Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
  • Patent number: 10351537
    Abstract: The present invention provides processes for the preparation of Lesinurad (1), as well as intermediates useful in the preparation thereof. In particular, the processes of the invention utilize novel intermediate compounds of Formulas (3) and (11), which provide improvements over the known processes for the preparation of Lesinurad (1).
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: July 16, 2019
    Assignee: Apotex Inc.
    Inventors: Prabhudas Bodhuri, Melanie R. A. Green, Avedis Karadeolian, Gamini Weeratunga, Boris Gorin
  • Patent number: 10336735
    Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: July 2, 2019
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Luke Lairson, Arnab K. Chatterjee, Michael Bollong, Baiyuan Yang, Peter G. Schultz
  • Patent number: 10323016
    Abstract: The present invention is directed to novel compounds of formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: June 18, 2019
    Assignees: UNIVERSITE DE LILLE 2 DROIT ET SANTE, INSTITUT PASTEUR DE LILLE, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)
    Inventors: Julie Charton, Benoit Deprez, Florence Leroux, Bart Staels, Anne Muhr-Tailleux, Nathalie Hennuyer, Sophie Lestavel, Manuel Lassalle, Barbara Dubanchet
  • Patent number: 9987208
    Abstract: 8-[2-(2-Pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) has an action to promote synthesis and regeneration of elastin, and is useful as an agent for the prophylaxis or improvement of wrinkles, and an anti-aging drug.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: June 5, 2018
    Assignee: Nishizaki Bioinformation Research Institute
    Inventors: Tomoyuki Nishizaki, Akito Tanaka
  • Patent number: 9931324
    Abstract: The present invention relates to indolizine compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: April 3, 2018
    Assignee: Merck Patent GmbH
    Inventors: Srinivasa R. Karra, Andreas Goutopoulos
  • Patent number: 9795137
    Abstract: The invention relates to co-crystals of metalaxyl and prothioconazole, to methods of making them, to compositions containing them and to the methods of using said co-crystals and said compositions to treat crops and plants.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: October 24, 2017
    Assignee: Bayer CropScience LP
    Inventor: David Frizzell
  • Patent number: 9781931
    Abstract: A composition for controlling plant diseases comprising a tetrazolinone compound represented by a formula (1): wherein n is an integer of any one of 0 to 5; R1 represents a halogen atom and the like; R2 represents a C1-C3 alkyl group and the like; the R1 or R2 can have independently halogen atom(s) in the alkyl moiety; with the proviso that when n is an integer of 2 or more, two or more of the R1 may be different from each other, and an carboxamide compound, preferably the composition for controlling plant diseases wherein a weight ratio of the tetrazolinone compound to the carboxamide compound is that of the tetrazolinone compound/the carboxamide compound=0.1/1 to 10/1, shows an excellent controlling efficacy on plant diseases.
    Type: Grant
    Filed: July 15, 2014
    Date of Patent: October 10, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Yuichi Matsuzaki
  • Patent number: 9655364
    Abstract: A composition for controlling plant diseases comprising a tetrazolinone compound represented by a formula (1): wherein n is an integer of any one of 0 to 5; R1 represents a halogen atom and the like; R2 represents a C1-C3 alkyl group and the like; the R1 or R2 can have independently halogen atom(s) in the alkyl moiety; with the proviso that when n is an integer of 2 or more, two or more of the R1 may be different from each other, and an QoI compound, preferably the composition for controlling plant diseases wherein a weight ratio of the tetrazolinone compound to the QoI compound is that of the tetrazolinone compound/the QoI compound=0.1/1 to 10/1, shows an excellent controlling efficacy on plant diseases.
    Type: Grant
    Filed: July 15, 2014
    Date of Patent: May 23, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Yuichi Matsuzaki
  • Patent number: 9487476
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: November 8, 2016
    Assignee: YALE UNIVERSITY
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 9445601
    Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: September 20, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stefan Dutzmann, Klaus Stenzel, Manfred Jautelat
  • Patent number: 9402827
    Abstract: Sodium 2-(5-bromo-4-(4-cyclopropyl-naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses such compositions for the treatment of a variety of diseases and conditions.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: August 2, 2016
    Assignee: ARDEA BIOSCIENCES, INC.
    Inventors: Jeffrey Miner, Jean-Luc Girardet, Barry D. Quart
  • Patent number: 9296710
    Abstract: The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, and generalized anxiety disorder.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: March 29, 2016
    Assignee: Eli Lilly and Company
    Inventors: Teresa Tse Ki Man, James Allen Monn, Carlos Montero Salgado, Lourdes Prieto, David Edward Tupper, Lesley Walton
  • Patent number: 9290461
    Abstract: There is disclosed a crystalline DMSO solvate of prothioconazole as well as amorphous prothioconazole. Methods for making these solid forms, microbicidal compositions comprising them and uses thereof are also disclosed.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: March 22, 2016
    Assignee: ADAMA MAKHTESHIM LTD
    Inventors: Sharona Zamir, Doron Mason, Inna Faktorovitch
  • Patent number: 9216179
    Abstract: Sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are described.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: December 22, 2015
    Assignee: ARDEA BIOSCIENCES, INC.
    Inventors: Jeffrey Miner, Jean-Luc Girardet, Barry D. Quart
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9034855
    Abstract: The present application relates to novel substituted phenylacetamides and phenylpropanamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: May 19, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Chantal Fürstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • 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
  • Patent number: 9012360
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20150105410
    Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Laszlo R. TREIBER, Irina ZAMANSKY, Jean-Luc GIRARDET
  • Patent number: 9006277
    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: August 29, 2014
    Date of Patent: April 14, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Przewloka, 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: 20150099721
    Abstract: A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 9, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jaime Acquaviva, Suqin He, David Proia
  • Publication number: 20150094348
    Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.
    Type: Application
    Filed: November 28, 2014
    Publication date: April 2, 2015
    Inventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
  • Publication number: 20150094349
    Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating Bcr-Abl, FLT-3, EGFR, c-Kit, B-raf, and NPM-ALK associated cancers, in a subject in need thereof.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: Zhenjian Du, Kevin Paul Foley
  • Publication number: 20150094284
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: December 3, 2014
    Publication date: April 2, 2015
    Inventors: Jean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
  • Patent number: 8993608
    Abstract: The present invention relates to compounds that inhibit the activity of Hsp90 and inhibit topoisomerase II.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: March 31, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zhenjian Du, Minghu Song, Weiwen Ying
  • 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
  • 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
  • Patent number: 8980930
    Abstract: Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: March 17, 2015
    Assignee: The Johns Hopkins University
    Inventors: Jun Liu, Curtis Chong, David J. Sullivan
  • Publication number: 20150073026
    Abstract: Triazole derivatives useful as anti-tubercular compounds; process for preparation of the triazoles and a method for inhibiting growth of Mycobacterium bovis BCG and Mycobacterium tuberculosis H37Ra using the triazoles.
    Type: Application
    Filed: September 23, 2014
    Publication date: March 12, 2015
    Inventors: Dhiman SARKAR, Sunita Ranjan DESHPANDE, Shailaja Pramod MAYBHATE, Anjali Prabhakar LIKHITE, Sampa SARKAR, Arshad KHAN, Preeti Madhukar CHAUDHARY, Sayalee Ramchandra CHAVAN
  • Publication number: 20150064257
    Abstract: The invention relates to co-crystals of metalaxyl and prothioconazole, to methods of making them, to compositions containing them and to the methods of using said co-crystals and said compositions to treat crops and plants.
    Type: Application
    Filed: March 12, 2013
    Publication date: March 5, 2015
    Inventor: David Frizzell
  • Patent number: 8969396
    Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating Bcr-Abl, FLT-3, EGFR, c-Kit, B-raf, and NPM-ALK associated cancers, in a subject in need thereof.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: March 3, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zhenjian Du, Kevin Paul Foley
  • 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
  • Publication number: 20150044233
    Abstract: Methods for determining the presence of cancer stem cells by detecting GD2 expression. Also provided are methods for reducing proliferation of cancer stem cells by contacting the cells with a GD2 targeting agent, such as an anti-GD2 antibody or a GD3 synthase inhibitor. GD3 synthase inhibitor compounds are also provided.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 12, 2015
    Inventors: Venkata Battula, Michael Andreeff, Sendurai A. Mani, Tapasree Roy Sarkar
  • Patent number: 8946273
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: February 3, 2015
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha A. De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
  • Patent number: 8946121
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: February 3, 2015
    Assignee: DSM IP Assets B.V.
    Inventors: Jacobus Stark, Angelique De Rijk
  • Publication number: 20150033373
    Abstract: A novel canola variety designated VR 9561 GS and seed, plants and plant parts thereof, produced by crossing Pioneer Hi-Bred International, Inc. proprietary inbred canola varieties. Methods for producing a canola plant that comprises crossing canola variety VR 9561 GS with another canola plant. Methods for producing a canola plant containing in its genetic material one or more traits introgressed into VR 9561 GS through backcross conversion and/or transformation, and to the canola seed, plant and plant part produced thereby. This discovery relates to the canola variety VR 9561 GS, the seed, the plant produced from the seed, and variants, mutants, and minor modifications of canola variety VR 9561 GS. This discovery further relates to methods for producing canola varieties derived from canola variety VR 9561 GS.
    Type: Application
    Filed: July 23, 2013
    Publication date: January 29, 2015
    Applicant: PIONEER HI BRED INTERNATIONAL INC
    Inventors: Jayantilal Devabhai Patel, Igor Falak, Winnifred Marie Mcnabb
  • Publication number: 20150025094
    Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, hal
    Type: Application
    Filed: August 1, 2012
    Publication date: January 22, 2015
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan University
    Inventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
  • Publication number: 20150018374
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1 is F, Cl or Br; R2 is H or F; and R3 is Cl or Br; and (b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 15, 2015
    Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, James Francis Bereznak
  • Patent number: 8927548
    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: January 13, 2012
    Date of Patent: January 6, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Kowalczyk-Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
  • 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: 20140364469
    Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: August 25, 2014
    Publication date: December 11, 2014
    Inventors: Stefan DUTZMANN, Klaus STENZEL, Manfred JAUTELAT
  • Publication number: 20140341850
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Applicant: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140336194
    Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventor: Shi Yin FOO
  • Publication number: 20140336231
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) prothioconazole and (B) fluxapyroxad and optionally (C) a further fungicidally active compound. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungicidally of plants or crops (e.g. cereals such as wheat, barley, lye, oats, millet and triticale; soya beans; rice; corn/maize; oil seed rape including canola; beans, peas, peanuts; sugar beet, fodder beet, beetroot; potatoes; cotton), and to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Application
    Filed: July 22, 2014
    Publication date: November 13, 2014
    Inventor: STEPHANIE GARY
  • Patent number: 8883827
    Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: November 11, 2014
    Assignee: Oslo University Hospital HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20140315943
    Abstract: A pharmaceutical composition comprising an mTOR/PI3K inhibitor, and an Hsp90 inhibitor according to the following formulae (I) and (Ia) or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.
    Type: Application
    Filed: May 23, 2012
    Publication date: October 23, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: David Proia, Suqin He
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse