Additional Hetero Ring Which Is Unsaturated Patents (Class 544/333)
  • Patent number: 10687533
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides and especially as fungicides.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: June 23, 2020
    Assignee: Syngenta Participations AG
    Inventors: Farhan Bou Hamdan, Daniel Stierli, Stephane André Marie Jeanmart, Christopher Richard Ayles Godfrey, Thomas James Hoffman, Renaud Beaudegnies, Martin Pouliot
  • Patent number: 10633368
    Abstract: Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.
    Type: Grant
    Filed: January 16, 2017
    Date of Patent: April 28, 2020
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Hu Huang, Wenfeng Huang, Guoliang Tu, Jiegen Liu, Zhongming Xu, Qianghui Wu, Zhaoyang Meng, Yuling Fang
  • Patent number: 10485872
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: November 26, 2019
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventor: Yoko Endo
  • Patent number: 10221162
    Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: March 5, 2019
    Assignee: AMGEN INC.
    Inventors: Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, Julie Anne Heath, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Aarif Yusuf Khakoo, David John Kopecky, Su-Jen Lai, Zhihua Ma, Lawrence R. McGee, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Kevin Yang, Wen-Chen Yeh, Mikkel V. Debenedetto, Robert P. Farrell, Simon J. Hedley, Ted C. Judd, Frank Kayser
  • Patent number: 10155741
    Abstract: The present invention relates to compounds of formula I wherein R1? is methyl; R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropylmethyl, or hydroxmethyl; R3 is Cl, F, CF3, methyl, methoxy, or cyclopropyl; R4 is hydrogen, methyl, F or Cl; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: December 18, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Marius Hoener, Juergen Wichmann
  • Patent number: 10149908
    Abstract: The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: December 11, 2018
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventor: Yoko Endo
  • Patent number: 10034886
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: July 31, 2018
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs, Daniel Glynn, Mark Mills
  • Patent number: 9994567
    Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: June 12, 2018
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Jiazhong Zhang
  • Patent number: 9957252
    Abstract: The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: May 1, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Gary D. Gustafson, Asako Kubota, Maurice C. Yap, Zachary A. Buchan, Kimberly M. Steward, Michael T. Sullenberger, William J. Hoekstra, Christopher M. Yates
  • Patent number: 9937175
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: April 10, 2018
    Assignee: Sanofi
    Inventor: Christopher L. VanDeusen
  • Patent number: 9839664
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: December 12, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9795613
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: October 24, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs, Daniel Glynn, Mark Mills
  • Patent number: 9776998
    Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: October 3, 2017
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Jiazhong Zhang
  • Patent number: 9598430
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: March 21, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9550737
    Abstract: A series of benzimidazole derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: January 24, 2017
    Assignee: UCB Biopharma SPRL
    Inventors: Daniel Christopher Brookings, Mark Daniel Calmiano, Ellen Olivia Gallimore, Helen Tracey Horsley, Martin Clive Hutchings, James Andrew Johnson, Boris Kroeplien, Fabien Claude Lecomte, Martin Alexander Lowe, Timothy John Norman, John Robert Porter, Joanna Rachel Quincey, James Thomas Reuberson, Matthew Duncan Selby, Michael Alan Shaw, Zhaoning Zhu, Anne Marie Foley
  • Patent number: 9533982
    Abstract: Disclosed are negative 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: Grant
    Filed: March 20, 2015
    Date of Patent: January 3, 2017
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Andrew S. Felts
  • Patent number: 9505746
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: November 29, 2016
    Assignee: Genentech, Inc.
    Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
  • Patent number: 9499551
    Abstract: Disclosed herein are substituted pyrrolopyridine and pyrrolopyrazine compounds and compositions useful in the treatment of TAK mediated diseases, such as cancer, having the structure of Formula (I): wherein R1, R2, R3, and R4 are as defined in the detailed description. Methods of modulation of TAK activity in a human or animal subject are also provided, providing therapeutic benefit to subjects with disease conditions, especially cancer.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: November 22, 2016
    Assignee: Confluence Life Sciences, Inc.
    Inventors: Eric Jon Jacobsen, James Robert Blinn, John Robert Springer, Susan L. Hockerman
  • Patent number: 9474755
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: October 25, 2016
    Assignee: Celgene International II SARL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9469627
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 18, 2016
    Assignee: Sanofi
    Inventors: Christopher L. Vandeusen, Franz J. Weiberth, Harpal S. Gill, George Lee, Andrea Hillegass
  • Patent number: 9464084
    Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: October 11, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De Angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
  • Patent number: 9315502
    Abstract: The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: April 19, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
  • Patent number: 9266870
    Abstract: A heteroaromatic methyl cyclic amine derivative represented by formula (IA) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: February 23, 2016
    Assignee: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Aya Futamura, Yuko Araki, Masahito Abe, Hiroshi Ohta, Ryo Suzuki, Dai Nozawa
  • Patent number: 9221791
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: December 29, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 9206180
    Abstract: A quantitative model that describes the assembly of diketopyrrolopyrrole-based donors and a perylenediimide acceptor into chiral superstructures, as a result of both hydrogen bonding and ?•••? stacking. This model provides thermodynamic parameters (?H° and ?S°) for all noncovalent interactions involved in the assembly and explains the subtle supramolecular cues that convert disordered aggregates into well-defined helical assemblies.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: December 8, 2015
    Assignee: New York University
    Inventors: Adam B. Braunschweig, Stephen Rieth, Zhong Li, Charlotte E. Hinkle
  • Patent number: 9209408
    Abstract: Novel benzoxazole derivatives are provided to reduce driving voltage of light-emitting elements, and to reduce power consumption of light-emitting elements, light-emitting devices, and electronic devices. A benzoxazole derivative represented by the general formula (G1) is provided. Since the benzoxazole derivative represented by the general formula (G1) has an electron-injecting property, the benzoxazole derivative can be suitably used for light-emitting elements, light-emitting devices, and electronic devices.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: December 8, 2015
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Hiroko Nomura, Takahiro Ushikubo, Satoshi Seo
  • Patent number: 9173396
    Abstract: The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: November 3, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Thomas Bretschneider, Adeline Köhler, Joachim Kluth, Martin Füβlein, Peter Jeschke, Reiner Fischer, Friedrich August Mühlthau, Olga Malsam, Arnd Voerste, Klaus-Helmut Müller, Yoshitaka Sato
  • Patent number: 9085562
    Abstract: Disclosed are negative 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: Grant
    Filed: March 5, 2012
    Date of Patent: July 21, 2015
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates, Brian A. Chauder
  • Patent number: 9045466
    Abstract: An amidine compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: June 2, 2015
    Assignees: TAISHO PHARMACEUTICAL CO., LTD, TOYAMA CHEMICAL CO., LTD.
    Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Publication number: 20150148349
    Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Patent number: 9040692
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 26, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Publication number: 20150141395
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 26, 2013
    Publication date: May 21, 2015
    Inventor: Kap-Sun Yeung
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Patent number: 9034880
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150133446
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 14, 2015
    Inventors: R. Michael Lawrence, Michael M. Miller, Dietmar Alfred Seiffert, Shoshana L. Posy, Pancras C. Wong, Jacques Banville, Edward H. Ruediger, Daniel H. Deon, Alain Martel, François Tremblay, Julia Guy, Jean-François Lavallée, Marc Gagnon
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Patent number: 9028728
    Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Patent number: 9023872
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Ixchelsis Limited
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Publication number: 20150119390
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 30, 2015
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Patent number: 9018216
    Abstract: The invention relates to solid forms of the Formula (I) wherein X is —PO(OH)2, —PO(OH)O?M+, or —PO(O?)2.2M+, wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of the compound and method of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: April 28, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hardwin O'Dowd, Dainius MacIkenas, Bin Song
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Publication number: 20150111870
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 23, 2015
    Applicant: JOHNSON & JOHNSON
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS, KELLY MCCLURE, VIRGINIA TANIS