Piperidines Patents (Class 514/315)
  • Patent number: 8680102
    Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: March 25, 2014
    Assignee: Sanofi
    Inventors: Francis Barth, Daniel Bichon, Murielle Rinaldi-Carmona, Christian Congy
  • Publication number: 20140080871
    Abstract: The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: AMICUS THERAPEUTICS, INC.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Publication number: 20140073670
    Abstract: The present invention relates to a pharmaceutical formulation of fexofenadine hydrochloride in a solvent system suitable as a liquid fill composition. In another aspect, the invention also relates to a process for the preparation of the pharmaceutical formulation and the use of the composition for the treatment of allergic reactions in a patient.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 13, 2014
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Sudhakara Rao BADABHAGNI, Nilesh JAISWAL, Praveen KHULLAR, Kum PRASAD
  • Publication number: 20140051725
    Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8-12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compounds are effective to enhance glucocerebrosidase activity.
    Type: Application
    Filed: April 22, 2013
    Publication date: February 20, 2014
    Applicant: Mount Sinai School of Medicine of New York Univers
    Inventor: Mount Sinai School of Medicine of New York University
  • Publication number: 20140045891
    Abstract: Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: Mitos Pharmaceuticals, Inc.
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Patent number: 8633221
    Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: January 21, 2014
    Assignee: Mount Sinai School of Medicine of New York University
    Inventors: Jian-Qiang Fan, Satoshi Ishii
  • Patent number: 8633310
    Abstract: Herein are described compounds having a structure or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: January 21, 2014
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20140018317
    Abstract: A compound having a structure of:
    Type: Application
    Filed: February 17, 2012
    Publication date: January 16, 2014
    Applicant: University of Pittsburgh-Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Patent number: 8629274
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: January 14, 2014
    Assignee: Novira Therapeutics, Inc.
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Publication number: 20140011841
    Abstract: Described are compositions comprising imino sugar acids for the treatment of energy utilization disease (e.g. metabolic syndrome, including any disease or disorder associated therewith, for example central obesity, elevated levels of triglycerides and diabetes, including type 1 diabetes, type 2 diabetes and insulin resistance), processes for producing said compositions from various plant sources, together with various products, compounds, compositions, medical uses and methods based thereon.
    Type: Application
    Filed: February 5, 2013
    Publication date: January 9, 2014
    Inventors: Robert James NASH, Francis Xavier WILSON, Graeme HORNE
  • Publication number: 20130338110
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
  • Patent number: 8604057
    Abstract: The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: December 10, 2013
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Patent number: 8604206
    Abstract: The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: December 10, 2013
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Patent number: 8604066
    Abstract: A medication, a pharmaceutical composition, and method for the treatment of respiratory poisoning in animals and humans caused by organophosphorus compounds, whereby said medication and said pharmaceutical composition comprise at least one oxime and one blocker of organic cation transporters (OCT).
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: December 10, 2013
    Assignee: SERB
    Inventors: Frédéric J. Baud, Pascal Houze, Maya Kayouka
  • Patent number: 8604059
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: December 10, 2013
    Assignee: BKG Pharma APS
    Inventor: Birgit Kjældgaard Giwercman
  • Publication number: 20130324540
    Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: Obschestvo Ogranichennoi Otvetstvennostyu "Pharmenterprises"
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
  • Patent number: 8598159
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 3, 2013
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
  • Patent number: 8592419
    Abstract: The invention provides the compounds of formula (): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: November 26, 2013
    Assignee: MUSC Foundation for Research Development
    Inventors: Alicja Bielawska, Yusuf A. Hannun, James Norris, Zdzislaw M. Szulc, Jian-yun Dong, Jacek Bielawski, David A. Schwartz, David H. Holman, Ahmed M. El-Zawahry, John McKillop
  • Patent number: 8586575
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Publication number: 20130296245
    Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
    Type: Application
    Filed: November 14, 2011
    Publication date: November 7, 2013
    Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
  • Publication number: 20130296323
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
    Type: Application
    Filed: February 27, 2013
    Publication date: November 7, 2013
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
  • Patent number: 8575165
    Abstract: Methods for treating an inflammatory disorder and for inhibiting the production of IL-23 using 2,4-pyrimidinediamine compounds represented by formula (I):
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: November 5, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Tarikere Gururaja, Donald G. Payan, Kin Tso, Taisei Kinoshita, Rongxian Ding, Rajinder Singh, Stephanie Yung, Hui Li, Esteban Masuda
  • Patent number: 8574607
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Patent number: 8575168
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: November 5, 2013
    Assignee: IRM LLC
    Inventors: Mihai Azimioara, Christopher Cow, Robert Epple, Gerald Lelais, John Mecom, Victor Nikulin
  • Patent number: 8569313
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: October 29, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Publication number: 20130280323
    Abstract: 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: Application
    Filed: April 12, 2013
    Publication date: October 24, 2013
    Inventors: Qi Fang, Don A. Archibald, Madhu Sudan Hariharan, Roger E. Gordon
  • Publication number: 20130281294
    Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.
    Type: Application
    Filed: June 17, 2013
    Publication date: October 24, 2013
    Inventors: HUAZHANG HUANG, Ratnakar Asolkar
  • Patent number: 8563581
    Abstract: Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
    Type: Grant
    Filed: February 2, 2006
    Date of Patent: October 22, 2013
    Assignee: Mitos Pharmaceuticals, Inc.
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 8557836
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: October 15, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8557844
    Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: October 15, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Frances Mary Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
  • Patent number: 8546563
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
  • Patent number: 8541450
    Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur
  • Publication number: 20130237567
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Application
    Filed: April 25, 2013
    Publication date: September 12, 2013
    Applicants: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • Patent number: 8524741
    Abstract: Provided herein are piperidine alkaloids and uses thereof in neurological disorders and physical enhancement applications.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: September 3, 2013
    Assignee: Synapsin Pharmaceuticals, Inc.
    Inventors: Denis Dorsey, Mark S. Kindy
  • Publication number: 20130224255
    Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.
    Type: Application
    Filed: February 23, 2012
    Publication date: August 29, 2013
    Applicant: Abbott Cardiovascular Systems Inc.
    Inventors: Syed F.A. Hossainy, Paul M. Consigny
  • Publication number: 20130217574
    Abstract: The present invention relates to compositions that include a combination of one or more pesticides and one or more adjuvants.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 22, 2013
    Applicant: BAYER CROPSCIENCE LP
    Inventor: BAYER CROPSCIENCE LP
  • Patent number: 8513301
    Abstract: A kind of piperphentonamine hydrochloride lyophilized powder for injection and a preparation method thereof. The injection is prepared by one portion of piperphentonamine hydrochloride, 2.5-30 parts of excipient and 400-600 parts of water for injection with pH 1.5-5.5 via freeze-drying. The excipient is mannitol, dextran, lactose, saccharose, polyethylene glycol, poloxamer, glycine, etc.; It is preferred that the injection comprises one part of piperphentonamine hydrochloride, 10 parts of mannitol and 500 parts of water for injection with pH 2.0-3.0. The product is prepared by adding said piperphentonamine hydrochloride and excipient into water for injection, heating at 40° C.-90° C., ultrasonic dissolving, degerming, individually packing, pre-freezing and multistage drying, and packaging. Individually packing into a tubular glass bottle with brown color is preferred. The appearance, color & luster and solubility of the injection are excellent, the stability is good and with long storage period.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: August 20, 2013
    Assignee: Guangzhou Zhongwei Biotechnology Ltd.
    Inventors: Huayin Wan, Rubing Li, Yonghe Li, Lijian Zhou, Tieqiu Liu, Xiaohui Zhong
  • Patent number: 8501775
    Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: August 6, 2013
    Assignee: SALTIGO GmbH
    Inventors: Achim Harder, Georg von Samson-Himmlstjerna, Bernd-Wieland Kruger, Heinz Melhorn, Jurgen Schmidt
  • Publication number: 20130195798
    Abstract: One can treat a viral infection by first administering at least one first antiviral compound for a first time period and then, after the end of the first time period, concurrently or subsequently administering the at least one first antiviral compound and at least one second antiviral compound for a second period. In some cases, after the end of the second period, the same at least one second antiviral compound that was administered during the second time period may be administered for a third time period without concurrent or subsequent administration of the at least one first antiviral compound.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 1, 2013
    Applicants: The Chancellors, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: United Therapeutics Corporation, The Chancellors, Masters and Scholars of the Univ
  • Patent number: 8497262
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: July 30, 2013
    Assignee: Dart NeuroScience (Cayman) Ltd
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
  • Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • Patent number: 8492568
    Abstract: The present invention provides chromane derivatives as transient receptor potential vanilloid (TRPV) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: July 23, 2013
    Assignee: Glenmark Pharamceuticals S.A.
    Inventors: V. S. Prasada Rao Lingam, Abraham Thomas, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20130183390
    Abstract: The present invention relates to compositions that include a combination of one or more pesticides and one or more adjuvants.
    Type: Application
    Filed: January 2, 2013
    Publication date: July 18, 2013
    Applicant: BAYER CROPSCIENCE LP
    Inventor: BAYER CROPSCIENCE LP
  • Patent number: 8486970
    Abstract: [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: May 26, 2008
    Date of Patent: July 16, 2013
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 8486971
    Abstract: The invention relates to compounds of the formula (I), where: R1 is: a —NR5R6 group; an unsubstituted or substituted phenyl; R2 is: a (C1-C4)alkyl; an —X—R7 group; R3 and R4 each are independently a substituted phenyl; R5 is a hydrogen atom or a (C1-C4)alkyl; R6 is an unsubstituted or substituted (C1-C4)alkyl; or R5 and R6 together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C1-C5)alkylene; R7 is an —OR8 group, a —NR9R10 group, an —SO2—(C1-C4)alkyl group; R8 is a hydrogen atom or a (C1-C4)alkyl; R9 is a hydrogen atom or a (C1-C4)alkyl; R10 is a hydrogen atom, a —COR11 group, an —SO2R11 group or a —CO(CH2)mOH group; R11 is an unsubstituted or substituted (C1-C4)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Jean-Philippe Ducoux, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Publication number: 20130172319
    Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.
    Type: Application
    Filed: February 26, 2013
    Publication date: July 4, 2013
    Applicants: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: Cambridge Enterprise Limited, David J. Grainger, David John Fox
  • Publication number: 20130172385
    Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).
    Type: Application
    Filed: May 9, 2008
    Publication date: July 4, 2013
    Applicant: LANXESS DEUTSCHLAND GMBH
    Inventors: Achim Harder, Georg von Samson-Himmlstjerna, Bernd-Wieland Kruger, Heinz Mehlhorn, Jurgen Schmidt