Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/300)
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Patent number: 7517880Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 1, 2002Date of Patent: April 14, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Patent number: 7514564Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: May 2, 2006Date of Patent: April 7, 2009Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
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Publication number: 20090088458Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: July 28, 2006Publication date: April 2, 2009Inventors: Robert S. Meissner, James J. Perkins, Yuntae Kim, Barbara Hanney, Carol A. McVean
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Publication number: 20090054436Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: October 17, 2008Publication date: February 26, 2009Inventors: Robert M. Borzilleri, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20090048309Abstract: 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: ApplicationFiled: January 25, 2006Publication date: February 19, 2009Applicant: Shenyang Research Institute of Chemical IndustryInventors: Chunhe Yang, Liwen Geng, Defeng Zhou, Ling Peng, Hong Zhang, Dongliang Cui, Zhinian Li, Liangqing Wang, Shouguo Zang, Zeyong Zhang
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Publication number: 20080312262Abstract: 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: ApplicationFiled: August 21, 2008Publication date: December 18, 2008Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
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Publication number: 20080306108Abstract: 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: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: MEDICURE INTERNATIONAL INC.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Wenlian Zhang
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Patent number: 7459469Abstract: 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: GrantFiled: November 9, 2005Date of Patent: December 2, 2008Assignee: Targacept, Inc.Inventors: Julio A. Munoz, John Genus, James R. Moore
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Patent number: 7459562Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: GrantFiled: April 21, 2005Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Lyndon A. M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Patent number: 7456290Abstract: 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: GrantFiled: November 18, 2003Date of Patent: November 25, 2008Assignee: Bayer Cropscience S.A.Inventor: Manuel Vangelisti
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Publication number: 20080287505Abstract: 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: ApplicationFiled: May 19, 2008Publication date: November 20, 2008Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20080280895Abstract: The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g.Type: ApplicationFiled: March 17, 2005Publication date: November 13, 2008Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Michael Quirmbach, Dirk Behnke, Christiane Marti
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Publication number: 20080275044Abstract: 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: ApplicationFiled: April 11, 2008Publication date: November 6, 2008Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Patent number: 7446117Abstract: 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: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Publication number: 20080269265Abstract: 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: ApplicationFiled: June 25, 2008Publication date: October 30, 2008Inventors: 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
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Publication number: 20080262039Abstract: 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: ApplicationFiled: April 15, 2008Publication date: October 23, 2008Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Michael Przewosny, Bernd Sundermann, Jewoo Lee
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Publication number: 20080255208Abstract: 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: ApplicationFiled: September 12, 2006Publication date: October 16, 2008Applicant: Bayer CropScience AGInventors: 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
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Publication number: 20080255124Abstract: 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: ApplicationFiled: October 13, 2005Publication date: October 16, 2008Applicant: Smithkline Beecham CorporationInventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
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Publication number: 20080255134Abstract: 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: ApplicationFiled: November 8, 2005Publication date: October 16, 2008Applicant: Artesian Therapeutics, Inc.Inventors: Malcolm George Taylor, Burkhard Klenke, Peter D. Suzdak, Reza Mazhari
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Patent number: 7425570Abstract: 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: GrantFiled: December 21, 2004Date of Patent: September 16, 2008Assignee: Medicure International Inc.Inventor: Wasimul Haque
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Publication number: 20080221132Abstract: 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: ApplicationFiled: September 10, 2007Publication date: September 11, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20080194645Abstract: 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: ApplicationFiled: January 14, 2008Publication date: August 14, 2008Inventors: Linus S. Lin, William K. Hagmann, Sanjeev Kumar, Wenji Yin, George Doss
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Patent number: 7407959Abstract: 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: GrantFiled: November 18, 2005Date of Patent: August 5, 2008Assignee: Merck Frosst Canada & Co.Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
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Publication number: 20080166299Abstract: 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: ApplicationFiled: December 6, 2007Publication date: July 10, 2008Applicant: Trustees of The University of PennsylvaniaInventors: Hank F. Kung, Mei Ping Kung
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Patent number: 7384967Abstract: 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: GrantFiled: October 6, 2003Date of Patent: June 10, 2008Assignee: Novo Nordisk A/SInventors: 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
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Publication number: 20080124402Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: October 25, 2005Publication date: May 29, 2008Applicant: MERCK & CO., INC.Inventors: Yuntae Kim, Joshua Close, Mark E. Duggan, Barbara Hanney, Robert S. Meissner, Jeffrey Musselman, James J. Perkins, Jiabing Wang
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Patent number: 7378446Abstract: 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: GrantFiled: July 9, 2004Date of Patent: May 27, 2008Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki, Takeshi Murata, Fumio Watanabe, Hiroshi Fukuda, Susumu Komiyama, Tadakatsu Hayase
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Patent number: 7365085Abstract: 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: GrantFiled: March 26, 2003Date of Patent: April 29, 2008Assignee: SmithKline Beecham CorporationInventors: Ajita Bhat, John Jeffrey McAtee, Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Robert A. Stavenger
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Publication number: 20080081825Abstract: 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: ApplicationFiled: April 27, 2005Publication date: April 3, 2008Inventors: Hisao Nakai, Shingo Yamamoto, Masafumi Sugitani
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Patent number: 7342115Abstract: 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: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7332608Abstract: 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: GrantFiled: November 9, 2006Date of Patent: February 19, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 7320993Abstract: 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: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7307092Abstract: 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: GrantFiled: April 20, 2006Date of Patent: December 11, 2007Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Patent number: 7235566Abstract: Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.Type: GrantFiled: July 28, 2004Date of Patent: June 26, 2007Assignee: 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
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Patent number: 7214799Abstract: 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: GrantFiled: February 9, 2005Date of Patent: May 8, 2007Assignee: BioStratum, Inc.Inventors: Raja Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
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Patent number: 7205302Abstract: 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: GrantFiled: April 25, 2002Date of Patent: April 17, 2007Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
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Patent number: 7202260Abstract: 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: GrantFiled: June 14, 2004Date of Patent: April 10, 2007Assignee: Schering AGInventors: Andreas Huth, Martin Krueger, Ludwig Zorn, Stuart Ince, Rolf Bohlmann, Karl Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
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Patent number: 7199265Abstract: 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: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
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Patent number: 7189383Abstract: 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: GrantFiled: August 1, 2003Date of Patent: March 13, 2007Assignee: Mallinckrodt Inc.Inventor: John J. R. Mertens
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Patent number: 7175872Abstract: 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: GrantFiled: March 2, 2004Date of Patent: February 13, 2007Assignee: Nestec S.A.Inventors: Thomas Hofmann, Harald Ottinger, Oliver Frank, Tomislav Soldo, Imre Blank, Renaud Villard, Fabien Robert
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Patent number: 7166621Abstract: 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: GrantFiled: November 25, 2002Date of Patent: January 23, 2007Assignees: 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
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Patent number: 7153815Abstract: 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: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7153876Abstract: 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: GrantFiled: August 6, 2003Date of Patent: December 26, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 7151112Abstract: 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: GrantFiled: December 23, 2003Date of Patent: December 19, 2006Assignee: UCB SAInventors: Neil S Cutshall, Scott C Jeffrey
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Patent number: 7144897Abstract: 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: GrantFiled: May 31, 2002Date of Patent: December 5, 2006Assignees: Elan Oharmaceuticals, Inc., Pharmacia & Upjohn, Co.Inventors: John Freskos, David L. Brown, Yvette M. Fobian, Larry Fang, Arthur Glenn Romero, Varghese John
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Patent number: 7144978Abstract: 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: GrantFiled: July 15, 2004Date of Patent: December 5, 2006Assignee: Pan Asia Bio Co., Ltd.Inventors: Junlian Huang, Michael Min Xu, Xiaojian Hu, Yuhong Xu
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Patent number: 7138525Abstract: 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 alkyType: GrantFiled: July 27, 2004Date of Patent: November 21, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Nagaaki Sato, Makoto Ando, Shiho Ishikawa, Tsuyoshi Nagase, Keita Nagai, Akio Kanatani
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Patent number: 7132546Abstract: 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: GrantFiled: December 21, 2001Date of Patent: November 7, 2006Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Hirohiko Kimura, Shunji Yuki, Kazuhiro Yamamoto, Takashi Okada
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Patent number: 7129238Abstract: 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: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7129234Abstract: The invention relates to compounds of formula IType: GrantFiled: November 25, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventors: Mavis D. Adam, Mark D. Andrews, Geoffrey E. Gymer, David Hepworth, Harry R. Howard, Jr., Donald S. Middleton, Alan Stobie