Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/408)
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Patent number: 7511149Abstract: 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: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090082376Abstract: The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090048227Abstract: Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Pasun K. Chakravarty, Pengcheng Patrick Shao, Feng Ye
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Publication number: 20090012297Abstract: A method in one embodiment includes contacting a strongly hydrogen bonded organic material with an ionic liquid having a fluoride anion for solubilizing the strongly hydrogen bonded organic material; and maintaining the ionic liquid at a temperature of about 90° C. or less during the contacting. A method in another embodiment includes contacting a strongly hydrogen bonded organic material with an ionic liquid having an acetate or formate anion for solubilizing the strongly hydrogen bonded organic material; and maintaining the ionic liquid at a temperature of less than about 90° C. during the contacting.Type: ApplicationFiled: April 23, 2008Publication date: January 8, 2009Inventors: Philip F. Pagoria, Amitesh Maiti, Alexander Gash, Thomas Yong Han, Christine Orme, Laurence Fried
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Publication number: 20090012093Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: November 6, 2003Publication date: January 8, 2009Inventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
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Publication number: 20090012062Abstract: The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: ApplicationFiled: December 18, 2006Publication date: January 8, 2009Inventors: Jose Ignacio Andres-Gil, Manuel Jesus Alcazar-Vaca, Rosa Maria Alvarez-Escobar, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Jacqueline Macritchie, Donald Simpson, Sonia Martinez Gonzalez
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Publication number: 20080293742Abstract: The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R1-R5 are as defined in the specification; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapyType: ApplicationFiled: December 11, 2006Publication date: November 27, 2008Inventors: David Cheshire, Nicholas Kindon, Antonio Mete, Bryan Roberts
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Publication number: 20080280877Abstract: The invention relates to EP2 antagonist azetidines of formula (I) wherein Ar, R1, X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.Type: ApplicationFiled: May 5, 2008Publication date: November 13, 2008Inventors: Kevin Neil Dack, Sarah Elizabeth Skerratt, Siew Kuen Yeap
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Publication number: 20080161292Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: December 27, 2007Publication date: July 3, 2008Applicant: Abbott LaboratoriesInventors: Vincent L. Giranda, Julie M. Miyashiro, Thomas D. Penning, Keith W. Woods
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Patent number: 7371743Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: February 11, 2005Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7342019Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attaType: GrantFiled: December 18, 2002Date of Patent: March 11, 2008Assignee: AstraZeneca ABInventors: Anna Ingrid Kristina Berggren, Stig Jonas Boström, Stig Thomas Elebring, Peter Greasley, Emma Terricabras, Johan Michael Wilstermann
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Patent number: 7273867Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disordersType: GrantFiled: December 5, 2001Date of Patent: September 25, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
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Patent number: 7265108Abstract: Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(=Q1)- (wherein Q1 represents oxygen, sulfur or ?N—R11 (wherein R11 represents hydrogen or C1-6 alkyl)) and nitrogen, etc.; and Z1 represents piperidin-diyl, etc.], salts thereof and hydrates of the foregoing.Type: GrantFiled: July 1, 2005Date of Patent: September 4, 2007Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Mutsuko Ono, Koki Kawano, Yoshihiko Norimine, Tatsuhiro Onogi, Takashi Yoshinaga, Kiyoaki Kobayashi, Hiroyuki Suzuki, Hiroe Minami, Kohei Sawada
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7205306Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: May 14, 2002Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G Arvanitis, Paul J Gilligan, Richard A Hartz
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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: 7179807Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: August 20, 2003Date of Patent: February 20, 2007Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Stéphane De Lombaert, Raymond F. Horvath, Dario Doller, Kevin J. Hodgetts, Lu Yan Zhang, Bernd Kaiser, Xuechun Zhang, Yasuchika Yamaguchi, Cunyu Zhang, Jim Darrow
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7132425Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.Type: GrantFiled: December 10, 2003Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Patent number: 7132424Abstract: This invention provides compounds defined by Formula I R1-Q-D-(V1)m—R2I or a pharmaceutically acceptable salt thereof, wherein R1, Q, D, V1, m, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition.Type: GrantFiled: August 5, 2003Date of Patent: November 7, 2006Assignee: Warner-Lambert Company LLCInventor: Joseph Armand Picard
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7119094Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: November 20, 2000Date of Patent: October 10, 2006Assignee: Warner-Lambert CompanyInventors: Michael S. South, John J. Parlow, Darin E. Jones, Brenda Case, Tom Dice, Richard Lindmark, Michael J. Hayes, Melvin L. Rueppel, Rick Fenton, Gary W. Franklin, Horng-Chih Huang, Wei Huang, Carrie Kusturin, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney
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Patent number: 7105522Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is hydrogen, hydroxy, cyano, amino, mono-or di(C1-4alkyl)amino, formyl, carboxyl, C1-6alkyl, hydroxyC1-6alkyl, polyhaloC1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkylcarbonyl, aminocarbonyl, —S(?O)m—NH2, mono-or di(C1-4alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, aryl, arylC1-6alkyl or aryloxy; R2 is hydrogen; halo; mercapto; formyl; cyano; carboxy; azido; hydroxy; oxiranyl; amino; mono- or di(C1-4alkyl)amino; formylamino; R5R6N—C(?O)—; R7—N?C(R8)—; C1-6alkyl-S(?O)m; aryl-S(?O)m; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C1-6alkyloxy; hydroxyC1-6alkyloxy; aminoC1-6alkyloxy; mono- or di(C1-4alkyl)amino-C1-6alkyloxy; C1-6alkylcarbonyl; arylcarbonyl; Het1carbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aryl; aryloxy; arylC1-6alkyloxy; arylthio; arylC1Type: GrantFiled: March 13, 2002Date of Patent: September 12, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Paul Adriaan Jan Janssen, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Lucien Maria Henricus Koymans, Marc René de Jonge, Jan Heeres, Frederik Frans Desire Daeyaert, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Amuri Kilonda
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Patent number: 7064201Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.Type: GrantFiled: August 1, 2003Date of Patent: June 20, 2006Assignee: Nereus Pharmaceuticals, Inc.Inventors: Yoshio Hayashi, Michael A. Palladino, Jr., Jennifer Grodberg
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Patent number: 7056925Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: August 13, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Gaoquan Li, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Hing L. Sham, Gary T. Wang
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Patent number: 7041667Abstract: Compounds of Formula 1 [Region ?]—[Region ?]—[Region ?]—[Region ?]??(1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: May 9, 2006Assignee: Pfizer, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 6995161Abstract: Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.Type: GrantFiled: February 16, 2001Date of Patent: February 7, 2006Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Raymond F. Horvath, Stephane DeLombaert, Kevin J. Hodgetts, Dario Doller, Cunyu Zhang
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Patent number: 6964965Abstract: The present invention provides substituted pyrazine derivatives of Formula I, that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.Type: GrantFiled: April 17, 2003Date of Patent: November 15, 2005Assignee: Pharmacia & UpjohnInventors: Jeffrey W. Corbett, Michael Dalton Ennis, Kristine E. Frank, Jian-Min Fu, Robert Louis Hoffman, Patrick R. Verhoest
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Patent number: 6949551Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides What is described are dihalopropene compounds of the formula (I) in which R1 and R2 are halogen, Y is —O—, —S— or —NH—, X is —O—, —S(O)r— or —NR5— (where r=0, 1, 2 and R5 is hydrogen or C1-C8-alkyl), X? is a direct C—C bond, —O—, —S(O)r— or —NR5— (where R5 is as defined above), R3 is hydrogen, halogen, nitro, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C10-cycloalkyl or has one of the meanings defined for A, A has the meaning given in the description (inter alia aryl, heterocyclyl), B is a divalent bridge having the meanings given in the description (inter alia alkylene) and R4 is a monovalent C6-C14-aryl radical or nitrogen-containing heteroaryl radical having at least one ring heteroatom which has the meanings given in the description. These compounds can be used for preparing pesticides.Type: GrantFiled: November 7, 2002Date of Patent: September 27, 2005Assignee: Bayer Cropscience S.A.Inventors: Jörg Tiebes, Ralf Braun, Joachim Dickhaut, Harald Jakobi, Stephen Lindell, Vincent L. Salgado, Eva Wojtech, Daniela Jans, Jutta Maria Waibel, Waltraud Hempel, Ronald Wilhelm
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Patent number: 6900210Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Qiang Sun, Jie Chen, Huan He
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Patent number: 6867210Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: March 12, 2001Date of Patent: March 15, 2005Assignee: Euro-Celtique S.A.Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Patent number: 6806369Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: November 5, 2002Date of Patent: October 19, 2004Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Publication number: 20040198728Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.Type: ApplicationFiled: September 22, 2003Publication date: October 7, 2004Applicant: Cell Therapeutics, Inc.Inventors: Feng Hong, J. Peter Klein
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Patent number: 6787544Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: February 20, 2001Date of Patent: September 7, 2004Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura
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Publication number: 20040147748Abstract: The present invention provides a compound according to formula I 1Type: ApplicationFiled: December 10, 2003Publication date: July 29, 2004Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Publication number: 20040102448Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of dirombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: October 23, 2003Publication date: May 27, 2004Applicant: Pharmacia CorporationInventors: Michael S. South, John J. Parlow, Darin E. Jones, Brenda Case, Tom Dice, Richard Lindmark, Michael J. Hayes, Melvin L. Rueppel, Horng-Chih Huang, Wei Huang, Scott A. Long, Matthew W. Mahoney, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Rick Fenton, Gary W. Franklin, Carrie Kusturin
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Patent number: 6713472Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.Type: GrantFiled: January 18, 2002Date of Patent: March 30, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
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Patent number: 6706021Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: March 27, 2003Date of Patent: March 16, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6699856Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.Type: GrantFiled: July 25, 2002Date of Patent: March 2, 2004Assignee: Merck & Co., Inc.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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Publication number: 20040029883Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.Type: ApplicationFiled: November 19, 2002Publication date: February 12, 2004Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
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Publication number: 20040029886Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticidesType: ApplicationFiled: November 7, 2002Publication date: February 12, 2004Inventors: Jorg Tiebes, Ralf Braun, Joachim Dickhaut, Harald Jakobi, Stephen Lindell, Vincent L. Salgado, Eva Wojtech, Daniela Jans, Jutta Maria Waibel, Waltraud Hempel, Ronald Wilhelm
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Patent number: 6689781Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.Type: GrantFiled: July 20, 2001Date of Patent: February 10, 2004Assignees: Elan Pharmaceuticals, Inc., American Home Products CorporationInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Publication number: 20040006230Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: July 15, 2002Publication date: January 8, 2004Applicant: Pharmacia CorporationInventors: Michael S. South, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Gary W. Franklin, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, Carrie L. Kusturin, Richard J. Lindmark, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney, John J. Parlow, Melvin L. Rueppel
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Patent number: 6673795Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification. The invention is a pharmaceutical composition containing an effective amount of the compound of formula 1, its preparation and to a method of treatment, control or prevention of acute and/or chronic neurological disorders by administering a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: May 29, 2002Date of Patent: January 6, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Hans-Peter Maerki, Thierry Masquelin, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
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Publication number: 20030236402Abstract: Compounds represented by formula I: 1Type: ApplicationFiled: July 25, 2002Publication date: December 25, 2003Applicant: Merck Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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Publication number: 20030220339Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.Type: ApplicationFiled: January 29, 2003Publication date: November 27, 2003Applicant: Tularik Inc.Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman