Boron Or Silicon Containing Patents (Class 544/69)
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Patent number: 5789353Abstract: An oil-soluble dispersant obtainable by reacting a polyalkenyl succinic acylating agent and N-(2-(4-morphinyl)ethyl)-1,2-ethane diamine.Type: GrantFiled: April 21, 1997Date of Patent: August 4, 1998Assignee: Ethyl Petroleum Additives LimitedInventor: Roger Scattergood
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Patent number: 5777165Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignee: The Procter & Gamble CompanyInventors: 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
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Patent number: 5776658Abstract: 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: GrantFiled: September 29, 1995Date of Patent: July 7, 1998Assignee: AGFA-Gevaert AGInventors: Claus-Peter Niesert, Georg Pawlowski, Willi-Kurt Gries, Klaus-Juergen Przybilla
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Patent number: 5736535Abstract: 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: GrantFiled: January 19, 1995Date of Patent: April 7, 1998Assignee: Zeneca LimitedInventors: Peter Robert Bernstein, Philip Duke Edwards, Andrew Shaw, Ashokkumar Bhikkappa Shenvi, Royston Martin Thomas, Chris Allan Veale, Peter Warner, Donald John Wolanin
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Patent number: 5728693Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##Type: GrantFiled: June 25, 1996Date of Patent: March 17, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas Martin Stevenson
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Patent number: 5702952Abstract: 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: GrantFiled: February 21, 1997Date of Patent: December 30, 1997Assignee: Axis Biochemicals ASAInventors: Erling Sundrehagen, Frank Frantzen
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Patent number: 5684171Abstract: 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: GrantFiled: February 11, 1997Date of Patent: November 4, 1997Assignee: The Goodyear Tire & Rubber CompanyInventors: Lawson Gibson Wideman, Theodore Lamson Folk, Martin Paul Cohen
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Patent number: 5656759Abstract: 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: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Sony CorporationInventors: Kengo Ito, Masanobu Hida, Kaori Isaji
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Patent number: 5646172Abstract: 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: GrantFiled: September 7, 1995Date of Patent: July 8, 1997Assignee: Roussel UclafInventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
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Patent number: 5639739Abstract: 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: GrantFiled: March 24, 1995Date of Patent: June 17, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Celia Dominguez, Joseph Cacciola, John Matthew Fevig
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Patent number: 5631364Abstract: 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: GrantFiled: March 31, 1994Date of Patent: May 20, 1997Assignee: AXIS Biochemicals ASAInventors: Erling Sundrehagen, Frank Frantzen
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Patent number: 5589477Abstract: 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: GrantFiled: February 26, 1993Date of Patent: December 31, 1996Assignee: Nippon Shinyaku Company, LimitedInventors: Shoichi Chokai, Tomiyoshi Aoki, Kiyoshi Kimura
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Patent number: 5585390Abstract: 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: GrantFiled: May 9, 1995Date of Patent: December 17, 1996Assignee: Adir Et CompagnieInventors: Muriel Duflos, Sylvie Robert-Piessard, Lucien Welin, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, G erard Adam
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Patent number: 5563127Abstract: 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: GrantFiled: December 27, 1994Date of Patent: October 8, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Eugene C. Amparo, William H. Miller, Gregory J. Pacofsky, John Wityak, Patricia C. Weber, John J. V. Duncia, Joseph B. Santella, III
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Patent number: 5543516Abstract: 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: GrantFiled: May 18, 1994Date of Patent: August 6, 1996Assignee: Edison Polymer Innovation CorporationInventor: Hatsuo Ishida
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Patent number: 5538967Abstract: 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: GrantFiled: January 18, 1995Date of Patent: July 23, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventors: Jeffrey K. Long, Thomas M. Stevenson
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Patent number: 5536847Abstract: 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: GrantFiled: June 6, 1995Date of Patent: July 16, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5512451Abstract: 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: GrantFiled: March 25, 1994Date of Patent: April 30, 1996Assignee: British Technology Group LimitedInventor: Larry J. Kricka
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Patent number: 5504206Abstract: Intermediates useful in preparing the aglycon or core structure of esperamicin are disclosed, as are methods of making and using the same.Type: GrantFiled: September 26, 1994Date of Patent: April 2, 1996Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, David A. Clark
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Patent number: 5496943Abstract: 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: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5473068Abstract: 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: GrantFiled: February 17, 1994Date of Patent: December 5, 1995Assignee: Yeda Research and Development Co. Ltd. at the Weizmann Institute of ScienceInventors: Valeri Krongauz, Frida Buchhultz, Alexander Zelichenok, Shlomo Yitzchaik
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Patent number: 5466798Abstract: 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: GrantFiled: October 15, 1993Date of Patent: November 14, 1995Assignee: The Regents of the University of CaliforniaInventors: Bakthan Singaram, Gary B. Fisher, Joseph C. Fuller, John Harrison, Christian T. Goralski
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Patent number: 5399693Abstract: 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: GrantFiled: January 23, 1990Date of Patent: March 21, 1995Assignee: British Technology Group LimitedInventors: Jeffrey C. Watkins, Arwel W. Jones
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Patent number: 5385892Abstract: 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: GrantFiled: January 4, 1993Date of Patent: January 31, 1995Assignee: Ministero Dell "Universita" E Dell Ricerca Scientifica E TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5371216Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.Type: GrantFiled: January 28, 1993Date of Patent: December 6, 1994Assignee: Huls AktiengesellschaftInventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
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Patent number: 5332715Abstract: 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: GrantFiled: November 18, 1992Date of Patent: July 26, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinz-Josef Loher, Klaus Bauer, Hermann Bieringer
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Patent number: 5329046Abstract: 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: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Hoechst AktiengesellschaftInventors: Hans-Tobias Macholdt, Siegfried Schiessler, Jorg Gitzel, Erwin Dietz
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Patent number: 5324710Abstract: 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: GrantFiled: April 21, 1992Date of Patent: June 28, 1994Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
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Patent number: 5322945Abstract: 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: GrantFiled: February 19, 1993Date of Patent: June 21, 1994Assignee: Yeda Research and Development Co. Ltd.Inventors: Valeri Krongauz, Frida Buchhultz, Alexander Zelichenok, Shlomo Yitzchaik
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Patent number: 5314879Abstract: 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: GrantFiled: February 28, 1991Date of Patent: May 24, 1994Assignee: Ministero Delli `Universita` E Della Ricerca Scientifica E TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5296598Abstract: 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: GrantFiled: January 6, 1993Date of Patent: March 22, 1994Assignee: Ministero dell'Universita' e della Ricerca Scientifica e TechnologicaInventors: Roberto Cipolli, Enrico Masarati, Cristina Rossi, Roberto Oriani, Gilberto Nucida
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Patent number: 5266695Abstract: 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: GrantFiled: October 5, 1992Date of Patent: November 30, 1993Assignee: Edison Polymer Innovation CorporationInventor: Hatsuo Ishida
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Patent number: 5235051Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.Type: GrantFiled: October 16, 1991Date of Patent: August 10, 1993Assignee: Huls AktiengesellschaftInventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
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Patent number: 5221761Abstract: 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: GrantFiled: April 29, 1992Date of Patent: June 22, 1993Assignees: Instituto Guido Donegani, Enichem America, Inc.Inventors: Kwan-Yue A. Jen, Terence Moran
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Patent number: 5216103Abstract: 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: GrantFiled: October 10, 1991Date of Patent: June 1, 1993Assignee: Enichem Synthesis S.p.A.Inventors: Silvestro Costanzi, Carlo Neri, Rossella Farris
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Patent number: 5212303Abstract: 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: GrantFiled: September 28, 1992Date of Patent: May 18, 1993Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5183889Abstract: 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: GrantFiled: December 9, 1991Date of Patent: February 2, 1993Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5164400Abstract: 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: GrantFiled: July 13, 1990Date of Patent: November 17, 1992Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Takashi Manabe, Hiroyuki Okumura, Hiroshi Matsuda, Naoaki Fujii
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Patent number: 5157117Abstract: The invention relates to novel compounds of the formula: ##STR1## useful as an intermediate in the preparation of quinoline carboxylic acid medicaments.Type: GrantFiled: July 1, 1991Date of Patent: October 20, 1992Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Naomi Takagi, Hironobu Fubasami, Hiroshi Matsukubo
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Patent number: 5144035Abstract: 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: GrantFiled: April 10, 1990Date of Patent: September 1, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Toshimitsu Yamada
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Patent number: 5126063Abstract: 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: GrantFiled: September 27, 1990Date of Patent: June 30, 1992Assignee: Mobil Oil CorporationInventors: Angeline B. Cardis, Liehpao O. Farng, Abraham O. M. Okorodudu, Andrew G. Horodysky
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Patent number: 5120843Abstract: 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: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5120845Abstract: 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: GrantFiled: July 24, 1991Date of Patent: June 9, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5103000Abstract: 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: GrantFiled: September 10, 1990Date of Patent: April 7, 1992Assignee: Daiso Co., Ltd.Inventors: Shuzo Akiyama, Kenichiro Nakashima, Yasumi Shimizu, Yutaka Kamada, Junichi Kadoya
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Patent number: 5101027Abstract: .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: GrantFiled: December 17, 1990Date of Patent: March 31, 1992Assignee: Monsanto CompanyInventors: George W. J. Fleet, Ian Bruce
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Patent number: 5093336Abstract: 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: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5080708Abstract: 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: GrantFiled: April 13, 1989Date of Patent: January 14, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Freund, Thomas Kuekenhoehner, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen, Norbert Meyer, Hans Theobald
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Patent number: 5059605Abstract: 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: GrantFiled: April 10, 1990Date of Patent: October 22, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting
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Patent number: 5059696Abstract: 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: GrantFiled: March 15, 1990Date of Patent: October 22, 1991Assignee: Merck & Co., Inc.Inventors: Robert K. Anderson, Ann E. DeCamp, Alan T. Kawaguchi, Anthony O. King, Sander G. Mills, Ralph P. Volante
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Patent number: 5047526Abstract: 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: GrantFiled: June 22, 1989Date of Patent: September 10, 1991Assignee: Shin-Etsu Chemical Co., Ltd.Inventor: Keiji Yamamoto