Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/375.1)
  • Patent number: 10844016
    Abstract: Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: November 24, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Stefan Werner, Stefanie Mesch, Arwed Cleve, Nico Bräuer, Simon Anthony Herbert, Markus Koch, Henrik Dahllöf, Maren Osmers, Elizabeth Hardaker, Anton Lishchynskyi
  • Patent number: 10131654
    Abstract: The present invention comprises compounds of Formula I and their use in the inhibition of cell proliferation in therapeutic treatments. Pharmaceutical compositions comprising at least one compound of Formula I and at least one pharmaceutical excipient are disclosed, as well as methods of using compounds of Formula I and pharmaceutical compositions thereof for treatment of hyper-proliferative diseases and other disorders.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: November 20, 2018
    Assignee: Translational Drug Development, LLC
    Inventors: Tong Wang, Stephen Gately
  • Patent number: 9199947
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: December 1, 2015
    Assignee: Sanofi
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Patent number: 9187410
    Abstract: The present invention provides a process for isolating tigecycline which process comprises the step of spray drying a solution of tigecycline in a solvent. Preferably the solvent is water or an organic solvent. In another aspect, there is provided tigecycline obtainable by spray drying, particularly in amorphous form. In particular, the invention provides tigecycline obtainable by spray drying according to the process of the invention.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: November 17, 2015
    Assignee: Hovione Inter Limited
    Inventors: Zita Mendes, Guy Villax
  • Patent number: 9150526
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: October 6, 2015
    Assignee: Sanofi
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Patent number: 9079862
    Abstract: The present invention relates to a novel process for preparing acetanilides of the formula (I) by reacting a 2-halo-N-halomethylacetanilide of the formula (II) with an azole of the formula (III) H-A??(III) wherein the substituents R, R1, R2, R3, R4, A, X and X1 in the formulae (I), (II) and (III) have the meanings as indicated in the description.
    Type: Grant
    Filed: December 13, 2012
    Date of Patent: July 14, 2015
    Assignee: BASF SE
    Inventors: Michael Keil, Wolfgang Reichert, Christopher Koradin, Yüksel Battal
  • Patent number: 9073871
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: July 7, 2015
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20150141477
    Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Marc Nazare, Detlef Kozian, Andreas Evers, Werngard Czechtizky
  • Patent number: 9023883
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 5, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150099728
    Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20150080446
    Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Application
    Filed: September 16, 2014
    Publication date: March 19, 2015
    Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
  • Patent number: 8957066
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Biomarin Pharmaceutical Inc.
    Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20150045399
    Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: September 2, 2014
    Publication date: February 12, 2015
    Applicant: Alexar Therapeutics, Inc.
    Inventor: Raju Mohan
  • Patent number: 8952026
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 10, 2015
    Assignee: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei
  • Publication number: 20150018403
    Abstract: A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and pharmaceutical use thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: January 15, 2015
    Inventors: Takahisa MOTOMURA, Takuya MATSUO, Gakujun SHOMI
  • Publication number: 20150011592
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: January 8, 2015
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20140371467
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Applicant: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20140364623
    Abstract: The present invention relates to a novel process for preparing acetanilides of the formula (I) by reacting a 2-halo-N-halomethylacetanilide of the formula (II) with an azole of the formula (III) H-A??(III) wherein the substituents R, R1, R2, R3, R4, A, X and X1 in the formulae (I), (II) and (III) have the meanings as indicated in the description.
    Type: Application
    Filed: December 13, 2012
    Publication date: December 11, 2014
    Applicant: BASF SE
    Inventors: Michael Keil, Wolfgang Reichert, Christopher Koradin, Yüksel Battal
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140323537
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 30, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, PAULA ANN BORIACK-SJODIN, OSCAR MIGUEL MORADEI, LEI JIN, KENNETH W. DUNCAN
  • Publication number: 20140323436
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R6b, R7, R8a, R8b, R9a, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Bruce Lawrence FINKELSTEIN, Andrew Edmund TAGGI, Jeffrey Keith LONG, Paula Louise SHARPE, Chi-Ping TSENG, Stephen Frederick MCCANN, Amy X DING, Steven Lewis SWANN, JR.
  • Publication number: 20140315961
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Publication number: 20140315904
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Patent number: 8859606
    Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Grant
    Filed: January 21, 2013
    Date of Patent: October 14, 2014
    Assignee: Allergan, Inc.
    Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
  • Publication number: 20140296315
    Abstract: A compound represented by the following formula: wherein n is 1 or 2, or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicant: JAPAN TOBACCO INC.
    Inventors: Takahisa Motomura, Gakujun Shomi
  • Publication number: 20140288140
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei
  • Publication number: 20140288129
    Abstract: Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
  • Publication number: 20140288141
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • Patent number: 8822521
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: September 2, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, Chi-Ping Tseng, Stephen Frederick McCann, Steven Lewis Swann, Jr.
  • Publication number: 20140235689
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R1, R1a, R2, R3, R4, Q1 and Q2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: MOUMITA KAR
  • Patent number: 8809333
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: August 19, 2014
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140212475
    Abstract: Compositions and pharmaceutical compositions including one or more selenium-containing COX-2 inhibitors are provided according to aspects of the present invention. Methods of treating a subject having or suspected of having cancer are provided according to aspects of the present invention which include administering a therapeutically effective amount of a pharmaceutical composition including a selenium-containing COX-2 inhibitor.
    Type: Application
    Filed: January 31, 2014
    Publication date: July 31, 2014
    Applicant: THE PENN STATE RESEARCH FOUNDATION
    Inventors: Gavin P. Robertson, Chandagalu D. Raghavendra Gowda, Dhimant H. Desai, Shantu G. Amin
  • Patent number: 8791272
    Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: July 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Oost, Ralf Anderskewitz, Dieter Wolfgang Hamprecht, Christoph Hoenke, Domnic Martyres, Wolfgang Rist, Peter Seither
  • Publication number: 20140206706
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as 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. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 8772507
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: July 8, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Xiangping Qian, Andrew I. McDonald, Han-Jie Zhou, Luke W. Ashcraft, Bing Yao, Hong Jiang, Jennifer Kuo Chen Huang, Jianchao Wang, David J. Morgans, Jr., Bradley P. Morgan, Gustave Bergnes, Dashyant Dhanak, Steven D. Knight, Nicholas D. Adams, Cynthia A. Parrish, Kevin Duffy, Duke Fitch, Rosanna Tedesco
  • Patent number: 8754238
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: June 17, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter Ian Dosa
  • Patent number: 8735398
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: May 27, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Patent number: 8735321
    Abstract: An object of the present invention is a process for the preparation of particles which comprise two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is the use of an agrochemical active ingredient for inhibiting the crystallization of another agrochemical active ingredient in a preparation process for particles which comprise the two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is particles which comprise two agrochemical active ingredients in amorphous form. The use in plant protection is also described.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: May 27, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck
  • Publication number: 20140142143
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 22, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20140121258
    Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxyl}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula (I). Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 1, 2014
    Applicant: ALLERGAN, INC.
    Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
  • Publication number: 20140038975
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 6, 2014
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140038923
    Abstract: The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay.
    Type: Application
    Filed: December 12, 2011
    Publication date: February 6, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Karen Wagner, Christophe Morisseau, Aaron Wecksler, Guodong Zhang
  • Patent number: 8642614
    Abstract: The present invention provides a compound of the formula: where n, m, X1, X2, X3, X4, R1, R2 and R3 are those defined herein. Some aspects of the invention also provides methods for using these compounds and compositions comprising the same.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: February 4, 2014
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Hang Yin, Linda R. Watkins
  • Publication number: 20140018326
    Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Publication number: 20140005235
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, A5, A6, G1, G2, R1, R2, R3, L, Q1, Q2, R4, R5, R6, R7, Q2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, and Y9 are as defined in claim 1; or salts or N-oxides thereof.
    Type: Application
    Filed: March 19, 2012
    Publication date: January 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph, Marcel Jung, Ottmar Franz Hueter, Peter Renold, Thomas Pitterna
  • Patent number: 8614332
    Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure is a heteroaryl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, —(CH2)n—Z—(CH2)m—OPO(OR7)R9, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: December 24, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Denis E. Ryono, Peter T. W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino, Richard B. Sulsky
  • Patent number: RE45336
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: January 13, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Patent number: RE45337
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: January 13, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jay Xu