Abstract: N-substituted amides which inhibit hydrolysis of elastin, are described, which compounds are tri-and di- fluoromethyl ketone amide and non-naturally occurring n-substituted amino acids derivatives.
Type:
Grant
Filed:
April 16, 1991
Date of Patent:
June 22, 1993
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
Type:
Grant
Filed:
June 21, 1990
Date of Patent:
June 1, 1993
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
Abstract: The invention relates to new 1,4-diazepines of the general formula ##STR1## in which R.sub.1, R.sub.2 R.sub.3, X and A have the meaning indicated in the specification.The new compounds are intended for use for the treatment of pathological states and diseases in which PAF (platelet activating factor) is involved.
Type:
Grant
Filed:
September 19, 1990
Date of Patent:
May 26, 1992
Assignee:
Boehringer Ingelheim KG
Inventors:
Albrecht Harreus, Karl-Heinz Weber, Werner Stransky, Gerhard Walther, Gojko Muacevic, Jorge C. Stenzel, Wolf-Dietrich Bechtel
Abstract: The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.
Type:
Grant
Filed:
May 7, 1991
Date of Patent:
May 26, 1992
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Andreas Bomhard, Joachim Heider, Manfred Psiorz, Norbert Hauel, Berthold Narr, Klaus Noll, Christian Lillie, Walter Kobinger, Willi Diederen
Abstract: Disclosed are substituted bis(4-aminophenyl-sulfonees of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.
Type:
Grant
Filed:
December 7, 1990
Date of Patent:
January 28, 1992
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Joachim K. Seydel, Helmut Pieper, Gerd Kruger, Klaus Noll, Johannes Keck, Uwe Lechner
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
Abstract: This invention relates to pharmaceutical compositions containing quinolin-2,5-diones of formula ##STR1## wherein A, B, R.sup.1 to R.sup.3 and X are defined hereinbelow, some of which are novel, which compounds have valuable pharmacological properties, particularly analgesic antipyretic and/or antiphlogistic effects, to new intermediates and processes for preparing them.
Type:
Grant
Filed:
September 27, 1989
Date of Patent:
November 26, 1991
Assignee:
Karl Thomae GmbH
Inventors:
Erich Muller, Josef Nickl, deceased, Armin Heckel, Gunther Engelhardt
Abstract: The invention relates to a process for the preparation of lactide, in particular of optically pure L(-)- or D(+)-lactide, on an industrial scale.
Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
Type:
Grant
Filed:
September 22, 1989
Date of Patent:
October 1, 1991
Assignee:
Boehringer Ingelheim KG
Inventors:
Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
Abstract: The use of 6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine and pharmacological acid addition salts thereof for the release of growth hormone.
Abstract: 5,11-Dihydro-6H-pyrido[2,3-b][1,4]-benzo-diazepinones substituted in the 11-position corresponding to general formula I ##STR1## wherein R.sup.1 and R.sup.2 represent hydrogen atoms or alkyl groups having 1 to 3 carbon atoms, A.sup.1 is a straight-chained or branched alkylene group with 1 to 5 carbon atoms, A.sup.2 is a methylene group or, if R.sup.1 is hydrogen and R.sup.2 is methyl, A.sup.2 may also be an ethylene group, and the physiologically acceptable acid addition salts thereof are suitable for treating bradycardia and bradyarrhythmia and spasm in the colon, bladder and bronchi.
Type:
Grant
Filed:
June 15, 1989
Date of Patent:
June 25, 1991
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gerhard Mihm, Wolfgang Eberlein, Welfhard Engel, Gunter Trummlitz, Norbert Mayer, Henri Doods, Rudolf Hammer
Abstract: The invention relates to new morpholines and morpholine-N-oxides of formula ##STR1## wherein the substituents are defined hereunder, which compounds have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat, and the effect of lowering the atherogenic .beta.-lipoproteins VLDL and LDL, and a performance enhancing effect in animals.
Type:
Grant
Filed:
March 23, 1989
Date of Patent:
June 25, 1991
Assignee:
Dr. Karl Thomae, GmbH
Inventors:
Manfred Reiffen, Michael Mark, Robert Sauter, Wolfgang Grell
Abstract: New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
Type:
Grant
Filed:
July 31, 1987
Date of Patent:
November 20, 1990
Assignee:
Karl Thomae GmbH
Inventors:
Wolfhard Engel, Wolfgang Eberlein, Gunter Trummlitz, Gerhard Mihm, Norbert Mayer, Adriaan de Jonge
Abstract: The invention relates to new thieno-traizolo-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 Cl 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:
October 3, 1988
Date of Patent:
November 6, 1990
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Albrecht Harreus, Jorge C. Stenzel, Gojko Muacevic, Wolfgang Troger, Gerhard Walther
Abstract: A metering valve for a pressurized dispensing container. The container is intended to operate in the inverted position. An element having a raised peripheral portion is provided about the valve housing which substantially closes the space between the wall of the container and the valve housing. The element prevents the settling of active substances of the material being dispensed in the region of the inlet opening of the metering valve.
Type:
Grant
Filed:
January 30, 1989
Date of Patent:
July 31, 1990
Assignee:
Boehringer Ingelheim KG
Inventors:
Adolf Knecht, Ottfried Daab, Hans-Hermann Weil