Abstract: The invention relates to the use of 9-amino-pyridazino-?4',5':3,4!pyrrolo?2,1-a!isoquinolines of the formula ##STR1## and the physiologically acceptable salts thereof with acids, bases and complexing agents for preparing agents for treating chronic inflammatory processes, ulcerative colitis and Crohn's disease, and for producing agents having an antiproliferative activity. The definitions of substituents R.sub.1 to R.sub.9 are given in the specification. The invention also relates to new compounds of general formula I which are also defined in the specification and their use as cerebroprotective agents.
Type:
Grant
Filed:
May 17, 1996
Date of Patent:
October 14, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter Losel, Otto Roos
Abstract: This invention relates to a process for preparing xanthine derivatives of formula I: ##STR1## characterized in that a uracil derivative of formula A or B ##STR2## is dissolved in a suitable organic-aqueous solvent and cyclized in the presence of LiOH.
Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 7, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter Losel, Otto Roos
Abstract: The invention relates to the use of carbocyclically and heterocyclically fused dihydropyridines as cerebroprotective agents, as agents for treating chronic inflammatory processes and as agents for inhibiting blood clotting, and also relates to new compounds of formula Ie ##STR1##
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
September 9, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Walter Losel, Otto Roos, Dietrich Arndts, Franz Josef Kuhn, Ilse Strelle
Abstract: The present invention relates to a new and improved process for preparing 2-amino-6-chloropurine comprising the step of reacting guanine in the presence of ammonium sulphate with hexamethyldisilazane. The process of this invention advantageously results in a high yield of 2-amino-6-chloropurine and may be carried out on a laboratory or an industrial scale.
Abstract: Compound of general formula I ##STR1## wherein A denotes a benzo, indolo or thienyl group;B denotes the group --0--, --S-- or --CHR.sup.5 --, wherein R.sup.5 is hydrogen, (C.sub.1-6)alkyl, phenyl or benzyl;R.sup.3 denotes 2- or 3-thienyl, (C.sub.4-7)cycloalkyl, (C.sub.4-6)cycloalkyl(C.sub.1-5)alkyl or ##STR2## wherein R is (C.sub.1-4)alkyl, hydroxy, --N.sub.3, halogen (F, Cl, Br, I), CF.sub.3 or (C.sub.1-4)alkoxy,u is 0, 1, 2 or 3, andm, R.sup.2, R.sup.4, R.sup.7, R.sup.8 and R.sup.9 are as defined in the specification, as well as pharmaceutical preparations containing these compounds and the pharmaceutical use thereof.
Type:
Grant
Filed:
December 21, 1994
Date of Patent:
August 26, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Otto Roos, Walter Losel, Dietrich Arndts
Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.
Type:
Grant
Filed:
March 28, 1995
Date of Patent:
August 5, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Rolf Banholzer, Rudolf Bauer, Richard Reichl
Abstract: In an inhaler for powdered drugs, flat carriers are used which have regular microstructures between which the powder for inhalation is embedded.
Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
July 1, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter Losel, Otto Roos
Abstract: New xanthine compounds of formula I: ##STR1## wherein the substituents are defined herein, which xanthines are useful as adenosine antagonists.
Type:
Grant
Filed:
December 22, 1994
Date of Patent:
June 24, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Ulrike Kufner-Muhl, Werner Stransky, Gerhard Walther, deceased, Karl-Heinz Weber, Helmut Ensinger, Franz Josef Kuhn, Gunter Schingnitz, Erich Lehr
Abstract: A method of preparing sugar acetonides, such as for example 1,2:5,6-Di-O-isopropylidene-.alpha.-D-glucofuranose, by reacting the corresponding sugar, e.g. D-(+)-glucose, with acetone in the presence of a Lewis acid and a carboxylic acid derivative of general formula ##STR1## wherein X is a leaving group which may be readily replaced by a hydroxyl group.
Type:
Grant
Filed:
September 6, 1994
Date of Patent:
May 6, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Rainer Sobotta, Franz Dietrich Klinger, Heinrich Schneider
Abstract: The invention relates to a propellant-free inhaler which has a storage chamber (6) for a powdered substance to be inhaled, which is associated with a metering device (8), which is manually operated by means of a button, having a metering chamber (7) for receiving a given dose of the powdered substance. The device also has a lateral mouth piece (11) for active breathing in, with an air channel (7) for distributing the particular dose of the powdered substance in the air stream. To ensure that the dosage provided is highly reproducible, a high proportion of this dose leaves the inhaler and the medicinal substance is reproducibly dispersed, a trigger operated pump (12,19,20) is provided which can be manually primed before the inhalation process by means of a button (1,42) and which can be actuated in synchronism with the breathing, thereby generating a current of foreign air which disperses the metered substance.
Type:
Grant
Filed:
May 3, 1994
Date of Patent:
April 8, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerhard Poss, Jurgen Wittekind, Andreas Kuhnel
Abstract: The invention is directed to a process for preparing a 1,3-dialkyl-5-hydroxyoxindole of formula 1: ##STR1## comprising heating an N-alkyl-p-alkoxy-(.alpha.-haloacyl)anilide of formula 2: ##STR2## wherein the substituents are as defined herein, in the presence of an anhydrous zinc halide to a temperature in the range from about 120.degree. C. to about 160.degree. C., and isolating the 1,3-dialkyl-5-hydroxyoxindole prepared.
Abstract: Novel benzomorphan derivatives of the formula ##STR1## wherein R.sup.1 -R.sup.8 are as defined herein. The benzomorphan derivatives are useful for treating cerebral ischaemia of various origins, epilepsy and neurodegenerative diseases.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
March 4, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Herbert Merz, Enzio Mueller, Werner Stransky, Ilse Streller
Abstract: A method for stimulating diuresis comprising administering a composition comprising 8-(3-oxocyclopentyl)-1,3-di-n-propyl-7H-purine-2,6-dione and, optionally, a loop diuretic, is disclosed.
Type:
Grant
Filed:
July 6, 1995
Date of Patent:
February 4, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Stefan Adamus, Wolfram Gaida, Christopher Meade, Ulrike K ufner-Muhl
Abstract: The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR2## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
September 2, 1993
Date of Patent:
January 21, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Birgit Jung, Erich Burger
Abstract: The invention relates to a propellant-free inhalation device with a supply of pulverized medical substance in a supply chamber, which has a rotatable dosing means with one or more dosing chambers to receive in one defined position the dose of the medical substance to be inhaled from the supply chamber and to discharge the dose in another position. The inhalation device further is provided with a mouthpiece for active inhalation and an air channel to distribute the dose discharged from the dosing chamber in the flow of breathing air.
Abstract: A process for preparing nevirapine which comprises reacting 2-chloro-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridine carboxamide with cyclopropylamine followed by cyclisation of the product, wherein the reaction with cyclopropylamine is carried out in the presence of an oxide or hydroxide of an element of the second main or sub-group of the periodic table of elements.
Type:
Grant
Filed:
January 12, 1995
Date of Patent:
October 29, 1996
Assignee:
Boehringer Ingelheim KG
Inventors:
Heinrich Schneider, Albrecht Christmann
Abstract: The invention relates to the use of 9-amino-pyridazino-[4', 5':3,4]pyrrolo[2,1-a]isoquinolines of the formula ##STR1## and the physiologically acceptable salts thereof with acids, bases and complexing agents for preparing agents for treating chronic inflammatory processes, ulcerative colitis and Crohn's disease, and for producing agents having an antiproliferative activity. The definitions of substituents R.sub.1 to R.sub.9 are given in the specification. The invention also relates to new compounds of general formula I which are also defined in the specification and their use as cerebroprotective agents.
Type:
Grant
Filed:
November 7, 1994
Date of Patent:
October 15, 1996
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter L osel, Otto Roos