Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/375.1)
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Patent number: 6987112Abstract: The present invention is directed to compounds represented by Formula (1); wherein A, R, X, Y and n are as defined in the description, the salts thereof, and insecticide/acaricide compositions characterized by comprising one or more of said compounds and/or said salts as the active ingredients.Type: GrantFiled: November 1, 2001Date of Patent: January 17, 2006Assignee: Nippon Soda Co., Ltd.Inventors: Yasushi Shibata, Renpei Hatano, Takao Iwasa, Satoru Makita, Daisuke Hanai, Masao Yamaguchi, Naomi Ichikawa
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Patent number: 6972287Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).Type: GrantFiled: May 31, 2000Date of Patent: December 6, 2005Assignee: Pfizer Inc.Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
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Patent number: 6967196Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.Type: GrantFiled: February 22, 2000Date of Patent: November 22, 2005Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
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Patent number: 6964978Abstract: The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention.Type: GrantFiled: December 6, 2000Date of Patent: November 15, 2005Assignee: Pharmacia CorporationInventors: Michael J. Hageman, Xiaorong He, Tugrul T. Kararli, Lesley A. Mackin, Patricia J. Miyake, Brian R. Rohrs, Kevin J. Stefanski
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Patent number: 6958339Abstract: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.Type: GrantFiled: February 2, 2001Date of Patent: October 25, 2005Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Jun Ishikawa, Makoto Takeuchi
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Patent number: 6953860Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.Type: GrantFiled: June 12, 2003Date of Patent: October 11, 2005Inventors: Ahmed F. Abdel-Magid, Bruce D. Harris, Cynthia A. Maryanoff
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Patent number: 6949578Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.Type: GrantFiled: July 14, 2004Date of Patent: September 27, 2005Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
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Patent number: 6906196Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted arylType: GrantFiled: September 18, 2002Date of Patent: June 14, 2005Assignee: Onconova Therapeutics, Inc.Inventors: M. V. Ramana Reddy, Stanley C. Bell
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Patent number: 6903092Abstract: Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: June 7, 2005Inventor: Peter Bernstein
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6872711Abstract: The present invention relates to novel ?-substituted-?-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.Type: GrantFiled: October 22, 2001Date of Patent: March 29, 2005Assignee: Ilex Oncology Research S.A.Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
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Patent number: 6872741Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).Type: GrantFiled: September 11, 2003Date of Patent: March 29, 2005Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Publication number: 20040248943Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: December 9, 2004Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20040230060Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III 1Type: ApplicationFiled: June 12, 2003Publication date: November 18, 2004Inventors: Ahmed F. Abdel-Magid, Bruce D. Harris, Cynthia A. Maryanoff
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Publication number: 20040198780Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: March 23, 2004Publication date: October 7, 2004Applicant: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Publication number: 20040192930Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.Type: ApplicationFiled: November 3, 2003Publication date: September 30, 2004Applicant: G.D. Searle & Co.Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter, Stephen H. Docter, Stella S. Yu
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Patent number: 6770597Abstract: The compound of the formula: wherein Y, X, Z, T and Q are defined in the specification,Type: GrantFiled: July 17, 2002Date of Patent: August 3, 2004Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Masamitsu Tsukamoto, Mark Read
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Patent number: 6759538Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: GrantFiled: November 1, 2002Date of Patent: July 6, 2004Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Henry Lu, Sarkiz D. Issankani, Thomas Sun
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Publication number: 20040116353Abstract: The invention relates to compounds of formula: 1Type: ApplicationFiled: September 18, 2003Publication date: June 17, 2004Inventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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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: 20040092495Abstract: The present invention relates to biguanide derivatives of formula (I), wherein R1, R2, R3 and R4 have the meanings as given in claim (1). Compounds are useful in the treatment of pathologies associated with hyperglycaemia, such as diabetes.Type: ApplicationFiled: September 22, 2003Publication date: May 13, 2004Inventors: Gerard Moinet, Daniel Cravo
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Patent number: 6696477Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation. Compounds of particular interest are defined by Formula I wherein A, Y, R1, R2, R3, R4 and R5 are as defined in the specification.Type: GrantFiled: November 29, 2001Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas
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Patent number: 6686318Abstract: The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R1, R2, R3, R4 and Z have the meanings given in the description, to a process for their preparation, and to their use as herbicides.Type: GrantFiled: April 22, 2003Date of Patent: February 3, 2004Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Kurt Findeisen, Joachim Kluth, Karl-Heinz Linker, Klaus-Helmut Müller, Otto Schallner, Markus Dollinger
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6673818Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: April 16, 2002Date of Patent: January 6, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Patent number: 6649629Abstract: The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhType: GrantFiled: December 22, 2000Date of Patent: November 18, 2003Assignee: Nitromed, Inc.Inventors: Upul K. Bandarage, Xinqin Fang, David S. Garvey, L. Gordon Letts, Joseph D. Schroeder, Sang William Tam
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Publication number: 20030208067Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: May 28, 2002Publication date: November 6, 2003Inventors: Sheldon Xiaodong Cao, David Paul Dumas, Xiaohua Chen, Jae Young Yang
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Patent number: 6638321Abstract: The invention relates to novel monobenzene oxidation bases containing at least one cationic group Z, Z being chosen from aliphatic chains containing at least one quaternized unsaturated ring, to their use for the oxidation dyeing of keratin fibers, to dye compositions containing them and to oxidation dyeing processes using them.Type: GrantFiled: June 7, 1999Date of Patent: October 28, 2003Assignee: L'OrealInventors: Alain Genet, Alain Lagrange
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Patent number: 6632830Abstract: ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.Type: GrantFiled: April 28, 2000Date of Patent: October 14, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown
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Patent number: 6624309Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.Type: GrantFiled: September 25, 2002Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Publication number: 20030176708Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: December 12, 2002Publication date: September 18, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6613914Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.Type: GrantFiled: March 1, 2002Date of Patent: September 2, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ahmed F. Abdel-Magid, Bruce D. Harris, Cynthia A. Maryanoff
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Publication number: 20030153508Abstract: An N-containing five-membered ring compound of formula (I) 1Type: ApplicationFiled: July 23, 2002Publication date: August 14, 2003Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Publication number: 20030153596Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: July 9, 2002Publication date: August 14, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
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Publication number: 20030119886Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: September 25, 2002Publication date: June 26, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6583182Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.Type: GrantFiled: November 30, 2001Date of Patent: June 24, 2003Assignee: Chelator LLCInventors: Harry S Winchell, Joseph Y Klein, Elliot D Simhon, Rosa L Cyjon, Ofer Klein, Haim Zaklad
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Publication number: 20030104324Abstract: A compound represented by the following formula (I) to (VII): 1Type: ApplicationFiled: May 30, 2002Publication date: June 5, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Shigeki Uehira, Kiyoshi Takeuchi
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Patent number: 6559102Abstract: The invention relates to novel substituted 3-aryl-pyrazoles of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X are each as defined in the description, and also to processes for their preparation and to their use as herbicides.Type: GrantFiled: October 24, 2002Date of Patent: May 6, 2003Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Karl-Heinz Linker, Joachim Kluth, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Publication number: 20030073722Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: April 17, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20030065007Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1Type: ApplicationFiled: October 9, 2002Publication date: April 3, 2003Inventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
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Patent number: 6541632Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.Type: GrantFiled: June 19, 2002Date of Patent: April 1, 2003Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
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Patent number: 6518295Abstract: The present invention relates to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (1) of the specification, as well as their physiologically acceptable salts, in the manufacture of medicaments, useful in human and/or veterinary therapy, for the treatment of disorders that are mediated by an excess of substance P, and especially disorders of the central nervous system such as anxiety, depression, schizophrenia, manic depressive psychosis, sexual dysfunction, drug addiction, cognitive disorders, and locomotive disorders.Type: GrantFiled: February 1, 2001Date of Patent: February 11, 2003Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Jordi Frigola-Constansa
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Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Publication number: 20030022891Abstract: The present invention related to compounds of the formula 1Type: ApplicationFiled: November 28, 2001Publication date: January 30, 2003Inventors: Anandan Palani, Mark D. McBriar, Sherry A. Shapiro, Ruo Xu, John Clader
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Publication number: 20030004196Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.Type: ApplicationFiled: June 12, 2002Publication date: January 2, 2003Inventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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Patent number: 6495492Abstract: The invention relates to novel substituted 3-aryl-pyrazoles of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X are each as defined in the description, and also to processes for their preparation and to their use as herbicides.Type: GrantFiled: February 20, 2001Date of Patent: December 17, 2002Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Karl-Heinz Linker, Joachim Kluth, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Patent number: 6495699Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R5, X, Y, and are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.Type: GrantFiled: August 6, 2001Date of Patent: December 17, 2002Assignee: Agouron Pharmaceuticals Inc.Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
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Patent number: 6492421Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 30, 1998Date of Patent: December 10, 2002Assignees: Athena Neurosciences, Inc., American Home Products Corp.Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Louis John Lombardo, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen, Reinhardt Bernhard Baudy, Susan Ashwell