Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Publication number: 20140045872Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
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Publication number: 20140045778Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: ApplicationFiled: January 3, 2013Publication date: February 13, 2014Applicants: THE KITASATO INSTITUTE, MEIJI SEIKA PHARMA CO., LTD.Inventors: MEIJI SEIKA PHARMA CO., LTD., THE KITASATO INSTITUTE
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Publication number: 20140045829Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
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Patent number: 8648081Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: GrantFiled: May 8, 2012Date of Patent: February 11, 2014Assignee: Eli Lilly and CompanyInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Publication number: 20140038924Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: October 3, 2013Publication date: February 6, 2014Applicant: IPCA LABORATORIES LIMITEDInventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki MOJE
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Publication number: 20140031320Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: October 3, 2013Publication date: January 30, 2014Applicant: IPCA LABORATORIES LIMITEDInventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki MOJE
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Publication number: 20140031386Abstract: The present invention relates to a use of haloid acid salt and sulfonate of a compound of formula I and a salt of the compound of formula I in preparation of medicament for preventing or treating diseases caused by thrombosis or embolism. The present invention provides acid addition salts, especially haloid acid and sulfonic acid addition salts of a compound of formula I having high inhibition effect on platelet aggregation, and preparation method of the same, a medicament comprising the same, and a use and/or method for preventing or treating diseases caused by thrombosis or embolism.Type: ApplicationFiled: April 9, 2012Publication date: January 30, 2014Applicant: GUANGZHOU HEERSHI PHARMA DEVELOPMENT CO., LTDInventor: Xiaojing Yan
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Publication number: 20140031385Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: April 17, 2013Publication date: January 30, 2014Applicant: Medicis Phamaceutical CorporationInventors: Stephen D. Barrett, James B. Kramer, Mark L. Boys, Huifen Chen
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Publication number: 20140024659Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.Type: ApplicationFiled: April 5, 2012Publication date: January 23, 2014Applicant: BASF SEInventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
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Patent number: 8633317Abstract: Salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: GrantFiled: June 8, 2011Date of Patent: January 21, 2014Assignee: AbbVie Inc.Inventors: Geoff G. Z. Zhang, Paul J. Brackemeyer, Ahmad Y. Sheikh
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Patent number: 8633217Abstract: Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: GrantFiled: June 8, 2011Date of Patent: January 21, 2014Assignee: AbbVie Inc.Inventors: Geoff G. Z. Zhang, Douglas H. Hoffman, Jonathan Miller
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Publication number: 20140018331Abstract: The present invention relates to a method of ameliorating the drawbacks of anti-platelet drug named clopidogrel. The method of the present invention comprises administration of an (S)oxo-clopidogrel or its derivative of the Formula IIA in its free or pharmaceutically acceptable salt form for alleviating the symptoms of thrombosis or embolism by inhibiting blood platelet aggregation. Compositions for use in such methods are also provided.Type: ApplicationFiled: August 7, 2013Publication date: January 16, 2014Applicant: IPCA Laboratories LimitedInventors: Ashok KUMAR, Nellithanath Thankachen Byju
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Publication number: 20140018373Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: ApplicationFiled: December 22, 2011Publication date: January 16, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Publication number: 20130344116Abstract: The present invention relates to compositions and methods of the preparation of an oral particle essentially consisting of an amorphous structure and a submicron domain, wherein both amorphous structure and submicron domain comprise a drug, and wherein the particle shows crystalline property. The desired ratio of the amorphous structure to the submicron domain is between 0.1:5 and 1:1. And, the desired average particle diameter is between mesh 12 (1680 microns) and mesh 100 (149 microns).Type: ApplicationFiled: October 29, 2012Publication date: December 26, 2013Applicant: Magnifica Inc.Inventors: David Wong, James A. Lee, Peter P. Yang
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Publication number: 20130337064Abstract: To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range. The pharmaceutical composition is characterized by containing (A) N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by the following formula (1), a pharmacologically acceptable salt thereof, or a hydrate of any of these, and (B) one or more species selected from the group consisting of a sugar alcohol and a water-swelling additive.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Masazumi KOJIMA, Yoshio KUNO, Hiroaki NAKAGAMI, Shinji SAGASAKI, Koichi ISHIDOH, Gaku SEKIGUCHI
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Publication number: 20130331321Abstract: 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: ApplicationFiled: March 15, 2013Publication date: December 12, 2013Applicant: HEART METABOLICS LIMITEDInventor: HEART METABOLICS LIMITED
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Patent number: 8604202Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and B1, B2 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: GrantFiled: April 8, 2009Date of Patent: December 10, 2013Assignee: Merck Patent GmbHInventors: Daniel Cravo, Franck Lepifre, Sophie Hallakou-Bozec, Christine Charon
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Patent number: 8604051Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: GrantFiled: February 6, 2013Date of Patent: December 10, 2013Assignee: UCB Pharma S.A.Inventors: Martin Clive Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
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Publication number: 20130324571Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 18, 2013Publication date: December 5, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Publication number: 20130324537Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: ApplicationFiled: November 21, 2012Publication date: December 5, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130316986Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: IPCA LABORATORIES LIMITEDInventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki MOJE
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Publication number: 20130316987Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: IPCA LABORATORIES LIMITEDInventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki MOJE
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Publication number: 20130317021Abstract: The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: May 23, 2013Publication date: November 28, 2013Inventors: Andrea WOLKERSTORFER, Oliver Szolar, Norbert Handler, Stephen Cusack, Thibault Sauvaitre, Céline Simon, Christophe Morice, Bruno Giethlen, Thierry Langer, Mark Smith, Sung-Sau So, Dirk Classen-Houben, Helmut Buschmann
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Publication number: 20130317022Abstract: The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: May 23, 2013Publication date: November 28, 2013Applicants: European Molecular Biology Laboratory, F. Hoffmann-La Roche AGInventors: Andrea WOLKERSTORFER, Oliver SZOLAR, Norbert HANDLER, Stephen CUSACK, Thibault SAUVAITRE, Céline SIMON, Christophe MORICE, Bruno GIETHLEN, Thierry LANGER, Mark SMITH, Sung-Sau SO, Dirk CLASSEN-HOUBEN, Helmut BUSCHMANN
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Publication number: 20130316999Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: August 7, 2013Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
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Publication number: 20130309290Abstract: A stent is provided in combination with delivery of a tocopherol agent, and in particular a des-methyl tocopherol agent, and further beneficially a gamma-tocopherol agent, so as to reduce restenosis along the vessel or other lumenal wall where the stent is implanted. In particular applications, the stent is an endolumenal stent, and more specific beneficial applications is an endovascular stent, and the gamma-tocopherol elutes from a coating or carrier coupled with the stent. Certain combinations are provided with the des-methyl-tocopherol or phytyl substituted chromanol, e.g. gamma-tocopherol, combined with an additional agent such as an anti-restenosis agent, e.g. sirolimus, tacrolimus, everolimus, or paclitaxel, in order to provide synergistic benefit to tissues along the stented or recanalized regions. Other forms of tocopherol or tocotrienol, or other phytyl substituted chromanols, and other compounds such as palm oil, are ailso contemplated. for use to treat restenosis.Type: ApplicationFiled: July 29, 2013Publication date: November 21, 2013Applicant: CeloNova BioSciences, Inc.Inventors: James W. Larrick, James C. Peacock, III
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Publication number: 20130309191Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.Type: ApplicationFiled: November 30, 2012Publication date: November 21, 2013Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate Van Well
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Publication number: 20130296317Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.Type: ApplicationFiled: October 25, 2011Publication date: November 7, 2013Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau
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Patent number: 8574607Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.Type: GrantFiled: May 21, 2010Date of Patent: November 5, 2013Assignee: Syngenta Crop Protection, Inc.Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
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Patent number: 8569335Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: GrantFiled: April 9, 2009Date of Patent: October 29, 2013Assignees: EMS S.A., Universidade Estadual Paulista Julio de Mesquinta Filho—UNESPInventors: Ednir D. Vizioli, Chung M. Chin, Renato F. Menegon, Lorena Blau, Jean L. Santos, Maria D. Longo
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Publication number: 20130280323Abstract: Disclosed herein is a soft elastic capsule that includes an acid resistant, capsule shell that defines an encapsulated space having a predetermined volume, a liquid or semisolid fill comprising a first active ingredient located within the encapsulated space, and a first compressed tablet a having a minimal dimension of 2 mm, being located within the encapsulated space, unanchored to the capsule shell, and surrounded by the fill, said tablet comprising a second active ingredient that is substantially insoluble in the fill. A method of manufacturing a soft elastic capsule is also disclosed.Type: ApplicationFiled: April 12, 2013Publication date: October 24, 2013Inventors: Qi Fang, Don A. Archibald, Madhu Sudan Hariharan, Roger E. Gordon
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Patent number: 8563575Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: GrantFiled: June 22, 2011Date of Patent: October 22, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki
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Publication number: 20130274284Abstract: The present application relates to process for the preparation of prasugrel, its pharmaceutically acceptable salts, and its intermediates.Type: ApplicationFiled: August 2, 2011Publication date: October 17, 2013Applicants: DR. REDDY'S LABORATORIES, INC., Dr. Reddy's Laboratories Ltd.Inventors: Raghupathi Reddy Anumula, Goverdhan Gilla, Sampath Aalla, Dattatray Shamrao Metil, Srinivas Kurella, Kavitha Charagondla
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Publication number: 20130274195Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.Type: ApplicationFiled: December 24, 2012Publication date: October 17, 2013Inventors: CELERA CORPORATION, LEIDEN UNIVERSITY MEDICAL CENTER (LUMC) Acting on Behalf of ACADEMIC HOSPITAL LEIDEN
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Patent number: 8557994Abstract: The present invention relates to deuterium-enriched pyridinone carboxamides and their derivatives of the formula I, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT4) receptor subtype 4, and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, speech improvement in autistic children, sleep apnea in Alzheimer's patients, irritable bowel syndrome, gastroesophageal reflux disease, Crobn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, arterial fibrillation, arrhythmia, ischemic stroke, gastric emptying disorders, gastritis,Type: GrantFiled: July 26, 2010Date of Patent: October 15, 2013Inventor: Daljit Singh Dhanoa
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Publication number: 20130267554Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: ApplicationFiled: November 9, 2012Publication date: October 10, 2013Applicant: CERENIS THERAPEUTICS HOLDING SAInventors: Daniela Carmen ONICIU, Jean-Louis Henri DASSEUX, Otto GEOFFROY, Ronald BARBARAS
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Publication number: 20130259904Abstract: Prasugrel containing quickly released stable oral pharmaceutical compositions containing micronized prasugrel base, and starch or a starch derivative, and processes for the preparation thereof, and the use thereof for treating atherothrombotic events of patients suffering from acute coronary syndrome in which patients were subjected to percutaneous coronary intervention.Type: ApplicationFiled: April 2, 2012Publication date: October 3, 2013Applicant: EGIS PHARMACEUTICALS PLCInventors: András FEHÉR, Zsolt Zsigmond, Péter Tonka-Nagy, György Tibor Ujfalussy
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Publication number: 20130261107Abstract: In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 31, 2011Publication date: October 3, 2013Applicant: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Carrie K. Jones, Jose Manuel Bartolome-Nebreda, Susana Conde-Ceide, James Gregor MacDonald, Manuel Jesus Alcazar Vaca
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Publication number: 20130251814Abstract: The present invention discloses a magnetic nanodrug for treating thrombosis, which comprises a core formed of magnetic nanoparticles, a shell enveloping the core and made of carboxyl-functionalized polyaniline, and a thrombosis-treatment drug covalently bonded to the shell. The magnetic nanodrug of the present invention is non-toxic to vascular endothelial cells, has superior stability, features superparamagnetism, and can be uniformly dissolved in water. Therefore, the magnetic nanodrug for treating thrombosis can be guided by an external magnetic field to concentrate on a specified region and increase the effect of thrombosis treatment.Type: ApplicationFiled: September 14, 2012Publication date: September 26, 2013Inventors: Mu-Yi Hua, Hung-Wei Yang, Tony Wu, Rung-Ywan Tsai, Yunn-Hwa Ma, Jyh-Ping Chen
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Publication number: 20130252953Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.Type: ApplicationFiled: November 29, 2011Publication date: September 26, 2013Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
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Patent number: 8541443Abstract: An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, and method for producing the same.Type: GrantFiled: September 19, 2012Date of Patent: September 24, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Tetsuya Suzuki, Makoto Ono
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Patent number: 8541422Abstract: The present invention relates to a method of ameliorating the drawbacks of anti-platelet drug named clopidogrel. The method of the present invention comprises administration of an (S)oxo-clopidogrel or its derivative of the Formula IIA in its free or pharmaceutically acceptable salt form for alleviating the symptoms of thrombosis or embolism by inhibiting blood platelet aggregation. Compositions for use in such methods are also provided.Type: GrantFiled: August 26, 2011Date of Patent: September 24, 2013Assignee: IPCA Laboratories LimitedInventors: Ashok Kumar, Nellithanath Thankachen Byju
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Patent number: 8536336Abstract: The present invention provides for compounds of formula (I) wherein A2, L2, R1g, R2A, R3A, R4A, R1a, R1b, q1, and z are as defined in the specification, are prodrugs of CB2 receptors ligands and as such are useful in the prevention and treatment of various diseases and conditions including, but not limited to, pain.Type: GrantFiled: December 15, 2010Date of Patent: September 17, 2013Assignee: AbbVie Inc.Inventors: Derek W. Nelson, Michael J. Dart, Xueqing Wang, Bo Liu, Teodozyj Kolasa, Meena Patel
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Patent number: 8536337Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: GrantFiled: March 23, 2012Date of Patent: September 17, 2013Assignee: IPCA Laboratories LimitedInventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki Moje
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Patent number: 8530483Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.Type: GrantFiled: May 28, 2009Date of Patent: September 10, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg, Eric Hostetler
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Publication number: 20130231333Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: September 15, 2011Publication date: September 5, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Nicholas D. Smith, Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Andiliy G. Lai, Jackaline D. Julien, Mark R. Herbert, Celine Bonnefous, Karensa L. Douglas
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Publication number: 20130231364Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: January 25, 2013Publication date: September 5, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou