Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/152)
  • Patent number: 5801246
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 1, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Patent number: 5766510
    Abstract: A process for producing a liquid crystalline compound represented by the following general formula (A): ##STR1##
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: June 16, 1998
    Assignee: Dai Nippon Printing Co., Ltd.
    Inventors: Junichi Hanna, Masahiro Funahashi, Masanori Akada, Masayuki Ando, Yozo Kosaka
  • Patent number: 5733648
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5714479
    Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: February 3, 1998
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
  • Patent number: 5698574
    Abstract: The present invention relates to 5-membered heteroaryl-oxazolidinones, to processes for their preparation and to their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: July 17, 1995
    Date of Patent: December 16, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Riedl, Dieter Habich, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
  • Patent number: 5684152
    Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, William K. Hagmann
  • Patent number: 5672583
    Abstract: Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: September 30, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Kevin Chapman, William Hagmann, Philippe Durette, Craig Esser, Ihor Kopka, Charles Caldwell
  • Patent number: 5670528
    Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 - are hydrogen or alkyl,Y is a group ##STR2## --O--CH.sub.2, --CH.sub.2 --O--, --S--CH.sub.2 --, --CH.sub.2 --S--, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 --O--N.dbd.C(R')-- andR is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: September 23, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5668148
    Abstract: Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1## wherein: Ar1 and Ar2 can be independantly aromatic, heteroaromatic, or condensed heteroaromatic unsubstituted or substituted with amino, alkoxy, sulfonamido, alkyl, heteroalkyl, halo;m is 0 or 1;n is 0, 1, or 2;het is an aromatic or nonaromatic heterocyclic ring, substituted with alkyl, halo, or alkoxy substituents; andX is a branched or straight chain aliphatic or halogen substituent.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: September 16, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Linda S. Payne, Steven D. Young, Mary Jo L. Zaborowski
  • Patent number: 5656261
    Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: August 12, 1997
    Assignees: The Picower Institute for Medical Research, Alteon Inc.
    Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
  • 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: 5599825
    Abstract: There are provided methine compounds having the following structure and their analogs, with a high solubility and are usefull as an active ingredient for pharmaceutical composition for treatment of cancer: ##STR1##
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: February 4, 1997
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
  • Patent number: 5576432
    Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: November 19, 1996
    Assignee: Eastman Kodak Company
    Inventors: Roger Lok, Antony J. Williams
  • Patent number: 5534532
    Abstract: This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: January 25, 1995
    Date of Patent: July 9, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert A. Groneberg, John R. Regan, Kent W. Neuenschwander, Anthony C. Scotese
  • Patent number: 5530117
    Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: June 25, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
  • Patent number: 5527914
    Abstract: Methine compounds are described, which can be represented by general formula [Ic]: ##STR1##
    Type: Grant
    Filed: May 3, 1994
    Date of Patent: June 18, 1996
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Takanori Hioki, Tadashi Ikeda
  • Patent number: 5525436
    Abstract: The subject invention relates to solid polymer electrolyte membranes comprising proton conducting polymers stable at temperatures in excess of 100.degree. C., the polymer being basic polymer complexed with a strong acid or an acid polymer. The invention further relates to the use of such membranes in electrolytic cells and acid fuel cells. Particularly, the invention relates to the use of polybenzimidazole as a suitable polymer electrolyte membrane.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: June 11, 1996
    Assignee: Case Western Reserve University
    Inventors: Robert F. Savinell, Morton H. Litt
  • Patent number: 5523312
    Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 4, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5519136
    Abstract: A radiation-sensitive compound has the general formula ##STR1## wherein A represents the ring members required to complete a 5- or 6-membered heterocyclic ring which may optionally be fused to an optionally substituted aromatic nucleus,B represents H, acryl, aroyl, heterocyclyl carbonyl or ##STR2## R represents an optionally substituted alkyl group, E and G, which may be the same or different, each represents H or CH.sub.p X.sub.3-p,J and K, which may be the same or different, each represents an aryl or heterocyclic group, which may optionally include a substitutent additional to E or G,X represents Cl or Br, andm, n and p, which may be the same or different, each represents an integer equal to 0, 1 or 2.The compound can be used to form radiation sensitive compositions for the production of radiation sensitive plates in lithographic printing plate manufacture.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: May 21, 1996
    Inventor: John R. Wade
  • Patent number: 5502201
    Abstract: The title compounds of the formula ##STR1## in which R.sup.1 and R.sup.2, independently of one another, represent hydrogen, straight-chain or branched C.sub.1 -C.sub.4 -alkyl, straight-chain or branched C.sub.1 -C.sub.4 -alkoxy, nitro, fluorine, chlorine, bromine, SO.sub.2 Cl, cyano or SO.sub.2 -C.sub.1 -C.sub.4 -alkyl, andX represents sulphur or oxygen,can be prepared from the corresponding 2-mercapto-benzothiazoles or 2-mercapto-benzoxazoles by chlorination with thionyl chloride in the presence of phosphorous acid compounds of the formulaYP(OR.sup.5).sub.2 (III),in whichR.sup.5 represents hydrogen, straight-chain or branched, substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl, phenyl or C.sub.7 -C.sub.10 -aralkyl andY represents hydrogen or OR.sup.5.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: March 26, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventor: Volker Ka/ ss
  • Patent number: 5496942
    Abstract: A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: March 5, 1996
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
  • Patent number: 5496826
    Abstract: New central nervous system agents conform to formula I: ##STR1## wherein R=H or C.sub.1-4 alkoxy;X=CH or N;Y=NH, O or S;Z=C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-3 alkenyl, NH.sub.2, C.sub.1-4 alkylamino, or C.sub.1-4 alkoxyalkyl, with the proviso that Z may not be CH.sub.3 when R=H, X=CH, and Y=NH and Z may not be CH.sub.3 when R=H, X=N and Y=NH and NHC(O)Z is in the para- position.
    Type: Grant
    Filed: September 2, 1994
    Date of Patent: March 5, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brett T. Watson, Astrid A. Ortiz
  • Patent number: 5484928
    Abstract: Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: January 16, 1996
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Hubert Sturm, Heinrich Thaler, Werner Veit
  • Patent number: 5476945
    Abstract: A methine compound represented by the following formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2 each represent a non-metallic atomic group necessitated for forming a five-membered or six-membered, nitrogen-containing heterocyclic ring, R.sub.1 and R.sub.2 each represent an alkyl group, X represents an inorganic anion, k represents a number necessitated for adjusting the electric charge of the molecule to zero, and n represents 0 or 1; with the proviso that when n is 1, the five-membered or six-membered, nitrogen-containing heterocyclic ring formed by Z.sub.2 is cationic, k is not zero and X represents chloride ion. The compound is useful as a spectral sensitizing dye and an antitumor agent.
    Type: Grant
    Filed: October 19, 1993
    Date of Patent: December 19, 1995
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Akihiko Ikegawa, Toshinao Ukai, Masayuki Kawakami
  • Patent number: 5466813
    Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: November 14, 1995
    Assignee: Eastman Kodak Company
    Inventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
  • Patent number: 5463068
    Abstract: Organic compounds of reduced sulphur content and sulphur-free organic compounds can be prepared from organic mercapto and/or disulphide compounds in a particularly advantageous manner by hydrogenolytic elimination of hydrogen sulphide if the elimination of hydrogen sulphide is carried out in the presence of an organic solvent by means of an aqueous, non-oxidizing, strong acid and elemental iron, aluminium and/or zinc in the presence of catalytic amounts of nickel and/or cobalt.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: October 31, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ferdinand Hagedorn, Helmut Fiege, Hans-Joachim Traenckner
  • Patent number: 5424442
    Abstract: A water-soluble methine compound represented by the following general formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents a non-metallic atomic group required for forming a 5-membered or 6-membered nitrogen-containing heterocyclic ring; R.sub.1 and R.sub.2, which may be the same or different, each represents an alkyl group; Q.sub.1 and Q.sub.2 each represents an atomic group required, in combination, for forming a 4-thiazolidinone ring, a 5-thiazolidinone ring, a 4-imidazolidinone ring, a 4-oxazolidinone ring, a 5-oxazolidinone ring, a 5-imidazolidinone ring or a 4-dithiolanone ring; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5, which may be the same or different, each represents a methine group; R represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group; m represents 1 or 2; i and h each represents 0 or 1; l represents 1 or 2; and j and k each represents 0, 1, 2 or 3.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: June 13, 1995
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Koya, Toshinao Ukai, Haruo Takei
  • Patent number: 5391772
    Abstract: Described is a process for converting an alcohol to an azide with S.sub.N 2 inversion using a phosphoryl azide, e.g. diphenylphosphoryl azide (DPPA). Good yields of azide in high enantiomeric excess can be achieved specifically for benzylic alcohols and alpha-hydroxy alkyl esters. The process is carried at preferably room temperature in an inert dry aprotic solvent, e.g. toluene, and in the presence of a proton acceptor, e.g. 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to afford high yields of high enantiomeric purities.
    Type: Grant
    Filed: July 8, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Andrew S. Thompson, Edward J. J. Grabowski
  • Patent number: 5389620
    Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: February 14, 1995
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
  • Patent number: 5371232
    Abstract: A process for preparing a compound of the formula I ##STR1## where R.sup.1 to R.sup.4 are each, independently of one another, hydrogen, alkyl, alkoxy, hydroxyl or halogen, comprises reacting a compound of the formula II ##STR2## with a compound of the formula III ##STR3## in the presence of sulfur or a sulfur donor at elevated temperature. The compounds prepared according to the invention are suitable, for example, as diazo components.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: December 6, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Christoph Bomba, Guido Kuth, Paul Guenthert, Erwin Hahn
  • Patent number: 5362878
    Abstract: Compounds of the formula ##STR1## wherein R.sup.21 and R.sup.22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula ##STR2## and the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: November 8, 1994
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ernest S. Hamanaka, Peter A. McCarthy, Thien Truong, Frederick J. Walker
  • Patent number: 5318946
    Abstract: 2-(Heteroaryloxyphenoxy)alkylsulfonate compounds which are effective for the selective control of grass weed species in the presence of crops are described. Also described are a method for the selective herbicidal use of the compounds and a method for their preparation.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: June 7, 1994
    Assignee: American Cyanamid Company
    Inventors: Michael E. Condon, Michael A. Guaciaro
  • Patent number: 5286741
    Abstract: There are provided N-oxy- and thioalkylcarbonyloxyalkylpyrrole compounds of formula I and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.
    Type: Grant
    Filed: October 27, 1992
    Date of Patent: February 15, 1994
    Assignee: American Cyanamid Company
    Inventors: David G. Kuhn, Stephen F. Donovan, Joseph A. Furch
  • Patent number: 5284599
    Abstract: A mesomorphic compound represented by the following formula (I):R.sub.1 --A.sub.1 --B.sub.1 --A.sub.2 --R.sub.2 (I),wherein R.sub.1 and R.sub.2 respectively denote a linear or branched alkyl group having 3-18 carbon atoms capable of including one or non-neighboring two or more methylene groups which can be replaced with at least one species of --Z--, ##STR1## CH.dbd.CH-- and --C.tbd.C--, wherein Z denotes --O-- or --S-- and R.sub.3 denotes hydrogen or an alkyl group having 1-5 carbon atoms; B.sub.1 denotes ##STR2## A.sub.1 denotes a single bond, ##STR3## A.sub.2 denotes a single bond, --A.sub.3 -- or --A.sub.3 --A.sub.4 -- wherein A.sub.3 and A.sub.4 respectively denote any one of ##STR4## and Y.sub.1 and Y.sub.2 respectively denote any one of hydrogen, fluorine, chlorine, bromine, --CH.sub.3, --CN and --CF.sub.3.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: February 8, 1994
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takashi Iwaki, Takao Takiguchi, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
  • Patent number: 5276206
    Abstract: 2-mercaptobenzothiazole and benzothiazole are prepared from dibenzothiazyl disulphide by reacting dibenzothiazyl disulphide in the presence of an alkali and/or alkaline earth hydroxide solution at temperatures from 40.degree. to 120.degree. C. until a constant pH value in the range from 8 to 10 has been reached, then treating the reaction mixture with an aqueous solution of mineral acids at temperatures from 10.degree. to 100.degree. C., and subsequently removing benzothiazole by distillation or extraction from the reaction mixture containing 2-mercaptobenzothiazole.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: January 4, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Adolf Sicheneder, Bardo Becker
  • Patent number: 5266320
    Abstract: The use of an aminovinyl-substituted heterocyclic compound of the general formula I ##STR1## in which R.sup.1 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, or halogen, and, if more than one radical R.sup.1 are present, these may be the same or different,R.sup.2 denotes cyano or C.sub.1 -C.sub.20 -alkoxycarbonyl or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.1 -C.sub.18 -alkoxy, halogen, cyano, C.sub.1 -C.sub.20 -alkoxycarbonyl, or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl, and, if more than one radical R.sup.3 are present, these may be the same or different,X denotes NH, O or S,m is equal to 1 or 2, andn is an integer from 1 to 5,as a stabilizer for organic materials.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: November 30, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Holderbaum, Alexander Aumueller, Hubert Trauth
  • Patent number: 5256661
    Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: October 26, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5254692
    Abstract: 2,6-dialkyl-4-(benzothiazol- or benzoxazol-7-yl)-1,4-dihydropyridines which exhibit positive inotropic action with largely neutral vascular behavior, of the formula ##STR1## in which R.sup.1 and R.sup.5 are identical or different and represent straight-chain or branched alkyl having up to 8 carbon atoms,R.sup.2 represents nitro or cyano, orR.sup.1 and R.sup.2 together form a lactone ring of the formula ##STR2## R.sup.3 represents a radical of the formula ##STR3## and R.sup.4 represents hydrogen, orand physiologically acceptable salts thereof.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: October 19, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Horst Boshagen, Jurgen Stoltefuss, Alexander Straub, Rainer Gross, Joachim Hutter, Siegbert Hebisch, Martin Bechem
  • Patent number: 5250692
    Abstract: A water-soluble methine compound represented by the following general formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents a non-metallic atomic group required for forming a 5-membered or 6-membered nitrogen-containing heterocyclic ring; R.sub.1 and R.sub.2, which may be the same or different, each represents an alkyl group; Q.sub.1 and Q.sub.2 each represents an atomic group required, in combination, for forming a 4-thiazolidinone ring, a 5-thiazolidinone ring, a 4-imidazolidinone ring, a 4-oxazolidinone ring, a 5-oxazolidinone ring, a 5-imidazolidinone ring or a 4-dithiolanone ring; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5, which may be the same or different, each represents a methine group; R represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group; m represents 1 or 2; i and h each represents 0 or 1; l represents 1 or 2; and j and k each represents 0, 1, 2 or 3.
    Type: Grant
    Filed: April 18, 1991
    Date of Patent: October 5, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Koya, Toshinao Ukai, Haruo Takei
  • Patent number: 5243047
    Abstract: A compound contains a ligand group and at least one group of the general formula --XR.sub.n where X is a linking group which contains at least one hetero-atom, R is a saturated hydrocarbyl group containing at least six carbon atoms or is an unsaturated hydrocarbyl group containing at least three carbon atoms. The ligand group can be a polyhydroxyhydrocarbyl, a triazole, an imidazole, an indazole, a thiazole, an oxazole, a carbamate, an xanthate or a phthalazine. The compounds can be used to improve bonding between a metal and a coating material in contact with the metal surface. The metal may be a tire cord and the coating material rubber or a rubber composition.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: September 7, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventor: John R. Lawson
  • Patent number: 5236619
    Abstract: A mesomorphic compound represented by the following formula (I):R.sub.1 --A.sub.1 --B.sub.1 --A.sub.2 --R.sub.2 (I),wherein R.sub.1 and R.sub.2 respectively denote a linear or branched alkyl group having 3-18 carbon atoms capable of including one or non-neighboring two or more methylene groups which can be replaced with at least one species of ##STR1## wherein Z denotes --O-- or --S-- and R.sub.3 denotes hydrogen or an alkyl group having 1-5 carbon atoms; B.sub.1 denotes ##STR2## A.sub.1 denotes a single bond, ##STR3## A.sub.2 denotes a single bond, --A.sub.3 -- or --A.sub.3 --A.sub.4 -- wherein A.sub.3 and A.sub.4 respectively denote any one of ##STR4## and Y.sub.1 and Y.sub.2 respectively denote any one of hydrogen, fluorine, chlorine, bromine, --CH.sub.3, --CN and --CF.sub.3.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: August 17, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takashi Iwaki, Takao Takiguchi, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5210200
    Abstract: A dye compound of a general formula (I): ##STR1##where R.sub.1 represents a hydrogen atom, or a substituent; R.sub.2 and R.sub.3 independently represent a substituent; X represents a nitrogen atom or --C(R.sub.5).dbd.; R.sub.5 represents a substituent; and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group as bonded to the nitrogen atom in the formula via an unsaturated carbon atom, which dye compound is fast to heat and light and is useful for color image formation and as a filter dye; and a thermal transfer dye donating material having a dye donating layer containing a thermal transferring dye on a support, where the thermal transferring dye is represented by: ##STR2##where X.sup.2 represents --N.dbd., or --C(R.sup.22).dbd.; R.sup.21, R.sup.22, R.sup.23 and R.sup.24 independently represent a hydrogen atom, or a non-metallic substituent; R.sup.25, R.sup.26, R.sup.27 and R.sup.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: May 11, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Yasuhiro Shimada, Hisashi Mikoshiba, Hideo Usui
  • Patent number: 5206375
    Abstract: The novel compound of the general formula I ##STR1## where X is fluorine, chlorine, bromine, SO.sub.2 Y or unsubstituted or substituted hydroxyl or mercapto, Y is alkyl, alkenyl, cycloalkyl, aralkyl, aryl, chlorine or unsubstituted or substituted hydroxyl or amino, R is hydrogen, C.sub.1 -C.sub.4 -alkyl or a radical which can be introduced by electrophilic substitution or a radial of the formula --CH.dbd.T, in which T is a radical of a methyleneactive compound or of an amine, and R.sup.1 is hydrogen, acyl or unsubstituted or substituted alkyl, cycloalkyl or alkenyl, and R.sup.2 is hydrogen or unsubstituted or substituted alkyl or alkenyl, or R.sup.1 and R.sup.2 together with the nitrogen form a saturated heterocyclic structure and R.sup.1 and R.sup.2 together form a radical of the formula ##STR2## are useful as diazo and/or coupling components or generally as dye intermediates, depending on their constitution.
    Type: Grant
    Filed: April 8, 1992
    Date of Patent: April 27, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Schefczik, Karl-Heinz Etzbach, Heinz Eilingsfeld
  • Patent number: 5196454
    Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: March 23, 1993
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5153358
    Abstract: A novel process for the preparation of .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids is disclosed. These .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids are useful as intermediates for the preparation of enzyme inhibitors (for example, renin inhibitors) and other peptides or amino acid derivatives or analogs.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: October 6, 1992
    Assignee: Abbott Laboratories
    Inventor: Thomas M. Zydowsky
  • Patent number: 5138067
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or heterocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together with R.sub.2 form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.
    Type: Grant
    Filed: May 29, 1991
    Date of Patent: August 11, 1992
    Assignee: Shionogi & Co. Ltd.
    Inventors: Susumu Kamata, Tatsuo Tsuri, Nobuhiro Haga, Takeaki Matsui, Morio Kishi, Kimio Takahashi, Sanji Hagishita, Kaoru Seno
  • Patent number: 5032590
    Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: July 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 5032168
    Abstract: Disclosed herein are derivatives of 4-((aryloxy)phenoxy)fluoroalkanoic acid and their use as active herbicides for the pre- and postemergent control of grassy weeds, especially in the presence of broadleaf crops.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: July 16, 1991
    Assignee: DowElanco
    Inventor: James A. Turner