Silicon Containing Patents (Class 546/14)
-
Patent number: 5541325Abstract: The present invention relates to compounds of the formula ##STR1## wherein R represents hydrogen; C.sub.1-6 alkyl; C.sub.3-6 cycloalkyl; phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; or thienyl optionally substituted with halo or C.sub.1-6 alkyl; and.dbd.C.dbd.X is a radical of the formula:.dbd.C.dbd.O (a),.dbd.C.dbd.N--O--R.sup.1 (b), or.dbd.C.dbd.CH--R.sup.2 (c);the addition salts thereof and stereochemically isomeric forms thereof, said compounds being useful as intermediate to potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflications.Type: GrantFiled: April 18, 1995Date of Patent: July 30, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
-
Patent number: 5539117Abstract: The present invention is directed to 2-acetyl-6-cyanopyridine compounds that are useful as intermediates in the synthesis of oligo-2,6-pyridines. The present invention is also directed to new, simpler, less expensive methods for synthesizing such oligopyridines using the novel 2-acetyl-6-cyanopyridine compounds as intermediates.Type: GrantFiled: July 19, 1994Date of Patent: July 23, 1996Inventors: Robert A. Snow, Daniel J. Delecki, Chandra R. Shah, K. Robert Hollister
-
Patent number: 5538950Abstract: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.Type: GrantFiled: May 12, 1994Date of Patent: July 23, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Naoki Fukami, Masashi Hashimoto, Hirokazu Tanaka, Natsuko Kayakiri
-
Patent number: 5536732Abstract: This invention relates to novel N-derivatives of 1-deoxy nojirimycin, to the method for their preparation and to their use in the treatment of diabetes and the use against retro-viruses, particularly in the treatment of acquired immuno-deficiency syndrome (AIDS).Type: GrantFiled: July 14, 1993Date of Patent: July 16, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Brigitte Lesur, Jean-Bernard Ducep, Charles Danzin
-
Patent number: 5536847Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: July 16, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
-
Patent number: 5532243Abstract: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.Type: GrantFiled: February 14, 1992Date of Patent: July 2, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Paul J. Gilligan
-
Patent number: 5530153Abstract: Process for the preparation of aryldimethyl(3-arylpropyl)silanes by a route comprising hydrosilylation followed by a modified Grignard reaction.Type: GrantFiled: January 27, 1995Date of Patent: June 25, 1996Assignee: Hoechst AktiengesellschaftInventor: Hans H. Schubert
-
Patent number: 5527827Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --C(Ar.sup.3).dbd.CHCO.sub.2 H Iare inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: October 27, 1994Date of Patent: June 18, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Daniel Delorme, Yves Ducharme, Richard Friesen, Erich L. Grimm, Carole Lepine
-
Patent number: 5527912Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: March 27, 1995Date of Patent: June 18, 1996Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
-
Patent number: 5521187Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: March 15, 1994Date of Patent: May 28, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
-
Patent number: 5516908Abstract: The present invention relates to novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifiuoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient.Type: GrantFiled: April 18, 1995Date of Patent: May 14, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
-
Patent number: 5514738Abstract: New stabilizers of the formula (I) ##STR1## in which m+n is a number from 1 to 100 and n varies from zero to 90% of the sum of m+n,A is --O-- or ##STR2## where R.sub.6 is e.g. hydrogen or C.sub.1 -C.sub.18 alkyl, R.sub.1 and R.sub.4 which can be identical or different are C.sub.1 -C.sub.8 alkyl, phenyl, C.sub.1 -C.sub.8 alkoxy, OH, ONa or OK,R.sub.2 is C.sub.2 -C.sub.12 alkylene or also a direct bond if A is --O-- and R.sub.1 and R.sub.4 are C.sub.1 -C.sub.8 alkyl or phenyl,R.sub.3 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.5 -C.sub.12 cycloalkenyl, C.sub.7 -C.sub.12 aralkyl, a saturated or unsaturated radical of a bicyclic or tricyclic C.sub.7 -C.sub.12 hydrocarbon or C.sub.6 -C.sub.10 aryl which is unsubstituted or substituted by C.sub.1 -C.sub.8 alkyl,R.sub.5 is hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl or phenyl,X.sub.1 is as defined for R.sub.1 or is a group (R.sub.7).sub.3 SiO-- with R.sub.7 being C.sub.1 -C.sub.8 alkyl,X.sub.2 is e.Type: GrantFiled: January 19, 1995Date of Patent: May 7, 1996Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Primo Carrozza, Ramanathan Ravichandran
-
Patent number: 5514685Abstract: The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.Type: GrantFiled: May 15, 1995Date of Patent: May 7, 1996Assignee: Sandoz Ltd.Inventor: Karl Baumann
-
Patent number: 5514642Abstract: Cyclohexenone oxime ethers of the formula I ##STR1##Type: GrantFiled: February 13, 1995Date of Patent: May 7, 1996Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Dieter Kolassa, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber, Uwe Kardorff
-
Patent number: 5502203Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.Type: GrantFiled: May 31, 1995Date of Patent: March 26, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
-
Patent number: 5502065Abstract: The present invention provides compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 21, 1994Date of Patent: March 26, 1996Assignee: Pfizer Inc.Inventors: Alan D. Brown, Roger P. Dickinson, Martin J. Wythes
-
Patent number: 5496961Abstract: Organosilicon compounds having Si-bonded hydrogen atoms are reacted with organic compounds having aliphatic multiple bonds in the presence of triazene oxide-transition metal complexes. The triazene oxide-transition metal complexes are activated by heating at temperatures of from 50.degree. C. to 250.degree. C. and/or by irradiation with light.Type: GrantFiled: May 10, 1995Date of Patent: March 5, 1996Assignee: Wacker-Chemie GmbHInventors: Jochen Dauth, Josef Wolferseder, Bernward Deubzer
-
Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
-
Patent number: 5470978Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.Type: GrantFiled: November 18, 1992Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: Anita Melikian-Badalian, Paul L. Ornstein
-
Patent number: 5468742Abstract: The invention relates to new 8-vinyl- and 8-ethinylquinolonecarboxylic acids, process for their preparation, and antibacterial agents and feed additives containing them.Type: GrantFiled: November 1, 1993Date of Patent: November 21, 1995Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Himmler, Thomas Schenke, Andreas Krebs, Klaus Grohe, Klaus-Dieter Bremm, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
-
Patent number: 5463058Abstract: Novel polymethylpiperidine compounds of general formula (I) containing silane groups and effective as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.The meanings of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n are defined in the text.Type: GrantFiled: February 21, 1995Date of Patent: October 31, 1995Assignee: Ciba-Geigy CorporationInventors: Primo Carrozza, Giovanni Da Roit
-
Patent number: 5461071Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.Type: GrantFiled: October 21, 1994Date of Patent: October 24, 1995Assignee: Merck & Co., Inc.Inventors: Evon A. Bolessa, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez Perez, Angeles Cabello Arroyo, Teresa Diez Matas, Isabel Martin Fernandez, Francisca Vincente Perez, Suzanne M. Mandala, Deborah L. Zink, Rosemary Thornton, John R. Thompson, James E. Curotto
-
Patent number: 5455248Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: September 14, 1993Date of Patent: October 3, 1995Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
-
Patent number: 5453509Abstract: This invention relates to a method of preparation of 1,2-dihydropyridine compounds having the structure: ##STR1## which comprises reacting a compound having the structure: ##STR2## The reaction is performed under suitable reaction conditions and in an appropriate solvent so as to form the 1,2-dihydropyridine compound. In a similar manner 1,2-dihydroquinolines, dihydroisoquinolines, dihydropyridones, dihydroquinolones and dihydroisoquinolones may also be prepared. The invention is also directed to compounds prepared by this method.Type: GrantFiled: October 8, 1993Date of Patent: September 26, 1995Assignee: Synaptic Pharmaceutical CorporationInventors: T. G. Murali Dhar, Charles Gluchowski
-
Patent number: 5451563Abstract: Fungicidal heterocyclic silyl compounds of the general formula ##STR1## have been discovered wherein Het is a six membered heterocyclic moiety; R is hydrogen or a trisubstituted silyl group; R.sup.1, R.sup.2 and R.sup.3 are independently selected from substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or pyridyl groups; m is 0 or 1 and n is zero, one or two.Type: GrantFiled: March 16, 1994Date of Patent: September 19, 1995Assignee: Rohm and Haas CompanyInventors: Steven H. Shaber, Edward M. Szapacs, Reynolds Charles H.
-
Patent number: 5446032Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, and B are variables. These compounds are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.Type: GrantFiled: February 28, 1994Date of Patent: August 29, 1995Assignee: British Biotech Pharmaceuticals LimitedInventors: Mark Whittaker, Andrew Miller
-
Patent number: 5446158Abstract: A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.Type: GrantFiled: October 12, 1990Date of Patent: August 29, 1995Assignee: Merck & Co., Inc.Inventors: Todd K. Jones, Sander G. Mills, David Askin, Robert A. Reamer, Richard Desmond, David M. Tschaen, Ralph P. Volante, Ichiro Shinkai
-
Patent number: 5446182Abstract: A method for the removal and concentration of desired ions such as Pd(II), Ru(III), Pd(IV), Au(III), Au(I), Ag(I), and Hg(II) from a multiple ion source solution which may contain larger concentrations of other undesired ions including H.sup.+ comprises bringing the source solution into contact with a compound comprising a sulfur and electron withdrawing group containing ligand covalently bonded through an organic spacer silicon grouping to a solid inorganic support. The sulfur and electron withdrawing group containing ligand portion(s) of the compound has an affinity for the desired ions to form a complex thereby removing the desired ions from the source solution. The desired ions are removed from the compound by contacting the compound with a much smaller volume of a receiving solution having a greater affinity for the desired ions than does the sulfur and electron withdrawing group containing ligand portion of the compound.Type: GrantFiled: February 15, 1994Date of Patent: August 29, 1995Assignee: Brigham Young UniversityInventors: Ronald L. Bruening, Bryon J. Tarbet, Reed M. Izatt, Jerald S. Bradshaw
-
Patent number: 5442065Abstract: A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.Type: GrantFiled: September 9, 1993Date of Patent: August 15, 1995Assignee: Board of Regents, The University of Texas SystemInventors: Philip D. Magnus, Theodore Iliadis, Shane A. Eisenbeis, Robin A. Fairhurst
-
Process for producing (E)-alkoxyimino or hydroxyimino-acetamide compounds and intermediates therefor
Patent number: 5442063Abstract: The present invention relates to a process for producing (E)-alkoxyiminoacetamide compounds useful as agricultural fungicides and a process for producing (E)-hydroxyiminoacetamide compounds useful as intermediates for producing them. The present invention also relates to an industrial process for producing (E)-methoxyiminoacetamide compounds useful as agricultural fungicides. This process is advantageous in terms of the cost, safety and the like.Type: GrantFiled: November 2, 1993Date of Patent: August 15, 1995Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Moriyasu Masui, Kuniyoshi Nishida -
Patent number: 5436339Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##Type: GrantFiled: July 14, 1992Date of Patent: July 25, 1995Assignee: Abbott LaboratoriesInventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao
-
Patent number: 5427860Abstract: Described are preferred methods for promoting interfacial bonding between surfaces containing oxide, hydrous oxide or hydroxyl groups. The methods involve attaching silane coupling agents to the opposed surfaces and, in turn, bonding the opposed silane coupling agents to each other to thereby promote interfacial bonding between the surfaces. Also described are preferred compositions for promoting such interfacial bonding.Type: GrantFiled: October 7, 1992Date of Patent: June 27, 1995Inventors: Martel Zeldin, Wilmer K. Fife
-
Patent number: 5426200Abstract: Organosiloxanes comprising at least one chemically bonded transition metal complex of Pt, Pd, Rh, Ru, Os or Ir, having a triazene, tetrazene, tetrazdiene, pentazdiene or triazene oxide ligand and are used as hydrosilylation catalysts that can be activated by light and/or heat.Type: GrantFiled: July 19, 1994Date of Patent: June 20, 1995Assignee: Wacker-Chemie GmbHInventors: Jochen Dauth, Udo Peetz, Bernward Deubzer
-
Patent number: 5420136Abstract: A class of predominantly hydrophobic non-azo N-substituted 1,8-naphthalimide compounds, each bearing, at its 3-position, a nucleofuge and, at its 4-position, a heteroatomic electron-releasing group. The heteroatomic electron-releasing group is being characterized as having a heteroatom directly linked to the 4-position of the ring, and having at least one hydrogen directly attached to the heteroatom. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species initiate chemical changes in lipid bilayer membranes of viruses and other target cells. These changes can eradicate viruses and other target cells. The activated species can also cause structural changes in lipid and any associated proteins and polypeptides at a level beneath the surface of the membrane, leading to polymerization and crosslinking.Type: GrantFiled: August 9, 1993Date of Patent: May 30, 1995Assignee: MicroBioMed CorporationInventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
-
Patent number: 5418267Abstract: The present invention relates to novel piperidine compounds of the formula (I) ##STR1## in which A is e.g. a group of the formula ##STR2## where R.sub.4 is e.g. hydrogen or methyl, X.sub.3 is e.g. --O-- or --NH-- and R.sub.5' is e.g. ethylene, propylene or decamethylene, R.sub.1 is e.g. methyl, methoxy, ethoxy or OH, R.sub.2 and R.sub.3 are e.g. methyl, m+n is e.g. a number from 1 to 40, n varies e.g. from zero to 50% of the sum m+n, X.sub.1 is e.g. as defined for R.sub.1 or is a group (CH.sub.3).sub.3 SiO-- and X.sub.2 is e.g. hydrogen, methyl, ethyl, a group (CH.sub.3).sub.3 Si-- or a group ##STR3## and, when m+n is a number from 3 to 10, X.sub.1 and X.sub.2 together also form a direct bond. The compounds of the formula (I) are effective in stabilizing an organic material against thermal, oxidative and light-induced degradation.Type: GrantFiled: April 28, 1994Date of Patent: May 23, 1995Assignee: Ciba-Geigy CorporationInventors: Primo Carrozza, Valerio Borzatta
-
Patent number: 5414066Abstract: Room temperature vulcanizable platinum group metal catalyzed silicone compositions are provided which utilize an N-heterocyclic adhesion promoter, such as 2,6 bis(trimethoxysilyltrimethyleneoxy)pyridine. Cohesive bonding is effected on various substrates.Type: GrantFiled: August 5, 1994Date of Patent: May 9, 1995Assignee: General Electric CompanyInventors: Judith Stein, Mark W. Davis
-
Patent number: 5412104Abstract: Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.Type: GrantFiled: March 1, 1993Date of Patent: May 2, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5405960Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.Type: GrantFiled: August 9, 1994Date of Patent: April 11, 1995Assignee: SynthelaboInventors: Isaac Chekroun, Guy Rossey, Michel Magnat
-
Patent number: 5395854Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.Type: GrantFiled: September 22, 1993Date of Patent: March 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
-
Patent number: 5391744Abstract: Bioactive cocaine analogs of the general formulae: ##STR1## are provided wherein X' is H or (C.sub.1 -C.sub.5)alkyl, X is H, halo, alkyl, alkoxy, perfluoroalkyl, nitro, alkoxycarbonyl, dialkoxyphosphonyl, acyl, perfluoroacyl, azido (substituted)silyl or (substituted)thio, and Y is H, halo, nitro, amino or (substituted)amino, alkoxycarbonyl, carboxy, alkyl or alkoxy; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 1993Date of Patent: February 21, 1995Assignee: Mayo Foundation For Medical Education and ResearchInventor: Alan P. Kozikowski
-
Patent number: 5391742Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: April 15, 1994Date of Patent: February 21, 1995Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
-
Patent number: 5385892Abstract: The ethylamino phenyl ethers of the invention and compositions thereof are endowed with high activities as inhibitors of the growth of several species of pathogen fungi and are applied to plants or to plant parts and are effective in preventing the diseases caused by pathogen fungi, such as, e.g., those belonging to Erysiphe and Helminthosporium genera.Type: GrantFiled: January 4, 1993Date of Patent: January 31, 1995Assignee: Ministero Dell "Universita" E Dell Ricerca Scientifica E TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5382594Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.Type: GrantFiled: March 1, 1993Date of Patent: January 17, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
-
Patent number: 5382572Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates; wherein:(A) X is selected from the group consisting of N--R.sup.3, O, S, and C(R.sup.3).sub.2 ;(B) R.sup.3 is selected from H and a range of substituents;(C) R.sup.1 is an etherifying or esterifying group;(D) R.sup.2 is selected from a range of substituents;(E) m is 0 or an integer from 1 to 4; and(F) R.sup.4 and R.sup.5 are the same and are selected from alkyl and acyl groups;together with the pharmaceutically acceptable salts of the compounds of Formula 1.0 that are acidic or basic.Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.Type: GrantFiled: March 1, 1993Date of Patent: January 17, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
-
Patent number: 5380846Abstract: Addition-curable platinum group metal catalyzed silicone compositions are provided which utilize an N-heterocyclic adhesion promoter, such as bis(trimethoxysilyltrimethylene) 2,6 pyridine dicarboxylate. Cohesive bonding is effected on both plastic and metal substrates at temperatures of less than 100.degree. C. and in less than 1 hour.Type: GrantFiled: June 13, 1994Date of Patent: January 10, 1995Assignee: General Electric CompanyInventor: Judith Stein
-
Patent number: 5380788Abstract: Room temperature vulcanizable platinum group metal catalyzed silicone compositions are provided which utilize an N-heterocyclic adhesion promoter, such as 2,6 bis(trimethoxysilyltrimethyleneoxy)pyridine. Cohesive bonding is effected on various substrates.Type: GrantFiled: December 13, 1993Date of Patent: January 10, 1995Assignee: General Electric CompanyInventors: Judith Stein, Mark W. Davis
-
Patent number: 5378694Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R.sup.4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R.sup.1 is H.Type: GrantFiled: March 1, 1993Date of Patent: January 3, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles, Stuart B. Rosenblum
-
Patent number: 5371223Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: October 8, 1993Date of Patent: December 6, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
-
Patent number: 5371216Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.Type: GrantFiled: January 28, 1993Date of Patent: December 6, 1994Assignee: Huls AktiengesellschaftInventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
-
Patent number: 5371222Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: October 16, 1992Date of Patent: December 6, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto