Abstract: Oxoquinazoline derivatives of formulae ##STR1## (the symbols are defined in the specification) are well-tolerated drugs for treating hyperuricaemia.
Abstract: The invention relates to 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:
April 20, 1988
Date of Patent:
August 15, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
Abstract: The use of 6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine and the pharmacological acid addition salts thereof for the release of growth hormone.
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 alkynyl 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 fluorine, 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:
November 23, 1987
Date of Patent:
June 27, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerhart Griss, deceased, Claus Schneider, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or disubstituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
Type:
Grant
Filed:
May 26, 1988
Date of Patent:
May 23, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 6 carbon atoms;n and m are each independently 0, 1 or 2, the sum of n and m being 1 or 2;X, Y and Z are each independently oxygen, sulfur, --NR.sub.4 --, .dbd.CR.sub.5 --, --CHR.sub.5 --, ##STR2## provided that only one of X, Y and Z is O, S, ##STR3## and one or two of X, Y and Z are --NR.sub.4 --; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.5 is hydrogen or, together with a vicinal radical R.sub.5, a phenyl ring, or when m and n are both 1, the dihydro form with its double bond in conjugation with the C-term=inal carboxylic group;or a non-toxic, pharmacologically acceptable salt thereof. The compounds as well as their salts are useful as antihypertensives.
Type:
Grant
Filed:
May 26, 1988
Date of Patent:
May 2, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke
Abstract: This invention relates to the transdermal administration of compounds of general formula I ##STR1## wherein R.sub.1, R.sub.2 and X have the meanings given in the text, and to a therapeutic system for the transdermal administration of this compound.
Type:
Grant
Filed:
December 2, 1986
Date of Patent:
May 2, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Victor Brantl, Volkmar Haselbarth, Bernd Zierenberg
Abstract: The invention relates to the purification of polymers, particularly resorbable polyesters, using shear fields produced mechanically or by fluid dynamics.
Type:
Grant
Filed:
March 18, 1988
Date of Patent:
March 7, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Dieter Bendix, Dieter Reichert, Michael Scharfe
Abstract: A charging valve consisting of a valve sleeve and a valve stem fixed in the interior thereof comprises a valve which acts by compression and tension, the tension or compression being exerted by resilient parts of the valve stem adjacent to both valves.
Abstract: This invention relates to a pharmaceutical tablet containing active substance prone to hydrolysis and having a long shelf life which comprises (1) one or more layers free from active substance and (2) a layer containing said active substance in a concentration sufficient to inhibit hydrolysis.
Abstract: The invention relates to novel N-alkylnorscopines wherein the alkyl group may have 2 to 10 carbon atoms, which are useful in the preparation of valuable pharmaceutical compositions. These compounds may be prepared from the corresponding N-alkylnorscopolamines by hydrogenolysis with complex hydrides, which reaction is preferably carried out with sodium borohydride in ethanol at ambient temperature.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di- substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
Type:
Grant
Filed:
June 26, 1986
Date of Patent:
August 30, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 6 carbon atoms;n and m are each independently 0, 1 or 2, the sum of n and m being 1 or 2;X, Y and Z are each independently oxygen, sulfur, --NR.sub.4 --, .dbd.CR.sub.5 --, --CHR.sub.5 --, ##STR2## provided that only one of X, Y and Z is O, S, ##STR3## and one or two of X, Y and Z are --R.sub.4 --; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.5 is hydrogen or, together with a vicinal radical R.sub.5, a phenyl ring, or when m and n are both 1, the dihydro form with its double bond in conjugation with the C-terminal carboxylic group;or a non-toxic, pharmacologically acceptable salt thereof. The compounds as well as their salts are useful as antihypertensives.
Type:
Grant
Filed:
May 6, 1987
Date of Patent:
August 23, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke
Abstract: 5,6,-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## are prepared by heating a 1-(3-furyl)-3,4-dihydro-isoquinoline of the formula ##STR2## in a primary or secondary amine to at least 80.degree. C. for several hours, the amine is removed, the reaction product is treated with dilute acid, and the reaction product is purified and isolated.
Type:
Grant
Filed:
June 16, 1987
Date of Patent:
August 23, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Walter Losel, Otto Roos, Gerd Schnorrenberger
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
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
Abstract: Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.
Type:
Grant
Filed:
June 4, 1986
Date of Patent:
January 19, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
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