Silicon Containing Patents (Class 546/14)
  • Patent number: 6031095
    Abstract: This invention relates to a highly selective process for preparation of E-.omega.-phenyl-.omega.-(3-pyridyl)-.omega.-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefor.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: February 29, 2000
    Assignee: Eli Lilly and Company
    Inventors: Katrina Ann Nelson, Joseph John Nunes
  • Patent number: 6013814
    Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: January 11, 2000
    Assignee: Research Institute for Medicine and Chemistry, Inc.
    Inventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal, Gaddam Subba Reddy
  • Patent number: 6005128
    Abstract: The present invention provides a silacyclopentadiene derivative represented by the following Formula (1): ##STR1## wherein X.sub.1 and Y.sub.1 represent independently a halogen atom, an amino group, a hydroxyl group, or an amino group or a hydroxyl group each having a substituent; R.sub.1 to R.sub.4 represent independently a hydrogen atom, a halogen atom, an alkyl group, an amino group, a silyl group, an aryl group, a cyano group, or the respective groups describe above each having a substituent; out of the groups represented by R.sub.1 to R.sub.4, those adjacent may be combined with each other to form rings; when R.sub.1 and R.sub.4 are phenyl groups or when combined are R.sub.1 with R.sub.2 and R.sub.3 with R.sub.4 respectively to form benzene rings, X.sub.1 and Y.sub.1 are not a chlorine atom or a hydroxyl group; and when R.sub.1 and R.sub.4 are methyl groups, X.sub.1 and Y.sub.1 are not bromine atoms.
    Type: Grant
    Filed: March 10, 1998
    Date of Patent: December 21, 1999
    Assignee: Chisso Corporation
    Inventors: Kohei Tamao, Shigehiro Yamaguchi, Manabu Uchida
  • Patent number: 5998464
    Abstract: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Richard L. Tolman
  • Patent number: 5994327
    Abstract: A process for the preparation of 14-alkoxyindolomorphinans and 14-alkoxybenzofuranomorphinans is disclosed. The process facilitates the preparation of a large variety of 14-alkoxy substituted indolomorphinans and benzofuranomorphinans in which a 3-hydroxy substituent is present.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: November 30, 1999
    Assignee: Astra AB
    Inventors: Helmut Schmidhammer, Peter Schwarz, Zhong-Yong Wei
  • Patent number: 5990308
    Abstract: This invention relates to a highly selective process for preparation of E-.omega.-phenyl-.omega.-(3-pyridyl)-.omega.-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefore.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: November 23, 1999
    Assignee: Eli Lilly and Company
    Inventors: Katrina Ann Nelson, Joseph John Nunes
  • Patent number: 5977140
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 2, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5969140
    Abstract: Naphthalene derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: October 19, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
  • Patent number: 5965761
    Abstract: The invention provides novel cross-linkable, photoactive silane derivatives and mixtures with 3-aryl-acrylic acid esters and amides. The present invention also provides orienting layers for liquid crystals, and non-structured and structured optical elements and multi-layer systems based on the silane mixtures and derivatives.
    Type: Grant
    Filed: October 24, 1997
    Date of Patent: October 12, 1999
    Assignee: Rolic AG
    Inventors: Richard Buchecker, Fran.cedilla.ois Herzog, Guy Marck, Andreas Schuster
  • Patent number: 5955606
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: September 21, 1999
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5939573
    Abstract: A di(polycyclic amino)dialkoxysilane which is of value as an auxiliary catalyst component for polymerizing an .alpha.-olefin to produce an .alpha.-olefin polymer having a high stereoregularity and a broad molecular weight distribution is prepared by reacting a secondary polycyclic-amine compound with an organomagnesium compound in an ether solvent, to produce a polycyclic-amido magnesium compound, and reacting the polycyclic-amido magnesium compound with a tetraalkoxysilane in a solvent mixture of an ether solvent and an inert hydrocarbon solvent.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: August 17, 1999
    Assignee: Ube Industries, Ltd.
    Inventors: Shigeru Ikai, Yasuhisa Sakakibara, Toshifumi Fukunaga
  • Patent number: 5935968
    Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: ##STR1## to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: August 10, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Joanne Waldstreicher, Georgianna S. Harris
  • Patent number: 5932587
    Abstract: The heterocyclic-fused pyridines are prepared by reaction of the corresponding heterocyclic-fused pyridine aldehydes with appropriately substituted Grignard or Wittig reagents. The heterocyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of dislipidaemia and arteriosclerosis.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: August 3, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Carsten Schmeck, Matthias Muller-Gliemann, Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher
  • Patent number: 5925653
    Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O).sub.q where q=0, 1 of 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: July 20, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Wolfgang Schaper, Martin Markl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5919944
    Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: July 20, 1998
    Date of Patent: July 6, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 5919798
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 6, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5917045
    Abstract: A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a ring nitrogen atom and bears, at the 4 position, an amino nitrogen atom, carrying a hydrogen. The remaining unsatisfied valences, if present, of the ring nitrogen atoms or the amino nitrogen atoms, or all, are occupied by one or more alkyl substituents. Each of the 1,8-naphthalimide ring system is free of an azo substituent and is also free of a nucleofuge. 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 can cause structural changes in lipid and any associated proteins and polypeptides, extra- or intra-cellular or transmembrane, leading to polymerization and crosslinking.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 29, 1999
    Assignee: MicroBioMed Corporation
    Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5912347
    Abstract: A process for preparing a morphinan derivative by providing a dihydrofuranyl bridged tetracycle halide of the formula (19) ##STR1## in which X is halogen, R is an alkyl group of from 1 to about 10 carbon atoms, and R.sub.1 is a protecting group. The pentacycle halide is converted into a morphinan derivative of formula (20) ##STR2## in which R is a previously defined.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: June 15, 1999
    Assignee: Mallinckrodt Inc.
    Inventors: Tomas Hudlicky, Gabor Butora
  • Patent number: 5910491
    Abstract: Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.
    Type: Grant
    Filed: August 19, 1997
    Date of Patent: June 8, 1999
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Pavankumar N.V. Petluru, Dasharatha Reddy, Dhanabalan Murali, Kochat Haridas, Peddaiahgari Seetharamulu, Shijie Yao
  • Patent number: 5869499
    Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.
    Type: Grant
    Filed: March 3, 1996
    Date of Patent: February 9, 1999
    Assignee: Pfizer Inc
    Inventors: Kunio Satake, Hiroaki Wakabayashi
  • Patent number: 5864038
    Abstract: Novel compounds having the structure: ##STR1## where X in .beta. configuration is phenyl, naphthyl; 2,3 or 4-iodophenyl; 2,3 or 4-(trimethylsilyl)phenyl; 3,4,5 or 6-iodonaphthyl; 3,4,5 or 6-(trimethylsilyl)naphthyl; 2,3 or 4-(trialkylstannyl)phenyl; or 3,4,5 or 6-(trialkylstannyl)naphthylY in .beta. configuration is Y.sub.1 or Y.sub.2,whereY.sub.1 is 2-fluoroethoxy, 3-fluoropropoxy, 4-fluorobutoxy, 2-fluorocyclopropoxy, 2 or 3-fluorocyclobutoxy, R,S 1'-fluoroisopropoxy, R 1'-fluoroisopropoxy, S 1'-fluoroisopropoxy, 1',3'-difluoroisopropoxy, R,S 1'-fluoroisobutoxy, R 1'-fluoroisobutoxy, S 1'-fluoroisobutoxy, R,S 4'-fluoroisobutoxy, R 4'-fluoroisobutoxy, S 4'-fluoroisobutoxy, or 1',1'-di(fluoromethyl)isobutoxy, andY.sub.
    Type: Grant
    Filed: August 17, 1995
    Date of Patent: January 26, 1999
    Assignee: Emory university
    Inventors: Mark M. Goodman, Bing Zhi Shi, Robert N. Keil
  • Patent number: 5852030
    Abstract: A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: December 22, 1998
    Assignee: Toray Industries, Inc.
    Inventors: Hiroshi Nagase, Akira Mizusuna, Koji Kawai, Izumi Nakatani
  • Patent number: 5849749
    Abstract: The 6-(hydroxymethyl-ethyl)pyridines are prepared by a process in which the 3-hydroxymethylpyridines which are hydroxyl-protected in the 6-position are oxidized to the 3-aldehyde, this is then converted into the corresponding oxoheptenoic acid derivative using a Wittig-Homer reaction, after this the oxo group is reduced to the hydroxyl group and then the isomers are separated by chromatography. The 6-(hydroxymethyl-ethyl)pyridines are suitable as active compounds in medicaments, in particular in medicaments having antiarteriosclerotic activity.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: December 15, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Fey, Rolf Angerbauer, Delf Schmidt, Hilmar Bischoff, Wolfgang Kanhai, Martin Radtke, Wolfgang Karl
  • Patent number: 5849750
    Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: December 15, 1998
    Assignee: California Institute of Technology
    Inventor: Andrew Gordon Myers
  • Patent number: 5849768
    Abstract: .alpha.-Unsaturated amines of the formula: ##STR1## wherein X.sup.1 and X.sup.2 are such that one is an electron-attracting group with the other being a hydrogen atom or an electron-attracting group; R.sup.1 is a group attached through a nitrogen atom; R.sup.2 is a hydrogen atom or a group attached through a carbon, nitrogen or oxygen atom; n is an integer equal to 0, 1 or 2; A is a heterocyclic group or a cyclic hydrocarbon group, and salts thereof and their agrochemical use as insecticidal and/or miticidal agents are described.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 15, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Isao Minamida, Koichi Iwanaga, Tetsuo Okauchi
  • Patent number: 5849914
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Patent number: 5834447
    Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)--amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.
    Type: Grant
    Filed: December 8, 1995
    Date of Patent: November 10, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5808124
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: September 15, 1998
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5777008
    Abstract: Novel oligomeric compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, are disclosed as stabilisers for protecting organic material against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 7, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Rita Pitteloud
  • 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: 5777122
    Abstract: A process for cleaving cinchona alkaloids to a quinoline derivative and an enantiomerically pure, functionalized 1-azabicyclo(2.2.2)octane, includes treating a cinchona alkaloid with a complex metal hydride while simultaneously oxidizing by exposure to air in an ether or tetrahydrofuran. Enantiomerically pure 1-azabicyclo(2.2.2)octanes of the formula ##STR1## in which R is hydrogen, a straight-chain or branched alkoxycarbonyl group with 1 to 12 carbon atoms, a straight-chain or branched alkyl group with 1 to 12 carbon atoms, alkylated silyl groups, or a substituted phenyl or benzyl substituent, are also provided.
    Type: Grant
    Filed: February 5, 1997
    Date of Patent: July 7, 1998
    Assignee: Buchler GmbH
    Inventor: H. Martin R. Hoffmann
  • Patent number: 5760018
    Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: June 2, 1998
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Richard Thomas Lewis, Angus Murray MacLeod, Graeme Irvine Stevenson
  • Patent number: 5756422
    Abstract: Substituted quinoline compounds, processes for their preparation, composition containing them, and their use as safenersCompounds of the formula I and salts thereof ##STR1## in which R.sup.1 ?lacuna! CN, C(.dbd.Z)--Q(A.sub.i X.sub.i).sub.q --R, --C(.dbd.Z)--QR*, 1,2,3,4-tetrazol-5-yl, 1,3,4-triazol-2-yl, 1,3-oxazol-2-yl,and the remaining radicals are as defined in claim 1, are suitable for use as safeners for protecting crop plants such as, for example, cereals, rice and maize, against herbicide damage.Some of the compounds are known and some are novel and they can be prepared from quinolin-8-oxy derivatives by the processes of claim 7.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: May 26, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Xenia Holdgrun, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5750680
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: May 12, 1998
    Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & Technology
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5744604
    Abstract: Methyl (3R, 6E)-3-?(tert-butyldimethylsilyl)oxy!-7-?2', 6'-diisopropyl-4'-(4"-fluorophenyl)-5'-(methoxymethyl)pyridin-3'-yl!-5-oxy -6-heptenoate or other 3-oxy-5-oxo-6-heptenoic acid derivative is prepared by the reaction of an aromatic aldehyde and an oxyglutaric acid derivative in an aliphatic alcohol containing a small amount of water in the presence of an alkali metal carbonate or hydrogen carbonate.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: April 28, 1998
    Assignee: Ube Industries, Ltd.
    Inventors: Katsumasa Harada, Akio Matsushita, Yasuhiro Kawachi, Hiroshi Sasaki
  • Patent number: 5741794
    Abstract: Compounds of formula (I), wherein: A represents: a) a --VR.sup.6 group wherein v is --C(.dbd.O), --C(.dbd.O)O--, --CH.sub.2 O--, --CH.sub.2 OC(.dbd.O)--, --C(.dbd.S)--, --CH.sub.2 OC(.dbd.O)NH--, --C(.dbd.S)O--, --CH.sub.2 S--, --C(.dbd.O)NHSO.sub.2 --, --SO.sub.2 NHC(.dbd.O)-- or --CH.sub.2 OSiPh.sub.2 --; b) a --CH.sub.2 NR.sup.9 R.sup.10 group or a --CONR.sup.9 R.sup.10 group wherein each of R.sup.9 and R.sup.10 is independently hydrogen, -alkyl-, -alkenyl-, -alkynyl, -cycloalkyl, -cycloalkenyl, pyridyl (any of which may optionally be substituted) or a group --D as defined above or R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring; c) a group Y where Y is a 5- or 6-membered optionally substituted heterocyclic ring containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or d) a group --CH.sub.2 Y or --C(.dbd.
    Type: Grant
    Filed: September 1, 1994
    Date of Patent: April 21, 1998
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Stephen Arthur Bowles, Christopher David Floyd, Andrew Miller, Mark Whittaker, Lars Michael Wood
  • Patent number: 5741795
    Abstract: Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.
    Type: Grant
    Filed: October 17, 1996
    Date of Patent: April 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Susan D. Aster, Donald W. Graham, Derek J. Von Langen
  • Patent number: 5739137
    Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: February 28, 1996
    Date of Patent: April 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
  • Patent number: 5728856
    Abstract: Stable silylenes, and analog carbenes are prepared.
    Type: Grant
    Filed: January 18, 1996
    Date of Patent: March 17, 1998
    Inventor: Michael Denk
  • Patent number: 5726195
    Abstract: Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is ?S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1-?5-?4-?(5-nitro-2-thienyl)ethynyl!ph enyl!-2H-tetrazol-2-yl!-D-allo-heptitol 7-(2-amino-3-methyl-1-oxopentyl)sulfamate. These compounds inhibit isoleucyl-tRNA synthetases and are useful as antimicrobial and antiparasitic agents.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: March 10, 1998
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Jason M. Hill, Guixue Yu, Youe-Kong Shue, Thomas M. Zydowsky, Julius Rebek
  • Patent number: 5726226
    Abstract: Compounds of 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; R.sub.1 and R.sub.3, which may be identical or different, are for example C.sub.1 -C.sub.18 alkyl or phenyl; R.sub.2 is C.sub.2 -C.sub.12 alkylene; G is for example a group of formula (IId) ##STR2## in which R.sub.5 and R.sub.6 are for example hydrogen; R.sub.4 is for example C.sub.1 -C.sub.18 alkyl; L.sub.1 has for example any one of the meanings given to R.sub.1 or is a group (R.sub.28).sub.3 SiO-- where R.sub.28 is C.sub.1 -C.sub.18 alkyl; and L.sub.2 is for example hydrogen, Na, K, C.sub.1 -C.sub.8 alkyl or a group (R.sub.28).sub.3 Si-- with R.sub.28 as defined above.The compounds of formula (I) are useful as light, heat and oxidation stabilizers for organic materials.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: March 10, 1998
    Assignee: Ciba Specialty Chemcials Corporation
    Inventors: Valerio Borzatta, Primo Carrozza
  • Patent number: 5726162
    Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: March 10, 1998
    Assignee: Rohm and Haas Company
    Inventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
  • Patent number: 5723450
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, halogen, an aliphatic radical or an aromatic radical, X is O, S or optionally substituted imino, Y is a bond or an optionally substituted bivalent hydrocarbon radical and Z is optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and their use as pesticides, in particular as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: March 3, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5721297
    Abstract: Novel piperidyl organosiloxanes, well adapted for the light/UV-stabilization of a wide variety of polymer substrates, e.g.
    Type: Grant
    Filed: July 1, 1992
    Date of Patent: February 24, 1998
    Assignee: Rhone-Poulenc Chimie
    Inventors: Michel Gay, Sylvie Lavault
  • Patent number: 5719158
    Abstract: Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek von Langen
  • Patent number: 5710102
    Abstract: Difluorovinylsilane compounds having the structural formula I ##STR1## and compositions thereof, and methods for the control of insect and acarid pests and protection of plants.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: January 20, 1998
    Assignee: American Cyanamid Company
    Inventors: Keith Douglas Barnes, Yulin Hu
  • Patent number: 5705513
    Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.
    Type: Grant
    Filed: December 28, 1994
    Date of Patent: January 6, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5703192
    Abstract: A new family of polyorganometallosiloxane-2- or -4-pyridine compounds are provided for corrosion resistant coatings on light metals such as aluminum, magnesium, zinc, steel and their allows. The novel compounds contain backbones modified by metal alkoxides, metallocenes and metallophthalocyanates where the metal is Zr, Ti, Mo, V, Hf, Nb, Si, B and combinations thereof. Methods of making the new compounds are also provided.
    Type: Grant
    Filed: November 29, 1995
    Date of Patent: December 30, 1997
    Assignee: Associated Universities, Inc.
    Inventor: Toshifumi Sugama
  • Patent number: 5703100
    Abstract: In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 30, 1997
    Assignee: SIBIA Neurosciences, Inc.
    Inventors: Ian A. McDonald, Jeffrey P. Whitten, Nicholas D. Cosford