Two Carboxamido Carbonyls Having Benzene Ring Between The Carbonyls And No Carboxamido Nitrogen Between The Carbonyls Patents (Class 564/156)
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Publication number: 20010037040Abstract: 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: ApplicationFiled: April 30, 2001Publication date: November 1, 2001Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
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Publication number: 20010020097Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: March 30, 1999Publication date: September 6, 2001Inventors: JAMES E. AUDIA, BEVERLY K. FOLMER, VARGHESE JOHN, LEE H. LATIMER, JEFFREY S. NISSEN, WARREN J. PORTER, EUGENE D. THORSETT, JING WU
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Patent number: 6274762Abstract: The invention provides an improved process for the preparation of a compound containing a 2,4,6-triiodinated benzene ring, said process comprising reacting a 2,4,6-unsubstituted 5-amino-benzoic acid or derivative there of with an iodine halide iodinating agent in an aqueous reaction medium, characterised in that the iodinating agent is added to an aqueous medium containing the 5-amino-benzoic acid or derivative at two different temperature ranges: (A) one or more primary portions of the agent are added at a temperature in the range 40 to 70° C. and then one or more secondary portions of the agent are added at a temperature in the range 75 to 95° C. or (B) one or more primary portions of the agent are added at a temperature in the range 75 to 95° C. and then one or more secondary portions of the agent are added at a temperature of 60 to 70° C.Type: GrantFiled: November 12, 1999Date of Patent: August 14, 2001Assignee: Nycomed Imaging ASInventors: Dick Malthe-Sorenssen, Ole Magne Homestad, Britt Sterud
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Patent number: 6252104Abstract: A naphthol derivative represented by the general formula (I), [wherein Y and Y′ indicate —(CONH)n—X or —COR; X is a phenyl group, a naphthyl group, an anthraquinonyl group, a benzimidazolonyl group or a carbazolyl group; R is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, a halogen atom, a benzyloxy group, a phenyloxy group or a phenacyloxy group; R2 is a hydrogen atom, an alkaline metal, an alkyl group having 1 to 6 carbon atoms, an acyl group having 1 to 6 carbon atoms or a phenylalkyl group; Z is a group selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a nitroso group and an amino group (Z may be substituted on any ring of the naphthalene ring); and n is an integer of 1 or 2; provided that R2 and Z do not simultaneously indicate a hydrogen atom when both R simultaneously indicate a hydroxyl group], and a process for producing the same.Type: GrantFiled: December 12, 1996Date of Patent: June 26, 2001Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Shigeru Ito, Kenji Minami, Masaya Kitayama
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Patent number: 6187812Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the index have the following meanings: X is oxygen or sulfur; R is hydrogen or alkyl; R1 is hydrogen or alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy; m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2; R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino; R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino; unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclyType: GrantFiled: February 3, 2000Date of Patent: February 13, 2001Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6153771Abstract: 5-Substituted isophthalic acid bis(allylamides) and bis(allylamide epoxides) in which said 5-substituent is --NO.sub.2, --NH.sub.2, --NHR.sup.1 or --NR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are independently optionally substituted alkyl, alkenyl, acyl, aryl, aralkyl or alkaryl groups.Type: GrantFiled: September 30, 1998Date of Patent: November 28, 2000Assignee: Nycomed Imaging ASInventors: David Redick Lane, Janis Vasilevskis
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Patent number: 6136943Abstract: A multi-branched compound which can give a compound having a relatively high molecular weight but a low viscosity and having excellent coating performances, and can give a solvent-less composition having sufficient coating performances and having a low viscosity sufficient for forming a coating, and which can serve to decrease the amount of a low-molecular-weight compound having performance problems and the multi-branched compound is obtained by reacting a core compound obtained by subjecting (a) a polyamino compound having a molecule containing a primary or secondary amino group and (b-1) an active-hydrogen-containing (meth)acrylic compound in Michael addition reaction with (c) a vinyl-group-containing compound having a functional group reactive with the active hydrogen.Type: GrantFiled: August 31, 1998Date of Patent: October 24, 2000Assignee: Toyo Ink Mfg. Co., Ltd.Inventors: Miki Kawashima, Minoru Nakamura, Hiroaki Tanaka
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Patent number: 6137006Abstract: The invention provides a process by which ultra low salt content triiodinated aromatic compounds may be isolated from a highly acidic hot triiodination raction medium in a straightforward fashion. The process involves increasing the pH to above 5 with sodium hydroxide, addition of sodium bisulphite and/or sodium dithionite, addition of seed crystals, cooling slowly, and washing the collected precipitate with water.Type: GrantFiled: November 9, 1999Date of Patent: October 24, 2000Assignee: Nycomed Imaging ASInventors: William Thieking, Einar Odd Ingvoldstad, Trygve Gulbrandsen
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Patent number: 6103925Abstract: The present invention relates to dimethyl-substituted cyclohexanediene derivatives, to a process for their preparation, to their use as pharmaceuticals and to corresponding pharmaceuticals.Type: GrantFiled: September 22, 1998Date of Patent: August 15, 2000Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Frank Mauler
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Patent number: 6048968Abstract: Cationic azo dyes of the formula I ##STR1## where the variables are as defined in the specification, amines as their intermediates, processes for preparing them, their use for dyeing and printing natural or synthtic substrates, and their mixtures are described.Type: GrantFiled: May 5, 1999Date of Patent: April 11, 2000Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Torsten Freund, Rainer Tresch
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Patent number: 6017917Abstract: Guanidine derivatives of the formula: ##STR1## wherein R.sup.1 is [di(lower)alkylamino](lower)alkyl, morpholinyl(lower)alkyl, lower alkylpiperazinyl or [lower alkylpyrrolidinyl](lower)alkyl,R.sup.2 is halogen, lower alkyl or lower alkoxy, andR.sup.3 is halogen, lower alkyl, lower alkoxy or mono(or di or tri)halo(lower)alkyl,and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: June 26, 1998Date of Patent: January 25, 2000Assignee: Fujisawa Pharamceutical Co., Ltd.Inventors: Atsushi Kuno, Yoshikazu Inoue, Kumi Yamasaki
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Patent number: 6005010Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: August 20, 1997Date of Patent: December 21, 1999Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
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Patent number: 5945545Abstract: Compounds of this invention have the formula: ##STR1## and pharmaceutically acceptable salts, e.g.Type: GrantFiled: December 11, 1997Date of Patent: August 31, 1999Assignee: Merck & Co., Inc.Inventors: Melissa S. Egbertson, George D. Hartman, Laura M. Vassallo
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Patent number: 5932616Abstract: 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: April 4, 1994Date of Patent: August 3, 1999Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia Univerisity in the City of New YorkInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
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Patent number: 5888481Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).Type: GrantFiled: September 29, 1995Date of Patent: March 30, 1999Assignee: AlliedSignal Inc.Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind
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Patent number: 5886046Abstract: This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.Type: GrantFiled: January 19, 1996Date of Patent: March 23, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
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Patent number: 5863950Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.Type: GrantFiled: October 27, 1994Date of Patent: January 26, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Siegfried H. Reich, Kathleen Lewis, Michael Melnick, Mary Ann M. Fuhry, Stephen Warren Kaldor
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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: 5834544Abstract: The present invention relates to compounds containing dual substitutions of an aromatic amine and hindered phenol functionality useful as stabilizers for organic materials. These compounds are of the general formula: ##STR1## R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, substituted or unsubstituted aryl, and substituted or unsubstituted alkyl of 1 to 20 carbon atoms;R.sub.3 is alkylene of 1 to 10 carbon atoms;m is 0 or 1;n is an integer of 1 to 10;q is an integer of 0 to 8;z is 1 or 2, provided that, when q is 0, z must be 1;X represents the links of a chain q links in length, said links being selected from the group consisting of carbon, nitrogen, oxygen, sulfur, silicon, and mixtures thereof; andY is an aromatic group or .PHI., provided that Y can be .PHI.only when q is 0 and m is 1.Type: GrantFiled: October 20, 1997Date of Patent: November 10, 1998Assignee: Uniroyal Chemical Company, Inc.Inventors: Chung-Yuan Lin, R. Scott Archibald
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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: 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: 5783712Abstract: The invention relates to compounds having at least one vinyl ether group which also contain in the molecule at least one further functional group selected from acrylate, methacrylate, epoxy, alkenyl, cycloalkenyl and vinylaryl groups, to compositions, especially for stereolithography, comprising those vinyl ether compounds, and to a method of producing three-dimensional objects using those compositions.Type: GrantFiled: August 13, 1996Date of Patent: July 21, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Bettina Steinmann, Adrian Schulthess, Max Hunziker
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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: 5731350Abstract: Benzenedicarboxylic acid diguanides of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are useful antiarrhythmic pharmaceuticals having a cardioprotective component, even for the prevention of ischemically induced damage, in particular in the induction of ischemically induced cardiac arrhythmias. As a result of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for the treatment of acute or chronic damage caused by ischemia. Moreover, they are distinguished by potent inhibitory action on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.Type: GrantFiled: November 7, 1996Date of Patent: March 24, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5714518Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.Type: GrantFiled: October 27, 1994Date of Patent: February 3, 1998Assignee: Agouron PharmaceuticalsInventors: Siegfried H. Reich, Mark J. Pino, Dzuy T. Nguyen, Anthony J. Trippe
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Patent number: 5703129Abstract: A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.Type: GrantFiled: September 30, 1996Date of Patent: December 30, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Kevin Felsenstein, David W. Smith, Michael A. Poss, Prasad Chaturvedula, Charles P. Sloan
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Patent number: 5700811Abstract: This invention is directed to compounds having the structure: ##STR1## wherein 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 thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.Type: GrantFiled: May 19, 1994Date of Patent: December 23, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind
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Patent number: 5693311Abstract: A compound of the following formula II ##STR1## in which R.sub.7, R.sub.8, R'.sub.7, R'.sub.8, collectively, contain 10-24 hydroxyl groups and are selected, independently, from H, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.10)alkyl substituted with one or more radicals selected from hydroxyl groups, (C.sub.1 -C.sub.3)alkoxy groups and hydroxylated (C.sub.1 -C.sub.3)alkoxy groups, is useful as a contrast agent in diagnostic X-Ray radiography.Type: GrantFiled: March 17, 1995Date of Patent: December 2, 1997Assignee: Guerbet S.A.Inventors: Myriam Petta, Dominique Meyer
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Patent number: 5686633Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.Type: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5674905Abstract: Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors.Type: GrantFiled: December 19, 1994Date of Patent: October 7, 1997Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Caroline Minli Rachel Low, Michael John Pether, Jonathan Michael Richard Davies, David John Dunstone, Iain Mair McDonald
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Patent number: 5663413Abstract: The invention relates to novel contrast media particularly useful for X-ray diagnostic investigations of human and animal body.Type: GrantFiled: May 24, 1995Date of Patent: September 2, 1997Assignee: Dibra S.p.A.Inventors: Fulvio Uggeri, Pier Lucio Anelli, Marino Brocchetta, Massimo Visigalli
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Patent number: 5639881Abstract: Pyrimido[4,5-g]quinazoline quinone derivatives were synthesized as anthranone-like reductive alkylating agents. Like many naturally-occurring antibiotics, these quinone derivatives are designed to afford an alkylating quinone methide species upon reduction and leaving group elimination. Kinetic studies of pyrimido[4,5-g]quinazoline hydroquinones provided evidence of quinone methide intermediates able to trap nucleophiles (alkylation) and protons. The rate of quinone methide formation is determined by the hydroquinone free energy. Thus, a linear free energy relationship for quinone methide formation was obtained by plotting rates of quinone methide formation, as the log, versus the quinone reduction potential. The pyrimido[4-5-g]quinazoline quinone methides fall on this free energy plot, showing that these species are formed by the same mechanism as the other structurally-diverse quinone methides previously studied in this research group.Type: GrantFiled: November 8, 1991Date of Patent: June 17, 1997Assignee: Arizona Board of Regents acting on behalf of Arizona State UniversityInventors: Edward B. Skibo, Robert H. Lemus
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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: 5616799Abstract: A process for the preparation of glycoloylanilide of the formula (G) ##STR1## is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.Type: GrantFiled: April 17, 1995Date of Patent: April 1, 1997Assignee: Hoechst AktiengesellschaftInventors: Siegfried Planker, Theodor Papenfuhs
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Patent number: 5608108Abstract: 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 effect 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: April 17, 1995Date of Patent: March 4, 1997Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia Univeristy in the City of New YorkInventors: Paul A. Marks, Richard A. Rifkind, Ronald Breslow, Branko Jursic
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Patent number: 5599982Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.Type: GrantFiled: March 30, 1995Date of Patent: February 4, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons G. M. De Knaep, Luc J. R. Moens, Eduard J. C. Vreysen
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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: 5575905Abstract: The invention provides a process for the preparation of a 2,4,6-triiodinated or 2,4,6,2',4',6'-hexaiodinated 3,5-disubstituted-aniline or 3,3'-disubstituted-5,5'-linked bisaniline, which process comprises electrochemically iodinating a 3,5-disubstituted-aniline or a 3,3'-disubstituted-5,5'-linked bisaniline in an acidic solvent which comprises water and optionally at least one water-miscible organic solvent.Type: GrantFiled: May 24, 1995Date of Patent: November 19, 1996Assignee: Nycomed Imaging ASInventors: Lars-G oran Wistrand, Klaes Golman, Finn Radner
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Patent number: 5532412Abstract: An aromatic o-hydroxyamide compound of the formula (I) ##STR1## wherein the formula: ##STR2## is a divalent aromatic group the formula: ##STR3## R.sup.1 =H, halogen, C.sub.1-10 alkyl group, or C.sub.1 -alkoxyl group, Ar.sub.1, Ar.sub.2, Ar.sub.3 =a divalent aromatic groups, X, Y=O or S, and n=0 or 1, has an excellent ultraviolet ray-absorption and heat-resistance and is useful for enhancing an ultraviolet ray-resistance of polymeric materials, for example, wholly aromatic polyamide fibers.Type: GrantFiled: September 13, 1994Date of Patent: July 2, 1996Assignee: Teijin LimitedInventors: Toshitsugu Matsuki, Toshihiro Santa
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Patent number: 5502061Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: September 26, 1994Date of Patent: March 26, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Y. Hui, Charles D. Jones, Louis N. Jungheim, Pamela A. Pennington
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Patent number: 5434186Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.Type: GrantFiled: September 28, 1993Date of Patent: July 18, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
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Patent number: 5424349Abstract: Tertiary amides have been developed which have low volatility and good thermal stability and which are effective in stabilizing organic materials that are normally susceptible to oxidative deterioration. The novel antioxidants are tertiary amides corresponding to the formula: ##STR1## wherein R is a mono-, di-, or trivalent aromatic or saturated aliphatic hydrocarbon group containing 1-20 carbons; n is an integer of 1-3 which is equal to the valence of R; R' is phenyl, benzyl, or C.sub.1 -C.sub.6 alkyl; m is an integer of 1-3; R" is a C.sub.1 -C.sub.4 alkylene group; Z and Z' are independently selected from hydrogen and alkyl; and Q is carbonyl or sulfonyl.Type: GrantFiled: August 9, 1993Date of Patent: June 13, 1995Assignee: Albemarle CorporationInventor: Vincent J. Gatto
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Patent number: 5414120Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.Type: GrantFiled: November 12, 1993Date of Patent: May 9, 1995Assignee: Bayer AGInventors: Klaus Pohmer, Rainer Weber, Cornelia Dorzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
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Patent number: 5395971Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X--Y).Type: GrantFiled: March 11, 1994Date of Patent: March 7, 1995Assignee: The Board of Regents of The University of OklahomaInventors: Kenneth M. Nicholas, Anurag S. Srivastava
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Patent number: 5396003Abstract: A process for the recovery and purification of 1,1,2-trichloroethane from the intermediates produced for the production of ioversol for reuse thereof.Type: GrantFiled: May 27, 1993Date of Patent: March 7, 1995Assignee: Mallinckrodt Medical PMCInventor: William Z. McCarthy
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Patent number: 5393788Abstract: Novel oxamide derivatives are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful as inhibitors of PDE IV and are therefor useful in the treatment of disease states mediated or exacerbated thereby.Type: GrantFiled: March 2, 1993Date of Patent: February 28, 1995Assignee: SmithKline Beecham CorporationInventors: Paul E. Bender, Siegfried B. Christensen, IV, Klaus M. Esser, Cornelia J. Forster, Michael D. Ryan, Philip L. Simon
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Patent number: 5391808Abstract: N,N,N',N'-Tetrasubstituted 1,4-diamino-2-butenes where the substituents are alkyl, cycloalkyl, aralkyl, aryl or mixtures thereof provide effective antioxidant protection to lubricants and/or synthetic polymers.Type: GrantFiled: November 1, 1993Date of Patent: February 21, 1995Assignee: Ciba-Geigy CorporationInventors: Joseph E. Babiarz, Glen T. Cunkle, Werner Rutsch
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Patent number: 5387607Abstract: O-Benzyloxime ethers of the formula I ##STR1## where X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: December 13, 1993Date of Patent: February 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5356613Abstract: The compound N-(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl)-glycolamido]-N'-methyl-2,4,6 -triiodoisophthalamide and similar such compounds may be used as x-ray contrast agents which are water-soluble, safe and in an aqueous solution are non-viscous. Methods of preparing N-(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl)-glycolamido]-N'-methyl-2,4,6 -triiodoisophthalamide and the analogous compounds are provided.Type: GrantFiled: May 8, 1992Date of Patent: October 18, 1994Assignee: Mallinckrodt Medical, Inc.Inventors: Youlin Lin, Rebecca A. Wallace, David H. White
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Patent number: 5349109Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X-Y).Type: GrantFiled: August 26, 1993Date of Patent: September 20, 1994Assignee: The Board of Regents of the University of OklahomaInventors: Kenneth M. Nicholas, Anurag S. Srivastava