Polycyclo Ring System Having The Asymmetrical Triazine Ring As One Of The Cyclos Patents (Class 544/183)
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Patent number: 12098151Abstract: The present invention provides a compound having antiviral activity, especially having arenavirus proliferation inhibitory activity, and/or a medicament comprising the compound. More preferably, the present invention provides a compound having proliferation inhibitory activity on the Old World arenaviruses such as Luna virus, Lassa virus, and lymphocytic choriomeningitis virus and/or the New World arenaviruses such as Junin virus, and/or a medicament comprising the compound.Type: GrantFiled: September 30, 2022Date of Patent: September 24, 2024Assignees: NATIONAL UNIVERSITY COPORATION HOKKAIDO UNIVERSITY, SHIONOGI & CO., LTD.Inventors: Akihiro Ishii, Akihiko Sato, Makoto Kawai, Yoshiyuki Taoda
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Patent number: 11927568Abstract: A wireless ultrasound sensor 404 for non-destructive testing of a test object 502, the sensor comprising: an ultrasound transducer 406; a first induction coil 408, electrically coupled to the ultrasound transducer; a second induction coil 414, electrically coupled in parallel with the first induction coil; wherein the first and second induction coils are arranged to enable the transducer to be inductively operated by a remote device 504; and wherein the diameter of the second induction coil is greater than the diameter of the first induction coil.Type: GrantFiled: July 22, 2021Date of Patent: March 12, 2024Assignee: THE UNIVERSITY OF BRISTOLInventors: Cheng Huan Zhong, Anthony Croxford, Paul Wilcox
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Patent number: 11666565Abstract: The present invention resides in the discovery that Smad3, a key downstream mediator of TGF-? signaling, plays a critical role in development and progression of cancer. Thus, this application provides for a novel method of treating cancer by inhibiting Smad3 signaling, such as through administration of SIS3, an inhibitor of Smad3. Further provided are compositions and kits useful for treating cancer by way of inhibiting Smad3 signaling.Type: GrantFiled: March 8, 2016Date of Patent: June 6, 2023Assignee: The Chinese Universitv of Hong KongInventor: Hui Yao Lan
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Patent number: 11649236Abstract: The present invention provides a compound represented by Formula (I): wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.Type: GrantFiled: May 30, 2019Date of Patent: May 16, 2023Assignee: SHIONOGI & CO., LTD.Inventors: Yoshiyuki Taoda, Yuto Unoh
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Patent number: 11413292Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, Z, R1 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.Type: GrantFiled: February 11, 2019Date of Patent: August 16, 2022Assignee: Merck, Sharp & Dohme LLCInventors: Mark W. Embrey, Timothy John Hartingh, Marc Labroli, Izzat T. Raheem
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Patent number: 11306106Abstract: The present invention provides a pharmaceutical composition containing the following compound having antiviral action: wherein each of the symbols is defined in the specification.Type: GrantFiled: July 24, 2020Date of Patent: April 19, 2022Assignee: Shionogi & Co., Ltd.Inventor: Makoto Kawai
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Patent number: 11286262Abstract: The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.Type: GrantFiled: October 5, 2018Date of Patent: March 29, 2022Assignee: SHIONOGI & CO., LTD.Inventors: Kazuya Okamoto, Tatsuhiko Ueno
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Patent number: 11104682Abstract: The present application provides salt forms of N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-(pyridin-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide and N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamide, which are useful as inhibitors of TAM kinases, as well as processes and intermediates related thereto.Type: GrantFiled: March 19, 2020Date of Patent: August 31, 2021Assignee: Incyte CorporationInventors: Zhongjiang Jia, Yongzhong Wu, Yongchun Pan, Jiacheng Zhou, Qun Li
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Patent number: 11040981Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat cancer.Type: GrantFiled: October 9, 2018Date of Patent: June 22, 2021Assignee: Syros Pharmaceuticals, Inc.Inventors: David Moebius, Jason J. Marineau, Yi Zhang, Claudio Edmundo Chuaqui, Goran Malojcic, William Sinko, Huiping Amy Guan, Stephane Ciblat, Clint James, Amandine Xolin, Sylvain Bernard, Malay Doshi
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Patent number: 10759814Abstract: The present invention provides a pharmaceutical composition containing the following compound having antiviral action: wherein each of the symbols is defined in the specification.Type: GrantFiled: August 9, 2017Date of Patent: September 1, 2020Assignee: SHIONOGI & CO., LTD.Inventor: Makoto Kawai
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Patent number: 10633397Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.Type: GrantFiled: December 17, 2018Date of Patent: April 28, 2020Assignee: SHIONOGI & CO., LTD.Inventor: Makoto Kawai
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Patent number: 10329295Abstract: The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.Type: GrantFiled: March 7, 2016Date of Patent: June 25, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Jongwon Lim, Michael D. Altman, Jason D. Brubaker, Craig R. Gibeau
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Patent number: 10294241Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.Type: GrantFiled: April 27, 2016Date of Patent: May 21, 2019Assignee: SHIONOGI & CO., LTD.Inventor: Makoto Kawai
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Patent number: 10000496Abstract: Compounds and compositions useful for treating disorders related to KIT and PDGFR are described herein.Type: GrantFiled: July 22, 2016Date of Patent: June 19, 2018Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Kevin J. Wilson, Yulian Zhang
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Patent number: 9994575Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.Type: GrantFiled: October 20, 2015Date of Patent: June 12, 2018Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
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Patent number: 9944651Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.Type: GrantFiled: April 4, 2017Date of Patent: April 17, 2018Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
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Patent number: 9598416Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: GrantFiled: December 11, 2012Date of Patent: March 21, 2017Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marie-Pierre Collin, Dirk Brohm, Mélanie Héroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
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Patent number: 9475815Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: GrantFiled: February 20, 2013Date of Patent: October 25, 2016Assignee: BAYER INTELLETUAL PROPERTY GMBHInventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Voehringer, Niels Lindner
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Patent number: 9469638Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: GrantFiled: November 7, 2014Date of Patent: October 18, 2016Assignee: SHIONOGI & CO., LTD.Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Patent number: 9403834Abstract: A compound of formula (I), wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: March 10, 2014Date of Patent: August 2, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Srinivasu Pothukanuri
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Patent number: 9388189Abstract: New pyrrolotriazinone derivatives having the chemical structure of Formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).Type: GrantFiled: October 15, 2013Date of Patent: July 12, 2016Assignee: Almirall, S.A.Inventors: Montserrat Erra Sola, Marta Carrascal Riera, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Francisco Javier Bernal Anchuela, Lluis Miquel Pages Santacana, Marta Mir Cepeda, Gaspar Casals Coll, Maria Begoña Hernandez Olasagarre
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Patent number: 9340547Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).Type: GrantFiled: April 26, 2012Date of Patent: May 17, 2016Assignee: Almirall, S.A.Inventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Taltavull Moll, Montserrat Erra Sola
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Patent number: 9206184Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: GrantFiled: December 14, 2012Date of Patent: December 8, 2015Assignee: BAYER INTELLECTUAL PROPERTY GmbHInventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer
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Patent number: 9050345Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: March 7, 2014Date of Patent: June 9, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Kavitha Govindrajulu, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
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Patent number: 9040691Abstract: This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.Type: GrantFiled: June 26, 2012Date of Patent: May 26, 2015Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jürgen Klar, Verena Vöhringer, Joachim Telser, Mario Lobell, Frank Süβmeier, Volkhart Min-Jian Li, Michael Böttger, Stefan Golz, Dieter Lang, Karl-Heinz Schlemmer, Thomas Schlange, Andreas Schall, Wenlang Fu
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Publication number: 20150141423Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.Type: ApplicationFiled: June 4, 2013Publication date: May 21, 2015Applicant: Syngenta Participations AGInventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
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Patent number: 9034485Abstract: The present invention relates to compounds of the formula (1) and to the use thereof in organic electronic devices, and to organic electronic devices which comprise compounds of the formula (1), preferably as hole-transport materials and/or as emitting materials.Type: GrantFiled: December 22, 2009Date of Patent: May 19, 2015Assignee: Merck Patent GmbHInventors: Arne Buesing, Holger Heil, Philipp Stoessel, Amir Hossain Parham, Rocco Fortte, Jonas Valentin Kroeber
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Publication number: 20150133453Abstract: Compounds of the formula I in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.Type: ApplicationFiled: April 6, 2013Publication date: May 14, 2015Applicant: Merck Patent GmbHInventors: Dieter Dorsch, Hans-Peter Buchstaller
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Publication number: 20150111854Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: December 5, 2014Publication date: April 23, 2015Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
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Publication number: 20150111887Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.Type: ApplicationFiled: October 15, 2014Publication date: April 23, 2015Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
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Publication number: 20150099752Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).Type: ApplicationFiled: April 26, 2012Publication date: April 9, 2015Applicant: ALMIRALL, SAInventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Tal Tavul Moll, Montserat Eraa Sola
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Publication number: 20150094309Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: December 18, 2014Publication date: April 2, 2015Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Patent number: 8987441Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.Type: GrantFiled: September 21, 2011Date of Patent: March 24, 2015Assignee: Shionogi & Co., Ltd.Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
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Publication number: 20150080371Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: ApplicationFiled: December 11, 2012Publication date: March 19, 2015Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
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Publication number: 20150065485Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20150031676Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: ApplicationFiled: February 20, 2013Publication date: January 29, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Vöhringer, Niels Lindner
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Publication number: 20150031876Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: September 5, 2014Publication date: January 29, 2015Applicant: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Patent number: 8940412Abstract: An organic electroluminescence device and a material for producing the organic electroluminescence device. The organic electroluminescence device includes an organic thin film layer between a cathode and an anode, the organic thin film layer including one or more layers, in which the organic thin film layer includes one or more light emitting layers and at least one of the light emitting layers includes a phosphorescent material and a host material. The host material has an essential structure in which a naphthalene ring is bonded to a fluorene skeleton, dibenzofuran skeleton, or dibenzothiophene skeleton. The organic electroluminescence device is a phosphorescent device having high efficiency and long lifetime.Type: GrantFiled: December 22, 2009Date of Patent: January 27, 2015Assignee: Idemitsu Kosan Co., Ltd.Inventors: Yoriyuki Takashima, Toshihiro Iwakuma, Toshinari Ogiwara, Chishio Hosokawa, Mitsunori Ito
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Patent number: 8937175Abstract: The invention relates to novel compounds as ligands for transition metal complexes and materials made thereof that can be used, for example, as emitters in organic light-emitting electrochemical cells (OLEECs). According to the invention, non-fluorinated electron-poor emitter materials are disclosed for the first time that can be used in organic light-emitting electrochemical cells.Type: GrantFiled: May 31, 2011Date of Patent: January 20, 2015Assignee: Osram GmbHInventors: Andreas Kanitz, Daniel Stark
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Patent number: 8927710Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: GrantFiled: June 14, 2010Date of Patent: January 6, 2015Assignee: Shionogi & Co., Ltd.Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20140378305Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: SYNGENTA LIMITEDInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Patent number: 8916598Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: August 11, 2011Date of Patent: December 23, 2014Assignee: Proteotech IncInventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow
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Publication number: 20140336173Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: ApplicationFiled: December 10, 2012Publication date: November 13, 2014Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
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Patent number: 8865623Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: GrantFiled: January 6, 2010Date of Patent: October 21, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20140256719Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.Type: ApplicationFiled: March 7, 2014Publication date: September 11, 2014Inventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Kavitha Govindrajulu, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
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Patent number: 8829185Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.Type: GrantFiled: March 7, 2012Date of Patent: September 9, 2014Assignee: Bayer HealthCare LLCInventors: Julie A. Dixon, Steven Magnuson, Barton Phillips, Yamin Wang, Tindy Li, Kyle Parcella, Jason Newcom, Harold C. E. Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Kristen M. Allegue, Zhen Liu
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Patent number: 8815417Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.Type: GrantFiled: August 16, 2011Date of Patent: August 26, 2014Assignee: Samsung Display Co., Ltd.Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
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Patent number: 8802675Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.Type: GrantFiled: January 31, 2010Date of Patent: August 12, 2014Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
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Publication number: 20140221377Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Publication number: 20140221333Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 19, 2012Publication date: August 7, 2014Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro