Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/169)
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Patent number: 10457817Abstract: The present invention generally relates to methods and compounds for preventing metal corrosion. More specifically, the method comprises contacting a hydrocarbon-containing liquid with a composition in an effective amount to prevent metal corrosion.Type: GrantFiled: May 2, 2017Date of Patent: October 29, 2019Assignee: Ecolab USA Inc.Inventors: Kekeli Ekoue-Kovi, Neetu Tomar, Deepak Jadhav, Kim B. Peyton, Jennifer L. Sorrells, Ian Michael Jones
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Publication number: 20150094346Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.Type: ApplicationFiled: December 10, 2014Publication date: April 2, 2015Applicant: NOVARTIS AGInventors: Jun CAO, Bernhard ERB, Robin Alec FAIRHURST, Arnaud GRANDEURY, Shinji HATAKEYAMA, Magdalena KOZICZAK-HOLBRO, Philipp LUSTENBERGER, Bernd RIEBESEHL, Nicola TUFILLI, Thomas ULLRICH, Xiang WU, Jianguang ZHOU
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Publication number: 20150065490Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE
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Publication number: 20150025094Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halType: ApplicationFiled: August 1, 2012Publication date: January 22, 2015Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan UniversityInventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
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Publication number: 20140045829Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
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Publication number: 20140038943Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 10, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
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Patent number: 8604214Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.Type: GrantFiled: June 14, 2012Date of Patent: December 10, 2013Assignee: Ewha University-Industry Collaboration FoundationInventors: Hea-Young Parkchoo, Kyung-Eun Doh, Mijung Yim, Jung-Min Lee
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Publication number: 20130245080Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.Type: ApplicationFiled: September 5, 2012Publication date: September 19, 2013Applicant: NOVARTIS AGInventors: Jun CAO, Bernhard ERB, Robin Alec FAIRHURST, Arnaud GRANDEURY, Shinji HATAKEYAMA, Magdalena KOZICZAK-HOLBRO, Xinzhong LAI, Philipp LUSTENBERGER, Bernd RIEBESEHL, Nicola TUFILLI, Thomas ULLRICH, Xiang WU, Jianguang ZHOU
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Publication number: 20130040999Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.Type: ApplicationFiled: June 14, 2012Publication date: February 14, 2013Applicant: Ewha University-Industry Collaboration FoundationInventors: Hea-Young PARKCHOO, Kyung-Eun Doh, Mijung Yim, Jung-Min Lee
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Publication number: 20120225895Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
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Publication number: 20120041041Abstract: Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Inventor: Robin Alec FAIRHURST
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Patent number: 8097731Abstract: A composition comprising: (A) a lubricant, and (B) at least one alcohol that is the reaction product of mercaptobenzothiazoles, mercaptothiazolines, or mercaptobenzimidazoles with various epoxies.Type: GrantFiled: September 10, 2008Date of Patent: January 17, 2012Assignee: Crompton CorporationInventors: Robert G. Rowland, Ronald D. Abbott
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Patent number: 7951954Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: GrantFiled: March 12, 2007Date of Patent: May 31, 2011Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Publication number: 20110105749Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 14, 2010Publication date: May 5, 2011Inventors: Weiwen YING, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
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Patent number: 7828858Abstract: Disclosed are mixtures of sulfide dyes and dyeing compositions comprising mixtures of sulfide dyes. The dye mixtures are useful for the dyeing of organic materials, such as keratin fibers, preferably human hair.Type: GrantFiled: September 13, 2006Date of Patent: November 9, 2010Assignee: Ciba CorporationInventors: Christian Cremer, Victor Paul Eliu, Beate Fröhling, Olof Wallquist
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Publication number: 20090239917Abstract: Compounds of formula (I): wherein: R1 represents a (C3-C8)cycloalkyl group, R2 represents a group of formula (II) as defined in the description, X represents an oxygen atom or an N—OR? group wherein R? represents a hydrogen atom, a linear or branched (C1-C6)alkyl group, an aryl group or an aryl-(C1-C6)alkyl group in which the alkyl moiety may be linear or branched. Medicinal products containing the same which are useful as hypoglycaemic and hypolipaemic agents.Type: ApplicationFiled: March 5, 2007Publication date: September 24, 2009Applicant: Les Laboratoires ServierInventors: Aurelie Hurtevent, Jean-Martial L'Helgoual'ch, Pascal Carato, Nicolas Lebegue, Veronique Leclerc, Morgan Le Naour, Pascal Berthelot, Catherine Dacquet, Alain Ktorza, Daniel-Henri Caignard
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Publication number: 20090221653Abstract: The present invention provides compounds of formula (I) wherein the variables are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 28, 2006Publication date: September 3, 2009Applicant: AstraZeneca ABInventors: Andrew Bailey, Roger Bonnert, Stephen Connolly, Anthony Ingall, Garry Pairaudeau, Michael Stocks
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Patent number: 7534475Abstract: A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged ?/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.Type: GrantFiled: March 8, 2005Date of Patent: May 19, 2009Assignee: Fujifilm CorporationInventors: Hideyuki Nishikawa, Ryo Hamasaki, Atsuhiro Ohkawa
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Patent number: 7517880Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 1, 2002Date of Patent: April 14, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20090076279Abstract: A composition comprising: (A) a lubricant, and (B) at least one alcohol that is the reaction product of mercaptobenzothiazoles, mercaptothiazolines, or mercaptobenzimidazoles with various epoxies.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Robert G. Rowland, Ronald D. Abbott
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Publication number: 20090062259Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: ApplicationFiled: March 12, 2007Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Publication number: 20080171767Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.Type: ApplicationFiled: November 29, 2005Publication date: July 17, 2008Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Roger Salmon, David Philip Bacon, Ewan James Turner Chrystal, David William Langton, Andrew Jonathan Knee, Gordon Richard Munns, Laura Quaranta, Hans-Georg Brunner, Renaud Beaudegnies, Fredrik Cederbaum, Fiona Murphy Kessabi
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Patent number: 7071221Abstract: Compounds of formula (I): wherein: X represents oxygen or sulphur or a group CH2 or R1, R2, R3, R4, R5 and R6 are as defined in the description, A represents an alkylene chain as defined in the description, B represents alkyl or alkenyl substituted by a group ?or R9, or B represents a group ?or R9, D represents a benzene, pyridine, pyrazine, pyrimidine or pyridazine nucleus.Type: GrantFiled: July 29, 2004Date of Patent: July 4, 2006Assignee: Les Laboratoires ServierInventors: Véronique Leclerc, Sylvie Pailloux, Pascal Carato, Carine Introvigne, Nicolas Lebegue, Pascal Berthelot, Catherine Dacquet, Jean Albert Boutin, Daniel Henri Caignard, Pierre Renard
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Patent number: 7008561Abstract: The present invention relates to compounds of formula (1) and the salts thereof which correspond to formula (2). In the formulae, A is C2- to C4-alkylene, x is a number from 1 to 100, y is a number from 1 to 4, and R is a cation. The compound of formula (1) and/or formula (2) forms a persistent film on metal surfaces, particularly on metal surfaces under stress in metal working and in the operation of crude oil and natural gas processing.Type: GrantFiled: April 30, 2002Date of Patent: March 7, 2006Assignee: Clariant GmbHInventors: Uwe Dahlmann, Michael Feustel, Rainer Kupfer
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Patent number: 6992228Abstract: This disclosure relates to a method for producing and using catalysts in the production of bisphenols, and in particular to a method for producing catalysts which contain poly-sulfur mercaptan promoters, and using these catalysts in the production of bisphenol-A and its derivatives.Type: GrantFiled: July 25, 2003Date of Patent: January 31, 2006Assignee: General Electric CompanyInventors: Jimmy Lynn Webb, James Lawrence Spivack
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Patent number: 6919362Abstract: Compounds of formula (I): wherein: X represents an oxygen or a sulphur or CH2 or R1 and R2 represent a hydrogen atom, or a group as defined in the description, A represents an alkylene chain as described in the description, B is as defined in the description, R3 and R4 represent a hydrogen atom or a group as defined in the description, D represents an optionally substituted benzene, optionally substituted pyrazine, optionally substituted pyrimidine or optionally substituted pyridazine and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.Type: GrantFiled: February 1, 2001Date of Patent: July 19, 2005Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Elodie Blanc-Delmas, Said Yous, Patrick Depreux, Gérald Guillaumet, Catherine Dacquet, Nigel Levens, Jean Albert Boutin, Caroline Bennejean, Pierre Renard
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Patent number: 6852711Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.Type: GrantFiled: November 19, 2002Date of Patent: February 8, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 6583157Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PAPAR&ggr;. In particular, the compounds of the invention modulate the function of PAPAR&ggr;. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.Type: GrantFiled: June 27, 2001Date of Patent: June 24, 2003Assignees: Tularik Inc., Japan Tobacco, Inc.Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein, Atsushi Hagiwara, Noboru Furukawa, Hisashi Shinkai
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Patent number: 6548667Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: GrantFiled: December 6, 2001Date of Patent: April 15, 2003Assignee: Samsung Electronics Co. Ltd.Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Patent number: 6465499Abstract: Sulphonylbenzazolones of the formula in which R1, R2, R3, R4, R5 and Q are each as defined in the description, a process for preparing these compounds and their use as microbicides in crop protection and in the protection of materials.Type: GrantFiled: November 21, 2000Date of Patent: October 15, 2002Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Hans-Ludwig Elbe, Robert Markert, Ralf Tiemann, Klaus Stenzel
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Patent number: 6437142Abstract: A new process prepares retiferol derivatives of formula I: wherein A is —C≡C— or —CH═CH—, and R1 and R2 are independently of each other lower alkyl or lower perfluoroalkyl, one version couples ketones of formula II with compounds of formula III. A second version couples phosphinoxides of formula IV with aldehydes of formula V. Compounds of formula I are useful in the treatment or prevention of hyperproliferative skin diseases and for reversing the conditions associated with photodamage.Type: GrantFiled: March 26, 2001Date of Patent: August 20, 2002Assignee: Basilea Pharmaceutica AGInventors: Hans Hilpert, Beat Wirz
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Patent number: 6362138Abstract: This invention relates to compounds which are suitable as ash-free antiwear additives and antioxidants, to lubricant compositions comprising said compounds as well as to their use. are particularly preferred. In the preferred compounds I′, R2 is isooctyloxycarbonylmethyl, R3 is isooctyloxycarbonylmethylthiomethyl and R4 is hydrogen; or R2 is tert-nonyl and R3 is tert-nonylthiomethyl and R4 is hydrogen; or R2 is isooctyloxycarbonylmethyl, R3 is hydrogen and R4 is isooctyloxycarbonylmethylthiomethyl; or R2 is tert-nonyl, R3 is hydrogen and R4 I is tert-nonylthiomethyl.Type: GrantFiled: September 15, 2000Date of Patent: March 26, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Hugo Camenzind, Samuel Evans, Alfred Dratva, Peter Hänggi
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Patent number: 6222048Abstract: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).Type: GrantFiled: June 12, 1997Date of Patent: April 24, 2001Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
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Patent number: 6150307Abstract: This invention relates to compounds which are suitable as ash-free antiwear additives and antioxidants, to lubricant compositions comprising said compounds as well as to their use. Compounds of formulae ##STR1## are particularly preferred. In the preferred compounds I',R.sub.2 is isooctyloxycarbonylmethyl, R.sub.3 is isooctyloxycarbonylmethylthiomethyl and R.sub.4 is hydrogen; orR.sub.2 is tert-nonyl and R.sub.3 is tert-nonylthiomethyl and R.sub.4 is hydrogen; orR.sub.2 is isooctyloxycarbonylmethyl, R.sub.3 is hydrogen and R.sub.4 is isooctyloxycarbonylmethylthiomethyl; orR.sub.2 is tert-nonyl, R.sub.3 is hydrogen and R.sub.4 I is tert-nonylthiomethyl.In the preferred compounds II',R.sub.2 and R.sub.2 ' are isooctyloxycarbonylmethyl, R.sub.3 and R.sub.3 ' are isooctyloxycarbonylmethylthiomethyl and R.sub.4 and R.sub.4 ' are hydrogen; orR.sub.2 and R.sub.2 ' are tert-nonyl, R.sub.3 and R.sub.3 ' are tert-nonylthiomethyl and R.sub.4 and R.sub.4 ' are hydrogen; orR.sub.2 and R.sub.Type: GrantFiled: August 3, 1998Date of Patent: November 21, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Hugo Camenzind, Samuel Evans, Alfred Dratva, Peter Hanggi
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Patent number: 6087508Abstract: There are described processes for the preparation of a compound of formula I ##STR1## and novel intermediates in the preparative process.Type: GrantFiled: March 10, 1998Date of Patent: July 11, 2000Assignee: AstraZeneca UK LimitedInventor: Christopher Goodwin
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Patent number: 6080869Abstract: A compound of formula I, including optical isomers thereof, whereinX represents --SO.sub.2 NH-- or --NHSO.sub.Type: GrantFiled: September 2, 1998Date of Patent: June 27, 2000Assignee: Astra Pharmaceuticals LimitedInventors: Roger Victor Bonnert, Roger Charles Brown
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Patent number: 6008365Abstract: A compound of formula I, including optical isomers thereof, ##STR1## wherein X represents --SO.sub.2 NH-- or --NHSO.sub.2 --,p, q and r independently represent 2 or 3,Y represents thienyl optionally substituted by alkyl or halogen, or phenylthio- or phenyloptionally substituted by akyl or halogen, andeach R independently represents H or alkyl,and pharmaceutically acceptable salts, esters and amides thereof.Type: GrantFiled: September 2, 1998Date of Patent: December 28, 1999Assignee: Astra Pharmaceuticals Ltd.Inventors: Roger Victor Bonnert, Roger Charles Brown
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Patent number: 6004957Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: July 22, 1998Date of Patent: December 21, 1999Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Patent number: 5980779Abstract: A process for producing a liquid crystalline compound represented by the following general formula (A): ##STR1##Type: GrantFiled: April 3, 1998Date of Patent: November 9, 1999Assignee: Dai Nippon Printing Co., Ltd.Inventors: Junichi Hanna, Masahiro Funahashi, Masanori Akada, Masayuki Ando, Yozo Kosaka
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Patent number: 5932601Abstract: 2,4-Oxazolidinedione derivative represented by the formula: ##STR1## wherein R stands for an optionally substituted hydrocarbon residue or heterocyclic group; Y stands for a group represented by --CO--, --CH(OH)-- or --NR.sup.3 -- (wherein R.sup.3 stands for an optionally substituted alkyl group); m is 0 or 1; n is 0, 1 or 2; A stands for a C.sub.1-7 divalent aliphatic hydrocarbon group; R.sup.1 stands for hydrogen or an alkyl group; ring E stands for a benzene ring having 1 or 2 substituents; L and M respectively stand for hydrogen, or L and M may optionally be combined with each other to form a bond; with a proviso that the partial formula: ##STR2## does not include the formula: ##STR3## wherein R' stands for an alkyl group; or a salt thereof, which has excellent actions of lowering blood sugar and lipid in blood.Type: GrantFiled: October 30, 1995Date of Patent: August 3, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hiroyuki Odaka, Yu Momose, Mitsuru Kawada
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Patent number: 5929100Abstract: Compounds of formula I, ##STR1## wherein X represents naphthyl optionally substituted by alkyl or halogen; andp, q and r independently represent 2 or 3,and pharmaceutically acceptable salts thereof;processes for their preparation and methods for their use.Type: GrantFiled: March 3, 1997Date of Patent: July 27, 1999Assignee: Astra Pharmaceuticals LimitedInventors: Roger Bonnert, Roger Brown, Peter Cage, David Cheshire, Francis Ince
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Patent number: 5919807Abstract: The invention relates to benzothiazoles and benzoxazoles of general formula ##STR1## wherein R.sup.1 to R.sup.3, X, Z and n are defined as in claim 1, the enantiomers, diastereomers and salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Dr. Karl Thomae GmbHInventors: Peter Muller, Rudolph Hurnaus, Roland Maier, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Leo Thomas, Gerhard Hallermayer
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Patent number: 5863915Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.Type: GrantFiled: May 15, 1997Date of Patent: January 26, 1999Assignee: Bayer CorporationInventors: Harold C. E. Kluender, Brian R. Dixon, David R. Brittelli
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Patent number: 5856479Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.Type: GrantFiled: May 16, 1997Date of Patent: January 5, 1999Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
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Patent number: 5846989Abstract: A compound of formula I, including optical isomers thereof, ##STR1## wherein X represents --SO.sub.2 NH-- or --NHSO.sub.2 --,p, q and r independently represent 2 or 3,Y represents thienyl optionally substituted by alkyl or halogen, or phenylthio- or phenyl optionally substituted by alkyl or halogen, andeach R independently represents H or alkyl,and pharmaceutically acceptable salts, esters and amides thereof.Type: GrantFiled: February 7, 1997Date of Patent: December 8, 1998Assignee: Astra Pharmaceuticals LimitedInventors: Roger Victor Bonnert, Roger Charles Brown, Peter Alan Cage, Francis Ince, Garry Pairaudeau
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Patent number: 5834500Abstract: Sulfur-containing heterocyclic bradykinin antagonists, process for their preparation, and their useCompounds of the formula (I) ##STR1## in which one of the radicals X.sub.1, X.sub.2 or X.sub.3 is C--O--R.sup.2 and the other X.sub.1, X.sub.2, and X.sub.3, in each case, and X.sub.4, are then, identically or differently, N or CR.sup.1 ; R.sup.1 and R.sup.3 are, identically or differently, H, halogen, (C.sub.1 -C.sub.6)-alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (C.sub.6 -C.sub.12)-aryl, (C.sub.6 -C.sub.12)-aryl-(C.sub.1 -C.sub.3)-alkyl, C(O)--OR.sup.6, C(O)--H, (C.sub.2 -C.sub.5)-alkenyl, NO.sub.2, SO.sub.3 R.sup.7, CN or C(O)--NHR.sup.8, where alkyl, aryl and alkenyl can optionally be substituted.Type: GrantFiled: May 16, 1997Date of Patent: November 10, 1998Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Holger Heitsch, Gerhard Nolken, Klaus Wirth, Bernward Scholkens
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Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
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Patent number: 5763465Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.Type: GrantFiled: October 31, 1996Date of Patent: June 9, 1998Assignee: Astra Pharmaceuticals LimitedInventors: Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
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Patent number: 5750701Abstract: A compound of the formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, X represents a moiety of formula (a), in which A.sup.1 represents --CH.dbd.CH.dbd., NH, S or O; A.sup.2 represents an oxo or a thioxo group; A.sup.3 represents H or an alkylcarbonyl group; and A.sup.4 represents hydroxy or NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represents H or alkyl; R.sup.0 and R.sup.1 each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b), wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.Type: GrantFiled: September 16, 1996Date of Patent: May 12, 1998Assignee: SmithKline Beecham plcInventors: Lee James Beeley, David Kenneth Dean
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Patent number: RE37556Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group, m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.Type: GrantFiled: February 8, 1999Date of Patent: February 19, 2002Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi