Chalcogen Or Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/135)
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Publication number: 20030236232Abstract: A class of novel benzo(b)thiophene is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.Type: ApplicationFiled: December 3, 2002Publication date: December 25, 2003Inventors: Michael Dean Kinnick, Ho-Shen Lin, Michael John Martinelli, John Michael Morin, Michael Enrico Richett
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Publication number: 20030225076Abstract: Diarylanines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: ApplicationFiled: September 13, 2002Publication date: December 4, 2003Inventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Publication number: 20030195238Abstract: Compounds of general formula (I): 1Type: ApplicationFiled: November 8, 2002Publication date: October 16, 2003Inventors: Ana Martinez Gil, Ana Castro Morera, Maria Concepcion Martin Perez, Mercedes Alonso Cascon, Isabel Dorronsoro Diaz, Francisco Jose Moreno Munoz, Francisco Wandosell Jurado
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Patent number: 6617339Abstract: Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: December 5, 2000Date of Patent: September 9, 2003Assignee: Syngenta LimitedInventor: Michael Barry Gravestock
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Patent number: 6559171Abstract: The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.Type: GrantFiled: November 1, 2001Date of Patent: May 6, 2003Assignee: Eli Lilly and CompanyInventors: Charles Howard Mitch, Steven James Quimby
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Patent number: 6537948Abstract: The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].Type: GrantFiled: January 31, 2001Date of Patent: March 25, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitomo Tohyama, Yuzuru Sanemitsu
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Publication number: 20020115697Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: ApplicationFiled: August 28, 2001Publication date: August 22, 2002Inventors: Lone Jeppesen, Per Sauerberg
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Patent number: 6395762Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: July 12, 2001Date of Patent: May 28, 2002Assignee: American Home Products CorporationInventors: William Floyd Fobare, Jill Freymuller
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Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
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Publication number: 20020025973Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: July 12, 2001Publication date: February 28, 2002Applicant: American Home Products CorporationInventors: William F. Fobare, Jill Freymuller
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 6300325Abstract: This invention relates to novel benzo-2-triazole substituted compounds, pharmaceutical compositions, processes for their preparation, and use thereof in treating IL-8, GRO&agr;, GRO&bgr;, GRO&ggr; and NAP-2 mediated diseases.Type: GrantFiled: July 9, 1999Date of Patent: October 9, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, Melvin C. Rutledge
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Patent number: 6187798Abstract: The present invention provides aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: June 1, 1999Date of Patent: February 13, 2001Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Lone Jeppesen, John S. Ward
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Patent number: 6130225Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined in the description, to a process for their preparation and to their use as herbicides.Type: GrantFiled: February 2, 1999Date of Patent: October 10, 2000Assignee: Bayer AktiengesellschaftInventors: Mark-Wilhelm Drewes, Roland Andree, Markus Dollinger
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Patent number: 6124312Abstract: The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.Type: GrantFiled: June 1, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Charles H Mitch, Steven J Quimby, Jon K Reel, Celia A Whitesitt
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Patent number: 6100252Type: GrantFiled: December 8, 1998Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Yoshiyuki Inada
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Patent number: 6069159Abstract: The present invention provides heterocyclic compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: May 10, 1999Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Lone Jeppesen, John S Ward
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Patent number: 6040442Abstract: The presently claimed process provides a method for preparing compounds of the formula ##STR1## phosphorous (III) compound and a diester of azodicarboxylate.Type: GrantFiled: June 1, 1995Date of Patent: March 21, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6015813Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 8, 1998Date of Patent: January 18, 2000Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Per Sauerberg
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Patent number: 5977129Abstract: The present invention relates to compounds of formula I: whereinone or both G is an azacyclic ring of formula II: ##STR1## and Z is oxygen or sulfur and the remaining variables are as defined in the specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: May 3, 1995Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5972978Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: February 19, 1999Date of Patent: October 26, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5948916Abstract: Novel arylthiadiazole derivatives and salts thereof useful for preventing and treating human viral infection and a novel virucide which contains the arylthiadiazole derivative or a salt thereof are provided. N,N-dimethyl ?3-(3-(amino-2,6-dichlorophenyl)-1,2,5-thiadiazol-4-yl! carbamate or its salt, and virucide containing the same as an effective component.Type: GrantFiled: June 9, 1997Date of Patent: September 7, 1999Assignee: Rational Drug Design LaboratoriesInventors: Katsushi Ijichi, Shiro Shigeta, Masanori Baba, Masatoshi Fujiwara, Tomoyuki Yokota, Hiromitsu Takayama, Shin-ichiro Sakai, Yasuaki Hanasaki, Teruhiko Ide, Hiroyuki Watanabe, Kimio Katsuura
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Patent number: 5929247Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: July 27, 1999Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5919809Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: November 4, 1993Date of Patent: July 6, 1999Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5914338Abstract: The present invention relates to therapeutically active azatricyclic compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 1, 1997Date of Patent: June 22, 1999Assignee: Novo NordiskInventors: Lone Jeppesen, Preben H. Olesen, Per Sauerberg
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Patent number: 5821371Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: October 13, 1998Assignee: Eli Lilly and ComanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5821370Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward
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Patent number: 5767280Abstract: The present invention relates to a process for making intermediates useful for preparing therapeutically active azacyclic or azabicyclic compounds.Type: GrantFiled: June 1, 1995Date of Patent: June 16, 1998Assignee: Eli Lilly and CompanyInventors: Roger L. Robey, John S. Ward
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Patent number: 5760222Abstract: Bleaches, a method for bleaching substrates using these materials and detergent compositions containing same are reported. The bleaches are thiadiazole dioxide derived mono- and di- oxaziridines. Substrates such as fabrics may be bleached in an aqueous solution containing the oxaziridine.Type: GrantFiled: December 3, 1996Date of Patent: June 2, 1998Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventor: Janet Lynn Coope
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Patent number: 5747514Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.Type: GrantFiled: July 19, 1996Date of Patent: May 5, 1998Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
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Patent number: 5731441Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: March 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5703065Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.Type: GrantFiled: May 7, 1996Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventor: Harry R. Howard, Jr.
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Patent number: 5675023Abstract: The present invention relates to a chromone derivative and an aldose reductase inhibitor comprising said compound as efective component, which is represented by the following formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, etc., R.sub.3 represents an oxygen atom, a sulfur atom, etc., R.sub.7 represents a phenyl group substituted or not substituted, etc., and R represents a hydrogen atom or a lower alkoxy group. The present compounds exhibit superior inhititory action on aldose reductase and are useful for the treatment of various complications of diseases in diabetes, such as cataract, retinopathy, keratopathy, nephropathy, and neuropathy.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Tsumura & Co.Inventors: Yasushi Igarashi, Takuji Yamaguchi, Yoshimitsu Ogawa, Mika Tomita, Hiroko Hayashi, Toshitsugu Sato, Kunio Hosaka
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5672709Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: September 30, 1997Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5665745Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5661165Abstract: Disclosed are ((4-phenyl-1,2,5--thiadiazol-3-yl)oxy)methyl ester thiocyanic acid compounds corresponding to the formula: ##STR1## wherein X represents --Br, --Cl, --F, --CF.sub.3, --OCF.sub.3, --CN, C.sub.1 -C.sub.7 straight or branched chain alkyl, C.sub.1 -C.sub.7 straight or branched chain alkoxy or --COOR wherein R is --H or C.sub.1 -C.sub.7 straight or branched chain alkyl and n is an integer of from 0-5.These compounds have been found to exhibit antimicrobial and marine antifouling activity in industrial and commercial applications and compositions containing these compounds are so employed.Type: GrantFiled: July 10, 1996Date of Patent: August 26, 1997Assignee: The Dow Chemical CompanyInventors: Ravi B. Shankar, R. Garth Pews, Duane R. Romer
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Patent number: 5650419Abstract: Described herein are compounds of the formula; ##STR1## wherein: Thi is a unsubstituted or substituted thiadiazolyl;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxylcarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, substituted or unsubstituted phenyl, alkyltetrazolyl or a substituted or unsubstituted imidazolyl, dihydroimidazolyl, pyrazolyl, furyl, thiazolyl or thienyl or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.Type: GrantFiled: August 30, 1996Date of Patent: July 22, 1997Assignee: Sanofi, S.A.Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz
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Patent number: 5646289Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 6, 1995Date of Patent: July 8, 1997Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5614535Abstract: Compounds of the formula I ##STR1## in which R.sup.1 and X have the meanings herein defined, their physiologically unobjectionable salts and/or solvates inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporosis, tumoral diseases, apoplexy, cardiac infarction, inflammations, arteriosclerosis and osteolytic disorders.Type: GrantFiled: August 18, 1995Date of Patent: March 25, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Horst Juraszyk, Joachim Gante, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5589439Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.Type: GrantFiled: July 28, 1995Date of Patent: December 31, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Koichi Moriya, Fritz Maurer, Seishi Ito, Katsuaki Wada, Kazuhiro Ukawa, Ryo Watanabe, Asami Ito, Natsuko Minegishi
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Patent number: 5578634Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.Type: GrantFiled: May 12, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 5563159Abstract: There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C.sub.1 -C.sub.6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a phenyl group, a heterocyclic group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a bicycloalkyl group or a tricycloalkyl group, all of which may be substituted. Also disclosed are a fungicidal/insecticidal/acaricidal agent containing the dithiocarbonimide derivative as an active ingredient, an intermediate for use in the production of the dithiocarbonimide derivative, and a process for producing the dithiocarbonimide derivative from the intermediate.Type: GrantFiled: December 2, 1994Date of Patent: October 8, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Tomoyuki Kusaba, Tadashi Ohsumi, Tsuguhiro Katoh, Makoto Fujimura, Norio Kimura, Kazuya Ujihara, Kimitoshi Umeda
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Patent number: 5556909Abstract: Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.Type: GrantFiled: December 2, 1994Date of Patent: September 17, 1996Assignee: Sanofi Winthrop Inc.Inventor: Ranjit C. Desai
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5550139Abstract: Isothiazolidin-3-one-1,1 dioxide, 3-oxo-1,2,5-thiadiazolidine-1,1,-dioxide and derivatives thereof, reduce or inhibit the activity of serine proteases. Such compounds are useful as anti-inflammatory and anti-metastatic agents.Type: GrantFiled: January 3, 1994Date of Patent: August 27, 1996Assignee: The Wichita State UniversityInventor: William C. Groutas
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Patent number: 5547920Abstract: Thiadiazole derivatives with excellent herbicidal effectiveness, wide herbicidal spectrum and excellent selectivity are disclosed. The thiadiazole derivatives are represented by one of the formula [I]14 [IV].Type: GrantFiled: June 28, 1994Date of Patent: August 20, 1996Assignee: Tosoh CorporationInventors: Yasuaki Hanasaki, Kazuaki Tsukuda, Hiroyuki Watanabe, Kenji Tsuzuki, Mitsuyuki Murakami, Noritoshi Niimi
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Patent number: 5527813Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: March 2, 1994Date of Patent: June 18, 1996Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Preben H. Olesen
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman