Halogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/334)
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Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 6984735Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.Type: GrantFiled: November 26, 2003Date of Patent: January 10, 2006Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
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Patent number: 6982331Abstract: The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl2). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. Phosgene may be replaced by equivalent reagents. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.Type: GrantFiled: June 27, 2003Date of Patent: January 3, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Timothy J. Doyle, Alan H. Benke, Peter K. Wehrenberg, Louie A. Nady, Gilbert Rodriguez
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Patent number: 6946555Abstract: The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: ?wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: ?wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.Type: GrantFiled: February 19, 2003Date of Patent: September 20, 2005Assignee: Pfizer IncInventors: Michael Butters, Alan John Pettman
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Patent number: 6887875Abstract: Diarylpyrimidine compounds of Formula I are provided, wherein.Type: GrantFiled: May 22, 2002Date of Patent: May 3, 2005Assignee: Neurogen CorporationInventors: Jianhua Huang, Kevin Hodggetts, Dario Doller, Ping Ge, Yasuchika Yamaguchi
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Patent number: 6844351Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: May 31, 2000Date of Patent: January 18, 2005Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Publication number: 20040266774Abstract: The present invention is a compound and pharmaceutical composition comprising a compound of formula (I): 1Type: ApplicationFiled: June 14, 2004Publication date: December 30, 2004Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Kiyotaka Ito, Glen W. Spears, Fumie Takahashi, Akira Yamada, Masaki Tomishima, Hiroshi Miyake
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Publication number: 20040259887Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: ApplicationFiled: May 13, 2004Publication date: December 23, 2004Applicant: Pfizer IncInventor: Robert L. Dow
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Patent number: 6822095Abstract: The present invention relates to a process for preparing 4,6-dichloropyrimidine by reaction of 4-chloro-6-hydroxypyrimidine with an acid chloride.Type: GrantFiled: December 19, 2001Date of Patent: November 23, 2004Assignee: Bayer AktiengesellschaftInventors: Franz-Josef Mais, Günther Cramm, Alexander Klausener, Guido Steffan
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Patent number: 6818631Abstract: Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).Type: GrantFiled: August 15, 2003Date of Patent: November 16, 2004Assignee: Nippon Soda Co. Ltd.Inventors: Yuki Nakagawa, Sergey Bobrov, Charles R. Semer, IV, Thomas A. Kucharek, Masahiro Haramoto
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Patent number: 6809109Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: June 25, 2003Date of Patent: October 26, 2004Assignee: Bristol-Myers Squibb CompanyInventors: James D. Rodgers, Haisheng Wang
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Publication number: 20040186321Abstract: The invention relates to a method for producing ketones by reacting boric acid derivates with carbocylic acid anhydrides in the presence of a transition metal catalyst. The carboxylic acid anhydrides can either be used in isolated form or produced from carboxylic acids in a reaction mixture. This method enables the simple embodiment of a multitude of functionalised ketones in a single reaction step.Type: ApplicationFiled: May 25, 2004Publication date: September 23, 2004Inventors: Lukas Goossen, Keya Ghosh
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Publication number: 20040133001Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: February 18, 2004Publication date: July 8, 2004Inventors: Jia-Ning Xiang, Siegfried B. Christensen IV, Jinhwa Lee
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Patent number: 6759101Abstract: Compounds that are useful as components in liquid crystal compositions, particularly in ferroelectric liquid crystal compositions. Compounds of the invention are rod-like molecules with a mesogenic (generally linear) core to which an alkene tail and an alkyl or alkoxy tail with a perfluoroalkyl terminal portion are bonded. Compounds of the invention can contain a variety of one, two or three ring cores, wherein the rings maybe aromatic or alicyclic. Alkenes of the invention are useful as components to improve LC properties of mixtures, for example, to lower melting point of lower freezing point, of LC compositions.Type: GrantFiled: January 3, 2001Date of Patent: July 6, 2004Assignee: Displaytech, Inc.Inventors: Neil Gough, Rohini Vohra, Michael Wand, Kundalika More, William N. Thurmes
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Publication number: 20040116445Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: ApplicationFiled: November 18, 2003Publication date: June 17, 2004Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Matthew S. Miller, Rabindranath Tripathy, Jeffry L. Vaught
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Publication number: 20040097508Abstract: Amides of the general formula I 1Type: ApplicationFiled: June 23, 2003Publication date: May 20, 2004Inventors: Wilfried Lubisch, Achim Moller, Hans-Jorg Treiber, Monika Knopp
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Publication number: 20040082785Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.Type: ApplicationFiled: November 26, 2003Publication date: April 29, 2004Applicant: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
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Patent number: 6727241Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.Type: GrantFiled: June 12, 2002Date of Patent: April 27, 2004Assignee: ChemocentryxInventor: Brian McMaster
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Publication number: 20040058937Abstract: Pleuromutilin compounds of the formula: 1Type: ApplicationFiled: October 17, 2003Publication date: March 25, 2004Inventors: Steven Aitken, Gerald Brooks, Steven Dabbs, Colin Henry Frydrych, Steven Howard, Eric Hunt
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Publication number: 20040054181Abstract: The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl2). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. Phosgene may be replaced by equivalent reagents. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.Type: ApplicationFiled: June 27, 2003Publication date: March 18, 2004Inventors: Timothy J. Doyle, Alan H. Benke, Peter K. Wehrenberg, Louie A. Nady, Gilbert Rodriguez
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Patent number: 6686469Abstract: The invention relates to compounds of the general formula wherein R1 is unsubstituted or mono- to penta-substituted aryl, whereby the substituents are selected from the group consisting for instance of OH, Halogen, CN, C1-C6-alkyl, optionally substituted C3-C8-cycloalkyl and optionally substituted C3-C8-cycloalkenyl; A is for instance a single bond, C1-C12-alkylene or O; X1 and X2, independently of one another, are R10; X3 is H or R10; R10 is for instance halogen, CN, NO2, C1-C6-alkyl, C3-C8-cycloalkyl or C1-C6-haloalkyl; R21 and R22, independently of one another are for instance H, halogen, CN, NO2, OH, SH, C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-alkyl-C3-C8-cycloalkyl or C3-C8-cycloalkyl-C1-C6-alkyl; R23 and R24, independently of one another, are for instance H, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C1-C6-haloalkyl or C3-C8-halocycloalkyl; m is 1, 2, 3 or 4; and n is 0, 1 or 2; as well as the physiologically acceptable addition compounds, a method of producingType: GrantFiled: November 5, 2001Date of Patent: February 3, 2004Assignee: Novartis Animal Health US, Inc.Inventors: Martin Eberle, André Jeanguenat, Werner Zambach, Arthur Steiger, Saleem Farooq
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Publication number: 20040019037Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: ApplicationFiled: July 10, 2003Publication date: January 29, 2004Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Patent number: 6680385Abstract: A method for the preparation of aryl methyl ketones converts a variety of ethyl arenas to the corresponding aryl methyl ketones using a dioxygen-containing gas as the oxidant. The catalyst used for the reaction is a metal complex bearing general formulas as disclosed.Type: GrantFiled: January 25, 2002Date of Patent: January 20, 2004Assignees: The Hong Kong Polytechnic University, Sichuan UniversityInventors: Albert Sun-Chi Chan, Jian-Ying Qi, Cheng-Chao Pai, Xian-Jun Li, Li-Sheng Deng, Wen-Zao Li, Bin Sun, Jia-Yuan Hu
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Publication number: 20030232842Abstract: Novel dihydropyrimidines and combinations thereof with other antiviral agents, suitable for combating HBV infections.Type: ApplicationFiled: March 10, 2003Publication date: December 18, 2003Inventors: Siegfried Goldmann, Jurgen Stoltefuss, Ulrich Niewohner, Karl-Heinz Schlemmer, Jorg Keldenich, Arnold Paessens, Erwin Graef, Olaf Weber, Karl Deres
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6635767Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: GrantFiled: December 12, 2000Date of Patent: October 21, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
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Publication number: 20030195354Abstract: An amide compound given by formula [I]: 1Type: ApplicationFiled: December 12, 2002Publication date: October 16, 2003Inventor: Hiroshi Sakaguchi
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Publication number: 20030181718Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: ApplicationFiled: February 10, 2003Publication date: September 25, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6613909Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: GrantFiled: December 6, 2001Date of Patent: September 2, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
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Patent number: 6600044Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.Type: GrantFiled: June 18, 2001Date of Patent: July 29, 2003Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
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Patent number: 6589947Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.Type: GrantFiled: October 26, 2000Date of Patent: July 8, 2003Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Ernest S. Hamanaka, Yuhpyng Liang Chen
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Patent number: 6576303Abstract: Novel liquid crystal compound having a negative and absolutely large value of dielectric anisotropy, being excellent in compatibility with other liquid crystalline compounds at a low temperature and being stable chemically and physically, as well as a liquid crystal composition comprising this compound, and a liquid crystal display device comprising this liquid crystal composition are provided, said compound is expressed by the general formula (1): R1—A1—B1—A2—B2—A3—B3—Z—B4—A4—R2 (1) wherein A1, A2, A3 and A4 represent a single bond, 1,4-cyclohexylene, 1,4-phenylene which may be substituted with a fluorine atom(s) or the like; B1, B2, B3 and B4 represent a single bond, 1,2-ethylene, 1,2-ethenylene, 1,2-ethynylene, oxymethylene, methyleneoxy or the like; R1 and R2 represent an alkyl group having 1 to 10 carbon atoms or the like; and Z represents (I) to (VI): wherein X represents H or F, and Y represents difluoromethyl grType: GrantFiled: August 24, 2000Date of Patent: June 10, 2003Assignee: Chisso CorporationInventors: Norio Tamura, Atsuko Fujita, Hiroyuki Tekeuchi, Fusayuki Takeshita, Etsuo Nakagawa
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Patent number: 6555684Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.Type: GrantFiled: October 9, 2001Date of Patent: April 29, 2003Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Grayland Page Dobson
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Patent number: 6537996Abstract: Compounds of formula 1 are effective modulators of p38 MAP kinase. wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl; and A is —CH— or —N—; and pharmaceutically acceptable salts thereof.Type: GrantFiled: February 23, 2001Date of Patent: March 25, 2003Assignee: Iconix Pharmaceuticals, Inc.Inventors: David J. Morgans, Jr., Silke Thode, Dongxu Sun
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Patent number: 6525198Abstract: The invention relates to a method for the preparation of 4,6-dichloropyrimidine by reacting 4-chloro-6-methoxypyrimidine with at least one sulphur-containing chlorinating agent selected from the group consisting of SCl2, SOCl2, and SO2Cl2 in the presence of at least one phosphorus compound having the formula R3P═Yn (1), in which R represents C1-C10-alkyl or C6-C10-aryl, each of which may optionally be substituted by up to five identical or different substituents selected from the group consisting of fluorine, chlorine, bromine, C1-C4-alkyl, and C1-C4-alkoxy, Y represents oxygen or sulphur, and n represents zero or 1.Type: GrantFiled: February 7, 2002Date of Patent: February 25, 2003Assignee: Bayer AktiengesellschaftInventors: Franz-Josef Mais, Alexander Klausener, Günther Cramm, Guido Steffan
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Patent number: 6525001Abstract: Compounds of formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation, wherein J is (J-1), (J-2), (J-3), (J-4), (J-5), (J-6) or (J-7); and J, W, X, Y, Z, A, R1-R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of formula (I).Type: GrantFiled: June 2, 2000Date of Patent: February 25, 2003Assignee: Mid-American Commercialization CorporationInventors: Gerard Michael Koether, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Publication number: 20030004348Abstract: Disclosed are a fluorinating agent represented by the general formula (1): 1Type: ApplicationFiled: July 10, 2002Publication date: January 2, 2003Inventors: Hiroshi Sonoda, Kazunari Okada, Akira Takahashi, Kouki Fukumura, Hidetoshi Hayashi, Teruyuki Nagata, Yasuhiro Takano
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Publication number: 20020195585Abstract: Compounds that are useful as components in liquid crystal compositions, particularly in ferroelectric liquid crystal compositions. Compounds of the invention are rod-like molecules with a mesogenic (generally linear) core to which an alkene tail and an alkyl or alkoxy tail with a perfluoroalkyl terminal portion are bonded. Compounds of the invention can contain a variety of one, two or three ring cores, wherein the rings maybe aromatic or alicyclic. Alkenes of the invention are useful as components to improve LC properties of mixtures, for example, to lower melting point of lower freezing point, of LC compositions.Type: ApplicationFiled: January 3, 2001Publication date: December 26, 2002Inventors: Neil Gough, Rohini Vohra, Michael Wand, Kundalika More, William N. Thurmes
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Patent number: 6492363Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: August 16, 2001Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6491989Abstract: Fluorinated naphthalene derivatives of the formula (I) R1(—A1—M1)a(—A2—M2)b—B—(—M3—A3)c—(M4—A4)d—R2 (I) where B is having the meaning and R1(—A1—M1)a(—A2—M2) and (—M3—A3)(M4—A4)R2 are mesogenic radicals, are suitable as components of liquid-crystal mixtures, in particular ferroelectric liquid-crystal mixtures.Type: GrantFiled: July 10, 2000Date of Patent: December 10, 2002Assignee: Aventis Reseach & Technologies GmbH & Co. KGInventors: Javier Manero, Wolfgang Schmidt, Barbara Hornung
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Patent number: 6485797Abstract: A ferroelectric liquid crystal mixture, especially useful for operation in the &tgr;Vmin−mode, comprises a 5-Arylindane derivative of the formula (I), wherein Y is CH, CF or N and R1(—A1—M1)a(—A2—M2)b—, (M3—A3—)cR2 are mesogenic groups.Type: GrantFiled: August 31, 2000Date of Patent: November 26, 2002Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Wolfgang Schmidt, Javier Manero, Barbara Hornung, Rainer Wingen, Ayako Ogawa
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Publication number: 20020147204Abstract: A compound of the formula: 1Type: ApplicationFiled: March 26, 2002Publication date: October 10, 2002Applicant: Sumitomo Pharmaceuticals Company, LimitedInventors: Kazuhito Ikeda, Tohru Tatsuno, Hiroki Ogo, Toshio Nishihara, Tatsuya Fujibayashi, Ryu Nagata
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Patent number: 6444817Abstract: Compounds of the formula where A, B, D, R1 and R2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases. The novel compounds are prepared via compounds of the formula H2N—CH2—G—M.Type: GrantFiled: October 8, 1999Date of Patent: September 3, 2002Assignee: Abbott LaboratoriesInventors: Hans-Joachim Böhm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
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Patent number: 6441171Abstract: The invention relates to a method for the preparation of 4,6-dichloropyrimidine by reacting 4-chloro-6-methoxypyrimidine with phosgene as chlorinating agent in the presence of a nitrogen-containing auxiliary.Type: GrantFiled: January 24, 2002Date of Patent: August 27, 2002Assignee: Bayer AktiengesellschaftInventors: Franz-Josef Mais, Günther Cramm, Alexander Klausener, Guido Steffan
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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
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Patent number: RE39127Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39129Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39130Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: June 6, 1994Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39131Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atoms or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5-or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori