Silicon Containing Patents (Class 546/14)
  • Patent number: 5371061
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each independently represents hydrogen, optionally substituted alkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aralkyl, alkaryl, hydroxy, alkoxy, alkenyloxy, alkynyloxy, alkylcarbonyl, alkoxycarbonyl, amino, mono- or dialkylamino, alkoxycarbonylamino, optionally substituted heterocycle or arylamino, dialkylcarbamoyl, trialkylsilyl or fused ring structure, or together form an alkenylene chain or an alkylene chain which is optionally interrupted by oxygen or sulphur or --NR--, R being hydrogen or alkyl; R.sub.3 represents hydrogen or halogen, or optionally substituted alkyl, alkoxy, aryl or aryloxy, or cyano, carboxy, alkoxycarbonyl, (alkylthio) carbonyl, alkylcarbonyl, amido, alkylamido, nitro, alkenyloxy, alkynloxy, alkylthio, haloalkylthio, alkenylthio, alkynylthio, alkylsulphinyl, alkylsulphonyl, alkyloximinoalkyl or alkenyloximinoalkyl; R.sub.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: December 6, 1994
    Assignee: American Cyanamid Company
    Inventors: Hans-Joachim Bissinger, Axel Kleemann, Richard J. G. Searle
  • Patent number: 5364942
    Abstract: Sulphonylbenzyl-substituted imidazopyridines can be prepared by reacting correspondingly substituted imidazopyridines with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted imidazopyridines can be employed as active compounds in medicaments, in particular for the treatment of hypertension and atherosclerosis.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: November 15, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Hanko, Jurgen Dressel, Peter Fey, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Claudia Hirth-Dietrich, Andreas Knorr, Johannes-Peter Stasch, Stefan Wohlfeil, Ozkan Yalkinoglu
  • Patent number: 5359073
    Abstract: A class of N,N'-cycloalkyl/alkyl benzamides of certain 1H-imidazo[4,5-b]pyridine and 3H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of the formula: ##STR1## wherein each of X.sup.a and X.sup.b is independently selected from nitrogen atom and --CH--, with the proviso that when one of X.sup.a and X.sup.b is selected as nitrogen atom, then the other of X.sup.a and X.sup.b must be --CH--; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R.sup.5, R.sup.6, R.sup.7 and R.sup.
    Type: Grant
    Filed: November 24, 1992
    Date of Patent: October 25, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard M. Weier, Ish K. Khanna, Michael A. Stealey, Janet A. Julien, Kirk T. Lentz
  • Patent number: 5359065
    Abstract: An improved method of preparing an ortho-, meta- or para-silyl aromatic or heteroaromatic compound represented by the formula ##STR1## wherein X is oxygen or sulfur,R.sub.1 represents the atoms necessary to complete an unsubstituted or substituted aromatic or heteroaromatic ring, andR.sub.2, R.sub.3 and R.sub.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: October 25, 1994
    Assignee: Eastman Kodak Company
    Inventor: Sundaram Krishnamurthy
  • Patent number: 5359076
    Abstract: The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) ##STR1## wherein R and R.sup.1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R.sup.
    Type: Grant
    Filed: December 9, 1992
    Date of Patent: October 25, 1994
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Katsuya Awano, Takayoshi Ishizaki, Eisuke Kojima, Shinji Kudoh, Yasuhiko Sakoe, Koji Saito
  • Patent number: 5356885
    Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.
    Type: Grant
    Filed: April 24, 1991
    Date of Patent: October 18, 1994
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
  • Patent number: 5356914
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: October 18, 1994
    Assignee: Beecham Group p.l.c.
    Inventors: Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
  • Patent number: 5354738
    Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: September 4, 1992
    Date of Patent: October 11, 1994
    Assignees: G. D. Searle & Co., The Monsanto Company
    Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5350750
    Abstract: .beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives of formula I ##STR1## in which R.sup.A, n, R.sup.4 and R.sup.3, have the meaning indicated in the claims, as well as their production and their use in pharmaceutical agents are described.
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: September 27, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Huth, Martin Kruger, Dieter Seidelmann, Ralph Schmiechen, Werner Krause, Herbert Schneider, Lechoslaw Turski
  • Patent number: 5338853
    Abstract: N-(2,2,6,6-tetraalkyl-4-piperidinyl)amic acid hydrazides contain a light stabilizing group, a heat stabilizing group and an amic acid hydrazide functionality in the same molecule. The amic acid hydrazide functionality in the compounds enhances the photooxidative stabilizing properties of the hindered amine groups and contributes thermal and oxidative stabilizing and metal complexing properties to the compounds. The novel compounds are excellent light stabilizers for polyolefins, have low volatility and are not readily lost from polymeric systems via volatilization, migration or extraction.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: August 16, 1994
    Assignee: Elf Atochem North America, Inc.
    Inventors: Ronald E. MacLeay, Harold C. Lange
  • Patent number: 5336771
    Abstract: The present invention relates to processes and intermediates for the preparation of spiro-heteroazolones. The latter compounds are useful as aldose reductase inhibitors.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: August 9, 1994
    Assignee: Pfizer Inc.
    Inventors: Charles W. Murtiashaw, George J. Quallich
  • Patent number: 5332825
    Abstract: This invention relates to two processes for preparing aminoacetonitriles in one vessel under anhydrous conditions. Process I involves the steps of: (A) reacting trimethylsilyl cyanide and an aldehyde in a water miscible amide solvent to obtain a silyl blocked cyanohydrin solution; (B) adding a catalytic amount of water to the silyl blocked cyanohydrin solution from Step (A); and (C) passing ammonia through the solution to obtain an aminoacetonitrile. Process II involves the steps of: (A') reacting trimethylsilyl cyanide with an aldehyde in the absence of solvent to form a silyl blocked cyanohydrin; (B') adding a water miscible amide solvent to the silyl blocked cyanohydrin from Step (A') to obtain a solution; and (C') passing ammonia through the solution to obtain an aminoacetonitrile. Aminoacetonitriles are important intermediates in the preparation of amino acids, thiadiazoles, acylaminoacetonitriles, and imidazole derivatives.
    Type: Grant
    Filed: October 13, 1993
    Date of Patent: July 26, 1994
    Assignee: Eastman Kodak Company
    Inventor: Paul R. Buckland
  • Patent number: 5332740
    Abstract: Novel DC-89 derivatives represented by general formula (I): ##STR1## wherein X represents Cl or Br; R.sup.1 represents hydrogen, CONR.sup.2 R.sup.3 (in which R.sup.2 and R.sup.3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group), ##STR2## (in which n represents an integer of 4 to 7), ##STR3## (in which R.sup.4 represents oxygen, N--CH.sub.3 or N--CH.sub.2 CH.sub.2 NH.sub.2), ##STR4## (in which R.sup.5 R.sup.6 and R.sup.7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and ##STR5## (in which Y represents hydrogen or CO.sub.2 CH.sub.3); provided that when R.sup.1 is hydrogen, CONR.sup.2 R.sup.3 or SiR.sup.5 R.sup.6 R.sup.7, ##STR6## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.
    Type: Grant
    Filed: April 13, 1993
    Date of Patent: July 26, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiromitsu Saito, Satoru Nagamura, Akira Asai, Eiji Kobayashi, Katsushige Gomi
  • Patent number: 5332715
    Abstract: Plant-protecting substituted isoxazolines, isoxazoles, isothiazolines and isothiazoles, and also processes for their preparation and their useCompounds of the formula I(R.sup.1)(R.sup.2)(R.sup.3)Si--A--Het--B--CO--Z (I)whereHet is an isoxazole-, isoxazoline-, isothiazole- or isothiazoline-3,5-diyl radical,A and B are a bond or alkylene,R.sup.1, R.sup.2 and R.sup.3 are substituted or unsubstituted, saturated or unsaturated alkyl or, if desired, phenylalkyl or phenyl,Z is OH, OR where R is saturated or unsaturated, substituted or unsubstituted alkyl or substituted or unsubstituted phenyl or benzyl or trialkylsilylmethoxy, substituted or unsubstituted phenylamino or oxazolinyl or amino, mono- or dialkylamino or -hydrazino, cycloalkylamino, NH.sub.2 NH.sub.2, pyridino, morpholino, dimethylmorpholino, a radical --ON.dbd.CR.sup.4 R.sup.5 or O--CHR.sup.7 --CO--OR.sup.6 where R.sup.4, R.sup.5 =alkyl and/or R.sup.4 CR.sup.5 is cycloalkyl and R.sup.6, R.sup.
    Type: Grant
    Filed: November 18, 1992
    Date of Patent: July 26, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Josef Loher, Klaus Bauer, Hermann Bieringer
  • Patent number: 5332814
    Abstract: Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: July 26, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Heinz Moser
  • Patent number: 5321066
    Abstract: 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 stabilising an organic material against thermal, oxidative and light-induced degradation.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: June 14, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Primo Carrozza, Valerio Borzatta
  • Patent number: 5314879
    Abstract: The invention relates to the manufacture and use of aryl-propyl-aminic compounds having the following formula ##STR1## that have a high antifungal activity and are useful in the agricultural field as fungicides.
    Type: Grant
    Filed: February 28, 1991
    Date of Patent: May 24, 1994
    Assignee: Ministero Delli `Universita` E Della Ricerca Scientifica E Tecnologica
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 5315006
    Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.
    Type: Grant
    Filed: April 6, 1993
    Date of Patent: May 24, 1994
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Gary J. Drtina, Leif Christensen
  • Patent number: 5310910
    Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.
    Type: Grant
    Filed: April 6, 1993
    Date of Patent: May 10, 1994
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Gary J. Drtina, Leif Christensen
  • Patent number: 5304548
    Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: April 19, 1994
    Assignee: The Upjohn Company
    Inventors: Ronald B. Gammill, Frank P. Bell
  • Patent number: 5302589
    Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: April 12, 1994
    Assignee: Glaxo, Inc.
    Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
  • Patent number: 5296484
    Abstract: The compounds of the formula: ##STR1## wherein the substituents are herein below defined; are plant fungicides, insecticides, and miticides.
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: March 22, 1994
    Assignee: DowElanco
    Inventors: Michael J. Coghlan, Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
  • Patent number: 5296480
    Abstract: The invention provides compounds having the formula ##STR1## wherein R, X and R.sup.6 are defined in the specification which have activity as angiotensin II antagonists.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: March 22, 1994
    Assignee: American Cyanamid Company
    Inventor: Howard Newman
  • Patent number: 5296492
    Abstract: A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: March 22, 1994
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Akira Shiozawa, Atsuro Inubushi, Kazuhisa Narita, Yukihiro Sagawa, Makoto Hosono, Masashi Iida
  • Patent number: 5294622
    Abstract: The compounds of the formula: ##STR1## where the substituents are herein below defined, are fungicides, insecticides, and miticides.
    Type: Grant
    Filed: March 24, 1992
    Date of Patent: March 15, 1994
    Assignee: DowElanco
    Inventors: Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
  • Patent number: 5290935
    Abstract: A process for producing phosphonate esters containing the 2-(pyridyl)ethyl group by reacting a vinylpyridine with a di- or trihydrocarbylphosphite in the presence of a selected silane, protic acid, or Lewis acid is disclosed. Also disclosed are novel silylphosphonate esters containing the 2-(pyridyl)ethyl group. All of the compounds produced herein are useful as catalysts for increasing the molecular weight of polyamides.
    Type: Grant
    Filed: July 29, 1993
    Date of Patent: March 1, 1994
    Assignee: E. I. Du Pont De Nemours and Company
    Inventors: David L. Thorn, Owen W. Webster, Robert C. Wheland
  • Patent number: 5290941
    Abstract: An efficient process for the preparation of styrylbenzoxazoles and derivatives thereof comprises reacting a methylbenzoxazole with an aromatic aldehyde in the presence of strong base at low temperature, followed by warming. The condensation products are inhibitors of H.sup.+ K.sup.+ -ATPase, and are also useful as penultimate compounds in the preparation of inhibitors of HIV reverse transcriptase.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: March 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ralph P. Volante, Joseph E. Lynch, Ioannis Houpis, Audrey Molina
  • Patent number: 5288730
    Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 represents phenyl or thienyl, either of which groups may be optionally substituted by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl;R.sup.2 represents benzyl which may be substituted in the benzyl ring by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, S0.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a C0.sub.2 R.sup.b, --C0.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: February 22, 1994
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Christopher J. Swain, Martin R. Teall, Brian J. Williams
  • Patent number: 5286865
    Abstract: 1-Hydrocarbyloxy substituted hindered amine compounds which also contain a reactive functional group such as hydroxy, amino, oxirane or carboxyl can be chemically attached to selected polymer substrates by condensation reactions to give polymers containing a chemically-bonded, non-migrating stabilizer having excellent stabilization efficacy for protecting said polymer substrate from the adverse effects of actinic light.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: February 15, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
  • Patent number: 5286862
    Abstract: The present invention relates to a process for the preparation of compounds of the formula I ##STR1## where X is CH.dbd.CH, N.dbd.CH, CH.dbd.N or S,R.sup.1 and R.sup.2 independently of one another are H, halogen, alkyl, alkoxy, alkylthio, haloalkyl, haloalkoxy, haloalkylthio or the bivalent methylenedioxy group,R.sup.3 is a radical of the formulae (A), (B) or (C) ##STR2## where R.sup.4 and R.sup.5 independently of one another are H, halogen, alkyl, alkoxy or a radical of the formula (D) ##STR3## in which R.sup.6 is H or halogen andY is CH.sub.2, O or S, andm, n, o, p and q are 0, 1, or 2, which comprises reacting a compound of the formula IIH.sub.2 C.dbd.CH--CH.sub.2 --R.sup.3 (II)where R.sup.3 is as defined in formula I, with dichloromethylsilane in the presence of a catalyst suitable for hydrosilylation reactions, and reacting the resulting intermediate of the formula III ##STR4## where R.sup.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: February 15, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Hans H. Schubert
  • Patent number: 5281710
    Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.
    Type: Grant
    Filed: September 1, 1992
    Date of Patent: January 25, 1994
    Assignee: The Scripps Research Institute
    Inventors: Adrian L. Smith, Chan-Kou Hwang, Sebastian V. Wenderborn, Kyriacos C. Nicolaou, Erwin P. Schreiner, Wilhelm Stahl, Wei-Min Dai, Peter E. Maligres, Toshio Suzuki
  • Patent number: 5278332
    Abstract: New derivatives of cyclohexane in substantially pure form suitable as pharmaceutical, foodstuff or as a stabilizer.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: January 11, 1994
    Assignee: Perstorp AB
    Inventors: Matti Siren, Lars Perrson
  • Patent number: 5274161
    Abstract: New derivatives of cyclohexane in substantially pure form suitable as a pharmaceutical, foodstuff or as a stabilizer.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: December 28, 1993
    Assignee: Perstorp AB
    Inventors: Matti Siren, Lars Perrson
  • Patent number: 5272162
    Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5272270
    Abstract: The invention relates to a process for the preparation of 1-alkyl-1,2,3,4-tetrahydroisoquinoline derivatives of the general formula ##STR1## The compounds can be used for the preparation of tetrahydroisoquinolines of the reticuline type, or of the norreticuline type, by reductive removal of the OH groups or, if they carry an acyl protective group on the nitrogen, for the preparation of isoquinolines of the papaverine type by acid-catalyzed hydrolysis with removal of the acyl groups and simultaneous removal of the hydroxyl groups.These 1-alkyl-1,2-dihydroisoquinoline derivatives can then be used for the preparation of isoquinolines of the papaverine type by aromatization by means of acids or hydrazine.
    Type: Grant
    Filed: August 12, 1991
    Date of Patent: December 21, 1993
    Assignee: Consortium fur Elektrochemische Industrie GmbH
    Inventors: Rolf Hirsenkorn, Silvia Orlitsch
  • Patent number: 5264586
    Abstract: Chimeric analogs of calicheamicin that include an analog of calicheamicinone linked to an ester or glycoside, (-)-calicheamicinone and its analogs are disclosed.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: November 23, 1993
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Adrian L. Smith, Chan-Kou Hwang, Emmanuel Pitsinos
  • Patent number: 5262426
    Abstract: A class of N,N'-cycloalkyl/alkyl benzamides of certain 4H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of the formula: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, pyridinyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is independently selected from hydrido, hydroxy, alkyl, alkoxy, fluoro, chloro, bromo, haloalkyl, alkylthio, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, cyano, amino, monoalkylamino and dialkylamino; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heterocyclic, heterocyclicalkyl, aryl, alkenyl and cycloalkenyl, and wherein any of said R.sup.9 and R.sup.
    Type: Grant
    Filed: January 22, 1993
    Date of Patent: November 16, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard M. Weier, Ish K. Khanna, Michael A. Stealey, Janet A. Julien
  • Patent number: 5258469
    Abstract: A process for producing phosphonate esters containing the 2-(pyridyl)ethyl group by reacting a vinylpyridine with a di- or trihydrocarbylphosphite in the presence of a selected silane, protic acid, or Lewis acid is disclosed. Also disclosed are novel silylphosphonate esters containing the 2-(pyridyl)ethyl group. All of the compounds produced herein are useful as catalysts for increasing the molecular weight of polyamides.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: November 2, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David L. Thorn, Owen W. Webster, Robert C. Wheland
  • Patent number: 5258169
    Abstract: Silicon diimide having a carbon content of at most 0.5% by weight and a chlorine content of at most 20 ppm is prepared by reacting ammonia with organyl amino silane at 50.degree.-300.degree. C. at elevated pressure and is useful as an intermediate for high grade silicon nitride.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: November 2, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Wannagat, Adrian Schervan, Martin Jansen, Hans-Peter Baldus, Aloys Eiling
  • Patent number: 5256666
    Abstract: 3-Isoxazolylphenyl compounds Ia and Ib ##STR1## where R is halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkenyl; haloalkenyl; unsubstituted or substituted phenylethenyl; alkynyl; cycloalkyl; aryl; hetaryl; CO.sub.2 R.sup.6 or CONR.sup.7 R.sup.8,R.sup.6 is hydrogen, alkyl, cycloalkyl or benzyl;R.sup.7 and R.sup.8 are each hydrogen, alkyl, cycloalkyl or benzyl or, together with the nitrogen atom to which they are bonded, form a heterocyclic radical;n is 0, 1 or 2;R.sup.1 is halogen or alkyl;R.sup.2 is hydrogen; alkyl; alkenyl; alkynyl or cyano;R.sup.3 and R.sup.4 independently of one another are each unsubstituted or substituted alkyl, alkenyl, cycloalkyl, phenyl, naphthyl, pyridyl or pyrimidinyl; or R.sup.3 and R.sup.4 together form unsubstituted or substituted alkylene;R.sup.5 is hydrogen; unsubstituted or substituted alkyl or one of the groups stated for R.sup.3 ;X is CH.sub.2, O, S or NR.sup.9 andR.sup.
    Type: Grant
    Filed: November 13, 1992
    Date of Patent: October 26, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Mueller, Hans Theobald, Harald Rang, Volker Harries
  • Patent number: 5254685
    Abstract: A tricyclic compound represented by the general formula (1) and salts thereof. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: October 19, 1993
    Assignees: Wakunaga Seiyaku Kabushiki Kaisha, Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaharu Yokomoto, Akira Yazaki, Norihiro Hayashi, Shunso Hatono, Satoshi Inoue, Yasuhiro Kuramoto
  • Patent number: 5254563
    Abstract: Compounds of formula I ##STR1## in which R.sup.A, B (which is CR.sup.4) and R.sup.3 and have the meaning indicated in the application, as well as their production and their use in pharmaceutical agents, are described.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: October 19, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Huth, Martin Kruger, Dieter Rahtz, Dieter Seidelmann, Ralph Schmiechen, Lechoslaw Turski, John S. Andrews, Herbert H. Schneider
  • Patent number: 5250691
    Abstract: Compounds having the formula ##STR1## exhibiting antibacterial activity.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: October 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Henner Straub, Jakob-Matthias Drossard
  • Patent number: 5246944
    Abstract: Substituted quinolines and azaquinolines (1,5-naphthridines) attached through an oxymethylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: September 21, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Prasun K. Chakravarty
  • Patent number: 5243060
    Abstract: The present invention provides linear organosilicon polymers including diethynyl-(substituted)arylene units, and a process for their preparation. These novel polymers possess useful properties including electrical conductivity, liquid crystallinity, and/or photoluminescence. These polymers possess good solubility in organic solvents. A preferred example is produced according to the following reaction scheme. ##STR1## These polymers can be solvent-cast to yield excellent films and can also be pulled into fibers from concentrated solutions. All possess substantial crystallinity as revealed by DSC analysis and observation through a polarizing microscope, and possess liquid crystalline properties.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: September 7, 1993
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Thomas J. Barton, Yiwei Ding
  • Patent number: 5241067
    Abstract: Hindered amine light stabilizers are provided in which the hindered amine is contained in a unit of formula ##STR1## and R.sup.1, R.sup.2, R.sup.3, and A are as defined as in the Summary of the Invention. Unique polymeric and non-polymeric compounds containing this unit are useful as additives for the stabilization of polymeric compositions which are normally subject to thermal, oxidative or actinic light degradation.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: August 31, 1993
    Assignee: Elf Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5240916
    Abstract: Substituted naphthyridines of the formula (1): ##STR1## wherein one of A, B, C, or D is N, and the others are CR.sup.1 ;R.sup.1 and R.sup.2 are independently H or halo.X, Y and Z are defined in the specification.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: August 31, 1993
    Assignee: DowElanco
    Inventors: Blake A. Caley, Michael J. Coghlan, Leon N. Davis, Barry A. Dreikorn
  • Patent number: 5237064
    Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: August 17, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gary H. Rasmusson
  • Patent number: 5235051
    Abstract: Pyridinium salts of the formula ##STR1## are prepared. The compounds are useful as phase transfer catalysts for the preparation of methacryloyloxyalkylalkoxysilanes and acryloyloxyalkylalkoxysilanes.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: August 10, 1993
    Assignee: Huls Aktiengesellschaft
    Inventors: Gunther Bernhardt, Margret Haas, Heinz Kragl, Gerald L. Larson
  • Patent number: RE34805
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: December 6, 1994
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon