Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/183)
  • Patent number: 9562045
    Abstract: The present invention provides compounds of general formula 1 useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: February 7, 2017
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Budde Mahendar, Saidulu Mattapally, Mettu Ravinder, Sanjay Kumar Banerjee, Vaidya Jayathirtha Rao
  • Patent number: 9249139
    Abstract: The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: February 2, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Budde Mahendar, Saidulu Mattapally, Mettu Ravinder, Sanjay Kumar Banerjee, Vaidya Jayathirtha Rao
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150099887
    Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone 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 furanone 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 furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 8969570
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: March 3, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • Publication number: 20150056699
    Abstract: This invention provides a compound having the structure wherein A is a ring structure, with or without substitution; Z is present or absent and when present is wherein n is 0, 1, 2, 3, or 4; Y is —(CR11R12)—, —NH(CR11R12)—, or —O(CR11R12)—, wherein R11 and R12 are each hydrogen or combine to form a carbonyl; R1, R2, R3, R4, R5 and R6 are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester or amide; ? represents a bond, which is present or absent and when ? is present, then R7 and R8 are absent; R7 and R8 are present when ? is absent and are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester, amide or R5 and R7 combine to form a carbonyl or R6 and R8 combine to form a carbonyl; R9 and R10 are each hydrogen o
    Type: Application
    Filed: August 24, 2012
    Publication date: February 26, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Dalibor Sames, Xiaoguang Li, Shu Li, Andrew Kruegel, Richard Karpowicz, Ignacio Carrera, Souvik Rakshit
  • Patent number: 8962844
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: February 24, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Dongpeng Wan
  • Patent number: 8962843
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: February 24, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8940897
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: January 27, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8933233
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8933232
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8927724
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: January 6, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch, Dongpeng Wan, Jon Christian Baber
  • Patent number: 8921560
    Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: December 30, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 8916709
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 23, 2014
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Jon Christian Baber
  • Patent number: 8907095
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: October 20, 2008
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yan Xia, Craig D. Boyle, William J. Greenlee, Samuel Chackalamannil, Charles Lee Jayne
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140350246
    Abstract: The present invention relates to 7-membered nitrogen-containing heterocyclic compounds and methods of making the same. Using a novel aza-[4+3] cycloaddition reaction, the 7-membered heterocyclic compounds are synthesized by reacting a first reactant and a second reactant. Exemplary first reactants and second reactants include ?-halohydroxamates and dienes, respectively.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Applicant: Board of Regents of the Nevada System of Higher Education, on behalf of the University of Nevada
    Inventor: Christopher S. Jeffrey
  • Patent number: 8853406
    Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I).
    Type: Grant
    Filed: August 5, 2008
    Date of Patent: October 7, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Alain Philippe Poncelet, Bruno Schoentjes, Pierre-Henri Storck, Virginie Sophie Poncelet, Carina Leys
  • Publication number: 20140296530
    Abstract: The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
    Type: Application
    Filed: January 30, 2014
    Publication date: October 2, 2014
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Budde MAHENDAR, Saidulu MATTAPALLY, Mettu RAVINDER, Sanjay Kumar BANERJEE, Vaidya Jayathirtha RAO
  • Publication number: 20140275006
    Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
  • 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: 20140235665
    Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Publication number: 20140228321
    Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 14, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
  • Publication number: 20140221357
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 7, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140200227
    Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: January 14, 2014
    Publication date: July 17, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
  • Patent number: 8759341
    Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: June 24, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
  • Publication number: 20140148477
    Abstract: The present invention provides an animal ectoparasite-controlling agent and a method for preventing or treating infection in animals caused by parasites by using the controlling agent. An animal ectoparasite-controlling agent exhibiting excellent insecticidal activity, and a method for preventing or treating infection in animals caused by parasites by using the controlling agent are obtained by using a compound having a pyrazole ring at the 4-position of the piperidine ring as an active ingredient.
    Type: Application
    Filed: July 19, 2012
    Publication date: May 29, 2014
    Applicant: OTSUKA AGRITECHNO CO., LTD.
    Inventors: Yasuhiro Endo, Yuichi Shirai
  • Publication number: 20140135500
    Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
  • Publication number: 20140128365
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 8, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
  • Publication number: 20140113908
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY, Beatrix WAGNER
  • Publication number: 20140107110
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8680276
    Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: March 25, 2014
    Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
  • Publication number: 20140051719
    Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Applicant: Simon Fraser University
    Inventors: David Jaro Vocadlo, Ernest John McEachern, Keith Stubbs
  • Patent number: 8609686
    Abstract: The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: December 17, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Nell, Alexandros Vakalopoulos, Frank Süβmeier, Barbara Albrecht-Küpper, Katja Zimmerman, Joerg Keldenich, Daniel Meibom
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Patent number: 8563580
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: October 22, 2013
    Assignee: Georgetown University
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Publication number: 20130274287
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 17, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
  • Publication number: 20130267710
    Abstract: This invention provides novel (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof, preferably in substantially enantiomerically enriched forms, intermediates thereto, and processes of their synthesis.
    Type: Application
    Filed: January 24, 2013
    Publication date: October 10, 2013
    Inventor: Robert M. Moriarty
  • Patent number: 8541441
    Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: September 24, 2013
    Assignee: Simon Fraser University
    Inventors: David Jaro Vocadlo, Ernest John McEachern, Keith Stubbs
  • Patent number: 8536164
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 17, 2013
    Assignee: Pfizer Inc.
    Inventors: Todd W. Butler, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
  • Publication number: 20130237515
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.
    Type: Application
    Filed: February 28, 2013
    Publication date: September 12, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
  • Patent number: 8461340
    Abstract: There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: June 11, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hiroshi Hakuta, Tsutomu Imagawa, Hirohito Oooka, Shinya Fukuhara
  • Patent number: 8431707
    Abstract: The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: April 30, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hirohito Oooka, Shinya Fukuhara
  • Patent number: 8367666
    Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: February 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takashi Sasatani, Yoshiharu Hiramatsu, Susumu Mitsumori
  • Patent number: 8334300
    Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: December 18, 2012
    Assignee: Bayer Aktiengesellshaft
    Inventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
  • Publication number: 20120309964
    Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.
    Type: Application
    Filed: February 24, 2011
    Publication date: December 6, 2012
    Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
  • Publication number: 20120289700
    Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).
    Type: Application
    Filed: December 17, 2010
    Publication date: November 15, 2012
    Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
  • Patent number: RE45364
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: February 3, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa