Additional Nitrogen Attached Directly To The -c(=x)- Group By Nonionic Bonding Patents (Class 548/140)
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Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Publication number: 20140142146Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 8524894Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: GrantFiled: June 4, 2010Date of Patent: September 3, 2013Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
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Publication number: 20120277259Abstract: The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 10, 2012Publication date: November 1, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
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Publication number: 20120258929Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.Type: ApplicationFiled: June 23, 2006Publication date: October 11, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
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Publication number: 20120178780Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20120121708Abstract: A method for preparing an acetazolamide microparticle having a mean particle size ranged between 0.36 ?m and 18 ?m is provided. The method includes steps of dissolving an acetazolamide in a solvent to form an acetazolamide solution; and mixing the acetazolamide solution with a supercritical fluid at a temperature and a pressure above a critical point of the supercritical fluid for forming the acetazolamide microparticle, wherein the solvent is miscible with the supercritical fluid.Type: ApplicationFiled: November 15, 2010Publication date: May 17, 2012Applicant: National Taiwan UniversityInventors: Yan-Ping Chen, Feng-Nien Tsai
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Publication number: 20120041011Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 1, 2011Publication date: February 16, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110077234Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: Novo Nordisk A/SInventors: Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
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Publication number: 20110021549Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 21, 2010Publication date: January 27, 2011Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR JOSHI
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Publication number: 20100249129Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
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Publication number: 20100099662Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: ApplicationFiled: January 9, 2008Publication date: April 22, 2010Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20090324569Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: December 31, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20090216013Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: August 8, 2008Publication date: August 27, 2009Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedso, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswara Santhosh
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Publication number: 20090118501Abstract: Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes.Type: ApplicationFiled: July 7, 2006Publication date: May 7, 2009Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedso, Marit Kristiansen, Lone Jeppesen
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Publication number: 20090105482Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.Type: ApplicationFiled: July 14, 2006Publication date: April 23, 2009Applicant: Novo Nordisk A/SInventors: Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
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Publication number: 20090082350Abstract: Disclosed are heterocylic or heteroaryl compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20080242860Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.00 mol % and further at least one compound represented by the following formula (I): X-(L)n-Y ??Formula (I) wherein X represents a group adsorptive to a silver halide, L represents a divalent connecting group comprising one of an atom and an atomic group including at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Y denotes a reducible group and n denotes an integer of 0 or 1.Type: ApplicationFiled: June 3, 2008Publication date: October 2, 2008Applicant: FUJIFILM CORPORATIONInventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
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Patent number: 7060718Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: March 11, 2003Date of Patent: June 13, 2006Assignee: Amgen Inc.Inventor: Jonathan B. Houze
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Patent number: 6583165Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: February 21, 2001Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6344570Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogType: GrantFiled: July 11, 2000Date of Patent: February 5, 2002Assignee: AstraZeneca UK LimitedInventors: David R Brittain, Craig Johnstone
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Publication number: 20010006975Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: January 8, 2001Publication date: July 5, 2001Applicant: BAYER CORPORATION and ONYX PHARMACEUTICALS West Haven, CT and Richmond, CA, respectivelyInventors: Jill E. Wood, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 6187799Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: GrantFiled: May 22, 1998Date of Patent: February 13, 2001Assignees: Onyx Pharmaceuticals, Bayer CorporationInventors: Jill E Wood, Hanno Wild, Daniel H Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 5847148Abstract: The present invention provides novel thiadiazole derivatives represented by formula I: ##STR1## or pharmaceutical acceptable salts thereof wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.Type: GrantFiled: April 10, 1997Date of Patent: December 8, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Eric J. Jacobsen, Mark A. Mitchell, Heinrich J. Schostarez, Donald E. Harper
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Patent number: 5814646Abstract: A method of protecting a warm-blooded mammal from the progression of Alzheimer's disease, which comprises administering an effective amount of a compound of general formula. ##STR1## in which: R.sup.1 represents an optionally substituted aromatic or heteroaromatic group;L.sup.1 and L.sup.2 each independently represents a bond or an unbranched (1-4C) alkylene group, which alkylene group may optionally bear a (1-4C) alkyl, phenyl or phenyl (1-2C) alkyl substituent;one of Y.sup.1 and Y.sup.2 represents NR.sup.3 and the other represents O, S or NR.sup.3, in which R.sup.3 represent hydrogen, hydroxyl, (1-4C) alkoxy, (1-4C) alkyl or di (1-4C) alkylamino;Z represents O or S; andR.sup.2 represents (3-8C) cycloalkyl, heterocyclyl, and optionally substituted aromatic or heteroaromatic group, or together with L.sup.2, (1-10C) alkyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 2, 1995Date of Patent: September 29, 1998Assignee: Eli Lilly and CompanyInventors: Lawrence J. Heinz, Jill A. Panetta, Michael L. Phillips, Jon K. Reel, John K. Shadle, Richard L. Simon, Celia A. Whitesitt
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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: 5395818Abstract: The invention relates to novel heterocyclyltriazolinones of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, hydroxyl, cyano or alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, arylsulphonyl, amino or heterocyclyl, each of which is optionally substituted,R.sup.2 represents hydrogen, hydroxyl, mercapto, halogen or alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, arylalkyl, amino or heterocyclyl, each of which is optionally substituted, andHet represents an optionally substituted heterocycle of the formula ##STR2## in which X in each case represents oxygen, sulphur, an NH group or an N-alkyl group,a process for their preparation and their use as herbicides.Type: GrantFiled: July 2, 1993Date of Patent: March 7, 1995Assignee: Bayer AktiengesellschaftInventors: Wilhelm Haas, Kurt Findeisen, Heinz Forster, Karl-Heinz Linker, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5350856Abstract: This invention relates to a process for producing a compound of the formula ##STR1## comprising reacting a compound having the formula ##STR2## with cyanogen chloride or cyanogen bromide.Type: GrantFiled: January 10, 1990Date of Patent: September 27, 1994Assignee: ICI Americas Inc.Inventor: Raymond A. Felix
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Patent number: 5155122Abstract: The present invention is novel compounds which are 3,5-di-tertiary-butyl-4-hydroxyphenyl substituted 1,2,4- and 1,3,4-thiadazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like.Type: GrantFiled: August 23, 1991Date of Patent: October 13, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, Michael D. Mullican, Gary P. Shrum, Paul C. Unangst, Michael W. Wilson
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5087284Abstract: New thiadiazole ureas are provided for the control of plant growth, especially of undesirable weeds and grasses. Particularly effective are compounds which contain an organic substituent in the 5-position of the thiadiazole portion.Type: GrantFiled: October 31, 1989Date of Patent: February 11, 1992Assignee: Rhone-Poulenc, Inc.Inventor: Patrick R. Driscoll
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 4987233Abstract: The present invention provides a process for preparing herbicidal ureas and insecticidal carbamates and carbamate derivatives comprising reacting an amine, alcohol, or oxime nucleophile with a urea in an inert organic solvent.Type: GrantFiled: June 15, 1988Date of Patent: January 22, 1991Assignee: Eli Lilly and CompanyInventors: Ralph K. Achgill, Laurence W. Call
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Patent number: 4876044Abstract: Novel thiadiazole compounds are produced having the following general formula: ##STR1## wherein X is S or SO.sub.2R.sub.1 is a lower alkyl (cyclic or non-cyclic) radicalR.sub.2 is hydrogen or a lower acyclic hydrocarbon radicalR.sub.3 is a lower acyclic hydrocarbon or cycloalkyl radical or alkoxy radical, andR.sub.4 is hydrogen, a lower acyclic hydrocarbon radical or cycloalkyl radical, provided R.sub.3 and R.sub.4 are not both cycloalkyl, and[B] Tautomers of [A] wherein R.sub.2 is hydrogen.Synthesis of these compounds is disclosed, including synthesis of those compounds which exhibit tautomerism.The compounds show particular utility as agricultural pesticides and most favorably as herbicides.Type: GrantFiled: October 2, 1969Date of Patent: October 24, 1989Inventors: Tony Cebalo, Robert E. Buntrock
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Patent number: 4810282Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.Type: GrantFiled: June 10, 1987Date of Patent: March 7, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4695311Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.Type: GrantFiled: May 9, 1986Date of Patent: September 22, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4686294Abstract: Compounds of the formula ##STR1## are described in which R.sub.1 represents a perfluoroalkyl radical of from 1 to 2 carbon atoms, and at least one of R.sub.2 and R.sub.3 represents hydrogen, and the other, or both represent lower alkyl, and R.sub.4 represents a lower alkyl radical which may be unsubstituted or bear certain substitution, and which are useful as herbicides in a method for controlling weeds and wild grasses. Compositions containing such compounds are also described. Finally, novel fluoro-thio semicarbazides are described which are useful intermediates in the production of the compounds of Formula I.Type: GrantFiled: December 20, 1968Date of Patent: August 11, 1987Assignee: Ciba-Geigy CorporationInventors: Karl Hoegerle, Hans J. Cellarius, Paul Rathgeb, Jurg Rumpf
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Patent number: 4639526Abstract: 2-(alkyl, alkenyl and alkylmercapto)-5-[N-(alkanoyl, chloroalkanoyl, alkoxycarbonyl, phenoxy carbonyl, N'-[alkyl and alkenyl]-aminocarbonyl and N'-alkyl-N'-[alkyl and alkenyl]-aminocarbonyl)-amino]-1,3,4-thiadiazoles, i.e. 2-(alkyl, alkenyl and alkylmercapto)-5-[N-(alkanoylamino, chloroalkanoylamino, alkoxycarbonylamino, phenoxycarbonylamino, N'-[alkyl and alkenyl]-ureido and N'-alkyl-N'-[alkyl and alkenyl]-ureido)]-1,3,4-thiadiazoles, which possess herbicidal properties, and which may be produced by conventional methods.Type: GrantFiled: August 29, 1968Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Carl Metzger, Ludwig Eue, Helmuth Hack
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Patent number: 4599424Abstract: New thiadiazole ureas are provided for the control of plant growth, especially of undesirable weeds and grasses. Particularly effective are compounds which contain an organic substitutent in the 5-position of the thiadiazole portion.Type: GrantFiled: October 3, 1979Date of Patent: July 8, 1986Assignee: Rhone-Poulenc, Inc.Inventor: Patrick R. Driscoll
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Patent number: 4576629Abstract: Herbicidal thiadiazole ureas are provided wherein the 5-position of the thiadiazole ring is hetero substituted and which exhibit enhanced selective herbicidal activity.Type: GrantFiled: March 15, 1984Date of Patent: March 18, 1986Assignee: Union Carbide CorporationInventors: Robert B. Morland, Anson R. Cooke, John R. Bishop
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Patent number: 4528022Abstract: A defoliating composition comprising a compound have the structural formula ##STR1## wherein R is F, Cl, 3-Br, 4-Br, I, CN or CX.sub.3, where X is F, Cl or Br; R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; and R.sup.2 is C.sub.1 -C.sub.4 alkyl and a carrier for said compound is disclosed.Type: GrantFiled: November 15, 1983Date of Patent: July 9, 1985Assignee: Uniroyal, Inc.Inventors: Allen R. Blem, James A. McGuinness
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Patent number: 4518414Abstract: Thiadiazole derivatives of the formula ##STR1## where R.sup.1, A, X, Y, Z, m and n have the meanings given in the description, are used for controlling undesirable plant growth.Type: GrantFiled: January 11, 1983Date of Patent: May 21, 1985Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Peter Plath, Bruno Wuerzer
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Patent number: 4500715Abstract: 1,3,4-Thiazole derivatives of the formula ##STR1## wherein R.sub.26 ' denotes a C.sub.1 -C.sub.8 -alkyl radical which is optionally substituted by hydroxyl, halogen, cyano, C.sub.1 -C.sub.4 -alkoxy, carboxyl, aminocarbonyl or C.sub.1 -C.sub.4 -alkoxycarbonyl, a C.sub.2 -C.sub.4 -alkenyl radical, a cyclohexyl radical which is optionally substituted by C.sub.1 -C.sub.4 -alkyl, a phenyl, benzyl or phenylethyl radical which is optionally substituted by halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, a C.sub.1 -C.sub.2 -alkylcarbonyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylaminocarbonyl, aminocarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylaminosulphonyl, 2-thienyl, 2-furyl, 2-tetrahydrofuryl, amino, C.sub.1 -C.sub.4 -alkylamino or di-(C.sub.1 -C.sub.4 -alkyl)-amino radical or a phenylamino or benzylamino radical which is optionally substituted by C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy and R.sub.27 ' denotes a C.sub.1 -C.sub.Type: GrantFiled: January 26, 1981Date of Patent: February 19, 1985Assignee: Bayer AktiengesellschaftInventor: Hauke Furstenwerth
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Patent number: 4435567Abstract: A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.Type: GrantFiled: December 28, 1981Date of Patent: March 6, 1984Assignee: Chinoin Gyogyszer es Vesgyeszeti Termekek Gyara R. T.Inventors: Gyorgy Lugosi, Antal Simay, Janos Bodnar, Laszlo Simandi, Eva Somfai
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Patent number: 4338449Abstract: 4,5-Dihydro-4-acyl-1,3,4-thiadiazol-2-ylureas are herbicides active against pigweed and foxtail.Type: GrantFiled: June 15, 1981Date of Patent: July 6, 1982Assignee: Eli Lilly and CompanyInventors: Eddie V. P. Tao, Gilbert S. Staten
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Patent number: 4335247Abstract: The specification describes a nitrosourea derivative having the general formula: Cl--(CH.sub.2).sub.2 --N(NO)CO--NHR, wherein --NHR represents a 2-(1,3,4-thiadiazolyl)amino group, an amino residue of a neutral .alpha.-amino acid, or an amino residue of a neutral .alpha.-amino acid whose carboxyl group is amidated with 2-(1,3,4-thiadiazolyl)amine, or a pharmaceutically acceptable acid addition salt thereof. The above nitrosourea derivative and its salt are useful as antitumor drugs. The above nitrosourea derivative may be prepared either by nitrosating a urea derivative of the general formula: Cl--(CH.sub.2).sub.2 NHCONHR or by reacting N-(2-chloroethyl)-N-nitrosocarbamic acid or a reactive derivative thereof with an amino compound of the general formula: R--NH.sub.2.Type: GrantFiled: February 23, 1981Date of Patent: June 15, 1982Assignee: Kowa Co., Ltd.Inventors: Kichitaro Takatori, Takashi Yamaguchi, Masahiko Nagakura
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Patent number: 4314842Abstract: This invention concerns certain substituted 1,3,4-thiadiazol-2-yl-4-hydroxy-1-methyl-2-imidazolidinones having herbicidal activity, their preparation, and the control of weeds therewith.Type: GrantFiled: October 8, 1980Date of Patent: February 9, 1982Assignee: PPG Industries, Inc.Inventor: Jerome M. Lavanish
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Patent number: 4273574Abstract: A novel compound having the structural formula ##STR1## is disclosed, which is particularly useful as a post-emergent herbicide for combating unwanted vegetation in the presence of peanuts, rice and grain sorghum.Type: GrantFiled: August 14, 1980Date of Patent: June 16, 1981Assignee: Gulf Oil CorporationInventor: Joel L. Kirkpatrick