Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/300)
  • Publication number: 20090054436
    Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
    Type: Application
    Filed: October 17, 2008
    Publication date: February 26, 2009
    Inventors: Robert M. Borzilleri, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
  • Publication number: 20090048309
    Abstract: The present invention belongs to the field of agricultural fungicide and in particular disclosed N-(2-substituted phenyl)-N-methoxycarbamates and their preparation as well as use. Compounds according to the present invention are shown as the general formula I. Compounds according to the present invention have very good fungicidal activities and can be used for the control of plant fungicidal diseases, such as wheat powdery mildew, melon powdery mildew, apple powdery mildew, grape powdery mildew, strawberry powdery mildew, wheat rust, soybean rust, wheat Pythium root rot, cucumber Alternaria blight, rice “bakanae” disease, rice sheath blight, cucumber Fusarium wilt, cucumber anthracnose, rice blast, rice false smut, corn southern leaf blight.
    Type: Application
    Filed: January 25, 2006
    Publication date: February 19, 2009
    Applicant: Shenyang Research Institute of Chemical Industry
    Inventors: Chunhe Yang, Liwen Geng, Defeng Zhou, Ling Peng, Hong Zhang, Dongliang Cui, Zhinian Li, Liangqing Wang, Shouguo Zang, Zeyong Zhang
  • Publication number: 20080312262
    Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
    Type: Application
    Filed: August 21, 2008
    Publication date: December 18, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
  • Publication number: 20080306108
    Abstract: Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue.
    Type: Application
    Filed: June 6, 2008
    Publication date: December 11, 2008
    Applicant: MEDICURE INTERNATIONAL INC.
    Inventors: Wasimul Haque, James Diakur, Vinh Pham, Wenlian Zhang
  • Patent number: 7459562
    Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
    Type: Grant
    Filed: April 21, 2005
    Date of Patent: December 2, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Lyndon A. M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
  • Patent number: 7459469
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: December 2, 2008
    Assignee: Targacept, Inc.
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Patent number: 7456290
    Abstract: Process for the preparation of 2-aminomethylpyridine derivative of general formula (I) or a salt thereof, formula (I) in which:—n represents 0, 1, 2 or 3,—X is halogen atom,—each Y may be the same or different and may be a halogen atom, a halogenoalkyl, an alkoxycarbonyl or an alkylsulphonyl.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: November 25, 2008
    Assignee: Bayer Cropscience S.A.
    Inventor: Manuel Vangelisti
  • Publication number: 20080287505
    Abstract: The present invention provides novel substituted 2-methyl-2-phenoxy-N-propyl-propionamides and derivatives thereof that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.
    Type: Application
    Filed: May 19, 2008
    Publication date: November 20, 2008
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20080280895
    Abstract: The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g.
    Type: Application
    Filed: March 17, 2005
    Publication date: November 13, 2008
    Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Michael Quirmbach, Dirk Behnke, Christiane Marti
  • Publication number: 20080275044
    Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a process for the producing such compounds, and the use thereof to treat or inhibit pain and/or various other disorders or conditions.
    Type: Application
    Filed: April 11, 2008
    Publication date: November 6, 2008
    Applicant: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
  • 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: 20080269265
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: June 25, 2008
    Publication date: October 30, 2008
    Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, David Gunn, Martha Rodriguez, Ming Wang, Tiffany Turner, Catherine Brennan
  • Publication number: 20080262039
    Abstract: Vanilloid receptor ligand compounds corresponding to formula I: a process for producing such compounds, pharmaceutical compositions containing them, and the use of such compounds to treat pain and various other vanilloid receptor mediated conditions.
    Type: Application
    Filed: April 15, 2008
    Publication date: October 23, 2008
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Michael Przewosny, Bernd Sundermann, Jewoo Lee
  • Publication number: 20080255124
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: October 13, 2005
    Publication date: October 16, 2008
    Applicant: Smithkline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
  • Publication number: 20080255134
    Abstract: The present invention provides compounds of formula (I) possessing inhibitory activity against ? adrenergic receptors and phosphodiesterase (PDE), including type 3 phosphodiesterase (PDE-3). The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated and for treating cardiovascular disease, stroke, epilepsy, an ophthalmic disorder or migraine.
    Type: Application
    Filed: November 8, 2005
    Publication date: October 16, 2008
    Applicant: Artesian Therapeutics, Inc.
    Inventors: Malcolm George Taylor, Burkhard Klenke, Peter D. Suzdak, Reza Mazhari
  • Publication number: 20080255208
    Abstract: The present invention relates to 2,5-di-substituted-4-pyridinyloxy-substituted-phenyl-amidine derivatives, notably to 2,5-dialkyl-4-pyridinyloxy-substituted-phenyl-amidine derivatives, of formula (I) in which the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions (I).
    Type: Application
    Filed: September 12, 2006
    Publication date: October 16, 2008
    Applicant: Bayer CropScience AG
    Inventors: Peter Luemmen, Klaus Kunz, Jorg Greul, Oliver Guth, Benoit Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Jean-Pierre Vors, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Peter Losel, Olga Malsam
  • Patent number: 7425570
    Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT), stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: September 16, 2008
    Assignee: Medicure International Inc.
    Inventor: Wasimul Haque
  • Publication number: 20080221132
    Abstract: The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
    Type: Application
    Filed: September 10, 2007
    Publication date: September 11, 2008
    Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
  • Publication number: 20080194645
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Application
    Filed: January 14, 2008
    Publication date: August 14, 2008
    Inventors: Linus S. Lin, William K. Hagmann, Sanjeev Kumar, Wenji Yin, George Doss
  • Patent number: 7407959
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: August 5, 2008
    Assignee: Merck Frosst Canada & Co.
    Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
  • Publication number: 20080166299
    Abstract: The invention relates to radiolabeled compounds and their use in methods of imaging amyloid deposits, as well as to methods of their manufacture. The invention also relates to compounds for inhibiting the aggregation of amyloid proteins that form amyloid deposits, methods for delivering therapeutic agents to amyloid deposits, as well as methods of making compounds that inhibit the aggregation of amyloid proteins.
    Type: Application
    Filed: December 6, 2007
    Publication date: July 10, 2008
    Applicant: Trustees of The University of Pennsylvania
    Inventors: Hank F. Kung, Mei Ping Kung
  • Patent number: 7384967
    Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: October 6, 2003
    Date of Patent: June 10, 2008
    Assignee: Novo Nordisk A/S
    Inventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
  • Publication number: 20080124402
    Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner.
    Type: Application
    Filed: October 25, 2005
    Publication date: May 29, 2008
    Applicant: MERCK & CO., INC.
    Inventors: Yuntae Kim, Joshua Close, Mark E. Duggan, Barbara Hanney, Robert S. Meissner, Jeffrey Musselman, James J. Perkins, Jiabing Wang
  • Patent number: 7378446
    Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: May 27, 2008
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki, Takeshi Murata, Fumio Watanabe, Hiroshi Fukuda, Susumu Komiyama, Tadakatsu Hayase
  • Patent number: 7365085
    Abstract: Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: April 29, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Ajita Bhat, John Jeffrey McAtee, Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Robert A. Stavenger
  • Publication number: 20080081825
    Abstract: The present invention provides a compound having p38 MAP kinase inhibitory activity. Because of having p38 MAP kinase inhibitory activity, the compounds represented by the formula (I): wherein each symbol is as defined in the description, salts thereof, N-oxides thereof, solvates thereof, or prodrugs thereof are useful in preventing and/or treating diseases that are supposedly caused or deteriorated by abnormal production of cytokines including inflammatory cytokines or chemokines, or by overresponse thereto, namely cytokine-mediated diseases such as inflammatory diseases, respiratory diseases, cardiovascular diseases and bone diseases.
    Type: Application
    Filed: April 27, 2005
    Publication date: April 3, 2008
    Inventors: Hisao Nakai, Shingo Yamamoto, Masafumi Sugitani
  • 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: 7332608
    Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: February 19, 2008
    Assignee: SANOFI-AVENTIS Deutschland GmbH
    Inventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • 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: 7307092
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: December 11, 2007
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
  • Patent number: 7235566
    Abstract: Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: June 26, 2007
    Assignee: Smithkline Beecham p.l.c.
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, John Liddle, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Patent number: 7214799
    Abstract: The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): and salts thereof. The invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: May 8, 2007
    Assignee: BioStratum, Inc.
    Inventors: Raja Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
  • Patent number: 7205302
    Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: April 17, 2007
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
  • Patent number: 7202260
    Abstract: Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.
    Type: Grant
    Filed: June 14, 2004
    Date of Patent: April 10, 2007
    Assignee: Schering AG
    Inventors: Andreas Huth, Martin Krueger, Ludwig Zorn, Stuart Ince, Rolf Bohlmann, Karl Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
  • Patent number: 7199265
    Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: April 3, 2007
    Assignee: Karo Bio AB
    Inventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
  • Patent number: 7189383
    Abstract: The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the general formula (I) wherein: R is (C1–C6) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1–6; and m=0 or 1; and X is a halogen atom.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: March 13, 2007
    Assignee: Mallinckrodt Inc.
    Inventor: John J. R. Mertens
  • Patent number: 7175872
    Abstract: Pyridinium-Betain compounds of the general formula (A): wherein R1 is H or a primary amino acids that is attached to the structure, X is OH or its ionized form O?, Y is OH, SH, or their ionized forms O? and S?, Z is H, an alkyl group, or a glycosidic group, or a phosphate or ester derivative thereof, and n is an integer of 0 to 4 to represent the chain length of the compound. A counter-ion is associated with these compounds and is preferably an ion of sodium, potassium, ammonium, calcium, magnesium, chloride, nitrate, carbonate, sulphate, phosphate, or the like. These compounds can be used as taste modifiers in various foodstuffs.
    Type: Grant
    Filed: March 2, 2004
    Date of Patent: February 13, 2007
    Assignee: Nestec S.A.
    Inventors: Thomas Hofmann, Harald Ottinger, Oliver Frank, Tomislav Soldo, Imre Blank, Renaud Villard, Fabien Robert
  • Patent number: 7166621
    Abstract: Fungicidal compounds of the general formula (I): wherein X and Y are independently H, halo, C1-8 alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkoxy, C1-8 alkylthio, nitro, amino, mono- or di-(C1-6)alkylamino, mono- or di-(C2-6)alkenylamino, mono- or di-(C2-6)alkynylamino, formylamino, C1-4 alkyl(formyl)amino, C1-4 alkylcarbonylamino, C1-4 alkyl(C1-4 alkylcarbonyl)amino, cyano, formyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, carboxy, C1-4 alkylcarbonyloxy, aryl(C1-4)alkylcarbonyloxy, C1-4 alkylsulphinyl, C1-4 alkylsulphonyl, C1-4 alkylsulphonyloxy, aryl, heteroaryl, aryloxy, arylthio, heteroaryloxy or heteroarylthio wherein any of the foregoing alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, groups or moieties are optionally substituted; R1 is phenyl, cyano, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms,
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: January 23, 2007
    Assignees: Syngenta Limited, Syngenta Crop Protection, Inc.
    Inventors: William Guy Whittingham, Kevin Robert Lawson, Paul Anthony Worthington, Charles Adam Russell, Roger Salmon, Leslie Francis May, Mario Jorg, Johannes Paul Pachlatko
  • Patent number: 7153876
    Abstract: Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: August 6, 2003
    Date of Patent: December 26, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder
  • Patent number: 7153815
    Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.
    Type: Grant
    Filed: January 10, 2003
    Date of Patent: December 26, 2006
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
  • Patent number: 7151112
    Abstract: This invention is directed to methods of using a compound of the formula and pharmaceutically acceptable salts thereof, wherein n, X, R1 and R2 are disclosed herein, for treating inflammatory events in an animal subject.
    Type: Grant
    Filed: December 23, 2003
    Date of Patent: December 19, 2006
    Assignee: UCB SA
    Inventors: Neil S Cutshall, Scott C Jeffrey
  • Patent number: 7144978
    Abstract: Multi-armed functional polyethylene glycol polymers with active terminal groups may be used in conjugation with small molecule pharmaceuticals, proteins and peptides to enhance half-life and bioavailability of the drug and improve solubility, stability and immunological competence.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: December 5, 2006
    Assignee: Pan Asia Bio Co., Ltd.
    Inventors: Junlian Huang, Michael Min Xu, Xiaojian Hu, Yuhong Xu
  • Patent number: 7144897
    Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: December 5, 2006
    Assignees: Elan Oharmaceuticals, Inc., Pharmacia & Upjohn, Co.
    Inventors: John Freskos, David L. Brown, Yvette M. Fobian, Larry Fang, Arthur Glenn Romero, Varghese John
  • Patent number: 7138525
    Abstract: A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alky
    Type: Grant
    Filed: July 27, 2004
    Date of Patent: November 21, 2006
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Nagaaki Sato, Makoto Ando, Shiho Ishikawa, Tsuyoshi Nagase, Keita Nagai, Akio Kanatani
  • Patent number: 7132546
    Abstract: The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: [wherein A is CO or SO2; Cy is an aryl group or a heterocyclic group; each of R1 and R2 which are independent of each other, is a halogen atom, a cyano group, a nitro group, an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, a cycloalkyl group which may be substituted, a cycloalkenyl group which may be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an amino group which may be substituted or a —B-Q group; R3 is a -M1-M2-R5 group; R4 is a hydrogen atom or an alkyl group which may be substituted; x is an integer of from 0 to 5; y is an integer of from 0 to 4; and z is an integer of from 0 to 1].
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: November 7, 2006
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Fuminori Kato, Hirohiko Kimura, Shunji Yuki, Kazuhiro Yamamoto, Takashi Okada
  • Patent number: 7129238
    Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: October 31, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
  • Patent number: 7129246
    Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for, and intermediates used in, their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: October 31, 2006
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Timothy Johnson, Michael Stocks
  • Patent number: 7129234
    Abstract: The invention relates to compounds of formula I
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: October 31, 2006
    Assignee: Pfizer Inc.
    Inventors: Mavis D. Adam, Mark D. Andrews, Geoffrey E. Gymer, David Hepworth, Harry R. Howard, Jr., Donald S. Middleton, Alan Stobie
  • Patent number: 7122547
    Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
    Type: Grant
    Filed: November 9, 1999
    Date of Patent: October 17, 2006
    Assignees: Schering AG, Novartis AG
    Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
  • Patent number: 7115608
    Abstract: The present invention is concerned among others with compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Q is halo, C1-6 alkyl or C2-6 alkenyl; X is (a-2) with q and r being O and Z being O, S or SO; R1 is aryl; R2 is selected from formyl; C1-6alkyloxycarbonylalkyl; Het2; Het2C1-6alkyl, C1-6alkylthio; C1-6alkyl optionally substituted with one or two substituents each independently selected from hydroxy, and halo; R3 is selected from formyl; C1-6alkyl optionally substituted with one or two C1-6alkyloxy; R4 is hydrogen, with HTV inhibiting properties
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: October 3, 2006
    Assignees: Centre National de la Recherche Schentifique, Institute Curie
    Inventors: Jérôme Guillemont, Abdellah Benjahad, Dominique Mabire, Chi Hung N'Guyen, David Grierson, Claude Monneret, Emile Bisagni, Gérard Sanz, Laurence Decrane