The invention further relates to a DPP-4 inhibitor for subcutaneous or transdermal use.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Michael MARK, Leo THOMAS