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)
  • Patent number: 5585492
    Abstract: 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: Grant
    Filed: October 11, 1994
    Date of Patent: December 17, 1996
    Assignee: 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
  • Patent number: 5525474
    Abstract: 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: Grant
    Filed: January 31, 1994
    Date of Patent: June 11, 1996
    Assignee: Boehringer Mannheim Corporation
    Inventors: Gerald F. Sigler, Charles F. Walter, Todd Glancy, Erasmus Huber, Frank E. Klein
  • Patent number: 5491149
    Abstract: 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: Grant
    Filed: August 26, 1994
    Date of Patent: February 13, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Prabhakar K. Jadhav
  • Patent number: 5489688
    Abstract: 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: Grant
    Filed: March 24, 1994
    Date of Patent: February 6, 1996
    Assignee: Pfizer Inc.
    Inventor: Frank J. Urban
  • Patent number: 5470921
    Abstract: 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: Grant
    Filed: May 20, 1994
    Date of Patent: November 28, 1995
    Assignee: Sandoz Ltd.
    Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
  • Patent number: 5446161
    Abstract: 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: Grant
    Filed: July 20, 1992
    Date of Patent: August 29, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Balraj K. Handa, Peter J. Machin, Joseph A. Martin, Sally Redshaw, Gareth J. Thomas
  • Patent number: 5423998
    Abstract: 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: Grant
    Filed: April 13, 1993
    Date of Patent: June 13, 1995
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavallotti
  • Patent number: 5385918
    Abstract: 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: Grant
    Filed: February 9, 1993
    Date of Patent: January 31, 1995
    Assignee: Miles Inc.
    Inventors: Richard D. Connell, David G. Osterman, Michael E. Katz, Rudolf Hanko, Stephan Schneider
  • Patent number: 5364867
    Abstract: 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: Grant
    Filed: November 30, 1992
    Date of Patent: November 15, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne
  • Patent number: 5338859
    Abstract: 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: Grant
    Filed: February 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Hoechst Celanese Corporation
    Inventor: Apurba Bhattacharya
  • Patent number: 5322848
    Abstract: 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: Grant
    Filed: May 22, 1992
    Date of Patent: June 21, 1994
    Assignee: Dr. Lo Zembeletti S.p.A.
    Inventors: Robert Colle, Giulio Dondio, Giuseppe Giardina, Lorenzo Leurini, Vittorio Vecchietti
  • Patent number: 5294616
    Abstract: 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: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5268472
    Abstract: 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: Grant
    Filed: October 5, 1992
    Date of Patent: December 7, 1993
    Assignee: Ausimont S.p.A.
    Inventors: Carlo Venturello, Claudio Cavallotti, Fiorella Achilli
  • Patent number: 5214054
    Abstract: 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: Grant
    Filed: July 17, 1990
    Date of Patent: May 25, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
  • Patent number: 5214057
    Abstract: 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: Grant
    Filed: August 20, 1991
    Date of Patent: May 25, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Lars Jacob S. Knudsen, Anker S. Jorgensen, Knud E. Andersen, Ursula Sonnewald
  • Patent number: 5214148
    Abstract: 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: Grant
    Filed: July 2, 1992
    Date of Patent: May 25, 1993
    Assignee: Glaxo Inc.
    Inventors: Paul L. Feldman, Marcus F. Brackeen
  • Patent number: 5198451
    Abstract: 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: Grant
    Filed: November 20, 1990
    Date of Patent: March 30, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Knud E. Andersen, Lars J. Stray Knudsen, Ursula Sonnewald, Per O. Sorensen
  • Patent number: 5194588
    Abstract: 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: Grant
    Filed: March 9, 1990
    Date of Patent: March 16, 1993
    Assignee: ICI Americas Inc.
    Inventors: Philip D. Edwards, John A. Schwartz, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger
  • Patent number: 5179111
    Abstract: 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: Grant
    Filed: December 14, 1988
    Date of Patent: January 12, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Biere, Ralph Rohde, Herbert H. Schneider, Lechoslaw Turski
  • Patent number: 5120843
    Abstract: 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: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5089507
    Abstract: 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: Grant
    Filed: September 25, 1989
    Date of Patent: February 18, 1992
    Assignee: Dr. L. Zambeletti SpA
    Inventors: Vittorio Vecchietti, Roberto Colle, Antonio Giordani, Giulio Dondio
  • Patent number: 5081135
    Abstract: 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: Grant
    Filed: September 10, 1990
    Date of Patent: January 14, 1992
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Patrick Fauveau
  • Patent number: 5071859
    Abstract: 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: Grant
    Filed: December 14, 1989
    Date of Patent: December 10, 1991
    Inventors: Lars Jacob S. Knudsen, Anker S. Jorgensen, Knud E. Andersen, Ursula Sonnewald
  • Patent number: 5055450
    Abstract: 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: Grant
    Filed: March 13, 1990
    Date of Patent: October 8, 1991
    Assignee: ICI Americas Inc.
    Inventors: Philip D. Edwards, John A. Schwartz, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger
  • Patent number: 5039685
    Abstract: 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: Grant
    Filed: May 10, 1989
    Date of Patent: August 13, 1991
    Assignee: Novo Nordisk A/S
    Inventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
  • Patent number: 4983614
    Abstract: 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: Grant
    Filed: December 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Les Laboratoires Meram
    Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
  • Patent number: 4970022
    Abstract: 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: Grant
    Filed: August 19, 1987
    Date of Patent: November 13, 1990
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler
  • Patent number: 4968798
    Abstract: 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: Grant
    Filed: December 22, 1988
    Date of Patent: November 6, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Dieter Gunther, Dieter Ohlendorf, Rainer Wingen
  • Patent number: 4916230
    Abstract: 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: Grant
    Filed: July 2, 1984
    Date of Patent: April 10, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Patent number: 4916175
    Abstract: 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: Grant
    Filed: November 5, 1987
    Date of Patent: April 10, 1990
    Assignee: Sandoz Ltd.
    Inventor: Lajos Avar
  • Patent number: 4910312
    Abstract: 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: Grant
    Filed: June 16, 1988
    Date of Patent: March 20, 1990
    Assignee: Warner-Lambert Company
    Inventor: Michael R. Pavia
  • Patent number: 4910190
    Abstract: 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: Grant
    Filed: January 20, 1987
    Date of Patent: March 20, 1990
    Assignee: 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
  • Patent number: 4873327
    Abstract: 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: Grant
    Filed: March 8, 1988
    Date of Patent: October 10, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Martin Anderson, Anthony G. Brinnand
  • Patent number: 4772615
    Abstract: 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: Grant
    Filed: October 14, 1987
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventor: Michael R. Pavia
  • Patent number: 4740508
    Abstract: 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: Grant
    Filed: April 22, 1985
    Date of Patent: April 26, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4672139
    Abstract: Benzoylurea compounds of the formula ##STR1## wherein the meaning of each of the symbols is described in the specification.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: June 9, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Martin Anderson
  • Patent number: 4656180
    Abstract: 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: Grant
    Filed: March 5, 1985
    Date of Patent: April 7, 1987
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
  • Patent number: 4638000
    Abstract: 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: Grant
    Filed: January 14, 1985
    Date of Patent: January 20, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4537698
    Abstract: 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: Grant
    Filed: May 31, 1983
    Date of Patent: August 27, 1985
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Wolfgang Sucrow, Wolfgang Schatull, Peter Fuss
  • Patent number: 4481315
    Abstract: 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: Grant
    Filed: February 28, 1983
    Date of Patent: November 6, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Rody, Mario Slongo
  • Patent number: 4444928
    Abstract: 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: Grant
    Filed: August 4, 1982
    Date of Patent: April 24, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 4433152
    Abstract: 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: Grant
    Filed: May 19, 1982
    Date of Patent: February 21, 1984
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mutsumi Muramatsu, Toshio Satoh, Hiroyasu Sekine, Atsushi Tendo, Yoshio Kikawa, Kaname Kondo
  • Patent number: 4383999
    Abstract: 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: Grant
    Filed: April 28, 1982
    Date of Patent: May 17, 1983
    Assignee: Smithkline Beckman Corporation
    Inventors: William E. Bondinell, John J. Lafferty, Charles L. Zirkle
  • Patent number: 4336405
    Abstract: 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: Grant
    Filed: July 11, 1980
    Date of Patent: June 22, 1982
    Assignee: Polaroid Corporation
    Inventor: Elbert M. Idelson
  • Patent number: 4289686
    Abstract: 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: Grant
    Filed: September 17, 1979
    Date of Patent: September 15, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Rody, Mario Slongo
  • Patent number: 4261895
    Abstract: 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: Grant
    Filed: October 23, 1978
    Date of Patent: April 14, 1981
    Assignee: Sandoz Ltd.
    Inventor: Erik Wiskott
  • Patent number: 4259337
    Abstract: 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: Grant
    Filed: May 12, 1977
    Date of Patent: March 31, 1981
    Assignee: Roussel Uclaf
    Inventors: Lucien Nedelec, Jacques Guillaume, Claude Dumont
  • Patent number: 4247694
    Abstract: 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: Grant
    Filed: October 10, 1978
    Date of Patent: January 27, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Michael Rasberger
  • Patent number: 4223147
    Abstract: 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: Grant
    Filed: September 19, 1977
    Date of Patent: September 16, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Harald Oertel, Paul Uhrhan, Reinhard Lantzsch, Ernst Roos, Hans Schroer, Dieter Arlt
  • Patent number: 4145426
    Abstract: 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: Grant
    Filed: July 18, 1977
    Date of Patent: March 20, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel