Two Or More Oxygen In The Hetero Ring Patents (Class 514/101)
  • Patent number: 10377781
    Abstract: The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N-substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: August 13, 2019
    Inventors: Sandip Bharate, Ajay Kumar, Sudhakar Manda, Prashant Joshi, Sonali Bharate, Abubakar Wani, Sadhana Sharma, Ram Vishwakarma
  • Patent number: 8901167
    Abstract: Disclosed are compositions and methods for the inhibition of biofilm formation or reduction of existing or developing biofilms in a patient. These methods also inhibit the aggregation of bacteria that form biofilms in the airways. The methods include administering to a subject that has or is at risk of developing biofilms a compound or formulation that inhibits the formation or polymerization of actin microfilaments or depolymerizes actin microfilaments at or proximal to the site of biofilm formation. Such a compound can be administered in combination with a compound or formulation that inhibits the accumulation or activity of cells that are likely to undergo necrosis at or proximal to the site of biofilm formation (i.e., neutrophils). The methods and compositions can further include the use of anti-DNA and/or anti-mucin compounds, as well as other therapeutic compounds and compositions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: December 2, 2014
    Assignee: National Jewish Health
    Inventors: Jerry A. Nick, Travis S. Walker, G. Scott Worthen
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Publication number: 20140045797
    Abstract: The present invention concerns conjugate compounds comprising a bisphosphonate covalently bonded to a prostatic acid phosphatase inhibitor and compositions comprising such conjugates. Methods for treating and inhibiting prostate cancer bone metastases, and determining whether a conjugate is useful for such treatment are also provided. In some instances, the bisphosphonate is alendronate, and it is covalently bonded to either tartaric acid or glyceric acid.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
  • Patent number: 8598146
    Abstract: The present invention provides novel cell-based and animal-based assays for determining antagonists of PKC? and uses of the isolated antagonist compounds for modulating insulin clearance and secretion. The invention also provides novel animals and cells such as animals and cells suitable for use in the assays.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: December 3, 2013
    Assignee: Garvan Institute of Medical Research
    Inventors: Trevor John Biden, Carsten Schmitz-Peiffer
  • Patent number: 8017597
    Abstract: An object of the present invention is to elucidate an analgesic effect as one of new cPA bioactivities and thus to provide a novel analgesic agent. The present invention provides an analgesic agent which comprises a cyclic phosphatidic acid derivative that is one type of phospholipid.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: September 13, 2011
    Assignee: Ochanomizu University
    Inventors: Kimiko Murofushi, Harumi Kanashiki
  • Patent number: 7923438
    Abstract: The invention relates to the use of a compound of the formula (I) for the treatment of bacterial infections caused by mycobacteria, nocardia or corynebacteria, wherein E is phosphorus; X1, X2 and X3 are oxygen; and R1 and R2 are as defined in the specification.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: April 12, 2011
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Seibert, Luigi Toti, Joachim Wink
  • Patent number: 7652071
    Abstract: The invention relates to the use of certain cyclic acetals or ketals for improving the penetration of pharmaceutical agents into cells and organs.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: January 26, 2010
    Assignees: Alpha-Biocare GmbH, Convet GmbH & Co. KG
    Inventors: Achim Harder, Iris Heep, Stefan Herrmann, Jeffry-Lynn Grunkemeyer, Jochen Kalbe, Heinz Mehlhorn, Jürgen Schmidt, Günther Schmahl
  • Publication number: 20090291102
    Abstract: There are provided various compounds and compositions comprising polyunsaturated fatty acid monoglycerides and derivatives thereof. These compounds and compositions can be useful as cancer chemopreventive agents. They can also be useful for enhancing solubility of various active agents and enhancing their bioavailability.
    Type: Application
    Filed: August 5, 2009
    Publication date: November 26, 2009
    Inventor: Samuel FORTIN
  • Publication number: 20090130051
    Abstract: Novel flavonoid compounds having anti-oxidant activity are described. The compounds and compositions have been shown to exhibit anti-oxidant properties and are particularly useful in the treatment of ischemia and reperfusion injuries. The invention also describes a method to chemically synthesize such flavonoid compounds and test their efficacy. Such compounds and corresponding pharmaceutically acceptable derivatives and/or salts have uses in the areas of pharmaceuticals, nutraceutical, and veterinary applications.
    Type: Application
    Filed: March 10, 2006
    Publication date: May 21, 2009
    Applicants: Howard Florey Institute Of Experimental Physiology And Medicine, Neuprotect Pty Ltd
    Inventors: Bevyn Jarrott, Clive Newton May, Owen Llewellyn Woodman, Gregory James Dusting
  • Publication number: 20090028925
    Abstract: The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
    Type: Application
    Filed: May 26, 2006
    Publication date: January 29, 2009
    Inventors: Mark D. Erion, Hongjian Jiang, Serge H. Boyer
  • Publication number: 20080249067
    Abstract: The present invention describes organophosphorus compounds of general formula (I) their preparation and their uses in the activation of gamma/delta T-cells, in the screening of GcpE and LytB enzyme inhibitors and in the prophylaxis and treatment of diseases in humans and animals.
    Type: Application
    Filed: June 11, 2008
    Publication date: October 9, 2008
    Applicant: Bioagency AG
    Inventors: Hassan Jomaa, Matthias Eberl, Boran Altincicek, Martin Hintz, Oliver Wolf, Ann-Kristin Kollas, Armin Reichenberg, Jochen Wiesner
  • Publication number: 20070281882
    Abstract: Provided is a method of stimulating collagen synthesis and proteoglycan (lumican and keratocan) accumulation. Collagenase isolated keratocytes were cultured with or without insulin with or without ascorbate. Insulin stimulates the synthesis of collagen but does not affect the accumulation of lumican and keratocan. Insulin plus ascorbate, however, stimulates the synthesis of collagen and increased the accumulation of these proteoglycans. The accumulation of PGDS, a KSPG that does not interact with collagen, is not affected by ascorbate. Only the collagen made in the presence of ascorbate was pepsin resistant. EDB overrode the effects of ascorbate on pepsin resistance and proteoglycan accumulation.
    Type: Application
    Filed: June 5, 2007
    Publication date: December 6, 2007
    Inventors: Kurt Musselmann, John R. Hassell, Brad Kane, Bridgette Alexandrou
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Publication number: 20040096493
    Abstract: There is provided an emulsion composition for therapeutic administration comprising: (a) at least one mono-electron transfer agent phosphate derivative; (b) at leas tone di-electron transfer agent phosphate derivative; wherein the amount of transfer agent phosphate derivatives is no less than equimolar to the amount of di-electron transfer agent phosphate; and (c) a suitable carrier.
    Type: Application
    Filed: December 23, 2003
    Publication date: May 20, 2004
    Inventor: Simon Michael West
  • Publication number: 20040081672
    Abstract: The present invention relates to application of niacinamide, niacin, and niacin esters (nicotinic acid esters) derivatives of skin beneficial organic acids (henceforth called “derivatives”) for the synergistic treatment or prevention of topical disorders of skin such as acne, rosacea, skin wrinkles, age-spots, canker sores, striae distensae (stretch marks), pimples, and skin redness. These “derivatives” are made by a very simple in-situ method. These “derivatives” provide enhanced bioavailability of both ingredients that are combined to form such derivatives. The “derivatives” of present invention can be formulated in a wide variety of delivery systems including traditional water and oil emulsions, suspensions, colloids, solutions, or anhydrous systems.
    Type: Application
    Filed: October 25, 2002
    Publication date: April 29, 2004
    Inventor: Shyam K. Gupta
  • Publication number: 20030220301
    Abstract: Metformin salts of lipophilic acids, their pharmaceutical formulations, and methods of administrating the metformin salts for the treatment of hyperglycemia.
    Type: Application
    Filed: February 14, 2003
    Publication date: November 27, 2003
    Applicant: Sonus Pharmaceuticals, Inc.
    Inventors: Manjari Lal, Nagesh Palepu, Dean Kessler
  • Patent number: 6559137
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: May 6, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Publication number: 20030013660
    Abstract: Dioxolane analogs of the following formula: 1
    Type: Application
    Filed: October 15, 2001
    Publication date: January 16, 2003
    Applicant: Shire BioChem Inc.
    Inventors: Giorgio Attardo, Boulos Zacharie, Rabindra Rej, Jean-Francois Lavallee, Louis Vaillancourt, Real Denis, Sophie Levesque
  • Publication number: 20030008849
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: December 27, 2000
    Publication date: January 9, 2003
    Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Patent number: 6417176
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: July 9, 2002
    Assignee: Tularik, Inc.
    Inventor: Jonathan B. Houze
  • Publication number: 20020028791
    Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1
    Type: Application
    Filed: July 18, 2001
    Publication date: March 7, 2002
    Inventors: Robert F. Kaltenbach, George L. Trainor
  • Patent number: 5951748
    Abstract: Methods and compositions for inhibiting fouling in vinyl monomers are disclosed. Alkylphosphonate esters or acids thereof are added to vinyl monomers, particularly ethylene dichloride, that are undergoing processing to inhibit fouling.
    Type: Grant
    Filed: July 29, 1998
    Date of Patent: September 14, 1999
    Assignee: BetzDearborn Inc.
    Inventor: Graciela B. Arhancet
  • Patent number: 5880111
    Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
  • Patent number: 5698541
    Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: December 16, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
  • Patent number: 5489580
    Abstract: Novel compounds and use therefor in treating neoplastic and immune system disorders are disclosed. The compound of the present invention comprises a substituted lysophospholipid, which includes a C12 to C20 alkyl ether, a C12 to C20 thioether, or a substituted C3 to C6 heterocycle containing at least two ring heteroatoms, selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof; and also includes a choline group or a C4 to C7 heterocycle containing heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof.The method for treating neoplastic or immune system disorders includes administering an effective dose of a compound of the present invention in a therapeutic manner. Effective doses of these compounds result in cytotoxic effects upon various leukemic cell lines.The compounds of this invention have the advantage that these compounds possess antineoplastic and immunomodulatory characteristics.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: February 6, 1996
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Richard I. Duclos, Jr., Donna J. Fournier
  • Patent number: 5455249
    Abstract: Background of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or ##STR2## R.sup.3 and R.sup.4 are each, independently, hydrogen, Ar, or --(CR.sup.6 R.sup.7).sub.a Y(CR.sup.8 R.sup.9).sub.b Z, or R.sup.3 and R.sup.4 may be taken together to form a 5-7 membered ring;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, arylalkyl, cycloalkyl, or Ar;R.sup.6, R.sup.7, R.sup.8, and R.sup.9, are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.10, --SR.sup.10, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.10, --CO.sub.2 R.sup.10, --CONHR.sup.10, --SO.sub.2 R.sup.10, --SO.sub.3 R.sup.10, --OSO.sub.3 R.sup.10, --NR.sup.10 R.sup.11, --NHCOR.sup.10, --NHCO.sub.2 R.sup.10, --NHSO.sub.2 R.sup.10, --NHSO.sub.3 R.sup.10, or Ar;X is O or NOR.sup.12 ;Y is --O--, --CH.sub.2 --, --NR.sup.13 --, --S--, --S(O)--, --S(O).sub.2 --, or --C(O)--;R.sup.10, R.sup.11, R.sup.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: October 3, 1995
    Inventors: Jerauld S. Skotnicki, Andri L. Smith
  • Patent number: 5278152
    Abstract: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: January 11, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann, Irvin Winkler, Matthias Helsberg, Christoph Meichsner
  • Patent number: 5128331
    Abstract: The invention relates to new gem-diphosphonates derivatives substituted by phenol groups of formula (I): ##STR1## as well as the process for their preparation and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: July 7, 1992
    Assignee: Symphar S.A.
    Inventors: Lan Nguyen, Eric Niesor, Hieu Phan, Pierre Maechler, Craig Bentzen
  • Patent number: 4962207
    Abstract: The present application discloses novel potassium salts of particular tellurium and selenium compounds which are useful for the stimulation of the production of cytokines.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: October 9, 1990
    Assignee: Bar-Ilan University
    Inventors: Michael Albeck, Benjamin Sredni
  • Patent number: 4940706
    Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
  • Patent number: 4925856
    Abstract: A therapeutically effective class of low toxicity aldoxime-substituted functionalized imidazolium compounds and compositions is disclosed which is effective in the treatment of living species poisoned by organophosphorus chemicals which inactivate the enzyme acetylcholinesterase. In vivo administration of therapeutically effective amounts of these aldoxime-substituted imidazolium derivatives has been found to save mammals having inhibited acetylcholinesterase due to injection with lethal dosages of Soman.
    Type: Grant
    Filed: April 19, 1989
    Date of Patent: May 15, 1990
    Assignee: SRI International
    Inventors: Ralph N. Harris, III, Clifford D. Bedford, Dane A. Goff, Duane E. Hilmas, Robert A. Howd, Richard A. Kenley, Gary A. Koolpe, Robert O. Pick
  • Patent number: 4891363
    Abstract: Compounds of formula (I): ##STR1## (wherein: l is 2-4; A and B are oxygen or sulfur; one of R.sup.1 and R.sup.2 represents a long chain alkyl, alkylcarbamoyl or aliphatic acyl group and the other of R.sup.1 and R.sup.2 represents a group of formula (III) or (II.sub.f): ##STR2## in which E represents a single bond, a bivalent heterocyclic group or a group of formula --CO--, --COO-- or --CONR.sup.6 --, where R.sup.6 is hydrogen or an imino-protecting group; m is 0-3; n is 0-10; q is 0 or 1; R.sup.4 is optionally protected hydroxy, mercapto group or carboxy; Q is an amino or nitrogen-containing heterocyclic group;R.sub.f.sup.4 R.sub.f.sup.5 and R.sub.f.sup.6 are independently selected from the group consisting of hydrogen atoms and C.sub.1 -C.sub.6 alkyl groups, or R.sub.f.sup.4 and R.sub.f.sup.5 or R.sub.f.sup.4, R.sub.f.sup.5 and R.sub.f.sup.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: January 2, 1990
    Assignee: Sankyo Company Limited
    Inventors: Norio Nakamura, Nobuyuki Ookawa, Hiroyuki Koike, Toshio Sada, Takeshi Oshmia, Yoshio Iizuka, Hideki Miyazaki
  • Patent number: 4870065
    Abstract: The present invention relates to novel compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and stand for alkyl having 1 to 4 carbon atoms optionally substituted by one or more halogen atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl or lower alkoxy-alkyl group,R.sub.3 stands for alkyl having 1 to 6 carbon atoms or alkenyl having 2 to 6 carbon atoms,R.sub.4 and R.sub.5 are the same or different and represent hydrogen, alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, benzyl, phenyl substituted by one or more alkyl having 1 to 3 carbon atoms and/or by one or more halogen atoms, lower alkoxy-alkyl, a group of the formula --(CH.sub.2).sub.n --R.sub.6, wherein n is an integer between 0 to 3 and R.sub.
    Type: Grant
    Filed: September 26, 1985
    Date of Patent: September 26, 1989
    Assignee: Eszakmagyarorszagi Vegyimuvek
    Inventors: Karoly Balogh, Zsolt Dombay, Karoly Fodor, Gregna nee ToErzsebet, Erno Lorik, Magdolna Magyar nee Tomorkenyi, Jozsef Nagy, Karoly Pasztor, Pal Santha, Gyula Tarpai, Istvan Toth, Eszter Urszin nee Simon
  • Patent number: 4835192
    Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: May 30, 1989
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence Melvin, Jr.
  • Patent number: 4818772
    Abstract: A compound with alpha 1-blocking activity having the formula: ##STR1## wherein R.sub.1 is --H, --CH.sub.3 or --COCH.sub.3 ; R.sub.2 is --H or CH.sub.3 ; and R.sub.3 is ##STR2## wherein .SIGMA. is --H or one or more substituents selected from the group consisting of halogen, --OH and --OCH.sub.3 ; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 9, 1982
    Date of Patent: April 4, 1989
    Assignee: Societe Cortial S.A.
    Inventors: Henri Pontagnier, Christian Courtiol, Marie-Helene Creuzet, Claude Feniou, Gisele Prat
  • Patent number: 4777163
    Abstract: The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.
    Type: Grant
    Filed: July 24, 1987
    Date of Patent: October 11, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Rudi Gall
  • Patent number: 4752614
    Abstract: Certain tellurium compounds have been found to have the ability to stimulate the in vivo and in vitro production of cytokines and their receptors. These compounds may be utilized in the treatment of certain tumors, autoimmune diseases, immune diseases and infectious diseases.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: June 21, 1988
    Assignee: Bar-Ilan University
    Inventors: Michael Albeck, Benjamin Sredni
  • Patent number: 4723984
    Abstract: New 1-hydroxyethyl-azole derivatives of the general formula ##STR1## in which R represents an alkyl radical, an optionally substituted cycloalkyl radical or an optionally substituted phenyl radical,X represents a nitrogen atom or a CH group,Y represents a grouping --OCH.sub.2 --, -- CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--,Z represents a halogen atom, an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy or halogenoalkylthio radical, an optionally substituted phenyl radical, an optionally substituted phenoxy radical, an optionally substituted phenylalkyl radical or an optionally substituted phenylalkoxy radical andm is 0, 1, 2 or 3,a process for their preparation and their use as plant growth regulators and fungicides.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: February 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Graham Holmwood, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Wilhelm Brandes
  • Patent number: 4617295
    Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: October 14, 1986
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva
  • Patent number: 4614734
    Abstract: This invention relates to phosphoroamidothioate and phosphoroamidodithioate compounds, to compositions thereof which are useful as pesticides, for example, as athropodicides (that is, insecticides and acaricides), nematocides, and fungicides, and to a method of controlling pests, such as insects, acarids, nematodes, and fungi. The compounds of the invention are effective against soil insects, especially the corn rootworm, when applied by soil application techniques and are also effective when applied to agricultural plants and other plants by foliar application techniques.
    Type: Grant
    Filed: June 25, 1984
    Date of Patent: September 30, 1986
    Assignee: Rohm and Haas Company
    Inventors: Joel R. Smolanoff, J. Michael Fitzpatrick, Janet Ollinger
  • Patent number: 4567168
    Abstract: A cyanohydrin phosphate of the formula ##STR1## wherein R represents a hydrogen atom or an optionally substituted radical selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aralkenyl and aryl, or an optionally substituted heterocyclic radical,R.sup.1 and R.sup.2 are identical or different and individually represent optionally substituted radicals selected from alkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, alkylthio, alkenylthio, alkinylthio, arylthio, aralkylthio, alkylamino (monoalkylamino or dialkylamino), arylamino and aralkylamino, or together represent alkanediyl, alkanedioxy, aminoalkyloxy or alkanediamino, andX represents oxygen or sulphur,are obtained by the reaction of a phosphoric acid chloride of the general formula ##STR2## wherein X, R.sup.1 and R.sup.2 have the meaning given above, with an aldehyde of the general formulaR--CHO (III)wherein R has the meaning given above, in the presence of an approximately equimolar quantity of water-soluble cyanides.
    Type: Grant
    Filed: January 28, 1982
    Date of Patent: January 28, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Hans-Jochem Riebel, Ingeborg Hammann, Bernhard Homeyer, Wilhelm Stendel
  • Patent number: 4514392
    Abstract: Novel, aryl N-(alkylthio-phosphorothio)acyl carbamates represented by structure: ##STR1## wherein the R groups represent various alkyl substituents, and Ar represents an aryl radical with various organic substituents, which exhibit superior insecticidal and miticidal activity.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: April 30, 1985
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva