Silicon Containing Patents (Class 548/406)
  • Patent number: 5795987
    Abstract: Dioxetanes which couple with organic and biological molecules of the formula: ##STR1## wherein X is a leaving group which is removed by an activating agent to produce light, wherein A is a coupling substituent, Ar is a substituent selected from the group consisting of phenyl and naphthyl to provide a label are described. R.sub.1 is an optional linker substituent and can have between 1 and 30 carbon atoms with some of the carbon atoms being oxygen, sulfur, nitrogen or phosphorus. Ar as phenyl is preferred. The dioxetane coupled molecules are useful in assays of all types where luminescence can be used as an indicator.
    Type: Grant
    Filed: August 12, 1997
    Date of Patent: August 18, 1998
    Assignee: Board of Governors of Wayne State University
    Inventors: Arthur P. Schaap, Louis J. Romano
  • Patent number: 5776658
    Abstract: Compounds of the general formula I: (SIL--X--).sub.m IN (I), in which SIL is a radical of the formula Si(R.sup.1)(R.sup.2)(R.sup.3), where R.sup.1 is an alkyl, haloalkyl or alkoxy radical of 1 to 8 carbon atoms, an alkenyl radical, an alkenyloxy or acyloxy radical of 2 to 8 carbon atoms, an aryl or aryloxy radical of 6 to 10 carbon atoms, or a dialkyl-, diaryl- or alkylaryl-methyleneaminooxy radical having C.sub.1 -C.sub.4 -alkyl or C.sub.6 -aryl groups; and R.sup.2 and R.sup.3 are identical or different radicals with the meaning of R.sup.1 or X--IN; X is a group C.sub.n H.sub.2n ; IN is the radical of a compound which is active as a photoinitiator or photosensitizer and which has at least one carbonyl group located on an aromatic nucleus; m is a number from 1 to 4; and n is a number from 2 to 12, or of the formula II: Si.sub.o O.sub.o-1 (--X--IN).sub.p R.sup.4.sub.2o+2-p (II), in which R.sup.4 is a radical with the meaning of R.sup.1, and two or more radicals R.sup.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: July 7, 1998
    Assignee: AGFA-Gevaert AG
    Inventors: Claus-Peter Niesert, Georg Pawlowski, Willi-Kurt Gries, Klaus-Juergen Przybilla
  • Patent number: 5770743
    Abstract: Dioxetanes which couple with organic and biological molecules of the formula: ##STR1## wherein X is a leaving group which is removed by an activating agent other than an enzyme which is removed by an activating agent to produce light, wherein A is a coupling substituent, Ar is a substituent selected from the group consisting of phenyl and naphthyl to provide a label are described. R.sub.1 is an optional linker substituent and can have between 1 and 30 carbon atoms with some of the carbon atoms being oxygen, sulfur, nitrogen or phosphorus. Ar as phenyl is preferred. The dioxetane coupled molecules are useful in assays of all types where luminescence can be used as an indicator.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: June 23, 1998
    Assignee: Board of Governors of Wayne State University
    Inventors: Arthur P. Schaap, Louis J. Romano, Jaidev S. Goudar
  • Patent number: 5744487
    Abstract: A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful as an active ingredient of pharmaceutical compositions is provided.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: April 28, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Masahiro Ohshima, Norimichi Iwase, Shigeo Sugiyama, Koichi Sugawara, Misao Okitsu, Yoshikuni Tamao, Yasuhiro Morinaka
  • Patent number: 5736583
    Abstract: An uncapped polysiloxane composition is provided having the formula: ##STR1## wherein: R is selected from R.sub.2 or --OR.sub.9 wherein R.sub.9 is hydrogen or alkyl;R.sub.1 is selected from R.sub.2, an amine containing group of the formula --(CH.sub.2).sub.n --F.sub.n1 --B.sub.n2 --F--NH.sub.2 functional carboxyl group of the general formula: ##STR2## wherein at least one R.sub.1 is a pyrrolidone-containing functional carboxyl group as shown; R.sub.2 is as defined below; R.sub.5 is hydrogen, alkyl or alkali metal; F is linear or branched alkylene; B is --NR.sub.9, oxygen or sulfur, wherein R.sub.9 is hydrogen or lower alkyl (C.sub.1-6);R.sub.2 can be the same or different and is selected from alkyl, aryl, alkenyl or alkeynyl;R.sub.3 and R.sub.4, are selected from alkyl, aryl, capped or uncapped polyoxyalkylene, alkaryl, aralkylene or alkenyl;a is an integer from 0 to 50,000; andb is an integer from 0 to 100.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: April 7, 1998
    Assignee: Mona Industries, Inc.
    Inventors: Abe Berger, Dennis L. Fost
  • Patent number: 5703258
    Abstract: A flame retardant organic silicon and phosphorus containing compound is produced by reacting a silicon halides compound with an organic phosphorus compound to produce an organic silicon and phosphorus halides compound which is then reacted with an organic compound to produce an organic silicon and phosphorus containing compound. This organic silicon and phosphorus containing compound is incorporated in an otherwise more flammable organic material under reaction conditions and in an amount sufficient to reduce the combustibility of the otherwise more flammable organic material. The organic silicon and phosphorus containing compound may also be utilized as coating agents, adhesives, surfactants, insecticides, hydraulic fluid and other uses.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: December 30, 1997
    Inventor: David H. Blount
  • Patent number: 5691436
    Abstract: A mixture of silicon and phosphorus are heated and reacted with halide to produce silicon tetrahalides, silicon-phosphorus halide and phosphorus trihalides compositions. These compositions are reacted with any suitable organic, inorganic-organic and/or inorganic compound to produce novel organic silicon-phosphorus containing compositions. These compositions may be utilized as flame retardants, coating agents, adhesives and many other uses.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: November 25, 1997
    Inventor: David H. Blount
  • Patent number: 5679798
    Abstract: There is provided organosilane compounds containing one or more carboxyl acid group(s) that may be represented by the general formula: ##STR1## wherein: R which can be the same or different, are hydrogen,and monovalent hydrocarbon radicals and substituted hydrocarbon radicalsR.sup.1 which can be the same or different can be substituted or unsubstituted alkyl, substituted or unsubstituted aryl, alkenyl, alkynyl or --R.sup.2 --B.sub.n1 --F.sub.n --R.sup.3 ;x can be zero to 3;R.sup.2 is linear or branched alkylene of 1-12 carbon atoms, preferably propylene or isobutylene;B is --NR.sup.6, sulfur or oxygen;R.sup.6 is hydrogen or lower alkyl (C.sub.1-6);n.sup.1 is zero or 1;F is linear or branched alkylene of 1-10 carbon atoms, preferably ethylene;n is zero or 1, with the proviso that if n.sup.1 is 1, n is 1 and if n.sup.1 is 0, n is 0;R.sup.3 is ##STR2## R.sup.5 is hydrogen, lower alkyl (C.sub.1-6) or alkali metal.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: October 21, 1997
    Assignee: Mona Industries, Inc.
    Inventors: Abe Berger, Dennis L. Fost
  • Patent number: 5670492
    Abstract: Provided are DC-89 derivatives represented by the formula: ##STR1## wherein X represents Cl or Br, R represents hydrogen or COR.sup.1, and W represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention have excellent anti-tumor activity and are useful as anti-tumor agents.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: September 23, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
  • Patent number: 5656206
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 12, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 5654439
    Abstract: A novel 6-chloro-3-vinyl-pyridine of formula ##STR1## where X represents --H, --SO.sub.2 Ph, --CO.sub.2 Et, --COCH.sub.3 and --CHO; which is used for the synthesis of Epibatidine of formula ##STR2## by reacting said 6-chloro-3-vinyl pyridine with N-1-alkyl-2,5-di(trialkyl silyl) pyrrolidine of formula ##STR3## to obtain N-alkyl Epibatidine which is hydrogenated to obtain the Epibatidine.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: August 5, 1997
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ganesh Pandey, Trusar Damu Bagul, Gingipalli Lakshmaiah
  • Patent number: 5651923
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5648502
    Abstract: 4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R.sup.3 is (C.sub.1 -C.sub.6) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein, and removing the silyl group R.sub.3 Si--. The product is useful as an intermediate in making pharmaceutical products.
    Type: Grant
    Filed: July 7, 1995
    Date of Patent: July 15, 1997
    Assignee: Pfizer Inc.
    Inventors: Laurence E. Burgess, Gary R. Schulte
  • Patent number: 5623043
    Abstract: A silicone-containing phospholipid composition is provided having the general formula: ##STR1## wherein: A can be H, M or R--Y--; A, can be H, OH, OM or R--Y--O; A.sub.1 is selected from H, OH, OM or R--Y--O--; M is a cation; Y is alkylene or substantially alkylene; x is 0 or an integer from 1-5; and R is a quaternized organosilicone amidoamine reactant moiety of the formula: ##STR2## wherein: R.sub.10 is the silicone backbone chain to which at least one pyrrolidone containing amidoamine functional group is attached;R.sub.6 is hydrogen, alkyl, hydroxyalkyl, alkenyl cycloalkyl or polyoxyalkylene;R.sub.7 and R.sub.8 are selected from alkyl, hydroxyalkyl, carboxyalkyl and polyoxyalkylene;F is linear or branched alkylene; X.sup.- is an anion; n is 0 or 2; n.sup.1 is 0 or 1; n.sup.2 is 0 or 1; n.sup.3 is an integer from 2 to 12. B is --NR.sub.11 sulfur or oxygen, wherein R11 is hydrogen or lower alkyl; with the proviso that when n.sup.1 is 0 and n.sup.2 is 1, n.sup.1 is 1, when n is 2 and n.sup.2 is 1, n.sup.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: April 22, 1997
    Assignee: Mona Industries, Inc.
    Inventors: Dennis L. Fost, Abe Berger
  • Patent number: 5612480
    Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: March 18, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Thomas E. Barta, Richard A. Mueller
  • Patent number: 5596061
    Abstract: A polysiloxane composition is provided having the formula ##STR1## wherein: R.sub.1, can be R.sub.2 or at least one pyrrolidone containing group of the general formula: ##STR2## wherein; R.sub.5 is hydrogen, lower alkyl or alkali metal; F, is linear or branched alkylene of 1-12 carbon atoms; n is 0 or 2; n.sup.1 is 0 or 1; n.sup.2 is 0 or 1; and B is --NR.sub.9, sulfur or oxygen, wherein R, is hydrogen or lower alkyl; with the proviso that when n is 0 and n.sup.2 is 1, n.sup.1 is 1, when n is 2 and n.sup.2 is 1, n.sup.1 is 0 or 1 and when n is 2 and n.sup.2 is 0, n.sup.1 is 0;R.sub.2 is selected from alkyl, aryl and olefinic (vinyl);R.sub.3 and R.sub.4, are selected from alkyl, aryl, capped or uncapped polyoxyalkylene, alkaryl, aralkylene or alkenyl;a is an integer from 0 to 50,000; andb is an integer from 0 to 100.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: January 21, 1997
    Assignee: Mona Industries, Inc.
    Inventors: Abe Berger, Dennis L. Fost
  • Patent number: 5585509
    Abstract: Metallocene complexes of the general formula I ##STR1## where the substituents Y, M, x, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as described in the disclosure, and ligand systems of the general formula II ##STR2## as intermediates.
    Type: Grant
    Filed: March 1, 1995
    Date of Patent: December 17, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Franz Langhauser, David Fischer, J urgen Kerth, G unther Schweier, Hans-Herbert Brintzinger, Elke Barsties, Werner Roell
  • Patent number: 5536847
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: July 16, 1996
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
  • Patent number: 5525735
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: June 11, 1996
    Assignee: AFFYMAX Technologies NV
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5525734
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: June 11, 1996
    Assignee: Affymax Technologies N.V.
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5508427
    Abstract: A bisimide compound of the following general formula (I). ##STR1## (wherein each of the R's is an alkyl group having 1 to 4 carbon atoms, a phenyl group or a phenyl group substituted with an alkyl or alkoxy group having 1 to 4 carbon atoms, a plurality of these R's may be the same or different, each of the Z's is ##STR2## a plurality of these Z's may be the same or different, Y is an arylene group or an aryleneoxy group whose terminal oxygen atom bonds to (CH.sub.2).sub.n, n is an integer of 0 to 20, and m is an integer of 1 to 30.), and a process for the production of the above bisimide compound, which comprises reacting a bisamic acid corresponding to this bisimide compound in a cyclodehydration reaction.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: April 16, 1996
    Assignee: Tomoegawa Paper Co., Ltd.
    Inventors: Toshio Tagami, Yukinori Sakumoto, Takeshi Hashimoto
  • Patent number: 5502065
    Abstract: The present invention provides compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: March 26, 1996
    Assignee: Pfizer Inc.
    Inventors: Alan D. Brown, Roger P. Dickinson, Martin J. Wythes
  • Patent number: 5502206
    Abstract: The liquid-crystalline organosiloxanes containing, per molecule, at least one Si--C-bonded chiral tartarimide radical of the formula ##STR1## in which M, A.sup.5 and k are as defined in claim 1, can be employed as chiral filter materials, for decorative purposes and in optical elements.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: March 26, 1996
    Assignee: Consortium fu/ r elektrochemische Industrie GmbH
    Inventors: Ingo P. Zahn, Franz-Heinrich Kreuzer, Hans-Peter Weitzel
  • Patent number: 5492925
    Abstract: There are provided thienyl- and furylpyrrole compounds of formula I ##STR1## and their use for the control of insects and acarina. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects and acarina.
    Type: Grant
    Filed: August 31, 1993
    Date of Patent: February 20, 1996
    Assignee: American Cyanamid Company
    Inventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan, Jack K. Siddens, deceased
  • Patent number: 5461071
    Abstract: 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: Grant
    Filed: October 21, 1994
    Date of Patent: October 24, 1995
    Assignee: 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: 5455360
    Abstract: Disclosed are a conductive pyrrole derivative monomolecular film covalently bonded to a substrate surface and method of manufacturing the same, and a monomer used for forming the conductive pyrrole derivative monomolecular film and method of manufacturing the same. The invention relates to a monomolecular ultrathin film comprising 1-pyrrolyl groups and silicon groups. The monomer used for forming the film is provided by reacting .omega.-(1-pyrrolyl)-1-alkene compound to a monosilane derivative compound, in which three out of four hydrogen atoms of monosilane are replaced with halogen or alkoxy groups, in the presence of a transition metal catalyst. A substrate is dipped and held in a nonaqueous solution of the above-noted monomer, thus chemically bonding a monomolecular film to a substrate surface. Furthermore, a polypyrrole derivative ultrathin film is formed by the electrolytic or catalytic polymerization of the monomolecular film.
    Type: Grant
    Filed: August 18, 1993
    Date of Patent: October 3, 1995
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventors: Norihisa Mino, Kazufumi Ogawa, Toshinobu Ishihara, Mikio Endo, Tohru Kubota, Katsuya Takemura
  • Patent number: 5455353
    Abstract: A process for the production of a .beta.-aminoalcohol 2-[3(S)-amino-2(R)-hydroxy-4-phenylbutyl]-N-tert.butyl-decahydro-(4aS,8aS) -isoquinoline-3(S)-carboxamide of the formula ##STR1## via the oxazolidinone corresponding to the aminoalcohol 10, as well as intermediates occurring in this process.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: October 3, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5451685
    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: July 13, 1994
    Date of Patent: September 19, 1995
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
  • Patent number: 5426189
    Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.
    Type: Grant
    Filed: May 24, 1994
    Date of Patent: June 20, 1995
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Raymond Murphy
  • Patent number: 5401765
    Abstract: A class of 1,4,5-triphenyl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I ##STR1## wherein R.sup.1 is one or more groups independently selected from hydrido, methyl, ethyl, methoxy, ethoxy, methylthio, methylsulfinyl, methylsulfonyl, hydroxy, nitro, amino, N-methylamino, acetamido, trifluoromethyl, bromo, iodo, fluoro and chloro; wherein R.sup.2 is selected from hydrido, methyl, ethyl, cyano, trifluoromethyl, difluorochloromethyl, difluoromethyl, pentafluoroethyl and heptafluoropropyl; wherein R.sup.3 is one or more groups independently selected from hydrido, methyl, ethyl, methoxy, ethoxy, methylthio, methylsulfinyl, methylsulfonyl, hydroxy, nitro, amino, N-methylamino, acetamido, trifluoromethyl, bromo, iodo, fluoro and chloro; and wherein R.sup.4 is methyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 30, 1993
    Date of Patent: March 28, 1995
    Assignee: G. D. Searle
    Inventor: Len F. Lee
  • Patent number: 5391749
    Abstract: Substituted naphthacenediones of the formula I ##STR1## in which R.sup.1 to R.sup.8 are H and at least one of R.sup.1 to R.sup.8, for example R.sup.2 and R.sup.3 or R.sup.2 and R.sup.6, are, for example, C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 alkenoxy, C.sub.1 -C.sub.20 -alkylsulfinyl, --CN, --CF.sub.3, --NO.sub.2, --Si(CH.sub.3).sub.3 or --COO(C.sub.1 -C.sub.12 alkyl), are suitable, when incorporated into polymers having hydroxyalkyl groups, for currentless deposition of metals onto the polymer surface. They are in some cases suitable as photoinitiators.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: February 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Marcus Baumann, Jurgen Finter, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
  • Patent number: 5391763
    Abstract: Quinolone carboxylic acids 7 -substituted by azabicyclo groups have antibacterial activity.
    Type: Grant
    Filed: August 26, 1993
    Date of Patent: February 21, 1995
    Assignee: Pfizer Inc.
    Inventor: Katherine E. Brighty
  • Patent number: 5385929
    Abstract: 2-(4-Fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[( hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, and their lactone forms, and salts and solyates thereof, inhibit cholesterol biosynthesis, and thus are useful in treating hypercholesterolemia.
    Type: Grant
    Filed: May 4, 1994
    Date of Patent: January 31, 1995
    Assignee: Warner-Lambert Company
    Inventors: Susan M. Bjorge, Ann E. Black, Bruce D. Roth, Thomas Woolf
  • Patent number: 5384412
    Abstract: Intermediates useful in preparing the calicheamicin and esperamicin oligosaccharides, and particularly the sulfur- and O-substituted hydroxylamine-containing B ring of both oligosaccharides, are disclosed as are methods of making and using the same, including the preparation of chimeric antibiotics using the same.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: January 24, 1995
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Robert D. Groneberg, Erwin P. Schreiner, Wilhelm Stahl
  • Patent number: 5354772
    Abstract: Compounds of the formula ##STR1## wherein one of R and R.sub.o is ##STR2## and the other is primary or secondary C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-6 cycloalkyl or phenyl-(CH.sub.2).sub.m --,whereinR.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5a is hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, andm is 1, 2 or 3, with the provisos that both R.sub.5 and R.sub.5a must be hydrogen when R.sub.4 is hydrogen, R.sub.5a must be hydrogen when R.sub.5 is hydrogen, not more than one of R.sub.4 and R.sub.5 is trifluoromethyl, not more than one of R.sub.4 and R.sub.5 is phenoxy, and not more than one of R.sub.4 and R.sub.5 is benzyloxy,R.sub.2 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.3-6 cycloalkyl, C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: October 11, 1994
    Assignee: Sandoz Pharm. Corp.
    Inventor: Faizulla G. Kathawala
  • Patent number: 5352797
    Abstract: The coupling agent is comprised of a pyrrolidyl group capable of being incorporated in the chain of an electroconducting polymer, and a silane group --Si(OR.sup.1).sub.3 which may be chemically bound to a glass substrate in order to form an adherent coating of said polymer. It is obtained by an addition reaction implementing an epoxide function and a primary or secondary amine function.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: October 4, 1994
    Assignee: Office National d'Etudes et de Recherches Aerospatiales
    Inventors: Bertrand Bloch, Andre Attias, Jacques Ancelle, Claude Andrieux, Pierre Audebert
  • Patent number: 5349069
    Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: September 20, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John K. Thottathil, Wen S. Li
  • Patent number: 5346910
    Abstract: Maleimide derivatives of oxotremorine and their alkylthiol addition products having the general formulae: ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl, hydroxyalkyl, acyloxy, trialkylsilyloxy or R.sub.1 and R.sub.2 taken together are substituted or unsubstituted pyrrolidine or piperidine, and pharmaceutical compositions for the treatment of central cholinergic disfunction.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: September 13, 1994
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Herbert J. Brabander
  • Patent number: 5342982
    Abstract: Silicon-containing organic compounds useful as starting materials of functional polymer materials, as well as a process for preparing the same, are provided. The silicon-containing organic compounds are represented by the following general formula: ##STR1## where R.sup.1 is a .pi. conjugated type divalent organic group having 2 to 30 carbon atoms, R.sup.2 is a hydrocarbon group having 1 to 30 carbon atoms, X.sup.1 is a halogen atom, m and n satisfy the conditions of 1.ltoreq.m.ltoreq.2 and n.gtoreq.2, respectively. A compound of the above general formula is prepared by reacting an organometallic compound of the following general formula:M.sup.1 -R.sup.1 -M.sup.2where M.sup.1 and M.sup.2 are each a metal selected from Group 1, 2 and 12 metals in the Periodic Table, with a silane compound of the following general formula: ##STR2## where R.sup.2 is a hydrocarbon group having 1 to 30 carbon atoms, X.sup.1, X.sup.2 and X.sup.3 are each a halogen atom.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: August 30, 1994
    Assignee: Nippon Oil Company, Limited
    Inventors: Masaki Minami, Keizo Ikai, Mitsuo Matsuno
  • Patent number: 5334728
    Abstract: Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofur an, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: August 2, 1994
    Assignee: The Trustees of The University of Pennsylvania
    Inventors: Hank F. Kung, Raymond Murphy
  • Patent number: 5328928
    Abstract: This invention provides new N-acylated arylpyrroles effective for the control of insects, acarids, nematodes, fungi and mollusks and useful for the protection of growing plants from the destructive actions of said pests. The invention also provides pesticidal compositions containing the new N-acylated arylpyrroles and methods for the preparation of thereof.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: July 12, 1994
    Assignee: American Cyanamid Company
    Inventors: Roger W. Addor, Stephen F. Donovan, Robert E. Diehl, Kenneth A. Kremer
  • Patent number: 5298625
    Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3 XII.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: March 29, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John K. Thottathil, Wen S. Li
  • Patent number: 5296610
    Abstract: An N-substituted polyamideimide essentially composed of identical or different repeating units of the formula I ##STR1## where R.sup.1 is one of the following tetravalent aromatic radicals ##STR2## and X is a bond or one of the following linkers ##STR3## where R.sup.2 and R.sup.4 are each, independently of one another, one of the following divalent aromatic radicals ##STR4## and where X has the abovementioned meanings and where R.sup.3 is hydrogen or a monovalent radical such as C.sub.1 -C.sub.6 -alkyl or phenyl, and the C.sub.1 -C.sub.6 -alkyl-, C.sub.1 -C.sub.6 -alkoxy-, aryl- or halogen-substituted derivatives thereof, and precursors (monomers) therefor, are described.
    Type: Grant
    Filed: February 4, 1993
    Date of Patent: March 22, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Wolf, Juergen Koch
  • Patent number: 5284959
    Abstract: Poly(dianhydride) compounds having formulae (I) and (II): ##STR1## where m is 0 to 50. ##STR2## wherein n is 0 to 20 and X is bond junction, oxygen atom, sulfur atom, SO.sub.2, C(CF.sub.3), CO, C(CH.sub.3).sub.2, CF.sub.2 --O--CF.sub.2, CH.sub.2, and CHOH.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: February 8, 1994
    Assignee: Olin Corporation
    Inventors: Bruce A. Marien, Keith O. Wilbourn
  • Patent number: 5270331
    Abstract: Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.
    Type: Grant
    Filed: January 26, 1993
    Date of Patent: December 14, 1993
    Assignee: Pfizer, Inc.
    Inventors: Wayne E. Barth, Kelvin Cooper, Edward F. Kleinman, Lawrence A. Reiter, Ralph P. Robinson
  • 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: 5258357
    Abstract: Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur;R.sup.1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl;R.sup.2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl or naphthyl, a substituted or unsubstituted 5- to 6-membered heterocyclic structure or one of the groups stated for R.sup.1, orR.sup.1 and R.sup.2 together are a 4- to 7-membered chain which contains, in addition to methylene groups, one of the following groups as ring member: oxygen, sulfur, N-methyl or carbonyl;R.sup.3 and R.sup.4 are each nitro, cyano, halogen, substituted or unsubstituted amino, alkoxy, alkylthio, a substituted or unsubstituted 5- to 6 -membered heterocyclic structure, substituted or unsubstituted alkenyl, alkynyl, phenyl, phenoxy or phenylthio, or one of the groups stated for R.sup.1 ;R.sup.5 is formyl, 4,5-dihydrooxazol-2-yl or COYR.sup.6 (Y=O,S);R.sup.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: November 2, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Muenster, Gerd Steiner, Wolfgang Freund, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5256671
    Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;the dotted line represents an optional double bond;X represents H, --OH, .dbd.O or halo;R.sup.1 represents H, phenyl or thienyl, which phenyl or thienyl groups may be optionally substituted by halo or trifluoromethyl;R.sup.2 represents phenyl, thienyl or benzyl, any of which groups may be optionally substituted by halo or trifluoromethyl; 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, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.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 29, 1992
    Date of Patent: October 26, 1993
    Assignee: Merck Sharp & Dohme, Limited
    Inventors: Tamara Ladduwahetty, Christopher J. Swain
  • 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
  • Patent number: RE35802
    Abstract: The coupling agent is comprised of a pyrrolidyl group capable of being incorporated in the chain of an electroconducting polymer, and a silane group --Si(OR.sup.1).sub.3 which may be chemically bound to a glass substrate in order to form an adherent coating of said polymer. It is obtained by an addition reaction implementing an epoxide function and a primary or secondary amine function.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: May 19, 1998
    Assignee: Office National d'Etudes et de Recherches Aerospatiales
    Inventors: Bertrand Bloch, Andre Attias, Jacques Ancelle, Claude Andrieux, Pierre Audebert