Additional Polycyclo Heterocyclic Ring System Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/454)
  • Patent number: 6028203
    Abstract: Oxybisphthalic compounds such as 4,4'-oxybis(N-methylphthalimide) and 4,4'-oxybis(phthalic anhydride) are prepared from the corresponding nitro- or halo-substituted phthalic compounds by reaction with an alkanoate or carbonate salt in a non-polar solvent and in the presence of a hexaalkylguanidinium salt as phase transfer catalyst. A carboxylic acid such as 4-chlorobenzoic acid may be used as an additional catalyst. Reaction rates and yields are higher than with other phase transfer catalysts.
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: February 22, 2000
    Assignee: General Electric Company
    Inventors: Daniel Joseph Brunelle, Thomas Link Guggenheim
  • Patent number: 6025494
    Abstract: A compound of formula (I) ##STR1## and salts and solvates thereof, in which: R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl;R.sup.1 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, haloC.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkylC.sub.1-3 alkyl, arylC.sub.1-3 alkyl or heteroarylC.sub.1-3 alkyl;R.sup.2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring ##STR2## attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; andR.sup.3 represents hydrogen or C.sub.1-3 alkyl, or R.sup.1 and R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: February 15, 2000
    Assignee: ICOS Corporation
    Inventor: Alain Claude-Marie Daugan
  • Patent number: 6022307
    Abstract: The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: February 8, 2000
    Assignee: American Cyanamid Company
    Inventors: Mark E. Salvati, Nancy H. Eudy, William A. Hallett, Dennis William Powell
  • Patent number: 6022495
    Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: February 8, 2000
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 6022497
    Abstract: Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted six-membered heterocyclic group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline) type compounds.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: February 8, 2000
    Assignee: PPG Industries Ohio, Inc.
    Inventor: Anil Kumar
  • Patent number: 6017945
    Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: January 25, 2000
    Assignee: Pfizer Inc.
    Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
  • Patent number: 6001867
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms;X is H, or halogen;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, --CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: December 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
  • Patent number: 5965745
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: October 12, 1999
    Assignee: Pfizer Inc
    Inventors: Matthew F. Brown, Anthony Marfat
  • Patent number: 5961892
    Abstract: Described are novel photochromic polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho?1,2-b!pyrans, 3H-naphtho?2,1-b!pyrans and indeno?2,1-f!naphtho?1,2-b!pyrans, each having at least one polyalkoxylated substituent of from 2 to 50 alkoxy units per substituent. Specific substituents may also be present on the naphtho, indeno and pyrano portions of the compounds.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: October 5, 1999
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Barry Van Gemert, Kevin J. Stewart
  • Patent number: 5955520
    Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: September 21, 1999
    Assignee: PPG Industries, Inc.
    Inventors: Harry G. Heller, Julian R. Levell
  • Patent number: 5932725
    Abstract: The present invention relates to a novel chromene compound having favorable photochromic properties, developing a color of a high density, exhibiting a small degree of initial color and permitting the color to quickly fade.
    Type: Grant
    Filed: April 30, 1998
    Date of Patent: August 3, 1999
    Assignee: Tokuyama Corporation
    Inventors: Yuichiro Kawabata, Tsuneyoshi Tanizawa, Tadashi Hara
  • Patent number: 5929106
    Abstract: Dihydroisoindole compounds of formula (I), wherein the substituents are as defined herein, are disclosed as being useful as endothelin receptor antagonists. The compounds are applied in the treatment of cardiovascular and renal diseases.
    Type: Grant
    Filed: October 27, 1997
    Date of Patent: July 27, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Robert Gene Franz, M. Amparo Lago, Aiming Gao
  • Patent number: 5912357
    Abstract: A compound of formula (I): ##STR1## and the pharmaceutically acceptable base salts thereof, wherein: R is CO.sub.2 R.sup.12 where R.sup.12 is H or a biolabile ester-forming group, or R is tetrazol-5-yl, and either (a) R.sup.1 is ##STR2## and R.sup.2 is F, Cl, Br, I, CH.sub.3 or CF.sub.3, or (b) R.sup.1 is C.sub.3 -C.sub.6 alkyl and R.sup.2 is C.sub.2 -C.sub.4 alkyl, useful as steroid 5-.alpha.-reductase inhibitors.
    Type: Grant
    Filed: February 15, 1996
    Date of Patent: June 15, 1999
    Assignee: Pfizer Inc
    Inventors: Julian Blagg, Graham Nigel Maw, David James Rawson
  • Patent number: 5879592
    Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the naphtho- or benzo-portions and/or pyran portions thereof. These compounds may be represented by one of the following graphic formulae: ##STR1## wherein R.sub.1 is an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: March 9, 1999
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5874588
    Abstract: Diketopyrrolopyrroles of formula I ##STR1## are prepared by reacting a diketopyrrolopyrrole of formula II ##STR2## with a) formic acid or b) a compound of formula IIIX'--H (III)or with an alkali metal formate or alkaline earth metal formate together with carbon monoxide in the presence of a catalyst, wherein, in formulae I, II and III, A is a direct bond or a group ##STR3## wherein phenylene is bound to the pyrrolopyrrole, R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 alkylmercapto, --CF.sub.3, --CN or --NO.sub.2, X is X' or OH, X' is --OR.sub.4 or --N(R.sub.5)(R.sub.6), wherein R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl; phenyl or naphthyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, --CN or --NO.sub.2, R.sub.5 and R.sub.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: February 23, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Bernd Lamatsch, Olof Wallquist
  • Patent number: 5849755
    Abstract: 3-amidochromanylsulfonyl(thio)ureas of the formula (I): ##STR1## which are valuable pharmaceutically active compounds for the treatment of disturbances of the cardiovascular system, in particular for the treatment of arrhythmias, for preventing sudden cardiac death or for influencing a reduced contractility of the heart, and processes for their preparation, their use and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Christian Englert, Uwe Gerlach, Dieter Mania, Wolfgang Linz, Heinz Gogelein, Erik Klaus
  • Patent number: 5840745
    Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: November 24, 1998
    Assignee: Pharmacia S. p. A.
    Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
  • Patent number: 5821256
    Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: October 13, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
  • Patent number: 5808094
    Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN,G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --,R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: September 15, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
  • Patent number: 5807883
    Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: September 15, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Masataka Hikota, Toshiro Shikano, Masaaki Nagasaki
  • Patent number: 5795981
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: August 18, 1998
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5789402
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 4, 1998
    Assignee: Eli Lilly Company
    Inventors: James E. Audia, David J. Hibschman, Joseph H. Krushinski, Jr., Thomas E. Mabry, Jeffrey S. Nissen, Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
  • Patent number: 5783116
    Abstract: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: October 16, 1997
    Date of Patent: July 21, 1998
    Assignee: PPG Industries, Inc.
    Inventor: Jibing Lin
  • Patent number: 5767085
    Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 16, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Nils Langeland Johansen, Jesper Lau, Kjeld Madsen, Behrend Friedrich Lundt, Henning Th.o slashed.gersen, Birgit Sehested Hansen, Bernd Peschke
  • Patent number: 5767139
    Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: June 16, 1998
    Assignee: Pfizer, Inc.
    Inventors: Graham Nigel Maw, Julian Blagg, Colin William Greengrass, Paul William Finn
  • Patent number: 5767290
    Abstract: The present invention relates to a process for preparing protected amines or amino acids. The invention furthermore relates to the use of tocopheryl radicals or radicals derived therefrom as protective groups for amines and amino acids, and to compounds obtained in this process as intermediates and to processes for preparing dipeptides and oligopeptides.
    Type: Grant
    Filed: February 26, 1997
    Date of Patent: June 16, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Rosenau, Wolf-Dieter Habicher, Chen-Loung Chen
  • Patent number: 5750691
    Abstract: Transformations of taxol, baccatin III and of 10-deacetyl baccatin III provide access to novel taxol analogs and key intermediates thereto.
    Type: Grant
    Filed: August 7, 1995
    Date of Patent: May 12, 1998
    Assignee: The Scripps Research Institute
    Inventors: K. C. Nicolaou, Philippe G. Nantermet, Rodney K. Guy, Hiroaki Ueno
  • Patent number: 5750724
    Abstract: The compounds of formula I: ##STR1## wherein R.sup.1, R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; or, R.sup.1 is defined as above and R.sup.4 and R.sup.5, taken together, are ortho substituted methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl; n is 3 or 4; or pharmaceutically acceptable salts thereof, are useful in the treatment of depression and related disorders.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: May 12, 1998
    Assignee: American Home Products Corporation
    Inventors: Young H. Kang, Gary P. Stack
  • Patent number: 5744070
    Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are 3H-naphtho?2,1-b!pyrans having an acyl or aroyl oxy-bearing substituent at the number 6 carbon atom and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 7, 8, 9 or 10 carbon atom of the naphthopyran. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.
    Type: Grant
    Filed: December 20, 1995
    Date of Patent: April 28, 1998
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 5719104
    Abstract: Bicyclic imides of formulae (I) and (II) and their agriculturally-suitable salts, are disclosed which are useful for controlling undesirable vegatation, wherein G is O or S; n and m are each independently 0; 1; 2; or 3; provided that m+n is 2 or 3; q is 1 or 2; X is CH.sub.2 ; CH(halogen); CF.sub.2 ; CHOCH.sub.2 F; CHOCF.sub.3 ; CHOCH.sub.2 CF.sub.3 ; O; S(O).sub.0-2 ; NH; N(C.sub.1 -C.sub.4 alkyl); or N(C.sub.1 -C.sub.4 haloalkyl); and R.sup.1. R.sup.2, and Q are as defined in the disclosure. Also disclosed are compositions containing the bicyclic imides of formulae (I) and (II) and a method for controlling growth of undesired vegetation comprising applying to the locus to be protected an effective amount, of the bicyclic imides formulae (I) and (II).
    Type: Grant
    Filed: October 3, 1996
    Date of Patent: February 17, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: John J. Kilama, Karlheinz Drauz, Wonpyo Hong, Matthias Schafer
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5707557
    Abstract: Photochromic compounds with a 3H-naphthopyran structure having at least one pyrene moiety in the 3-position, a method for preparing such compounds, and the use of such compounds for producing photochromic articles from an organic synthetic material.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: January 13, 1998
    Assignee: Optische Werke G. Rodenstock
    Inventors: Manfred Melzig, Herbert Zinner
  • Patent number: 5696137
    Abstract: Azaheterocyclylmethyl-chromans of the formula: ##STR1## in which E represents an azaheterocyclyl group selected from the group consisting of: ##STR2## wherein R.sup.6 represents hydrogen, hydroxyl, halogen or phenyl; andn represents an integer 0-8;and the other substituents are as defined herein;or an optically isomeric form thereof or a salt thereof;are useful to treat anxiety, depression and psychoses.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 9, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean Marie Viktor De Vry, Wolfgang Dompert, Henning Sommermeyer
  • Patent number: 5696146
    Abstract: Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO.sub.2 H or tetrazol-5 yl; R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; and R.sup.2 is C.sub.2 -C.sub.4 alkyl, together with compositions containing, uses of, process for the preparation of, and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: December 9, 1997
    Assignee: Pfizer Inc.
    Inventors: Julian Blagg, Graham Nigel Maw, David James Rawson
  • Patent number: 5693824
    Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN, G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --, R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: December 2, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
  • Patent number: 5691362
    Abstract: Compounds represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein the variables are as defined in the specification; methods of treating asthma, cough, bronchospasm, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: November 25, 1997
    Assignee: Schering-Plough Corporation
    Inventors: Kevin D. McCormick, Andrew T. Lupo, Jr.
  • Patent number: 5691373
    Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: November 25, 1997
    Assignee: Warner-Lambert Company
    Inventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
  • Patent number: 5686481
    Abstract: Indole derivatives of formula (1) wherein the substituents are defined herein are disclosed. The compounds are useful in methods of antagonizing endothelin receptors, treating hypertension, treating renal failure and treating cerebrovascular disease. Pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: November 11, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Jack Dale Leber
  • Patent number: 5684032
    Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: October 5, 1995
    Date of Patent: November 4, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Jack Dale Leber, Scott Kevin Thompson, Stacie Marie Halbert
  • Patent number: 5681836
    Abstract: The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo?b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo?b!furan moiety by a methylene group, which are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 receptor subtype and having a selective affinity for the D.sub.4 subtype over other dopamine receptor subtypes, possess advantageous qualities in terms of their improved aqueous solubility relative to the corresponding free base and, as such, provide for greater ease of formulation and display enhanced pharmacokinetic properties, including oral absorption.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: October 28, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson
  • Patent number: 5670499
    Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 23, 1997
    Assignee: Eli Lilly and Company
    Inventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
  • Patent number: 5670531
    Abstract: Amino acid derivatives having both enkephalinase and ACE inhibiting properties corresponding to the formula: ##STR1##
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 23, 1997
    Assignee: Societe Civile Bioprojet
    Inventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil, Helene Greciet, Lucette Duhamel, Pierre Duhamel, Claude Gros, Jean-Charles Schwartz, Jeanne-Marie Lecomte
  • Patent number: 5665765
    Abstract: New compounds of formula: ##STR1## wherein: A-B, n and Y are as defined in the description,their optical isomers and physiologically tolerable salts thereof with appropriate acids.The products of the invention may be used as medicaments.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: September 9, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
  • Patent number: 5665722
    Abstract: A class of chemical compounds comprising a benzo [b] furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo [b] furan moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 9, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer
  • Patent number: 5665723
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John H. Hutchinson, Wasyl Halczenko
  • Patent number: 5658500
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5658501
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b] pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5656206
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 12, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 5656750
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: Polaroid Corporation
    Inventors: Richard M. Allen, Peter K. Chu
  • Patent number: 5654296
    Abstract: The compound ##STR1## wherein ring A represents a benzene ring;Ar represents an aromatic group;R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group;m represents an integer of 1 to 6;n represents an integer of 2 to 3;- - - - - represents a single bond or a double bond;X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where - - - - - is a single bond or .dbd.N-- where - - - - - is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: August 5, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai