Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.07)
  • Patent number: 10442782
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: October 15, 2019
    Assignee: CHDI Foundation, Inc.
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Patent number: 10005736
    Abstract: The present invention relates to compounds of formula I wherein R1? is CH3 R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl or cyclopropyl; R3 is Cl, F, CF3, cyano, methyl, methoxy or cyclopropyl; R4 is hydrogen, methyl or F; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: June 26, 2018
    Assignee: Hoffman-La Roche Inc.
    Inventors: Marius Hoener, Juergen Wichmann
  • Patent number: 9663473
    Abstract: The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R1, R2, R3, R4, R6, R7, R8 and R9 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: May 30, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Olivier Corminboeuf, Sylvaine Cren, Xavier Leroy, Davide Pozzi
  • Patent number: 9611224
    Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3 and R4 are described in this application, and methods of using said compounds in the treatment of cancer.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: April 4, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Xiaochun Han, Yan Lou, Christophe Michoud, Steven Gregory Mischke, Stacy Remiszewski, Kenneth Carey Rupert
  • Patent number: 9593120
    Abstract: The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: March 14, 2017
    Assignee: ALGENIS SPA
    Inventors: Max Rutman, Jean-Jacques Pilorget, Jimmy Stehberg, Wolfgang Vanscheidt, Constanza Sigala
  • Patent number: 9579302
    Abstract: Described herein is the surprising discovery that ketone bodies protect cell and tissues from ionizing radiation. Based on this finding, methods of protecting animal tissue and cells from damage caused by radiation exposure are disclosed which include, contacting the tissue with a therapeutically effective amount of an agent including at least one ketone ester, thereby protecting the tissue from radiation damage. Ketone esters can be used to minimize, reduce and/or prevent tissue damage following intentional and accidental radiation exposure, as well as increasing the therapeutic efficacy of radiation therapies by protecting non-target tissue from incidental radiation damage.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: February 28, 2017
    Assignees: TDELTAS, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Richard L. Veech, Kieran Clarke
  • Patent number: 9309200
    Abstract: The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: April 12, 2016
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Wilhelm Amberg, Udo Lange, Michael Ochse, Frauke Pohlki, Berthold Behl, Mario Mezler, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 9139531
    Abstract: Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: September 22, 2015
    Assignee: URQUIMA, S.A.
    Inventors: Rafel Prohens Lopez, Cristina Puigjaner Vallet, Rafael Barbas Canero, Jose Luis Del Rio Pericacho, Josep Marti Via
  • Patent number: 9120755
    Abstract: Stable crystalline Form II and stable crystalline Form III of ivabradine hydrochloride and processes for their preparation are disclosed.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: September 1, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Mukul Hariprasad Sharma, Piyush Rajendra Sharma, Jaiprakash Ajitsingh Parihar
  • Patent number: 9090624
    Abstract: The present invention relates to novel aromatic bicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the CXCR4 receptor.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: July 28, 2015
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Thong Vu, John E. Donello, Gerard Rodrigues, Veena Viswanath, Michael E. Garst
  • Patent number: 9045431
    Abstract: Processes and intermediates for preparing salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and pharmaceutically acceptable solvates and hydrates thereof, that are useful for, inter alia, weight management.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: June 2, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Anna Shifrina
  • Publication number: 20150148335
    Abstract: The invention relates to a liquid formulation comprising propylene glycol and an effective amount of an inodilator, an angiotensin converting enzyme inhibitor, or a combination of an inodilator and an angiotensin converting enzyme inhibitor and to use of the formulation for treating cardiac disease and/or hypertension.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 28, 2015
    Inventors: Nicholas Bova, Stephen Page, Giuseppe Pippia
  • Publication number: 20150147393
    Abstract: The present invention concerns palatable veterinary compositions made from one or more pharmaceutical active ingredients having a smell and/or a taste that is repulsive to animals, and a preparation method for preparing said oral veterinary compositions.
    Type: Application
    Filed: June 1, 2013
    Publication date: May 28, 2015
    Applicant: Ceva Sante Animale
    Inventors: Laurence Peyrot, Florence Guimberteau
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Publication number: 20150110871
    Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.
    Type: Application
    Filed: January 3, 2015
    Publication date: April 23, 2015
    Inventor: David Wong
  • Publication number: 20150079170
    Abstract: The present invention relates to novel tablet dosage forms and methods of preparing these forms, which can be used for different classes of pharmaceutical active ingredients posing stability issues in a single unit system. The dosage form includes a first layer, which includes a tablet of one or more active pharmaceutical ingredients, which is inlayed in the first layer along with other pharmaceutically acceptable excipients, and a second layer that includes one or more active pharmaceutical ingredients optionally with other pharmaceutically acceptable excipients.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 19, 2015
    Inventors: Girish Kumar JAIN, Ramakant GUNDU, Rahul DABRE
  • Publication number: 20150064249
    Abstract: The invention is directed to a pharmaceutical tablet formulation for the veterinary medical sector containing an instable ACE inhibitor or a pharmaceutically acceptable salt thereof as a first pharmaceutically active substance, and pimobendan or a pharmaceutically acceptable salt thereof as a second pharmaceutically active substance, comprising granules which contain carrier core particles coated with at least one layer wherein the first pharmaceutically active substance is present, the granules being embedded in a tablet matrix wherein the second pharmaceutically active substance is present. It is provided a “fixed-dose-combination” which allows to ease the treatment and administration of the medication, improves the medication compliance by reducing the pill burden to the animal holder and enables the better observation of and adherence to the therapy by decreasing the number of tablets to be administered.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 5, 2015
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin Folger, Ragna Hoffmann, Florent Robin
  • Publication number: 20150038491
    Abstract: The present invention relates to a solid composition containing ivabradine or a pharmaceutically acceptable salt thereof. Further, the invention relates to a method for the preparation of such a composition as well as a pharmaceutical product comprising such a composition.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 5, 2015
    Applicant: ratiopharm GmbH
    Inventors: Dominique MEERGANS, Daniela STUMM, Jens GEIER
  • Publication number: 20150025062
    Abstract: The present invention is directed to a method of enhancing visual function in a subject, comprising administering to the subject in need of such enhancement, a therapeutically effective amount of an inhibitor of a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the HCN channel inhibitor.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Publication number: 20150005260
    Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.
    Type: Application
    Filed: January 2, 2013
    Publication date: January 1, 2015
    Inventors: Faiez Zannad, Patrick Rossignol
  • Publication number: 20140364417
    Abstract: The present disclosure relates to a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising coadministration of a therapeutically effective amount of ivabradine or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of ranolazine. Also provided are methods for modulating ventricular and atrial rate. This disclosure also relates to pharmaceutical formulations that are suitable for such combined administration.
    Type: Application
    Filed: May 2, 2014
    Publication date: December 11, 2014
    Inventors: Luiz Belardinelli, Richard Verrier, Dewan Zeng
  • Publication number: 20140363505
    Abstract: The invention relates to a new fixed dose combination of benazepril with pimobendan.
    Type: Application
    Filed: December 19, 2012
    Publication date: December 11, 2014
    Inventors: Jernej Grmas, Zdenka Jerala-Strukelj, Sebastjan Reven
  • Publication number: 20140364416
    Abstract: One embodiment described herein is related to methods and compositions, such as nutraceutical formulations and dietary supplements, comprising C16:1n7-palmitoleate or derivatives thereof. The methods and compositions comprising C16:1n7-palmitoleate, or derivatives thereof, safely and effectively prevent or mitigate manifestations of cardiovascular disease, including coronary artery disease and the accumulation of cholesterol or lipid deposits in the blood vessels of a subject.
    Type: Application
    Filed: April 1, 2014
    Publication date: December 11, 2014
    Applicant: Tersus Pharmaceuticals, LLC
    Inventor: Jeffrey Green
  • Patent number: 8900605
    Abstract: The present invention relates to a solid composition containing ivabradine or a pharmaceutically acceptable salt thereof. Further, the invention relates to a method for the preparation of such a composition as well as a pharmaceutical product comprising such a composition.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: December 2, 2014
    Assignee: ratiopharm GmbH
    Inventors: Dominique Meergans, Daniela Stumm, Jens Geier
  • Publication number: 20140349998
    Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20140336179
    Abstract: The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride.
    Type: Application
    Filed: July 31, 2012
    Publication date: November 13, 2014
    Applicant: SANDOZ AG
    Inventors: Josef Wieser, Ulrich Griesser, Michael Enders, Volker Kahlenberg
  • Publication number: 20140323471
    Abstract: Stable crystalline Form II and stable crystalline Form III of ivabradine hydrochloride and processes for their preparation are disclosed.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 30, 2014
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Mukul Hariprasad Sharma, Piyush Rajendra Sharma, Jaiprakash Ajitsingh Parihar
  • Publication number: 20140315890
    Abstract: Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 23, 2014
    Inventors: Rafel Prohens Lopez, Cristina Puigjaner Vallet, Rafael Barbas Canero, Jose Luis Del Rio Pericacho, Josep Marti Via
  • Publication number: 20140302125
    Abstract: There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin II receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.
    Type: Application
    Filed: August 23, 2012
    Publication date: October 9, 2014
    Applicant: Wockhardt Ltd.
    Inventors: Mandar Madhukar Kodgule, Premchand Dalichandji Nakhat, Amit Gupta, Girish Kumar Jain
  • Publication number: 20140275034
    Abstract: A method for repelling blood-sucking and biting insects, ticks and mites involving treating an object or area with a blood-sucking and biting insects, ticks and mites repelling effective amount of camphor lactams, verbenone lactams, dolicholactams, dolicholactone, and their precursors, and mixtures thereof, and optionally a carrier.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Inventors: Kamlesh R. Chauhan, Bheema R. Paraselli
  • Publication number: 20140227351
    Abstract: Taste masked multi-layered particles include an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and including a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture including 60-90% (w/w) EC and 10-40% (w/w) HPMC, where the pharmaceutically active ingredient is water-soluble and includes either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions including such particles.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Martin FOLGER, Stefan LEHNER, Annette GRAVE, Norbet POELLINGER, Randolph SEIDLER
  • Publication number: 20140221352
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8796259
    Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: August 5, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
  • Publication number: 20140206618
    Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 24, 2014
    Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
  • Publication number: 20140206606
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Patent number: 8772278
    Abstract: The present invention relates to a method of prophylaxis or treatment of systemic diseases in cats, wherein the method comprising administration of a therapeutically effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to a cat in need of such a treatment.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Marcus Stark, Ulrike Sent, Ingo Lang
  • Publication number: 20140179683
    Abstract: Disclosed is a sustained-release preparation of ivabradine or pharmaceutically acceptable salts thereof. The preparation contains ivabradine or pharmaceutically acceptable salts thereof and a sustained-release framework material, wherein the sustained-release framework material is selected from polyoxyethylene, or a mixture of polyoxyethylene and polyvinyl acetate or polyvinyl pyrrolidone.
    Type: Application
    Filed: June 18, 2012
    Publication date: June 26, 2014
    Applicant: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Kai Liu, Yuxia Wu
  • Publication number: 20140171415
    Abstract: The present invention relates to an If blocker or a pharmaceutically acceptable salt thereof for the treatment and/or prevention of a canine patient suffering from heart diseases, preferably heart diseases such as dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia. Each of these diseases may or may not result in heart failure (HF) in canine patients. The invention also relates to improving the quality of life, improving the general health condition as well as a prolonging the life expectancy in canine patients suffering from heart diseases and/or heart failure due to one or more of the following etiologies dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia.
    Type: Application
    Filed: December 11, 2013
    Publication date: June 19, 2014
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Saskia KLEY, Ingo LANG, Joerg Christian MEIL, Randolph SEIDLER, Michael MARKERT
  • Publication number: 20140155382
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: November 22, 2013
    Publication date: June 5, 2014
    Applicant: ABBVIE INC.
    Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
  • Patent number: 8741890
    Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
  • Patent number: 8741889
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
  • Patent number: 8729066
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: May 20, 2014
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Publication number: 20140107057
    Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140100217
    Abstract: The present invention provides a compound comprising a general formula 1: In general formula 1, X is at least one of O and S. A is a ring bridge. Y1 is at least one of H, alkyl, fluoroalkyl, aryl and heteroaryl. Z1, Z2, Z3 are, individually or alternatively, at least one of H, carbonyl, OH, O-alkyl, O-acyl, N—R1R2 (where R1 or R2 are, individually or alternatively, at least one of H, alkyl, acyl, and sulfonyl), alkyl, acyl, fluoroalkyl, aryl, and heteroaryl. R1 is at least one of alkyl, acyl, alkoxycarbonyl, aryloxycarbonyl, and aminocarbonyl. R2 is at least one of H, alkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, aryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminoacyl and peptidyl. The present invention furthermore relates to the use of the compound as a pharmaceutical active compound, and to the use of the pharmaceutical active compound to treat bacterial diseases, neurodegenerative diseases and tumors.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 10, 2014
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAET ZU KOELN
    Inventors: HANS-GUENTHER SCHMALZ, CÉDRIC MICHAEL REUTER, RONALD KUEHNE, HARTMUT OSCHKINAT, MATTHIAS MUELLER, ROBERT OPITZ
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140073574
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
  • Publication number: 20140057873
    Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.
    Type: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Inventor: Michael Farber
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath