1,2-thiazoles (including Hydrogenated) Patents (Class 546/271.1)
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Patent number: 6924298Abstract: Oxazoline compounds having a 3,5-disubstituted-4-pyridyl group in the 2-position and a thienyl, thiazolyl or an arylphenyl group in the 4-position are effective in controlling aphids, insects and mites.Type: GrantFiled: June 22, 2001Date of Patent: August 2, 2005Assignee: Dow AgroSciences LLCInventors: Francis Eugene Tisdell, Scott Jerome Bis, Vidyadhar Babu Hegde, Timothy Patrick Martin, Denise Marie Perreault, Maurice Chee Hoong Yap, Katherine Anne Guenthenspberger, James Edwin Dripps, James Michael Gifford, Joe Raymond Schoonover, Laura Lee Karr, Leonard Paul Dintenfass, Paul Allen Neese
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6855825Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2-C6 alkyl, and R5 and R6 are each independently H or C1-C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: December 18, 2003Date of Patent: February 15, 2005Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6821992Abstract: The invention relates to compounds of general formula I, where A1, R1, R2 and Y are as defined in the description; and to their use as phytopathogenic fungicides.Type: GrantFiled: July 9, 2002Date of Patent: November 23, 2004Assignee: Aventis CropScience S.A.Inventors: Tracey Cooke, David Hardy, Brian Moloney, Peter Stanley Thomas, Chris Richard Steele, Geoffrey Gower Briggs
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Patent number: 6800760Abstract: Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.Type: GrantFiled: July 3, 2003Date of Patent: October 5, 2004Assignee: Chiron CorporationInventors: Paul A. Renhowe, Sabina Pecchi, Timothy D. Machajewski, Cynthia M. Shafer, Clarke Taylor, William R. McCrea, Jr., Christopher McBride, Elisa Jazan
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Publication number: 20040186114Abstract: Disclosed are compounds of formula (I) 1Type: ApplicationFiled: February 27, 2004Publication date: September 23, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong
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Patent number: 6777410Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: April 8, 2003Date of Patent: August 17, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20040158072Abstract: The invention relates to crystals from optionally substituted 2-(2-pyridinyl)methylthio-1H-benzimidazole hydrates and to a method for the production thereof.Type: ApplicationFiled: February 4, 2004Publication date: August 12, 2004Inventors: Hartmut Loebermann, Karl-Heinz Caster
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Publication number: 20040147525Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: 1Type: ApplicationFiled: July 22, 2003Publication date: July 29, 2004Applicant: SANKYO COMPANY, LIMITEDInventors: Tomio Kimura, Kazumasa Aoki, Akira Nakao
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Publication number: 20040147574Abstract: Novel isothiazole compounds, including derivatives thereof, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, hyperproliferative disorders and fibrotic diseases.Type: ApplicationFiled: January 26, 2004Publication date: July 29, 2004Applicant: Pfizer IncInventor: Michael J. Munchhof
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Publication number: 20040116473Abstract: Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.Type: ApplicationFiled: September 17, 2003Publication date: June 17, 2004Applicant: Pfizer IncInventors: Michael J. Munchhof, Laura C. Blumberg
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Publication number: 20040097499Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: ApplicationFiled: July 3, 2003Publication date: May 20, 2004Inventors: MacKlin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamid H. Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6730792Abstract: The present invention relates to a &bgr;3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof, which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type II diabetes and/or obesity. The compound can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compound can be used to reduced neurogenic inflammation or as an antidepressant agent. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.Type: GrantFiled: December 13, 2002Date of Patent: May 4, 2004Assignee: Eli Lilly and CompanyInventors: Britta Evers, Cynthia Darshini Jesudason, Rushad Eruch Karanjawala, David Michael Remick, Daniel Jon Sall, Miles Goodman Siegel, Wolfgang Stenzel, Russell Dean Stucky, John Arnold Werner
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Patent number: 6720425Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: December 9, 2002Date of Patent: April 13, 2004Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20040030132Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.Type: ApplicationFiled: October 31, 2002Publication date: February 12, 2004Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6689888Abstract: The present invention provides processes useful in the preparation of certain &bgr;3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.Type: GrantFiled: February 20, 2003Date of Patent: February 10, 2004Assignee: Pfizer Inc.Inventors: Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
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Publication number: 20040023807Abstract: 3-Arylisothiazoles of the formula I 1Type: ApplicationFiled: November 14, 2002Publication date: February 5, 2004Inventors: Ingo Sagasser, Olaf Menke, Michael Rack, Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Matthias Witschel, Cyrill Zagar, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6667326Abstract: The invention relates to compounds of the general formula wherein R1, R2, R3, R4, R5, X1, X2, X3, m and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for the control of pests on domestic and farm animals.Type: GrantFiled: May 16, 2002Date of Patent: December 23, 2003Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Jacques Bouvier, Urs Müller
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Patent number: 6664047Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: April 24, 2000Date of Patent: December 16, 2003Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Stephen T. Yue
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Publication number: 20030225091Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1Type: ApplicationFiled: November 15, 2002Publication date: December 4, 2003Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Publication number: 20030220197Abstract: Novel isothiazole derivatives of the formula (I) wherein A represents a group selected from (1), (2) and (3) in which R1, R2, R3, R4 and R5 have the meanings given in the specification processes for the preparation of the novel compounds and their use as microbicides.Type: ApplicationFiled: October 9, 2002Publication date: November 27, 2003Inventors: Yoshinori Kitagawa, Koichi Ishikawa, Haruko Sawada, Yasuo Araki, Takuma Shigyo, Lutz Assmann
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Patent number: 6620831Abstract: The present invention relates to an indazole derivative, pharmaceutically acceptable salt, solvated product and isomer thereof substituted with 1,1-dioxoisothiazolidine which are useful as inhibitors for Cyclin Dependent Kinase(CDK). The present invention also relates to an agent for inhibiting and treating diseases involving cell proliferation, e.g., cancer, inflammation, restenosis, angiogenesis, etc. which comprises the compound of formula (1) as an active ingredient together with a pharmaceutically acceptable carrier.Type: GrantFiled: November 4, 2002Date of Patent: September 16, 2003Assignee: LG Life Sciences Ltd.Inventors: Jin-Ho Lee, Chang-Yong Hong, Tae-Sik Park, Jong-Hyun Kim, Sei-Hyun Choi, Sook-Kyung Yoon, Hyun-Ho Chung, Shin-Wu Jeong, Kwang-Yeon Hwang, Dong-Kyu Shin
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Patent number: 6605725Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: November 2, 2001Date of Patent: August 12, 2003Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6593349Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: GrantFiled: March 11, 2002Date of Patent: July 15, 2003Assignee: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Publication number: 20030125364Abstract: A novel antirheumatic agent comprising as an active ingredient a compound of formula I: 1Type: ApplicationFiled: December 4, 2002Publication date: July 3, 2003Inventors: Saichi Matsumoto, Hirokuni Jyoyama, Shinji Kakudo, Kohji Hanasaki, Kenzo Koizumi, Tsuneaki Sakata, Ryuji Suzuki
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Publication number: 20030114681Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: August 30, 2002Publication date: June 19, 2003Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Publication number: 20030055087Abstract: The present invention relates to a compound of the formula [1′] 1Type: ApplicationFiled: May 10, 2002Publication date: March 20, 2003Applicant: Japan Tobacco Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: 6525076Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: February 8, 2000Date of Patent: February 25, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020193597Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: March 11, 2002Publication date: December 19, 2002Applicant: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Patent number: 6492397Abstract: A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis.Type: GrantFiled: July 26, 2000Date of Patent: December 10, 2002Assignee: Pharmacia CorporationInventors: David B. Reitz, Robert E. Manning
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Patent number: 6489344Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: June 18, 1999Date of Patent: December 3, 2002Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
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Patent number: 6486308Abstract: Minor groove binding molecules are covalently bound to oligonucleotides which in their base sequence are complementary to a target sequence of single stranded or double stranded DNA, RNA or hybrids thereof. The covalently bound oligonucleotide minor groove binder conjugates strogly bind to the target sequence of the complementary strand.Type: GrantFiled: December 18, 2000Date of Patent: November 26, 2002Assignee: Epoch Biosciences, Inc.Inventors: Igor V. Kutyavin, Eugeny A. Lukhtanov, Howard B. Gamper, Rich B. Meyer, Jr.
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Publication number: 20020103230Abstract: Organic compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II.Type: ApplicationFiled: August 30, 2001Publication date: August 1, 2002Inventors: Paul A. Renhowe, Timothy Machajewski, Cynthia M. Shafer, Mary Ellen Wernette-Hammond, Sabina Pecchi
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Publication number: 20020055523Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo [c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.Type: ApplicationFiled: August 9, 2001Publication date: May 9, 2002Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
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Publication number: 20020035137Abstract: Compounds of formula (I) 1Type: ApplicationFiled: July 31, 2001Publication date: March 21, 2002Inventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, Thorsten K. Oost, David A. Janowick
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Patent number: 6303639Abstract: Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), in which the radicals have the meanings given in the specification and claims, and physiologically tolerated salts and physiologically functional derivatives thereof, and processes for their preparation, are described. The compounds are suitable, for example, as hypolipidemic agents.Type: GrantFiled: September 29, 1999Date of Patent: October 16, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Wendelin Frick, Reinhard Kirsch, Heiner Glombik, Hubert Heuer
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Patent number: 6271236Abstract: Compounds of the formula wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl.Type: GrantFiled: September 26, 2000Date of Patent: August 7, 2001Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Publication number: 20010008900Abstract: A new administration regimen giving an extended plasma concentration profile of a H+, K+-ATPase inhibitor. The extended plasma profile is received by two or more consecutive administrations of a unit dose of a H+, K+-ATPase with 0.5-4 hours interval or by a pharmaceutical composition with extended release, which may be administered once daily.Type: ApplicationFiled: October 21, 1997Publication date: July 19, 2001Inventors: CHRISTER CEDERBERG, GEORGE SACHS
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Patent number: 6245774Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12Type: GrantFiled: June 20, 1995Date of Patent: June 12, 2001Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
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Patent number: 6242612Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.Type: GrantFiled: August 7, 2000Date of Patent: June 5, 2001Assignee: G. D. Searle & Co.Inventors: Matthew J. Graneto, Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
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Patent number: 6191155Abstract: Novel isothiazolecarboxylic acid derivatives of the formula in which R is as defined in the description, a process for preparing the novel compounds and their use for protecting plants against attack by undesirable microorganisms and animal pests.Type: GrantFiled: June 5, 2000Date of Patent: February 20, 2001Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Dietmar Kuhnt, Hans-Ludwig Elbe, Christoph Erdelen, Stefan Dutzmann, Gerd Hänssler, Klaus Stenzel, Astrid Mauler-Machnik, Haruko Sawada, Haruhiko Sakuma