Chalcogen Bonded Directly To Chalcogen Patents (Class 514/347)
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Publication number: 20020035135Abstract: Novel, stable pharmaceutical formulations for the oral administration of high purity torsemide modification II are disclosed. These formulations release high purity torsemide modification II in water at a constant and high purity rate, and the high purity torsemide modification II therein does not rearrange to torsemide modification I over time. Methods for their manufacture are also disclosed.Type: ApplicationFiled: February 21, 2001Publication date: March 21, 2002Inventors: Minutza Leibovici, Ruth Tenengauzer, Mira Kopel, Judith Aronhime, Marco Kordova
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Publication number: 20020016346Abstract: Elevated intra-ocular pressure is reduced by administration directly to the eye of compounds that inhibit function of a Na+—K+—2Cl−2 cotransporter mechanism discovered in trabecular meshwork cells of mammalian eyes. These compounds are useful in treatment of diseases of the eye associated with elevated intra-ocular pressure, such as ocular hypertension and glaucoma. A screening method is provided to discover additional compounds with utility for lowering intra-ocular pressure by substantially inhibiting the Na+—K+—Cl−2 cotransporter mechanism in trabecular meshwork cells.Type: ApplicationFiled: February 16, 2001Publication date: February 7, 2002Applicant: The Regents University of California, a California CorporationInventors: James D. Brandt, Martha E. O'Donnell, Fitz-Roy E. Curry
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Patent number: 6316459Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyType: GrantFiled: October 25, 1994Date of Patent: November 13, 2001Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
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Patent number: 6297282Abstract: The present application relates to compounds of formula (I) wherein A represents oxygen, sulfur or —NH—, m is 0-2, and R1, R2, R3, R6 and R7 have the meanings given in the specification, to a process for their preparation, as well as to their use in the inhibition of cyclooxygenase II.Type: GrantFiled: October 26, 1999Date of Patent: October 2, 2001Assignee: Nycomed Austria GmbHInventors: Michael Hartmann, Peter Kremminger, Heinz Blaschke, Dagmar Stimmeder, Harald Fellier, Franz Rovenszky
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Patent number: 6291516Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.Type: GrantFiled: October 14, 1999Date of Patent: September 18, 2001Assignee: Curis, Inc.Inventors: Henryk Dudek, Benxiu Ji
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Patent number: 6288086Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: June 14, 2000Date of Patent: September 11, 2001Assignee: American Cyanamid CompanyInventor: Aranapakam Mudumbai Venkatesan
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Patent number: 6284767Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: December 8, 1998Date of Patent: September 4, 2001Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Dale J. Kempf, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, John M. Lipari, Laman Alani, Soumojeet Ghosh, Rong R. Gao, Dilip Kaul
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Patent number: 6281212Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof. Z is a substituted or unsubstitured aromatic group. Y is a covalent bond, —O— or —CO—. n is an integer from one to about five. X is a covalent bond or —CO—. Ra is an aliphatic or a substituted aliphatic group; Rb is an aliphatic group substituted with an aromatic group or substituted aromatic group; and, taken together with the nitrogen atom bonded to Ra and Rb, can form a substituted or unsubstituted non-aromatic heterocyclic ring.Type: GrantFiled: July 11, 1997Date of Patent: August 28, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Patent number: 6251917Abstract: Compounds of the formula where R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.Type: GrantFiled: May 26, 1999Date of Patent: June 26, 2001Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber
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Patent number: 6228873Abstract: Elevated intra-ocular pressure is reduced by administration directly to the eye of compounds that inhibit function of a Na+—K+—2Cl−2 cotransporter mechanism discovered in trabecular meshwork cells of mammalian eyes. These compounds are useful in treatment of diseases of the eye associated with elevated intra-ocular pressure, such as ocular hypertension and glaucoma. A screening method is provided to discover additional compounds with utility for lowering intra-ocular pressure by substantially inhibiting the Na+—K+—Cl−2 cotransporter mechanism in trabecular meshwork cells.Type: GrantFiled: June 8, 1998Date of Patent: May 8, 2001Assignee: The Regents of the University of CaliforniaInventors: James D. Brandt, Martha E. O'Donnell, Fitz-Roy E. Curry
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Patent number: 6201024Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: January 26, 1999Date of Patent: March 13, 2001Assignee: AstraZeneca UK LimitedInventors: Andrew Baxter, Thomas McInally, Michael Mortimore, David Cladingboel
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Patent number: 6200995Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: January 20, 1999Date of Patent: March 13, 2001Assignee: Tularik Inc.Inventors: Fabienne De la Brouse-Elwood, Jin-Long Chen, Timothy D. Cushing, John A. Flygare, Jonathan B. Houze, Juan C. Jaen, Lawrence R. McGee, Shi-Chang Miao, Steven Marc Rubenstein, Patrick C. Kearney
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Patent number: 6200996Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: January 27, 2000Date of Patent: March 13, 2001Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
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Patent number: 6187944Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.Type: GrantFiled: August 16, 1999Date of Patent: February 13, 2001Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
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Patent number: 6166045Abstract: A new modification of torasemide, named modification III, has been discovered. Modification III is storage stable and achieves high levels in serum shortly after oral administration. Torasemide of modification III can be used to produce a diuretic effect. A method of making torasemide of modification III is disclosed.Type: GrantFiled: June 2, 1998Date of Patent: December 26, 2000Assignee: Roche Diagnostics GmbHInventors: Bruno Dreckmann-Behrendt, Artur Burger, Judith M. Rollinger
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Patent number: 6100266Abstract: For the treatment of cancer, inflammation, and other conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or enzymes involved in the shedding of L-selectin, CD23, the TNF receptors, IL-1 receptors, or IL-6 receptors, disclosed are compounds of the general formulaB--X--(CH.sub.2).sub.m --(CR.sup.1 R.sup.2).sub.n --W--COY.Type: GrantFiled: January 29, 1999Date of Patent: August 8, 2000Assignee: Darwin Discovery LimitedInventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen
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Patent number: 6093828Abstract: A novel physical form of (E)-3-[6-[[(2,6-dichlorophenyl)-thio]methyl]-3-(2-phenylethoxy)-2-pyridiny l]-2-propenoic acid and its use in therapy is disclosed.Type: GrantFiled: December 16, 1997Date of Patent: July 25, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Victor Witold Jacewicz, Michael Anthony Harris, Richard Keith Anderson
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Patent number: 6057362Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease-hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 11, 1999Date of Patent: May 2, 2000Assignee: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6046217Abstract: 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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: September 11, 1998Date of Patent: April 4, 2000Assignee: Merck Frosst Canada & Co.Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
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Patent number: 5955505Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.Type: GrantFiled: August 20, 1997Date of Patent: September 21, 1999Assignee: Nippon Suisan Kaisha, Ltd.Inventors: Jiro Takeo, Shinya Yamashita, Keiji Wada, Yoshiyuki Chiba
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Patent number: 5914336Abstract: A method of controlling the serum solubility of orally administered torasemide is disclosed. A new crystallin modification of torasemide, called modification III which has significantly higher rates of solubilization than the known crystallin form of torasemide, modification I, is blended with amounts of modification I to produce a preselected level of torasemide in serum at a given time following administration. Compositions containing amounts of modification I and modification III, sufficient to achieve the desired serum levels of torasemide, are also disclosed.Type: GrantFiled: June 2, 1998Date of Patent: June 22, 1999Assignee: Boehringer Mannheim GmbHInventor: Bruno Dreckmann-Behrendt
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Patent number: 5914340Abstract: This invention provides methods for the treatment or inhibiting of dermatitis which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B.sub.4 antagonist.Type: GrantFiled: March 13, 1998Date of Patent: June 22, 1999Assignee: Eli Lilly and CompanyInventors: Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
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Patent number: 5902817Abstract: The present invention relates to thio derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: GrantFiled: April 9, 1997Date of Patent: May 11, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. Maclin, Barbara S. Slusher
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Patent number: 5883131Abstract: A compound of the formula ##STR1## wherein n, p, q, X, Y, Z and Ar are as defined herein, useful in the treatment of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis or other diseases characterized by matrix metalloprotenase activity, as well as AIDS, sepsis, septic shock or other diseases involving the production of TNF.Type: GrantFiled: July 9, 1997Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Laurence E. Burgess, James P. Rizzi, David J. Rawson
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Patent number: 5817684Abstract: This invention provides methods for the treatment or prevention of cerebral focal ischemia which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a leukotriene B.sub.4 antagonist.Type: GrantFiled: December 2, 1997Date of Patent: October 6, 1998Assignee: Eli Lilly and CompanyInventors: Jerome H. Fleisch, William T. Jackson, Jason S. Sawyer
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Patent number: 5792778Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.Type: GrantFiled: August 8, 1996Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
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Patent number: 5773459Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Gerald McMahon
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Patent number: 5700460Abstract: A method for attracting and controlling insects comprising offering to said insects for ingestion an effective amount of a compound of the formula: ##STR1## wherein the structural variables are as defined in the specification.Type: GrantFiled: October 10, 1996Date of Patent: December 23, 1997Assignee: Rhone-Poulenc Inc.Inventors: Thomas Charles Davidson, Georgina M. Werner
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Patent number: 5679695Abstract: The present invention relates to a method of treating a retrovirus utilizing a compound of the formula(R.sub.2).sub.n R.sub.1 --Ar--X--Y--R(T.sub.1)(T.sub.2).sub.m IThe present invention also relates to pharmaceutical compositions in which the active ingredient has a compound of formula I.Type: GrantFiled: January 25, 1995Date of Patent: October 21, 1997Assignee: The University of ConnecticutInventor: Frederick William Wassmundt
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Patent number: 5670528Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 - are hydrogen or alkyl,Y is a group ##STR2## --O--CH.sub.2, --CH.sub.2 --O--, --S--CH.sub.2 --, --CH.sub.2 --S--, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 --O--N.dbd.C(R')-- andR is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.Type: GrantFiled: November 22, 1995Date of Patent: September 23, 1997Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5637624Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: March 9, 1993Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Sulfonamidocarbonylpyridine-2-carboxamides and pyridine-n-oxides which are useful as pharmaceuticals
Patent number: 5610172Abstract: Sulfonamidocarbonylpyridine-2-carboxamides and their pyridine-N-oxides, process for their preparation, and their use as pharmaceuticalsThe invention relates to sulfonamidocarbonylpyridine-2-carboxamides and their pyridine-N-oxides according to the formula I ##STR1## Said compounds are used as pharmaceuticals against fibrotic disorders, as fibrosuppressants and as inhibitors of proline hydroxylase and of collagen biosynthesis.Type: GrantFiled: March 24, 1995Date of Patent: March 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Martin Bickel, Volkmar G unzler-Pukall -
Patent number: 5596008Abstract: A class of substitute pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1 is haloalkyl; wherein R.sup.2 is aryl optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfinyl, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, halo, alkoxy and alkylthio; wherein R.sup.3 is aryl substituted at a substitutable position with a radical selected from alkylsulfonyl and sulfamyl; and wherein R.sup.4 is selected from halo, alkoxy and alkynyloxy; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 10, 1995Date of Patent: January 21, 1997Assignee: G. D. Searle & Co.Inventor: Len F. Lee
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Patent number: 5589492Abstract: A compound of the formula A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; A.sup.2 represents a benzene ring having three optional substituents; A.sup.3 represents a moiety of formula --(CH.sub.2).sub.m --CHR.sup.1 -- wherein R.sup.1 represents a halogen atom or a moiety of formula S(O).sub.p A.sup.4 wherein A.sup.4 represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl, alkylcarbonyl or an aromatic heterocyclyl group and p represents zero or an integer 1 or 2 and m represents zero or an integer in the range of from 1 to 5, or A.sup.3 represents a moiety of formula --CH.dbd.CR.sup.1 -- wherein R.sup.1 is as defined above; R.sup.2 represents OR.sup.3 wherein R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, or R.sup.2 represents --NR.sup.4 R.sup.Type: GrantFiled: December 12, 1994Date of Patent: December 31, 1996Assignee: SmithKline Beecham PLCInventor: David Haigh
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Patent number: 5587367Abstract: A pharmaceutical or cosmetic composition is disclosed comprising in combination a retinoid and a sterol capable of inhibiting the biosynthesis of cholesterol resulting in a synergistic effect in the treatment of disorders of epidermic keratinization, proliferation and/or sebaceous function.Type: GrantFiled: May 23, 1995Date of Patent: December 24, 1996Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)Inventors: Uwe Reichert, Rainer Schmidt, Braham Shroot
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Patent number: 5583091Abstract: A composition comprises (a) halogenated aromatic 1,2- or 1,3- dinitrile, (b) a substituted urea and (c) a halogen-containing aromatic alkyl sulphoxide or sulphone. The composition may include other materials for example inorganic diluents such as silica, alumina, titanium, dioxide, zinc oxide, etc. and may also include other anti-microbial agents such are anti-bacterial agents. The composition has anti-microbial properties, particularly anti-fungal and anti-algal properties. The composition can be incorporated into materials such as paint or plastics to provide anti-microbial properties.Type: GrantFiled: December 7, 1994Date of Patent: December 10, 1996Assignee: Zeneca LimitedInventors: Bryan S. Backhouse, Malcolm Greenhalgh
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Patent number: 5565485Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: August 22, 1994Date of Patent: October 15, 1996Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy J. Kevin, Douglas J. Pettibone, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Richard B. Toupence, Jay M. Matthews
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Patent number: 5504081Abstract: The present invention relates to the use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for combating fish parasites.Type: GrantFiled: September 22, 1993Date of Patent: April 2, 1996Assignee: Bayer AktiengesellschaftInventors: Reinhold Lohr, Hans-Christian Mundt, Peter Andrews
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Patent number: 5486530Abstract: Use of torasemide for the treatment of brain edemas and orally and parenterally administerable torasemide.Type: GrantFiled: January 30, 1995Date of Patent: January 23, 1996Assignee: Boehringer Mannheim GmbHInventors: Tim Boelke, Lothar Kling, Reinhard Koenig
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Patent number: 5470819Abstract: This invention relates to derivatives of acrylic acid useful in agriculture (especially as fungicides but also as plant growth regulators, insecticides and nematocides), to processes for preparing them, to agricultural (especially fungicidal) compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants, to regulate plant growth and to kill or control insect or nematode pests.The invention provides a compound having the formula (I): ##STR1## and stereoisomers thereof, wherein W is a substituted pyridinyl or substituted pyrimidinyl group linked to A by any of its ring carbon atoms; A is either an oxygen atom or S(O).sub.n wherein n is 0, 1 or 2; X, Y and Z, which are the same or different, are hydrogen or halogen atoms, or hydroxy, optionally substituted alkyl (including haloalkyl), optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy.Type: GrantFiled: May 9, 1994Date of Patent: November 28, 1995Assignee: Zeneca LimitedInventors: Vivienne M. Anthony, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Ian Ferguson, Patrick J. Crowley, Michael G. Hutchings
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Patent number: 5462954Abstract: Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.Type: GrantFiled: November 1, 1994Date of Patent: October 31, 1995Assignee: Eli Lilly and CompanyInventors: S. Richard Baker, Robert D. Dillard, Paul E. Floreancig, J. Scott Sawyer, Michael J. Sofia
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Patent number: 5457118Type: GrantFiled: April 20, 1994Date of Patent: October 10, 1995Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele
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Patent number: 5411973Abstract: Compounds of formula I ##STR1## wherein X, A, B, R.sup.1 and R.sup.2 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable ester thereof, processes for preparing the compounds and pharmaceutical compositions comprising them. The compounds are useful as potassium channel openers and as therapeutic agents in the treatment of urinary incontinence.Type: GrantFiled: May 18, 1993Date of Patent: May 2, 1995Assignee: Zeneca LimitedInventors: Keith Russell, James R. Empfield, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5403850Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 --or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H,(2) C1-16 alkyl or (3) the formula ##STR3## wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR4## is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula:--SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H C1-4 alkyl or benzyl; or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.Type: GrantFiled: April 29, 1994Date of Patent: April 4, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Tadao Okegawa
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Patent number: 5401757Abstract: A composition comprises (a) halogenated aromatic 1,2- or 1,3-dinitrile, (b) a substituted urea and (c) a halogen-containing aromatic alkyl sulphoxide or sulphone. The composition may include other materials for example inorganic diluents such as silica, alumina, titanium, dioxide, zinc oxide, etc. and may also include other anti-microbial agents such as anti-bacterial agents. The composition has anti-microbial properties, particularly anti-fungal and anti-algal properties. The composition can be incorporated into materials such as paint or plastics to provide anti-microbial properties.Type: GrantFiled: October 18, 1993Date of Patent: March 28, 1995Assignee: Zeneca LimitedInventors: Bryan S. Backhouse, Malcolm Greenhalgh
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Patent number: 5391559Abstract: The invention relates to the compound of formula (I) ##STR1## and the addition salts thereof with a pharmaceutically acceptable acid or base.A pharmaceutical product which is useful for treating an ischemic or hypoxic disorder or a peripheral or central oedema.Type: GrantFiled: January 5, 1993Date of Patent: February 21, 1995Assignee: Adir et CompagnieInventors: Bernard Masereel, Bernard Pirotte, Marc Schynts, Jacques Delarge
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Patent number: 5366982Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the general formula ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: February 17, 1993Date of Patent: November 22, 1994Assignee: Rhone-Poulenc Rorer S.A.Inventors: Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles