Patents Examined by Jacqueline Haley
  • Patent number: 5827871
    Abstract: Use of a compound of general formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, arylC.sub.1-6 alkoxy, --CO.sub.2 R.sup.4, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n CONR.sup.5 R.sup.6, --(CH.sub.2).sub.n SO.sub.2 NR.sup.5 R.sup.6, C.sub.1-6 alkanoylamino(CH.sub.2).sub.n, or C.sub.1-6 alkylsulphonylamino(CH.sub.2).sub.n ;R.sup.4 represents hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.5 and R.sup.6 each independently represent hydrogen or C.sub.1-6 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a ring;n represents 0, 1 or 2; andR.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring;or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT.sub.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: October 27, 1998
    Assignee: Smithkline Beecham plc
    Inventors: Francis David King, Laramie Mary Gaster, Alberto Julio Kaumann, Rodney Christopher Young
  • Patent number: 5824807
    Abstract: Azabicylobutane can be produced by reacting azetidines under aqueous conditions to eliminate aza and 3-position substituents to effect cyclization. New azetidinyl compounds are described which can be intermediates in the preparation of the azabicyclobutane.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: October 20, 1998
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Paritosh R. Dave, Thomas G. Archibald
  • Patent number: 5824806
    Abstract: TNAZ can be prepared directly from N-tertiarybutyl-3,3-dinitroazetidine compounds. The compounds may be in the form of the tertiary amine or the quaternary amine. The reaction is in the presence of acetic anhydride and nitrate ions. It gives high yields and uses mild conditions.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: October 20, 1998
    Assignee: The United States of America as represented by the The Secretary of the Army
    Inventors: Daniel Stec, III, Ralph L. Perez, Paritosh R. Dave, Thomas G. Archibald
  • Patent number: 5808099
    Abstract: ADNAZ, N-acetyl, 3,3 dinitroazetidine, is a new compound and this invention provides the compound, its compositions, preparation and uses. As a compound, it forms a eutectic with TNAZ. It can be used to prepare other compounds. It can be readily nitrated to remove the acetyl group and form TNAZ.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: September 15, 1998
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Daniel Stec, III, Paritosh R. Dave
  • Patent number: 5773630
    Abstract: N-Substituted cyclic imides are obtained by reacting a cyclic acid anhydride with an amine in the presence of a solvent and an acid catalyst at 80.degree. to 200.degree. C. and with removal of the water formed, it being particularly advantageous to carry out this reaction in the presence of a stabilizer and an inert, dipolar aprotic cosolvent, optionally to add an inert organic solvent of low or zero polarity to the reaction mixture present after the reaction, to add a non-aqueous base in an amount of 0.5 to 50% by weight, based on the cyclic anhydride of the formula (II) used, and to separate off the precipitate formed to give a filtrate containing the N-substituted cyclic imide.
    Type: Grant
    Filed: February 6, 1996
    Date of Patent: June 30, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Torsten Groth, Karl-Erwin Piejko, Winfried Joentgen, Josef Kasbauer, Bernd Alig, Werner Struver
  • Patent number: 5770742
    Abstract: 5-Thiophene-substituted tryptamine analogs are provided, which exhibit selectivity towards 5-HT.sub.D1 receptors and consequently show potential in alleviation of the symptoms of migraine. The analogs are represented by the following general chemical formula: ##STR1## in which X represents H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or halogen, at the 4- or 5-position of the thiophene nucleus; Y represents a direct bond or a C.sub.1 -C.sub.3 alkylene group optionally substituted with hydroxyl: and Z represents amino, mono- or di-N-lower alkyl-substituted amino, or optionally N-lower alkyl-substituted pyrrolidine.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: June 23, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Qingchang Meng, Abdelmalik Slassi, Sumanas Rakhit
  • Patent number: 5708018
    Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: February 2, 1996
    Date of Patent: January 13, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Susanne R. Haadsma-Svensson, Bengt R. Andersson, Clas A. Sonesson, Chiu-Hong Lin, R. Nicholas Waters, Kjell A. I. Svensson, Per A. E. Carlsson, Lars O. Hansson, N. Peter Stjernlof
  • Patent number: 5705636
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen or a nitrogen protecting group, useful as intermediates in the preparation of compounds having antibacterial activity.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: January 6, 1998
    Assignee: Glaxo Wellcome S.p.A.
    Inventors: Russell John Thomas, Stefano Biondi, Tino Rossi, Stefania Anna Contini
  • Patent number: 5696269
    Abstract: The invention concerns a process for the preparation of chlorinated derivatives of pyridine compounds by a chlorination reaction of the corresponding pyridine compounds with molecular chlorine, carried out in the gaseous phase by means of bis(trichloromethyl)sulfone as a free radical initiator.The obtained chlorinated derivatives of pyridine compounds, such as 2,6-dichloropyridine, can be used as chemical intermediates.
    Type: Grant
    Filed: February 3, 1993
    Date of Patent: December 9, 1997
    Assignee: Reilly Chemicals S.A.
    Inventors: James Franklin, Francine Janssens
  • Patent number: 5693804
    Abstract: Disclosed are compounds of formula I: ##STR1## wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl;Z is nitrogen or CH;Ar.sub.1 and Ar.sub.2 independently represent aryl groups; andY is hydrogen; orY and R.sub.1 or R.sub.2 together represent CH.sub.2 ;CH.sub.2 CH.sub.2 ; CH.sub.2 O; CH.sub.2 S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or the pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and in preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: December 2, 1997
    Assignee: Molecular Geriatrics Corporation
    Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
  • Patent number: 5691351
    Abstract: Compounds having the structure ##STR1## where m is an integer of from one to nine; n is an integer of from one to four; W is selected from substituted or unsubstituted quinolyl, benzothiazolyl, or quinoxalyl, X is selected from C.sub.1-6 alkylene, C.sub.2-6 alkenylene and C.sub.2-6 alkynylene; Y is selected from halogen, C.sub.1-6 alkyl and C.sub.1-6, alkoxy; and Z is selected from --C(O)B; --C(R.sub.2).sup.2 --O--N.dbd.A--C(O)B; and --C(R.sup.2).dbd.N--O--A--C(O)B where A is C.sub.1-6 alkylene and B is --OH, --O--M.sup.+, --OD where D is a metabolically cleavable group, --OR.sup.6 where R.sup.6 is hydrogen or C.sub.1-6 alkyl, --NR.sup.6 R.sup.7 where R.sup.7 is hydrogen, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy, or where R.sup.6 and R.sup.7 taken together form a five to eight membered ring optionally containing one heteroatom selected from nitrogen, oxygen or sulfur, are inhibitors of leukotriene biosynthesis.
    Type: Grant
    Filed: February 6, 1996
    Date of Patent: November 25, 1997
    Assignee: Abbott Laboratories
    Inventors: Teodozyj Kolasa, David E. Gunn, Clint D. W. Brooks
  • Patent number: 5686481
    Abstract: Indole derivatives of formula (1) wherein the substituents are defined herein are disclosed. The compounds are useful in methods of antagonizing endothelin receptors, treating hypertension, treating renal failure and treating cerebrovascular disease. Pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: November 11, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Jack Dale Leber
  • Patent number: 5684034
    Abstract: A class of novel 1-indole-3-acetamides represented by the formula; ##STR1## is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: November 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
  • Patent number: 5683994
    Abstract: Compounds of formula I are disclosed, ##STR1## as well as processes for their production and pharmaceutical agents containing these compounds suitable for treating disorders of calcium metabolism.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: November 4, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Christos Tsaklakidis, Angelika Esswein, Gerd Zimmermann, Frieder Bauss
  • Patent number: 5679799
    Abstract: There is disclosed a method for producing oxyindoles, which comprises reacting a 2-halogenophenylacetic acid or its salt with ammonia in the presence of a copper salt catalyst, and heating a mixture of the produced 2-aminophenylacetic acid or its salt and oxyindoles in the presence of an acid catalyst, to subject the 2-aminophenylacetic acid or its salt to a ring-closure reaction. According to this method, relatively readily available 2-halogenophenylacetic acids are used as a starting raw material to industrially produce highly pure oxyindoles in high yield in one pot without involving complicated steps. Further, since the amination is carried out at a temperature greatly lower than that of the conventional art, the lowering of the pH of the reaction liquid can be suppressed. Therefore, the restrictions on the specifications of the reaction apparatus, such as corrosion prevention and pressure resistance, can be mitigated.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: October 21, 1997
    Assignee: K-I Chemical Industry Co., Ltd.
    Inventors: Katsuhisa Isogai, Kohei Hasegawa
  • Patent number: 5679694
    Abstract: The invention relates to compounds of formula (I) which have been found to possess anti-tumor activity. Pharmaceutical compositions and methods of treating tumors are also disclosed.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: October 21, 1997
    Assignees: The Wellcome Foundation Ltd., University College Cardiff Consultants Limited
    Inventors: Karl Witold Franzmann, Jeremy Nigel Stables, Patrick Vivian Richard Shannon, Nagaraja Kodanda Ranganatha Rao, Laddawan Chunchatprasert
  • Patent number: 5677324
    Abstract: The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R.sup.3 is hydroxy when the dashed line does not represent a covalent bond and R.sup.3 is absent when the dashed line represents a covalent bond; R.sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4- to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle.
    Type: Grant
    Filed: August 4, 1995
    Date of Patent: October 14, 1997
    Assignee: Pfizer Inc.
    Inventors: Alexander Roderick Mackenzie, Sandra Marina Monaghan
  • Patent number: 5674816
    Abstract: Linear olefin monomers, and particularly alpha-olefins, having a pour point greater than -102.degree., a flash point greater than 10.degree. and a boiling point greater than 121.degree. are proposed as frac fluids in treatment of oil and gas wells by fracturing. Linear olefin monomers are injected into the well, and fracturing pressures applied to the well to fracture the well. Linear olefin monomers may be mixed with a liquified drive fluid such as CO.sub.2, preferably with the CO.sub.2 forming a miscible bank ahead of the linear olefin monomers for use in driving the load fluid from the well.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 7, 1997
    Inventor: Dwight N. Loree
  • Patent number: 5672718
    Abstract: The present invention relates to novel N-phenylacetamino nitriles of the general formula (I), ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl, cycloalkyl, aryl or heterocyclyl which are in each case optionally substituted, andR.sup.2 represents hydrogen, or represents alkyl which is optionally substituted, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, represent cycloalkyl or heterocyclyl which are in each case optionally substituted,R.sup.3 represents halogen, alkyl or alkoxy,R.sup.4 represents hydrogen, halogen, alkyl, halogenoalkyl or alkoxy,R.sup.5 represents halogen, alkyl or alkoxy, andm represents a number 0, 1, 2 or 3, processes for their preparation and their use for the preparation of agents for controlling pests.
    Type: Grant
    Filed: November 15, 1995
    Date of Patent: September 30, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Gunther Beck
  • Patent number: 5670656
    Abstract: A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: September 23, 1997
    Assignee: Zeneca Limited
    Inventors: John Michael Cox, Kevin James Gillen, Russell Martin Ellis, Shaheen Khatoon Vohra, Stephen Christopher Smith, Ian Richard Matthews