Plural Nitrogens In Alcohol Moiety Patents (Class 560/251)
  • Patent number: 6218536
    Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.
    Type: Grant
    Filed: October 7, 1998
    Date of Patent: April 17, 2001
    Assignee: Ciba Specialty Chemcials Corporation
    Inventors: Glen Thomas Cunkle, Thomas F. Thompson, Volker H. von Ahn, Roland A. E. Winter
  • Patent number: 6187955
    Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof wherein each of A and B is a C2-C8 alkylene, D is a single bond, —CO— or a C1-C6 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R1 is H, a lower alkyl or the like, 1 is 1 to 10 and G is H, —OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: February 13, 2001
    Assignee: Kao Corporation
    Inventors: Minoru Nagai, Hiromitsu Kawada, Mayumi Tsuchiya, Seiji Yamasaki, Akira Yamamuro, Toshiya Ono
  • Patent number: 6143790
    Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: November 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
  • Patent number: 6140361
    Abstract: 2-Deoxystreptamine is an aminocyclitol whose structural stability and abundant functionality make it an attractive scaffold for the combinatorial generation of small molecules. The ability to selectively functionalize the various positions of 2-deoxystreptamine with an almost infinite number of different groups ensures that the libraries so generated will be both spatially and functionally diverse. These compounds can then be screened for biological activity to afford lead compounds for pharmaceutical programs. Additionally, biological ligand mimics based on 2-deoxystreptamine can be readily appended, either directly or through a tether, to solid surfaces or incorporated covalently into gels to afford novel materials useful in separation science.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: October 31, 2000
    Assignee: Scriptgen Pharmaceuticals, Inc.
    Inventors: Gary R. Gustafson, David G. Powers, Mark A. Wuonola
  • Patent number: 6124270
    Abstract: A cationic amphipathic compound of formula (I), ##STR1## wherein A is a single bond, an NH--R' grouping or (a), wherein --R'-- is a straight or branched, optionally substituted, saturated or unsaturated C.sub.1-22 aliphatic chain optionally interrupted by one or more O, S or N heteroatoms and one or more saturated, unsaturated or aromatic carbocyclic or heterocyclic radicals; each of R.sub.1, R.sub.2 and R.sub.3, which are the same or different, is a higher acyl or alkyl grouping; each of R.sub.7, R.sub.8 and R.sub.9, which are the same or different, is a (CH.sub.2).sub.n alkylene radical where 1.ltoreq.N.ltoreq.6; each of R.sub.4, R.sub.5 and R.sub.6, which are the same or different, is a hydrogen atom or an optionally substituted C.sub.1-22 alkyl, alkenyl, alkynyl or acyl radical optionally interrupted by one or more heteroatoms selected from), S and N, or one or more saturated, unsaturated or aromatic carbocyclic or heterocyclic radicals, or else at least two of the groupings R.sub.4, R.sub.5 and R.sub.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: September 26, 2000
    Assignee: Pasteur Merieux Serums et Vaccins
    Inventor: Jean Haensler
  • Patent number: 6080767
    Abstract: The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: June 27, 2000
    Assignee: Aventis Pharmaceuticals Products Inc.
    Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
  • Patent number: 6077970
    Abstract: The present invention relates to carboxylic acid esters of 2-hydroxy-5-isoalkyl-beta-methylstyrenes wherein the said isoalkyl substituent comprises 8-18 carbon atoms.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: June 20, 2000
    Assignee: Henkel Corporation
    Inventor: Leroy Krbechek
  • Patent number: 6011063
    Abstract: Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: June 3, 1997
    Date of Patent: January 4, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Patent number: 5837873
    Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: November 17, 1998
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Lynn M. Codacovi, Steven J. Wittenberger
  • Patent number: 5798383
    Abstract: The prevent invention provides a compound of formula (I): ##STR1## wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 hydroxyalkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.2-4 alkoxyalkoxy, C.sub.1-4 alkylthio, hydroxy, halo, cyano, amino, C.sub.1-4 alkylamino, di (C.sub.2-8) alkylamino, C.sub.2-6 alkanoylamino, carboxy, C.sub.2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo?b!furyl, thienyl, benzo?b!thienyl, pyridyl or quinolyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halo, C.sub.1-4 alkoxy, optionally-substituted phneyl, phenoxy or phenylthio, X is C.sub.1 -C.sub.4 alkylene, C.sub.2 -C.sub.4 alkenylene, --(CHR.sup.1).sub.m --Q.sup.1 --(CHR.sup.2).sub.n --, --O--(CHR.sup.1).sub.j --Q.sup.2 -- and --(CHR.sup.1)--O--N.dbd. in which the N.dbd. moiety is attached to the cycloalkene ring; and in which Q.sup.1 is O, S, SO, SO.sub.2, NR.
    Type: Grant
    Filed: May 8, 1997
    Date of Patent: August 25, 1998
    Assignee: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai, Rodney W. Stevens
  • Patent number: 5723655
    Abstract: The present invention relates to an amine compound represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 represent individually a linear or branched C.sub.1 -C.sub.24 alkyl or alkenyl group which may be substituted by a hydroxyl group, X.sup.1 represents a C.sub.1 -C.sub.6 alkylene or alkenylene group which may be substituted by a hydroxyl, sulfonic or carboxyl group, Y.sup.1 represents a carboxyl or sulfonic group, or a sulfuric acid residue, Y.sup.2 represents a hydroxyl group, a sulfuric acid residue or a group --OCO--X.sup.1 --COOH, Z represents a sulfoalkyl group or a group obtained by removing an amino group from an amino acid or a salt thereof, and n represents a number of 0 or 1, or a salt or quaternized product thereof, an intermediate useful for the preparation thereof, and detergent compositions containing such an amine compound.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: March 3, 1998
    Assignee: Kao Corporation
    Inventors: Mitsuru Uno, Tomohito Kitsuki, Katsumi Kita
  • Patent number: 5705681
    Abstract: Diquaternary ammonium esters useful as bleach activators are disclosed as are bleach compositions comprising such an ester and peroxygen compound yield peroxide in solution.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: January 6, 1998
    Assignee: Witco Corporation
    Inventors: Philip H. Steiger, Shaun F. Clancy, Owen Portwood
  • Patent number: 5698740
    Abstract: A hole-transport material having excellent hole-transport capability and durability, suitable for use in an organic EL device and as an organic photoconductive material, has the formula (1).
    Type: Grant
    Filed: February 12, 1997
    Date of Patent: December 16, 1997
    Assignee: Toyo Ink Manufacturing Co., Ltd.
    Inventors: Toshio Enokida, Tadashi Ogawa, Yasumasa Suda
  • Patent number: 5662827
    Abstract: Disclosed are bleaching compositions comprising diquaternary ammonium esters which are useful as bleach activators with a peroxygen compound to yield peroxide in solution.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: September 2, 1997
    Assignee: Witco Corporation
    Inventors: Philip H. Steiger, Shaun F. Clancy, Owen Portwood
  • Patent number: 5635571
    Abstract: Polyoxazolines having the structural formula: ##STR1## wherein R is phenylene or alkylene containing 2 to 18 carbon atoms, R.sup.2 is C.sub.1-4 alkyl and R.sub.1 is selected from the group consisting of C.sub.1-12 alkyl, vinyl, isopropylidene, pentafluoroethyl, phenyl, hydroxyphenyl which is optionally interrupted by up to 20 ethylene oxide groups, C.sub.1-2 -alkoxyphenyl which is optionally interrupted by up to 20 ethylene oxide groups and .paren open-st.CH.sub.2 CH.sub.2 --O.paren close-st..sub.r CH.sub.3 in which r ranges from 1-20, X is NH.sub.2 or OH, n ranges from 2 to 50 and m ranges from 0 to 50, wherein R.sub.1 is hydroxyphenyl optionally interrupted by up to 20 ethylene oxide groups only when X is NH.sub.2, are polymerizable to form hyperbranched polymers which have a number average molecular weight ranging from 5,000 to 150,000, a weight average molecular weight ranging from 5,500 to 5,000,000 and a polydispersity ranging from 1.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: June 3, 1997
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Jean M. J. Frechet, Koji Yui
  • Patent number: 5631401
    Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: May 20, 1997
    Assignee: Abbott Laboratories
    Inventors: Herman H. Stein, William R. Baker, Anthony K. L. Fung, Saul H. Rosenberg, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, William J. McClellan, Stephen J. O'Connor, Rajnandan Prasad, Wang Shen, Gerard M. Sullivan
  • Patent number: 5606092
    Abstract: A monoazo compound of the following formula, ##STR1## wherein D is phenylene or naphthylene; X is halogeno, pyridinio or ##STR2## B is --OR.sub.3, --SR.sub.4, ##STR3## in which R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, alkyl, phenyl, naphthyl or benzyl, r is 0 or 1, and E is O, SO, SO.sub.2, CH.sub.2 or NR.sub.8, in which R.sub.8 is hydrogen or C.sub.1 -C.sub.4 alkyl; R, R.sub.1, R.sub.2 and R.sub.7 are each hydrogen or alkyl; A.sub.1, A.sub.2 and A.sub.3 are each phenylene, naphthylene or alkylene; Z.sub.1, Z.sub.2 and Z.sub.3 are each --SO.sub.2 CH.dbd.CH.sub.2 or --SO.sub.2 CH.sub.2 CH.sub.2 Y, in which Y is a splittable group; and p is 0 or 1; which compound is useful for dyeing or printing fiber materials to obtain a product dyed or printed in a color superior in various fastness properties with superior build-up property.
    Type: Grant
    Filed: October 20, 1995
    Date of Patent: February 25, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masayuki Miki, Kingo Akahori, Yutaka Kayane, Takeshi Washimi
  • Patent number: 5457108
    Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: October 10, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
  • Patent number: 5440060
    Abstract: The demands on the properties of pigments, in particular in the areas of emulsion paints and printing inks, which are continuously becoming more specific made it necessary to develop selective and environmentally safe dispersing and emulsifying agents and coupling auxiliaries.The compounds according to the invention are alkoxylation products prepared from fatty amine dialkylenediamines which, if desired, are linked to give recurring structural units by means of esterification with dicarboxylic acids and in which, preferably, the hydroxyl end groups of these fatty amine alkylenediamine alkoxylates have been esterified with fatty acids, aromatic carboxylic acids and/or resin acids and any hydroxyl groups still present have been converted to the corresponding mono-ester-containing anionic radicals by means of dicarboxylic acids and sulfites.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: August 8, 1995
    Assignee: Hoechst AG
    Inventors: Heinz Uhrig, Albert Munkel
  • Patent number: 5405997
    Abstract: Methanesulfonamides are structurally depicted by Formula I' ##STR1## or its pharmacologically acceptable salts where R.sub.3 is a C.sub.1-7 alkyl substituted with C.sub.3-7 cycloalkyl, or a C.sub.1-10 alkyl substituted with one to eight fluorine atoms, one to three hydroxy, one to three C.sub.1-5 acyloxy or one to three C.sub.1-4 alkoxy substituents. These compounds are useful as Class III antiarrhythmic agents and are stable against rapid metabolism. Methods for treating cardiac arrhythmias with the compounds of Formula I' as well as compositions thereof are also described.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: April 11, 1995
    Assignee: The Upjohn Company
    Inventors: Jackson B. Hester, Jr., Salvatore C. Perricone, J. Kenneth Gibson
  • Patent number: 5403850
    Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 --or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H,(2) C1-16 alkyl or (3) the formula ##STR3## wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR4## is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula:--SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H C1-4 alkyl or benzyl; or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: April 4, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Yoshinobu Arai, Tadao Okegawa
  • Patent number: 5399746
    Abstract: Diquaternary ammonium esters useful as bleach activators are disclosed, as are bleach compositions comprising such an ester and a peroxygen compound which yields peroxide in solution.
    Type: Grant
    Filed: February 7, 1994
    Date of Patent: March 21, 1995
    Assignee: Witco Corporation
    Inventors: Philip H. Steiger, Shaun F. Clancy, Owen Portwood
  • Patent number: 5395971
    Abstract: 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: Grant
    Filed: March 11, 1994
    Date of Patent: March 7, 1995
    Assignee: The Board of Regents of The University of Oklahoma
    Inventors: Kenneth M. Nicholas, Anurag S. Srivastava
  • Patent number: 5380941
    Abstract: A process for preparing ureas of the formula ##STR1## where the ring A can be substituted and benzo-fused andn is 0 or 2,R.sup.4 and R.sup.5 are hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,L is unsubstituted or substituted C.sub.2 -C.sub.4 -alkylene, or NR.sup.5 and L are together the radical of the formula ##STR2## and Z is hydroxyl or a radical which can be eliminated under alkaline reaction conditions,by reacting a phenylurea of the formula ##STR3## where R.sup.4 and the ring A each have the abovementioned meanings, with an amine of the formula ##STR4## where n, R.sup.5, L and Z each have the abovementioned meanings, at from 80.degree. to 180.degree. C. in the presence or absence of an inert diluent is described.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: January 10, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Siegel, Manfred Patsch
  • Patent number: 5371278
    Abstract: The use of a minimal excess of acetoxyacetylchloride as a reagent in the synthesis of N,N'-bis(2,3-dihydroxypropyl)-5-N-(2-hydroxy-ethyl)glycolamido-2,4,6-triio doisophthalamide.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: December 6, 1994
    Assignee: Mallinckrodt Medical PMC
    Inventors: William Z. McCarthy, Mills T. Kneller, Youlin Lin, Rebecca A. Wallace, David H. White
  • Patent number: 5359128
    Abstract: The invention comprises compositions and methods for the treatment of psoriasis.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: October 25, 1994
    Inventor: Izhak Blank
  • Patent number: 5354882
    Abstract: The reactive dyes have the formula ##STR1## where n is 0 or 1,R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,R.sup.4 is fluorine, chlorine, bromine, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl or a radical of the formula ##STR2## L is a bridge member, A is substituted or unsubstituted C.sub.2 -C.sub.8 -alkylene,Y is vinyl or a radical of the formula --CH.sub.2 --CH.sub.2 --Q, where Q is a group which is detachable under alkaline reaction conditions, andD is phenyl or naphthyl, which may each be substituted.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: October 11, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Siegel, Manfred Patsch
  • Patent number: 5349109
    Abstract: 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: Grant
    Filed: August 26, 1993
    Date of Patent: September 20, 1994
    Assignee: The Board of Regents of the University of Oklahoma
    Inventors: Kenneth M. Nicholas, Anurag S. Srivastava
  • Patent number: 5334761
    Abstract: The present invention discloses cationic lipids useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Also disclosed are lipids useful both for the delivery of macromolecules and also useful as intermediates for making other such lipids.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: August 2, 1994
    Assignee: Life Technologies, Inc.
    Inventors: Gulilat Gebeyehu, Joel A. Jessee, Valentina C. Ciccarone, Pamela Hawley-Nelson, Anna Chytil
  • Patent number: 5326902
    Abstract: Oxyalkyne compounds corresponding to the formula I ##STR1## in which the substituent Y in the meta- or para-position is R.sup.1 represents CH.sub.3 or NH.sub.2, R.sup.2 represents H or CH.sub.3, R.sup.3 represents H, C.sub.1-3 -alkyl or COCH.sub.3, and Ar represents an aromatic residue selected from the group ##STR2## with the proviso that the substituents R.sup.4, R.sup.5 and R.sup.6 are the same or different and each substituent represents H, F, Cl, Br, C.sub.1-6 -alkyl, CF.sub.3 or C.sub.1-6 -alkoxy, and R.sup.7 represents H, F, Cl, Br, C.sub.1-3 -alkyl or CF.sub.3,in the form of their racemates or mixtures of diastereoisomers or in optically active form, which are suitable active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: March 24, 1993
    Date of Patent: July 5, 1994
    Assignee: Gruenenthal GmbH
    Inventors: Ulrich Seipp, Werner Vollenberg, Werner Englberger, Cornelia Geist, Michael Haurand
  • Patent number: 5326786
    Abstract: Compounds represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent a hydrogen atom or a protective group for a hydroxyl group, or R.sub.1 and R.sub.2 combine to represent a protective group for hydroxyl groups, andR.sub.3 represents CH.sub.3 O-- or CH.sub.3 NH--.These compounds exhibit a strong effect to inhibit proliferation of cancer cells and are expected to be used as a carcinostatic agent.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: July 5, 1994
    Assignee: Ohgen Research Laboratories Ltd.
    Inventor: Kiyoshi Akiyama
  • Patent number: 5306837
    Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: April 26, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5270472
    Abstract: Amides of alkanoyl L-carnitines of general formula (1). ##STR1## wherein R is a straight or branched alkanoyl group having from 2 to 8 carbon atoms selected from acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, hexanoyl, 1-methylbutyryl, t-butylacetyl, 2-ethylbutyryl, 3-methylvaleryl, 4-methylvaleryl, 2-ethylhexanoyl and 2-propylpentanoyl;R' is the monovalent residue of a naturally occurring aminoacid selected from: ##STR2## X.sup.- is the anion of a pharmacologically acceptable acid are active in regenerating the nervous tissue, inhibiting neuronal degeneration, enhancing the processes of learning and memory and for the treatment of coma.Orally or parenterally administrable compositions in unit dosage form comprise between about 50 and about 500 mg of an amide of formula (1).
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: December 14, 1993
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Giulio Taglialatela, Nicola Fanto, Mose Santaniello, Claudio Cavazza
  • Patent number: 5256393
    Abstract: The use of azeotropic distillation to dry 5-amino-N,N'bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide, an intermediate in the production of N,N'-bis(2,3-dihydroxypropyl)-5-N-(2-hydroxyethyl)glycolamido-2,4,6-triiod oisophthalamide.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: October 26, 1993
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: William Z. McCarthy, Mills T. Kneller, Youlin Lin, David H. White
  • Patent number: 5256806
    Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: October 26, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5202464
    Abstract: Inositol compounds grouped into an aminocyclitol family are disclosed which have stereospecific structure and optical activity and find application to the manufacture of medicinal products and agricultural chemicals. The compound is produced with use of optically active L-quebrachitol as a starting material and by way of specific steps of reaction.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: April 13, 1993
    Assignee: The Yokohama Rubber Co., Ltd.
    Inventors: Seiichiro Ogawa, Akihiro Isaka, Kunio Kageyama, Morihisa Machida
  • Patent number: 5182371
    Abstract: The reactive dyes have the formula ##STR1## where n is 0 or 1,R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,R.sup.4 is fluorine, chlorine, bromine, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl or a radical of the formula ##STR2## L is a bridgemember, A is substituted or unsubstituted C.sub.2 -C.sub.8 -alkylene,Y is vinyl or a radical of the formula --CH.sub.2 --CH.sub.2 --Q, where Q is a group which is detachable under alkaline reaction conditions, andD is phenyl or naphthyl, which may each be substituted.The present dyes are useful in dyeing or printing hydroxyl- or nitrogen-containing fibres.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: January 26, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Siegel, Manfred Patsch
  • Patent number: 5175257
    Abstract: Chelating compounds of specified N.sub.2 S.sub.2 N.sub.3 S derived structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable ester orthioester linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
    Type: Grant
    Filed: January 14, 1991
    Date of Patent: December 29, 1992
    Assignee: NeoRx Corporation
    Inventors: Sudhakar Kasina, Ananthachari Srinivasan, John M. Reno, Linda M. Gustavson, Jeffrey N. Fitzner, David S. Jones
  • Patent number: 5155271
    Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## in which Q is substituted or unsubstituted C.sub.1 -C.sub.6 alkyl, A is a direct bond or a bridging member, s is the number 1 or 2, Z is a radical of the formula --CH.sub.2 CH.sub.2 OH, --CH.dbd.CH.sub.2 or --CH.sub.2 CH.sub.2 --Y, and Y is a leaving group, and the benzene or napthalene nucleus I can be further substituted, which comprises reacting compounds of the formula ##STR2## with compounds of the formulaQ--OH (3)in which A, s, Z and Q are as defined under formula (1), in the presence of hydrogenation catalysts, and then carrying out further conversion reactions where appropriate.The compounds obtained by the process according to the invention are suitable as intermediates for the preparation of reactive dyes.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Aeschlimann
  • Patent number: 5152916
    Abstract: Aqueous aldehyde solutions for trapping hydrogen sulfide comprising 5 to 50% by weight of an aldehyde and 1 to 5% by weight, relative to the aldehyde solution of a formulation comprising10 to 80% by weight of an ester of oxalkylated alkylalkylenediamines, which may be quaternized and 20 to 90% by weight of water or of a C.sub.1 -C.sub.4 -alcohol.
    Type: Grant
    Filed: August 21, 1990
    Date of Patent: October 6, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hermann Hoffmann, Frederic Mabire
  • Patent number: 5117057
    Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-disubstitutedhydrazines, methods of using such compositions and N'-substituted-N, N'-disubstitutedhydrazines. Specifically, the invention relates to insect growth regulating compositions, and methods of using such compositions, which include compounds having a nucleus of the formula ##STR1## where A', B', D and J are independently any atom or group of atoms; where E is a tertiary carbon containing organic radical, a haloalkyl having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen, and is attached to the nitrogen shown in the formula by a carbon-to-nitrogen single bond; where one G.sub.1 is C, N, O and S, and both G.sub.2 's and the other G.sub.1 are carbon; or one G.sub.2 is S or P, and both G.sub.1 's and the other G.sub.
    Type: Grant
    Filed: June 14, 1991
    Date of Patent: May 26, 1992
    Assignee: Rohm and Haas Company
    Inventors: Adam C. Hsu, Harold E. Aller, Raymond A. Murphy, Dat P. Le, Donald W. Hamp, Barry Weinstein
  • Patent number: 5112953
    Abstract: Chelating compounds of specified structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
    Type: Grant
    Filed: December 29, 1989
    Date of Patent: May 12, 1992
    Assignee: NeoRx Corporation
    Inventors: Linda M. Gustavson, Ananthachari Srinivasan, Sudhakar Kasina, John M. Reno, Jeffrey N. Fitzner, David S. Jones
  • Patent number: 5095137
    Abstract: The amides of cyclomethylen-1,2-bicarboxylic acids having the formula: ##STR1## wherein A represents ##STR2## R.sup.1 represents --H, --CH.sub.3, --CH.sub.2 --CH.sub.3, --CH(CH.sub.3).sub.2, ##STR3## R.sup.2 represents --H, CH.sub.3, --CH.sub.2 --CH.sub.3, --CH(CH.sub.3).sub.2, --CH.sub.2 --CH.sub.2 --CH.sub.3, --CH.sub.2 --CH(CH.sub.3).sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.3, --CH.sub.2 --C.sub.6 H.sub.5, --C.sub.6 --H.sub.5 ;R.sup.3 represents --H, --CH.sub.3, --C.sub.2 H.sub.5, ##STR4## R.sup.5 represents --H, --CH.sub.3, --C.sub.2 H.sub.5, --CH.sub.2 C.sub.6 H.sub.5, ##STR5## Y=--H, --CH.sub.3, --CH(CH.sub.3).sub.2 Z=--H,--CH.sub.3, --C(CH.sub.3).sub.3, --CH(C.sub.2 H.sub.5).sub.2, ##STR6## R.sup.4 =R.sup.5, ##STR7## m is 0 or 1 and n is an integer varying between 0 and 3, are endowed with ACE-inhibiting activity and are thus therapeutically useful as anti-hypertension agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: March 10, 1992
    Assignee: Laboratori Guidotti SpA
    Inventors: Luigi Turbanti, Guido Cerbai, Marco Criscuoli
  • Patent number: 5072025
    Abstract: 3-substituted-4-hydroxy- and 4-acetoxystyrene compounds, especially 3,5-di(methyl, bromo or chloro)-4-acetoxystyrene as well as a process for its preparation. 2,6-dimethylphenol is acylated with acetic anhydride and HF catalyzed to produce 3,5-dimethyl-4-hydroxy-acetophenone. After subsequent esterification with acetic anhydride and catalyzed hydrogenation to form 1-(3',5'-dimethyl-4'-acetoxyphenyl)ethanol, this intermediate is then dehydrated with an acid and a polymerization inhibitor to produce 3,5-dimethyl-4-acetoxystyrene.
    Type: Grant
    Filed: July 26, 1990
    Date of Patent: December 10, 1991
    Assignee: Hoechst Celanese Corporation
    Inventors: Richard Vicari, Mohammad Aslam, Wilson B. Ray, Kenneth G. Davenport, Ralph Dammel, Juergen Lingnau, Karl-Friedrich Doessel
  • Patent number: 5072042
    Abstract: Phenylhydrazones of formula I ##STR1## in which R.sup.1 to R.sup.6 and m and n have the meanings stated above, and the manufacture thereof. The substances are suitable for combating disease and for cosmetic use.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: December 10, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest, William V. Murray, Michael P. Wachter, Stanley Bell
  • Patent number: 5047421
    Abstract: Compounds are described of the general formula: ##STR1## wherein: R.sub.1 is acyl of the formula --C(.dbd.O)--R.sub.5 ; R.sub.2, R.sub.3, and R.sub.4 are each selected from the group consisting of hydrogen and acyl of the formula:--C(.dbd.O)--R.sub.5wherein R.sub.5 is selected from the group consisting of alkyls, substituted alkyls, alkenyls, substituted alkenyls, cycloalkyls, substituted cycloalkyls, arylalkylenes, substituted arylalkylenes, alkylenecycloalkyls, alkylene substituted cycloalkyls, alkynyls substituted alkynyls, aryls and substituted aryls, wherein R.sub.2, R.sub.3 and R.sub.4 are selected such that at least one of R.sub.2, R.sub.3 and R.sub.4 is an acyl.When R.sub.2, R.sub.3 and R.sub.4 include one or more acyls that are not identical to the acyl of R.sub.1, these compounds of formula I are novel compounds. The invention also includes processes to produce the compounds of formula I.Compounds of formula I complex and/or chelate tissue tri-valent ions, especially iron (Fe.sup.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: September 10, 1991
    Assignee: Oral-D
    Inventor: Donald E. Green
  • Patent number: 5043469
    Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizable aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.
    Type: Grant
    Filed: April 13, 1990
    Date of Patent: August 27, 1991
    Assignee: Eastman Kodak Company
    Inventors: Philip T. S. Lau, Danny R. Thompson
  • Patent number: 5041462
    Abstract: Novel substituted acetamide compounds of the formula ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a lower acyl group, or an aryl group; R.sup.2 is cyano group or aminocarbonyl group; R.sup.3 is a halogen atom, nitro group, a lower alkoxy group, a group of the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 is hydrogen atom, a lower alkyl group or a group of the formula: --COCH.sub.2 OR.sup.1 ; R.sup.5 is hydrogen atom or a lower alkyl group), or a cyclic amino group of the formula: ##STR2## (wherein R.sup.6 and R.sup.7 are each an alkylene group having 1 to 3 carbon atoms, and X is oxygen atom or methylene), or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: August 20, 1991
    Assignee: Toyo Boseki Kabushiki Kaisha
    Inventors: Hiroaki Taguchi, Takeo Katsushima, Masakazu Ban, Mitsuru Takahashi, Kiyotaka Shinoda, Akihiko Watanabe
  • Patent number: 5011992
    Abstract: Novel substituted benzamides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: April 30, 1991
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ivo Monkovic, David Willner
  • Patent number: RE34805
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: December 6, 1994
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon