The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/227)
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Patent number: 5585492Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.Type: GrantFiled: October 11, 1994Date of Patent: December 17, 1996Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Barbara B. Chen, Michael Clare, Bipinchandra N. Desai, Stevan W. Djuric, Stephen H. Docter, Alan F. Gasiecki, Richard A. Haack, Chi-Dean Liang, Julie M. Miyashiro, Thomas D. Penning, Mark A,. Russell, Stella S. Yu
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Patent number: 5525474Abstract: Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: ##STR1## wherein: X=hydrogen or acetyl;n=1 to p where p=MW of Z/1000;Z=a poly(amino acid) or polysaccharide; andR3=a bond or ##STR2## wherein R2=an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.Type: GrantFiled: January 31, 1994Date of Patent: June 11, 1996Assignee: Boehringer Mannheim CorporationInventors: Gerald F. Sigler, Charles F. Walter, Todd Glancy, Erasmus Huber, Frank E. Klein
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Patent number: 5491149Abstract: This invention relates to substituted dihydroxypropylamines, a process to prepare intermediates useful for the synthesis of these compounds, compositions comprising such compounds, and a method of treating retroviral infection.Type: GrantFiled: August 26, 1994Date of Patent: February 13, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Prabhakar K. Jadhav
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Patent number: 5489688Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.Type: GrantFiled: March 24, 1994Date of Patent: February 6, 1996Assignee: Pfizer Inc.Inventor: Frank J. Urban
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Patent number: 5470921Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.Type: GrantFiled: May 20, 1994Date of Patent: November 28, 1995Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
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Patent number: 5446161Abstract: Compounds of the formula ##STR1## wherein and their pharmaceutically acceptable acid addition salts inhibit proteases of vital origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.Type: GrantFiled: July 20, 1992Date of Patent: August 29, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Balraj K. Handa, Peter J. Machin, Joseph A. Martin, Sally Redshaw, Gareth J. Thomas
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5385918Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, n, X.sup.1 and Z are defined in the specification.Type: GrantFiled: February 9, 1993Date of Patent: January 31, 1995Assignee: Miles Inc.Inventors: Richard D. Connell, David G. Osterman, Michael E. Katz, Rudolf Hanko, Stephan Schneider
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Patent number: 5364867Abstract: 4-Phenylpiperidines of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy or lower-alkoxy;R.sub.2 is hydrogen, hydroxy, lower-alkanoyl, aroyl, lower-alkoxycarbonyl, lower-alkanoyloxy, lower-alkoxycarbonyl, or CONR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are the same or different lower-alkyl or R.sub.3 and R.sub.4 together represent a lower-alkylene chain;X is methylene or carbonyl;Y is methylene, C.dbd.NOH, hydroxymethylene or carbonyl;or pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of psychoses and other ailments of the central nervous system.Type: GrantFiled: November 30, 1992Date of Patent: November 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne
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Patent number: 5338859Abstract: The present invention provides a process for the production of calcium salts of hydantoic acids and which comprises the steps of reacting a hydantoin with a calcium base material such as calcium hydroxide in an aqueous medium at a sufficient temperature and for a sufficient period of time to form the calcium salt of the corresponding hydantoic acid and then separating the calcium salt of such acid from the reaction mass. This separation can include the further steps of cooling the reaction mass down to facilitate the precipitation of the acid/salt crystals and then separating the precipitate by means of filtering or centrifugating. These acids can then be subjected to a HNO.sub.2 -mediated decarbamoylation process followed by an optical resolution step to thus provide high yields of D-p-hydroxyphenylglycine which is a key synthetic immediate or building block for semi-synthetic penicillin and cephalosporins.Type: GrantFiled: February 12, 1993Date of Patent: August 16, 1994Assignee: Hoechst Celanese CorporationInventor: Apurba Bhattacharya
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Patent number: 5322848Abstract: A compound, or solvate or salt thereof, of formula ##STR1## R.sub.1 is hydrogen, halogen, or C.sub.1-6 alkyl; R.sub.2 and R.sub.3 are hydrogen or C.sub.1-6 alkyl;R.sub.5 together with R.sub.4 forms a --(CH).sub.2).sub.2 -- group optionally substituted by one or two C.sub.1-6 alkyl;W is halogen or when A is gem-dimethyl substituted piperidine, is OH;a is 1 or 2,useful in the treatment of pain.Type: GrantFiled: May 22, 1992Date of Patent: June 21, 1994Assignee: Dr. Lo Zembeletti S.p.A.Inventors: Robert Colle, Giulio Dondio, Giuseppe Giardina, Lorenzo Leurini, Vittorio Vecchietti
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5268472Abstract: Nitrogen-containing heterocyclic (poly) peroxycarboxylic acid monopersulfates which have the formula: ##STR1## wherein the symbols have the following meanings: R represents a hydrogen atom or an alkyl, (hetero)cycloalkyl, (hetero)aryl, alkyl-aryl or arylalkyl group, wherein said groups are optionally substituted, or a carboxylic group or a peroxycarboxylic group, or any other substituents non-reactive in the presence of the peroxycarboxylic group;R.sup.1 represents an alkyl group > C.sub.5 ;n is a number selected from 0,1 and 2;m is a number selected from 1, 2 and 3;and the heterocyclic ring may be in its turn condensed with at least one further (hetero) aromatic or (hetero)cycloalkylic ring. The invention relates to a preparation process for, and to their use, as bleaching agents.Type: GrantFiled: October 5, 1992Date of Patent: December 7, 1993Assignee: Ausimont S.p.A.Inventors: Carlo Venturello, Claudio Cavallotti, Fiorella Achilli
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Patent number: 5214054Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: July 17, 1990Date of Patent: May 25, 1993Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5214057Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which an ether group forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl- or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1-8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1-4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.Type: GrantFiled: August 20, 1991Date of Patent: May 25, 1993Assignee: Novo Nordisk A/SInventors: Lars Jacob S. Knudsen, Anker S. Jorgensen, Knud E. Andersen, Ursula Sonnewald
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Patent number: 5214148Abstract: N-Phenyl-N-(4-piperdinyl)amide derivatives are disclosed having the general formula (I): ##STR1## wherein X, Ar, R and R.sup.1 are defined, including isomeric forms thereof and acid addition salts thereof. The compounds exhibit analgesic activity. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).Type: GrantFiled: July 2, 1992Date of Patent: May 25, 1993Assignee: Glaxo Inc.Inventors: Paul L. Feldman, Marcus F. Brackeen
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Patent number: 5198451Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein Y is ##STR2## wherein R.sup.1 and R.sup.2 independently are C.sub.3-8 cycloalkyl phenyl or thienyl all of which may be optionally substituted with halogen, trifluoromethyl, C.sub.1-16 alkyl or C.sub.1-6 alkoxy;s is 1, 2 or 3;x is --CH.sub.2 --, --O-- or ##STR3## -wherein R.sup.3 is hydrogen or C.sub.1-6 -alkyl; r is 2, 3 or 4; R.sup.4 and R.sup.5 each represents hydrogen or may together represent a bond and R.sup.6 is OH or C.sub.1-8 -alkoxy; and pharmaceutically acceptable acid addition salts are potent inhibitors of GABA uptake from the synaptic cleft.Type: GrantFiled: November 20, 1990Date of Patent: March 30, 1993Assignee: Novo Nordisk A/SInventors: Knud E. Andersen, Lars J. Stray Knudsen, Ursula Sonnewald, Per O. Sorensen
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Patent number: 5194588Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.Type: GrantFiled: March 9, 1990Date of Patent: March 16, 1993Assignee: ICI Americas Inc.Inventors: Philip D. Edwards, John A. Schwartz, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger
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Patent number: 5179111Abstract: Imidazole derivatives of general Formula I ##STR1## wherein R.sup.1 means hydrogen, an optionally substituted C.sub.1-10 hydrocarbon or hetaryl residue, or a cyclic ether residue,R.sup.2 means hydrogen, halogen, an optionally substituted amino, nitro, azide, thiocyanate or cyano group, a linear or branched C.sub.1-10 -alkyl residue optionally substituted with halogen, or -OR.sup.1 wherein R.sup.1 has the above-mentioned meanings, andR.sup.1 and R.sup.2 jointly with the oxygen atom form a saturated or unsaturated 5- to 7-membered ring which can contain still another hetero atom,R.sup.3 means hydrogen, a linear or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxyalkyl group,R.sup.4 means -COOR.sup.5, -CONR.sup.6 R.sup.7, -CN, ##STR2## and their use as medicinal agents are disclosed.Type: GrantFiled: December 14, 1988Date of Patent: January 12, 1993Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Ralph Rohde, Herbert H. Schneider, Lechoslaw Turski
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5089507Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.3 is hydrogen, C.sub.1-6 alkyl or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5 are independently hydrogen, hydroxyl, halogen, C.sub.1-6 alkyl or aryl, provided both R.sub.4 and R.sub.5 are not simultaneously hydrogen; and p is an integer from 1 to 4,is useful for the treatment of pain or hyponatraemic disease states.Type: GrantFiled: September 25, 1989Date of Patent: February 18, 1992Assignee: Dr. L. Zambeletti SpAInventors: Vittorio Vecchietti, Roberto Colle, Antonio Giordani, Giulio Dondio
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Patent number: 5081135Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of hydrogen ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.Type: GrantFiled: September 10, 1990Date of Patent: January 14, 1992Assignee: Roussel UclafInventors: Constantin Agouridas, Patrick Fauveau
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Patent number: 5071859Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which an ether group forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1 -C.sub.8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1 -C.sub.4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.Type: GrantFiled: December 14, 1989Date of Patent: December 10, 1991Inventors: Lars Jacob S. Knudsen, Anker S. Jorgensen, Knud E. Andersen, Ursula Sonnewald
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Patent number: 5055450Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.Type: GrantFiled: March 13, 1990Date of Patent: October 8, 1991Assignee: ICI Americas Inc.Inventors: Philip D. Edwards, John A. Schwartz, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger
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Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 4983614Abstract: The invention relates to benzhydryloxyethylpiperidine derivatives corresponding to one of the formulae below: ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different, represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an aryloxy group or the trifluoromethyl group,R represents hydrogen, a cation, an alkyl group, an aryl group or an arylalkyl group, andn is equal to 0 or 1, and their pharmaceutically acceptable salts, useful in the treatment of spasmodic states and allergies.Type: GrantFiled: December 28, 1988Date of Patent: January 8, 1991Assignee: Les Laboratoires MeramInventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
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Patent number: 4970022Abstract: Mustard oils of the formula IR--(A.sup.1 --Z.sup.1).sub.n --A.sup.2 --Z.sup.2 --A.sup.3 --NCSin which A.sup.1, A.sup.2, A.sup.3, R, Z.sup.1, Z.sup.2 and n have the meaning specified in claim 1 can be used as components of liquid-crystalline phases.Type: GrantFiled: August 19, 1987Date of Patent: November 13, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler
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Patent number: 4968798Abstract: Liquid-crystalline, 1-substituted piperidine-4-carboxylic acid esters, process for their preparation, and their use in liquid-crystalline mixturesThe novel 1-substituted piperidine-4-carboxylic acid esters of the general formula (I) ##STR1## are liquid-crystalline and exhibit, in particular, S.sub.c or S.sub.c * phases. In this formula, R.sup.1 or R.sup.2 is a radical of the general formula (II) ##STR2## in which the rings are aromatic, heteroaromatic or optionally heteratom-containing cycloaliphatic molecular components, such as 1,4-phenylene, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene, which are linked via a single bond (in the case where n and p=zero) or via functional groups Z.sub.1 or Z.sub.2 such as CO- or CH.sub.2 -O, and in which k, n, m, p and q are zero or 1, where k+m+p is at least 1 and p=zero when m=zero. The other radical R.sup.1 or R.sup.2 is an optionally substituted straight-chain or branched alkyl group having 1 to 20 carbon atoms, X.sub.1 denotes, S, phenylenoxy or CH.sub.2, and X.sub.Type: GrantFiled: December 22, 1988Date of Patent: November 6, 1990Assignee: Hoechst AktiengesellschaftInventors: Dieter Gunther, Dieter Ohlendorf, Rainer Wingen
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Patent number: 4916230Abstract: This invention relates to a new one-step process for preparation of novel N-(acyloxyalkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for drugs having a primary or secondary amine function thereon.Type: GrantFiled: July 2, 1984Date of Patent: April 10, 1990Assignee: Merck & Co., Inc.Inventor: Jose Alexander
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Patent number: 4916175Abstract: Compounds are provided which are useful as light stabilizers for polymeric materials and which have the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are organic radicals, R.sub.3 and R.sub.15 are hydrogen or organic radicals and R is hydrogen, oxygen or an organic radical.Type: GrantFiled: November 5, 1987Date of Patent: April 10, 1990Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4910312Abstract: Selected analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: June 16, 1988Date of Patent: March 20, 1990Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4910190Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.Type: GrantFiled: January 20, 1987Date of Patent: March 20, 1990Assignee: ICI Americas Inc.Inventors: Scott H. Bergeson, Philip D. Edwards, John A. Schwartz, Andrew Shaw, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger, Donald J. Wolanin
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Patent number: 4873327Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sup.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.Type: GrantFiled: March 8, 1988Date of Patent: October 10, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Martin Anderson, Anthony G. Brinnand
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Patent number: 4772615Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: October 14, 1987Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4740508Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: April 22, 1985Date of Patent: April 26, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 4672139Abstract: Benzoylurea compounds of the formula ##STR1## wherein the meaning of each of the symbols is described in the specification.Type: GrantFiled: July 21, 1986Date of Patent: June 9, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Martin Anderson
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4638000Abstract: Novel condensed seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 and R.sup.5 are independently hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or lower alkyl; R.sup.6 is a condensed or non-condensed hetero-alicyclic containing at least one atom of N, O and S as a ring-forming atom which may be substituted; A is an alkylene chain; n is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases, such as hypertension, cardiopathy and cerebral apoploxy.Type: GrantFiled: January 14, 1985Date of Patent: January 20, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4537698Abstract: New piperidine derivatives ##STR1## in which R.sup.1 and R.sup.2 each independently is alkyl or alkoxy each of 1 to 10 C atoms, --Y--Z, F, Cl, Br or CN, and the radical R.sup.1 can also be H,Y is --CO--O--, --O--CO or a single bond,Z is --Q--R.sup.3 or alkyl having 1-10 C atoms,Q is 1,4-phenylene or 1,4-cyclohexylene,R.sup.3 is alkyl having 1-10 C atoms, F or CN, andA is 1,4-cyclohexylene or 1,3-dioxane-2,5-diyl, and their acid addition salts,can be used as components of dielectrics for electro-optical display elements.Type: GrantFiled: May 31, 1983Date of Patent: August 27, 1985Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Wolfgang Sucrow, Wolfgang Schatull, Peter Fuss
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Patent number: 4481315Abstract: Compounds which contain, in their molecule, at least one 2-(2'-hydroxyphenyl)-benztriazole group or one 2-hydroxybenzophenone group and at least one polyalkylpiperidine group are effective light stabilizers for organic materials, in particular for polymers. The use of the compounds as light stabilizers for lacquers is of particular importance.Type: GrantFiled: February 28, 1983Date of Patent: November 6, 1984Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Mario Slongo
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Patent number: 4444928Abstract: Polymers or oligometic compounds of the general formula ##STR1## in which X, X.sup.a and X.sup.b are an ester, amide or cyano group, Y, Y.sup.a and Y.sup.b are --O-- or --NR.sup.10 --, R.sup.1, R.sup.1a and R.sup.1b are a group which contains a polyalkylpiperidine radical, and R.sup.1a can also be alkyl, and R.sup.3, R.sup.3a and R.sup.3b are alkylene, alkenylene, arylene-dialkylene, cycloalkylene-dialkylene or monooxa-alkylene or polyoxa-alkylene, can be prepared by the polycondensation of malonic acid esters or amides or cyanoacetic acid esters or amides with difunctional compounds, preferably dihalogen compounds, in the presence of bases. The products obtained have a molecular weight of 800 to 20,000 and are outstanding light stabilizers for organic polymers.Type: GrantFiled: August 4, 1982Date of Patent: April 24, 1984Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
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Patent number: 4433152Abstract: A compound of the formula, ##STR1## wherein R represents a hydrogen atom, a naphthyl, indanyl, tetrahydronaphthyl or pyridyl group, or a phenyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, and an alkyl, alkenyl, alkoxy, alkanoyl, cyano, formyl, trifluoromethyl, phenyl, phenylalkyl, alkanoyl-amino, aminosulfonyl, carboxyl, alkoxycarbonyl, benzyloxycarbonyl, benzoylvinyl, phenylvinylcarbonyl, carboxyvinyl, and diphenyl-methyloxycarobnylvinyl group, A represents an oxygen or sulfur atom, and n represents an integer of 0 to 3, with the proviso that when n is an integer of 0, R must not be a hydrogen atom, or a pharmaceutically acceptable salt thereof is effectively useful for inhibiting a complement reaction, inflammation caused by an allergic reaction, and platelet aggregation.Type: GrantFiled: May 19, 1982Date of Patent: February 21, 1984Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mutsumi Muramatsu, Toshio Satoh, Hiroyasu Sekine, Atsushi Tendo, Yoshio Kikawa, Kaname Kondo
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Patent number: 4383999Abstract: N-Substituted azaheterocyclic carboxylic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.Type: GrantFiled: April 28, 1982Date of Patent: May 17, 1983Assignee: Smithkline Beckman CorporationInventors: William E. Bondinell, John J. Lafferty, Charles L. Zirkle
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Patent number: 4336405Abstract: There are described novel compounds which include a silver halide developing function, a colorless ligand which is a radical of an iminodiacetic acid and a radical containing an onium group. The compounds are useful in photography as silver halide developing agents and also may be complexed with metals to form dye developers.Type: GrantFiled: July 11, 1980Date of Patent: June 22, 1982Assignee: Polaroid CorporationInventor: Elbert M. Idelson
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Patent number: 4289686Abstract: Compounds which contain, in their molecule, at least one 2-(2'-hydroxyphenyl)-benztriazole group or one 2-hydroxybenzophenone group and at least one polyalkylpiperidine group are effective light stabilizers for organic materials, in particular for polymers. The use of the compounds as light stabilizers for lacquers is of particular importance.Type: GrantFiled: September 17, 1979Date of Patent: September 15, 1981Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Mario Slongo
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Patent number: 4261895Abstract: The compounds of formula I ##STR1## wherein R is(a) hydrogen,(b) cycloalkyl of 3 to 7 carbon atoms,(c) alkyl of 2 to 5 carbon atoms monosubstituted by hydroxy, with the proviso that the hydroxyl radical is separated by at least 2 carbon atoms from the carbonylthio moiety to which R is bound,(d) phenyl or phenylalkyl of 7 to 11 carbon atoms, each monosubstituted or independently disubstituted in the phenyl ring by alkyl of 1 to 4 carbon atoms or halogen of atomic number of from 9 to 35, or phenyl or phenylalkyl of 7 to 11 carbon atoms, each monosubstituted or independently disubstituted or independently trisubstituted in the phenyl ring by alkoxy of 1 to 4 carbon atoms, or(e) furyl, benzo[b]furyl, thienyl, benzo[b]thienyl, pyridyl, quinolyl, isoquinolyl, 2- or 3-pyrrolyl or indolyl other than 1-indolyl,R.sub.1 and R.sub.Type: GrantFiled: October 23, 1978Date of Patent: April 14, 1981Assignee: Sandoz Ltd.Inventor: Erik Wiskott
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Patent number: 4259337Abstract: Novel m-trifluoromethylphenyl-piperidines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, branched or straight chain alkyl of 1 to 5 carbon atoms, alkenyl of 3 to 5 carbon atoms, alkynyl of 3 to 5 carbon atoms and phenyl alkyl of 1 to 3 alkyl carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressive, anorexigenic and antiparkinsonian activity and their preparation and novel intermediates formed therein.Type: GrantFiled: May 12, 1977Date of Patent: March 31, 1981Assignee: Roussel UclafInventors: Lucien Nedelec, Jacques Guillaume, Claude Dumont
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Patent number: 4247694Abstract: The invention relates to metal salts of hydroxybenzoic acids which are complexed with a 4-amino-polyalkylpiperidine derivative or to mixed metal salts of a hydroxybenzoic acid and a polyalkylpiperidine carboxylic acid which may be complexed or not with an 4-amino-polyalkylpiperidine. The metal cation may be that of a di- or trivalent metal such as Ni, Co, Al, Zn or Ca. From hydroxybenzoic acids the 3,5-di-tert.butylbenzoic acid is preferred.These salts are valuable light stabilizers for plastics, especially for polyolefins, styrene polymers and polyamides or polyurethanes respectively. The salts show a strong tendency to retain water. For high compatibility with plastics a low water content is of importance.Type: GrantFiled: October 10, 1978Date of Patent: January 27, 1981Assignee: Ciba-Geigy CorporationInventor: Michael Rasberger
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Patent number: 4223147Abstract: The invention relates to new methylol derivatives of 2,2,6,6-tetraalkylpiperidines, to their production and to their use as chemically attached stabilizers for polymers containing reactive OH- and NH-groups.Type: GrantFiled: September 19, 1977Date of Patent: September 16, 1980Assignee: Bayer AktiengesellschaftInventors: Harald Oertel, Paul Uhrhan, Reinhard Lantzsch, Ernst Roos, Hans Schroer, Dieter Arlt
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Patent number: 4145426Abstract: Compounds of the structure: ##STR1## where A is either ##STR2## where R.sub.1 to R.sub.4 are various substituents are active as antibacterials and antifungals.Type: GrantFiled: July 18, 1977Date of Patent: March 20, 1979Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel