Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 549/50)
  • Patent number: 6340759
    Abstract: The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2 represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; and B represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: January 22, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Kohshi Ueno, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Noritaka Kitazawa, Keiko Takahashi, Noboru Yamamoto, Yuichi Suzuki, Manabu Matsunaga, Atsuhiko Kubota
  • Publication number: 20020002287
    Abstract: A process for the preparation of 3,4-alkylenedioxythiophene-2,5-dicarboxylic acid derivatives of the general formulae IV and V 1
    Type: Application
    Filed: June 8, 2001
    Publication date: January 3, 2002
    Inventor: Friedrich Jonas
  • Publication number: 20010034453
    Abstract: A process for the preparation of dialkoxythiophenes and alkylene-dioxythiophenes in high purity and very good yields by decarboxylation of dialkoxythiophene-dicarboxylic acids or alkylenedioxythiophenedicarboxylic acids, respectively, in solvents that have a higher boiling point than the product and contain no nitrogen bases.
    Type: Application
    Filed: March 21, 2001
    Publication date: October 25, 2001
    Inventors: Gunter Rauchschwalbe, Friedrich Jonas
  • Patent number: 6245255
    Abstract: A dispersion comprises a solvent having dispersed therein a liquid-crystal forming dye of structural Formula I, II or III: wherein the substituent are as defined in the specification. The dispersion is particularly useful in imaging and photographic elements.
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: June 12, 2001
    Assignee: Eastman Kodak Company
    Inventors: Margaret J. Helber, William J. Harrison, Kevin W. Williams, Steven W. Kortum
  • Patent number: 6184221
    Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: February 6, 2001
    Assignee: Hoechst Marion Roussel Deutschland GmbH
    Inventors: Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
  • Patent number: 6153645
    Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.
    Type: Grant
    Filed: September 10, 1999
    Date of Patent: November 28, 2000
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: John Finn, Xiang Yang Yu, Zhongguo Wang, Jason Hill, Dennis Keith, Paul Gallant, Philip Wendler
  • Patent number: 6147110
    Abstract: Compound of formula (I): ##STR1## wherein: B represents optionally substituted (C.sub.1 -C.sub.6)-alkylene,W represents oxygen or sulphur,R represents hydrogen, hydroxy, R', or OR', R' being as defined in the description,G.sub.1 and G.sub.11 are as defined in the description,G.sub.2 represents a group selected from: ##STR2## wherein R.sub.20, R.sub.21, and R.sub.2 are as defined in the description, and medicinal products containing the same which are useful as melatoninergic ligands.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: November 14, 2000
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Nicolas Ruiz, Valerie Wallez, Sophie Boye, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6133305
    Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: October 17, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6130339
    Abstract: Provided are novel, electropolymerizable monomers of the formulae: ##STR1##
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: October 10, 2000
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Devdatt S. Nagvekar, Balasubramanian Sankaran
  • Patent number: 6051722
    Abstract: The present invention provides, as heteroaromatic compounds made functional so as to be used for nonlinear optical materials, compounds represented by the following general formula (1), and also provides polymers obtained from these and nonlinear optical parts comprising such polymers. In the formula, Ar.sup.1 and Ar.sup.2 each represents a divalent aromatic group; R.sup.1, R.sup.2 and R.sup.3 each represents an atom or a group independently selected from a hydrogen atom or an alkyl group and an aromatic group; X.sup.1 represents a monovalent organic group; n represents an integer of 2 to 12; and Z.sup.1 and Z.sup.2 each represents a group independently selected from electron attractive functional groups.
    Type: Grant
    Filed: July 6, 1998
    Date of Patent: April 18, 2000
    Assignee: Hitachi Chemical Company, Ltd.
    Inventors: Yutaka Honda, Iwao Fukuchi, Kwan-Yue Alex Jen
  • Patent number: 6037340
    Abstract: Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: March 14, 2000
    Assignee: Cadus Pharmaceutical Corporation
    Inventors: Arlindo L. Castelhano, Bryan McKibben
  • Patent number: 5998408
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5824677
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5767141
    Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: June 16, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
  • 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: 5684165
    Abstract: Compounds of the formula I ##STR1## in which R is a C.sub.1 - to C.sub.22 -alkyl radical,A.sup.1 and A.sup.2 are hydrogen or methyl or,A.sup.1 is hydrogen and A.sup.2 is the nitro group, andB is the cyano group, the nitro group or an electron-attracting organic group having a double bond which is in conjugation with the thieno?3,2-b!thiophene ring system,have a high dipole moment and a high polarizability and are suitable for purposes of nonlinear optics. If R in the formula I is a C.sub.12 - to C.sub.22 -alkyl radical, monomolecular layers can be applied to a substrate by the Langmuir-Blodgett method. The resulting layer elements are suitable, inter alia, as waveguides.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: November 4, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
  • Patent number: 5521213
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: August 29, 1994
    Date of Patent: May 28, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
  • Patent number: 5464834
    Abstract: New N-substituted N'-heterobicyclic piperazines corresponding to the general formula I: ##STR1## wherein: R represents: ##STR2## D represents a single bond, except when R represents naphthyl, or a hydrocarbon chain having 1 to 8 carbon atoms inclusive which is straight-chain or branched by a gem-dimethyl; andA-B represents: --(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.3 --O--, or --CO--CH.dbd.CH--,as well as their possible stereoisomers, epimers, and pharmaceutically-acceptable acid addition salts thereof; and medicinal products containing the same, useful in the treatment of a disorder requiring a 5-HT.sub.1A receptor antagonist.
    Type: Grant
    Filed: June 11, 1993
    Date of Patent: November 7, 1995
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Jean-Michel Rivet
  • Patent number: 5463056
    Abstract: Thiophene derivatives of formula (I) ##STR1## wherein X and Y are the same or different O, S or N--R.sup.3,Z is a C.sub.1 -C.sub.6 -alkylene residue that may be substituted by R.sup.1 and R.sup.2,R.sup.1, R.sup.2 are the same or different hydrogen, or --(CH.sub.2).sub.n --OR.sup.4, --CH.dbd.CH.sub.2 or ##STR2## n is 1 to 10, R.sup.3 is aryl, C.sub.1-18 -alkyl or H,R.sup.4 is SO.sub.3.sup.- (H.sup.+,Na.sup.+,K.sup.+,Li.sup.+) or --(CH.sub.2 --CH.sub.2 --O).sub.m --R.sup.5,m is 1 to 10 andR.sup.5 is alkyl with 1 to 6 C atoms,wherein compounds in which X and Y are both O and R.sup.1 and R.sup.2 are both hydrogen atoms are excluded, are suitable for the preparation of polythiophenes which can be used as organic electrical conductors.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: October 31, 1995
    Assignee: Agta-Gevaerf AG
    Inventor: Friedrich Jonas
  • Patent number: 5457212
    Abstract: A process for the preparation of enantiomerically pure thienopyran derivatives of the formula ##STR1## is described. The thienopyran derivatives are relaxants of smooth muscle tone and as such are useful in vascular tissue for the treatment of hypertension disease, angina and other vascular disorders characterized by poor regional perfusion.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: October 10, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline J. Sanfilippo, Maud Urbanski
  • Patent number: 5432286
    Abstract: Substituted thieno[3,2-b]thiophenes, processes for their preparation and their useCompounds of the formula I ##STR1## in which R is a C.sub.1 - to C.sub.22 -alkyl radical,A.sup.1 and A.sup.2 are hydrogen or methyl orA.sup.1 is hydrogen and A.sup.2 is the nitro group, andB is the cyano group, the nitro group or an electron-attracting organic group having a double bond which is in conjugation with the thieno[3,2-b]thiophene ring system,have a high dipole moment and a high polarizability and are suitable for purposes of nonlinear optics. If R in the formula I is a C.sub.12 - to C.sub.22 -alkyl radical, monomolecular layers can be applied to a substrate by the Langmuir-Blodgett method. The resulting layer elements are suitable, inter alia, as waveguides.
    Type: Grant
    Filed: October 7, 1993
    Date of Patent: July 11, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
  • Patent number: 5393729
    Abstract: The invention relates to 3-aryl-pyrone derivatives of the general formula (I) ##STR1## in which the substituents are as defined in the specification. The compounds are useful as pesticides, herbicides and fungicides.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: February 28, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Andreas Krebs, Folker Lieb, Michael Ruther, Jorg Stetter, Christoph Erdelen, Ulrike Wachendorff-Neumann, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5380748
    Abstract: A trialkylamine derivative represented by the formula (1) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents lower alkyl;R.sup.3, R.sup.4 and R.sup.5 may be the same or different from one another and each represents hydrogen, lower alkyl, lower alkoxy, lower alkoxycarbonyl or halogen;R.sup.6 and R.sup.7 may be the same or different from each other and each represents hydrogen or lower alkyl;R.sup.8 represents hydrogen, lower alkyl, lower alkoxy or halogen;X represents oxygen, sulfur, --CH.dbd.N-- or --CH.dbd.CH--;Y represents oxygen, sulfur, methylene, N--R.sup.11 (wherein R.sup.11 represents lower alkyl), SO or SO.sub.2 ;Z represents --OCO(CH.sub.2).sub.p .about. or --OCH.sub.2 (CH.sub.2).sub.p .about. (wherein p represents a number of 0 to 4 and symbol .about.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: January 10, 1995
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Yoshiaki Muto, Hiromi Ichikawa, Kuniyoshi Ogura, Kyoji Chaki, Masao Seiki, Toshihiko Takemasa
  • Patent number: 5378713
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 3, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5304657
    Abstract: A hydrazine compound of the formula (I) or its salt: ##STR1## wherein A is a benzofuranyl group which may be substituted, a quinolinyl group which may be substituted, a benzothienyl group which may be substituted, a benzothiazolyl group which may be substituted, a thienothienyl group which may be substituted, a dihydrothienothienyl group which may be substituted, a dihydrocyclopentathienyl group which may substituted, a tetrahydrobenzothienyl group which may be substituted, an indanyl group which may be substituted, or a hexahydroindanyl group which may be substituted, W is a hydrogen atom, a cyano group, --COCOOR', --S--N(R")COOR' or --CH.sub.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: April 19, 1994
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Tadaaki Toki, Toru Koyanagi, Kiyomitsu Yoshida, Kazuhiro Yamamoto, Masayuki Morita
  • Patent number: 5286881
    Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 15, 1994
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
  • Patent number: 5284857
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: February 8, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5260453
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: November 9, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffrey B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5201936
    Abstract: Novel substituted thieno[3,2-b]pyran-5,7-diones of the general formula (I) ##STR1## Processes for their preparation and their use as herbicides and as plant growth regulators and novel intermediates of the formula (VI) ##STR2## (in which R.sup.1, R.sup.2, X, Y and Z have the meaning given in the description).
    Type: Grant
    Filed: October 15, 1991
    Date of Patent: April 13, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Jurgen Bertram, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt, Andrew Plant, Bernd-Wieland Kruger, Achim Harder, Norbert Mencke
  • Patent number: 5183818
    Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: February 2, 1993
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
  • Patent number: 5102905
    Abstract: The invention concerns heterocyclic nitromethane derivatives of the formula 1 as defined hereinafter (and their non-toxic salts) wherein the heterocyclic moiety Q is thienyl, benzothienyl or dibenzothienyl and may bear a wide variety of optional substituents, together with pharmaceutical compositions containing them. The nitromethane derivatives are inhibitors of the enzyme aldose reductase and are of value in the treatment of certain complications of diabetes and galactosemia.
    Type: Grant
    Filed: April 28, 1989
    Date of Patent: April 7, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey Morris, John Preston
  • Patent number: 5095032
    Abstract: Parasiticidal new substituted thienopyranones of the formula ##STR1## in which X represents O or S,R.sup.1 and R.sup.2 independently of one another represent hydrogen, halogen, CN, NO.sub.2, alkyl, aralkyl, aryl, alkylcarbonyl or alkoxycarbonyl, or, together with the adjacent C atoms, form a carbocyclic ring which is optionally interrupted by heteroatoms,R.sup.3 represents optionally substituted alkyl or phenyl,R.sup.4 represents hydrogen or alkyl,R.sup.3 and R.sup.4, together with the adjacent nitrogen atom, represent a heterocyclic 5- or 6-membered ring.Some of the intermediates for making them are also new.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Jurgen Bertram, Nikolaus Muller, Achim Harder
  • Patent number: 5030736
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: July 9, 1991
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 4996142
    Abstract: The invention relates to an adduct of a basic macromoleculer and biotin having the general formula: ##STR1## in which MM is the residue of a basic macromolecule formed by substituting the H-atom of one or more primary amino groups;alk represents an optionally substituted alkylene group having from 1 to 10 C-atoms;m is 0 or 1; andn is a positive integer,with the proviso that, where MM represents cytochrome C or histone, m is not 0.The adduct is useful in constructing non-radioactive nucleic acid hydridization probes.
    Type: Grant
    Filed: September 4, 1987
    Date of Patent: February 26, 1991
    Assignee: Agricultural Genetics Company Limited
    Inventors: Ali H. Al-Hakim, Roger Hull
  • Patent number: 4992435
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: September 23, 1988
    Date of Patent: February 12, 1991
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 4990647
    Abstract: Unsymmetric biaryl compounds are prepared by coupling two different halogenoaromatics by reaction with a metal and carrying out the reaction in the presence of catalytic amounts of a nickel compound, a promoter and a phosphorus-containing ligand.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: February 5, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Himmler, Rudolf Braden
  • Patent number: 4975451
    Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; and Ar.sup.1 is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 2-methyl[1-1'-biphenyl]-3-yl, or 6-phenoxy-2-pyridyl, exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively nontoxic to fish.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: December 4, 1990
    Assignee: FMC Corporation
    Inventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel, Leslie W. Stratton, Alan W. Fritz
  • Patent number: 4970309
    Abstract: This invention relates to a novel method of synthesizing di- and triarylmethane dye precursor compounds possessing a thiolactone ring-closing moiety, from the corresponding lactones.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: November 13, 1990
    Assignee: Polaroid Corporation
    Inventor: Patrick F. King
  • Patent number: 4929549
    Abstract: Novel 5-carbamoylthieno[2,3-b]thiophene-2-sulfonamides and derivatives thereof are prepared in reactions of 5-methoxycarbonylthieno-[2,3-b]thiophene-2-sulfonamide with alkylamines, alkoxyalkylamines and hydroxyalkylamines. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: February 8, 1989
    Date of Patent: May 29, 1990
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4923882
    Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.
    Type: Grant
    Filed: October 16, 1986
    Date of Patent: May 8, 1990
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanag, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
  • Patent number: 4894390
    Abstract: Aromatic sulfonamides useful in the treatment of elevated intraocular pressure having the structural formula: ##STR1## wherein A, R, R.sup.1, and R.sup.2 are as hereinafter defined, as well as the pharmaceutically and ophthalmologically acceptable salts thereof.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4876271
    Abstract: Novel substituted thieno[3,2-b]thiophene-2-sulfonamides are prepared by novel synthetic processes. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4863922
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: September 5, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Patent number: 4835272
    Abstract: A process for formation of a base, which comprises reacting an acetylide compound with a salt. The acetylide compound has the following formula:(R--C.tbd.C--).sub.n Mwherein R is a monovalent group selected from the group consisting of an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group and a heterocyclic group, each of which may have one or more substituent groups; M is an n-valent transition metal atom; and n is 1, 2 or 3. The salt is composed of an anion having an affinity for the transition metal (M) (the affinity of the anion for the transition metal is more than that of the acetylide anion (R--C.tbd.C.crclbar.)), and a cation derived from one selected from the group consisting of an alkali metal, an alkaline earth metal, ammonia and an organic base. A light-sensitive material containing the acetylide compound and the salt is also disclosed.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: May 30, 1989
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Sato, Shunichi Ishikawa, Ken Kawata
  • Patent number: 4808762
    Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; Z is oxygen, sulfur, or methylene; and Ar' is 2-methyl[1,1'-biphenyl]-3-yl, 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, or 6-phenoxy-2-pyridyl exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively harmless to aquatic fauna.
    Type: Grant
    Filed: September 9, 1987
    Date of Patent: February 28, 1989
    Assignee: FMC Corporation
    Inventors: Gary A. Meier, Scott M. Sieburth, Thomas G. Cullen, John F. Engel
  • Patent number: 4806562
    Abstract: Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: February 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4803286
    Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.
    Type: Grant
    Filed: August 19, 1987
    Date of Patent: February 7, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
  • Patent number: 4798831
    Abstract: Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: January 17, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John D. Prugh, George D. Hartman, Wasyl Halczenko
  • Patent number: 4725602
    Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: February 16, 1988
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4720503
    Abstract: N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e.g., methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e.g., methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products.
    Type: Grant
    Filed: August 2, 1985
    Date of Patent: January 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Allan N. Tischler, Debra L. Allison