Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/288)
  • Patent number: 10550083
    Abstract: 4-Alkoxy-3-hydroxypicolinic acids may be conveniently prepared from 4,6-dibromo-3-hydroxypicolinonitrile in a series of chemical steps selected from bromo substitution, nitrile hydrolysis and halogen reduction that are conducted as a single pot process. 4,6-Dibromo-3-hydroxypicolinonitrile may be prepared from furfural in a series of chemical steps selected from cyano-amination, amine salt formation and bromination-rearrangement.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: February 4, 2020
    Assignee: Dow AgroSciences LLC
    Inventors: Kenneth E. Stockman, Gregory T. Whiteker, Erich J. Molitor, Nakyen Choy
  • Patent number: 10464936
    Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.
    Type: Grant
    Filed: October 25, 2018
    Date of Patent: November 5, 2019
    Assignee: Xoc Pharmaceuticals, Inc.
    Inventors: Thomas Armer, Geoff McKinley, Scott Borland, Miguel Guzman, Ármin Szabolcs, János Gerencser
  • Patent number: 9051271
    Abstract: The present invention describes compounds of formula (I) Wherein: R1 is selected from C1-C6 alkyl, CF3, Phenyl & 2-thienyl R2 is selected from C1-C6 alkyl, phenyl & CF3 R3 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R4 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R5 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R6 is selected from H, —(CH2)nC(O)OR7 & C(O)C6H4—R7 R7 is selected from C1-C6 alkyl, phenyl optionally substituted by 1-3 substituents selected from CF3, NO2 and halo. n is 0-6 These compounds have been identified as novel anticancer agents.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: June 9, 2015
    Assignee: UNITED ARAB EMIRATES UNIVERSITY
    Inventors: Ibrahim Mahmoud Abdou, Alaa ElDin Abdel Aziz Salem, Abdu Adem, Hussein F. Zhodi, Hany Abdel Aziz El Deab
  • Publication number: 20150133669
    Abstract: The present invention relates to new processes for the preparation of 2-cyclopentyl-6-methoxy-isonicotinic acid, which is a useful intermediate for the synthesis of pyridine-4-yl derivatives as immunomodulating agent. Moreover, the present invention also relates to new intermediates used in those processes.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 14, 2015
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventor: Gunther Schmidt
  • Publication number: 20140256549
    Abstract: The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 11, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventor: David A. Morgenstern
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140234245
    Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Patent number: 8791091
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Patent number: 8754081
    Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: June 17, 2014
    Assignee: The United States of America as represented by the Secretary, Departmnet of Health and Human Services
    Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Terrence Burke, Jr., Gagani Athauda, Sarah Choyke, Alessio Giubellino, Nelly Tan, Zhen-Dan Shi
  • Patent number: 8716318
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: May 6, 2014
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Patent number: 8524896
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: September 3, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
  • Publication number: 20130143843
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8410155
    Abstract: The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Patent number: 8389525
    Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: March 5, 2013
    Inventors: Renee Desai, Ketan Desai
  • Patent number: 8278442
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: October 2, 2012
    Assignee: Prosidion Limited
    Inventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
  • Patent number: 8273773
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 25, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
  • Publication number: 20120189537
    Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
    Type: Application
    Filed: November 22, 2011
    Publication date: July 26, 2012
    Inventor: Krishna Menon
  • Publication number: 20110275645
    Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.
    Type: Application
    Filed: May 5, 2010
    Publication date: November 10, 2011
    Inventors: Renee Desai, Ketan Desai
  • Publication number: 20110245506
    Abstract: A process for manufacturing a 2,3-disubstituted-5-methoxymethylpyridine of formula (I), where Z is H or halogen; Z1 is H, halogen, CN or NO2; Y2 is OM, and M is an alkali metal or an alkaline earth metal, comprises the step of: (i) reacting a compound of formula (II) where Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is H or halogen; Z1 is H, halogen, CN or NO2; Y1 and Y2 are each independently OR1, NR1R2, or when taken together Y1Y2 is —O—, —S— or —NR3—; R1 and R2 are each independently H, C1-C4 alkyl optionally substituted with C1-C1 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is H or C1-C4 alkyl, in a methanol/H2O mixture, comprising at least 20% by weight H2O (based on the sum of water and bromide (II)), with a base comprising MOCH3 and/or MOH, where M is alkali metal or alkaline
    Type: Application
    Filed: December 7, 2009
    Publication date: October 6, 2011
    Applicant: Basf SE
    Inventor: David Cortes
  • Patent number: 8022221
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: September 20, 2011
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
  • Publication number: 20110190295
    Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
    Type: Application
    Filed: March 31, 2009
    Publication date: August 4, 2011
    Applicant: The Govt of the U.S.A., as rep.by the Sec.Dept of Hlth. and Human Svcs., Natl Institutes of Health
    Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Terrence Burke, JR., Gagani Athauda, Sarah Choyke, Alessio Giubellino, Nelly Tan, Zhen-Dan Shi
  • Publication number: 20110178136
    Abstract: Disclosed are amino acid and phosphate prodrugs of compounds of the Formula V wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: March 31, 2011
    Publication date: July 21, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110144164
    Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 16, 2011
    Applicant: H. LUNDBECK A/S
    Inventors: Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
  • Patent number: 7897624
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 1, 2011
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20110046088
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: February 20, 2008
    Publication date: February 24, 2011
    Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMTIED
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20110040092
    Abstract: The invention relates to a process for making HOF.RCN and using it to oxidise organic substrates in a quick and safe way. The process comprises passing diluted fluorine through a conduit and RCN in water through another conduit into a microreactor to form HOF.RCN and reacting this with an organic substrates.
    Type: Application
    Filed: September 5, 2008
    Publication date: February 17, 2011
    Applicant: THE SECRETARY OF STATE FOR DEFENSE
    Inventors: Christopher Murray, Graham Sandford
  • Patent number: 7888374
    Abstract: The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.
    Type: Grant
    Filed: January 23, 2006
    Date of Patent: February 15, 2011
    Assignee: Abbott Laboratories
    Inventors: Gang Liu, Hing L. Sham, Bruce G. Szczepankiewicz, Zhili Xin, Hongyu Zhao, Michael D. Serby, Bo Liu, Mei Liu
  • Patent number: 7868177
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, C1, C2, D, L1, L2 and R3-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Tie-2 and Aurora kinase enzymes thereby influencing angiogenesis and the process of cell cycle and cell proliferation, respectively, to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of various protein kinases.
    Type: Grant
    Filed: February 21, 2007
    Date of Patent: January 11, 2011
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Holly L. Deak, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero
  • Publication number: 20100311582
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.
    Type: Application
    Filed: January 23, 2009
    Publication date: December 9, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
  • Patent number: 7816353
    Abstract: Compounds of formula III: wherein R5a, R3, X, Y, Q, R1a and R1b are as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: October 19, 2010
    Assignee: Exelixis, Inc.
    Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu
  • Patent number: 7786043
    Abstract: The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R1, independent of one another, represents halogen, OH, CN, NO2, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, C2-C4 alkenyl, C2-C4 alkynyl, C3-C8 cycloalkyl, C1-C4 alkoxy-C1-C4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C1-C4 alkyl, NHR, NR2, C(Ra)?N—ORb, S(?O)pA1 or C(?O)A2, or two radicals R1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C1-C4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R2 represents C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, hydroxy, halogen, CN or NO2; whereby R2 can also represent
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: August 31, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Thomas Grote, Carsten Blettner, Markus Gewehr, Udo Hünger, Bernd Müller, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Ulrich Schöfl, Harald Köhle, Siegfried Strathmann, Maria Scherer, Reinhard Stierl, Jan Rether
  • Patent number: 7772233
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: August 10, 2010
    Assignee: Merck Serono, S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
  • Publication number: 20100173886
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
    Type: Application
    Filed: May 22, 2008
    Publication date: July 8, 2010
    Inventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
  • Publication number: 20100166655
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: March 15, 2007
    Publication date: July 1, 2010
    Applicants: JANSSEN PHARMACEUTICA N.V., ADDEX PHARMACEUTICALS S.A.
    Inventors: Hassan Julien Imogai, Vincent Mutel, Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MaCdonald, Shirley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Palrick Finn, Gagik Melikyan
  • Publication number: 20100125138
    Abstract: The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione.
    Type: Application
    Filed: November 12, 2009
    Publication date: May 20, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: David Paul Provencal, Todd Miller, Yuxin Zhao, Jonathon S. Salsbury
  • Patent number: 7687501
    Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1, R3, and R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: March 30, 2010
    Assignee: Schering Corporation
    Inventors: Chad E. Bennett, William J. Greenlee, Chad E. Knutson, Duane A. Burnett
  • Patent number: 7683097
    Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.
    Type: Grant
    Filed: May 25, 2005
    Date of Patent: March 23, 2010
    Assignee: Propharmacon Inc.
    Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
  • Publication number: 20090298872
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorder associated with the activation of steroid hormone nuclear receptors.
    Type: Application
    Filed: December 13, 2005
    Publication date: December 3, 2009
    Applicant: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, John Wityak
  • Patent number: 7544677
    Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 9, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
  • Publication number: 20090142554
    Abstract: A process for printing an image on a substrate by means of an ink-jet printer which comprises applying thereto a composition comprising a liquid medium and a mono-azo compound of Formula (1) and salts thereof: wherein: D is an optionally substituted aryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2 or an optionally substituted nitrogen heteroaryl group carrying at least one direct substituent selected from the group consisting of —SO3H, —CO2H, —PO3H2; R1 is H: optionally substituted alkyl: amino: —NR4R5; wherein R4 is H, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl; and R5 is optionally substituted alkyl, optionally substituted alkoxy, optionally substituted acyl, optionally substituted aryl, optionally substituted heterocyclyl: —OR6; wherein R6 is H or optionally substituted alkyl: or —SR7; wherein R7 is optionally substituted alkyl; R
    Type: Application
    Filed: October 13, 2006
    Publication date: June 4, 2009
    Inventors: Gavin Wright, Rachel Anne James, Roy Bradbury, Lynn Bradbury
  • Publication number: 20090118338
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: October 10, 2008
    Publication date: May 7, 2009
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
  • Patent number: 7528139
    Abstract: Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: March 17, 2005
    Date of Patent: May 5, 2009
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Guenter Hoelzemann, Helene Crassier, Alfred Jonczyk, Wolfgang Staehle, Wilfried Rautenberg
  • Patent number: 7511149
    Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Publication number: 20090054655
    Abstract: The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R1—X1—NY—R2, wherein: X1 represents —CO— or —SO2—; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R1 represents a substituted or unsubstituted hydrocarbon group, —NYR3 group or —OR3 group (in the formulae, R3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R2 represents a hydrogen atom or —CO—R4 group (in the formula, R4 represents a substituted or unsubstituted hydrocarbon group, —NYR5 group or —OR5 group (in the formulae, R5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R1 and R4 may bind to each other to form a further substi
    Type: Application
    Filed: April 5, 2007
    Publication date: February 26, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tomomi Ikemoto, Naohiro Fukuda
  • Publication number: 20090030010
    Abstract: This invention relates to compounds of general formula I in which R1 and R2 are described in this application, the use of the compounds of general formula I as inhibitors of protein tyrosine kinases for treatment of various diseases as well as the compounds of general formulas II and III as intermediate compounds for the production of compounds of general formula I, whereby X, R1a and R2a have the meaning that is described in general formulas II and III.
    Type: Application
    Filed: December 14, 2005
    Publication date: January 29, 2009
    Inventors: Wolfgang Schwede, Hermann Kuenzer, Antonius Ter Laak, Benjamin Bader, Roman Hillig, Ursula Moenning, Arndt Schmitz, Dieter Zopf
  • Patent number: 7446117
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: November 4, 2008
    Assignee: Glaxo Group Limited
    Inventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
  • Publication number: 20080119488
    Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: July 24, 2005
    Publication date: May 22, 2008
    Applicant: EXELIXIS, INC.
    Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu