1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • Patent number: 12084435
    Abstract: 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: Grant
    Filed: September 13, 2018
    Date of Patent: September 10, 2024
    Assignee: Qingdao Kingagroot Chemical Compound Co., Ltd.
    Inventors: Lei Lian, Yurong Zheng, Rongbao Hua, Jianfeng Wang, Xuegang Peng, Qi Cui
  • Patent number: 11993599
    Abstract: 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: Grant
    Filed: August 8, 2022
    Date of Patent: May 28, 2024
    Assignee: GENENTECH, INC.
    Inventors: Elisia Villemure, Joachim Rudolph, Mingshuo Zeng
  • Patent number: 11771697
    Abstract: 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: Grant
    Filed: April 30, 2019
    Date of Patent: October 3, 2023
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Eric Fischer, Nathanael Gray, Radoslaw Nowak, Katherine Donovan, Tinghu Zhang, Yao Liu
  • Patent number: 11672799
    Abstract: 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: Grant
    Filed: January 28, 2019
    Date of Patent: June 13, 2023
    Assignee: NOVARTIS AG
    Inventors: Atwood Kim Cheung, Natalie Dales, Timothy Brian Hurley
  • Patent number: 11566020
    Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
    Type: Grant
    Filed: April 12, 2021
    Date of Patent: January 31, 2023
    Assignee: Ribon Therapeutics, Inc.
    Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
  • Patent number: 11254643
    Abstract: 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: Grant
    Filed: October 16, 2018
    Date of Patent: February 22, 2022
    Assignee: Syngenta Participations AG
    Inventors: Helmars Smits, Denis Gribkov, Edouard Godineau, Christopher Charles Scarborough, Alan James Robinson, Michael Christian Dieckmann
  • Patent number: 11254653
    Abstract: 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: Grant
    Filed: May 15, 2020
    Date of Patent: February 22, 2022
    Assignee: Novartis AG
    Inventors: 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
  • Patent number: 11208399
    Abstract: 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: Grant
    Filed: May 15, 2020
    Date of Patent: December 28, 2021
    Assignee: Novartis AG
    Inventors: 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
  • Patent number: 11014913
    Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
    Type: Grant
    Filed: August 11, 2020
    Date of Patent: May 25, 2021
    Assignee: Ribon Therapeutics, Inc.
    Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
  • Patent number: 10961226
    Abstract: 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: Grant
    Filed: October 27, 2017
    Date of Patent: March 30, 2021
    Assignee: BASF SE
    Inventors: Eric George Klauber, Birgit Gockel, Sebastian Soergel, Roland Goetz, Henricus Maria Martinus Bastiaans, Jochen Dietz, Joachim Gebhardt
  • Patent number: 10899734
    Abstract: 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: Grant
    Filed: June 23, 2017
    Date of Patent: January 26, 2021
    Assignee: 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
  • Patent number: 10870641
    Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
    Type: Grant
    Filed: October 24, 2019
    Date of Patent: December 22, 2020
    Assignee: Ribon Therapeutics, Inc.
    Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
  • Patent number: 10710978
    Abstract: 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: Grant
    Filed: March 31, 2016
    Date of Patent: July 14, 2020
    Assignees: DANA-FARBER CANCER INSTITUTE, INC., FONDAZIONE CENTRO SAN RAFFAELE
    Inventors: Nathanael S. Gray, Sara Buhrlage, Kenneth Anderson, Francesca Cottini, Giovanni Tonon
  • Patent number: 10662157
    Abstract: 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: Grant
    Filed: March 27, 2017
    Date of Patent: May 26, 2020
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kohei Orimoto, Takamasa Tanabe, Yoshihiko Nokura, Yuji Nakajima
  • Patent number: 10550105
    Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: February 4, 2020
    Assignee: Ribon Therapeutics Inc.
    Inventors: Melissa Marie Vasbinder, Laurie B. Schenkel, Kerren Kalai Swinger, Kevin Wayne Kuntz
  • Patent number: 10492495
    Abstract: 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: Grant
    Filed: February 12, 2016
    Date of Patent: December 3, 2019
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Tetsutaro Kai, Eriko Okada, Takahiro Maekawa
  • Patent number: 10370366
    Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:
    Type: Grant
    Filed: October 6, 2017
    Date of Patent: August 6, 2019
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • Patent number: 10292970
    Abstract: 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: Grant
    Filed: November 30, 2015
    Date of Patent: May 21, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros Vakalopoulos, Damian Brockschnieder, Frank Wunder, Johannes-Peter Stasch, Tobias Marquardt, Lisa Dietz, Volkhart Min-Jian Li
  • Patent number: 10294256
    Abstract: 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: Grant
    Filed: December 12, 2017
    Date of Patent: May 21, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael G. Yang, Zili Xiao, John V. Duncia, David S. Weinstein
  • Patent number: 10280145
    Abstract: 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: Grant
    Filed: August 31, 2016
    Date of Patent: May 7, 2019
    Assignee: 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
  • Patent number: 10246469
    Abstract: 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: Grant
    Filed: September 29, 2016
    Date of Patent: April 2, 2019
    Assignees: Bristol-Myers Squibb Company, Syngene International Limited, Bristol-Myers Squibb Company
    Inventors: 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
  • Patent number: 10214520
    Abstract: 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: Grant
    Filed: July 14, 2015
    Date of Patent: February 26, 2019
    Assignee: GRUENENTHAL GMBH
    Inventors: Anita Wegert, Sven Kuehnert, Rene Michael Koenigs, Bert Nolte, Klaus Linz, Stephanie Harlfinger, Babette-Yvonne Koegel, Paul Ratcliffe, Fritz Theil, Olga Groeger, Birgit Braun
  • Patent number: 9951025
    Abstract: 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: Grant
    Filed: March 17, 2014
    Date of Patent: April 24, 2018
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams
  • Patent number: 9902722
    Abstract: 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: Grant
    Filed: April 1, 2015
    Date of Patent: February 27, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Ling Chen, Carolyn Diane Dzierba, Jonathan L. Ditta, John E. Macor, Joanne J. Bronson
  • Patent number: 9856249
    Abstract: 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: Grant
    Filed: September 10, 2015
    Date of Patent: January 2, 2018
    Assignee: Celtaxsys, Inc.
    Inventor: William Guilford
  • Patent number: 9849131
    Abstract: 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: Grant
    Filed: November 10, 2016
    Date of Patent: December 26, 2017
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Patent number: 9790215
    Abstract: 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: Grant
    Filed: March 13, 2014
    Date of Patent: October 17, 2017
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • Patent number: 9783529
    Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: October 10, 2017
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • Patent number: 9783525
    Abstract: 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: Grant
    Filed: September 15, 2015
    Date of Patent: October 10, 2017
    Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, NORTHWESTERN UNIVERSITY
    Inventors: Ottavio Arancio, Daniel Martin Watterson, Jeffrey Claude Pelletier, Saktimayee Mitra Roy
  • Patent number: 9682969
    Abstract: 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: Grant
    Filed: January 19, 2015
    Date of Patent: June 20, 2017
    Assignee: Flatley Discovery Lab, LLC
    Inventor: Bridget M. Cole
  • Patent number: 9657010
    Abstract: 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: Grant
    Filed: October 31, 2013
    Date of Patent: May 23, 2017
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy
  • Patent number: 9598446
    Abstract: 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: Grant
    Filed: February 25, 2015
    Date of Patent: March 21, 2017
    Assignee: 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
  • Patent number: 9512089
    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: Grant
    Filed: August 13, 2014
    Date of Patent: December 6, 2016
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 9308205
    Abstract: 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: Grant
    Filed: January 29, 2015
    Date of Patent: April 12, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Patent number: 9303026
    Abstract: 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: Grant
    Filed: December 20, 2013
    Date of Patent: April 5, 2016
    Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY. LTD.
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Patent number: 9296724
    Abstract: 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: Grant
    Filed: April 9, 2014
    Date of Patent: March 29, 2016
    Assignee: Xcovery Holding Company LLC
    Inventors: Congxin Liang, Zhigang Li
  • Patent number: 9206171
    Abstract: 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: Grant
    Filed: September 10, 2013
    Date of Patent: December 8, 2015
    Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: Jane Ryan, Margaret Anne Butt
  • Patent number: 9145372
    Abstract: 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: Grant
    Filed: November 15, 2011
    Date of Patent: September 29, 2015
    Assignee: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • Patent number: 9090565
    Abstract: 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: Grant
    Filed: November 13, 2012
    Date of Patent: July 28, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Patent number: 9040692
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 26, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Patent number: 9040537
    Abstract: 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-alkyl
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 26, 2015
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
  • Publication number: 20150141399
    Abstract: 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: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: 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
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Patent number: 9034874
    Abstract: 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: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: 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
  • Patent number: 9035049
    Abstract: 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: Grant
    Filed: April 4, 2012
    Date of Patent: May 19, 2015
    Assignee: Syngenta Limited
    Inventor: Jonathan Dallimore
  • Patent number: 9034873
    Abstract: 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: Grant
    Filed: July 26, 2007
    Date of Patent: May 19, 2015
    Assignee: 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
  • Publication number: 20150133425
    Abstract: 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: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: 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
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Publication number: 20150133422
    Abstract: 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: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose