Plural Carboxamide Groups Containing Or Containing Plural Carbonyls Bonded Directly To The Same Nitrogen Patents (Class 564/152)
- Two carboxamido carbonyls having benzene ring between the carbonyls and no carboxamido nitrogen between the carbonyls (Class 564/156)
- Amino nitrogen, not bonded directly to carbonyl, containing (Class 564/157)
- Hydroxy, bonded directly to carbon, or ether containing (H of -OH may be replaced by a substituted or unsubstituted ammonium ion or a Group IA or IIA light metal) (Class 564/158)
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Patent number: 5830869Abstract: The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis, periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.Type: GrantFiled: June 18, 1997Date of Patent: November 3, 1998Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
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Patent number: 5814612Abstract: The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the structure: ##STR1## wherein the configuration of the C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively.Type: GrantFiled: May 6, 1992Date of Patent: September 29, 1998Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia in the City of New YorkInventors: Jochen Buck, Ulrich Hammerling, Fadila Derguini, Koji Nakanishi
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Patent number: 5811462Abstract: Peptide analogs containing norbornene are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: May 2, 1997Date of Patent: September 22, 1998Assignee: Merck & Co., Inc.Inventors: Randall W. Hungate, Joseph P. Vacca, Byeong Moon Kim
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Patent number: 5789520Abstract: A curing agent having less odor and providing a cured resin which is excellent in appearance, mechanical properties, water resistance and chemical resistance, and a one-component type humidity-curing resin composition having excellent storage stability and providing a cured matter which is excellent in appearance and physical properties. Specifically, provided are polyaminoamide or ketimine obtained by dehydration of 2,5- and/or 2,6-bis(aminomethyl)-bicyclo?2.2.1!heptane with carboxylic acids or ketones, a curing agent for epoxy resins using the same and a one-component type humidity-curing epoxy resin or urethane prepolymer composition containing the curing agent.Type: GrantFiled: December 19, 1996Date of Patent: August 4, 1998Assignee: Mitsui Chemicals, Inc.Inventors: Minato Karasawa, Takeya Abe, Takuji Shimizu, Takeshi Iwaki
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Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5776902Abstract: The present invention makes available novel compounds useful for inhibiting kinases, phosphatases and SH2 domains, e.g., an interaction between a protein containing an SH2 domain and a phophotyrosine-containing polypeptide. In one embodiment, the present invention provides boronylphenyl analogs of phosphotyrosines which, in such forms as peptidomimetics, can be used to modulate signal transduction pathways in cells.Type: GrantFiled: May 31, 1995Date of Patent: July 7, 1998Assignee: Trustees of Tufts UniversityInventor: William W. Bachovchin
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Patent number: 5767285Abstract: This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.Type: GrantFiled: June 5, 1995Date of Patent: June 16, 1998Assignee: American Cyanamid CompanyInventors: Philip Ross Hamann, Lois Hinman, Irwin Hollander, Ryan Holcomb, William Hallett, Hwei-Ru Tsou, Martin J. Weiss
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Patent number: 5763610Abstract: A composition comprising a nitrogen-containing olefinic compound and a process for using the nitrogen-containing olefinic compound to produce a water-soluble polymer which has applications in a subterranean formation are provided. The nitrogen-containing olefinic compound can be made from an amine and an alkylating agent. The polymer produced can be used in drilling fluids, workover fluids, completion fluids, permeability corrections, water or gas coning prevention, fluid loss prevention, matrix acidizing, fracture acidizing, and combinations of any two or more thereof.Type: GrantFiled: February 21, 1997Date of Patent: June 9, 1998Assignee: Phillips Petroleum CompanyInventors: Iqbal Ahmed, Ahmad Moradi-Araghi, Odd Ivar Eriksen
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Patent number: 5763661Abstract: A method of preparing acylated .alpha.-amino carboxylic acid amides directly from amino nitriles in high yield and purity. The method involves acylating the amino nitrile with an acyl halide under Schotten-Baumann conditions, and hydrolyzing the resulting nitrile to the amide. The resulting acylated amino carboxylic acid amide precipitates and can be isolated by filtration in high purity.Type: GrantFiled: January 17, 1997Date of Patent: June 9, 1998Assignee: Hampshire Chemical Corp.Inventor: John B. Stallman
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Patent number: 5760257Abstract: A pigment-dispersible polyallylamine derivative represented by formula (I), and a pigment dispersant containing the same as an active ingredient exhibit excellent compatibility with a wide variety of resins and excellent pigment dispersibility. ##STR1## In formula (I), R.sup.1 represents a residue in which a free amino group or an amino group of a polyallylamine is bound to a polyester, a polyamide or a copolycondensate of an ester and an amide by a covalent bond (acid amide bond) or by salt (primary ammonium salt) formation through terminal carboxyl groups, and at least one of the R.sup.1 's is a residue that has the covalent bond, n is an integer of from 2 to 1,000, and X and Y, independently from each other, are hydrogen, a polymerization initiator residue or a chain transfer catalyst residue.Type: GrantFiled: October 16, 1996Date of Patent: June 2, 1998Assignee: Ajinomoto Co., Inc.Inventors: Hiroyuki Tanaka, Toshiaki Okayasu, Sae Sugiyama
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5753707Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.Type: GrantFiled: September 6, 1996Date of Patent: May 19, 1998Assignee: Kao CorporationInventors: Masahide Hoshino, Hiroshi Kusuoku, Tadashi Hase, Atsuko Otsuka, Ichiro Tokimitsu, Akira Yamamuro, Yoshiya Sugai, Koji Yoshino, Youichi Arai, Shinichi Meguro
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Patent number: 5736747Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: April 7, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5728878Abstract: N-vinyl compositions comprising 3-(N-vinylformamido)propionamides and 2-methyl-3-(N-vinylformamido)propionamides containing terminal amino, hydroxyl or a second N-vinyl group are obtained by amidation of the corresponding propionate ester with appropriate alkylamines. The invention also describes a process for preparing these compounds. The subject materials are useful as monomers in free radical polymerization as well as precursors in the preparation of unsaturated resins.Type: GrantFiled: July 2, 1996Date of Patent: March 17, 1998Assignee: Air Products and Chemicals, Inc.Inventors: Ning Chen, Walter Louis Renz, Robert Krantz Pinschmidt, Jr., William Eamon Carroll
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Patent number: 5708004Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: January 13, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Kathryn L. Reed
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Patent number: 5672765Abstract: Aromatic, ring-fluorinated compounds are prepared by reaction of corresponding chlorine compounds or bromine compounds with alkali metal fluorides using a diamide as solvent. Most of the diamides which can be used are novel compounds.Type: GrantFiled: July 14, 1995Date of Patent: September 30, 1997Assignee: Bayer AktiengesellschaftInventors: Albrecht Marhold, Marianne Lohr, Heinrich Wamhoff
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Patent number: 5663435Abstract: Reaction products of amino-alkylenecarboxylic acids with polyoxyalkylene compounds are used as paraffin dispersants for mineral oil middle distillates.Type: GrantFiled: November 29, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Gabriele Dralle-Voss, Knut Oppenlander, Klaus Barthold, Bernd Wenderoth, Wolfgang Kasel
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Patent number: 5656668Abstract: A class of pseudoceramide having the formula shown in which: R1 is a hydrocarbon group; R2-R8 are each independently H or CH.sub.3 ; R9 and R10 are each independently H or hydrocarbon group of up to 24 C atoms; X1 and X2, are independently H or OH; Y1 and Y2 are H or OH, at least one of Y1 and Y2 being OH; wherein the C atom Z, with associated R9 and R10, can be absent; and the C atoms W, with associated R7 and Y2, can be absent, is disclosed. These find use in compositions, particularly cosmetic compositions, suitable for topical application to skin, hair or nails.Type: GrantFiled: May 30, 1995Date of Patent: August 12, 1997Assignee: Quest International B.V.Inventors: Keith Robert Motion, Angela Janousek, Stephen David Watkins
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Patent number: 5654301Abstract: The present invention relates to compounds of the formula ##STR1##Type: GrantFiled: January 12, 1993Date of Patent: August 5, 1997Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5631389Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.Type: GrantFiled: April 30, 1996Date of Patent: May 20, 1997Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Robert Vermeer, Van Au, Bijan Harichian
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Patent number: 5629347Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.Type: GrantFiled: December 22, 1993Date of Patent: May 13, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
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Patent number: 5621133Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: April 15, 1997Inventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5618966Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: May 16, 1995Date of Patent: April 8, 1997Assignee: Pharm-Eco Laboratories, IncorporatedInventors: Biman Pal, Siya Ram, Bing Cai, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard Gabriel
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Patent number: 5616798Abstract: The invention relates to novel poly-iodinated compounds of general formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10, identical or different, are selected from an iodine atom, a group of formula ##STR2## provided that at least two of the R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 groups represent an iodine atom, utilizable in contrast media for radiography. The invention also relates to a process for the preparation of these compounds as well as a contrast medium containing them.Type: GrantFiled: October 25, 1993Date of Patent: April 1, 1997Assignee: Guerbet S.A.Inventors: Maryse Dugast-Zrihen, Dominique Meyer
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Patent number: 5614648Abstract: A method of producing an antioxidant containing derivatives of an organic compound, and in particular, an antioxidant glyceride derivative, comprises reacting a first compound with a second medium. By this reaction, a product is formed whereby an active component of the first compound, e.g., an antioxidant moiety, is covalently incorporated into the second medium.The second medium comprises glyceride derivatives, silicones, fluorocarbons and alkoxylates containing reactive groups such as hydroxy, amino, carboxyl, ester, or amides.Type: GrantFiled: January 10, 1995Date of Patent: March 25, 1997Inventors: George H. Greene, Robert Miller, James L. Williams, James C. Phillips, Jerry F. Stults, Jan P. E. Tellings
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Patent number: 5591884Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: January 7, 1997Assignee: Abbott LaboratoriesInventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5583248Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heteroeyelylearbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl:and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.Type: GrantFiled: April 5, 1995Date of Patent: December 10, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Martin, Gareth J. Thomas
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Patent number: 5571941Abstract: A process for purifying Iopamidol which uses a butanol as solvent is described. Iopamidol is obtained with high yields, also starting from aqueous solutions of the same and has characteristics in accordance with those required by pharmacopoeia.Type: GrantFiled: July 29, 1994Date of Patent: November 5, 1996Assignee: Zambon Group S.p.A.Inventors: Marco Villa, Maurizio Paiocchi
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Patent number: 5536853Abstract: Compounds of Formula 1 bind opioid receptors: ##STR1## wherein X and Y are each independently ##STR2##Type: GrantFiled: April 11, 1994Date of Patent: July 16, 1996Assignee: Chiron CorporationInventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber, Kevin R. Shoemaker, Dane Goff
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Patent number: 5527962Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.Type: GrantFiled: May 5, 1994Date of Patent: June 18, 1996Assignee: Alliance Pharmaceutical Corp.Inventors: Andre A. Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5523462Abstract: Cyclohexenone derivatives I ##STR1## The cyclohexenone derivatives I are suitable as herbicides and for regulating plant growth.Type: GrantFiled: April 19, 1994Date of Patent: June 4, 1996Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Thomas Zierke, Matthias Bratz, Ulf Misslitz, Norbert Meyer, Andreas Landes, Wilhelm Rademacher, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5521160Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.Type: GrantFiled: January 4, 1995Date of Patent: May 28, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans P. Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans P. Wessel
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Patent number: 5512699Abstract: Poly polyhydroxy fatty acid amide compounds and laundry, cleaning, fabric and personal care compositions comprising these compounds.Type: GrantFiled: November 21, 1994Date of Patent: April 30, 1996Assignee: The Procter & Gamble CompanyInventors: Daniel S. Connor, Yi-Chang Fu, Jeffrey J. Scheibel
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Patent number: 5504115Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: June 28, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5481005Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: November 28, 1994Date of Patent: January 2, 1996Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5476644Abstract: The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.Type: GrantFiled: April 13, 1994Date of Patent: December 19, 1995Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Thomas J. Caulfield, John L. Toner, Peng Guo, David L. Ladd
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Patent number: 5464549Abstract: The dispersants are formed by reacting (a) at least one dispersant having at least one primary or secondary amino group and/or at least one hydroxyl group, with (b) at least one polyolefinic compound substituted at each terminal position by a succinic group. Suitable substances for use as reactant (b) include compounds derived from at least one telechelic compound having up to 5000 carbon atoms and at least two terminal methylene groups by reaction with maleic anhydride or the like. The products are deemed to be effective dispersant/detergents for use in fuels and lubricants. In fuels the products are deemed to exhibit the property of inhibiting and/or reducing deposit formation such as intake valve deposits. In crankcase lubricants, the products are deemed to provide desirable viscosity index improving properties.Type: GrantFiled: December 12, 1991Date of Patent: November 7, 1995Assignee: Ethyl CorporationInventor: John F. Sieberth
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Patent number: 5463083Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: January 6, 1994Date of Patent: October 31, 1995Assignee: Cytomed, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
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Patent number: 5428116Abstract: New synthesis and analysis procedures for novel crosslinked polyamines and ampholytes. Polyamines are crosslinked with tartaric acid ester, malonic acid ester, or polycarboxylic acid esters of the citric acid cycle. The resulting crosslinked polyamine may further react with other compounds such as an .alpha.,.beta.-unsaturated or .alpha.-halo unsaturated carboxylic acids to prepare new ampholyte mixtures. The resulting novel ampholytes exhibit greater heterogeneity and complexity than presently prepared ampholytes, and can be used in analytical and preparative isoelectric focusing processes.Novel ampholyte analysis process entails analyzing chemical compounds, usually ampholytes, used in isoelectric focusing processes. The ampholyte is isoelectrically focused on an immobilized pH gradient, and then immersed in a picric acid solution to cause precipitation and visualization of amphoteric species.Type: GrantFiled: March 11, 1994Date of Patent: June 27, 1995Assignee: Board of Regents, The University of Texas SystemInventors: L. Scott Rodkey, Philip R. DeShong
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Patent number: 5416119Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: October 25, 1993Date of Patent: May 16, 1995Assignee: G. D. Searle & Co.Inventors: Barbara B. Chen, Gunnar J. Hanson, John S. Baran
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5414018Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein q is two or three; wherein r is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl containing moiety; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.12 and R.sup.13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 24, 1993Date of Patent: May 9, 1995Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson
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Patent number: 5397489Abstract: A lubricating oil soluble compound suitable for use as a dispersant additive is obtainable by reacting at elevated temperature a polyacrylate with a dispersant having at least one reactive nitrogen--containing moiety.Intermediates of the general formula IV ##STR1## where Y.sup.1 is a group derived from the reaction of the polyacrylate with the reactive nitrogen-containing moieties (i.e. primary or secondary amine) are novel.The process for preparing the lubricating oil soluble compounds can be a one step or multistep process.Lubricating oil compositions comprise a major proportion of lubricating oil and a minor proportion of the lubricating oil soluble compounds.Type: GrantFiled: October 26, 1992Date of Patent: March 14, 1995Assignee: BP Chemicals (Additives) LimitedInventor: William D. Carlisle
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Patent number: 5395958Abstract: The cyclopropene derivatives of the present invention are useful as the intermediates for producing cyclopropenone derivatives exhibiting strong inhibition activity of thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L and the like.Type: GrantFiled: September 27, 1993Date of Patent: March 7, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Eiichi Nakamura
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Patent number: 5380873Abstract: A coupling agent useful in conducting immunoassays, particularly assays for B12, is disclosed. The coupling agent has the formula ##STR1## Z and Z' can be the same or different and each is ##STR2## k, m and n are integers from 1 to 10, X is an alkylene group, a cycloalkylene group, an alkylcycloalkylene group, a bivalent aromatic group, or an aminoalkylene group, R and R' can be the same or different, and each is a substituted or unsubstituted aminoalkylene group having from 1 to 10 carbon atoms or a cycloalkylene or alkylcycloalkylene group having from 5 to 20 carbon atoms. Z and Z' are the same except that they can be the same or different when both are ##STR3## A method for purifying an aqueous intrinsic factor solution which contains R-protein is disclosed.Type: GrantFiled: December 22, 1992Date of Patent: January 10, 1995Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Christopher Welch
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Patent number: 5378729Abstract: The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 4, 1991Date of Patent: January 3, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5369108Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.Type: GrantFiled: October 4, 1991Date of Patent: November 29, 1994Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of ColumbiaInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
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Patent number: 5354742Abstract: The invention is directed to a pesticide composition comprising free flowing, essentially spherical, water-dispersible granules wherein said water-dispersible granules are from about 150 to about 850 microns in diameter; wherein said granules contain up to about 8.0% by weight moisture; wherein each individual water-dispersible granule is an aggregation of individual spherical microcapsules which contain at least one water-insoluble pesticide within a polymeric shell wall; and wherein said water-dispersible granule disintegrates upon contact with water to release said individual microcapsules.The invention also relates to dry flowable pesticidal formulations of the above water-dispersible granules, together with formulation adjuvants.The invention is further directed to a process for preparing a water-dispersible granule by spary drying an aqueous suspension comprising discrete microcapsules containing at least one water-insoluble pesticide within a polymeric shell wall suspended in an aqueous liquid.Type: GrantFiled: October 14, 1988Date of Patent: October 11, 1994Assignee: Monsanto CompanyInventors: John M. Deming, John M. Surgant, Sr.
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Patent number: 5352705Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: June 26, 1992Date of Patent: October 4, 1994Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe