Benzothiazines (including Hydrogenated) Patents (Class 544/49)
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Patent number: 6265399Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: December 8, 1999Date of Patent: July 24, 2001Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Patent number: 6252070Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: August 7, 2000Date of Patent: June 26, 2001Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Patent number: 6242207Abstract: A dry chemistry reagent matrix composition is provided containing a matrix material and a reagent composition containing 3-methyl-6(sulfonate salt)-benzothiazolinone-(2)-hydrazone (MBTH-S), N-ethyl-N-(3-sulfopropyl)aniline, and an oxidase enzyme or a peroxidase enzyme or a mixture thereof. The dry chemistry reagent matrix composition is useful in reagent test strips for determining the presence or concentration of an analyte in a fluid sample, such as blood.Type: GrantFiled: October 4, 1999Date of Patent: June 5, 2001Assignee: Amira MedicalInventors: Joel S. Douglas, Karen R. Drexler, John M. Gleisner, John H. Priest
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Patent number: 6083515Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: July 4, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6048858Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: April 11, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6040151Abstract: A dry chemistry dye indicator composition provides improved shelf life, stable color indication end point and capability for a system at near normal pH. The novel dry chemistry dye indication system comprises 3-Methyl-6-(sodium sulfonate)-benzothiazolinone-(2)-hydrazone (MBTH-S). A preferred dye systems are based on the dye couple (MBTH-S) and 8-anilino-1-naphthalenesulfonate (ANS), and the dye couple MBTH-S and N-(3-sulfopropyl)analine. These dye indicator systems are used in conventional blood chemistry test strips and are particularly preferred for indication of glucose in blood.Type: GrantFiled: March 22, 1999Date of Patent: March 21, 2000Assignee: Mercury Diagnostics, Inc.Inventors: Joel S. Douglas, Karen R. Drexler
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Patent number: 5874429Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): ##STR1## The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against .alpha..sub.1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.Type: GrantFiled: June 24, 1996Date of Patent: February 23, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5856503Abstract: Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.Type: GrantFiled: December 6, 1996Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Hans-Peter Marki, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Yu-Hua Ji
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Patent number: 5776719Abstract: A dry chemistry dye indicator composition provides improved shelf life, stable color indication end point and capability for a system at near normal pH. The novel dry chemistry dye indication system comprises 3-Methyl-6-(sodium sulfonate)-benzothiazolinone-(2)-hydrazone (MBTH-S). A preferred dye systems are based on the dye couple (MBTH-S) and 8-anilino-1-naphthalenesulfonate (ANS), and the dye couple MBTH-S and N-(3-sulfopropyl)analine. These dye indicator systems are used in conventional blood chemistry test strips and are particularly preferred for indication of glucose in blood.Type: GrantFiled: April 5, 1996Date of Patent: July 7, 1998Assignee: Mercury Diagnostics, Inc.Inventors: Joel S. Douglas, Karen R. Drexler
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Patent number: 5773437Abstract: The present invention relates to alkylenediamine derivatives which relieve urinating contraction and therefore are of value as active ingredients of therapeutic agents for treating dysuria.Type: GrantFiled: September 30, 1996Date of Patent: June 30, 1998Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Norihisa Miyake, Atsushi Tendo, Michiko Ishida, Haruhiko Shinozaki, Yutaka Nomura, Yasunori Goto
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Patent number: 5733906Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: October 12, 1993Date of Patent: March 31, 1998Assignee: Eli Lilly and CompanyInventors: Louis N. Jungheim, Timothy A. Shepherd
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Patent number: 5719151Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.Type: GrantFiled: January 13, 1995Date of Patent: February 17, 1998Inventors: Sydney Shall, Manoochehr Tavassoli
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Patent number: 5703073Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: October 13, 1995Date of Patent: December 30, 1997Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 5610318Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.Type: GrantFiled: May 31, 1995Date of Patent: March 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
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Patent number: 5602236Abstract: Metal-containing steroid mimic complexes are provided. Compositions containing a metal ion incorporated into a steroid skeleton structure and ligands useful in the preparation of such compositions are also provided. The metal ion is preferably a radionuclide, such as technetium, rhenium or gallium. Methods for using the metal complexes for diagnostic and therapeutic purposes are further provided.Type: GrantFiled: April 8, 1994Date of Patent: February 11, 1997Assignee: Mallinckrodt Medical, Inc.Inventor: Raghavan Rajagopalan
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Patent number: 5599811Abstract: Novel benzothiazine dioxides which are antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation, and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: February 21, 1995Date of Patent: February 4, 1997Assignee: Warner-Lambert CompanyInventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
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Patent number: 5563144Abstract: This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.Type: GrantFiled: June 6, 1995Date of Patent: October 8, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Dominique Damour, Richard Labaudiniere, Jean-luc Malleron, Serge Mignani
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Patent number: 5547953Abstract: Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and also a medicament containing them. Acylguanidines I ##STR1## with X equal to carbonyl or sulfonyl; R(1) equal to H, (cyclo)alkyl, phenyl; R(2) equal to H, alkyl, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine. The compounds have no unwanted salidiuretic but very good antiarrhythmic properties. They are able, as a consequence of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, to be used for the treatment of all acute or chronic ischemia-induced damage.Type: GrantFiled: December 22, 1994Date of Patent: August 20, 1996Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5504095Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.Type: GrantFiled: December 20, 1994Date of Patent: April 2, 1996Assignee: Pfizer Inc.Inventors: Masami Nakane, Kunio Satake, Kazuo Ando, Hiroaki Wakabayashi
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Patent number: 5468857Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is a specified linking group; and A, B and E, which may be the same or different, are H, hydroxy, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; except that when Z is unsubstituted phenyl and X and K are oxygen, A, B and E are not all hydrogen.Type: GrantFiled: February 3, 1994Date of Patent: November 21, 1995Assignee: Imperial Chemical Industries PLCInventors: Alan J. Buckley, Michael G. Huchings, Ian Ferguson, Kevin Beautement, John M. Clough, Patrick J. Crowley, Christopher R. A. Godfrey, Paul J. deFraine, Vivienne M. Anthony, Stephen P. Heaney
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Patent number: 5389653Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1993Date of Patent: February 14, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5328915Abstract: Arthropodicidal compounds, compositions and arthropodicidal use of compounds having the formula ##STR1## wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m and n are as defined in the text.Type: GrantFiled: September 17, 1992Date of Patent: July 12, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Jeffrey K. Long, Patrick D. Lowder, Thomas M. Stevenson
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Patent number: 5321025Abstract: The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 1, 1993Date of Patent: June 14, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Pierre A. R. Bruneau, Graham C. Crawley
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Patent number: 5308766Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.Type: GrantFiled: June 10, 1991Date of Patent: May 3, 1994Assignee: The Regents of the University of CaliforniaInventors: Edward A. Dennis, William N. Washburn
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Patent number: 5278316Abstract: Novel unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.Type: GrantFiled: December 19, 1990Date of Patent: January 11, 1994Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, Julian Aranda
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Patent number: 5260316Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl; C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 or CO; A represents O, S, or a direct bond; B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond; X represents oxygen or sulfur; R.sub.Type: GrantFiled: June 3, 1992Date of Patent: November 9, 1993Assignee: Ciba-Geigy CorporationInventors: John H. Van Duzer, Dennis M. Roland
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Patent number: 5248682Abstract: The present invention is novel compounds which are 2-substituted-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or 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. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.Type: GrantFiled: August 3, 1992Date of Patent: September 28, 1993Assignee: Warner-Lambert CompanyInventors: David T. Connor, Catherine R. Kostlan
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Patent number: 5212170Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.Type: GrantFiled: May 13, 1992Date of Patent: May 18, 1993Assignee: American Home Products CorporationInventor: Gary P. Stack
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Patent number: 5187276Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: November 28, 1990Date of Patent: February 16, 1993Assignee: Troponwerke GmbH & Co. KG.Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Thurman
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Patent number: 5149703Abstract: 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: September 6, 1991Date of Patent: September 22, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Cheuk K. Lau, Claude Dufresne
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Patent number: 5132304Abstract: The invention relates to the compounds corresponding to the general formula I ##STR1## in which: R.sup.1 represents a lower alkyl radical (having one to four carbon atoms), a phenyl radical or a benzyl radical. These compounds are useful as medicinal products or as synthesis intermediates for medicinal products.Type: GrantFiled: July 31, 1990Date of Patent: July 21, 1992Assignee: Laboratorios Del Dr. Esteve, S. A.Inventors: Jose M. Ribalta-Baro, Jordi F. Rigola-Constansa
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Patent number: 5097027Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.Type: GrantFiled: October 5, 1990Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5081118Abstract: A series of novel oxyethyl derivatives of certain selected enolic oxicam compounds are disclosed, including certain novel oxyethyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide (piroxicam). These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Said oxyethyl derivatives of enoic oxicam compounds like piroxicam are of the formulae: ##STR1## wherein R.sub.1 is hydrogen, methyl, fluorine or chlorine, and R.sub.2 is hydrogen or --COOR.sub.3 wherein R.sub.3 is alkyl having from one to eight carbon atoms.Type: GrantFiled: April 26, 1990Date of Patent: January 14, 1992Assignee: Pfizer Inc.Inventors: Andrew C. Braisted, Philip D. Hammen
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Patent number: 5004742Abstract: The present invention relates to novel benzothiazine-1,1-dioxide derivatives. These benzothiazine-1,1-dioxide derivatives have a high hyaluronidase-inhibiting activity and accordingly can be used in drugs such as anti-inflammatory agent, anti-allergic agent and the like.Type: GrantFiled: August 14, 1989Date of Patent: April 2, 1991Assignee: Nippon Hypox Laboratories IncorporatedInventors: Toshio Satoh, Yasunori Niiro, Hisao Kakegawa, Hitoshi Matsumoto
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Patent number: 5003074Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.Type: GrantFiled: September 28, 1988Date of Patent: March 26, 1991Assignee: Ciba-Geigy CorporationInventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
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Patent number: 4988809Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: February 21, 1990Date of Patent: January 29, 1991Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
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Patent number: 4952580Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.Type: GrantFiled: November 9, 1988Date of Patent: August 28, 1990Assignee: FMC CorporationInventors: Anthony J. Martinez, Thomas G. Cullen
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Patent number: 4948416Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.Type: GrantFiled: March 27, 1989Date of Patent: August 14, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4939140Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.Type: GrantFiled: October 27, 1988Date of Patent: July 3, 1990Assignee: Pfizer Inc.Inventors: Eric R. Larson, Banavara L. Mylari
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Patent number: 4937343Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: September 22, 1988Date of Patent: June 26, 1990Assignee: Troponwerke GmbH & Co. KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
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Patent number: 4919705Abstract: The present invention relates to a trifluoromethanesulfonamide derivative represented by the general formula given below, a herbicide with the derivative as the active ingredient and a method for the preparation of the derivative. ##STR1## [In the formula, X is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or a haloalkyl group having 1 to 4 carbon atoms, n is 1, 2 or 3 and A is --O--CR.sup.3 R.sup.4 --, --S--CR.sup.3 R.sup.4 --, --SO--CR.sup.3 R.sup.4 --, --SO.sub.2 --CR.sup.3 R.sup.4 -- or --SO.sub.2 --NR.sup.3 --. And, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each a hydrogen atom or an alkyl group having 1 to 4 carbon atoms.]These compounds are prepared depending on A in the above given general formula by the reaction of an amine derivative and a trifluoromethansulfonyl halide or trifluoromethanesulfonic anhydride or by the oxidation of a thiochroman ring-containing trifluoromethanesulfonamide derivative.Type: GrantFiled: September 6, 1988Date of Patent: April 24, 1990Assignee: Idemitsu Kosan Company LimitedInventors: Mitsuru Shibata, Yoshiyuki Hiramatsu, Ryoichi Adachi, Kenichiro Mitsutake
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Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4904299Abstract: Novel N-hydroxy-N'-sulfonylguanidine compounds are described which possess significant herbicidal and plant growth regulant activity for control of undesired vegetation.Type: GrantFiled: February 17, 1988Date of Patent: February 27, 1990Assignee: E. I. Du Pont de Nemours and Co.Inventor: Rafael Shapiro
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Patent number: 4892575Abstract: Herbicidal sulfonamides such as 2-[[[4-(methylamino)-6-(2, 2,2-trifluoroethoxy)-1,3,5-triazin-2-yl]-aminocarbonyl]aminosulfonyl]benzo ic acid, methyl ester are useful as herbicides and plant growth regulants.Type: GrantFiled: February 19, 1988Date of Patent: January 9, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventors: Martha M. Bolinski, Donald J. Dumas
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Patent number: 4874758Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and method of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.Type: GrantFiled: March 4, 1988Date of Patent: October 17, 1989Assignee: Warner-Lambert CompanyInventors: Mary E. Carethers, Wiaczeslaw A. Centenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
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Patent number: 4867781Abstract: Herbicidal sulfonamides are useful as general or selective herbicides, both pre-emergence and post-emergence.Type: GrantFiled: January 27, 1988Date of Patent: September 19, 1989Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4853025Abstract: Benzylsulfonylureas and arylsulfamoylureas are useful as pre-emergent and post-emergent herbicides and as plant growth regulants.Type: GrantFiled: February 16, 1988Date of Patent: August 1, 1989Assignee: E. I. Du Pont de Nemour and CompanyInventors: Robert J. Pasteris, Mark E. Thompson
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Patent number: 4842639Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.Type: GrantFiled: September 25, 1986Date of Patent: June 27, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng