Chalcogen Bonded Directly To Ring Carbon Of The Triazole Ring Patents (Class 548/263.2)
  • Patent number: 10889555
    Abstract: The present invention provides a novel sulfonamide compound having a ribonucleotide reductase inhibitory activity or a salt thereof, and a pharmaceutical composition containing the same as an active ingredient. A compound represented by Formula (I) [wherein, X1 represents an oxygen atom or the like; X2 represents an oxygen atom; X3 represents —NH—; X4 represents a hydrogen atom or the like; R1 represents —C(R11)(R12)— or the like; R11 and R12 are the same or different and each represents a hydrogen atom or the like; R2 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R3 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R4 represents a hydrogen atom or the like] or a salt thereof.
    Type: Grant
    Filed: January 24, 2020
    Date of Patent: January 12, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Seiji Miyahara, Hiroyuki Ueno, Shoki Hara, Yoshio Ogino
  • Patent number: 10703742
    Abstract: The present application relates to a novel and improved process for preparing 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives of the formula (I) in which R1A and R1B are independently selected from the group consisting of hydrogen, fluorine, chlorine, methyl, monofluoromethyl, difluoromethyl, trifluoromethyl, ethyl, methoxy, difluoromethoxy and trifluoromethoxy, to novel precursors for preparation thereof, and to the preparation and use of the crystalline polymorph I of (5-(4-chlorophenyl)-2-({1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl}methyl)-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I-A-1).
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: July 7, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Heiko Schirmer, Philipp Rubenbauer, Hans-Christian Militzer, Marie-Pierre Collin-Kröpelin, Frank Süßmeier, Kersten Matthias Gericke, Thomas Neubauer, Chantal Fürstner
  • Patent number: 10316003
    Abstract: Disclosed are a method of synthesizing prothioconazole and optically active isomers thereof and intermediates. The method includes reacting hydrazine with glyoxylic acid to produce a hydrazono acetic acid as an intermediate, and then reacting the intermediate with thiocyanate to produce the target product prothioconazole. The present method is very specific in terms of regioselectivity, resulting in minimum byproducts and a high product yield. The present method does not require special equipment, nor anhydrous or oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: June 11, 2019
    Assignee: ORIENTAL (LUZHOU) AGROCHEMICALS. CO., LTD.
    Inventors: Qiuju Sheng, Zhiming Zhang, Junliang Wang, Bangchi Chen
  • 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
  • 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: 20150119571
    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: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • 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: 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: 8957220
    Abstract: A preparation method of carfentrazone-ethyl comprises steps of: reacting 1-(5-amino-4-chloro-2-fluorophenyl)-4-difluoromethyl-3-methyl-1H-1,2,4-triazol-5-one with acrylic acid through a diazo arylation reaction to give 2-chloro-3-{2-chloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,3-triazol-1-yl]-4-fluorophenyl}propionic acid; and reacting the 2-chloro-3-{2-chloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,3-triazol-1-yl]-4-fluorophenyl}propionic acid with ethanol through an esterification reaction in a presence of an acidic catalyst to give carfentrazone-ethyl.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: February 17, 2015
    Assignees: Zhejiang Zhuji United Chemicals Co., Ltd, Luzhou Oriental Agrochemicals Co., Ltd.
    Inventors: Qunzhen Guo, Guoping Cai, Tangjun Wang, Jiandi Yu, Wei Liu
  • 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
  • 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: 20140364603
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • 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
  • Patent number: 8859601
    Abstract: The present application relates to new, substituted benzyl-1,2,4-triazolones and phenylsulfonyl-1,2,4-triazolones, 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: November 26, 2009
    Date of Patent: October 14, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulf Brüggemeier, Ingo Flamme, Chantal Fürstner, Joerg Keldenich, Peter Kolkhof, Martina Delbeck, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Truebel
  • Publication number: 20140275502
    Abstract: Aryl boronic esters and boronic acids containing the rhamnose carbamate moiety are coupled to a triazole with an appropriate leaving group, generating a 4-triazolylphenyl carbamate in good yield and without cleavage of the carbamate linkage.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Natalie C. GIAMPIETRO, Lawrence C. CREEMER, Gary D. CROUSE
  • Patent number: 8822519
    Abstract: The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype ? (PPAR?), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPAR? thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: September 2, 2014
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Chunhua Jin, Xiaoyu Liu, Zhenliang Chen, Xiaohe Zheng, Shoufeng Ming
  • Patent number: 8816070
    Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
  • Patent number: 8796324
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, 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: March 21, 2012
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiss, Jörg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Patent number: 8742133
    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 13, 2008
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
  • Patent number: 8729272
    Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: May 20, 2014
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Michael Keil, Joachim Gebhardt, Uwe Josef Vogelbacher, Frederik Menges, Michael Rack, Jens Renner, Bernd Wolf
  • Publication number: 20140113884
    Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.
    Type: Application
    Filed: April 4, 2012
    Publication date: April 24, 2014
    Inventors: John David Imig, William B. Campell, John Russell Falck
  • Publication number: 20140100213
    Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
    Type: Application
    Filed: November 4, 2013
    Publication date: April 10, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
  • Patent number: 8669371
    Abstract: An improved process for selectively chlorinating 4,5-dihydro-1-phenyl-1H-1,2,4-triazole-5-ones, including 4,5-dihydro-3-alkyl-1-phenyl-1H-1,2,4-triazole-5-ones and4-haloalkyl-4, 5-dihydro-3-alkyl-1-phenyl-1H-1,2,4-triazole-5-ones in the 4-position of the phenyl ring by dissolving the compounds in a synergistic ratio of polar aprotic solvents, preferably acetonitrile and N,N-dimethylformamide in a 7:3 ratio and reacting the solution with chlorine gas.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: March 11, 2014
    Inventor: Bomi Patel Framroze
  • Patent number: 8642278
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: February 4, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Patent number: 8633232
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: January 21, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20140005241
    Abstract: The present invention relates to compounds, compositions, and methods, for treating subjects suspected of needing treatment for a Nidovirales virus infection. In certain embodiments, the compounds comprise Nidovirales helicase inhibitors that do not significantly affect helicase ATPase enzymatic activity or nucleic acid binding activity of the helicase.
    Type: Application
    Filed: June 17, 2013
    Publication date: January 2, 2014
    Applicant: The Curators of the University of Missouri
    Inventors: Stefan G. Sarafianos, Adeyemi O. Adedeji, Kamlendra Singh
  • Publication number: 20130345435
    Abstract: A preparation method of carfentrazone-ethyl comprises steps of: reacting 1-(5-amino-4-chloro-2-fluorophenyl)-4-difluoromethyl-3-methyl-1H-1,2,4-triazol-5-one with acrylic acid through a diazo arylation reaction to give 2-chloro-3-{2-chloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,3-triazol-1-yl]-4-fluorophenyl}propionic acid; and reacting the 2-chloro-3-{2-chloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,3-triazol-1-yl]-4-fluorophenyl}propionic acid with ethanol through an esterification reaction in a presence of an acidic catalyst to give carfentrazone-ethyl.
    Type: Application
    Filed: January 12, 2012
    Publication date: December 26, 2013
    Inventors: Qunzhen Guo, Gouping Cai, Tangjun Wang, Jiandi Yu, Wei Liu
  • Patent number: 8614241
    Abstract: An ester compound represented by formula (1): wherein R3 represents hydrogen or methyl, R4 represents hydrogen or C1-C4 alkyl, and R5 represents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: December 24, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Noritada Matsuo
  • Publication number: 20130330365
    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: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130330366
    Abstract: In one aspect, the invention relates to compounds having the formula XII: 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: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130296322
    Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
  • Patent number: 8530669
    Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: September 10, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Noritada Matsuo
  • Publication number: 20130231313
    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: Application
    Filed: September 14, 2011
    Publication date: September 5, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Chantal Fürstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20130225646
    Abstract: The present application relates to novel substituted N-phenethyltriazoloneacetamides, 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: Application
    Filed: August 31, 2011
    Publication date: August 29, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Chantal Fürstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20130197217
    Abstract: The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
    Type: Application
    Filed: September 30, 2011
    Publication date: August 1, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Takeshi Kuwada, Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki, Naoki Miyakoshi
  • Publication number: 20130190330
    Abstract: The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, 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: Application
    Filed: February 25, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Chantal Furstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trubel
  • Publication number: 20130172384
    Abstract: This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: July 4, 2013
    Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Jonathan M. Ghergurovich, David Lee Musso, Cynthia A. Parrish
  • Publication number: 20130165560
    Abstract: Modified fillers are described which have adsorbed and/or attached chemical groups, such as a triazole and/or pyrazole thereon. Other modified fillers are also described. Elastomeric compositions containing the modified filler are further described, as well as methods to improve hysteresis and/or abrasion resistance in elastomeric compositions using the modified fillers of the present invention.
    Type: Application
    Filed: February 22, 2013
    Publication date: June 27, 2013
    Applicant: CABOT CORPORATION
    Inventor: CABOT CORPORATION
  • Publication number: 20130116252
    Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 9, 2013
    Applicant: NIPPON KAYAKU KABUSHIKI KAISHA
    Inventor: NIPPON KAYAKU KABUSHIKI KAISHA
  • Publication number: 20130079378
    Abstract: An ester compound represented by formula (1): wherein R3 represents hydrogen or methyl, R4 represents hydrogen or C1-C4 alkyl, and R5 represents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 28, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Noritada Matsuo
  • Publication number: 20130072689
    Abstract: An improved process for selectively chlorinating 4,5-dihydro-1-phenyl-1H-1,2,4-triazole-5-ones, including 4,5-dihydro-3-alkyl-1-phenyl-1H-1,2,4-triazole-5-ones and 4-haloalkyl-4,5-dihydro-3-alkyl-1-phenyl-1H-1,2,4-triazole-5-ones in the 4-position of the phenyl ring by dissolving the compounds in a synergistic ratio of polar aprotic solvents, preferably acetonitrile and N,N-dimethylformamide in a 7:3 ratio and reacting the solution with chlorine gas.
    Type: Application
    Filed: August 13, 2012
    Publication date: March 21, 2013
    Applicant: TAGROS CHEMICALS INDIA, LTD.
    Inventor: Bomi Patel Framroze
  • Publication number: 20130072461
    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: November 13, 2012
    Publication date: March 21, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: Synta Pharmaceuticals Corp.
  • Patent number: 8399464
    Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: March 19, 2013
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Hiroshi Kuramochi, Setsuko Niitsuma, Masaharu Nakamura, Yoshitaka Sato, Seiichi Saito, Arihiro Tomura, Yuh-ichiro Ichikawa, Yousuke Kasuga
  • Publication number: 20130011361
    Abstract: The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 10, 2013
    Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AG
    Inventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
  • Publication number: 20130005985
    Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.
    Type: Application
    Filed: March 15, 2011
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Michael Keil, Joachim Gebhardt, Uwe Josef Vogelbacher, Frederik Menges, Michael Rack, Jens Renner, Bernd Wolf
  • Patent number: 8329736
    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 20, 2012
    Date of Patent: December 11, 2012
    Assignee: Synta Pharmaceuticals, Corp.
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying, Teresa Kowalczyk Przewloka, Shijie Zhang, Kevin Foley, Zhenjian Du, Dan Zhou, Shuzhen Qin
  • Publication number: 20120309802
    Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Application
    Filed: February 18, 2011
    Publication date: December 6, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Noritada Matsuo
  • Patent number: 8318184
    Abstract: The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, depression, and generalized anxiety disorder.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: November 27, 2012
    Assignee: Eli Lilly and Company
    Inventors: James Allen Monn, Lourdes Prieto, Lorena Taboada Martinez, Carlos Montero Salgado, Bruce William Shaw