Plural C=o Groups, Other Than As Ketone Or Aldehyde Patents (Class 514/121)
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Patent number: 6174874Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.Type: GrantFiled: September 17, 1999Date of Patent: January 16, 2001Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Claude Dufresne, Yves Leblanc, Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien, Patrick Roy
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Patent number: 6030961Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound hearing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and in particular, augmenting expression of tumor suppressor genes, inducing tolerance to antigens, treating, preventing or ameliorating protozoan infection, or inhibiting histone deacetylase in cells. The compositions of the invention are to and the methods of the invention use oxyalkalene phosphate compounds.Type: GrantFiled: March 11, 1997Date of Patent: February 29, 2000Assignees: Bar-Ilan Research & Development Co., Ltd., Mor Research Applications Ltd.Inventors: Abraham Nudelman, Ada Rephaeli
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Patent number: 5955453Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.Type: GrantFiled: April 24, 1998Date of Patent: September 21, 1999Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Tao Jiang
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Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments
Patent number: 5955452Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 26, 1998Date of Patent: September 21, 1999Assignee: Roche Diagnostics GmbHInventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss -
Patent number: 5939455Abstract: This invention provides a method of augmenting the therapeutic activity of an oxyalkylene-containing compound, butyric acid, a butyric acid salt or butyric acid derivative by administering an inhibitor of .beta.-oxidation of fatty acids to a patient or to host cells. Pharmaceutical compositions are also included.Type: GrantFiled: March 11, 1997Date of Patent: August 17, 1999Assignee: Beacon Laboratories, Inc.Inventor: Ada Rephaeli
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Patent number: 5908610Abstract: Disclosed are injectable suspensions of gas filled microbubbles in an aqueous carrier liquid usable as contrast agents in ultrasonic echography. The suspensions comprise amphipathic compounds of which at least one may be a laminarized phospholipid as a stabiliser of the microbubbles against collapse with time and pressure. The concentration of phospholipids in the carrier liquid is below 0.01% wt but is at least equal to or above that at which phospholipid molecules are present solely at the gas microbubble-liquid interface. Also disclosed is a method of preparation of the stable suspensions of air or gas filled microbubbles.Type: GrantFiled: June 26, 1997Date of Patent: June 1, 1999Assignee: Bracco International B.V.Inventors: Michel Schneider, Jean Brochot, Jerome Puginier, Feng Yan
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Patent number: 5880112Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: April 8, 1997Date of Patent: March 9, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5863536Abstract: The present invention includes phosphoramidate derivatives, compositions containing the same, and methods of using them as NAALADase inhibitors, particularly for the treatment of glutamate abnormalities and associated nervous tissue insult in a animal and for treatment of prostate disease and prostate cancer by inhibition of NAALADase enzyme.Type: GrantFiled: December 31, 1996Date of Patent: January 26, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher, Kevin L. Tays, Keith M. Maclin
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Patent number: 5846955Abstract: This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: ##STR1## or pharmaceutically acceptable salts thereof wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or ##STR2## and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources;R.sub.3 is hydrogen or lower alkyl andR.sub.Type: GrantFiled: June 6, 1995Date of Patent: December 8, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Charles Pidgeon, Robert J. Markovich
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Patent number: 5824661Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.Type: GrantFiled: September 7, 1994Date of Patent: October 20, 1998Assignee: The Procter & Gamble CompanyInventors: Marion David Francis, Susan Mary Kaas, Frank Hallock Ebetino
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Patent number: 5712261Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.Type: GrantFiled: June 21, 1995Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5709890Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 20, 1997Date of Patent: January 20, 1998Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5686060Abstract: Disclosed are injectable suspensions of gas filled microbubbles in an aqueous carrier liquid usable as contrast agents in ultrasonic echography. The suspensions comprise amphipathic compounds of which at least one may be a laminarized phospholipid as a stabilizer of the microbubbles against collapse with time and pressure. The concentration of phospholipids in the carrier liquid is below 0.01% wt but is at least equal to or above that at which phospholipid molecules are present solely at the gas microbubble-liquid interface. Also disclosed is a method of preparation of the stable suspensions of air or gas filled microbubbles.Type: GrantFiled: April 12, 1995Date of Patent: November 11, 1997Assignee: Bracco International BVInventors: Michel Schneider, Jean Brochot, Jerome Puginier, Feng Yan
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Patent number: 5683994Abstract: Compounds of formula I are disclosed, ##STR1## as well as processes for their production and pharmaceutical agents containing these compounds suitable for treating disorders of calcium metabolism.Type: GrantFiled: December 18, 1995Date of Patent: November 4, 1997Assignee: Boehringer Mannheim GmbHInventors: Christos Tsaklakidis, Angelika Esswein, Gerd Zimmermann, Frieder Bauss
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Patent number: 5646133Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 14, 1996Date of Patent: July 8, 1997Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5597549Abstract: Disclosed are injectable suspensions of gas filled microbubbles in an aqueous carrier liquid usable as contrast agents in ultrasonic echography. The suspensions comprise amphipathic compounds of which at least one may be a laminarized phospholipid as a stabilizer of the microbubbles against collapse with time and pressure. The concentration of phospholipids in the carrier liquid is below 0.01% wt but is at least equal to or above that at which phospholipid molecules are present solely at the gas microbubble-liquid interface. Also disclosed is a method of preparation of the stable suspensions of air or gas filled microbubbles.Type: GrantFiled: March 31, 1995Date of Patent: January 28, 1997Assignee: Bracco International B.V.Inventors: Michel Schneider, Jean Brochot, Jerome Puginier, Feng Yan
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Patent number: 5591728Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents a hydroxyl, alkoxy or amino (unsubstituted or substituted) group,R.sub.2 represents an unsubstituted or substituted alkyl group,X.sub.1 represents --NH--,X.sub.2 represents --O--,R.sub.3 represents a hydrogen atom or an alkyl or phenyl group,R.sub.4 represents an alkyl group which is always substituted with one or more hydroxyl, benzyloxy, benzyloxycarbonylamino, amino, mono- or dialkylamino, acetoxy or 2,2-dimethyl-1,3-dioxolan-4-yl groups, such groups being identical or different,R.sub.5 represents a 3-indolylmethyl, naphthylmethyl, alkyl, phenyl or benzyl group, its isomers as well as its addition salts with a pharmaceutically acceptable acid or base,and medicinal products containing the same are useful as endothelin convertase inhibitor.Type: GrantFiled: July 3, 1995Date of Patent: January 7, 1997Assignee: Adir Et CompagnieInventors: Guillaume de Nanteuil, Georges Remond, Tony Verbeuren
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Patent number: 5563129Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.Type: GrantFiled: April 24, 1995Date of Patent: October 8, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5527789Abstract: A method of combatting cancer in a subject comprising administering to said subject dehydroepiandrosterone (DHEA) or an analog thereof in an amount effective to combat cancer is disclosed in which heart failure induced by the DHEA or analog thereof is combatted by administering to the subject a ubiquinone, in an amount effective to combat heart failure induced by the DHEA or analog thereof.A prefered DHEA analog for carrying out the invention is 16 alpha-fluoroepiandrosterone, and a preferred ubiquinone for carrying out the invention is Coenzyme Q.sub.10.Type: GrantFiled: August 2, 1994Date of Patent: June 18, 1996Assignee: East Carolina UniversityInventor: Jonathan W. Nyce
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Patent number: 5484833Abstract: Novel derivatives of non-steroidal anti-inflammatory, analgesic and/or antipyretic substances are provided which are useful in the treatment of superficial or deep inflammatory conditions, such as erythemas of various origins, inflammation of the joints or inflammation of bacterial origin.The derivatives of the invention are salts of non-steroidal anti-inflammatory, analgesic and/or antipyretic substances (NSAs) and phosphatidic acidsand preferably have the formula[NSA].sub.x [PA].sub.ywhereinNSA represents a cation derived from said non-steroidal anti-inflammatory analgesic and/or antipyretic substance,PA represents a phosphatidic acid or a mixture of different phosphatidic acids, andx:y is from 2:1 to 1:2.Type: GrantFiled: July 30, 1992Date of Patent: January 16, 1996Assignee: Indena S.p.A.Inventor: Ezio Bombardelli
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Patent number: 5470845Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.Type: GrantFiled: July 5, 1994Date of Patent: November 28, 1995Assignee: Bristol-Myers Squibb CompanyInventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5411948Abstract: Methods for the in vitro and in vivo inhibition of microbial colonization are provided. The methods use host cell phospholipid molecules ("receptors") which bind microorganisms.Type: GrantFiled: June 16, 1993Date of Patent: May 2, 1995Assignees: HCS Research and Development, MicroCarb, Inc.Inventors: Clifford A. Lingwood, Howard C. Krivan, Bo Nilsson
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Patent number: 5407913Abstract: This is a method for enhancing systemic tissue repair in patients with burns, trauma and peptic ulcers, as well as patients about to undergo, is undergoing or just having undergone surgery. The method comprises systemically administering to such individuals a therapeutic composition comprising IGF and IGFBP. The preferred form is IGF-I/IGFBP-3.Type: GrantFiled: December 3, 1992Date of Patent: April 18, 1995Assignee: Celtrix Pharmaceuticals, Inc.Inventors: Andreas Sommer, Christopher A. Maack
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Patent number: 5336671Abstract: The invention provides fungicidal compositions containing benzyl-tris(aryl)-phosphonium salts of the general formula ##STR1## in which R.sup.1 represents an optionally substituted alkyl or alkoxy group; R.sup.2 represents a hydrogen atom or an optionally substituted alkyl group; R.sup.3, R.sup.4 and R.sup.5 independently represent a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group; and A.sup.- represents an anion processes for the preparation of such compounds. Certain of the compounds of formula I are novel and the invention therefore also provides processes for the preparation of such compounds and their use as fungicides.Type: GrantFiled: October 18, 1991Date of Patent: August 9, 1994Assignee: Shell Research LimitedInventors: Heinz-Manfred Becher, Guido Albert, Jurgen Curtze
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Patent number: 5324747Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: July 15, 1992Date of Patent: June 28, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
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Patent number: 5280020Abstract: A drug is described which includes a physico-chemical complex between molecules of a phospholipid and an aminoketone derivative of fluoroglucinol which is useful, particularly when administered topically in the form of a liposomal aqueous microdispersion, for increasing the microcirculatory flow-rate and volume in the capillaries to the skin, both in normal conditions and in peripheral vasculopathy (primary or secondary Raynaud's disease), acrocyanosis and blocked arteries caused by arteriosclerosis, diabetes or endoangioitis obliterans.Type: GrantFiled: June 21, 1989Date of Patent: January 18, 1994Inventor: Sergio Bertini Curri
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Patent number: 5217972Abstract: New quinolone-carboxylic acids of the general formula (I) ##STR1## wherein the definitions for R.sub.1 -R.sub.9 are given in the description, a process for their preparation and their use as medicaments, in particular as antiviral agents.Type: GrantFiled: September 19, 1990Date of Patent: June 8, 1993Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Wolfgang Dummer, Kai Rossen, Arnold Paessens
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Patent number: 5154903Abstract: This invention pertains to an improved method of inhibiting peroxide-reduction catalytic activity and concomitant toxicity of asbestos and nonasbestos iron-containing silicates. These undesirable reactions can be substantially reduced or essentially eliminated by contacting these potentially harmful materials with an aqueous solution comprising a non-mutagenic non-toxic iron chelating agent, such as phytic acid, diethylenetriamine pentaacetic acid (DTPA) or derivatives of these.Type: GrantFiled: September 13, 1990Date of Patent: October 13, 1992Assignees: Massachusetts General Hospital, Boston Biomedical Research InstituteInventors: Philip J. Graceffa, Sigmund A. Weitzman
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Patent number: 5130306Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.Type: GrantFiled: June 6, 1990Date of Patent: July 14, 1992Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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Patent number: 5082832Abstract: Novel 2,2-dimethyl-cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein X.sub.1 and X.sub.2 are individually halogen, R.sub.1 is selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, optionally substituted aryl of 6 to 14 carbon atoms, perfluoroalkyl of 1 to 8 carbon atoms, --CN and ##STR2## R' is alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of ##STR3## Alk.sub.1 is optionally unsaturated alkyl of 1 to 8 carbon atoms no substituted or substituted with at least one functional group, Ar is aryl of 6 to 14 carbon atoms no substituted or substituted with at least one functional group, Alk.sub.2 and Alk.sub.3 and Alk.sub.2 ' and Alk.sub.Type: GrantFiled: October 18, 1989Date of Patent: January 21, 1992Assignee: Roussel UclafInventors: Joseph Cadiergue, Jean-Pierre Demoute, Jean Tessier
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Patent number: 5055459Abstract: A method for purging tumor cells from bone marrow of a host, the method comprisingextracting bone marrow cells from the host;treating extracted bone marrow cells with a therapeutic level of a compound having the structure: ##STR1## wherein R is CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, t-C.sub.4 H.sub.9 or C.sub.6 H.sub.5 ; R.sup.1 is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7).sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OCH.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.2 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 Ch.sub.2 Cl).sub.2.Type: GrantFiled: April 6, 1989Date of Patent: October 8, 1991Assignee: Board of Regents, The University of TexasInventors: Borje S. Andersson, David Farquhar
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Patent number: 4956355Abstract: Compounds of the general Formula (I) ##STR1## in which R is a hydrogen atom or a bromine atom, and R.sub.1 is a hydrogen atom, an SO.sub.2 OM group wherein M is a hydrogen or sodium atom, various sulphatide or phosphatide groups or a glucuronide group are disclosed for use in the prophylaxis and therapy of retroviral infections, especially infection by Human Immunodeficiency Virus. These compounds may be used concomitantly or in combination with various immunomodulators and/or antiviral agents.Type: GrantFiled: April 15, 1988Date of Patent: September 11, 1990Assignee: Colthurst LimitedInventor: Patrick T. Prendergast
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Patent number: 4826830Abstract: Topical application of glyciphosphoramide for treatment of cancerous ulcerations and tumor conditions are disclosed.Type: GrantFiled: July 31, 1985Date of Patent: May 2, 1989Inventors: Jui Han, Yan Sun
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Patent number: 4797391Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9,9a-disubstituted-2,3,9,9a-tetrahydro-fluoren-7-yl)o xy]alkanoic acids and alkanimidamides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.Type: GrantFiled: February 8, 1988Date of Patent: January 10, 1989Assignee: Merck & Co., Inc.Inventors: Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr., Adolph M. Pietruszkiewicz
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Patent number: 4701448Abstract: A metal salt of an organic phosphate, having good stability and cholesterol-lowering activity, is produced by reacting a known compound ##STR1## wherein R.sub.4 and R.sub.5 are hydrogen or methyl, with a reaction agent such as metal hydroxide.Type: GrantFiled: January 29, 1986Date of Patent: October 20, 1987Assignee: Asahi Denka Kogyo Kabushiki KaishaInventors: Akira Endo, Haruyuki Yamashita
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Patent number: 4588723Abstract: The invention relates to aminoalkyl-imidazothiadiazole-alkenecarboxylic acid amides, processes for their preparation, intermediates which are used in their preparation, medicaments containing said active compounds for use as antihypertensive agents, diuretics and uricosuric agents. Also included in the invention are methods for use of said compounds and compositions for the above indicated indications. The active compounds are identified herein by formula (I) and the novel intermediates used in preparing the compounds of Formula (I) are those described herein under Formula (II).Type: GrantFiled: July 26, 1984Date of Patent: May 13, 1986Assignee: Bayer AktiengesellschaftInventors: Axel Ingendoh, Horst Meyer, Bernward Garthoff
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Patent number: 4575500Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of a microorganism identified as MA-5000 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compound's structure is presented based upon analytical studies. The compound has antifungal activity.Type: GrantFiled: March 26, 1984Date of Patent: March 11, 1986Assignee: Merck & Co., Inc.Inventors: Richard W. Burg, Lucille J. Cole, Sebastian Hernandez
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Patent number: 4544651Abstract: Compounds for insecticidal control, having the formula ##STR1## in which R.sub.1 is methyl or ethyl; R.sub.2 is a straight or branched chain alkyl group having from 3 to 5 carbon atoms; R.sub.3 is hydrogen, methyl or carbomethoxy; and R.sub.4 is an alkyl group having from 1 to 4 carbon atoms, together with insecticidal compositions containing such compounds, and methods for controlling insects.Type: GrantFiled: April 16, 1984Date of Patent: October 1, 1985Assignee: Stauffer Chemical CompanyInventors: Charles G. Chavdarian, William G. Haag
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Patent number: 4541858Abstract: Novel chlorinated phosphorylmethylcarbonyl derivatives of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, aryl, aralkyl, alkoxy and aralkoxy andR.sup.2 represents an optionally substituted radical from the series comprising alkoxy and aralkoxy, orR.sup.1 and R.sup.2 together represent an alkanedioxy radical,X represents hydrogen or chlorine andR.sup.3 represents the grouping ##STR2## in which R.sup.4 represents hydrogen or optionally substituted alkyl andR.sup.5 represents optionally substituted alkoxycarbonyl radical or an optionally substituted pyrazolyl radical; orif X represents chlorine, R.sup.3 also may represent optionally substituted radical from the series comprising alkyl, cycloalkyl, alkylamino and cycloalkylamino,which possesses fungicidal activity as well as herbicidal activity, but not against rice. Some intermediates are also new.Type: GrantFiled: March 20, 1984Date of Patent: September 17, 1985Assignee: Bayer AktiengesellschaftInventors: Theodor Pfister, Ludwig Eue, Robert R. Schmidt, Gerd Hanssler