Additional Cyano Containing Patents (Class 546/287)
  • Patent number: 9399651
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: July 26, 2016
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, Wesley B. Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan R. Kett, Amy Zartman
  • Patent number: 9024032
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Publication number: 20140296295
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Walter HÜBSCH, Daniel MEIBOM, Alexandros VAKALOPOULOS, Barbara ALBRECHT-KÜPPER, Peter NELL, Katja ZIMMERMANN, Frank SÜßMEIER, Joerg KELDENICH
  • 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: 20130210795
    Abstract: The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: June 27, 2011
    Publication date: August 15, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexandros Vakalopoulos, Daniel Meibom, Peter Nell, Frank Sussmeier, Barbara Albrecht-Kupper, Katja Zimmermann, Joerg Keldenich, Dirk Schneider, Ursula Krenz
  • Patent number: 8426602
    Abstract: The present application relates to novel heteroaryl-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: April 23, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Daniel Meibom, Alexandros Vakalopoulos, Barbara Albrecht-Küpper, Katja Zimmermann, Peter Nell, Frank Süβmeier
  • Publication number: 20130040992
    Abstract: The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.
    Type: Application
    Filed: August 13, 2012
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
  • Patent number: 8093343
    Abstract: The invention described herein provides for novel nitric oxide-releasing polymers that comprise at least two adjacent units derived from acrylonitrile monomer units and containing at least one carbon-bound diazeniumdiolate. The diazeniumdiolated acrylonitrile-derived polymers can be used in medical devices therapeutically. Accordingly, the invention also provides a method of treating a biological disorder and a method of promoting angiogenesis that includes administering a medical device comprising a nitric oxide-releasing polymer comprising at least two adjacent units of acrylonitrile before exposure to nitric oxide and at least one nitric oxide releasing N2O2? group, wherein the N2O2? group is attached directly to the polyacrylonitrile backbone, to a specific location on or within the mammal in an amount effective to treat the biological disorder or promote angiogenesis.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: January 10, 2012
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Joseph A. Hrabie, Frank DeRosa, Larry K. Keefer
  • Publication number: 20110136871
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: May 22, 2009
    Publication date: June 9, 2011
    Applicant: BAYER SCHERING AKTIENGESELLSCHAFT
    Inventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süssmeier, Joerg Keldenich
  • Patent number: 7915424
    Abstract: The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: March 29, 2011
    Assignee: Eli Lilly and Company
    Inventors: Francisco Javier Agejas-Chicharro, Bruce Anthony Dressman, Jose Antonio Martinez Perez, James Allen Monn, Mohammad Sadegh Zia-Ebrahimi, Sonia Gutierrez Sanfeliciano, Steven Marc Massey, Steven Scott Henry
  • Publication number: 20110046162
    Abstract: The present application relates to novel substituted fused cyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: December 9, 2008
    Publication date: February 24, 2011
    Applicant: BAYER SCHERING PHARMA
    Inventors: Peter Nell, Alexandros Vakalopoulos, Frank Süssmeier, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Daniel Meibom
  • Publication number: 20110021487
    Abstract: The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
    Type: Application
    Filed: January 31, 2009
    Publication date: January 27, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Walter Hübsch, Peter Nell, Frank Süssmeier, Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann
  • Patent number: 7868026
    Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: January 11, 2011
    Assignee: Pfizer Inc.
    Inventors: Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
  • Patent number: 7825255
    Abstract: The invention relates to the compounds of formula (I), to a method for producing the same and to the use thereof as medicaments.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: November 2, 2010
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stásch
  • Publication number: 20100197655
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: January 12, 2010
    Publication date: August 5, 2010
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Patent number: 7514563
    Abstract: A process for producing cyano substituted arene boranes is described. The compounds are useful intermediates to pharmaceutical compounds using the cyano group as a reactant.
    Type: Grant
    Filed: June 8, 2006
    Date of Patent: April 7, 2009
    Assignee: Board of Trustees of Michigan State University
    Inventors: Milton R. Smith, III, Robert E. Maleczka, Ghayoor A. Chotana
  • 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
  • Patent number: 7504421
    Abstract: The invention relates to compounds of general formula (I), a method for the production thereof and the use thereof as pharmacologically effective substances for a broad medical indication spectrum. Furthermore, selective adenosine receptor ligands, preferably selective adenosine A1-, adenosine A2a- and/or adenosine A2b-receptor ligands are provided for the prophylaxis and/or the treatment of diseases, especially cardiovascular diseases, diseases of the urogenital region, diseases of the respiratory tract, inflammatory and neuroinflammatory diseases, diabetes, especially pancreatic diabetes, neurodegenerative diseases, pain states, cancer as well as liver fibrosis and liver cirrhosis.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: March 17, 2009
    Inventors: Ulrich Rosentreter, Rolf Henning, Marcus Bauser, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Klaus Dembowsky, Olga Salcher-Schraufstatter, Johannes-Peter Stasch, Thomas Krahn, Elisabeth Perzborn
  • Publication number: 20080176833
    Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.
    Type: Application
    Filed: December 13, 2007
    Publication date: July 24, 2008
    Inventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
  • Patent number: 7342115
    Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
    Type: Grant
    Filed: November 7, 2003
    Date of Patent: March 11, 2008
    Assignee: Neurogen Corporation
    Inventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
  • Patent number: 7332498
    Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: February 19, 2008
    Assignees: Cytokinetics, Inc., SmithKline Beecham Corporation
    Inventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
  • Patent number: 7320993
    Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: January 22, 2008
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Patent number: 7151182
    Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: December 19, 2006
    Assignee: Basilea Pharmaceutica AG
    Inventors: Hiroshi Fukuda, Tadakatsu Hayase, Eisaku Mizuguchi, Nobuo Shimma, Jun Ohwada, Nobuhiro Oikawa, Masahiro Sakaitani, Masao Tsukazaki, Isao Umeda
  • Patent number: 7135486
    Abstract: This application relates to compounds of formula (I), wherein R1, R2, R3, and R4 are defined as recited in the claims, or a tautomer, salt, hydrate, or alkoxide thereof. A process for preparing such materials, pharmaceutical compositions containing them, and methods of treating a cardiovascular disorder by administering them to a patient are also disclosed and claimed.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: November 14, 2006
    Assignee: Bayer Aktiengeselischaft
    Inventors: Ulrich Rosentreter, Rolf Henning, Marcus Bauser, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Klaus Dembowsky, Olga Salcher-Schraufstätter, Johannes-Peter Stasch, Thomas Krahn, Elisabeth Perzborn
  • Patent number: 7129255
    Abstract: This application relates to compounds of the formula wherein the groups R1–R6 are as defined in the specification and claims, and to a pharmaceutical composition containing the same, and to a method of using the same in treatment of cardiovascular disorders.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: October 31, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch, Mitsuyuki Shimada
  • Patent number: 7109218
    Abstract: Compounds of the formula (I) a process for their preparation and their use as medicaments are described.
    Type: Grant
    Filed: November 28, 2002
    Date of Patent: September 19, 2006
    Assignee: Bayer HealthCare AG
    Inventors: Ulrich Rosentreter, Thomas Krämer, Mitsuyuki Shimada, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Kerstin Henninger, Johannes-Peter Stasch, Ralf Wischnat
  • Patent number: 7074813
    Abstract: The present invention is directed to substituted N?-(arylcarbonyl)-benzhydrazides, N?-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: July 11, 2006
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
  • Patent number: 7015237
    Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: March 21, 2006
    Assignee: Warner-Lambert Company
    Inventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Michael William Wilson
  • Patent number: 6911451
    Abstract: Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: June 28, 2005
    Assignee: Celltech R&D Limited
    Inventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
  • Publication number: 20040242648
    Abstract: The present invention provides compounds that possess inhibitory activity against PDE-3 and L-type calcium channels. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine.
    Type: Application
    Filed: October 7, 2003
    Publication date: December 2, 2004
    Applicant: ARTESIAN THERAPEUTICS, INC.
    Inventors: Gregory S. Hamilton, Harry Jefferson Leighton
  • Publication number: 20040162427
    Abstract: The invention relates to the use of compounds of formula (I) as medicaments, to the novel compounds of formula (I) themselves, and to a method for the production thereof.
    Type: Application
    Filed: April 12, 2004
    Publication date: August 19, 2004
    Inventors: Ulrich Rosentreter, Thomas Krmer, Andrea Vaupel, Walter Hbsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes Stasch
  • Publication number: 20040110946
    Abstract: The invention relates to compounds of formula (I), a method for the production thereof and the use of the same as pharmaceuticals.
    Type: Application
    Filed: January 7, 2004
    Publication date: June 10, 2004
    Inventors: Ulich Rosentreter, Thomas Kramer, Andrea Vaupel, Walter Hubsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch, Mitsuyuki Shimada
  • Publication number: 20040102626
    Abstract: The invention relates to the compounds of formula (I), to a method for producing them and to their use as medicaments.
    Type: Application
    Filed: January 7, 2004
    Publication date: May 27, 2004
    Inventors: Ulrich Rosentreter, Thomas Kramer, Andrea Vaupel, Walter Hubsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes Peter Stasch, Mitsuyuki Shimada
  • Patent number: 6649767
    Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: November 18, 2003
    Assignee: Pfizer, Inc.
    Inventors: Kunio Satake, Noriaki Murase
  • Patent number: 6503933
    Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: January 7, 2003
    Assignee: Aventis CropScience UK Limited
    Inventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
  • Patent number: 6432960
    Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: August 13, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, Graham S. Poindexter
  • Patent number: 6392048
    Abstract: The present invention provides a process for preparing carbocyclic or heterocyclic nitrites by the vapor phase contact ammoxidation of carbocyclic compounds or heterocyclic compounds, in which the reaction is carried out effectively without the increase of the amount of ammonia or oxygen used or the introduction of steam to give the nitrites as the objective products stably with the passage of time in a high yield with a high selectivity.
    Type: Grant
    Filed: July 31, 2000
    Date of Patent: May 21, 2002
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Yutaka Sasaki, Hiroshi Utsumi, Akimitsu Morii, Kazuo Morishita
  • Patent number: 6392050
    Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: May 21, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Lui, Hans Panskus, Albert Schnatterer
  • Patent number: 6130334
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: October 10, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Ashok Maliakal, Kai Rossen, Ralph P. Volante, Jess Sager
  • Patent number: 6046221
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: April 4, 2000
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 6002012
    Abstract: There is provided a process for the preparation of [(5,6-dicarboxy-3-pyridyl)methyl]ammonium halides having the structural formula I ##STR1## The [(5,6-dicarboxy-3-pyridyl)methyl]ammonium halides are useful as intermediates in the preparation of herbicidal 5-(alkoxymethyl)-2-(2-imidazolin-2-yl)-nicotinic acids, esters and salts.
    Type: Grant
    Filed: March 20, 1998
    Date of Patent: December 14, 1999
    Assignee: American Cyanamid Company
    Inventor: Wen-Xue Wu
  • Patent number: 5959116
    Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: September 28, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5955615
    Abstract: Dyestuffs of the formula whereinD is the radical of a carbo- or heterocyclic diazo component,X represents O, NH, NT, NCOT, NCCH.sub.2 T or NSO.sub.2 T,and the other substituents have the meaning given in the description, are preferably suitable, if m=n=l=o, for dyeing and printing hydrophobic synthetic fiber materials and mixtures thereof with naturally occurring fiber materials.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: September 21, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventor: Rainer Hamprecht
  • Patent number: 5861419
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck Frosst Canad, Inc.
    Inventors: Daniel Dube, Richard Friesen, Rejean Fortin, Zhaoyin Wang, Jacques Yves Gauthier
  • Patent number: 5808015
    Abstract: Dyestuffs of the formula ##STR1## wherein D is the radical of a carbo- or heterocyclic diazo component,X represents O, NH, NT, NCOT, NCCH.sub.2 T or NSO.sub.2 T,are preferably suitable, if m=n=l=o, for dyeing and printing hydrophobic synthetic fiber materials and mixtures thereof with naturally occurring fiber materials.
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: September 15, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventor: Rainer Hamprecht
  • Patent number: 5763638
    Abstract: A process for the preparation of nitriles of formula ##STR1## wherein X is CH or N, and R.sub.1 and R.sub.2 are each independently of the other hydrogen, chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R.sub.1 and R.sub.2 together form a fused benzene ring, by reacting an aldehyde of formula ##STR2## with hydroxylaminosulfate in the presence of a tertiary amine base of formula ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen, methyl or ethyl, R.sub.5 is branched C.sub.3 -C.sub.5 alkyl or phenyl, and R.sub.6 and R.sub.7 are methyl or ethyl,in the temperature range from 100.degree. to 160.degree. C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: June 9, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Richard Breitschuh
  • Patent number: 5760063
    Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: June 2, 1998
    Assignee: Scriptgen Pharmaceuticals, Inc.
    Inventors: Kelvin T. Lam, David G. Powers
  • Patent number: 5716971
    Abstract: Pyridine derivatives of the formula ##STR1## wherein the ring A stands for an optionally further substituted benzene ring; the ring B stands for an optionally substituted pyridine ring; Q stands for hydroxyl group, or OQ.sup.1 or Q.sup.1 wherein Q.sup.1 stands for an optionally substituted aliphatic hydrocarbon group; and n denotes 0 or 1, or their salts, which have potassium.channel opening activity and are useful as therapeutic agents of circulatory diseases such as angina pectoris, hypertension, etc.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: February 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Toshifumi Watanabe
  • Patent number: 5708180
    Abstract: The reaction of cyanoolefins, aminocarbonylolefins or hydroxyiminoolefins with a Vilsmeier reagent leads to 2-halogenopyridines which bear aldehyde groups in the 3 and/or 5 position. These pyridinealdehydes are valuable intermediates for the preparation of pharmaceuticals and crop protection agents.
    Type: Grant
    Filed: November 27, 1996
    Date of Patent: January 13, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunther Beck, Helmut Heitzer