Additional Hetero Ring Containing Patents (Class 546/187)
  • Patent number: 5536847
    Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 16, 1996
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
  • Patent number: 5530009
    Abstract: This invention provides novel compound of the formula ##STR1## which is neurokinin receptor antagonist.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: June 25, 1996
    Assignee: Eli Lilly and Company
    Inventors: Sung Yong S. Cho, James D. Copp, Francis O. Ginah, Guy J. Hansen, Philip A. Hipskind, Bret E. Huff, Michael J. Martinelli, Michael A. Staszak, Roger W. Tharp-Taylor
  • Patent number: 5529998
    Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: July 27, 1995
    Date of Patent: June 25, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
  • Patent number: 5512589
    Abstract: A compound having the formula: ##STR1## wherein Ar, R.sup.4 and R.sup.5 are defined herein have pharmaceutical utility as proteolytic enzyme inhibitors.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: April 30, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Virendra Kumar, Chakrapani Subramanyam, Ranjit C. Desai, Dennis J. Hlasta, Manohar T. Saindane, Malcolm R. Bell, John J. Court, Robert P. Farrell
  • Patent number: 5506227
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Patent number: 5488119
    Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: January 30, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer-Reimann, Walter Fischer
  • Patent number: 5482957
    Abstract: Azole derivatives, process for their preparation, and their useAzole derivatives of the formula (I) ##STR1## in which A, L, O, R.sup.1, X, Y, Z and q have the meanings given, process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have for example the following meanings:R.sup.1 is (C.sub.2 -C.sub.10)-alkyl,Z is nitrogen,X and Y are independently of one another CR.sup.2,L is --CH.sub.2 --,q is zero or 1,A is a biphenyl radical which is substituted for example by R.sup.15,R.sup.2 is halogen or hydrogen,R.sup.15 is SO.sub.2 --NH--CO--OR.sup.6 andR.sup.6 is phenyl,are highly active antagonists of angiotensin II receptors.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: January 9, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Adalbert Wagner, Heinrich Englert, Heinz-Werner Kleemann, Hermann Gerhards, Bernward Scholkens, Reinhard Becker, Wolfgang Linz, Jean-Paul Vevert, John-Claude Caille
  • Patent number: 5478845
    Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: December 26, 1995
    Assignee: Novo Nordisk A/S
    Inventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
  • 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: 5468855
    Abstract: The invention relates to bislactone color formers having improved fastness to sublimation and migration stability, to their preparation, to pressure-sensitive and heat-sensitive recording materials containing said compounds and to their preparation. The novel bislactones have the formula (1) as defined in claim 1.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: November 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Rudolf Zink
  • Patent number: 5457204
    Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms; and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CO--N(R.sup.3)-- or --N(R.sup.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: October 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5457207
    Abstract: The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "spirovesamicols" which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: October 10, 1995
    Assignee: Regents of the University of Minnesota
    Inventors: Simon M. N. Efange, Stanley M. Parsons
  • Patent number: 5439958
    Abstract: The present invention relates to novel piperidine compounds of the formula (I) and to their use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.The definitions of R.sub.1, R.sub.2 and R.sub.3 are given in the text.
    Type: Grant
    Filed: July 21, 1994
    Date of Patent: August 8, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Roberto Scrima, Graziano Zagnoni, Michael H. Ackerman, James P. Galbo, Roland A. E. Winter
  • Patent number: 5436262
    Abstract: Derivatives of 2-(benzimidazol-2-yl)-1,3-diaminopropane, the process for their preparation as well as the pharmaceutical compositions containing them as active ingredients are described. The compounds exhibit anti-allergic activity.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: July 25, 1995
    Assignee: Dompe Farmaceutici SpA
    Inventors: Marco Mantovanini, Roberto Curti
  • Patent number: 5428041
    Abstract: Provided are bis-trifluoromethyl-substituted imidazolines as inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and therapeutic methods for their use as antihypercholesterolemic or antiatherosclerotic agents.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: June 27, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Jeffrey T. Billheimer, George A. Boswell, Jr., Indawati De Lucca, Spencer Drummond, Jr., Peter J. Gillies, James M. Trzaskos
  • Patent number: 5424404
    Abstract: Biscationic azo dyes useful for dyeing or printing polymeric material have the formula ##STR1## where R.sup.1 is hydrogen or unsubstituted or phenyl-substituted C.sub.1 -C.sub.5 -alkyl,R.sup.2 is hydrogen or C.sub.1 -C.sub.5 -alkyl,R.sup.3 and R.sup.4 are independently of each other hydrogen or methyl,D is the radical of a diazo component, unsubstituted or substituted phenylene or a radical of the formula ##STR2## where Z is a bridge member, Y is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.2 -C.sub.6 -alkylene, xylidene or phenylene,An.sup..crclbar.
    Type: Grant
    Filed: June 11, 1993
    Date of Patent: June 13, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Manfred Ruske, Udo Mayer
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5414010
    Abstract: Dimeric benzimidazoles are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic agents and for the treatment of disorders which respond to dopaminergic blockade including psychotic depression, substance abuse, and compulsive disorders.
    Type: Grant
    Filed: May 10, 1994
    Date of Patent: May 9, 1995
    Assignee: Warner-Lambert Company
    Inventors: Dennis M. Downing, Lawrence D. Wise, Jonathan L. Wright
  • Patent number: 5405845
    Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: April 11, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5395948
    Abstract: The invention relates to fluoran colour formers having improved fastness to sublimation and migration stability, to their preparation, to pressure-sensitive and heat-sensitive recording materials containing said compounds and to their preparation. The fluorans have the formula (I) as defined in claim 1.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: March 7, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Rudolf Zink
  • Patent number: 5393890
    Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.
    Type: Grant
    Filed: July 1, 1994
    Date of Patent: February 28, 1995
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masataka Syoji, Kozo Toyota, Chikahiko Eguchi, Ryoto Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
  • Patent number: 5387687
    Abstract: The present invention relates to novel tetramethylpiperidine compounds of the general formula (I) ##STR1## in which X and Y are e.g. a group of the formula (IIa) or (IIb) ##STR2## in which R.sub.1 and R.sub.2 are e.g. hydrogen or methyl. The said compounds are effective stabilizers for organic materials, in particular synthetic polymers, against the action of light, heat and oxidation.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: February 7, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Roberto Scrima, Graziano Zagnoni
  • Patent number: 5374724
    Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 20, 1994
    Assignee: Zeneca, Limited
    Inventors: Nigel Hall, Nigel Hughes, Prakash Patel
  • Patent number: 5369108
    Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.
    Type: Grant
    Filed: October 4, 1991
    Date of Patent: November 29, 1994
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
  • Patent number: 5356907
    Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: October 18, 1994
    Assignee: Roussel UCLAF
    Inventors: Francois Clemence, Michel Fortin, Odile Le Martret
  • Patent number: 5350744
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: September 27, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel
  • Patent number: 5346908
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: September 13, 1994
    Assignees: National Institutes of Health, Brown University
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5340822
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: August 23, 1994
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
  • Patent number: 5338853
    Abstract: N-(2,2,6,6-tetraalkyl-4-piperidinyl)amic acid hydrazides contain a light stabilizing group, a heat stabilizing group and an amic acid hydrazide functionality in the same molecule. The amic acid hydrazide functionality in the compounds enhances the photooxidative stabilizing properties of the hindered amine groups and contributes thermal and oxidative stabilizing and metal complexing properties to the compounds. The novel compounds are excellent light stabilizers for polyolefins, have low volatility and are not readily lost from polymeric systems via volatilization, migration or extraction.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: August 16, 1994
    Assignee: Elf Atochem North America, Inc.
    Inventors: Ronald E. MacLeay, Harold C. Lange
  • Patent number: 5338739
    Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.
    Type: Grant
    Filed: March 10, 1994
    Date of Patent: August 16, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5326771
    Abstract: Piperidylmethyl-substituted chroman derivatives can be prepared by first reducing corresponding chromancarboxylic acid derivatives, if appropriate with prior activation, with the cyclic amines and then reducing the carbonyl group, or by reacting chromanmethyl compounds directly with the cyclic amines. The substituted piperidylmethyl-substituted chroman derivatives can be employed as active compounds in medicaments, in particular for the treatment of diseases of the central-nervous system.
    Type: Grant
    Filed: November 30, 1992
    Date of Patent: July 5, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Georg Heine, Bodo Junge, Peter-Rudolf Seidel, Rudolf Schohe-Loop, Thomas Glaser, Jean M. V. De Vry, Wolfgang Dompert, Henning Sommermeyer
  • Patent number: 5310767
    Abstract: The present invention relates to novel tetramethylpiperidine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 and R.sub.3 are e.g. --(CH.sub.2).sub.2 --, R.sub.4 is e.g. --CO--, --COCO-- or --COCH.sub.2 CO--, n is e.g. 1 and R.sub.5 is e.g. hydrogen or allyl.These compounds are suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: May 10, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Valerio Borzatta, Graziano Vignali
  • Patent number: 5306720
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: April 26, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5306495
    Abstract: Compounds containing substituted piperidine groups, of the general formula (I) ##STR1## in which n is e.g. 1, 2 or 3, R.sub.1 is e.g. hydrogen or methyl, R.sub.2 is e.g. ethylene or trimethylene and if n is 1, A is e.g. hydrogen, --COOC.sub.18 H.sub.37 --n or --COC.sub.11 H.sub.23 --n, if n is 2, A is e.g. ##STR2## and if n is 3, A is e.g. ##STR3## are effective stabilizers for organic materials, especially synthetic polymers, which are subject to the action of light, heat and oxidation.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: April 26, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Graziano Vignali
  • Patent number: 5304548
    Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: April 19, 1994
    Assignee: The Upjohn Company
    Inventors: Ronald B. Gammill, Frank P. Bell
  • Patent number: 5294719
    Abstract: Compounds useful as a stabilizer for a variety of organic materials of an intermediate thereof, or as an intermediate of medicines or agricultural chemicals are disclosed, which are cyclohexylamine derivatives represented by the general formula [I]: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an acyl group having 2 to 7 carbon atoms or an arylalkyl group having 7 to 10 carbon atoms; R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.3 and R.sup.4 both represent a hydrogen atom, or one of R.sup.3 and R.sup.4 represents a hydrogen atom and the other represents a group --CH.sub.2 --R.sup.5, or R.sup.3 and R.sup.4 together form a group .dbd.CH--R.sup.5, in which R.sup.5 represents an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted phenyl group, a 2-furyl group, a cyclohexyl group or a 2-tetrahydrofuryl group; X represents an alkylene group having 1 to 3 carbon atoms; and n denotes 1 or 2.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: March 15, 1994
    Assignee: Mitsubishi Petrochemical Company Limited
    Inventors: Hideki Kurokawa, Mitsumasa Kaitoh, Akiyoshi Ohnishi
  • Patent number: 5290790
    Abstract: The compounds correspond to the general formula ##STR1## in which R.sub.1 represents a hydrogen atom or a group --COR.sub.2, in which R.sub.2 represents a benzene ring, cyclopentylmethyl, cyclohexylmethyl, cyclopentylethyl or cyclohexylethyl groups or cyclopentylamine, cyclohexylamine or phenylamine, chlorophenylamine or dichlorophenylamine groups; R represents a hydrogen atom or a group COR.sub.3, in which R.sub.3 represents an aliphatic group, a cyclane or benzene ring-system, a group a group (CH.sub.2).sup.m R.sub.4, a group --CH.dbd.CHR.sub.8 or a secondary amine group --NH(CH.sub.2).sub.n R.sub.
    Type: Grant
    Filed: December 30, 1991
    Date of Patent: March 1, 1994
    Assignees: National De La Sante et De La Recherche Medicale, Societe Civile Bioprojet, Universite De Caen - Esplanade De La Faix
    Inventors: Jean-Michel Arrang, Monigue Garborg, Jean-Charles M. Lancelot, Jeanne-Marie Lecomte, Max-Fernand Robba, Jean-Charles Schwartz
  • Patent number: 5286702
    Abstract: The present invention provides a novel phthalide compound represented by the following formula, which rapidly forms blue-blue black color with a developer when it is used as a recording material and, since a color image formed therewith has an intense absorption at 700.about.50 nm, it is usable for optical character reader; ##STR1## where R.sup.1 and R.sup.2 represent, independently, alkyl group having 6 or less carbon atoms; cycloalkyl group having 5 or 6 carbon atoms; aryl group; or heterocyclic ring connecting R.sup.1, R.sup.2 and N, R.sup.3 and R.sup.4 represent, independently, alkyl group having 6 or less carbon atoms; cycloalkyl group having 5 or 6 carbon atoms; aryl group; a heterocyclic ring connecting R.sup.3, R.sup.4 and N, X.sup.1 .about.X.sup.3 represent, independently, hydrogen atom, alkyl group having 6 or less carbon atoms, alkoxy group having 6 or less carbon atom or halogen atom, X.sup.
    Type: Grant
    Filed: April 24, 1992
    Date of Patent: February 15, 1994
    Assignee: Yamada Chemical Co., Ltd.
    Inventors: Yutaka Muraki, Hidekazu Ishida, Hajime Kawai, Katsuhiko Tsunemitsu
  • Patent number: 5281585
    Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
  • Patent number: 5258401
    Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: November 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick
  • Patent number: 5258383
    Abstract: DC-89 derivatives represented by the formula: ##STR1## wherein X represents hydrogen or CO.sub.2 CH.sub.3 ; and ##STR2## wherein Z represents Cl or Br; R represents hydrogen, CONR.sup.1 R.sup.2 (in which R.sup.1 and R.sup.2 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl) or ##STR3## (in which n represents an integer of 0 to 4; R.sup.3 represents CH.sub.2, ##STR4## oxygen, N--CH.sub.3, or N--CH.sub.2 CONR.sup.1 R.sup.2 in which R.sup.1 and R.sup.2 have the same significances as defined above); and W represents hydrogen or ##STR5## (in which W.sup.1 and W.sup.2 independently represent hydrogen or OR.sup.2 in which R.sup.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: November 2, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Katsushige Gomi
  • Patent number: 5256787
    Abstract: The compounds of formula VIIIa-1 ##STR1## where R.sub.1 is hydrogen, alkyl, O.sup.., OH, NO, CH.sub.2 CN, alkoxy, cycloalkoxy, alkenyl, phenylalkyl, alkanoyl, alkenoyl or benzoyl, are valuable intermediates for the preparation of selected hindered amine light stabilizers.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: October 26, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Valerio Borzatta, Roberto Scrima, Graziano Vignali
  • Patent number: 5250542
    Abstract: 3,4,4-trisubstitutedpiperidinyl-N-alkylcarboxylates and intermediates for their preparation are provided. These piperidine-N-alkylcarboxylates are useful as peripheral opioid antagonists.
    Type: Grant
    Filed: July 17, 1992
    Date of Patent: October 5, 1993
    Assignee: Eli Lilly and Company
    Inventors: Buddy E. Cantrell, Dennis M. Zimmerman
  • Patent number: 5248686
    Abstract: The invention relates to substituted arylamines and heteroarylamines, their preparation process and the pharmaceutical composition containing them. Said substituted amine is in accordance with the formula: ##STR1## in which R.sup.1 and R.sup.2 are optionally substituted alkyl radicals or form with N an optionally substituted piperazine or piperidine cycle, R.sup.3 and R.sup.4 represent a hydrogen atom or an organic radical, Y represents CR.sup.6 or N and R.sup.5 is an optionally substituted benzothiophenyl, benzofuranyl or naphthyl radical.These amines can be used in pharmaceutical compositions for the treatment of nervous depression or for stimulating vigilance.
    Type: Grant
    Filed: May 12, 1992
    Date of Patent: September 28, 1993
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Marc Kamenka, Alain Privat, Robert Chicheportiche, Jean Costentin
  • Patent number: 5245030
    Abstract: An IR-ray absorptive compound represented by the formula (1) or (2): ##STR1## and an optical recording medium having a substrate and an organic dye thin film, comprising the formulae (1) and/or (2).
    Type: Grant
    Filed: January 31, 1992
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
  • Patent number: 5241067
    Abstract: Hindered amine light stabilizers are provided in which the hindered amine is contained in a unit of formula ##STR1## and R.sup.1, R.sup.2, R.sup.3, and A are as defined as in the Summary of the Invention. Unique polymeric and non-polymeric compounds containing this unit are useful as additives for the stabilization of polymeric compositions which are normally subject to thermal, oxidative or actinic light degradation.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: August 31, 1993
    Assignee: Elf Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5239076
    Abstract: The invention relates to the novel compound 3,9-bis(1,2,2,6,6-pentamethyl-4-piperidyloxy)-2,4,8,10-tetraoxa-3,9-diphos phaspiro[5,5]undecane of formula I ##STR1## This compound can be used as stabilizer for organic material, especially as processing stabilizer for polyethylene and polypropylene.
    Type: Grant
    Filed: August 10, 1992
    Date of Patent: August 24, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans R. Meier, Peter Hofmann
  • Patent number: 5237067
    Abstract: This application is directed to optoelectronic materials which are bistable organic tautomeric compositions of dithio or diseleno carbamate esters of cyclic 1,3-dithia or -diselena-2-iminium salts. Specifically, it is concerned with compounds having the formula: ##STR1## Wherein X is S or Se; wherein R or R.sub.1 are alkyl, or alkyl that together form a ring of carbon atoms; wherein An is the anion of a strong acid. These molecules are in themselves molecular-sized optoelectric switching devices.
    Type: Grant
    Filed: February 4, 1992
    Date of Patent: August 17, 1993
    Inventor: Robert R. Schumaker
  • Patent number: 5235056
    Abstract: 1-Hydroxy-2,6-diaryl-4-piperidone ketal derivatives, such as the compound of formula I ##STR1## wherein Ar.sub.1 and Ar.sub.2 are each phenyl, R.sub.1 to R.sub.6 are all hydrogen, X.sub.1 and X.sub.2 are each --O-- and T is a direct bond, are novel compounds and are effective process stabilizers, such as polypropylene, for polymers processed at elevated tempertures providing both good melt flow stabilization and good resistance against discoloration during said processing.
    Type: Grant
    Filed: April 22, 1992
    Date of Patent: August 10, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Glen T. Cunkle, Donald J. Sabrsula
  • Patent number: 5230826
    Abstract: Compounds of the formula ##STR1## wherein X.sup.1 denotes fluorine or chlorine and X.sup.2 denotes hydrogen, fluorine or chlorine; R.sup.1 is 3E-alkenyl, 4-alkenyl, 2E-alkenyloxy or 3-alkenyloxy; n stands for the number 0 or 1; one of the groups Y.sup.1 and Y.sup.2 is a single covalent bond, --COO--, --OOC--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O-- or --OCH.sub.2 -- and the other of the groups Y.sup.1 and Y.sup.2 is a single covalent bond; and rings A.sup.1 and A.sup.2 each individually are substituted or unsubstituted trans-1,4-cyclohexylene, in which optionally 2 non-adjacent CH.sub.2 groups are replaced by oxygen, or substituted or unsubstituted 1,4-phenylene, in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; with the proviso that X.sup.2 denotes fluorine or chlorine and/or Y.sup.1 or Y.sup.2 denotes --CH.sub.2 O-- or --OCH.sub.2 -- when simultaneously X.sup.1 is fluorine and R.sup.1 is 3E-alkenyl,and their use for liquid crystalline mixtures and electro-optical purposes.
    Type: Grant
    Filed: October 26, 1988
    Date of Patent: July 27, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Richard Buchecker, Martin Schadt, Alois Villiger