1,2,4-triazoles (including Hydrogenated) Patents (Class 546/272.4)
  • Patent number: 11180461
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Grant
    Filed: February 7, 2020
    Date of Patent: November 23, 2021
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Patent number: 10829475
    Abstract: The present invention provides efinaconazole producing and purifying methods adapted to industrial scale that provide high-purity efinaconazole in high yield by simple operations using specific impurities as indices. The efinaconazole producing method comprises: step A of forming a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene in a volume (L) which is 2 to 5 times the mass (kg) of compound (II); step B of subjecting the toluene solution to reaction under heating; step C of washing the reaction mixture from step B to obtain a toluene solution of crude efinaconazole in which the residual amount of 4-MP is not more than 5 wt % of efinaconazole.
    Type: Grant
    Filed: February 19, 2020
    Date of Patent: November 10, 2020
    Assignee: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Masahito Watanabe, Takeshi Kanayama
  • Patent number: 10787431
    Abstract: Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(5-mercapto-1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: September 29, 2020
    Assignee: Dow AgroSciences LLC
    Inventors: Nicholas R. Babij, Qiang Yang, Sarah Ryan, Yan Hao, Gary Roth, Kaitlyn Gray
  • Patent number: 10604490
    Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: March 31, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Brandon Heath Brown, Troy Evan Reynolds
  • Patent number: 10344016
    Abstract: Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: July 9, 2019
    Assignee: AMGEN INC.
    Inventors: Paul John Dransfield, Zice Fu, Julie Anne Heath, Jeffrey T. Mihalic, Vatee Pattaropong
  • Patent number: 10160730
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: December 25, 2018
    Assignee: Autifony Therapeutics Limited
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Patent number: 9598395
    Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: March 21, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Richard A. Gatti, Liutao Du, Hailiang Hu, Robert Damoiseaux, Michael E. Jung, Jin-Mo Ku, Gladys Completo
  • Patent number: 9422252
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: August 23, 2016
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Patent number: 9394278
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: July 19, 2016
    Assignee: Ixchelsis Limited
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Patent number: 9150539
    Abstract: The retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-I) and type-2 (HIV-2), have been etiologically linked to the immunosuppressive disease known as acquired immunodeficiency syndrome (AIDS). HIV seropositive individuals are initially asymptomatic but typically develop AIDS related complex (ARC) followed by AIDS. Affected individuals exhibit severe immunosuppression which makes them highly susceptible to debilitating and ultimately fatal opportunistic infections. The invention is directed to a novel crystalline form of the RT inhibitor 3-chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl)oxy)benzonitrile used in the treatment HIV infection and AIDS.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: October 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Courtney K. Maguire
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20150119249
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)pyridin-3-yl-carboxamides of formula I and their use as herbicides, formula I. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)pyridin-3-yl-carboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas R, R1, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Publication number: 20150119576
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Manabu YAOSAKA, Tomohisa UTSUNOMIYA, Yuji MORIYAMA, Tomohiro MATSUMOTO, Kazutaka MATOBA
  • Publication number: 20150111747
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150111750
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 23, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Publication number: 20150111910
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Application
    Filed: May 22, 2013
    Publication date: April 23, 2015
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Publication number: 20150087646
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 26, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8987311
    Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
  • Publication number: 20150080412
    Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.
    Type: Application
    Filed: March 7, 2013
    Publication date: March 19, 2015
    Applicant: INCEPTION 2, INC.
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
  • Publication number: 20150072959
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150072859
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 12, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Publication number: 20150065345
    Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R1, R2, X, R4, R5 and R7 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Applicant: SYNGENTA LIMITED
    Inventor: Glynn Mitchell
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8962529
    Abstract: The present invention relates to novel, herbicidally active picolinic acid derivatives of the formula (I) and to processes for preparation thereof. The present invention further provides for the use thereof as a herbicide, especially as a herbicide for selective control of weed plants in useful plant crops, and as a plant growth regulator alone or in combination with safeners and/or in a mixture with other herbicides.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: February 24, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Harmut Ahrens, Marco Brünjes, Hansjörg Dietrich, Elmar Gatzweiler, Isolde Häuser-Hahn, Stefan Lehr, Dirk Schmutzler
  • Publication number: 20150051251
    Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 19, 2015
    Applicant: The Regents of the University of California
    Inventors: Richard A. Gatti, Liutao Du, Hailiang Hu, Robert Damoiseaux, Michael E. Jung, Jin-Mo Ku, Gladys Completo
  • Publication number: 20150051203
    Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
  • Patent number: 8957216
    Abstract: Provided herein are compounds useful for kinase inhibition.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: February 17, 2015
    Assignee: Amitech Therapeutic Solutions, Inc.
    Inventors: Lee Daniel Arnold, Eric A. Murphy
  • Patent number: 8952042
    Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: February 10, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
  • Patent number: 8946236
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Patent number: 8946266
    Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter′, Sven Franciscus Anna Van Brandt, Michel Surkyn
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Publication number: 20150018332
    Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: January 15, 2015
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
  • Publication number: 20150011592
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: January 8, 2015
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20150011517
    Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 8, 2015
    Inventor: Feng Lu
  • Patent number: 8927729
    Abstract: Pesticidal compositions and their uses are disclosed.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: January 6, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
  • Patent number: 8927458
    Abstract: Triazolylpyridine ketones expressed by the following formula (1) and use thereof as herbicides.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 6, 2015
    Assignee: Bayer CropScience AG
    Inventors: Andreas Van Almsick, Shinichi Narabu, Yoshitaka Sato, Kei Domon, Koichi Araki, Shinichi Shirakura, Seiji Ukawa, Teruyuki Ichihara, Chieko Ueno
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140364408
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 8901309
    Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: December 2, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tatsuki Koike, Minoru Nakamura, Takafumi Takai, Yuichi Kajita, Makoto Kamata
  • Patent number: 8901308
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: December 2, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
  • Publication number: 20140342906
    Abstract: Tetrazol-5-yl- and triazol-5-yl-aryl compounds of the general formula (I) as herbicides are described. In this formula (I), X, Z, W and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B are N and CY. Q is cyanoalkylcarbonyl or isoxazolyl.
    Type: Application
    Filed: January 10, 2013
    Publication date: November 20, 2014
    Inventors: Ralf Braun, Lothar Willms, Ines Heinemann, Isolde Haeuser-Hahn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Patent number: 8889673
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: November 18, 2014
    Assignee: Genentech, Inc.
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Publication number: 20140315913
    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: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140296237
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
  • Publication number: 20140288301
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
  • Publication number: 20140275531
    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: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Patent number: 8835464
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin