Plural Sulfurs Or Nitrogens In The Five-membered Hetero Ring (e.g., Thiatriazole, Etc.) Patents (Class 544/134)
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Publication number: 20100029625Abstract: A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].Type: ApplicationFiled: June 22, 2006Publication date: February 4, 2010Applicants: KYOWA HAKKO KIRIN CO., LTD., FUJIFILM CORPORATIONInventors: Ryuichiro Nakai, Emi Shimoike, Hideaki Kusaka, Chikara Murakata, Yoshinori Yamashita
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Publication number: 20100029641Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: August 27, 2009Publication date: February 4, 2010Applicant: WyethInventors: Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Goldberg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, JR., Puwen Zhang
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Publication number: 20100004219Abstract: 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 metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to whType: ApplicationFiled: October 31, 2007Publication date: January 7, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko
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Patent number: 7601722Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.Type: GrantFiled: December 12, 2007Date of Patent: October 13, 2009Assignee: WyethInventors: Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Goldberg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, Jr., Puwen Zhang
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Publication number: 20090179638Abstract: Disclosed is an assay for identifying compounds that modulate a neuronal apoptotic pathway, the assay comprises: a) contacting HSP90 protein with a probe to form a probe: HSP90 complex, the probe being displaceable by a test compound; b) measuring a signal from the probe so as to establish a reference level; c) incubating the probe:HSP90 complex with the test compound; d) measuring the signal from the probe; e) comparing the signal from step d) with the reference level, a modulation of the signal indicating that the test compound binds to HSP90. Also disclosed is a probe which is labeled with a detectable label and/or an affinity tag.Type: ApplicationFiled: February 1, 2007Publication date: July 16, 2009Applicant: AEGERA THERAPEUTICS INC.Inventors: Philip A. Barker, James B. Jaquith, Stephen J. Morris, Amir Salehi
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090118286Abstract: Use of heterobicyclic acrylamides of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description, for controlling pests, novel heterobicyclic acrylamides and processes for preparing these compounds, and also compounds of the formula (IA) in which A2, R1, R2, R5 and R6 are as defined in the description.Type: ApplicationFiled: February 27, 2006Publication date: May 7, 2009Applicant: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Jurgen Scherkenbeck, Graham Holmwood, Jurgen Wieschemeyer, Peter Losel, Olga Malsam, Mark Wilhelm Drewes, Karl-Heinz Kuck, Ulrike Wachendorf-Neumann, Christian Arnold, Vincent Lee Salgado, Thomas Bretschneider
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Publication number: 20090043091Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.Type: ApplicationFiled: September 19, 2008Publication date: February 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080167303Abstract: The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: July 10, 2008Applicant: WyethInventors: Casey Cameron McComas, Stephen Todd Cohn, Andrew Fensome, Joel Adam Golderg, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, Puwen Zhang
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Patent number: 7348427Abstract: Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein.Type: GrantFiled: December 2, 2004Date of Patent: March 25, 2008Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Roland W. Bürli, Jacob Kaizerman, Peter Jones
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Publication number: 20070167622Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: January 8, 2007Publication date: July 19, 2007Inventors: Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Kang Le, Qiang Zhang
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Patent number: 7173030Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 21, 2004Date of Patent: February 6, 2007Assignee: Biovitrum ABInventors: David Pyring, Martin Henriksson, Jan Vagberg, Meredith Williams, Cecilia Nilsson, Catrine Dreifeldt
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Patent number: 7141596Abstract: The present invention provides compounds that can modulate the activity of a target protein, such as a phosphatase, that selectively binds phosphorylated peptides or proteins. The present compounds can be useful in treating diseases or disorders, including, for example, diabetes and obesity, that are connected directly or indirectly to the activity of the target protein.Type: GrantFiled: October 7, 2004Date of Patent: November 28, 2006Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy Wai Tsun Yue, Michael J. Bower, Wenyu Zhu, Matthew L. Crawley, Richard B. Sparks, James R. Pruitt, Amy Takvorian
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Patent number: 7084139Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: June 6, 2002Date of Patent: August 1, 2006Assignee: SmithKline Beecham CorporationInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
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Patent number: 7074788Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: November 22, 2002Date of Patent: July 11, 2006Assignee: Biovitrum ABInventors: Guido Kurz, Marianne Nilsson, Jerk Vallgårda, Meredith Williams
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Patent number: 7022702Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis.Type: GrantFiled: May 10, 2002Date of Patent: April 4, 2006Assignee: QLT Inc.Inventors: Zaihui Zhang, Gregory B. Chopiuk, Timothy S. Daynard, Shisen Wang
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Patent number: 6852739Abstract: The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or N02 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof.Type: GrantFiled: February 25, 2000Date of Patent: February 8, 2005Assignee: Nitromed Inc.Inventors: David S. Garvey, L. Gordon Letts, Sang William Tam
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Patent number: 6624165Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: April 9, 2002Date of Patent: September 23, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Patent number: 6596718Abstract: A compound of the formula A compound of formula I has a good affinity to the A2A receptor and is useful for the treatment of diseases mediated by this receptor.Type: GrantFiled: November 18, 2002Date of Patent: July 22, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Norcross David Roger, Claus Riemer
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Publication number: 20030130258Abstract: The present invention relates to compounds with the formula (I) 1Type: ApplicationFiled: November 22, 2002Publication date: July 10, 2003Inventors: Guido Kurz, Marianne Nilsson, Jerk Vallgarda, Meredith Williams
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Patent number: 6503934Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).Type: GrantFiled: February 9, 2001Date of Patent: January 7, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Klaus-Ulrich Weithmann, Swen Hölder
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Patent number: 6486156Abstract: This invention relates to compounds of formula (1), wherein substituents are defined in the description, that inhibit farnesylation of mutant ras gene products tough inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation of ras.Type: GrantFiled: September 21, 2001Date of Patent: November 26, 2002Assignee: Astrazeneca ABInventors: Jean-Claude Arnould, Annie Antoinette Christiane Olivier
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Patent number: 6392040Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 9, 2001Date of Patent: May 21, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Publication number: 20010041701Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: ApplicationFiled: March 9, 2001Publication date: November 15, 2001Inventors: Robert H. Chen, MIn A. Xiang
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Patent number: 6218412Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).Type: GrantFiled: October 14, 1999Date of Patent: April 17, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Klaus-Ulrich Weithmann, Swen Hölder
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Patent number: 6191152Abstract: The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds.Type: GrantFiled: September 20, 1999Date of Patent: February 20, 2001Assignee: EGIS Gyógyszergyar Rt.Inventors: József Reiter, József Barkóczy, Gábor Berecz, Gyula Simig, András Egyed, Katalin Ivanicsné Megyeri, Sándor Drabant, Szabolcs Kertész, Anikó Miklósné Kovács, Ildikó Nagyné Gyönös, Mária Szécseyné Hegedüs, Gábor Szénási, János Wellmann, Katalin Pallagi, Éva Schmidt, Károly Tihanyi, Péter Trinka, Margit Csörgö
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Patent number: 6127537Abstract: A method for the preparation of 3-amino-1,2-propandiol derivatives of the formula (I) ##STR1## by reacting a compound of the formula (II) ##STR2## with RNH.sub.2, wherein R and R.sub.1 have the same meaning as given in the description. The formula (I) derivatives are .beta.-blockers used for treating hypertension.Type: GrantFiled: December 10, 1999Date of Patent: October 3, 2000Assignee: Everlight USA, Inc.Inventors: Biing-Jiun Uang, Jia-Wen Chang
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Patent number: 6093738Abstract: Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H.sup.+ /K.sup.+ -ATPase. The compounds are 3-substituted 1,2,4-thiadiazolo [4,5-.alpha.]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to the general formula: ##STR1## where X and Z either represent an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.Type: GrantFiled: February 21, 1997Date of Patent: July 25, 2000Inventors: Khashayar Karimian, Tim F. Tam, Denis Desilets, Sue Lee, Tullio Cappelletto, Wanren Li
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Patent number: 6087359Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: September 10, 1999Date of Patent: July 11, 2000Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo
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Patent number: 6051572Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: April 28, 1998Date of Patent: April 18, 2000Assignee: Merck Sharp & Dohme Ltd.Inventor: Jose Luis Castro Pineiro
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Patent number: 5877316Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 and R.sup.4 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, C.sub.1-6 alkoxy, C.sub.1-4 alkyl substituted by a hydroxy or C.sub.1-4 alkoxy group, OCF.sub.3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each independently hydrogen or C.sub.1-4 alkyl; R.sup.2, R.sup.3 and R.sup.5 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy substituted by a C.sub.1-4 alkoxy group, or trifluoromethyl; R.sup.6 represents C.sub.1-6 alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR.sup.7 R.sup.8.Type: GrantFiled: September 16, 1997Date of Patent: March 2, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Karen Elizabeth Haworth, Simon Neil Owen, Eileen Mary Seward
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Patent number: 5852011Abstract: Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents.Type: GrantFiled: January 19, 1996Date of Patent: December 22, 1998Assignee: Mitsui Chemicals, Inc.Inventors: Akio Matsunaga, Yuki Nakajima, Hiroshi Kohno, Hironori Komatsu, Hajime Edatsugi, Daiji Iwata, Kimiko Takezawa
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Patent number: 5814629Abstract: The invention relates to novel microbicidal and plant-immunising compounds of formula I ##STR1## wherein: X is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, SR.sub.8, N(R.sub.9)R.sub.10, CH.sub.2 OH, CHO or COOR.sub.8 ;R.sub.8 to R.sub.10 are hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.1 -C.sub.4 acyl or benzoyl;Z is hydrogen, halogen, or a methyl group that is unsubstituted or to which from 1 to 3 unsubstituted or substituted hetero atoms O, S and/or N are bonded; in free form or in the form of salts. They can be used in crop protection for controlling and preventing disease infestation.Type: GrantFiled: December 19, 1996Date of Patent: September 29, 1998Assignee: Novartis Finance CorporationInventors: Peter Stanetty, Walter Kunz
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Patent number: 5780392Abstract: This invention concerns heterocyclyl-1,3,4-thiadiazolyloxycetamides of the formula ##STR1## in which R.sup.1 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl or aralkyl, R.sup.2 is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkenyloxy or alkinyloxy or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are bound, form an optionally substituted, saturated or unsaturated nitrogen heterocycle which may contain other hetero-atoms and to which a benzo-grouping can be fused, and Het is an optionally substituted heterocyclyl group with the exception of thienyl. The Invention also concerns a method of preparing such compounds, intermediates used in their preparation and the use of such compounds as herbicides.Type: GrantFiled: October 4, 1996Date of Patent: July 14, 1998Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Hans-Joachim Diehr, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5767041Abstract: The invention relates to new substituted aryliminoheterocycles of the general formula (I) ##STR1## in which A represents oxygen, sulphur or the group N--R.sup.1 whereR.sup.1 represents hydrogen or in each case optionally substituted alkyl, alkenyl or akinyl,E represents one of the following groups ##STR2## where Q represents oxygen, sulphur or the group N--R.sup.1 (where R.sup.1 has the abovementioned meaning) andR.sup.2 represents hydrogen, cyano or in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R represents hydrogen or in each case optionally substituted alkyl, alkenyl or alkinyl, andAr represents in each case optionally substituted monocyclic or bicyclic aryl or heteroaryl,to processes for their preparation and to their use as herbicides.Type: GrantFiled: January 7, 1997Date of Patent: June 16, 1998Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5691336Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.Type: GrantFiled: September 8, 1995Date of Patent: November 25, 1997Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills
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Patent number: 5677302Abstract: Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H.sup.+ /K.sup.+ -ATPase. The compounds are 3-substituted 1,2,4-thiadiazolo ?4,5-.alpha.!benzimidazole and 3-substituted imidazo?1,2-d!-1,2,4-thiadiazoles corresponding to the general formula: ##STR1## where X and Z either represent an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is an electronegative group.Type: GrantFiled: February 26, 1996Date of Patent: October 14, 1997Assignee: Apotex Inc.Inventors: Khashayar Karimian, Tim F. Tam, Denis Desilets, Sue Lee, Tullio Cappelletto, Wanren Li
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Patent number: 5637699Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: May 22, 1995Date of Patent: June 10, 1997Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Paul E. Finke, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark S. Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian J. Williams
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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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: 5512576Abstract: 2-Substituted 1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.Type: GrantFiled: December 2, 1994Date of Patent: April 30, 1996Assignee: Sterling Winthrop Inc.Inventors: Ranjit C. Desai, Dennis J. Hlasta
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5482916Abstract: 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]-[IV].Type: GrantFiled: March 5, 1993Date of Patent: January 9, 1996Assignee: Tosoh CorporationInventors: Yasuaki Hanasaki, Kazuaki Tsukuda, Hiroyuki Watanabe, Kenji Tsuzuki, Mitsuyuki Murakami, Noritoshi Niimi
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Patent number: 5461175Abstract: A method for separating enantiomers of a derivative of an aryloxipropanolamine is disclosed, characterized in that the derivative is contacted with a chiral solid-phase chromatography material containing molecular imprints of an optically pure enantiomer of the derivative to be separated.Type: GrantFiled: July 8, 1994Date of Patent: October 24, 1995Inventors: Lutz Fischer, Ralf Muller, Klaus Mosbach, Bjorn Ekberg
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Patent number: 5416065Abstract: Thiadiazabicyclooctanes of formula I ##STR1## wherein Z is oxygen or sulfur;R.sub.53 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.54 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 alkenyloxy, C3-C6alkynyioxy, hydroxy or C.sub.1 -C.sub.6 haloalkoxy; orR.sub.53 and R.sub.54, together with the carbon atom to which they are bonded, form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring;W is a group of formulae W.sub.1 to W.sub.Type: GrantFiled: November 18, 1993Date of Patent: May 16, 1995Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Hans Moser, Georg Pissiotas
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Patent number: 5354860Abstract: A process for preparing S-(-)-3-morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5-thiadiazol e hemihydrate, i.e. S-timolol hemihydrate, wherein the compound is crystallized in optically pure form as the hemihydrate from a mixture containing an organic solvent, water and S-timolol base. This process can be used in the purification of S-timolol, especially for the removal of the corresponding R-enantiomer.Type: GrantFiled: July 8, 1992Date of Patent: October 11, 1994Inventor: Markku Peralampi
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Patent number: 5320839Abstract: Topical ophthalmic compositions comprising certain thiadiazoles are useful in the treatment of glaucoma and ocular hypertension. The thiadiazoles are slightly less potent than timolol; however, they have greatly reduced systemic side effects as compared to timolol.Type: GrantFiled: August 10, 1993Date of Patent: June 14, 1994Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Robert J. Adamski
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Patent number: 5318964Abstract: Hydroxamic acid derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hydroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.Type: GrantFiled: May 24, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5294596Abstract: The invention relates to novel heterocyclyltriazolinones of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen or represents alkyl or cycloalkyl, each of which is optionally substituted,R.sup.2 represents hydrogen, hydroxyl, mercapto or halogen or represents 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 21, 1993Date of Patent: March 15, 1994Assignee: Bayer AktiengesellschaftInventors: Wilhelm Haas, Kurt Findeisen, Karl-Heinz Linker, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt