Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 549/50)
-
Patent number: 6340759Abstract: 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: GrantFiled: March 31, 2000Date of Patent: January 22, 2002Assignee: 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: 20020002287Abstract: A process for the preparation of 3,4-alkylenedioxythiophene-2,5-dicarboxylic acid derivatives of the general formulae IV and V 1Type: ApplicationFiled: June 8, 2001Publication date: January 3, 2002Inventor: Friedrich Jonas
-
Publication number: 20010034453Abstract: 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: ApplicationFiled: March 21, 2001Publication date: October 25, 2001Inventors: Gunter Rauchschwalbe, Friedrich Jonas
-
Patent number: 6245255Abstract: 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: GrantFiled: May 23, 2000Date of Patent: June 12, 2001Assignee: Eastman Kodak CompanyInventors: Margaret J. Helber, William J. Harrison, Kevin W. Williams, Steven W. Kortum
-
Patent number: 6184221Abstract: 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: GrantFiled: August 4, 1998Date of Patent: February 6, 2001Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
-
Patent number: 6153645Abstract: 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: GrantFiled: September 10, 1999Date of Patent: November 28, 2000Assignee: Cubist Pharmaceuticals, Inc.Inventors: John Finn, Xiang Yang Yu, Zhongguo Wang, Jason Hill, Dennis Keith, Paul Gallant, Philip Wendler
-
Patent number: 6147110Abstract: 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: GrantFiled: December 23, 1998Date of Patent: November 14, 2000Assignee: Adir et CompagnieInventors: Daniel Lesieur, Nicolas Ruiz, Valerie Wallez, Sophie Boye, Caroline Bennejean, Pierre Renard, Philippe Delagrange
-
Patent number: 6133305Abstract: 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: GrantFiled: September 25, 1998Date of Patent: October 17, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 6130339Abstract: Provided are novel, electropolymerizable monomers of the formulae: ##STR1##Type: GrantFiled: June 1, 1999Date of Patent: October 10, 2000Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Devdatt S. Nagvekar, Balasubramanian Sankaran
-
Patent number: 6051722Abstract: 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: GrantFiled: July 6, 1998Date of Patent: April 18, 2000Assignee: Hitachi Chemical Company, Ltd.Inventors: Yutaka Honda, Iwao Fukuchi, Kwan-Yue Alex Jen
-
Patent number: 6037340Abstract: 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: GrantFiled: May 28, 1997Date of Patent: March 14, 2000Assignee: Cadus Pharmaceutical CorporationInventors: Arlindo L. Castelhano, Bryan McKibben
-
Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
-
Patent number: 5824677Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
-
Patent number: 5767141Abstract: 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: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
-
Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
-
Patent number: 5684165Abstract: 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: GrantFiled: April 14, 1995Date of Patent: November 4, 1997Assignee: Hoechst AktiengesellschaftInventors: Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
-
Patent number: 5521213Abstract: 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: GrantFiled: August 29, 1994Date of Patent: May 28, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
-
Patent number: 5464834Abstract: 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: GrantFiled: June 11, 1993Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Jean-Michel Rivet
-
Patent number: 5463056Abstract: 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: GrantFiled: May 27, 1994Date of Patent: October 31, 1995Assignee: Agta-Gevaerf AGInventor: Friedrich Jonas
-
Patent number: 5457212Abstract: 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: GrantFiled: September 30, 1994Date of Patent: October 10, 1995Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline J. Sanfilippo, Maud Urbanski
-
Patent number: 5432286Abstract: 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: GrantFiled: October 7, 1993Date of Patent: July 11, 1995Assignee: Hoechst AktiengesellschaftInventors: Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
-
Patent number: 5393729Abstract: 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: GrantFiled: September 3, 1993Date of Patent: February 28, 1995Assignee: Bayer AktiengesellschaftInventors: 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: 5380748Abstract: 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: GrantFiled: August 30, 1993Date of Patent: January 10, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Yoshiaki Muto, Hiromi Ichikawa, Kuniyoshi Ogura, Kyoji Chaki, Masao Seiki, Toshihiko Takemasa
-
Patent number: 5378713Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: November 4, 1991Date of Patent: January 3, 1995Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
-
Patent number: 5304657Abstract: 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: GrantFiled: October 10, 1991Date of Patent: April 19, 1994Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Tadaaki Toki, Toru Koyanagi, Kiyomitsu Yoshida, Kazuhiro Yamamoto, Masayuki Morita
-
Patent number: 5286881Abstract: 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: GrantFiled: September 30, 1992Date of Patent: February 15, 1994Assignee: Sumitomo Chemical Company LimitedInventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
-
Patent number: 5284857Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: December 21, 1990Date of Patent: February 8, 1994Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
-
Patent number: 5260453Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed.Type: GrantFiled: November 5, 1990Date of Patent: November 9, 1993Assignee: Ortho Pharmaceutical CorporationInventors: Jeffrey B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
-
Patent number: 5201936Abstract: 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: GrantFiled: October 15, 1991Date of Patent: April 13, 1993Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Bertram, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt, Andrew Plant, Bernd-Wieland Kruger, Achim Harder, Norbert Mencke
-
Patent number: 5183818Abstract: 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: GrantFiled: August 27, 1991Date of Patent: February 2, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
-
Patent number: 5102905Abstract: 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: GrantFiled: April 28, 1989Date of Patent: April 7, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey Morris, John Preston
-
Patent number: 5095032Abstract: 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: GrantFiled: July 19, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Bertram, Nikolaus Muller, Achim Harder
-
Patent number: 5030736Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: November 5, 1990Date of Patent: July 9, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
-
Patent number: 4996142Abstract: 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: GrantFiled: September 4, 1987Date of Patent: February 26, 1991Assignee: Agricultural Genetics Company LimitedInventors: Ali H. Al-Hakim, Roger Hull
-
Patent number: 4992435Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: September 23, 1988Date of Patent: February 12, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
-
Patent number: 4990647Abstract: 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: GrantFiled: April 24, 1989Date of Patent: February 5, 1991Assignee: Bayer AktiengesellschaftInventors: Thomas Himmler, Rudolf Braden
-
Patent number: 4975451Abstract: 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: GrantFiled: March 2, 1989Date of Patent: December 4, 1990Assignee: FMC CorporationInventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel, Leslie W. Stratton, Alan W. Fritz
-
Patent number: 4970309Abstract: 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: GrantFiled: December 7, 1989Date of Patent: November 13, 1990Assignee: Polaroid CorporationInventor: Patrick F. King
-
Patent number: 4929549Abstract: 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: GrantFiled: February 8, 1989Date of Patent: May 29, 1990Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh
-
Patent number: 4923882Abstract: 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: GrantFiled: October 16, 1986Date of Patent: May 8, 1990Assignee: 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: 4894390Abstract: 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: GrantFiled: October 21, 1988Date of Patent: January 16, 1990Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh
-
Patent number: 4876271Abstract: 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: GrantFiled: December 20, 1988Date of Patent: October 24, 1989Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh
-
Patent number: 4863922Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: June 15, 1988Date of Patent: September 5, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
-
Patent number: 4835272Abstract: 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: GrantFiled: July 16, 1987Date of Patent: May 30, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Sato, Shunichi Ishikawa, Ken Kawata
-
Patent number: 4808762Abstract: 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: GrantFiled: September 9, 1987Date of Patent: February 28, 1989Assignee: FMC CorporationInventors: Gary A. Meier, Scott M. Sieburth, Thomas G. Cullen, John F. Engel
-
Patent number: 4806562Abstract: Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.Type: GrantFiled: May 4, 1988Date of Patent: February 21, 1989Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh
-
Patent number: 4803286Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.Type: GrantFiled: August 19, 1987Date of Patent: February 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
-
Patent number: 4798831Abstract: Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.Type: GrantFiled: May 4, 1988Date of Patent: January 17, 1989Assignee: Merck & Co., Inc.Inventors: John D. Prugh, George D. Hartman, Wasyl Halczenko
-
Patent number: 4725602Abstract: 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: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
-
Patent number: 4720503Abstract: 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: GrantFiled: August 2, 1985Date of Patent: January 19, 1988Assignee: Merck & Co., Inc.Inventors: Bruce E. Witzel, Allan N. Tischler, Debra L. Allison