Patents Examined by Cecilia Shen
  • Patent number: 5096914
    Abstract: Benzopyran derivatives of the general formula I ##STR1## wherein the substituents are as defined herein are provided. The compounds show vasodilating and vascular spasmolytic activity and are useful in treating hypertension.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5095144
    Abstract: A process for dimerizing an aromatic halogen compound is disclosed, which comprises the step of: subjecting an aromatic halogen compound having at least one halogen atom bonded to an aromatic nucleus carbon to a dehalogenation-dimerization reaction in the presence of a catalyst, water, a reducing agent, and a halogen acceptor, the catalyst comprising a carrier supported thereon palladium and iron.
    Type: Grant
    Filed: July 17, 1990
    Date of Patent: March 10, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Keiichi Sato, Takahiko Takewaki, Yoshio Katsuro
  • Patent number: 5095124
    Abstract: The present invention relates to a two-stage liquid phase process wherein an alk-2-enyl glycidyl ether having the formula ##STR1## wherein R is hydrogen or lower alkyl; R' is C.sub.2 to C.sub.4 alkylene; n has a value of from 1 to 4 and n' has a value of from 0 to 4, is catalytically isomerized to the corresponding alk-1-enyl glycidyl ether in the first-stage of the reaction and the reaction mixture of the first-stage, containing the isomerization catalyst is then contacted with carbon dioxide in the presence of a phase transfer catalyst under a pressure ranging from atmospheric to about 400 psig in the second stage of the reaction.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: March 10, 1992
    Assignee: ISP Investments Inc.
    Inventors: Jeffrey S. Plotkin, Mark M. Miller, Paul D. Taylor
  • Patent number: 5095108
    Abstract: The non-solvated crystalline form "A" of 3-(-4-cynnamyl-1-piperazinyl)-iminomethylrifamycine SV finds application in the therapeutical practice.It represents a crystalline substance with absorption maximum of the infrared spectrum at 1644, 1585, 1340, 1350, 1295 and 1290-doublet, 1238, 1213, and triplet with low intesitivety at 726, 735 and 760 cm.sup.-1, as well as with characteristic diffraction maxima at 9,25 and 9,50 .theta.--most-intensive at 12,22 and doublet at 13,10 and 13,33 .theta. of the X-ray diffraction diagram.The obtaining of the non-solvated crystalline form "A" consists in the isolation of 3-(-4-cynnamyl-1-piperazinyl)-iminomethylrifamycine obtained in medium of indifferent organic solvent, preferably tetrahydrofuran or chloroform, and its dissolution in isopropanol or acetone or a mixture of both at a temperature from 30.degree. C. up to the ebullition temperature of the respective solvent.
    Type: Grant
    Filed: August 28, 1990
    Date of Patent: March 10, 1992
    Assignee: Technologichen Kombinat za Promishlena Microbiologia
    Inventors: Rumyana G. Konstantinova, Anka V. Evstatieva, Ivan A. Again, Velichka Dimova
  • Patent number: 5093496
    Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneificial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: April 4, 1991
    Date of Patent: March 3, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Patent number: 5091387
    Abstract: Disclosed are spirocyclic compounds of the formula: ##STR1## The compounds of formula I are oxytocin antagonists useful in the treatment of preterm labor and dysmenorrhea, and for the stoppage of labor preporatory to Caesarian delivery. Also disclosed are pharmaceutical compositions containing these compounds as well as methods for preparing the compounds.
    Type: Grant
    Filed: August 5, 1991
    Date of Patent: February 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Douglas J. Pettibone, Roger M. Friedinger
  • Patent number: 5091526
    Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: February 25, 1992
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, John W. Clader
  • Patent number: 5091532
    Abstract: A new process for the preparation of pigments of the formula ##STR1## comprises first reacting phthalodinitrile in an organic medium in the presence of a base with an alcohol and then with a compound of the formula ##STR2## in the presence of water at a pH of 1-6.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: February 25, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Kaletta, Meinhard Rolf
  • Patent number: 5091543
    Abstract: A method of preparing five- and six-membered cyclic carbonates is disclosed. The process comprises reacting a 1,2- or 1,3-diol with an acyclic diester of carbonic acid in the presence of a catalyst selected from alkylammonium salts, tertiary amines, and ion-exchange resins containing alkylammonium or tertiary amino groups. Cyclic carbonates free of polycarbonate by-products are obtained in high yields.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: February 25, 1992
    Assignee: Arco Chemical Technology, Inc.
    Inventor: Roger A. Grey
  • Patent number: 5091429
    Abstract: Derivatives of 4-amino-1-trifluoromethyltetralines of general formula: ##STR1## wherein: X represents an aromatic nucleus, namely phenyl, naphthyl, or thienyl able to carry one to two substituents chosen from halogeno, hydroxy, C.sub.1 to C.sub.8 alkoxy or trifluoromethyl;R.sub.1 represents a hydrogen atom or a halogen, a hydroxy group, a C.sub.1 to C.sub.8 alkoxy group, in one of positions 5, 6 or 7, or even a methylenedioxy group in positions 5 and 6 or 6 and 7;R.sub.2 represents a hydrogen atom or a halogen, a hydroxy group, a C.sub.1 to C.sub.8 alkoxy group in one of the other positions 5, 6 or 7, andR.sub.3 and R.sub.4 each represent a hydrogen atom, a methyl group or a linear or branched C.sub.1 to C.sub.n alkyl group, n being 2 or more, possibly halogenated, hydroxylated or aminated, or R.sub.3 and R.sub.
    Type: Grant
    Filed: July 22, 1989
    Date of Patent: February 25, 1992
    Assignee: Laboratoires Lucien
    Inventors: Jean-Pierre Begue, Micheline Charpentiermorize, Daniele Bonnet Delpon, Huguette Gilbert-Semon
  • Patent number: 5091541
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is O, S, NH, N-loweralkyl, or N-arylloweralkyl;Y is hydrogen, fluorine, chlorine, bromine, nitro, loweralkyl, loweralkoxy, or triloweralkylsilyl;R.sub.1 is loweralkyl, halogen-substituted loweralkyl, aryl, arylloweralkyl, cycloalkyl, heteroaryl or heteroarylloweralkyl;R.sub.2 is hydrogen, loweralkyl or arylloweralkyl;R.sub.3 is loweralkyl or arylloweralkyl;R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl;R.sub.5 is hydrogen or loweralkyl; andm is 0 or 1, with the proviso that when m is O, R.sub.1 may also be hydrogen.which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: February 25, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gerard J. O'Malley, Richard C. Allen, John I. White
  • Patent number: 5091428
    Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two, provided that when R.sup.3 is hydroxy, n is one or two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: February 25, 1992
    Assignee: Syntex Pharmaceuticals, Ltd.
    Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
  • Patent number: 5089502
    Abstract: A method is provided for inhibiting onset of or treating anxiety by administering a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: February 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Abraham Sudilovsky, Zola P. Horovitz
  • Patent number: 5089500
    Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmceutical formulations and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: February 18, 1992
    Assignee: Burroughs Wellcome Co.
    Inventor: Susan M. Daluge
  • Patent number: 5089497
    Abstract: Substituted piperazines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: February 18, 1992
    Assignee: Warner-Lambert Company
    Inventors: Juan C. Jaen, David G. Nickell, Donna M. Reynolds, Sarah J. Smith, Lawrence D. Wise, David J. Wustrow
  • Patent number: 5089506
    Abstract: Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl wherein each of R.sup.12 and R.sup.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: February 18, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Nancy M. Gray, Brian K. Cheng
  • Patent number: 5087698
    Abstract: A process for the optical resolution of racemic dropropizine, carried out using L(+)tartaric acid as the optical resolution agent in aqueous medium, is described.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: February 11, 1992
    Assignee: Dompe' Farmaceutici S.p.A.
    Inventor: Roberto Giani
  • Patent number: 5087621
    Abstract: The present invention relates to substituted azetidinylisothiazolopyridone derivatives which correspond to the general formula I: ##STR1## or its tautomeric formula ##STR2## It also relates to a process for preparing them and to their application as a medicinal product.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: February 11, 1992
    Assignee: Laboratorios del Dr. Esteve
    Inventors: Augusto C. Pinol, Jordi F. Constansa, Juan P. Corominas
  • Patent number: 5087697
    Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: December 19, 1990
    Date of Patent: February 11, 1992
    Assignee: Burroughs Wellcome Co.
    Inventor: Susan M. Daluge
  • Patent number: 5087627
    Abstract: A method for treatment of disorders of the cerebro-neural transmission system which comprises administering a compound of the formula (I) or a pharmaceutically acceptable salt thereof in a therapeutically effective amount, either alone or in admixture with one or more pharmaceutically acceptable excipients, ##STR1## wherein Ar or Ar' is unsubstituted or substituted phenyl or pyridyl; R is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkylenedioxy; A is C.sub.1 -C.sub.6 alkylene; and n is 0 or 1. A compound of the formula (II) or a pharmaceutically acceptable salt thereof, ##STR2## wherein R.sup.1 is hydrogen or fluorine; R.sup.2 is hydrogen or fluorine; R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkylenedioxy; A is lower C.sub.1 -C.sub.6 alkylene, and n is 0 or 1, provided that at least one of R.sup.1 or R.sup.2 is fluorine.
    Type: Grant
    Filed: February 28, 1990
    Date of Patent: February 11, 1992
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Takakazu Morita, Tadashi Iso, Hideyasu Yamauchi