Patents Represented by Attorney David E. Frankhouser
  • Patent number: 4785014
    Abstract: Disclosed is a method of treating cognitive decline in a normal aged primate by administering thereto a therapeutically effective amount of 2-[(2,6-dichlorophenyl)-amino]-2-imidazoline or a nontoxic, pharmaceutically acceptable salt thereof. Administration is preferably in amounts of at least about 0.001 mg/day.
    Type: Grant
    Filed: November 6, 1986
    Date of Patent: November 15, 1988
    Assignee: Yale University
    Inventors: Patricia S. Goldman-Rakic, Amy F. T. Arnsten
  • Patent number: 4762832
    Abstract: The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.
    Type: Grant
    Filed: December 18, 1986
    Date of Patent: August 9, 1988
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
  • Patent number: 4755385
    Abstract: There is described a solid pharmaceutical preparation for oral administration which produces high and long-lasting blood and tissue levels, containing 9-deoxo-11-deoxy-9,11-[imino[2-(2-methoxyethoxy)-ethylidene]oxy]-(9S)-eryt hromycin as active substance, in which the active substance must be intimately mixed with a basic excipient in a ratio of 1 mol of active substance to at least 2 gram-equivalents of basic excipient, and the preparations are coated with a gastric juice-resistant lacquer which is soluble in a pH range of between 5.5 and 6.8, and processes for preparing them. The solid pharmaceutical preparations include tablets, pellets or granules and a syrup can be produced from the latter.
    Type: Grant
    Filed: July 8, 1986
    Date of Patent: July 5, 1988
    Assignee: Dr. Karl Thomae, GmbH
    Inventors: Alain Etienne, Peter Gruber, Ulrich Busch
  • Patent number: 4743606
    Abstract: The present invention discloses 3-[2-(3',5'-di-tert-butyl-4'-hydroxyphenyl)ethenyl]pyridine and its use in treating inflammation, particularly chronic inflammatory diseases such as arthritis, and allergic disorders.
    Type: Grant
    Filed: March 25, 1986
    Date of Patent: May 10, 1988
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Edward S. Lazer
  • Patent number: 4737495
    Abstract: The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.
    Type: Grant
    Filed: May 30, 1986
    Date of Patent: April 12, 1988
    Assignee: Dr. Karl Tomae, GmbH
    Inventors: Andreas Bomhard, Manfred Psiorz, Joachim Heider, Norbert Hauel, Klaus Noll, Berthold Narr, Walter Kobinger, Christian Lillie
  • Patent number: 4732900
    Abstract: New 1,2,4-triazolo-carbamates of general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the specification, are acetylcholinesterase inhibitors and may be used as drugs for the treatment of senile dementia.
    Type: Grant
    Filed: October 25, 1985
    Date of Patent: March 22, 1988
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Dieter Hinzen, Franz-Josef Kuhn, Erich Lehr, Wilhelm Frolke, Wolfgang Troger, Helmut Ensinger, Gerhard Walther, Albrecht Harreus
  • Patent number: 4731374
    Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: March 15, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gerhart Griss, deceased, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
  • Patent number: 4725597
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently hydrogen, alkyl of 1 to 4 carbon atoms, hydroxyl, alkoxy of 1 to 4 carbon atoms, alkanoyloxy of 1 to 4 carbon atoms, halogen, trihalomethyl, di(lower alkyl of 1 to 4 carbon atoms)amino, (alkoxy of 1 to 4 carbon atoms)carbonyl, nitro, cyano or alkanoyl of 1 to 3 carbon atoms;R.sub.7 and R.sub.8 are independently hydrogen, methyl, hydroxyl, carboxyl, (alkoxy of 1 to 4 carbon atoms)carbonyl, hydroxymethyl, phenyl, or p-chlorophenyl;R.sub.9 and R.sub.10 are independently hydrogen or methyl;j and k are independently 0, 1, 2, or 3, their sum being no more than 4;m and n are independently 0, 1, 2, or 3, their sum being no more than 4;A is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --;R.sub.7 and R.sub.9 together are oxo, provided k is other than o;R.sub.8 and R.sub.10 together are oxo, provided m is other than o;R.sub.11 and R.sub.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: February 16, 1988
    Assignee: Boehringer Ingelheim Ltd.
    Inventors: John P. Devlin, Daniel W. McNeil, James J. Keirns, Edward L. Barsumian
  • Patent number: 4724236
    Abstract: Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: February 9, 1988
    Assignee: Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gunter Trummlitz, Wolfhard Engel, Gerhard Mihm, Rudolf Hammer, Norbert Mayer, Antonio Giachetti, Adriaan de Jonge
  • Patent number: 4722926
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or ##STR2## A is alkyl of 1 to 8 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; phenyl; or phenyl mono-, di- or tri-substituted independently with alkyl of 1 to 4 carbon atoms, halogen, trihalomethyl, alkoxy of 1 to 3 carbon atoms, carboxylic acyl of 1 to 3 carbon atoms, carboxyl, (alkoxy of 1 to 3 carbon atoms)carbonyl, nitro, cyano or di(alkyl of 1 to 3 carbon atoms)amino;R.sub.1, R.sub.2 and R.sub.3, are independently hydrogen, halogen, alkyl of 1 to 4 carbon atoms, trihalomethyl, nitro, cyano, di(alkyl of 1 to 4 carbon atoms)amino, (alkoxy of 1 to 4 carbon atoms)carbonyl, alkoxy of 1 to 4 carbon atoms or hydroxyl;R.sub.4 and R.sub.5 are independently hydrogen, alkyl of 1 to 4 carbon atoms, or phenyl;R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently hydrogen or methyl;Y is --CH.sub.2 -- or --CH.sub.2 --CH.sub.
    Type: Grant
    Filed: July 23, 1986
    Date of Patent: February 2, 1988
    Assignee: Boehringer Ingelheim Limited
    Inventors: Karl D. Hargrave, John P. Devlin, Edward A. Barsumian
  • Patent number: 4716169
    Abstract: The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.
    Type: Grant
    Filed: December 17, 1985
    Date of Patent: December 29, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Joachim Heider, Norbert Hauel, Volkhard Austel, Klaus Noll, Andreas Bomhard, Jacques van Meel, Willi Diederen
  • Patent number: 4707475
    Abstract: Disclosed is a method of lowering the prolactin level in the blood or serum of a person which method comprises administering a therapeutically effective amount of 2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo-[5,4-d]azepine or a non-toxic, pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: January 23, 1986
    Date of Patent: November 17, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Victor Brantl, Werner Bomann, Herbert Schill
  • Patent number: 4692448
    Abstract: Disclosed are novel bis(arylpiperazinyl)sulfur compounds represented by formula I ##STR1## wherein: R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, halogen, nitrile or methylthio; m and n are each independently 2 or 3; and X is a dithio, thio, sulfinyl or sulfonyl and nontoxic, pharmaceutically acceptable addition salts thereof. These compounds can be used for the prevention of allergic disorders, such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies, and the like.
    Type: Grant
    Filed: November 20, 1984
    Date of Patent: September 8, 1987
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: John P. Devlin, Karl D. Hargrave
  • Patent number: 4681884
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is hydrogen, methyl, hydroxyl, alkoxy of 1 to 4 carbon atoms, di(alkyl of 1 to 2 carbon atoms)amino-(alkoxy of 1 to 4 carbon atoms) or NHCOCOOR.sub.1 ;R.sub.3 is hydrogen or NHCOCOOR.sub.1 ;A is ##STR2## R.sub.4 is hydrogen, methyl, alkoxy of 1 to 4 carbon atoms, hydroxyl, amino, alkanoyloxy of 1 to 2 carbon atoms, di(alkyl of 1 to 2 carbon atoms)-amino-(alkoxy of 1 to 4 carbon atoms) or acetamido; andR.sub.5 is hydrogen, amino, alkoxy of 1 to 4 carbon atoms, halogen or NHCOCOOR.sub.1 ;and, when R.sub.1 is hydrogen, nontoxic, pharmaceutically acceptable salts thereof. The compounds as well as their salts are useful for the treatment of immunological, inflammatory and allergic disorders such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies and the like.
    Type: Grant
    Filed: May 10, 1985
    Date of Patent: July 21, 1987
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl G. Grozinger, James T. Oliver
  • Patent number: 4678792
    Abstract: This invention relates to a compound of formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; and R.sub.3 is a C.sub.7 -C.sub.9 aralkyl, the phenyl nucleus of which can be mono-, di-, or trisubstituted by halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, and nontoxic, pharmaceutically acceptable salts thereof. The compounds have useful antithrombic properties.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: July 7, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Josef Nickl, Erich Muller, Benthold Narr, Helmut Ballhause, Walter Haarmann
  • Patent number: 4670456
    Abstract: The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.
    Type: Grant
    Filed: May 24, 1985
    Date of Patent: June 2, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
  • Patent number: 4668674
    Abstract: There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a pharmaceutical material.The compound is characterized by a powerful activity against ulcers of the gastro-intestinal tract.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: May 26, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: G/u/ nter Trummlitz, Wolfhard Engel, Wolfgang Eberlein, Gerhard Mihm, Antonio Giachetti
  • Patent number: 4661481
    Abstract: Compounds of the formula ##STR1## having activity as antihistamine or inhibitors of mediator release from basophils or mast cells.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: April 28, 1987
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc
    Inventors: John P. Devlin, Karl D. Hargrave, Edward L. Barsumian, Genus J. Possanza
  • Patent number: 4659584
    Abstract: The specification describes a process and apparatus for charging eye rods with solutions or suspensions of active substance. The latter are applied dropwise, by means of a micrometering device, to specific points on the eye rods which are set in rotation, and simultaneously or subsequently the solvent or suspension agent is removed.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 21, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventor: Leonhard Schilk
  • Patent number: 4645770
    Abstract: The invention describes the use of 2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine and the acid addition salts thereof for the treatment of Parkinson's disease or Parkinsonism.
    Type: Grant
    Filed: February 3, 1986
    Date of Patent: February 24, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Oleh Hornykiewicz, Dieter Hinzen, Gunter Schingnitz