Boron Or Silicon Containing Patents (Class 544/69)
  • Patent number: 5789353
    Abstract: An oil-soluble dispersant obtainable by reacting a polyalkenyl succinic acylating agent and N-(2-(4-morphinyl)ethyl)-1,2-ethane diamine.
    Type: Grant
    Filed: April 21, 1997
    Date of Patent: August 4, 1998
    Assignee: Ethyl Petroleum Additives Limited
    Inventor: Roger Scattergood
  • Patent number: 5777165
    Abstract: N-alkyl polyhydroxy alkyl amines such as N-methyl glucamine having a Gardner Color of less than 1 are reacted with sources of fatty acyl groups such as methyl esters, anhydrides, and/or fatty acids that have greater than 98% transmittance at 460 nm in organic hydroxy solvents such as methanol to prepare N-alkyl polyhydroxy amine amides with good color. The N-alkyl polyhydroxyamines can be purified by crystallization, and/or subjected to reductive bleaching, to provide superior color. The reaction is preferably carried out at low temperature for short periods of time and with low catalyst levels to minimize formation of cyclic products. The resulting amide product can be further purified by treatment with anionic and cationic exchange resins to remove soap and amine impurities. The anionic ion exchange resin can be readily regenerated by acidifying it followed by washing with an organic solvent.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 7, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Junan Kao, Ephraim Lamar Kelly, Vicki Lynn Weber, Michael Steven Gibson, Donald Benjamin Appleby, Joseph Fredrich Sherman, Ronald Edward Pegoli, Mary Celine Schneider, Terry Franklin Formyduval, Larry Nelson Hawkins
  • Patent number: 5776658
    Abstract: Compounds of the general formula I: (SIL--X--).sub.m IN (I), in which SIL is a radical of the formula Si(R.sup.1)(R.sup.2)(R.sup.3), where R.sup.1 is an alkyl, haloalkyl or alkoxy radical of 1 to 8 carbon atoms, an alkenyl radical, an alkenyloxy or acyloxy radical of 2 to 8 carbon atoms, an aryl or aryloxy radical of 6 to 10 carbon atoms, or a dialkyl-, diaryl- or alkylaryl-methyleneaminooxy radical having C.sub.1 -C.sub.4 -alkyl or C.sub.6 -aryl groups; and R.sup.2 and R.sup.3 are identical or different radicals with the meaning of R.sup.1 or X--IN; X is a group C.sub.n H.sub.2n ; IN is the radical of a compound which is active as a photoinitiator or photosensitizer and which has at least one carbonyl group located on an aromatic nucleus; m is a number from 1 to 4; and n is a number from 2 to 12, or of the formula II: Si.sub.o O.sub.o-1 (--X--IN).sub.p R.sup.4.sub.2o+2-p (II), in which R.sup.4 is a radical with the meaning of R.sup.1, and two or more radicals R.sup.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: July 7, 1998
    Assignee: AGFA-Gevaert AG
    Inventors: Claus-Peter Niesert, Georg Pawlowski, Willi-Kurt Gries, Klaus-Juergen Przybilla
  • Patent number: 5736535
    Abstract: The present invention relates to certain novel substituted derivatives which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted derivatives, processes for preparing the substituted derivatives, pharmaceutical compositions containing such substituted derivatives and methods for their use.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: April 7, 1998
    Assignee: Zeneca Limited
    Inventors: Peter Robert Bernstein, Philip Duke Edwards, Andrew Shaw, Ashokkumar Bhikkappa Shenvi, Royston Martin Thomas, Chris Allan Veale, Peter Warner, Donald John Wolanin
  • Patent number: 5728693
    Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: March 17, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Martin Stevenson
  • Patent number: 5702952
    Abstract: The invention provides novel labelled boronic acid conjugates of formula ##STR1## (wherein V is a reporter moiety; W.sup.2 is a bond or an organic linker moiety;W.sup.1 is a *SO.sub.2 NR.sup.2, *CONR.sup.2 or *CH.sub.2 N.sup..sym. R.sup.2.sub.2 group bound at the *-marked atom to the phenyl ring;R.sup.1 is hydrogen or an electron withdrawing substituent group; andeach R.sup.2 independently is hydrogen or an optionally hydroxylated and optionally C.sub.1-6 -alkoxylated C.sub.1-6 -alkyl group) and salts thereof, e.g. for use in assays for cis-diols such as glycated blood proteins, having enhanced water-solubility and storage stability.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: December 30, 1997
    Assignee: Axis Biochemicals ASA
    Inventors: Erling Sundrehagen, Frank Frantzen
  • Patent number: 5684171
    Abstract: The present invention relates to a process for the preparation of organosilicon polysulfide compounds. The process involves reacting a mercaptoalkoxysilane with a dithiodimorpholine compound.
    Type: Grant
    Filed: February 11, 1997
    Date of Patent: November 4, 1997
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Lawson Gibson Wideman, Theodore Lamson Folk, Martin Paul Cohen
  • Patent number: 5656759
    Abstract: When the counter ion of hydrophilic cationic dyes is substituted with an organic anion including a sulfosuffinate anion such as diethylhexylsulfonate anion, an alkylbenzenesulfonate anion such as a dodecylbenzenesulfonate, an alkylsulfate anion such as a laurylsulfate anion, or a soap anion such as a laurylsulfate anion, the cationic dyes are imparted with hydrophobicity. An ink layer 3 containing the hydrophobic cationic dye is formed on a support 2 to provide a thermal transfer ink ribbon 10.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 12, 1997
    Assignee: Sony Corporation
    Inventors: Kengo Ito, Masanobu Hida, Kaori Isaji
  • Patent number: 5646172
    Abstract: Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
    Type: Grant
    Filed: September 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
  • Patent number: 5639739
    Abstract: The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs of the formula (I): ##STR1## in which the .alpha.-carbon is substituted with an optionally functionalized imidazole containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes, especially thrombin, Factor X and Factor VII.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: June 17, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Celia Dominguez, Joseph Cacciola, John Matthew Fevig
  • Patent number: 5631364
    Abstract: The invention provides novel labelled boronic acid conjugates of formula ##STR1## (wherein V is a reporter moiety; W.sup.2 is a bond or an organic linker moiety;W.sup.1 is a *SO.sub.2 NR.sup.2, *CON.sup.2 or *CH.sub.2 N.sym.R.sup.2 .sub.2 group bound at the *-marked atom to the phenyl ring;R.sup.1 is hydrogen or an electron withdrawing substituent group; andeach R.sup.2 independently is hydrogen or an optionally hydroxylated and optionally C.sub.1-6 -alkoxylated C.sub.1-6 -alkyl group) and salts thereof, e.g. for use in assays for cis-diols such as glycated blood proteins, having enhanced water-solubility and storage stability.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: May 20, 1997
    Assignee: AXIS Biochemicals ASA
    Inventors: Erling Sundrehagen, Frank Frantzen
  • Patent number: 5589477
    Abstract: The object of the present invention is to obtain new class of compounds which have improving effect on learning and memory disorders with good selectivity in central nervous system and little side effects and then to provide a good medicine for treatment of dementia.The present invention relates to the compounds represented by the following general formula or their pharmacologically acceptable salts and the drugs of improving learning or memory disorders comprising them as active ingredients. ##STR1## (wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, hydroxy, alkoxy, trifluoromethyl or halogen. A represents methyl, trifluoromethyl, or tert-butyl. Y represents O or NH.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: December 31, 1996
    Assignee: Nippon Shinyaku Company, Limited
    Inventors: Shoichi Chokai, Tomiyoshi Aoki, Kiyoshi Kimura
  • Patent number: 5585390
    Abstract: Compounds of the general formula: ##STR1## wherein m, X, Y, A, R.sub.2 and R.sub.3 are defined in the description, and medicaments containing the same.
    Type: Grant
    Filed: May 9, 1995
    Date of Patent: December 17, 1996
    Assignee: Adir Et Compagnie
    Inventors: Muriel Duflos, Sylvie Robert-Piessard, Lucien Welin, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, G erard Adam
  • Patent number: 5563127
    Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 and A are defined within.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: October 8, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Eugene C. Amparo, William H. Miller, Gregory J. Pacofsky, John Wityak, Patricia C. Weber, John J. V. Duncia, Joseph B. Santella, III
  • Patent number: 5543516
    Abstract: A method for preparing a desired benzoxazine compound comprises preparing a substantially homogeneous reaction mixture that includes a phenolic compound; a primary amine; and an aldehyde, but no solvent other than for the solvency which the reactants may have for each other. Following its preparation, the reaction mixture is maintained at a temperature, and for a period sufficient to cause the reactants to combine chemically to form the desired compound.
    Type: Grant
    Filed: May 18, 1994
    Date of Patent: August 6, 1996
    Assignee: Edison Polymer Innovation Corporation
    Inventor: Hatsuo Ishida
  • Patent number: 5538967
    Abstract: Substituted oxazines and thiazines, arthropodicidal compositions containing them and methods of controlling arthropods are provided. The oxazines and thiazines having the formula ##STR1## wherein Z is O or S; Q is phenyl or pyridyl substituted with alkenyl, alkynyl or substituted phenyl; andA, E, q, R.sup.1 and R.sup.2 are as described.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: July 23, 1996
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Jeffrey K. Long, Thomas M. Stevenson
  • Patent number: 5536847
    Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 16, 1996
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
  • Patent number: 5512451
    Abstract: In enhanced chemiluminescent (ECL) reactions of a fused aromatic diacyl cyclic hydrazide such as luminol, a peroxidase enzyme catalyst, an oxidant such as hydrogen peroxide and an enhancer, it has been found advantageous to use a combination of an organoboron enhancer such as 4-biphenylboronic acid with a non boron-containing enhancer, especially a phenolic or aromatic amine enhancer, particularly 4-iodophenol. ECL reactions are useful in diagnostic assay.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: April 30, 1996
    Assignee: British Technology Group Limited
    Inventor: Larry J. Kricka
  • Patent number: 5504206
    Abstract: Intermediates useful in preparing the aglycon or core structure of esperamicin are disclosed, as are methods of making and using the same.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: April 2, 1996
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, David A. Clark
  • Patent number: 5496943
    Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
  • Patent number: 5473068
    Abstract: A method of making a photochromic polysiloxane includes the steps of forming a photochromic spironaphthooxazine monomer including an alkene terminated side and, by addition reaction, covalently bonding the alkene carbon to [SiH] moieties of a siloxane polymer. Novel spironaphthooxazine monomers and photochromic polysiloxanes are disclosed.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: December 5, 1995
    Assignee: Yeda Research and Development Co. Ltd. at the Weizmann Institute of Science
    Inventors: Valeri Krongauz, Frida Buchhultz, Alexander Zelichenok, Shlomo Yitzchaik
  • Patent number: 5466798
    Abstract: The present invention relates to novel, powerful reducing agents, lithium aminoborohydrides which are prepared by addition of BH.sub.3 .cndot.THF to the corresponding dialkylamine at 25.degree. C. to give the intermediate amineborane complex. Subsequent deprotonation by strong base, e.g. n-BuLi, yields the aminoborohydride quantitatively. Lithium aminoborohydrides are powerful reducing agents, comparable in strength to lithium aluminum hydride. The activity is determined by the dialkylamine. Lithium pyrrolidinoborohydride has unique activity and selectivity in its reducing properties. Esters, lactones and anhydrides are reduced cleanly at 25.degree. C. to give the corresponding alcohols, while carboxylic acids are not reduced. Test reductions show that lithium pyrrolidinoborohydride is also capable of reducing a wide range of functional groups including amides, epoxides, oximes, nitriles and halides.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: November 14, 1995
    Assignee: The Regents of the University of California
    Inventors: Bakthan Singaram, Gary B. Fisher, Joseph C. Fuller, John Harrison, Christian T. Goralski
  • Patent number: 5399693
    Abstract: Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen;R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms;Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group;R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl;R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group;R.sup.2 R.sup.3 and R.sup.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: March 21, 1995
    Assignee: British Technology Group Limited
    Inventors: Jeffrey C. Watkins, Arwel W. Jones
  • Patent number: 5385892
    Abstract: The ethylamino phenyl ethers of the invention and compositions thereof are endowed with high activities as inhibitors of the growth of several species of pathogen fungi and are applied to plants or to plant parts and are effective in preventing the diseases caused by pathogen fungi, such as, e.g., those belonging to Erysiphe and Helminthosporium genera.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: January 31, 1995
    Assignee: Ministero Dell "Universita" E Dell Ricerca Scientifica E Tecnologica
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 5371216
    Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.
    Type: Grant
    Filed: January 28, 1993
    Date of Patent: December 6, 1994
    Assignee: Huls Aktiengesellschaft
    Inventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
  • Patent number: 5332715
    Abstract: Plant-protecting substituted isoxazolines, isoxazoles, isothiazolines and isothiazoles, and also processes for their preparation and their useCompounds of the formula I(R.sup.1)(R.sup.2)(R.sup.3)Si--A--Het--B--CO--Z (I)whereHet is an isoxazole-, isoxazoline-, isothiazole- or isothiazoline-3,5-diyl radical,A and B are a bond or alkylene,R.sup.1, R.sup.2 and R.sup.3 are substituted or unsubstituted, saturated or unsaturated alkyl or, if desired, phenylalkyl or phenyl,Z is OH, OR where R is saturated or unsaturated, substituted or unsubstituted alkyl or substituted or unsubstituted phenyl or benzyl or trialkylsilylmethoxy, substituted or unsubstituted phenylamino or oxazolinyl or amino, mono- or dialkylamino or -hydrazino, cycloalkylamino, NH.sub.2 NH.sub.2, pyridino, morpholino, dimethylmorpholino, a radical --ON.dbd.CR.sup.4 R.sup.5 or O--CHR.sup.7 --CO--OR.sup.6 where R.sup.4, R.sup.5 =alkyl and/or R.sup.4 CR.sup.5 is cycloalkyl and R.sup.6, R.sup.
    Type: Grant
    Filed: November 18, 1992
    Date of Patent: July 26, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Josef Loher, Klaus Bauer, Hermann Bieringer
  • Patent number: 5329046
    Abstract: The invention relates to biscationic acid amide and acid imide derivatives with an anion of formula (BR.sub.9 R.sub.10 R.sub.11 R.sub.12)--, where R.sub.9 to R.sub.12 are aliphatic, iso- or heterocyclic aromatic residues or aralkyl residues, which may be substituted by C.sub.1 -C.sub.4 -alkyl residues, C.sub.1 -C.sub.4 -alkoxy residues, aryl residues or halogen atoms (e.g. fluorine atoms), and mixtures of these compounds and mixed crystals with mixed anions and/or cations. The invention also relates to a process for preparing them. The new compounds are excellent colorless charge controllers in toners and developers for electrophotographic recording and as charge-enhancers in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Tobias Macholdt, Siegfried Schiessler, Jorg Gitzel, Erwin Dietz
  • Patent number: 5324710
    Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: June 28, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
  • Patent number: 5322945
    Abstract: A method of making a photochromic polysiloxane includes the steps of forming a photochromic spironaphthooxazine monomer including an alkene terminated side and, by addition reaction, covalently bonding the alkene carbon to [SiH] moieties of a siloxane polymer. Novel spironaphthooxazine monomers and photochromic polysiloxanes are disclosed.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: June 21, 1994
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Valeri Krongauz, Frida Buchhultz, Alexander Zelichenok, Shlomo Yitzchaik
  • Patent number: 5314879
    Abstract: The invention relates to the manufacture and use of aryl-propyl-aminic compounds having the following formula ##STR1## that have a high antifungal activity and are useful in the agricultural field as fungicides.
    Type: Grant
    Filed: February 28, 1991
    Date of Patent: May 24, 1994
    Assignee: Ministero Delli `Universita` E Della Ricerca Scientifica E Tecnologica
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 5296598
    Abstract: Derivatives of triazinylphosphonic acid having the general formula (I): ##STR1## obtained by means of the reaction of condensation of a cyanuric halide w an ester of phosphorous acid and subsequent reaction of substitution with a polyamine and an amine.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: March 22, 1994
    Assignee: Ministero dell'Universita' e della Ricerca Scientifica e Technologica
    Inventors: Roberto Cipolli, Enrico Masarati, Cristina Rossi, Roberto Oriani, Gilberto Nucida
  • Patent number: 5266695
    Abstract: The compounds are of the class of multi-functional benzoxazine compounds, useful in forming carbon-carbon composites by means of the pyrolysis of carbon fibers impregnated with such compounds.
    Type: Grant
    Filed: October 5, 1992
    Date of Patent: November 30, 1993
    Assignee: Edison Polymer Innovation Corporation
    Inventor: Hatsuo Ishida
  • Patent number: 5235051
    Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: August 10, 1993
    Assignee: Huls Aktiengesellschaft
    Inventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
  • Patent number: 5221761
    Abstract: A melt transesterification process for the production of polycarbonates, wherein at least one bis(aryl)carbonate is reacted with at least one dihydric phenol in the melted state, in the presence of a transesterification catalyst comprising at least one heterocyclic borate salt of the formula:M.sup.+ B(R).sub.n (A).sup.-.sub.4-n (I)where M.sup.+ is an alkali metal, tetra-alkylammonium, tetra-arylammonium, tetra-alkylphosphonium and tetra-arylphosphonium ion; R is H, alkyl, aryl or aralkyl; n is an integer from 0-3; and A is an aromatic or aliphatic heterocyclic ring.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: June 22, 1993
    Assignees: Instituto Guido Donegani, Enichem America, Inc.
    Inventors: Kwan-Yue A. Jen, Terence Moran
  • Patent number: 5216103
    Abstract: Polymeric stabilizers having a polysiloxanic structure contain reactive groups which can be linked to the polymeric structure to be stabilized and sterically hindered piperidinic groups. These polymeric stabilizers are particularly suitable for the stabilization of organic polymers against U.V. radiation and heat, when it is required for them not to be extracted by solvents, fats or soaps.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: June 1, 1993
    Assignee: Enichem Synthesis S.p.A.
    Inventors: Silvestro Costanzi, Carlo Neri, Rossella Farris
  • Patent number: 5212303
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents (i) ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --0--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: May 18, 1993
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 5183889
    Abstract: A benzonphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues.
    Type: Grant
    Filed: December 9, 1991
    Date of Patent: February 2, 1993
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 5164400
    Abstract: The invention relates to a compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen or lower alkyl,R.sup.3 is aryl or unsaturated, 5- or 6-membered heterocyclic group containing a sulfur atom, each of which may be substituted by one or more substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, aryloxy, trihalo(lower)alkyl, lower alkoxy and mono- or di(lower)alkylamino,R.sup.4 is hydrogen, halogen or lower alkyl,A is methylene, methine, oxa, thia, sulfinyl or sulfonyl,Y is vinylene or ethylene.Z is a group of the formula: ##STR2## wherein R.sup.5 is carboxy or protected carboxy, andR.sup.6 is hydrogen or hydroxy-protective group, andthe line is of a single or double bond, or a pharmaceutically acceptable salt thereof, useful as a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor.
    Type: Grant
    Filed: July 13, 1990
    Date of Patent: November 17, 1992
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Takashi Manabe, Hiroyuki Okumura, Hiroshi Matsuda, Naoaki Fujii
  • Patent number: 5157117
    Abstract: The invention relates to novel compounds of the formula: ##STR1## useful as an intermediate in the preparation of quinoline carboxylic acid medicaments.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: October 20, 1992
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Naomi Takagi, Hironobu Fubasami, Hiroshi Matsukubo
  • Patent number: 5144035
    Abstract: This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).
    Type: Grant
    Filed: April 10, 1990
    Date of Patent: September 1, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Hiromu Hara, Toshimitsu Yamada
  • Patent number: 5126063
    Abstract: Lubricating oil and grease compositions contain borated hydroxyalkyl esters of amine or metal salts of diorganodithiocarbamic acid, such as N,N'-di-(2-ethylhexyl) dithiocarbamic acid, and hydrocarbylene oxie, such as propylene oxide, as antioxidant, load-carrying and friction modifying additives.
    Type: Grant
    Filed: September 27, 1990
    Date of Patent: June 30, 1992
    Assignee: Mobil Oil Corporation
    Inventors: Angeline B. Cardis, Liehpao O. Farng, Abraham O. M. Okorodudu, Andrew G. Horodysky
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5120845
    Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: June 9, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
  • Patent number: 5103000
    Abstract: A packing for use in chromatography which comprises a cyclic amino-substituted silane compound having the formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are each an alkyl having 1 to 5 carbon atoms, an alkoxy having 1 to 3 carbon atoms, hydroxy or a halogen atom in which at least one of R.sup.1, R.sup.2 and R.sup.3 are an alkoxy group or a halogen atom; R.sup.4 is .omega.-piperidino, .omega.-piperazino or .omega.-morpholino group which is optionally substituted by a straight chain or branched chain lower alkyl group; n is an integer of from 2 to 10, said compound being grafted onto an inorganic carrier having hydroxyl group on its surface, and a method for separating water soluble organic compounds by chromatography using said packing.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: April 7, 1992
    Assignee: Daiso Co., Ltd.
    Inventors: Shuzo Akiyama, Kenichiro Nakashima, Yasumi Shimizu, Yutaka Kamada, Junichi Kadoya
  • Patent number: 5101027
    Abstract: .alpha.-Homojirimycin and 6-dpi-homojirimycin are each synthesized from 2 az ido-2-deoxy-3,4:6,7-di-O-isopropylidene-D-glycero-D-talo-heptono-1,5-la ctone in which the side chain acetonide is hydrolyzed to give the corresponding diol which is then protected with a silyl protecting agent to form a silyl ether. The latter compound is used as a divergent intermediate in which the piperidine ring is formed by joining the nitrogen function at C-2 to C-6 (A) with inversion of configuration at C-6 to form 6-epi-homomannojirimycin or (B) with retension of configuration at C-6 to form .alpha.-homomannojirimycin.
    Type: Grant
    Filed: December 17, 1990
    Date of Patent: March 31, 1992
    Assignee: Monsanto Company
    Inventors: George W. J. Fleet, Ian Bruce
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5080708
    Abstract: Isoxazole(isothiazole)-5-carboxamides of the formula ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, substituted or unsubstituted alkyl, alkoxy, substituted or unsubstituted cycloalkyl, a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and which may be substituted, or substituted or unsubstituted phenyl, orR.sup.2 is formyl, 4,5-dihydrooxazol-2-yl or a radical of the formula COYR.sup.5 or CONR.sup.6 R.sup.7, whereY is oxygen or sulfur,R.sup.5 ishydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, haloalkenyl, substituted or unsubstituted alkynyl,cycloalkyl,cycloalkenyl,substituted or unsubstituted phenyl,a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen,cycloalkanimino, phthalimido, succinimido, or a radical ##STR2## R.sup.3 and R.sup.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: January 14, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Freund, Thomas Kuekenhoehner, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen, Norbert Meyer, Hans Theobald
  • Patent number: 5059605
    Abstract: Fungicidal compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkenyloxy, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2, N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.
    Type: Grant
    Filed: April 10, 1990
    Date of Patent: October 22, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting
  • Patent number: 5059696
    Abstract: This invention discloses novel intermediates and novel process for their preparation where said intermediates are useful for the preparation of 5-oxygenated derivatives (T) of lovastatin and analogs thereof at the 8-acyl side chain and 6-position of the polyhydronaphthyl ring. Said derivatives of lovastatin (T) and analogs thereof are useful in treating hypercholesterolemia and are disclosed in the U.S. Pat. No. 4,963,538.
    Type: Grant
    Filed: March 15, 1990
    Date of Patent: October 22, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Anderson, Ann E. DeCamp, Alan T. Kawaguchi, Anthony O. King, Sander G. Mills, Ralph P. Volante
  • Patent number: 5047526
    Abstract: A dehydrogenative silylation process of organic compounds having active hydrogen which comprises reacting an organic compound having active hydrogen with t-butyldimethylsilane in the presence of a catalyst which is a metal of Group VIII of the periodic table or its compound. The reaction may be carried out in a solvent. When the organic compound is a strongly acidic compound, the reaction may be carried out without use of any catalyst.
    Type: Grant
    Filed: June 22, 1989
    Date of Patent: September 10, 1991
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventor: Keiji Yamamoto