Three Or More Carboxamide Groups Patents (Class 564/153)
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Patent number: 5965519Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative, antibiotic, antimycotic, antiviral and antineoplastic drugs, in particular in combination with a multiplicity of other emollients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of such agents through the epidermis for treatment of skin diseases and other disorders.Type: GrantFiled: July 23, 1996Date of Patent: October 12, 1999Assignee: Oregon Health Sciences UniversityInventors: Milton B. Yatvin, Michael HB Stowell
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Patent number: 5962530Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: May 29, 1998Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
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Patent number: 5955506Abstract: A group of benzamide compounds are disclosed. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The pharmaceutical compositions can arrest or slow the progressive loss of function.Type: GrantFiled: February 2, 1998Date of Patent: September 21, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: William David Flitter, William A. Garland, Allan L. Wilcox, Richard E. Paylor
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Patent number: 5948940Abstract: The invention provides a process for the production of iohexol comprising reacting 5-acetamido-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodophthalamide with a 2,3-dihydroxypropylating agent, the improvement comprising effecting that said process in the presence of a solvent comprising 2-methoxy-ethanol and, optionally, isopropanol.Type: GrantFiled: July 23, 1998Date of Patent: September 7, 1999Assignee: Nycomed Imaging ASInventors: Dick Malthe-S.o slashed.rensen, Odd Einar Ingvoldstad, Espen Myrbr.ang.ten
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Patent number: 5948778Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.Type: GrantFiled: May 19, 1998Date of Patent: September 7, 1999Assignee: Merrel Pharmaceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5939437Abstract: Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R.sup.1 is halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, substituted phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, m is 0, 1, 2, 3, or 4, provided that m is not more than 2 unless R.sup.1 is exclusively halo, x+y=0 or 1, R.sup.2 and R.sup.4 independently are II, or C.sub.1 to C.sub.3 alkyl, R.sup.3 is H or C.sub.1 to C.sub.15 hydrocarbyl, where one or more hydrogen atoms of die hydrocarbyl group may be replaced by a halogen atom, and where up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R.sup.3 does not contain a --O--O-- group, R.sup.5 is H or C.sub.1 to C.sub.Type: GrantFiled: December 20, 1996Date of Patent: August 17, 1999Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Katherine Isobel Mary Steel, David John Dunstone, Ildiko Maria Buck
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Patent number: 5910609Abstract: Compounds of general Formula I: ##STR1## are presented which have collagenase inhibition activity and are useful in the management of disease involving tissue degradation and the promotion of wound healing. Representative diseases involving include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption disease and tumor invasion.Type: GrantFiled: April 5, 1995Date of Patent: June 8, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Colin Campion, Alan Hornsby Davidson, Jonathan Philip Dickens, Michael John Crimmin
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Patent number: 5902897Abstract: The present invention relates to polyamines which are prepared by reactinga) unsaturated oligoesters having an average of 2 to 4 double bonds per molecule andb) optionally other unsaturated compounds suitable as Michael addition acceptors and having an average of 1 to 4 double bonds per molecule withc) (cyclo)aliphatic diamines having two primary amino groups andd) optionally other amino-functional compounds suitable as Michael addition donors.The present invention also relates to the use of these polyamines as a binder component in lacquers and coating compositions, particularly as reactants for blocked polyisocyanates in one-component stoving lacquers.Type: GrantFiled: July 19, 1996Date of Patent: May 11, 1999Assignee: Bayer AktiengesellschaftInventors: Christian Wamprecht, Theodor Engbert, Holger Casselmann, Josef Pedain, Jurgen Meixner
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Patent number: 5889059Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sub.Type: GrantFiled: August 5, 1996Date of Patent: March 30, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5882628Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I ##STR1## (wherein n is 0 or 1, and where n is 1 each C.sub.6 R.sub.5 moeity may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M.sub.1, two or three non-adjacent R groups in each C.sub.6 R.sub.5 moiety being iodine and at least one, and preferably two or three, R groups in each C.sub.6 R.sub.5 moiety being M or M.sub.1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C.sub.6 R.sub.5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M.sub.1 independently represents a C.sub.1-4 alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M.sub.1 moiety; with the proviso that where n is zero either at least one M.sub.Type: GrantFiled: June 6, 1995Date of Patent: March 16, 1999Assignee: Nycomed Imaging ASInventors: Torsten Almen, Sven Andersson, Lars-Goran Wistrand, Klaes Golman, Oyvind Antonsen, Rune Fossheim, Unni Nordby Wiggen, Hakan Wikstrom, Tomas Klingstedt, Ib Luenbach, Arne Berg, Harald Dugstad
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Patent number: 5871713Abstract: Biological or synthetic macromolecular polyamine compound. optionally of the dendrimer type, characterized in that it carries at least three radio-opaque iodine-containing derivatives.Type: GrantFiled: August 16, 1996Date of Patent: February 16, 1999Assignee: Guerbet S.A.Inventors: Dominique Meyer, Soizic Le Greneur
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Patent number: 5872262Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.Type: GrantFiled: December 8, 1997Date of Patent: February 16, 1999Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Hitesh K. Patel, Theodore O. Johnson, Jr., Carolyn DiIanni Carroll, Shiwei Tao
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Patent number: 5855630Abstract: Multiple amide polyether alcohol compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrocarbyl of 2 to 100 carbon atoms and substituted hydrocarbyl of 2 to 100 carbon atoms; R.sub.3 and R.sub.4 are each independently selected from the group consisting of hydrocarbyl of 1 to 100 carbon atoms, substituted hydrocarbyl of 1 to 100 carbon atoms and polyoxyalkylene alcohol of 2 to 200 carbon atoms; R.sub.5 is selected from the group consisting of alkylene of 2 to 20 carbon atoms and alkylene of 2 to 20 carbon atoms having at least one methylene group replaced by at least one oxygen atom or at least one acylated nitrogen atom; x and y are each from 1 to 50 and the weight average molecular weight of the additive compound is greater than about 600 when used as gasoline additives are found to decrease intake valve deposits.Type: GrantFiled: September 19, 1997Date of Patent: January 5, 1999Assignee: Shell Oil CompanyInventors: Jiang-Jen Lin, Sarah Louise Weaver
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Patent number: 5856572Abstract: Disclosed is a wholly aromatic polyamide prepared by reacting 1,4-naphthyl or 2,6-naphthyl containing diacids with aromatic diamines. The polymers of the invention are readily soluble in a variety of organic solvents including DMAc, NMP and pyridine, and have good thermal stability. Transparent, tough and flexible films of these polymers can be cast from the solutions thereof and these polyamides are easily processable high-performance polymer materials.Type: GrantFiled: August 14, 1996Date of Patent: January 5, 1999Assignee: Industrial Technology Research InstituteInventors: Guey-Sheng Liou, Sheng-Huei Hsiao, Jen-Chang Yang
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Patent number: 5851511Abstract: The invention relates to compounds of formula: ##STR1## in which T.sub.i, V.sub.i, T'.sub.i and V'.sub.i with i=0, 1 or 2, represent O, COND or NDCO, D being H, alkyl or (poly)hydroxyalkyl;Q.sub.i and Q'.sub.i with i=0, 1 or 2, represent alkylene or (poly)hydroxyalkylene;Ar.sub.i and Ar'.sub.i with i=1 or 2, represent ##STR2## in which R, R.sub.3, R.sub.4 are COOH and R', R'.sub.3, R'.sub.4 are CONR'.sub.1 R'.sub.2 or N(R'.sub.1)COR'.sub.2, R' and R'.sub.2 being H, alkyl or (poly)hydroxyalkyl such that R'.sub.1 and R'.sub.2 together comprise at least 4 hydroxyl groups,or R.sub.i and R'.sub.i with i=nothing, 3 or 4 represent CONR'.sub.1 R'.sub.2 or N(R'.sub.1)COR'.sub.2, R'.sub.1 and R'.sub.2 together comprising at least 6 hydroxyl groups,or else R.sub.i and R'.sub.i with i=3 or 4 represent T--Q--V--Ar, T, Q and V being as defined above for T.sub.i, Q.sub.i and V.sub.i and Ar having formula II,and A is a biocompatible radical of molecular weight less than 1200 having two valences such as to give with T.sub.Type: GrantFiled: March 21, 1997Date of Patent: December 22, 1998Assignee: Guerbet S.A.Inventors: Gael Le Lem, Dominique Meyer
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Patent number: 5849953Abstract: This invention refers to a new process for the synthesis of (S)-N,N'-bis?(2-hydroxy-1-(hydroxymethyl)ethyl!-5-?(2-hydroxy-1-oxopropyl! amino!-2,4,6-triiodo-1,3-benzendicarboxamide, of formula (III), ##STR1## starting from 5-amino-2,4,6-triiodo-1,3-benzendicarboxylic acid dichloride characterized by a new step of chromatographic purification through resins of (S)-5-??2-(acetyloxy)-1-oxopropyl!amino!-2,4,6-triiodo-1,3-benzendicarboxy lic acid dichloride, which enables the direct conversion to the compound of formula (III), without preventive isolation.Type: GrantFiled: June 12, 1997Date of Patent: December 15, 1998Assignee: Fructamine S.p.A.Inventor: Nicola Desantis
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Patent number: 5847206Abstract: 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: June 7, 1995Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutical Corp.Inventors: Andre Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5847212Abstract: Provided is a novel process for the preparation of iohexol having reduced number of isolated intermediates and significantly reduces or eliminates the use of ion-exchange resins required to desalinate the final product.Type: GrantFiled: April 21, 1997Date of Patent: December 8, 1998Assignee: Abbott LaboratoriesInventors: Xiu Chun Wang, Ashok V. Bhatia, Steven A. Chamberlin
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Patent number: 5840960Abstract: The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effective to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity.Type: GrantFiled: June 7, 1995Date of Patent: November 24, 1998Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Paul A. Marks, Richard A. Rifkind, Ronald Breslow, Branko Jursic
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Patent number: 5827890Abstract: Compounds of formula (1) are described, wherein R.sup.1 represents (a), where R.sup.3 is a hydrogen or halogen atom or a methyl, trifluoromethyl or methoxy group; R.sup.2 represents a hydrogen atom or a methyl group; and the salts, solvates, hydrates and prodrugs thereof. The compounds are potent and selective orally active inhibitors of the metalloproteinase gelatinase with a long duration of action, and in particular inhibit angiogenesis in vivo. They can therefore be expected to be of use in the prophylaxis or treatment of angiogenesis dependent disorders such as solid tumours and arthritic diseases.Type: GrantFiled: April 4, 1996Date of Patent: October 27, 1998Assignee: Celltech Therapeutics Ltd.Inventors: Nigel Robert Arnold Beeley, Thomas Andrew Millican
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Patent number: 5824821Abstract: The invention provides a process for the production of a 2,3-dihydroxypropylamino compound, said process comprising the reaction steps of:(i) obtaining an allylamino compound;(ii) epoxidizing said allylamino compound to yield an epoxypropylamino compound; and(iii) hydrolysing said epoxypropylamino compound to yield a 2,3-dihydroxypropylamino compound.This process may be used to produce simple 2,3-dihydroxypropylamino compounds such as APD or complex ones such as BAPD (an intermediate in the production of iohexol).Type: GrantFiled: February 7, 1997Date of Patent: October 20, 1998Assignee: Nycomed Imaging ASInventors: David Redick Lane, Janis Vasilevskis
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Patent number: 5817603Abstract: Substituted cyclohexene-1,2-dicarboxylic acid derivatives I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are herein defined, or the agriculturally useful salts of Ia and Ib and intermediates for their preparation, which compounds are useful as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: February 11, 1997Date of Patent: October 6, 1998Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Peter Plath, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5817861Abstract: A process for the preparation of (S)-N,N'-bis?2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino )-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.Type: GrantFiled: March 21, 1997Date of Patent: October 6, 1998Assignee: Bracco International BVInventors: Marco Villa, Antonio Nardi, Maurizio Paiocchi
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Patent number: 5817873Abstract: The present invention relates to polyiodinated compounds with a single molecular weight having a molecular concentration of iodine of greater than approximately 20% by weight, and in particular greater than approximately 30% by weight, containing at least 9 iodine atoms and having a molecular weight above 2000 and below approximately 50,000, and in particular above 2000 and below approximately 20,000, said compounds possessing either a zero overall electrical charge or at least two anionic charges, and persisting in the vascular compartment at a value equal to at least approximately 30% by weight of the injected dose in a subject five minutes after intravascular administration in the said subject.Type: GrantFiled: November 1, 1994Date of Patent: October 6, 1998Assignee: Guerbet S.A.Inventors: Dominique Meyer, Soizic le Greneur, Gael le Lem, Christian Simonot, Catherine Chambon
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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: 5811581Abstract: A process for the purification of opacifying contrastographic agents, comprising chromatographic and nanofiltration techniques combined together, the subsequent chromatographic separation of the crude product solution and a nanofiltration step, with a final deionization on ion exchange resins.Type: GrantFiled: February 20, 1997Date of Patent: September 22, 1998Assignee: Dibra S.p.A.Inventors: Rodolfo Piva, Carlo Felice Viscardi, Massimo Gagna
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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: 5801281Abstract: An improved process for preparing 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.Type: GrantFiled: November 12, 1997Date of Patent: September 1, 1998Assignee: Johnson Matthey PLCInventors: David Xu, Prasad Kapa, Oljan Repic, Thomas J. Blacklock
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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: 5786387Abstract: A compound represented by the formula (I) is disclosed. The compound of the formula (I) is useful as a fine particle drug carrier. When used as the fine particle drug carrier, the compound efficiently avoids a reticuloendothelial system and has a long circulation time in blood.Type: GrantFiled: January 25, 1996Date of Patent: July 28, 1998Assignee: Meiji Seika Kabushiki KaishaInventors: Hiroshi Watanabe, Kumi Taniguchi, Chikako Udagawa, Takashi Ando, Satoru Nakabayashi
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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: 5783735Abstract: A process for preparing polymeric amides is disclosed. The process comprises sequentially reacting a hydrocarbon polymer functionalized (e.g., via the Koch reaction) to contain acid, ester, thioacid and/or thioester groups with a heavy polyamine to form a partially derivatized product in which at least about 85% of the functional groups are converted to heavy (thio)amide groups, and then reacting the partially derivatized product with an excess of light amine to complete the derivatization by converting substantially all of the remaining functional groups to light (thio)amide groups. Products of the foregoing process are also disclosed, which products are useful as additives in fuels and in lubricants.Type: GrantFiled: May 25, 1995Date of Patent: July 21, 1998Assignee: Exxon Chemical Patents Inc.Inventors: Jacob I. Emert, Joseph V. Cusumano, David C. Dankworth, William D. Diana, William B. Eckstrom, Keith R. Gorda, Antonio Gutierrez, Jon E. Stanat, Warren A. Thaler, Stephen Zushma
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Patent number: 5780509Abstract: A compound bearing at least two 2,6-diiodophenyl-4-yl groups represented by formula (IV), particularly a polymer composed of two to eight iodinated tyrosine molecules condensed with each other.Type: GrantFiled: January 29, 1997Date of Patent: July 14, 1998Assignee: Muromachi Kagaku Kogyo Kaisha, Ltd.Inventors: Yoshiki Sugihara, Hiroshi Shionoya, Kiyomi Yamatsu
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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: 5773474Abstract: The invention provides a class of compounds and compositions thereof having the structure: ##STR1## wherein A is: ##STR2## The invention also concerns a method of selectively inducing terminal differentiation of neoplastic cells thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable conditions with an amount of the compound to selectively induce terminal differentiation. It also provides a method of treating a patient having a tumor characterized by proliferatoin of neoplastic cells comprising administration of an amount of the compound effective to inhibit proliferation and suppress oncogenicity of neoplastic cells.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: The Trustees of Columbia University in the City of New York and Sloan-Kettering Institute for Cancer ResearchInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind
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Patent number: 5770625Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is hydrogen or a branched or unbranched, substituted or unsubstituted aminoalkyl having from two to twenty atoms in the chain, R.sub.2 is hydrogen, methyl, or a branched or unbranched, substituted or unsubstituted alkyl having from two to twenty atoms in the chain; when R.sub.2 is methyl, R.sub.3 is either hydrogen or a substituted or unsubstituted aryl; and R.sub.4 is methyl, a branched or unbranched, substituted or unsubstituted alkyl, alkenyl, alkynyl, alkenynyl, or cycloalkyl having from two to twenty atoms in the chain, or a substituted or unsubstituted aryl group.The invention also concerns a method of preparing the compound from the venom, venom sacs or venom glands of the wasp Philanthus triangulun F. Additionally, the invention provides a method of chemically synthesizing the compound.Type: GrantFiled: July 14, 1994Date of Patent: June 23, 1998Assignee: The Trustees of Columbia University in the City of New YorkInventors: Koji Nakanishi, Amira T. Eldefrawi, Mohyee E. Eldefrawi, Peter N. R. Usherwood
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Patent number: 5763663Abstract: A process for the preparation of compounds of general formula (I) ##STR1## characterized in that the corresponding derivatives of general formula (II) ##STR2## are reacted with the compounds of general formula (III) ##STR3## wherein Z is halogen atom or a reactive residue of a sulfonic acid or a --N.sup.+ (R.sub.9).sub.3 cation wherein R.sub.9 is a (C.sub.1 -C.sub.6) alkyl group andR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 R.sub.6 R.sub.7 and R.sub.8 are as herein defined.Type: GrantFiled: March 24, 1997Date of Patent: June 9, 1998Assignee: Dibra S.p.A.Inventors: Lucio Pier Anelli, Marino Brocchetta, Ornella Gazzotti, Fulvio Uggeri
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Patent number: 5762910Abstract: Novel complexes of paramagnetic ions and compounds bearing long acyl chains have been synthesized as magnetic resonance imaging contrast agents. These novel liposoluble contrast agents may be administered alone, or with lipids, suspending agents or other additives. The lipids may be in the form of liposomes, micelles or lipid emulsions. The contrast agents of the invention have particular use in magnetic resonance imaging of the liver, blood pool and reticuloendothelial system.Type: GrantFiled: December 9, 1996Date of Patent: June 9, 1998Assignee: ImaRx Pharmaceutical Corp.Inventors: Evan C. Unger, DeKang Shen
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Patent number: 5760246Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.Type: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 5756548Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.Type: GrantFiled: March 6, 1997Date of Patent: May 26, 1998Assignee: Centaur Pharmaceuticals, Inc.Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
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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: 5750781Abstract: A process for preparing an aqueous solution of an ionic copolymer having a copolymer concentration of 20 % by weight or less and a viscosity of 20 ps or more at 25.degree. C. which comprises conducting copolymerization of an acrylamide compound(B) with a diallylamine compound(A) by continuously adding an aqueous solution of (B) having a concentration of 30% by weight or less to an aqueous solution of the diallylamine compound(A) having a concentration of 5% by weight or more and less than 10% by weight, and this process exhibit high conversion of diallylamine compounds, of which reactivity is low, and a copolymer having a high molecular weight can be obtained.Type: GrantFiled: June 7, 1995Date of Patent: May 12, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshifumi Yoshida, Akira Tanigawa, Satoshi Yamamoto
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Patent number: 5747514Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.Type: GrantFiled: July 19, 1996Date of Patent: May 5, 1998Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
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Patent number: 5741814Abstract: Cyclooctadiene derivative of the following formula (1): ##STR1## wherein A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each independently represent COOR.sup.5 (where R.sup.5 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a phenyl group, a C.sub.7 -C.sub.12 aralkyl group or CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group), or A.sup.1 and A.sup.2, and/or A.sup.3 and A.sup.4 may be combined together to represent group(s) of: ##STR2## in which X represents an oxygen atom or NR.sup.8 {where R.sup.8 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group),R.sup.0, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group and an C.sub.1 -C.sub.10 alkyl group,the symbol ------ represents a single or double bond, and when it is a double bond, then R.sup.1 and R.sup.Type: GrantFiled: September 3, 1996Date of Patent: April 21, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuyuki Nakajima, Hisayuki Watanabe, Michiaki Adachi, Michito Tagawa, Mitsugu Futagawa, Takashi Furusato, Hiroshi Ohya, Masanori Nishioka
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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: 5728877Abstract: A process for the preparation of compounds of general formula (I) ##STR1## characterized in that the corresponding derivatives of general formula (II) ##STR2## are reacted with the compounds of general formula (III) ##STR3## wherein Z is halogen atom or a reactive residue of a sulfonic acid or a --N.sup.+ (R.sub.9).sub.3 cation wherein R.sub.9 is a (C.sub.1 -C.sub.6) alkyl group andR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 R.sub.6 R.sub.7 and R.sub.8 are as herein defined.Type: GrantFiled: July 23, 1996Date of Patent: March 17, 1998Assignee: Dibra S.p.A.Inventors: Pier Lucio Anelli, Marino Brocchetta, Ornella Gazzotti, Fulvio Uggeri
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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: 5709846Abstract: Polyiodinated derivatives of formula: ##STR1## in which A is a moiety from an aromatic or aliphatic molecule,Za, Zb, Zc and Zd is Tz-Qz-Vz wherein Tz and Vz are O, COND or NDCO, and D is H or C.sub.1 to C.sub.6 alkyl or hydroxyalkyl and Qz is C.sub.1 to C.sub.6 alkylene or hydroxyalkylene or wherein Vz has the above meanings and Qz and/or Tz do not exist,Xa, Xb, Xc and Xd, which are identical or different, have formula ##STR2## in which Ar and Ar' are tri- or tetraiodinated phenyl groups carrying one or two amide groups substituted by optionally hydroxylated alkyls and T, Q and V have one of the meanings of the Tz, Qz and Vz, or X have, formula ##STR3## in which Ap and A'p have the above formula II and the T, Q and V groups have one of the meanings of the Tz, Qz and Vz.Use of these products as contrast agents in X-ray radiology.Type: GrantFiled: May 21, 1996Date of Patent: January 20, 1998Assignee: Guerbet S.A.Inventors: Gael Le Lem, Dominique Meyer
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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: 5705692Abstract: Provided is a novel process for the preparation of iohexol having improved yields and purity, reduced number of isolated intermediates, and significantly reduced volume of ion-exchange resins required to desalinate the final product.Type: GrantFiled: September 27, 1996Date of Patent: January 6, 1998Assignee: Abbott LaboratoriesInventors: Xiu C. Wang, Steve A. Chamberlin, Ashok V. Bhatia, Gregg E. Robinson, John Hufnagel