Sulfur Is Part Of A Substituent Which Contains Additional Nitrogen Patents (Class 514/593)
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Patent number: 6875793Abstract: This invention is directed to a novel solid matrixed controlled release, oral dosage form where the dosage form contains a therapeutically effective amount of a sulfonylurea or a salt or derivative thereof in the matrix. Further, the use of an aqueous alkalizing medium affords substantially complete bioavailability of the drug from the matrix of the tablet. The core tablets may optionally be coated with a coating material in the range of 2% to 10% with an enteric material or with a water insoluble material like ethyl cellulose.Type: GrantFiled: March 25, 2003Date of Patent: April 5, 2005Assignee: Penwest Pharmaceuticals Co.Inventors: Dileep Bhagwat, Donald Diehl, II, Anand R. Baichwal
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Patent number: 6852760Abstract: Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.Type: GrantFiled: September 17, 1999Date of Patent: February 8, 2005Assignee: Akesis Pharmaceuticals, Inc.Inventors: Stuart A. Fine, Kevin J. Kinsella
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Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Publication number: 20040072880Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 31, 2003Publication date: April 15, 2004Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Publication number: 20040048909Abstract: Biphenyl derivatives represented by the following formula (1): 1Type: ApplicationFiled: June 23, 2003Publication date: March 11, 2004Inventors: Takayuki Namiki, Kenichi Kishii, Masaki Mitani, Masashi Tamai, Naoki Hiyama, Makoto Kimura, Satoshi Ichinomiya
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Patent number: 6693094Abstract: The invention describes formulations that include either metformin, sulfonylurea or a biguanide-sulfonylurea combination as one active ingredient in addition to specific, other active ingredients. The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of the included biguanide (metformin) and/or sulfonylurea in the prevention and treatment of insulin resistance and diabetes mellitus. The carefully chosen additional active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and those adverse incidences associated with the concurrent use of metformin and/or the sulfonylureas. When clinically administered, the invention will provide therapeutic levels of metformin and of a sulfonylurea, alone or in combination, and broaden their usefulness.Type: GrantFiled: March 7, 2002Date of Patent: February 17, 2004Assignee: Chrono RX LLCInventors: Don C. Pearson, Kenneth T. Richardson
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Publication number: 20030109561Abstract: A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a sub-maximal amount of an insulin secretagogue, to a mammal in need thereof; and a pharmaceutical composition for use in such method.Type: ApplicationFiled: January 17, 2003Publication date: June 12, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Robin Edwin Buckingham, Stephen Alistair Smith
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Patent number: 6576632Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.Type: GrantFiled: April 13, 2000Date of Patent: June 10, 2003Assignee: Pfizer IncInventors: Steven W. Goldstein, Kelly P. Longo, James F. Blake, Mohamed M. A. Awad, Kenneth P. Raiche, Kevin W. Kramer
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Patent number: 6555519Abstract: SGLT2 inhibiting compounds are provided having the formula wherein n is 0, 1 or 2; A is or heteroaryl which may contain 1 to 4 heteroatoms in the ring which may be selected from N, O, S, SO, and/or SO2, bearing substituents R3 and R4; and R1 to R4 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents and/or one, two or more hypolipidemic agents.Type: GrantFiled: February 23, 2001Date of Patent: April 29, 2003Assignee: Bristol-Myers Squibb CompanyInventor: William N. Washburn
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Patent number: 6511989Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: November 2, 2001Date of Patent: January 28, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6500863Abstract: Novell IL-8 compounds and methods of using them are provided.Type: GrantFiled: June 13, 2001Date of Patent: December 31, 2002Assignee: SmithKline Beecham CorporationInventors: Qi Jin, Brent W. McCleland, Michael R. Palovich, Katherine L. Widdowson
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Patent number: 6414030Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I in which R1, R2, E, X, Y and Z have the meanings described herein, show effects on the autonomous nervous system. The invention relates to the use of the compounds of the formula I in the treatment and prophylaxis of dysfunctions of the autonomous nervous system, in particular of vagal dysfunctions, for example in the case of cardiovascular diseases. The invention also relates to the use of compounds of the formula I in combination with beta-receptor blockers and to products and pharmaceutical preparations which comprise at least one compound of the formula I and at least one beta-receptor blocker, and to novel compounds.Type: GrantFiled: November 9, 2001Date of Patent: July 2, 2002Assignee: Aventis Pharma Deutschland, GmbHInventors: Klaus Wirth, Heinrich Christian Englert, Helmut Bohn, Heinz Gögelein, Holger Heitsch, Uwe Gerlach
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Publication number: 20020082300Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I 1Type: ApplicationFiled: November 9, 2001Publication date: June 27, 2002Inventors: Klaus Wirth, Heinrich Christian Englert, Helmut Bohn, Heinz Gogelein, Holger Heitsch, Uwe Gerlach
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Patent number: 6399824Abstract: Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by reaction of a compound II with guanidine.Type: GrantFiled: September 18, 2001Date of Patent: June 4, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Armin Hofmeister, Max Hropot, Uwe Heinelt, Markus Bleich, Hans-Jochen Lang
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Patent number: 6350778Abstract: The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: May 19, 2000Date of Patent: February 26, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert, Klaus Wirth, Heinz Gögelein
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Patent number: 6140368Abstract: The present invention relates to a novel class of compounds that are potent inhibitors of HIV reverse transcriptase and HIV integrase. In addition to being multienzyme inhibitors, the inventive compounds of the present invention are remarkable in at least two other respects. First, they do not appear to be toxic to cells at typical therapeutic concentrations. Second, they appear to be equally effective against mutant strains of HIV reverse transcriptase commonly found in patients who have developed resistance to current reverse transcriptase inhibitors. Because the inventive compounds show promise in combatting viral resistance and are potent inhibitors of both HIV reverse transcriptase and integrase, they are ideal candidates for use in combination with existing therapies or alone in treating AIDS or HIV infection.Type: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignees: The Regents of the University of California, Rutgers, The University of New JerseyInventors: George L. Kenyon, Margaret Stauber, Karl Maurer, Dolan Eargle, Angelika Muscate, Andrew Leavitt, Diana C. Roe, Todd J. A. Ewing, Allan G. Skillman, Jr., Edward Arnold, Irwin D. Kuntz, Malin Young
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Patent number: 6103761Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: October 19, 1994Date of Patent: August 15, 2000Assignee: Warner-Lambert CompanyInventors: Bradley Dean Tait, Michael William Wilson
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Patent number: 6071910Abstract: A therapeutic method comprising counteracting or preventing pathologies mediated by IL-5, including those characterized by eosinophil infiltration, degranulation and inflammation, by administering to a mammal in need of such therapy, one or more compounds that bind to the eosinophil sulfonylurea receptor, optionally in combination with one or more topical anesthetics and/or glucocorticoids.Type: GrantFiled: December 5, 1997Date of Patent: June 6, 2000Assignee: Mayo Foundation for Medical Education and ResearchInventors: Gerald J. Gleich, Jennifer L. Bankers-Fulbright
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Patent number: 6011049Abstract: Combinations of a glitazone antidiabetic agent and a biguanide antidiabetic agent, and optionally a sulfonylurea antidiabetic agent, are useful for treating diabetes mellitus and improving glycemic control.Type: GrantFiled: November 9, 1998Date of Patent: January 4, 2000Assignee: Warner-Lambert CompanyInventor: Randall Wayne Whitcomb
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Patent number: 5981595Abstract: A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.Type: GrantFiled: July 1, 1993Date of Patent: November 9, 1999Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, William Howard Roark, Bruce David Roth
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Patent number: 5977177Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: June 4, 1998Date of Patent: November 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5972973Abstract: Combinations of a sulfonylurea antidiabetic agent and a glitazone antidiabetic agent are useful for treating diabetes mellitus and improving glycemic control.Type: GrantFiled: October 16, 1998Date of Patent: October 26, 1999Assignee: Warner-Lambert CompanyInventor: Randall Wayne Whitcomb
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Patent number: 5885980Abstract: A method of treating diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a pharmaceutically acceptable VO.sup.+2 generating compound and a therapeutically effective amount of micronized glyburide.Type: GrantFiled: June 25, 1996Date of Patent: March 23, 1999Assignee: Enrique G. GutierrezInventors: Enrique G. Gutierrez, Reynold Leboeuf
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Patent number: 5880155Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 15, 1996Date of Patent: March 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5859037Abstract: Combinations of a sulfonylurea antidiabetic agent and a glitazone antidiabetic agent are useful for treating diabetes mellitus and improving glycemic control.Type: GrantFiled: November 13, 1997Date of Patent: January 12, 1999Assignee: Warner-Lambert CompanyInventor: Randall Wayne Whitcomb
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Patent number: 5856360Abstract: This invention is directed to a pharmacologically acceptable composition for inhibiting or treating hemorrhagic shock in a mammal. The composition includes a K.sub.ATP inhibitor and a pharmacologically acceptable carrier, with the K.sub.ATP inhibitor being present in an amount sufficient to inhibit or treat hemorrhagic shock in the mammal. The invention is also directed to a method for inhibiting or treating hemorrhagic shock in a mammal. The method includes administering to the mammal an amount of a K.sub.ATP channel inhibitor sufficient to inhibit or treat hemorrhagic shock in the mammal. In a preferred form of the invention, the K.sub.Type: GrantFiled: May 3, 1996Date of Patent: January 5, 1999Assignee: Children's Hospital Medical CenterInventors: Andrew L. Salzman, Csaba Szabo
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Patent number: 5776980Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: November 7, 1996Date of Patent: July 7, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5698596Abstract: Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticalsBenzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: September 3, 1996Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5677344Abstract: A method is provided for treatment of Parkinson's disease or controlling movement of a Parkinsonian patient by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, (for example, tolbutamide), or quinine.Type: GrantFiled: May 24, 1993Date of Patent: October 14, 1997Assignee: E. R. Squibb & Sons, Inc.Inventors: Susan A. Greenfield, Denyse Levesque
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Patent number: 5652268Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use as a medicament or diagnostic, and medicament containing them.Substituted benzenesulfonylureas and -thioureas 1 ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 15, 1996Date of Patent: July 29, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5633239Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit outstanding effects on the cardiovascular system.Type: GrantFiled: February 16, 1996Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz G ogelein, Joachim Kaiser
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Patent number: 5607976Abstract: Substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use for the production of pharmaceutical preparations, and pharmaceutical preparations containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 8, 1996Date of Patent: March 4, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Peter Crause, Dieter Mania, Heinz G ogelein, Joachim Kaiser
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Patent number: 5574069Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto) alk (oxy) yl, E is O or S; Y is --[CR(3).sub.2 ]n-, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: February 23, 1995Date of Patent: November 12, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5565494Abstract: This invention provides certain benzenesulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier, and processes for preparing the benzenesulfonamide derivatives.Type: GrantFiled: March 10, 1995Date of Patent: October 15, 1996Assignee: Eli Lilly and CompanyInventors: Gerald B. Grindey, Cora S. Grossman, J. Jeffry Howbert, Karen L. Lobb, James E. Ray, John E. Toth
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Patent number: 5451580Abstract: A method is provided for treatment of neuronal insult, such as caused by lack of oxygen, which neurons are prone to Parkinsonian degeneration by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, for example, tolbutamide.Type: GrantFiled: September 22, 1993Date of Patent: September 19, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Kerry P. S. J. Murphy, Susan A. Greenfield
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Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5288757Abstract: The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels, pharmaceutical compositions and methods of using the ACAT inhibitors and closely related compounds which are also aminosulfonyl urea compounds.Type: GrantFiled: February 19, 1993Date of Patent: February 22, 1994Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5258406Abstract: This invention provides certain sulfonimidamide compounds, formulations and method of use of these compounds in treating susceptible neoplasms.Type: GrantFiled: December 16, 1992Date of Patent: November 2, 1993Assignee: Eli Lilly and CompanyInventors: John E. Toth, James E. Ray
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Patent number: 5234922Abstract: Methods for the treatment of secretory diarrhea comprised of administering to a patient in need thereof, an effective amount of a CFTR chloride channel blocker or a potassium channel opener are disclosed. The CFTR chloride channel blocker is a sulfonylurea of the group consisting of tolbutamide, glibenclamide, and related analogs. The potassium channel opener is selected from the group consisting of diazoxide, lemakalim, and minoxidil sulfate.Type: GrantFiled: September 28, 1992Date of Patent: August 10, 1993Assignee: University of Iowa Research FoundationInventors: Michael J. Welsh, David N. Sheppard
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Patent number: 5234955Abstract: This invention provides certain N-phenyl-N'-substitutedphenylsulfonylureas compounds, formulations, and a method for treating susceptible neoplasms in mammals using the sulfonylurea compounds.Type: GrantFiled: December 20, 1991Date of Patent: August 10, 1993Assignee: Eli Lilly and CompanyInventors: James E. Ray, John E. Toth, J. Jeffry Howbert
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Patent number: 5215985Abstract: A method is provided for treatment of neuronal insult, such as caused by lack of oxygen, by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, for example, tolbutamide.Type: GrantFiled: January 27, 1992Date of Patent: June 1, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Kerry P. S. J. Murphy, Susan A. Greenfield
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Patent number: 5214206Abstract: The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels, pharmaceutical compositions and methods of using the ACAT inhibitors and closely related compounds which are also aminosulfonyl urea compounds.Type: GrantFiled: August 19, 1991Date of Patent: May 25, 1993Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5116861Abstract: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.Type: GrantFiled: August 3, 1990Date of Patent: May 26, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Shigenori Ohkawa, Shoji Fukumoto
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Patent number: 5047429Abstract: A method is described for treating and/or preventing pulmonary oedema in patients comprising administering a suphonylurea compound or a pharmaceutically acceptable salt thereof to patients who suffer from or are susceptible to oedema. Glucose may also be simultaneously administered to the patients to prevent hypoglycemia.Type: GrantFiled: April 18, 1989Date of Patent: September 10, 1991Assignee: Hoechst AktiengesellschaftInventor: Piers C. G. Nye
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Patent number: 4916163Abstract: An improved, more bioavailable formulation of glyburide is provided which consists preponderantly by weight of spray-dried lactose is described. This formulation utililzes micronized glyburide, but is more economically manufacatured than heretofore known micronized glyburide formulations.Type: GrantFiled: June 4, 1985Date of Patent: April 10, 1990Assignee: The Upjohn CompanyInventor: Philip F. Ni
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Patent number: 4623658Abstract: Pesticidal benzoylurea compounds of the formula: ##STR1## wherein R represents a moiety --C(O)OR.sup.1 or --NR.sup.2 R.sup.3, and the meanings of each of the other symbols is described in the specification.Type: GrantFiled: February 3, 1986Date of Patent: November 18, 1986Assignee: Shell Oil CompanyInventor: Martin Anderson
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Patent number: 4562208Abstract: The new N-sulphenylated ureas can be prepared by reaction of the corresponding N-substituted carbamic acid-fluorides and a primary or secondary amine in the presence of a diluent and an acid-binding agent. They have microbicidal properties and can be used in particular for the protection of industrial materials and of plants.Type: GrantFiled: February 15, 1983Date of Patent: December 31, 1985Assignee: Bayer AktiengesellschaftInventors: Engelbert Kuhle, Wilfried Paulus, Hermann Genth, Wilhelm Brandes, Paul Reinecke