Abstract: The invention relates to new hetrazepines of general formula ##STR1## wherein A, Z, n, X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.
Type:
Grant
Filed:
September 8, 1994
Date of Patent:
July 2, 1996
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl H. Weber, Albrecht Harreus, Werner Stransky, Gerhard Walther, Jorge Casals-Stenzel, Gojko Muacevic, Hubert Heuer, Wolf-Dietrich Bechtel
Abstract: The present invention relates to a new process for preparing enantiomerically pure diarylprolinols, especially (R)-(+)- or (S)-(-)-2-(diphenylhydroxymethyl)-pyrrolidine (R)-(+)- or (S)-(-)-.alpha.,.alpha.-diphenyl-(2-pyrrolidinyl)-methanol) starting from proline.
Abstract: The present invention relates to an improved process for preparing 1,3-dimethyl-4,5-diaminouracil by catalytic reduction of 1,3-dimethyl-4-amino-5-nitrosouracil in the presence of a palladium/charcoal catalyst.
Abstract: In a device for initiating a mechanical switching operation in inhalers, in synchronism with the breathing, a membrane like transmitter element (47) is provided which cooperates with a release mechanism (45, 46, 50) on a switching device (13, 19c, 22).
Type:
Grant
Filed:
February 22, 1994
Date of Patent:
April 16, 1996
Assignee:
Boehringer Ingelheim KG
Inventors:
Andreas Kuhnel, Gerhard Poss, Jurgen Wittekind, Dieter Hochrainer
Abstract: Racemates are obtained from non-racemic 3-oxocyclopentane or 3-oxocyclohexane carboxylic acids or their esters by esterification and ketalization of the non-racemic acid with orthoformic acid ester in an alocohol, racemization and hydrolysis of the product obtained with an alcoholate and isolation of the racemate.
Abstract: In order to control and optimize the amount of inhalable active substance released when drugs are administered as inhalation powders, the invention calls for the use of auxiliaries consisting of mixtures of coarser particles (average particle size>20 .mu.m) and finer particles (average particle size<10 .mu.m).
Type:
Grant
Filed:
August 15, 1994
Date of Patent:
December 26, 1995
Assignee:
Boehringer Ingelheim KG
Inventors:
Klaus Arnold, Peter Grass, Adolf Knecht, Robert Roos, Gerhard Sluke, Herbet Thieme, Joachim Wenzel
Abstract: A novel process for preparing enantiomerically pure (S)- or (R)-but-3-en-2-ol compounds includes the following reaction steps:(a) reacting an alkyl ester of D- or L-lactic acid with a hydropyran compound to obtain a lactate ester having a hydropyranyl ether group,(b) reducing the lactate ester with an aluminum hydride at a temperature below 0.degree. C. to obtain a propionaldehyde having a hydropyranyl ether group,(c) reacting the propionaldehyde with an alkyl phosphonium salt to obtain a 3-butene having a hydropyranyl ether group, and(d) cleaving the hydropyranyl ether group to prepare the enantiomerically pure (S)- or (R)- but-3-en-2-ol.
Abstract: The invention relates to new tetrahydropyridine derivatives, processes for preparing them and their use as pharmaceutical compositions with cholinomimetic properties.
Type:
Grant
Filed:
October 29, 1993
Date of Patent:
June 6, 1995
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerhard Walther, Karl-Heinz Weber, Werner Stransky, Franz J. Kuhn, Erich Lehr, Enzio Muller, Gunter Schingnitz, Helmut Ensinger
Abstract: The invention relates to a propellent-free inhalation device having a supply of solidified medicinal substance to be inhaled, a manually operable metering device for removing a given dose of the medicinal substance for the inhalation process and having a mouthpiece for actively breathing in and an air space for distributing the particular dose of medicinal substance in the air stream. An abrasion device, in the form of a brush comprising a plurality of bristles, is used to abrade the medicinal substance to form the dose.
Abstract: The present invention relates to a process for preparing 3-amino-9,13b-dihydro-1H-dibenz[c,f]-imidazo[1,5-a]azepine-hydrochloride, as follows:a) hydrogenating 6-phthalimidomethyl-5H-dibenz[b,e]-azepine, to produce 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine;b) reacting the 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine with hydrazine, to produce 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine;c) reacting the 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine with bromooyanogen, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine; andd) precipitating the 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine in the presence of DMF and HCl, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine-hydrochloride.
Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
Type:
Grant
Filed:
June 15, 1990
Date of Patent:
March 23, 1993
Assignee:
Boehringer Ingelheim KG
Inventors:
Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
Abstract: The invention relates to new diazephines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein, processes for preparing them and their use as pharmaceutical compositions useful for treating PAF-induced disease.
Type:
Grant
Filed:
January 15, 1992
Date of Patent:
February 9, 1993
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Werner Stransky, Ulrike Kuefner-Muehl, Hubert Heuer, Franz Birke, Wolf-Dietrich Bechtel
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:
September 4, 1991
Date of Patent:
September 22, 1992
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
Abstract: An inhalator device includes a housing in which an ultrasonic atomizer is disposed. A device delivers a medication to the ultrasonic atomizer. A mouthpiece is disposed downstream of the ultrasonic atomizer in flow direction of the medication defining a space between the ultrasonic atomizer and the mouthpiece. The housing has an air inlet opening formed therein communicating with the space downstream of the ultrasonic atomizer.
Type:
Grant
Filed:
December 11, 1989
Date of Patent:
August 4, 1992
Assignees:
Siemens Aktiengesellschaft, Boehringer Ingelheim KG
Inventors:
Klaus van der Linden, Juergen Friedrich, Bernd Zierenberg
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 invention relates to the transdermal administration of 2-amino-6-n-propylamino-4,5,6,7-tetrahydrobenzothiazole or the (-)-enantiomer thereof and transdermal systems containing these active substances.
Type:
Grant
Filed:
November 8, 1990
Date of Patent:
May 12, 1992
Assignee:
Boehringer Ingelheim KG
Inventors:
Bernd Zierenberg, Michael Herschel, Uwe Rohr