Patents Examined by Michael Bucknum
  • Patent number: 5786479
    Abstract: A process for producing a 6-substituted 2(1H)-quinoxalinone of the formula (I): ##STR1## wherein X is a halogen atom, a trihalogeno-substituted C.sub.1-5 alkyl group or a nitro group, which comprises reacting a 6-substituted 2(1H)-quinoxalinone-N-oxide of the formula (II): ##STR2## wherein X is as defined above, with an alkali metal hydrosulfide and/or an alkali metal sulfide in the presence of from 1 to 20 mol times of an alkali.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: July 28, 1998
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Isao Hashiba, Masataka Hatanaka
  • Patent number: 5731342
    Abstract: This invention provides novel benzothiophene compounds.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: March 24, 1998
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Alan David Palkowitz
  • Patent number: 5728826
    Abstract: The invention describes a process for the epimer enrichment of compounds of formula (I) by silation, fractionated crystallization and acid hydrolysis.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: March 17, 1998
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Patent number: 5710273
    Abstract: A complex crystal is composed of anion of triiodine and cation of a fused compound consisting essentially of at least one nitrogen atom and at least 3 aromatic fused rings. Since the complex crystal has such a stable structure, it shows excellent heat resistance and excellent moisture resisting property. Furthermore, the complex crystal has light-polarizing performance because of an arrangement of the molecular chain of iodine. Moreover, the complex crystal exhibits excellent polarization because of an interaction between the fused compound and iodine. Therefore, the complex crystal is suitable for use as light-adjusting particles of a light valve or a light-adjusting glass.
    Type: Grant
    Filed: July 25, 1996
    Date of Patent: January 20, 1998
    Assignees: Toyota Jidosha Kabushiki Kaisha, Kabushiki Kaisha Toyota Chuo Kenkyusho
    Inventors: Arimitsu Usuki, Hisato Takeuchi, Narihito Tatsuda, Akane Okada, Toshio Kurauchi, Hiromitsu Tanaka, Shinobu Okayama, Kazuo Tojima, Akio Fukui, Toshiro Okamoto
  • Patent number: 5703083
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addidon salts thereof wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen, halogen, hydroxy, alkyl, alkoxy, amino, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, cyano, nitro, trifluoromethyl, or trifluoromethoxy;R.sub.8 is hydrogen or lower alkyl;X represents an optionally substituted alkylene group; andY represents a mono-, di- or trisubsituted cyclic amino groupwhich compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parldnsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: December 30, 1997
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Jun Yuan
  • Patent number: 5700946
    Abstract: The present invention provides a process for producing an N-vinyl compound, which comprises subjecting an N-(-alkoxyalkyl) compound to gas phase intramolecular alcohol elimination to convert said compound to an N-vinyl compound directly in one step, wherein a solid oxide containing phosphorus and an alkali metal and/or an alkaline earth metal is used as a catalyst. This process need not use any solvent or any auxiliary raw material and consequently can produce an N-vinyl compound simply and safely without generating any waste material derived from the auxiliary raw material.
    Type: Grant
    Filed: April 17, 1996
    Date of Patent: December 23, 1997
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Yuuji Shimasaki, Hideyuki Kanbe, Akira Kurusu
  • Patent number: 5700818
    Abstract: This invention discloses dyhydrobenzofuranyl-biphenyl carboxamides having 5HT.sub.1D antagonistic activity.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: December 23, 1997
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Laramie Mary Gaster
  • Patent number: 5700947
    Abstract: This invention is directed to nitric esters of derivatives of propionic acid, 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid, 5-benzoyl-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid, 6-methoxy-2-napthylacetic acid, characterized in that they have the following general formula: ##STR1## These nitric ester derivatives may be formulated into pharmaceutical compositions and administered for their anti-inflammatory and/or analgesic activity.
    Type: Grant
    Filed: April 5, 1996
    Date of Patent: December 23, 1997
    Assignee: NICOX S.A.
    Inventor: Piero Del Soldato
  • Patent number: 5696111
    Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: December 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
  • Patent number: 5693634
    Abstract: The present invention relates to compounds of formula (I) ##STR1## and salts and metabolically labile esters thereof. These compounds and compositions containing them have antibacterial activity. Processes for preparing these compounds are also disclosed, as well as methods of treatment of a human or non-human subject to combat bacterial infections.
    Type: Grant
    Filed: May 9, 1996
    Date of Patent: December 2, 1997
    Assignee: Glaxo Wellcome S.p.A.
    Inventors: Alcide Perboni, Giorgio Pentassuglia, Daniele Andreotti, John Alexander Winders
  • Patent number: 5693812
    Abstract: Polymorphic forms of the angiotensin II receptor antagonist, 3-?2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-i midazo?4,5-b!pyridine and a method for the preparation of these crystal forms.
    Type: Grant
    Filed: June 3, 1996
    Date of Patent: December 2, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Gerald S. Brenner, Louis S. Crocker, Hossain Jahansouz, Robert D. Larsen, Chris H. Senanayake, Andrew S. Thompson, Karen C. Thompson, Thomas R. Verhoeven
  • Patent number: 5690909
    Abstract: The invention relates to new fluorine-containing macrocyclic metal complexes that consist of a complexing agent of formula I and at least one metal ion of an element of atomic numbers 21-29, 42, 44 or 57-83 ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3 and A have a different meaning, agents containing these compounds, their use as NMR and x-ray diagnostic agents as well as process for the production of these compounds and agents.
    Type: Grant
    Filed: March 19, 1996
    Date of Patent: November 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Johannes Platzek, Bernd Raduchel, Ulrich Niedballa, Hanns-Joachim Weinmann, Hans Bauer, Klaus Roth
  • Patent number: 5691371
    Abstract: Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.
    Type: Grant
    Filed: September 27, 1995
    Date of Patent: November 25, 1997
    Assignee: Auckland UniServices Limited
    Inventors: William Alexander Denny, William Robert Wilson, Moana Tercel
  • Patent number: 5688792
    Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO.sub.2, SNR.sup.10 or S(O)NR.sup.10 ;R is (a) hydrogen,(b) C.sub.1 -C.sub.8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy or --O--CH.sub.2 --Ph,(c) C.sub.3 -C.sub.6 cycloalkyl,(d) amino,(e) C.sub.1 -C.sub.8 alkylamino,(f) C.sub.1 -C.sub.8 dialkylamino or(g) C.sub.1 -C.sub.8 alkoxy;R.sup.1 is H, except when X is O then R.sup.1 can be H, CH.sub.3, CN, CO.sub.2 H, CO.sub.2 R or (CH.sub.2).sub.m R.sup.11 (m is 1 or 2);R.sup.2 is independently H, F or Cl;R.sup.3 is H except when X is O and R.sup.1 is CH.sub.3 then R.sup.3 can be H or CH.sub.3 ;R.sup.10 is independently H, C.sub.1 -C.sub.4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C.sub.1 -C.sub.8 alkoxy, amino, C.sub.1 -C.sub.8 alkylamino, or C.sub.1 -C.sub.8 dialkylamino) or p-toluenesulfonyl;R.sup.11 is hydrogen, OH, OR, OCOR, NH.sub.
    Type: Grant
    Filed: March 5, 1996
    Date of Patent: November 18, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner, Douglas K. Hutchinson
  • Patent number: 5686480
    Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: November 11, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Ian James Collins, Paul David Leeson, Michael Rowley
  • Patent number: 5679804
    Abstract: Phosphonic esters I ##STR1## (A is an aromatic radical or an .alpha., .beta.-olefinically unsaturated group and R.sup.1 is C.sub.1 -C.sub.4 -alkyl or phenyl) are prepared by subjecting a phosphite II ##STR2## to a rearrangement reaction in the presence of a catalytic amount of a halide ion-donating compound to give I. The compounds I are used as intermediates for organic syntheses, in particular for the synthesis of polyenes.
    Type: Grant
    Filed: July 27, 1995
    Date of Patent: October 21, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Ditrich, Wolfgang Krause
  • Patent number: 5677443
    Abstract: A bioavailable crystalline form of cefuroxime axetil, obtained by treating known crystalline or amorphous cefuroxime axetil with water or with a water-miscible organic solvent or with a mixture thereof at a temperature of between +20.degree. C. and +100.degree. C., followed by cooling and separating the crystalline product by known methods.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: October 14, 1997
    Assignee: ACS Dobfar S.p.A.
    Inventors: Maurizio Zenoni, Mario Leone, Angelo Cattaneo, Leonardo Marsili
  • Patent number: 5672705
    Abstract: Compounds of formula (I), wherein R is an oxygen or sulphur atom or an NH or N-alk radical, and each of R.sub.1 and R.sub.2, which are the same or different, is a hydrogen or halogen atom or an alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar,--N.dbd.CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO.sub.3 H radical, the preparation thereof, and drugs containing such compounds, are disclosed.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: September 30, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Claude Aloup, Serge Mignani
  • Patent number: 5672738
    Abstract: Process for the preparation of 3-(N-aryl-amino)-propyl-2'-sulfatoethyl-sulfonyl compoundsCompounds of the formula (1)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OSO.sub.3 M(1)are prepared by reacting a compound of the formula (2) ##STR1## with 2-mercaptoethanol to give a compound of the formula (3)Ar--NH--(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --OH (3)at temperatures from 90.degree. to 270.degree. C. in the presence of a catalytic amount of a base, subsequently oxidizing the compound of the formula (3) to give a compound of the formula (4)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OH(4),and finally esterifying the compound of the formula (4) with at least one molar equivalent of sulfuric acid, oleum or halosulfonic acid to give a compound of the formula (1).Compounds of the formula (1) are valuable starting compounds for the preparation of reactive dyestuffs.
    Type: Grant
    Filed: November 17, 1995
    Date of Patent: September 30, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Christian Schumacher, Michael Meier, Werner Hubert Russ
  • Patent number: 5670497
    Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: September 23, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang