Patents Examined by Cecilia Shen
  • Patent number: 5086056
    Abstract: 2-(Heterocyclylalkyl)imidazopyridines having antihistaminic properties, compositions containing these compounds as active ingredient and novel 2-(Heterocyclylalkyl)imidazopyridines.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: February 4, 1992
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Francois M. Sommen, Joseph L. G. Torremans, Gaston S. M. Diels
  • Patent number: 5086060
    Abstract: The effects of acne and psoriasis are relived by applying either topically or by oral adminstration, a compound having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of H, Cl, straight or branched alkyl of 1 to 10 carbon atoms, NO.sub.2, COOR.sub.6, CN, OR.sub.6, NR.sub.6 R.sub.7, NR.sub.6 C(.dbd.S)NR.sub.7 R.sub.8, NF.sub.6 COR.sub.7, SO.sub.2 NR.sub.6 R.sub.7, CH(CH.sub.3)COOH, CONR.sub.6 R.sub.7, COR.sub.6, OCONR.sub.6 R.sub.7, NR.sub.6 COONR.sub.7, R.sub.9 OR.sub.6, NR.sub.6 SO.sub.2 R.sub.7, Si(CH.sub.3).sub.3, and NR.sub.6 CONR.sub.7 R.sub.8,R.sub.3 together with R.sub.4 forms a benzo ring or taken together with R.sub.2 forms a benzo or tetrahydrobenzo ring or together with R.sub.2 and R.sub.1 forms a: ##STR2## moiety or together with R.sub.2 forms a ##STR3## moiety or R.sub.2 together with R.sub.1 forms a benzo ring or R.sub.2 together with R.sub.3 forms a ##STR4## moiety, or R.sub.
    Type: Grant
    Filed: July 16, 1990
    Date of Patent: February 4, 1992
    Assignee: Eastman Kodak Company
    Inventors: Neil F. Haley, Xina Nair, Gerard J. Gendimenico, F. Christopher Zusi, R. Thomas Swann
  • Patent number: 5084084
    Abstract: Disclosed herein is uracil derivatives having a haloalkyl group at the 6-position and a phenyl group at the 3-position which has a specific substituent, which are represented by the formula (I) and showing penetrative translocation activity and a very high herbicidal activity, in which as compared with the conventional herbicidal compounds, the said uracil derivatives can be applied for either soil treatment or foliage treatment, thereby producing a quick and high herbicidal effect even at a very low dosage against a large variety of weeds including perennial weeds, and have the property to residual effect for an appropriate period of time.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: January 28, 1992
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Jun Satow, Kenzou Fukuda, Kaoru Itoh, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe
  • Patent number: 5082941
    Abstract: The process is characterized in that the diethylamine salt or the ammonium salt of 2,5-dihydroxybenzenesulphonic acid is used as starting material, which salt is tosylated in an ammoniacal medium to lead in both cases to the production of the ammonium salt of 2,5-dihydroxybenzenesulphonic acid monotosylate, which in its turn is converted initially to the corresponding piperazine disalt which is separated in an aqueous medium, and finally in an aqueous-alcoholic medium the piperazine salt of 2,5-dihydroxybenzenesulphonic acid monotosylate, also known as piperazine sultosylate, is obtained.Medicinal applications.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: January 21, 1992
    Assignee: Esteve Quimica S.A.
    Inventors: Josep M. R. Baro, Salvador M. Giral, Josep M. F. Pons de Vall
  • Patent number: 5082839
    Abstract: The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: January 21, 1992
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Karl-Heinz Weber, Albrecht Harreus, Jorge Casals-Stenzel, Gojko Muacevic, Wolfgang Troger, Gerhard Walther
  • Patent number: 5079254
    Abstract: Amide and ester derivatives of 6-amino-octahydro-1,7,8-indolizinetriol are described herein. The compounds are prepared from castanospermine by replacing the appropriate hydroxy function with an amino function while protecting the other hydroxy groups in the meantime. The compounds are useful as hexosaminidase inhibitors.
    Type: Grant
    Filed: June 4, 1990
    Date of Patent: January 7, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Paul S. Liu, Mohinder S. Kang
  • Patent number: 5079251
    Abstract: Pyrazinone derivatives useful as insecticides have the formula (I): ##STR1## wherein A is N or C-R.sup.1 ; R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, haloalkyl, cyano or nitro; R.sup.3 and R.sup.4 are independently selected from hydrogen, halogen, alkyl or cycloalkyl; R.sup.5 is cyano, halo, nitro, alkoxy, haloalkyl, haloalkoxy or --S(O).sub.n R.sup.10 ; R.sup.6 is halo, cyano, nitro, haloalkyl, haloalkoxy, alkoxycarbonyl or --S(O).sub.n R.sup.10 ; R.sup.7 is hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, haloalkylthio, alkoxycarbonyl, NR.sup.11 R.sup.12 or haloalkyl; R.sup.8 is H, halo, NR.sup.11 R.sup.12, alkyl, cycloalkyl or S(O).sub.n R.sup.10 ; and R.sup.9 is oxygen or sulphur; where n is 0, 1 or 2; and R.sup.10 is alkyl, haloalkyl or cycloalkyl and R.sup.11 and R.sup.12 are independently selected from hydrogen, alkyl, cycloalkyl, benzyl or substituted benzyl.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: January 7, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Steven Fitzjohn
  • Patent number: 5079252
    Abstract: The present invention relates to the valeryl ester of acyclovir and pharmacologically acceptable salts thereof and their use in medical therapy particularly in the treatment of viral infections. Also provided are processes for the preparation and pharmaceutical formulations containing the compounds according to the invention.
    Type: Grant
    Filed: July 13, 1989
    Date of Patent: January 7, 1992
    Assignee: Buroughs Welcome Co.
    Inventor: Lilia M. Beauchamp
  • Patent number: 5076831
    Abstract: Substituted 1,8-naphthalenedicarboximides of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, and Z have the meanings recited in the disclosure are disclosed as new compounds suitable for use as antidotes in herbicidal compositions.
    Type: Grant
    Filed: November 20, 1990
    Date of Patent: December 31, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Saupe, Norbert Meyer, Peter Plath, Ulrich Schirmer, Bruno Wuerzer, Karl-Otto Westphalen, Manfred Patsch, Juergen Pfister
  • Patent number: 5077037
    Abstract: Methods and compositions for enhancing magnetic resonance imaging in at least a portion of a warm-blooded animal.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: December 31, 1991
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: Rebecca A. Wallace
  • Patent number: 5077405
    Abstract: This invention relates to 3-(1-substituted-4-piperazinyl)-1H-indazoles having the following formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, arylloweralkyl, acyl, cycloalkylloweralkylene, and phenylsulfonyl; and R.sub.2 is hydrogen, lower alkyl, hydroxyloweralkyl of the formula -(loweralkylene)-OH, arylloweralkyl, acyl, cycloalkylloweralkylene, ##STR2## where Z is selected from hydrogen, halogen, loweralkoxy, CF.sub.3, NO.sub.2, and NH.sub.2 ; ##STR3## where Z is as defined above; ##STR4## where Z is as defined above; ##STR5## where R.sub.3 and R.sub.4 are each independently hydrogen and loweralkyl; ##STR6## where Z is as defined above; ##STR7## where R' and R" are each independently hydrogen and loweralkyl; X is hydrogen, loweralkyl, hydroxyl, halogen, loweralkoxy, CF.sub.3, NO.sub.2 and amino; n is an integer of 1 to 4, with the further proviso that R.sub.2 is not loweralkyl when R.sub.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: December 31, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5077295
    Abstract: A series of bridged bicyclic imides having a 4-[4-(3-benzisothiazolyl)-1-piperazinyl]butyl group attached to the imide nitrogen are useful antipsychotic agents.
    Type: Grant
    Filed: March 8, 1991
    Date of Patent: December 31, 1991
    Assignee: Pfizer Inc.
    Inventors: Gene M. Bright, John A. Love, III
  • Patent number: 5077415
    Abstract: Aromatic dianhydrides being substituted in the positions ortho to the bridging moiety, said substituent groups including halogen, alkyl, hydroxy, nitro, cyano, ester, alkoxy, perfluoroalkyl, mercapto and thioester groups, said dianhydrides providing certain beneficial properties to polyimides prepared therefrom.
    Type: Grant
    Filed: January 19, 1990
    Date of Patent: December 31, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Stanley J. Jasne, Pasquale A. Falcigno
  • Patent number: 5077298
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is hydrogen, chlorine, bromine or methyl, R.sub.3 is C.sub.1-5 alkyl or C.sub.3-5 alkenyl and R.sub.4 is C.sub.3-7 alkyl; C.sub.3-7 cycloalkyl; adamantyl; or optionally substituted phenyl, having valuable pharmaceutical, and in particular LH- and PRL-secretion inhibiting as well as neuroleptic activity.
    Type: Grant
    Filed: July 2, 1990
    Date of Patent: December 31, 1991
    Assignee: Sandoz Ltd.
    Inventor: Walter Haefliger
  • Patent number: 5075459
    Abstract: A treatment agent for inorganic siliconaceous fillers has as its main ingredient an organosilicon compound of general fomrula (I): ##STR1## in which X represents a functional group selected from among H.sub.2 NCH.sub.2 CH.sub.2 --, H.sub.2 NCH.sub.2 CH.sub.2 CH.sub.2 --, ##STR2## Y.sup.1 is CH.sub.2 .dbd.CHCH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 SiR.sub.n.sup.1 Z.sub.3-n.sup.1, R.sup.1 is a substituted or nonsubstituted monovalent hydrocarbon group, Z.sup.1 is an alkoxy group having 1-6 carbon atoms and n is an integer from 0-2, or of general formula (II): ##STR3## in which Y.sup.2 is ##STR4## --CH.sub.2 CH.sub.2 CH.sub.2 SiR.sub.m.sup.2 Z.sub.3-m.sup.2 or a substitutent or nonsubstituted monovalent hydrocarbon group, Z.sup.2 is an alkoxy group having 1-6 carbon atoms and m is an integer from 0-2.
    Type: Grant
    Filed: November 26, 1990
    Date of Patent: December 24, 1991
    Assignee: Toshiba Silicone Co., Ltd.
    Inventors: Keiji Kabeta, Kiyoaki Syuto
  • Patent number: 5075318
    Abstract: 8.alpha.-Acylaminoergoline useful in the treatment of psychotic disorders and Parkinson's disease.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: December 24, 1991
    Assignee: Sandoz Ltd.
    Inventor: Walter Haefliger, deceased
  • Patent number: 5073635
    Abstract: A process of preparing linearly-extended polyalkylenepolyamines, such as linear and branched polyethylenepolyamines, comprising contacting a difunctional aliphatic alcohol, such as monoethanolamine, with a reactant aliphatic amine, such as ethylenediamine, in the presence of a metal silicate catalyst wherein the metal is selected from Groups IIIB, IVB, VB and the lanthanide rare earth metals. Reactions of piperazines with alkanolamines to yield alcohol-extended and/or amine-extended piperazines are included in the process of this invention.
    Type: Grant
    Filed: June 22, 1990
    Date of Patent: December 17, 1991
    Assignee: The Dow Chemical Company
    Inventors: Robert G. Bowman, David C. Molzahn, George E. Hartwell
  • Patent number: 5071841
    Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
  • Patent number: 5071864
    Abstract: Aminoalkyl-substituted 2-aminothiazole derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2, which may be identical or different, are each hydrogen, C.sub.1 -C.sub.5 -alkyl, phenyl or C.sub.1 -C.sub.5 -alkanoyl, R.sup.3 is C.sub.1 -C.sub.5 -alkyl, phenyl which is unsubstituted or monosubstituted by halogen, C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy, or thienyl,n is an integer of from 2 to 6, andNR.sup.4 R.sup.5 is one of the groups a, b, c or d ##STR2## where Ar is a phenyl ring which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl, nitro or trifluoromethyl, or is pyridyl, pyrimidinyl or thienyl, R.sup.5 is H or C.sub.1 -C.sub.5 -alkyl and R.sup.7 is phenyl which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl or trifluoromethyl, or R.sup.7 is thienyl, with the proviso that R.sup.3 is C.sub.1 -C.sub.5 alkyl only when either R.sup.1 and R.sup.
    Type: Grant
    Filed: June 28, 1990
    Date of Patent: December 10, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Beatrice Rendenbach-Mueller, Liliane Unger, Hans-Juergen Teschendorf
  • Patent number: 5071848
    Abstract: Isothiazolo-quinoline derivatives are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: December 10, 1991
    Assignee: Abbott Laboratories
    Inventors: Daniel Tim-Wo Chu, Jacob J. Plattner, Linus L. Shen, Larry L. Klein