Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimides, Etc.) Patents (Class 548/473)
  • Patent number: 5789434
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The presently claimed compounds have the generalized formula ##STR1## in which each T represents a substituent group; x is 0, 1, or 2; D represents ##STR2## .delta. is 0 or 1; U' represents O, S, or N, with the proviso that when U' is N, then .delta.=0, and when U' is O or S, then .delta.=1; R.sup.14 is any of a variety of substituent groups; and G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, R.sup.11 represents H or an alkyl group, R.sup.12 represents an alkyl group, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 6, 1995
    Date of Patent: August 4, 1998
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Heinz Herbert Benz, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Stephan Schneider, Jill Elizabeth Wood, Michael Christopher VanZandt, Donald John Wolanin, Scott M. Wilhelm
  • Patent number: 5780644
    Abstract: Branched, dendrimeric-type macromolecules composed essentially of a central nucleus and of a series of polyoxaalkyl chains that depart from said nucleus and spread into the surrounding space branching in a cascade fashion useful as carriers of drugs, contrast agents, etc.
    Type: Grant
    Filed: March 15, 1995
    Date of Patent: July 14, 1998
    Assignee: Dibra S.p.A.
    Inventors: Luigia Gozzini, Monica Muttoni, Christoph DeHaen
  • Patent number: 5719295
    Abstract: A process for making bis(ether anhydrides) employs alkylamines having low melting temperatures thus allowing for novel intermediate process steps for preparing bis(ether anhydrides). The alkylamines have alkyl groups which contain at least three carbon atoms and have boiling temperatures in the range of 48.degree. to 250.degree. C. at atmospheric pressure. As a result of using these amines, liquid alkylamines now can be employed in the imidization process step. The N-alkyl nitrophthalimides prepared from the recovered imidization product according to this invention can now be purified using liquid/liquid extraction or vacuum distillation. The alkyl nitrophthalimides prepared according to this invention provide for displacement reactions which now can be run at a high solids level. Likewise, the exchange reaction can be run at a higher solids level, and thus achieves an efficiency level which is higher than conventional processes.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: February 17, 1998
    Assignee: General Electric Company
    Inventors: Brent Dellacoletta, Roy Ray Odle, Thomas L. Guggenheim, Ronald A. Greenberg, James P. Barren, Joseph A. King, Sunita Singh Baghel, Deborah A. Haitko, David G. Hawron
  • Patent number: 5714637
    Abstract: Fluoropolyethers having functional groups, consisting of randomly distributed sequences of perfluoropolyoxyalkylene units selected from: ##STR1## and included in one of the following formulas: ##STR2##T'--O--(CF.sub.2 CF.sub.2 O).sub.p (CF.sub.2 O).sub.s --CRR'--Y(II) ##STR3## where X is F or CF.sub.3 T, T', T"=a perfluoroalkyl group containing from 1 to 3 carbon atoms and one or two atoms of Cl, Br or I;R, R'=halogen atoms;Y=a functional group;o, q=numbers, zero included, such that o+q=1-20;n=a number ranging from 1 to 15;m/n=a number ranging from 0.01 to 0.5;p=a number ranging from 1 to 20;s/p=a number ranging from 0.5 to 2; andz/o+p=a number ranging from 0.01 to 0.05.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: February 3, 1998
    Assignee: Ausimont S.R.L.
    Inventors: Giuseppe Marchionni, Piero Gavezotti, Ezio Strepparola
  • Patent number: 5709947
    Abstract: A method for the preparation of a diaminobisimide compound of the formula (I) substantially free of oligomers: ##STR1## wherein Ar.sup.1 is an optionally substituted aromatic residue which provides for good conjugation between the nitrogen containing groups; andAr is an optionally substituted aromatic residue characterized in that at least two molar proportions of an aromatic diamine of the formula (II)H.sub.2 N--Ar.sup.1 --NH.sub.2 (II)wherein Ar.sup.1 is as defined above,are heated with one molar proportion of an aromatic tetracarboxylic acid of the formula (III) or the corresponding dianhydride,(HOOC).sub.2 Ar(COOH).sub.2 (III)wherein Ar is as defined above,optionally in the presence of a polar solvent and optionally including 0.1 to 2 molar proportions of a tertiary amine.The compounds of formula (I) are useful curing agents in epoxy resin formulations.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: January 20, 1998
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Jonathan Howard Hodgkin, Mervyn Benjamin Jackson, John West Loder
  • Patent number: 5705521
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in radiation oncology applications. The compounds are capable of acting on hemoglobin in whole blood.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: The Center for Innovative Technology
    Inventor: Donald J. Abraham
  • Patent number: 5703245
    Abstract: Process for reducing the content of water in imido-alkanpercarboxylic acids comprising heating a suspension of imido-alkanpercarboxylc acid in water up to the complete solid melting and subsequent separation of the organic phase from the aqueous phase and recovery of the organic phase containing the imido-alkanpercarboxylic acid.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: December 30, 1997
    Assignee: Ausimont, S.p.A.
    Inventors: Claudio Cavallotti, Gilberto Nucida, Claudio Troglia
  • Patent number: 5703242
    Abstract: Purification process of imido-alkancaboxylic acids from contaminants represented by acid-carboxylic, lactam or aminoacids and water comprising:A) Preparation of the imido-alkancarboxylic acid precursor by reaction of an anhydride a1) or the corresponding acids, with an aminoacid b1) with water; or a1) with a lactam b2) and water; at temperatures comprised between 100.degree. and 250.degree. C., under pressure of an inert gas from 1 to 30 bar, for reaction times from 2 to 20 hours; wherein the ratio by moles between a1/(b1 or b2)/water is comprised between 1/1.05-1.1/0.5-2.5; optional addition of water such that it is at least, of 2 moles for mole of a1);B) discharge of the precursor obtained in phase A) in a solvent immiscible with water;C) separation of the aqueous phases from the organic phase;D) recovery of the organic phase for the successive peroxidation reaction.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: December 30, 1997
    Assignee: Ausimont, S.p.A.
    Inventors: Claudio Cavallotti, Gilberto Nucida, Claudio Troglia
  • Patent number: 5693797
    Abstract: A process for the preparation of brominated phthalimides that involves mixing tetrabromophthalic anhydride, an organic acid, and an organic dispersing agent in water at approximately 110.degree. C. under 1 bar pressure is disclosed. An amine is added and the reaction mixture is stirred for six hours under approximately 5 bar pressure and heated at least to 120.degree. C. The reactant mass is washed in water and then methanol. The process decreases production time, increases whiteness and purity, and decreases yellowness and particle size of the resulting product.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: December 2, 1997
    Assignee: Unitex Chemical Corporation
    Inventor: James F. Day
  • Patent number: 5677330
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in a wide variety of treatments including hypoxia, hypothermia, ischemia, stroke, ARDS, COPD, surgical blood loss, acute nonvolemic hemodilutions, wounds, diabetic ulcers, chronic leg ulcers, pressure sores, tissue transplants, and sepsis. The compounds are capable of acting on hemoglobin in whole blood.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignees: The Center for Innovative Technology, Allos Therapeutics, Inc.
    Inventors: Donald J. Abraham, Michael Gerber
  • Patent number: 5672750
    Abstract: The present invention is directed to a process for preparing an aromatic amide. More specifically, the process involves reacting carbon monoxide, an amine and an aromatic chloride in the presence of an iodide or bromide salt, a catalyst, and a base.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: September 30, 1997
    Assignee: Eastman Chemical Company
    Inventor: Robert James Perry
  • Patent number: 5663336
    Abstract: A process for the synthesis of compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Uwe Trinks, Peter Traxler
  • Patent number: 5648375
    Abstract: Allosteric hemoglobin modifier compound activity on p50 is potentiated by using the compound in combination with a hydrophobic compound such as an anesthetic.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 15, 1997
    Assignee: Virginia Commonwealth University
    Inventor: Donald J. Abraham
  • Patent number: 5631259
    Abstract: Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituentsCompounds of the formulae I and II ##STR1## in which the substituents A, R.sup.1, R.sup.2 and R.sup.3 and n have the meanings given, have an antiviral and antiparasitic action.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard J ahne, Irvin Winkler, Matthias Helsberg, Heinz H anel
  • Patent number: 5610318
    Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 11, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
  • Patent number: 5605923
    Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: February 25, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 5602074
    Abstract: Substituted isoindolones I ##STR1## where R.sup.1 and R.sup.2 =H, unsubstituted or substituted alkyl, alkenyl, alkynyl, cyano, C.sub.1 -C.sub.6 -alkoxycarbonyl, formyl, C.sub.1 -C.sub.6 -alkylcarbonyl, unsubstituted or substituted phenylcarbonyl, C.sub.3 -C.sub.8 -cycloalkyl, or, if R.sup.1 =H, R.sup.2 additionally=unsubstituted or substituted phenyl, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, are an unsubstituted or substituted 3- to 8-membered carbo- or heterocycle;where R.sup.3 to R.sup.6 have the meanings given in the specification. The compounds are useful as herbicides and for the desiccation/defoliation of plants.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: February 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5575947
    Abstract: Imide-aromatic (poly)peroxyacids are herein disclosed, which have the formula (I): ##STR1## wherein A represents a residue of a substituted or unsubstituted benzene or naphthalene ring; R is a hydrogen atom, a lower alkyl group, a COOH group or a COOOH group; and n is an integer from 1 to 5.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: November 19, 1996
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavalotti
  • Patent number: 5554766
    Abstract: A process for preparing a water-soluble organic oxide which comprises reacting an oil-soluble organic compound with molecular oxygen in the presence of a water-insoluble sensitizer in an organic solvent phase under irradiation of light to produce a water-soluble organic oxide, and transferring the water-soluble organic oxide to a water phase which forms a layer in contact with said organic solvent phase.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: September 10, 1996
    Assignees: Cosmo Research Institute, Cosmo Oil Co., Ltd.
    Inventor: Haruhiko Takeya
  • Patent number: 5554750
    Abstract: The invention pertains to (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: September 10, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5550256
    Abstract: Novel bleach catalysts, a method for bleaching substrates using these catalysts and detergent compositions containing the catalysts are reported. The catalysts are quaternary imine salts. Substrates such as fabrics may be bleached in an aqueous solution containing these salts and a peroxygen compound.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: August 27, 1996
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Stephen A. Madison, Janet L. Coope
  • Patent number: 5534533
    Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: July 9, 1996
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Toshiyuki Kato, Yozo Hori
  • Patent number: 5495023
    Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
    Type: Grant
    Filed: May 3, 1994
    Date of Patent: February 27, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
  • Patent number: 5491144
    Abstract: Compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: February 13, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Uwe Trinks, Peter Traxler
  • Patent number: 5487818
    Abstract: A process for separating phthalimido-peroxycaproic acid (PAP) from solutions in organic solvents, wherein the organic solvents have a solubility in water equal to or lower to 10% by weight, is provided. The process employs the following steps:(a) dispersing the solution in an aqueous medium to form a suspension;(b) bubbling an inert gas into the resulting suspension; and(c) recovering PAP from the suspension.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: January 30, 1996
    Assignee: Ausimont S.p.A.
    Inventors: Claudio Cavallotti, Claudio Troglia, Roberto Garaffa
  • Patent number: 5464875
    Abstract: An improved aminomethylation process gives weakly-basic anion exchangers in an elegant way, with by-product obtained being able to be processed into a suitable starting material without problems.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: November 7, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Klipper, Stefan Antons, Guido Steffan, Alfred Mitschker, Werner Struver, Holger Lutjens
  • Patent number: 5455353
    Abstract: A process for the production of a .beta.-aminoalcohol 2-[3(S)-amino-2(R)-hydroxy-4-phenylbutyl]-N-tert.butyl-decahydro-(4aS,8aS) -isoquinoline-3(S)-carboxamide of the formula ##STR1## via the oxazolidinone corresponding to the aminoalcohol 10, as well as intermediates occurring in this process.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: October 3, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5442086
    Abstract: Disclosed are certain poly-methine compounds having the formula ##STR1## wherein each R.sup.1 is independently selected from cyano; carboxy; alkenyloxycarbonyl; an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; an unsubstituted or substituted, carbocyclic or heterocyclic aryl radical; an unsubstituted or substituted alkanoyl, cycloalkanoyl or aroyl radical; an unsubstituted or substituted carbamoyl radical; or an unsubstituted or substituted alkylsulfonyl, cycloalkylsulfonyl or arylsulfonyl radical; each R.sup.2 is independently selected from cyano or an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; each A is independently selected from an unsubstituted or substituted 1,2-phenylene or 1,2-naphthylene radical; each Z is independently selected from --0-- or --S--; and L is an organic linking group bonded by non-oxo carbon atoms to each Z atom.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: August 15, 1995
    Assignee: Eastman Chemical Company
    Inventors: James J. Krutak, Max A. Weaver, Clarence A. Coates, Jr., Samuel D. Hilbert, Terry A. Oldfield, William W. Parham, Wayne P. Pruett
  • Patent number: 5440048
    Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: August 8, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc
    Inventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
  • Patent number: 5438147
    Abstract: A persalt activator or salt thereof which is derived from an imidocarboyxlic acid or sulimidocarboxylic acid of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine or a group of the formula --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M,X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2, andL is a leaving group.
    Type: Grant
    Filed: April 30, 1992
    Date of Patent: August 1, 1995
    Assignee: Hoechst AG
    Inventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter Meller
  • Patent number: 5432191
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: July 11, 1995
    Assignee: The Center for Innovative Technology
    Inventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad, Gajanan S. Joshi, Jayashree Panikker
  • Patent number: 5419966
    Abstract: A solid support for oligonucleotide synthesis has the structure ##STR1## where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytrityl or H, and R is alkyl, aryl, arylalkyl, heteroalkyl, or heteroaryl. The dimethoxytrityl group is removed from the solid support by treatment with acid, and the oligonucleotide is built, step-by-step in a conventional synthesizer after attachment of the 3' end of the first oligonucleotide unit to the hydroxyl function connected to the R group.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: May 30, 1995
    Assignee: MicroProbe Corporation
    Inventors: Michael W. Reed, Rich B. Meyer, Jr., Charles R. Petrie, John C. Tabone
  • Patent number: 5420275
    Abstract: An assay method which comprises utilizing chemiluminescence of a pyridopyridazine compound of the formula ##STR1## wherein R.sub.1 is a hydrocarbon group or a heterocyclic group each of which may be substituted and R.sub.2 is hydroxy group, thiol group, amino group or a monosubstituted amino group, and when R.sub.2 is a monosubstituted amino group, R.sub.2 may be taken together with R.sub.1 to form the ring; R.sub.3 is hydrogen atom, a hydroxy group which may be substituted, an amino group which may be substituted, a thiol group which may be substituted, a halogen atom, a heterocyclic group, nitro group, cyano group, carboxyl group which may be esterified or amidated, azido group, sulfo group or an organic sulfonyl group, provided that when R.sub.1 is an aliphalic group, R.sub.3 is not hydrogen atom; and X is oxygen atom or sulfur atom/or a salt thereof; and a novel compound of the formula (I) wherein the symbols are as defined above with proviso that R.sub.3 is hydrogen atom, R.sub.
    Type: Grant
    Filed: November 2, 1993
    Date of Patent: May 30, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirotomo Masuya, Yoshio Aramaki
  • Patent number: 5414012
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having an indolyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 9, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5304556
    Abstract: Benzamide derivatives of the following formula (I) ##STR1## [wherein R.sup.1 : ##STR2## B, D: hydrogen atom, etc. E: pyridyl group, etc.n: integer from 0 to 2R.sup.2 : R.sup.3 R.sup.4 N-- etc.(R.sup.3,R.sup.4 : optionally substituted C.sub.6 -C.sub.14 aryl group, etc.)A; ##STR3## --CH.sub.2 --, --N.dbd.N--, --CH.dbd.N--, --N.dbd.CH--, --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --].Optical antipodes thereof or pharmaceutically acceptable salts thereof, show excellent PAF antagonism and are effective for therapy and prophylaxis of diseases caused by PAF (bronchial asthma, nephritis, shocks, cardiac infarction, cerebral hemorrhage, ulcer, DIC, autoimmune diseases, thrombosis, etc.).
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: April 19, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Akihiro Yamamoto, Shuji Morita, Yoshio Hayashi, Noboru Yamada, Toshihito Kitamura
  • Patent number: 5302740
    Abstract: Disclosed are certain poly-methine compounds having the formula ##STR1## wherein each R.sup.1 is independently selected from cyano; carboxy; alkenyloxycarbonyl; an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; an unsubstituted or substituted, carbocyclic or heterocyclic aryl radical; an unsubstituted or substituted alkanoyl, cycloalkanoyl or aroyl radical; an unsubstituted or substituted carbamoyl radical; or an unsubstituted or substituted alkylsulfonyl, cycloalkylsulfonyl or arylsulfonyl radical; each R.sup.2 is independently selected from cyano or an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; each A is independently selected from an unsubstituted or substituted 1,2-phenylene or 1,2-naphthylene radical; each Z is independently selected from --O-- or --S--; and L is an organic linking group bonded by non-oxo carbon atoms to each Z atom.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: April 12, 1994
    Assignee: Eastman Kodak Company
    Inventors: James J. Krutak, Max A. Weaver, Clarence A. Coates, Jr., Samuel D. Hilbert, Terry A. Oldfield, William W. Parham, Wayne P. Pruett
  • Patent number: 5290803
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: March 1, 1994
    Assignee: The Center of Innovative Technology
    Inventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad
  • Patent number: 5266587
    Abstract: The invention provides a new sub-class or organic peroxyacids comprising N-alkyl substituted peroxytrimellitimide of formula (I) in which R=hydrogen or linear or branched alkyl, which demonstrates an excellent combination of safe-handling and bleach performance rendering the sub-class particularly suitable for use as bleach and/or disinfectant in various bleach, bleach additive or washing compositions. Effective bleaching peroxyacids include those in which R=n propyl, iso-propyl, n butyl, sec-butyl, n pentyl and n heptyl. The invention also comprises processes for making the peroxyacids, compositions containing them and processes for washing and/or bleaching and/or disinfecting employing the invention peroxyacids or compositions containing them.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: November 30, 1993
    Assignee: Interox Chemicals Limited
    Inventors: John P. Sankey, A. Pryce James
  • Patent number: 5264586
    Abstract: Chimeric analogs of calicheamicin that include an analog of calicheamicinone linked to an ester or glycoside, (-)-calicheamicinone and its analogs are disclosed.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: November 23, 1993
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Adrian L. Smith, Chan-Kou Hwang, Emmanuel Pitsinos
  • Patent number: 5250701
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: October 5, 1993
    Assignee: Center for Innovative Technology
    Inventors: Donald J. Abraham, Ramnarayan Randad
  • Patent number: 5248785
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: May 18, 1992
    Date of Patent: September 28, 1993
    Assignees: Virginia Commonwealth University, Center for Innovative Technology
    Inventors: Donald J. Abraham, Ramnarayan Randad
  • Patent number: 5210197
    Abstract: Fungicidal substituted aminals of the formula ##STR1## in which A represents --CO--, --CS-- or --SO.sub.2 --,n represents 0 or 1,R.sup.1 represents optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl,R.sup.2 represents hydrogen or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl,R.sup.3 represents optionally substituted alkyl or may represent in the case where either n is 1 and A represents --SO.sub.2 -- or n is 1 and R.sup.4 represents cycloalkoximino or arylthio,R.sup.4 represents hydrogen, optionally substituted alkyl, alkenyl or alkynyl or bridged or fused radicals, or 1-cyanoalkoximino, --OR.sup.5, --SR.sup.5 or --NR.sup.6 R.sup.7, orR.sup.3 and R.sup.4 together complete a ring.
    Type: Grant
    Filed: October 12, 1990
    Date of Patent: May 11, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Wilhelm Brandes
  • Patent number: 5201934
    Abstract: Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur;R.sup.1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl;R.sup.2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl or naphthyl, or one of the groups stated for R.sup.1 ;R.sup.3 and R.sup.4 are nitro, cyano, halogen, substituted or unsubstituted amino, alkoxy, alkylthio, substituted or unsubstituted alkenyl, alkynyl, phenyl, phenoxy or phenylthio, or one of the groups stated for R.sup.1 ;R.sup.5 is formyl, 4,5-dihydrooxazol-2-yl or COYR.sup.6 (Y.dbd.O,S);R.sup.6 is hydrogen, cycloalkyl, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkenyl or phenyl,phthalimido, tetrahydrophthalimido, succinimido, maleimido, benzotriazolyl ora group --N.dbd.CR.sup.7 R.sup.8, whereR.sup.7 and R.sup.8 are hydrogen or alkyl, and R.sup.8 may also be cycloalkyl, phenyl, or R.sup.7 and R.sup.8 together form a 4- to 7-membered alkylene chain;and if R.sup.
    Type: Grant
    Filed: October 3, 1990
    Date of Patent: April 13, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Muenster, Gerd Steiner, Wolfgang Freund, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5137948
    Abstract: The invention relates to the preparation of halogenated imides derived from hydrazine and halogenated dicarboxylic acid anhydride and which can be used as flameproofing agents for plastics. The condensation of hydrazine and halogenated dicarboxylic acid anhydride is carried out in an aqueous medium, at a temperature ranging from 40.degree. to 225.degree. C., with a molar ratio of anhydride/hydrazine equal to between 0.5 and 3, preferably between 1 and 2.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: August 11, 1992
    Assignee: Atochem
    Inventors: Evelyne Bonnet, Andre Gagnieur, Bernard Gurtner
  • Patent number: 5132431
    Abstract: A process for the continuous preparation of imidoperoxycarboxylic acids of the formula ##STR1## in which A is C.sub.2 -C.sub.4 -alkylene, phenylene, naphthylene or a group of the formula ##STR2## and R is a group of the formula --COOH, --SO.sub.3 H or --Cl, and X is C.sub.1 -C.sub.19 -alkylene or arylene, in which a solution of imidocarboxylic acids of the formula ##STR3## in sulfuric acid or methanesulfonic acid and an aqueous solution of hydrogen peroxide are continuously metered into a static mixer, then the solution of the imidoperoxycarboxylic acid obtained in this way is treated with water and the precipitated product is isolated.
    Type: Grant
    Filed: February 1, 1991
    Date of Patent: July 21, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hermann Fuchs, Hanspeter Gethoffer, Walter Gilb
  • Patent number: 5132423
    Abstract: Reactions between a solid polar and a non-polar compound, especially nucleophilic aromatic substitution reactions between an alkali metal salt of a hydroxyaromatic compound or thio analog thereof and an activated halo- or nitro-substituted aromatic compound, are conducted in a non-polar organic solvent such as toluene or xylene, in the presence of a hexaalkylguanidinium or .alpha.,.omega.-bis(pentaalkylguanidinium)alkane salt, or a corresponding heterocyclic salt, as a phase transfer catalyst. The method is particularly useful for the preparation of bisimides from bisphenol A or 4,4'-biphenol salts and 4-nitro- or 4-halophthalimides.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: July 21, 1992
    Assignee: General Electric Company
    Inventors: Daniel J. Brunelle, Deborah A. Haitko, James P. Barren, Sunita Singh
  • Patent number: 5112989
    Abstract: A process for producing an unsaturated dicarboxylic acid imide compound of formula (I): ##STR1## wherein D represents a divalent organic group having at least one carbon/carbon double bond; R.sup.1 represents an n-valent organic group having at least one carbon atom; and n is an integer of 1 or above, which comprises reacting an unsaturated amide acid compound of formula (II): ##STR2## wherein D, R.sup.1, and n are as defined above, with an orthoester of formula (III): ##STR3## wherein R.sup.2 and R.sup.3, which may be the same or different, each represents a monovalent organic group having at least one carbon atom, to form an unsaturated dicarboxylic acid amide acid ester compound of formula (IV): ##STR4## wherein D, R.sup.1, R.sup.3, and n are as defined above, and then imidating the compound of formula (IV).
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: May 12, 1992
    Assignee: Matsushita Electric Works Ltd.
    Inventors: Tatsuo Yonemoto, Eiichiro Saito, Masahiro Matsumura
  • Patent number: 5106980
    Abstract: A process for the preparation of a quinophthalone of the formula ##STR1## in which X is hydrogen, chlorine or bromine and n is an integer from 1 to 4, by condensing 8-aminoquinaldine with a phthalic anhydride, optionally monosubstituted or polysubstituted by chlorine or bromine, in the presence of molten benzoic acid acting as diluent.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: April 21, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Burkhard Ort, Guido Kuth
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue