1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
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Patent number: 12084435Abstract: The present disclosure provides an herbicidal compound according to Formula I, which is a pyridine ring-substituted pyridazinol compound, as well as derivatives of the compound, an herbicidal composition comprising the compound, preparation methods thereof, and applications thereof.Type: GrantFiled: September 13, 2018Date of Patent: September 10, 2024Assignee: Qingdao Kingagroot Chemical Compound Co., Ltd.Inventors: Lei Lian, Yurong Zheng, Rongbao Hua, Jianfeng Wang, Xuegang Peng, Qi Cui
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Patent number: 11993599Abstract: The present disclosure relates to compounds and salts thereof that are useful for modulating target polypeptides and proteins, in particular BRM. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various BRM-mediated and/or BRG1-mediated diseases or disorders.Type: GrantFiled: August 8, 2022Date of Patent: May 28, 2024Assignee: GENENTECH, INC.Inventors: Elisia Villemure, Joachim Rudolph, Mingshuo Zeng
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Patent number: 11771697Abstract: The present invention relates to compounds, compositions and methods for treating diseases or conditions mediated by proteins of the SWI/SNF chromatin-remodeling complex, including PB1.Type: GrantFiled: April 30, 2019Date of Patent: October 3, 2023Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Eric Fischer, Nathanael Gray, Radoslaw Nowak, Katherine Donovan, Tinghu Zhang, Yao Liu
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Patent number: 11672799Abstract: The present invention provides a compound of formula IA or a pharmaceutically acceptable salt thereof; 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: GrantFiled: January 28, 2019Date of Patent: June 13, 2023Assignee: NOVARTIS AGInventors: Atwood Kim Cheung, Natalie Dales, Timothy Brian Hurley
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Patent number: 11566020Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.Type: GrantFiled: April 12, 2021Date of Patent: January 31, 2023Assignee: Ribon Therapeutics, Inc.Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
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Patent number: 11254643Abstract: The present invention provides, inter alia, a process for producing a compound of Formula (I): wherein A1, R1, R2, R3, R4, R5 and R6 are as defined herein. The present invention further provides intermediate compounds utilised in said process, and methods for producing said intermediate compounds.Type: GrantFiled: October 16, 2018Date of Patent: February 22, 2022Assignee: Syngenta Participations AGInventors: Helmars Smits, Denis Gribkov, Edouard Godineau, Christopher Charles Scarborough, Alan James Robinson, Michael Christian Dieckmann
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Patent number: 11254653Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.Type: GrantFiled: May 15, 2020Date of Patent: February 22, 2022Assignee: Novartis AGInventors: Christopher Farady, Nina Gommermann, Philipp Janser, Angela Mackay, Henri Mattes, Nichola Smith, Catherine Fooks Solovay, Nikolaus Johannes Stiefl, Eric Vangrevelinghe, Juraj Velcicky, Anette von Matt
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Patent number: 11208399Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.Type: GrantFiled: May 15, 2020Date of Patent: December 28, 2021Assignee: Novartis AGInventors: Christopher Farady, Nina Gommermann, Philipp Janser, Angela Mackay, Henri Mattes, Nichola Smith, Catherine Fooks Solovay, Nikolaus Johannes Stiefl, Eric Vangrevelinghe, Juraj Velcicky, Anette von Matt
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Patent number: 11014913Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.Type: GrantFiled: August 11, 2020Date of Patent: May 25, 2021Assignee: Ribon Therapeutics, Inc.Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
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Patent number: 10961226Abstract: The present invention relates to a process for the purification of pyrazolpyridazines of formula I wherein the variables are as defined in the specification, by adding HCl to a solution of the pyrazolpyridazine in an inert solvent under non-aqueous conditions, effecting crystallization of the HCl-salt, isolating the resulting precipitate.Type: GrantFiled: October 27, 2017Date of Patent: March 30, 2021Assignee: BASF SEInventors: Eric George Klauber, Birgit Gockel, Sebastian Soergel, Roland Goetz, Henricus Maria Martinus Bastiaans, Jochen Dietz, Joachim Gebhardt
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Patent number: 10899734Abstract: The present disclosure relates to chemical compounds that modulate pantothenate kinase (PanK) activity for the treatment of metabolic disorders (such as diabetes mellitus type II), neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment. 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: GrantFiled: June 23, 2017Date of Patent: January 26, 2021Assignee: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, INC.Inventors: Lalit Kumar Sharma, Richard E. Lee, Charles O. Rock, Suzanne Jackowski, Mi Kyung Yun, Chitra Subramanian, Jiuyu Liu
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Patent number: 10870641Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.Type: GrantFiled: October 24, 2019Date of Patent: December 22, 2020Assignee: Ribon Therapeutics, Inc.Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
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Patent number: 10710978Abstract: The application relates to compounds of Formula (I?): which modulate the activity of a kinase (e.g., STK4), a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of a kinase, such as STK4.Type: GrantFiled: March 31, 2016Date of Patent: July 14, 2020Assignees: DANA-FARBER CANCER INSTITUTE, INC., FONDAZIONE CENTRO SAN RAFFAELEInventors: Nathanael S. Gray, Sara Buhrlage, Kenneth Anderson, Francesca Cottini, Giovanni Tonon
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Patent number: 10662157Abstract: A compound of formula (I), or an N-oxide thereof is provided. In the compound of formula (I), Het1 represents Het1-1, Het1-2, Het1-3, Het1-4, Het1-5, Het1-6, Het1-7, Het1-8, or Het1-9, and the remaining variable groups are as defined in the specification. The compound of formula (I), or N-oxide thereof has a superior effect in controlling arthropod pests.Type: GrantFiled: March 27, 2017Date of Patent: May 26, 2020Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Kohei Orimoto, Takamasa Tanabe, Yoshihiko Nokura, Yuji Nakajima
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Patent number: 10550105Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.Type: GrantFiled: April 29, 2019Date of Patent: February 4, 2020Assignee: Ribon Therapeutics Inc.Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
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Patent number: 10492495Abstract: An agrochemical composition contains a component (A): a compound represented by formula (I) (wherein, R1, R2, R3a, R3b, R4a, R4b, and R5 each independently represents an unsubstituted or substituted C1-6 alkyl group or the like, n represents an integer of 0 to 4, o and p each independently represents an integer of 2 to 4, and X represents a carbon atom or a nitrogen atom) or a salt thereof, and a component (B): a hydrolysis inhibitor.Type: GrantFiled: February 12, 2016Date of Patent: December 3, 2019Assignee: Nippon Soda Co., Ltd.Inventors: Tetsutaro Kai, Eriko Okada, Takahiro Maekawa
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Patent number: 10370366Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:Type: GrantFiled: October 6, 2017Date of Patent: August 6, 2019Assignee: Flatley Discovery Lab, LLCInventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
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Patent number: 10292970Abstract: The present application relates to novel heteroaryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: November 30, 2015Date of Patent: May 21, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros Vakalopoulos, Damian Brockschnieder, Frank Wunder, Johannes-Peter Stasch, Tobias Marquardt, Lisa Dietz, Volkhart Min-Jian Li
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Patent number: 10294256Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.Type: GrantFiled: December 12, 2017Date of Patent: May 21, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Michael G. Yang, Zili Xiao, John V. Duncia, David S. Weinstein
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Patent number: 10280145Abstract: A compound has inhibitory activity on Discoidin Domain Receptor 1. A urea derivative is represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein, R1 is trifluoromethyl, trifluoromethoxy, or pentafluorosulfanyl; each R2 is independently a hydrogen atom or methyl which is optionally substituted by one hydroxyl or one saturated heterocyclyl having four to six ring-forming atoms; R3 is a hydrogen atom, halogen atom, C1-C3 alkyl, saturated heterocyclyl having four to six ring-forming atoms and optionally having an oxo group, or R5O—; and R4 is phenyl, pyridyl, pyridazinyl, or pyrimidinyl, which phenyl, pyridyl, pyridazinyl, or pyrimidinyl is optionally substituted by one R6.Type: GrantFiled: August 31, 2016Date of Patent: May 7, 2019Assignee: Toray Industries, Inc.Inventors: Yukihiro Nishio, Yuko Kubota, Masashi Yamamoto, Yutaka Nishimura, Tomohide Masuda, Hideyuki Tsutsui, Keiichi Okimura, Syuji Udagawa, Mie Kaino, Hiroyuki Meguro, Yumiko Sekiya
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Patent number: 10246469Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.Type: GrantFiled: September 29, 2016Date of Patent: April 2, 2019Assignees: Bristol-Myers Squibb Company, Syngene International Limited, Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Ling Chen, Jonathan L. Ditta, Carolyn Diane Dzierba, Prasada Rao Jalagam, Guanglin Luo, John E. Macor, Tarun Kumar Maishal, Susheel Jethanand Nara, Ramkumar Rajamani, Ramesh Kumar Sistla, Soodamani Thangavel
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Patent number: 10214520Abstract: The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the ? opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: GrantFiled: July 14, 2015Date of Patent: February 26, 2019Assignee: GRUENENTHAL GMBHInventors: Anita Wegert, Sven Kuehnert, Rene Michael Koenigs, Bert Nolte, Klaus Linz, Stephanie Harlfinger, Babette-Yvonne Koegel, Paul Ratcliffe, Fritz Theil, Olga Groeger, Birgit Braun
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Patent number: 9951025Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.Type: GrantFiled: March 17, 2014Date of Patent: April 24, 2018Assignee: VERSEON CORPORATIONInventors: Kevin Michael Short, Son Minh Pham, David Charles Williams
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Patent number: 9902722Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.Type: GrantFiled: April 1, 2015Date of Patent: February 27, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Ling Chen, Carolyn Diane Dzierba, Jonathan L. Ditta, John E. Macor, Joanne J. Bronson
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Patent number: 9856249Abstract: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4-h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.Type: GrantFiled: September 10, 2015Date of Patent: January 2, 2018Assignee: Celtaxsys, Inc.Inventor: William Guilford
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Patent number: 9849131Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.Type: GrantFiled: November 10, 2016Date of Patent: December 26, 2017Assignee: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
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Patent number: 9790215Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:Type: GrantFiled: March 13, 2014Date of Patent: October 17, 2017Assignee: FLATLEY DISCOVERY LAB, LLCInventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
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Patent number: 9783529Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:Type: GrantFiled: March 13, 2014Date of Patent: October 10, 2017Assignee: FLATLEY DISCOVERY LAB, LLCInventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
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Patent number: 9783525Abstract: The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38? MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising administration of MAP kinase inhibitors or compositions comprising MAP kinase inhibitors. In some embodiments, the disease is Alzheimer's Disease, ALS, Huntington's Disease or Parkinson's Disease.Type: GrantFiled: September 15, 2015Date of Patent: October 10, 2017Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, NORTHWESTERN UNIVERSITYInventors: Ottavio Arancio, Daniel Martin Watterson, Jeffrey Claude Pelletier, Saktimayee Mitra Roy
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Patent number: 9682969Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:Type: GrantFiled: January 19, 2015Date of Patent: June 20, 2017Assignee: Flatley Discovery Lab, LLCInventor: Bridget M. Cole
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Patent number: 9657010Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.Type: GrantFiled: October 31, 2013Date of Patent: May 23, 2017Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy
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Patent number: 9598446Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.Type: GrantFiled: February 25, 2015Date of Patent: March 21, 2017Assignee: ACHILLION PHARMACEUTICALS, INC.Inventors: Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Jason Allan Wiles, Avinash S. Phadke
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Patent number: 9512089Abstract: 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: GrantFiled: August 13, 2014Date of Patent: December 6, 2016Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 9308205Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.Type: GrantFiled: January 29, 2015Date of Patent: April 12, 2016Assignee: MERCK PATENT GMBHInventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
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Patent number: 9303026Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: December 20, 2013Date of Patent: April 5, 2016Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY. LTD.Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 9296724Abstract: Pyridazine derivatives (e.g., Formula I) have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: GrantFiled: April 9, 2014Date of Patent: March 29, 2016Assignee: Xcovery Holding Company LLCInventors: Congxin Liang, Zhigang Li
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Patent number: 9206171Abstract: This invention relates to antiviral agents, in particular to salts useful in the treatment of infections caused by Picornaviridae, such as human rhinovirus (HRV) and methods for their preparation. In one embodiment, the invention relates to a bis-dihydrogenphophate salt having the formula: The invention also relates to the use of these salts in the treatment of picornavirus infections. The salts of this invention are especially suitable for use in the treatment of HRV, however it is to be understood that the invention is also applicable to other viruses of the picornavirus family.Type: GrantFiled: September 10, 2013Date of Patent: December 8, 2015Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: Jane Ryan, Margaret Anne Butt
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Patent number: 9145372Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.Type: GrantFiled: November 15, 2011Date of Patent: September 29, 2015Assignee: AGENEBIO, INC.Inventor: John A. Lowe, III
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Patent number: 9090565Abstract: This invention relates to 1-pyridazinyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: November 13, 2012Date of Patent: July 28, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
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Patent number: 9040534Abstract: 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: GrantFiled: March 14, 2014Date of Patent: May 26, 2015Assignee: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
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Patent number: 9040692Abstract: 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: GrantFiled: March 11, 2014Date of Patent: May 26, 2015Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
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Patent number: 9040537Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkylType: GrantFiled: March 23, 2011Date of Patent: May 26, 2015Assignee: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20150141399Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: ApplicationFiled: February 5, 2015Publication date: May 21, 2015Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20150141433Abstract: 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: ApplicationFiled: September 26, 2014Publication date: May 21, 2015Inventors: David R. Anderson, Robert A. Volkmann
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Patent number: 9034874Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.Type: GrantFiled: July 17, 2013Date of Patent: May 19, 2015Assignee: NOVARTIS AGInventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
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Patent number: 9035049Abstract: The present invention relates to novel herbicidal compounds of Formula (I), or an agronomically acceptable salt of said compound wherein R1, R2, A1, Ra, Rb, Rc and Rd are as defined herein. The invention further relates to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: GrantFiled: April 4, 2012Date of Patent: May 19, 2015Assignee: Syngenta LimitedInventor: Jonathan Dallimore
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Patent number: 9034873Abstract: The present disclosure describes compounds of the following formula in which: the groups A, which may be identical or different, represent a group n is an integer equal to 1 or 2, Y represents an oxygen or sulfur atom, a methylene, hydroxymethylene, carbonyl or thiocarbonyl group, or a group of formula the groups R, which may be identical or different, represent a hydrogen, an alkyl, alkylamine, hydroxyl-alkyl or alkyloxy chain containing from 1 to 6 carbons, or a —COOH, —CONH2, —COOR2 or —CONHR2 group in which R2 is an alkyl chain containing from 1 to 6 carbons, or, when the substituents R are identical in the 2-pyridinyl groups, the substituents R2 may together form an ethereal cyclic alkyl chain, with the exception of the compounds: 2,6-di[5-(2-pyridyl)pyrrol-2-yl]pyridine and bis[5-(6-methyl-2-pyridyl)pyrrol-2-yl]methane.Type: GrantFiled: July 26, 2007Date of Patent: May 19, 2015Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Didier Max Dubreuil, Muriel Genevieve Pipelier, Jean-Paul Pradere, Hicham Bakkali, Patrice Lepape, Thierry Delaunay, Alexandra Tabatchnik
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Publication number: 20150133425Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 17, 2013Publication date: May 14, 2015Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
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Publication number: 20150133429Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: ApplicationFiled: January 14, 2015Publication date: May 14, 2015Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Publication number: 20150133422Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.Type: ApplicationFiled: November 8, 2013Publication date: May 14, 2015Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose