Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Patents (Class 514/259.5)
  • Patent number: 9273054
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: March 1, 2016
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Kai Long, Xiaomin Zhang, Haihua Yu
  • Patent number: 8975265
    Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: March 10, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
  • Publication number: 20150038329
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Publication number: 20150005289
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 1, 2015
    Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20140329838
    Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Application
    Filed: June 13, 2014
    Publication date: November 6, 2014
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jose Manuel Bartolome-Nebreda, Gregor Macdonald, Susana Conde-Ceide, Carrie K. Jones, Maria Luz Martin-Martin, Han Min Tong
  • Publication number: 20140315912
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Application
    Filed: July 18, 2011
    Publication date: October 23, 2014
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Publication number: 20140213599
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Application
    Filed: January 23, 2014
    Publication date: July 31, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Zehong WAN, Yingxia Sang, Qing Zhang
  • Patent number: 8771733
    Abstract: Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Maria T. Cruanes, Wei Xu, Laura M. Artino, Honggang Zhu
  • Publication number: 20140179715
    Abstract: Disclosed are 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1H)-one compounds that inhibit Lp-PLA2, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Application
    Filed: July 25, 2012
    Publication date: June 26, 2014
    Applicant: Glaxo Group Limited
    Inventors: Zehong Wan, Kai Long, Yingxia Sang, Xiaobo Su
  • Publication number: 20140179716
    Abstract: The present invention relates to novel bicyclic pyrimidone compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Application
    Filed: July 25, 2012
    Publication date: June 26, 2014
    Inventors: Zehong Wan, Kai Long, Xiaomin Zhang, Haihua Yu
  • Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20140142121
    Abstract: Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 22, 2014
    Inventors: Dario C. Altieri, Byoung Heon Kang
  • Patent number: 8729074
    Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Amgen Inc.
    Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
  • Publication number: 20140079666
    Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. 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: Application
    Filed: May 5, 2012
    Publication date: March 20, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Thomas R. Webb, Vincent A. Boyd
  • Publication number: 20140073653
    Abstract: The present invention relates to compounds of formula IVA, formula IVB, or formula IVC, useful as 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 diseases using such CFTR modulators.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 13, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Hayley Binch, Peter D.J. Grootenhuis, Albert Pierce, Lev T.D. Fanning
  • Publication number: 20140024659
    Abstract: 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: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: BASF SE
    Inventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
  • Patent number: 8614219
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: December 24, 2013
    Assignees: Sanofi-aventis, Mitsubishi Tanabe Pharma Corporation
    Inventors: Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
  • Publication number: 20130289053
    Abstract: Disclosed are formulations and related methods that comprise a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions; a specified linear polymer comprising lactide repeat units; and one or more solvents that have a solvent capacity.
    Type: Application
    Filed: March 8, 2013
    Publication date: October 31, 2013
    Inventor: Durect Corporation
  • Publication number: 20130245043
    Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Application
    Filed: March 14, 2012
    Publication date: September 19, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Carrie K. Jones, María Luz Martín-Martín, Han Min Tong
  • Publication number: 20130203778
    Abstract: The present patent application relates to a pharmaceutical composition comprising a fused pyrimidineone derivative having transient receptor potential modulating activity and a hydrophilic carrier.
    Type: Application
    Filed: March 21, 2011
    Publication date: August 8, 2013
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Ulhas Dhuppad, Sunil Chaudhari
  • Publication number: 20130190332
    Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 7, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
  • Patent number: 8431581
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: April 30, 2013
    Assignee: Avexa Limited
    Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Van de Graff, Lisa Jane Winfield
  • Patent number: 8431582
    Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: April 30, 2013
    Assignee: NUtech Ventures
    Inventors: Concetta DiRusso, Paul Black
  • Patent number: 8410118
    Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: April 2, 2013
    Assignee: NUtech Ventures
    Inventors: Concetta DiRusso, Paul Black
  • Publication number: 20130030012
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Glaxo Group Limited
    Inventors: Kai Long, Zehong Wan
  • Publication number: 20130029981
    Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.
    Type: Application
    Filed: June 18, 2012
    Publication date: January 31, 2013
    Applicant: Katholieke Universiteit Leuven
    Inventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
  • Patent number: 8338412
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: December 25, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco G. Salituro, John P. Duffy, John E. Cochran, Edmund M. Harrington, Mark A. Murcko, Keith P. Wilson, Michael Su, Vincent P. Galullo
  • Patent number: 8273752
    Abstract: The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: September 25, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Dmitry Zubov, Jochen Strayle, Michael Sperzel
  • Publication number: 20120220566
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 15, 2010
    Publication date: August 30, 2012
    Applicant: Rib-X Pharmaceuticals, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
  • Publication number: 20120202819
    Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.
    Type: Application
    Filed: September 27, 2010
    Publication date: August 9, 2012
    Applicant: Merck Sharp & Dohme Corporation
    Inventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
  • Publication number: 20120202792
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and/or reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 15, 2010
    Publication date: August 9, 2012
    Applicant: Rib-X Pharmaceuticals, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Shili Chen, Marco DeVivo, Rongliang Lou, Brian T. Wimberly
  • Publication number: 20120122680
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 3, 2010
    Publication date: May 17, 2012
    Applicant: E.I. Du Pont de Nemours and Company
    Inventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
  • Patent number: 8148364
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: April 3, 2012
    Assignees: Sanofi-Aventis, Mitsubishi Tanabe Pharma Corporation
    Inventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
  • Publication number: 20120071474
    Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Application
    Filed: March 19, 2010
    Publication date: March 22, 2012
    Applicant: AMGEN INC.
    Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
  • Publication number: 20110301174
    Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
    Type: Application
    Filed: June 8, 2011
    Publication date: December 8, 2011
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Patent number: 8067425
    Abstract: Embodiments of this invention provide novel cyclic compounds structurally related to diketopiperazines and methods for their therapeutic use. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterized by neuronal degeneration and/or death. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.
    Type: Grant
    Filed: August 31, 2004
    Date of Patent: November 29, 2011
    Assignee: Neuren Pharmaceuticals Limited
    Inventors: Margaret Anne Brimble, Jian Guan, Frank Sieg
  • Patent number: 8044050
    Abstract: The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: October 25, 2011
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Zoller, Hartmut Strobel, David William Will, Paulus Wohlfart
  • Publication number: 20110230459
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: March 10, 2011
    Publication date: September 22, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
  • Publication number: 20110224199
    Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: May 20, 2011
    Publication date: September 15, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
  • Publication number: 20110028476
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.
    Type: Application
    Filed: September 1, 2010
    Publication date: February 3, 2011
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20110028487
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
    Type: Application
    Filed: July 2, 2009
    Publication date: February 3, 2011
    Applicant: AVEXA LIMITED
    Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Van De Graff, Lisa Jane Winfield
  • Publication number: 20110008259
    Abstract: 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 diseases using such CFTR modulators.
    Type: Application
    Filed: June 11, 2010
    Publication date: January 13, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Peter D.J. Grootenhuis, Albert Pierce, Lev T.D. Fanning
  • Publication number: 20100267748
    Abstract: The present invention discloses 1H-pyrido[1,2-a]pyrimidin-4(9aH)-one derivatives or 1H-pyrimido[1,2-a]pyrimidin-4(9aH)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, cancer, diabetes, obesity, metabolic syndrome and the like.
    Type: Application
    Filed: October 14, 2009
    Publication date: October 21, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Dmitry Koltun, Alexey Ivanov, Natalya Vasilevich, Jeff Zablocki
  • Publication number: 20100216765
    Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
    Type: Application
    Filed: April 6, 2010
    Publication date: August 26, 2010
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
  • Patent number: 7781440
    Abstract: The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3? or GSK3? and cdk5/p25, such as Alzheimer disease.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: August 24, 2010
    Assignees: Sanofi-Aventis, Mitsubishi Pharma Corporation
    Inventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Severine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
  • Publication number: 20100210667
    Abstract: Disclosed are imidazo[1,2-c]pyrimidin-2-ylmethyl substituted piperidine derivatives having the formula: where Ar is and where R1, R2, R3, n, p and q are as defined herein, and their use as pharmaceuticals.
    Type: Application
    Filed: July 1, 2008
    Publication date: August 19, 2010
    Inventors: Giuseppe Alvaro, David Amantini, Sandro Belvedere
  • Publication number: 20100204237
    Abstract: Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(?O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: April 21, 2010
    Publication date: August 12, 2010
    Inventors: Hidenori Mikamiyama, Minamo Iwata, Yoshiyuki Taoda
  • Publication number: 20100190692
    Abstract: A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells originating in the brain and/or nervous system and/or the meninges and/or reactive neuroglia cells and/or primitive neuroectodermal tumor cells and/or on Kaposi sarcoma is provided. Furthermore a method for reducing degenerate GnRH-positive tumor cells and/or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and/or GnRH antagonist and/or an erythropoietin agonist, and/or a thrombopoietin agonist, and/or a endothelin antagonist and/or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.
    Type: Application
    Filed: February 5, 2010
    Publication date: July 29, 2010
    Inventor: JOHANNES C. VAN GROENINGHEN
  • Publication number: 20100168063
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.
    Type: Application
    Filed: December 21, 2007
    Publication date: July 1, 2010
    Applicant: Avexa Limited
    Inventors: Eric Dale Jones, Jonathan Alan Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherine MacFarlane