The Additional Hetero Ring Is Five-membered Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 546/268.4)
  • Patent number: 10370353
    Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: August 6, 2019
    Assignee: Mycovia Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, David Dale Wirth, Tracy Ehiwe, Thierry Bonnaud
  • Patent number: 10308632
    Abstract: Provided are polymorphic forms of compound 5 or 5*, or mixtures thereof, and polymorph forms of compound 14 or 14*, or mixtures thereof. Also provided are methods of preparing compound 5 or 5*, or mixtures thereof, and methods of preparing compound of 14 or 14*, or mixtures thereof, which are useful as antifungal agents. In particular, provided is new methodology for preparing polymorphs of the compounds described and substituted derivatives thereof.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: June 4, 2019
    Assignee: VPS-3, Inc.
    Inventors: David Dale Wirth, Christopher M. Yates
  • Patent number: 10239838
    Abstract: The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: March 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo
  • Patent number: 10208015
    Abstract: The invention relates to novel aryltriazolylpyridines of the general formula (I). Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects and arachnids in agriculture, and ectoparasites in veterinary medicine.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: February 19, 2019
    Assignee: BAYER ANIMAL HEALTH GMBH
    Inventors: Werner Hallenbach, Hans-Georg Schwarz, Ulrich Goergens, Kerstin Ilg, Andreas Turberg, Sebastian Horstmann, Adeline Koehler
  • Patent number: 10173998
    Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: January 8, 2019
    Assignees: Mycovia Pharmaceuticals, Inc., The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
  • Patent number: 10150754
    Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: December 11, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 10130645
    Abstract: There is disclosed is a method of treating disease using compound having formula SX-682 alone or in combination with an antineoplastic agent, microtubule affecting agents, antineoplastic agents, anti-angiogenesis agents, VEGF receptor kinase inhibitors, antibodies against the VEGF receptor, interferon, or radiation.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: November 20, 2018
    Assignee: Syntrix Biosystems, Inc.
    Inventors: John A. Zebala, Dean Y. Maeda, Aaron D. Schuler
  • Patent number: 10098343
    Abstract: The water dispersible granule according to the present disclosure includes aggregates, wherein each of the aggregates includes: one type of an agrochemical active ingredient powder and a carrier composed only of a low hygroscopic water-soluble powder, wherein the agrochemical active ingredient is tert-butyl {6-{[(Z)-(1-methyl-1H-5-tetrazolyl)phenylmethylene]aminooxymethyl}-2-pyridyl}carbamate.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: October 16, 2018
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yoshihisa Endo, Takahiro Maekawa
  • Patent number: 10046002
    Abstract: What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: August 14, 2018
    Assignee: SYNTRIX BIOSYSTEMS INC.
    Inventors: John A. Zebala, Dean Y. Maeda, Aaron D. Schuler
  • Patent number: 10017494
    Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: July 10, 2018
    Assignees: Mycovia Pharmaceuticals, Inc., The United States of America, as represented by the Department of Health and Human Services
    Inventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
  • Patent number: 10011593
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: July 3, 2018
    Assignee: ALLERGAN, INC.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang, Sandhya Rao, Rong Yang
  • Patent number: 10011585
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D Edmondson, Zhuyan Guo, Alan Hruza, Sung-Sau So, Wanying Sun, Amjad Ali, Rongze Kuang, Ying-Duo Gao, Anthony K Ogawa
  • Patent number: 9914726
    Abstract: Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and processes for their preparation.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: March 13, 2018
    Assignee: VPS-3, INC.
    Inventors: William J. Hoekstra, Daniel Knueppel, Jim Renga, Gregory Whiteker, Michael T. Sullenberger
  • Patent number: 9896436
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: February 20, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9840492
    Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: December 12, 2017
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, David Dale Wirth, Tracy Ehiwe, Thierry Bonnaud
  • Patent number: 9707248
    Abstract: There is disclosed is a method of treating cancer using compound having formula SX-682 alone or in combination with an antineoplastic agent, microtubule affecting agents, antineoplastic agents, anti-angiogenesis agents, VEGF receptor kinase inhibitors, antibodies against the VEGF receptor, interferon, or radiation.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: July 18, 2017
    Assignee: Syntrix Biosystems Inc.
    Inventors: John A. Zebala, Dean Y. Maeda, Aaron D. Schuler
  • Patent number: 9676770
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: June 13, 2017
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9650366
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: May 16, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang, Sandhya Rao, Rong Yang
  • Patent number: 9359336
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: June 7, 2016
    Assignee: Allergan, Inc.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang, Sandhya Rao, Rong Yang
  • Patent number: 9340553
    Abstract: Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: May 17, 2016
    Assignee: Pfizer Inc.
    Inventors: Spiros Liras, Vincent Mascitti, Benjamin Thuma
  • Patent number: 9328087
    Abstract: Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: May 3, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Carrie A. Costello, Jacqueline A. Ware, Robert J. Duguid
  • Patent number: 9309225
    Abstract: The present invention provides a compound of general formula 1, useful as potential anticancer agents against human cancer cell lines and process for the preparation thereof. R1=H, 4-F, 4-Cl, 4-Br, 4-OMe, 3-F, 2,4-diOMe, 2,5-diOMe, 3,5-diOMe, 3,4,5-triOMe, 4-ClBn R2=3-OPh, 4-F, 4-Cl, 4-Br, 4-OMe, 3,5-diOMe.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: April 12, 2016
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Ahmed Kamal, Budaganaboyina Prasad, Vadithe Lakshma Nayak, Vangala Saidi Reddy, Narrikolla Venkata Subba Reddy
  • Patent number: 9206160
    Abstract: This invention relates to a novel phenyl triazole derivative, pharmaceutical compositions containing this compound, and methods of treatment therewith. The compound of the invention is in particular considered useful for the treatment of central nervous system diseases and disorders which are responsive to modulation of GABAA receptors containing the ?5 subunit.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: December 8, 2015
    Assignee: SANIONA APS
    Inventors: Janus Schreiber Larsen, Magnus Gustafsson, Carsten Jessen
  • Patent number: 9186354
    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: Grant
    Filed: July 18, 2011
    Date of Patent: November 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Patent number: 9114137
    Abstract: Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: August 25, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maurizio Pulici, Chiara Marchionni, Gabriella Traquandi, Alessandra Scolaro, Daniele Donati
  • Patent number: 9056861
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilamide derivatives of the formula (I) in which R1, R2, R3, R4, R5 and Z are each as defined in the description, and to a novel crystal polymorph of these derivatives and to the use thereof in agrochemical formulations.
    Type: Grant
    Filed: September 22, 2014
    Date of Patent: June 16, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sergii Pazenok, Norbert Lui, Frank Volz, Britta Olenik, Christian Funke, Ruediger Fischer, Oliver Gaertzen, Martin-Holger Hinz, Arnd Neeff
  • 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
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040561
    Abstract: Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: May 26, 2015
    Assignee: Life Technologies Corporation
    Inventors: Jason Dallwig, David Hagen, Ching-Ying Cheung, Gerald Thomas, Stephen Yue
  • Patent number: 9029552
    Abstract: According to the present invention, a tetrazoyloxime derivative and a salt thereof, which are excellent in a control effect against plant disease injury, and a plant disease controlling agent containing the same as an active ingredient are provided.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: May 12, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Takeo Kobori, Hazumi Nomura, Ichirou Urihara, Hiroyasu Hosokawa, Atsunori Isshiki, Syuichi Ito, Jun Inagaki, Kazushige Fujii
  • Publication number: 20150126372
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 7, 2015
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbet M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Publication number: 20150119249
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)pyridin-3-yl-carboxamides of formula I and their use as herbicides, formula I. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)pyridin-3-yl-carboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas R, R1, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 9018384
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: April 28, 2015
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20150111747
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150111735
    Abstract: A pesticidal composition comprises a pyridine triazole compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse
  • Publication number: 20150105253
    Abstract: Salts of N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), W, X, Z and R represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B each represent nitrogen or carbon. M+ represents a cation.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 16, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Ralf Braun, Simon Doerner-Rieping, Hartmut Ahrens, Christian Waldraff, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Patent number: 9006269
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 14, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Patent number: 9006250
    Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 14, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Thomas L. Siddall, Norbert M. Satchivi, Paul R. Schmitzer
  • Patent number: 8987310
    Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: March 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James Barrow, Kelly-Ann Schlegel, Yoheng Shu, Zhi-Qiang Yang
  • Patent number: 8987311
    Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
  • Publication number: 20150080351
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • Patent number: 8975286
    Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: August 16, 2010
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8969352
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christine F. Gelin, Terry P. Lebold, Brock T. Shireman
  • Patent number: 8969572
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilamide derivatives of the formula (I) in which R1, R2, R3, R4, R5 and Z are each as defined in the description, and to a novel crystal polymorph of these derivatives and to the use thereof in agrochemical formulations.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Sergii Pazenok, Norbert Lui, Frank Volz, Britta Olenik, Christian Funke, RĂ¼diger Fischer, Oliver Gaertzen, Martin-Holger Hinz, Arnd Neeff
  • Publication number: 20150045557
    Abstract: The present invention provides a compound characterized by being represented by general formula (I): (wherein, A represents a halogen atom, alkyl group, haloalkyl group, alkoxy group, haloalkoxy group, alkylsulfonyl group, unsubstituted or substituted aryl group, cyano group or nitro group, n represents an integer of 0 to 5 (and A may be mutually the same or different when n is 2 or more), Y represents an alkyl group, M represents an alkaline metal or alkaline earth metal, and m represents an integer of 1 or 2).
    Type: Application
    Filed: March 6, 2013
    Publication date: February 12, 2015
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Keiichiro Matsuda, Masayuki Matsushita, Kaoru Noda, Satoshi Kajita
  • Patent number: 8952002
    Abstract: The present invention refers to aminoheteroaryl compounds of the following formula (I) as well as the preparation method and use thereof, wherein R1 and R3 are defined in the Description in details. The aminoheteroaryl compounds of the present invention are inhibitors of hepatocyte growth factor receptor (c-Met), have favorable inhibitory effect against c-Met and inhibitory effect against the proliferation of cancer cells, such that they may be used as therapeutic agents for the treatment of tumors and related diseases.
    Type: Grant
    Filed: January 17, 2013
    Date of Patent: February 10, 2015
    Assignee: Shanghai Allist Pharmaceuticals, Inc.
    Inventor: Huibing Luo
  • Patent number: 8951831
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: February 10, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Patent number: 8946434
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 3, 2015
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu