The Chalcogen, X, Is In A -c(=x)- Group (e.g., Beta - Phthalimidopropionaldehyde, Etc.) Patents (Class 548/479)
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Patent number: 6069247Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: October 5, 1998Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 6063924Abstract: Compounds of formulaA(B).sub.x (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine, diketopyrrolopyrrole or azo series, which radical A contains x N-atoms linked with B, preferably with at least one immediately adjacent or conjugated carbonyl group.B is a group of formula ##STR1## and, if x=2, 3 or 4, can also be one, two or three hydrogen atom(s), and wherein Q is a group of formula ##STR2## These soluble chromophores can be readily converted to the corresponding pigments by heating, even in the substrate into which they can be incorporated without any difficulty in dissolved form.R.sub.1 -R.sub.9 are as defined herein.Type: GrantFiled: July 22, 1996Date of Patent: May 16, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Veronique Hall-Goulle
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6037367Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.Type: GrantFiled: September 14, 1998Date of Patent: March 14, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, James S. Frazee
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Patent number: 6017471Abstract: A light-stable colored composition which includes a colorant and a radiation transorber. The colorant, in the presence of the radiation transorber, is adapted, upon exposure of the transorber to specific, narrow bandwidth radiation, to be mutable. The radiation transorber also imparts light-stability to the colorant so that the colorant does not fade when exposed to sunlight or artificial light.Type: GrantFiled: April 23, 1997Date of Patent: January 25, 2000Assignee: Kimberly-Clark Worldwide, Inc.Inventors: John Gavin MacDonald, Ronald Sinclair Nohr
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Patent number: 6008268Abstract: A method of generating reactive species which includes exposing a photoreactor composition to radiation, in which the photoreactor composition comprises a wavelength-specific sensitizer associated with one or more reactive species-generating photoinitiators. Also described are methods of polymerizing unsaturated monomers and curing an unsaturated oligomer/monomer mixture.Type: GrantFiled: January 22, 1998Date of Patent: December 28, 1999Assignee: Kimberly-Clark Worldwide, Inc.Inventors: Ronald Sinclair Nohr, John Gavin MacDonald
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Patent number: 5965745Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.Type: GrantFiled: July 1, 1998Date of Patent: October 12, 1999Assignee: Pfizer IncInventors: Matthew F. Brown, Anthony Marfat
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Patent number: 5939583Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## in which T is a pharmaceutically-acceptable substituent group; A is CH.sub.2, CH, or N; G is CH.sub.2 or CH; and R.sup.1 is any of a variety of disclosed substituent groups. The class of compounds of the invention includes ring-containing materials in which the units A and G are joined. The compounds of the invention are mixtures of diastereomers, or individual diastereomers making up these mixtures.Type: GrantFiled: October 30, 1997Date of Patent: August 17, 1999Assignee: Bayer CorporationInventors: Harold C. E. Kluender, Susan M. Bjorge, Lisa Marie Zadjura, William Frederick Brubaker
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Patent number: 5929217Abstract: Reactive dyes of the formula I ##STR1## where a is 1 or 2,b is 0 or 1,Z.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, carbamoyl or C.sub.1 -C.sub.6 -mono- or dialkylcarbamoyl,A is methylene, carbonyl, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,X is a direct linkage or a linker,Y.sup.1 is vinyl or a radical of the formula C.sub.2 H.sub.4 Q where Q is a group which can be eliminated under alkaline conditions,W is in case 1) the radical of a chromophore which may have further reactive groups, or in case 2) the radical of a coupling component to which additionally the radical of a diazo component may be linked via an azo bridge and which may have additional reactive groups, andL.sup.1 and L.sup.2 are each linkers,their intermediates and a process for dyeing or printing substrates having hydroxyl groups or nitrogen atoms using the novel dyes are described.Type: GrantFiled: March 22, 1996Date of Patent: July 27, 1999Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Hermann Loffler, Claus Marschner
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Patent number: 5919948Abstract: A novel ligand having the Formula 1 structure has proved remarkably successful in the amination of butadiene monoepoxide, which is a potentially desirable substrate for an asymmetric synthesis providing access to each enantiomer of vinylglycinol. ##STR1## This and other ligands described are useful for chiral induction of bond forming reactions with an epoxide substrate.Type: GrantFiled: June 7, 1995Date of Patent: July 6, 1999Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Barry M. Trost, Richard C. Bunt
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Patent number: 5919949Abstract: .alpha.-Hydroxy acid esters of formula ##STR1## wherein R2 is lower-alkyl, useful as intermediates in the production of .beta.-aminoalcohols.Type: GrantFiled: March 9, 1995Date of Patent: July 6, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5917038Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: April 11, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 5883284Abstract: The present invention provides a simple and inexpensive method for producing .alpha.-hydroxy-.beta.-aminocarboxylic acids and their esters.An ester of an N-protected .alpha.-amino acid ester is converted into a .beta.-ketosulfoxide, which is then processed with an acid to give an .alpha.-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected .alpha.-acyloxy-.beta.-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce .alpha.-hydroxy-.beta.-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.Type: GrantFiled: June 17, 1998Date of Patent: March 16, 1999Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Yutaka Honda, Kunisuke Izawa
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Patent number: 5861427Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group 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 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: January 19, 1999Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, David Ross Brittelli, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
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Patent number: 5854277Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group 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 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: December 29, 1998Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
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Patent number: 5852007Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: February 6, 1997Date of Patent: December 22, 1998Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 5786132Abstract: One embodiment of the present invention is a method and composition comprising a novel pre-dye molecule that is colorless and stable to ordinary light. The pre-dye molecule is capable of forming a color when exposed to certain wavelengths of electromagnetic radiation. A second embodiment of the present invention is a method of converting a conventional leuco dye to a colored composition by exposing the leuco dye admixed with a radiation transorber to certain wavelengths of electromagnetic radiation.Type: GrantFiled: May 29, 1996Date of Patent: July 28, 1998Assignee: Kimberly-Clark CorporationInventors: Ronald Sinclair Nohr, John Gavin MacDonald
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Patent number: 5728845Abstract: Novel nitriles are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimethoxyphenyl)propionitrile.Type: GrantFiled: August 29, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5728844Abstract: Novel amides are inhibitors of TNF.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-phthalimido-3-(3-cyclopentyloxy-4-methoxyphenyl)propionamide.Type: GrantFiled: December 26, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5658940Abstract: Novel succinimides and maleimides are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-3-(3",4"-dimethoxyphenyl)propionate.Type: GrantFiled: October 6, 1995Date of Patent: August 19, 1997Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5637702Abstract: Sulfur compounds of the formula ##STR1## where n is 0 or 2,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl or unsubstituted or substituted carbamoyl,A is methylene, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,X is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.8 -alkylene andY is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,and a process for their preparation are described.Type: GrantFiled: February 6, 1996Date of Patent: June 10, 1997Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Ernst Schefczik
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Patent number: 5610318Abstract: 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: GrantFiled: May 31, 1995Date of Patent: March 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
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Patent number: 5605914Abstract: Cyclic imides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-(2,6-dioxo-3-piperidinyl)-4-azaisoindoline-1,3-dione.Type: GrantFiled: June 10, 1994Date of Patent: February 25, 1997Assignee: Celgene CorporationInventor: George W. Muller
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Patent number: 5575947Abstract: 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: GrantFiled: January 19, 1989Date of Patent: November 19, 1996Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavalotti
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Patent number: 5561232Abstract: Compounds of formulaA(B).sub.x, (I),whereinx is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores am distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: October 6, 1994Date of Patent: October 1, 1996Assignee: Ciba-Geigy CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5520844Abstract: Bleaching agents constituted by at least one imidearomatic (poly)peroxyacid, having 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, an OH group, a COOH group, a COOOH group or a COOR' group wherein R' represents a C.sub.1 -C.sub.5 alkyl group, and n is an integer from 1 to 5.Type: GrantFiled: January 4, 1991Date of Patent: May 28, 1996Assignee: Ausimont S.p.A.Inventors: Carlo Venturello, Claudio Cavallotti, Fulvio Burzio
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Patent number: 5491232Abstract: Sulfur compounds of the formula ##STR1## where n is 0 or 2,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl or unsubstituted or substituted carbamoyl,A is methylene, carbonyl, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.8 -alkylene andY is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,and a process for their preparation are described.Type: GrantFiled: April 18, 1995Date of Patent: February 13, 1996Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Ernst Schefczik
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Patent number: 5487818Abstract: 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: GrantFiled: August 4, 1994Date of Patent: January 30, 1996Assignee: Ausimont S.p.A.Inventors: Claudio Cavallotti, Claudio Troglia, Roberto Garaffa
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Patent number: 5470988Abstract: Process for the preparation of purified phthalimidoalkanecarboxylic acidsThe present invention relates to a process for the preparation of purified phthalimidoalkanecarboxylic acids which are contaminated with phthalic acid, lactam and/or water, including the following measures:a) fusing the contaminated phthalimidoalkanecarboxylic acid,b) holding the melt for a period and at a temperature sufficient for the impurities to have substantially departed from the melt andc) cooling the purified product melt.Type: GrantFiled: January 13, 1994Date of Patent: November 28, 1995Assignee: Hoechst AktiengesellschaftInventor: Frank Jaekel
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Patent number: 5466825Abstract: Peroxycarboxylic acids of formula (I) are disclosed wherein the substituents are defined by the disclosure. The peroxycarboxylic acids are useful for washing, bleaching and disinfecting, and methods for using them in such processes are also disclosed. Further, a process for preparing the peroxycarboxylic acids is disclosed.Type: GrantFiled: June 18, 1993Date of Patent: November 14, 1995Assignee: Solvay Interox LimitedInventors: Graham Carr, Paul R. Harrison, Alun P. James
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Patent number: 5414012Abstract: 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: GrantFiled: February 22, 1994Date of Patent: May 9, 1995Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5310934Abstract: Process for purifying phthalimido-peroxycaproic acid (PAP) from chlorinated solvents, by dissolving it in a polar and volatile solvent selected from alcohols, ketones and aliphatic esters, and a following crystallization thereof and solvent stripping.Preferred solvents are aliphatic esters, in particular ethyl acetate.Type: GrantFiled: February 19, 1993Date of Patent: May 10, 1994Assignee: Ausimont S.p.A.Inventors: Claudio Cavallotti, Claudio Troglia, Roberto Garaffa
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Patent number: 5310751Abstract: All possible stereoisomer forms and mixtures thereof of a compound of the formula ##STR1## wherein X is halogen, Y is --0-- or --S-- and R is selected from the group consisting of optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, optionally substituted aryl and aralkyl of up to 14 carbon atoms and optionally substituted heterocyclic having pesticidal properties.Type: GrantFiled: July 1, 1992Date of Patent: May 10, 1994Assignee: Roussel UclafInventors: Didier Babin, Marc Benoit, Jacques Demassey, Jean-Pierre Demoute
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Patent number: 5302725Abstract: Aryl triflate compounds can generate a strong acid when exposed to irradiation of radiation and can be used as an acid generator in a radiologically-acid-producing agent system and a radiosensitive composition.Type: GrantFiled: October 20, 1992Date of Patent: April 12, 1994Assignee: Hitachi Chemical Co., Ltd.Inventors: Makoto Kaji, S. Peter Pappas
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Patent number: 5252745Abstract: Antimicrobial compounds of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of H, an amine protective group, and a moiety of the formula ##STR2## wherein R.sup.2, R.sup.5, and R.sup.6 are independently selected from H and an amine protective group;R.sup.3 and R.sup.4 are independently selected from H, lower alkyl, aryl, arylalkyl, CH.sub.2 OR, CH.sub.2 SR or CH(CH.sub.3)OR;R=H, propargyl lower alkyl, arylalkyl or aryl;wherein R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 can be joined to form a ring; and wherein when R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 are both H, the compound is either in free base form or in salt form.Type: GrantFiled: May 21, 1991Date of Patent: October 12, 1993Assignee: Rohm and Haas CompanyInventors: Margaret M. Bowers-Daines, Barry C. Lange
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Patent number: 5208340Abstract: Process for producing an aryl-imido-peralkanoic acid by means of the peroxidation with H.sub.2 O.sub.2 of the corresponding alkanoic (non-peroxy) acid, in the presence of a strong acid with a pKa value equal to, or lower than 3, and in the presence of a halogenated solvent, characterized in that said solvent is CH.sub.2 Cl.sub.2 or CHCl.sub.3, that the amount of alkanoic acid submitted to peroxidation is equal to or smaller than the solubility threshold of said alkanoic acid (in said solvent) and that a solution of said acid in said solvent is reacted with H.sub.2 O.sub.2 (at 10.degree.-35.degree. C.), with the molar ratio of said strong acid to said alkanoic acid being lower than 2.Type: GrantFiled: December 11, 1991Date of Patent: May 4, 1993Assignee: Ausimont S.p.A.Inventors: Claudio Cavallotti, Michele Merenda, Alessandro Zaro, Attilio Lagostina, Ugo P. Bianchi
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Patent number: 5142063Abstract: The present invention describes novel chiral rhodium-diphosphine complexes having the formula[Rh(X) (Y) (Lp)]owherein X represents a residue of the formula X--COO.sup.- in which Z signifies a group ##STR1## aryl or substituted aryl, wherein R.sup.1, R.sup.2, R.sup.3 =hydrogen, halogen, lower alkyl, aryl-lower alkyl, perfluoro-C.sub.1-20 -alkyl, aryl, substituted aryl, the group --OR.sup.7, --(CH.sub.2).sub.m --COA or AOC--(CF.sub.2).sub.n, with the proviso that at least one of R.sup.1, R.sup.2, and R.sup.3 represents --OR.sup.7, aryl or substituted aryl,R.sup.4, R.sup.5, R.sup.6 =hydrogen, halogen, lower alkyl, aryl-lower alkyl, perfluoro--C.sub.1-20 -alkyl, aryl, substituted aryl, --(CH.sub.2).sub.m --COA or AOC--(CF.sub.2).sub.n,R.sup.7 =hydrogen, lower alkyl, partially or completely halogenated lower alkyl, aryl, substituted aryl or aryl-lower alkyl,A=The residue --OR or NR'.sub.Type: GrantFiled: November 20, 1990Date of Patent: August 25, 1992Assignee: Hoffmann-La Roche, Inc.Inventors: Emil A. Broger, Yvo Crameri
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Patent number: 5118810Abstract: There is disclosed a process for preparing aldehydes from base sensitive amines. The process can be employed to obtain carboxylic acid methyl esters. In particular, thiazolidine carboxylic methyl ester can be produced which is useful as an intermediate in the preparation of bicyclic lactam compounds. These bicyclic lactam compounds are potent angiotesin converting enzyme (ACE) inhibitors useful in the treatment of hypertension, congestive heart failure, and the like.Type: GrantFiled: July 6, 1990Date of Patent: June 2, 1992Assignee: Merck & Co., Inc.Inventor: Conrad Santini
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5013777Abstract: The present invention comprises novel single-functional and mixtures of multi-functional oligomeric performance additive compounds having one or more components of Structure A ##STR1## (The definitions of R, Z1, Z2, Z3, A1, A2, A3 and y are given in the Summary Section), their uses and polymeric compounds and compositions containing them which have enhanced oxidative stabilities, enhanced ultraviolet (UV) and light stabilities and/or enhanced flame retardance. An example is the bis sulfonic acid bispotassium salt reaction product from an oligomeric caprolactone diol (TONE.RTM. 260), 2-sulfobenzoic acid anhydride and potassium carbonate, and use of this product, at levels up to about 3.0%, in a general purpose bisphenol A polycarbonate resin, to enhance the fire resistance or flame retardance of the polycarbonate resin.Type: GrantFiled: December 24, 1987Date of Patent: May 7, 1991Assignee: Atochem North America, Inc.Inventors: Ronald E. MacLeay, Jose Sanchez, Daryl L. Stein
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Patent number: 4945168Abstract: Aryl-(1-phthalimido)-alkyl ketones of the general formula ##STR1## are prepared by reacting a suitable aromatic compound with ##STR2## at least one hydrogen atom on the aromatic nucleus in an inert solvent and in the presence of iron-(III)-chloride with an N-phthaloyl-2-amino carboxylic acid chloride of the general formula ##STR3## They can be converted into corresponding 2-phenethanolamines or 2-phenethylamines by reduction of the keto group.Type: GrantFiled: August 22, 1988Date of Patent: July 31, 1990Assignee: Degussa AktiengesellschaftInventors: Franz Effenberger, Dieter Steegmuller
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Patent number: 4929755Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and H.sub.2 O or an organic hydroxyl compound to produce an N-acyl-.alpha.-amino acid or ester, respectively, the improvement comprising using as the .alpha.-enamide reactant, an .alpha.-enamide which has a chiral center that is essentially all L or D, thereby producing a reaction mixture containing diastereomeric N-acyl-.alpha.-amino acids or esters having two chiral centers, said mixture having essentially no enantiomeric pairs.Type: GrantFiled: December 19, 1986Date of Patent: May 29, 1990Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
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Patent number: 4920231Abstract: A process for the preparation of trifluoromethylvinyl compounds in all their possible streoisomeric forms and mixtures thereof comprising reacting a salt of trifluoroacetic acid with a halovinyl compound in the presence of a cuprous salt to obtain the same stereo-specific compound and all possible stereo-isomeric forms and mixtures thereof of 1R, trans compounds of the formula ##STR1## wherein R is an alcohol residue used in pyrethrinoid series, or an alcohol residue capable of blocking the acid function, and Z is aryl or haloaryl and the double bond has Z geometry having pesticide activity.Type: GrantFiled: March 30, 1989Date of Patent: April 24, 1990Assignee: Roussel UclafInventors: Werner Bonin, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4904795Abstract: Novel halogen-substituted phthalimides are provided which are the reaction product of a halogenated phthalic anhydride with an alkoxylated amine or the reaction product of a halogenated phthalic anhydride with a siloxy amine. The halogen-substituted phthalimides are useful in increasing the flame retardancy of thermoplastic and thermosetting resins, and are also effective as processing aids in improving the flowability and moldability of thermoplastic resins during melt processing.Type: GrantFiled: March 25, 1988Date of Patent: February 27, 1990Assignee: Pennwalt CorporationInventors: Joseph M. Bohen, Gerald H. Reifenberg, Daryl L. Stein
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Patent number: 4883806Abstract: Novel isomers and mixtures thereof of cyclopropane carboxylic acid derivatives with a 3-unsaturated side chain of the formula ##STR1## wherein A' is selected from the group consisting of (1) alkyl of 1 to 18 carbon atoms, (2) benzyl optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, alkadienyl of 4 to 8 carbon atoms, methylenedioxy or halogen, ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --C.tbd.CH and monocyclic aryl, ##STR3## wherein a is selected from the group consisting of hydrogen and methyl and R.sub.3 is an aliphatic group of 2 to 6 carbon atoms containing at least one carbon-carbon unsaturation ##STR4## wherein a and and R.sub.3 have the above definition and R.sub.1 ' and R.sub.Type: GrantFiled: September 23, 1987Date of Patent: November 28, 1989Assignee: Roussel UclafInventors: Jacques Martel, Jean Tessier, Andre Teche
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Patent number: 4881967Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.Type: GrantFiled: June 2, 1988Date of Patent: November 21, 1989Assignee: E. I. Du Pont De Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 4849449Abstract: Novel stereoisomers or mixtures of stereoisomers of compounds of the formula ##STR1## wherein R is the residue of an alcohol used in the pyrethrinoid field having remarkable pesticidal properties and being surprisingly stable.Type: GrantFiled: December 9, 1986Date of Patent: July 18, 1989Assignee: Roussel UclafInventors: Jean Tessier, Jean-Pierre DeMoute, Joseph Cadiergue
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Patent number: 4816598Abstract: The invention relates to 4-amino-butanoic acid derivatives of general formula: ##STR1## in which: M represents an alkali metal atom,R represents a protected amino group,R.sub.1 represents a labile group,R.sub.2 represents hydrogen, a branched- or straight-chain alkyl radical having from 1 to 6 carbon atoms, a lower methyloxyalkyl, a lower methylthioalkyl, a lower (lower alkyl)-aminoalkyl, a lower di-(lower alkyl)-aminoalkyl or a lower hydroxyalkyl radical or R.sub.2 represents one of the radicals of general formulae:Cy--A--, Cy--O--A'--, R--A'-- or R.sub.Type: GrantFiled: June 16, 1987Date of Patent: March 28, 1989Assignee: SanofiInventors: Marcel Descamps, Walter Verstraeten
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Patent number: 4801603Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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Patent number: 4607026Abstract: This invention relates to stereoisomeric forms and mixtures thereof of compounds of the formula ##STR1## having insecticidal, nematocidal, and acaricidal properties.Type: GrantFiled: September 29, 1982Date of Patent: August 19, 1986Assignee: Roussel UclafInventors: Jean Tessier, Andre Teche