Abstract: Disclosed are novel 8-arylalkyl-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines. These are useful in the treatment of HIV-1 infection.
Type:
Grant
Filed:
September 25, 1996
Date of Patent:
January 6, 1998
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles L. Cywin, MaryAnn Hoermann, Janice M. Klunder
Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 9, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
Abstract: The invention relates to new xanthine derivatives of general formula I, processes for preparing them and their use as pharmaceutical compositions.
Type:
Grant
Filed:
June 14, 1996
Date of Patent:
November 18, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Ulrike Kufner-Muhl, Karl-Heinz Weber, Gerhard Walther, Werner Stransky, Helmut Ensinger, Gunter Schingnitz, Franz Josef Kuhn, Erich Lehr
Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.
Type:
Grant
Filed:
February 20, 1996
Date of Patent:
November 4, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
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: Disclosed herein are compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or (1-4C) alkyl, R.sup.2 is (1-4C) alkyl or a therapeutically acceptable salt thereof. The compounds are useful for treating herpes infections.
Type:
Grant
Filed:
June 18, 1996
Date of Patent:
September 30, 1997
Assignee:
Bio-Mega/Boehringer Ingelheim Research, Inc.
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: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
Type:
Grant
Filed:
August 29, 1995
Date of Patent:
July 22, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
Abstract: The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.
Type:
Grant
Filed:
November 29, 1994
Date of Patent:
July 15, 1997
Assignee:
Boehringer Ingelheim Vetmedica GmbH
Inventors:
Wolfgang Resemann, Adolf Durr, Gunther Engelhardt, John Frances Quirke
Abstract: In an inhaler for powdered drugs, flat carriers are used which have regular microstructures between which the powder for inhalation is embedded.
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 trisubstituted pyrimido [5,4-d]-pyrimidines of general formula ##STR1## (wherein R.sub.a, R.sub.b and R.sub.c are defined as in claim 1) and the salts thereof, more particularly for pharmaceutical use the physiologically acceptable salts thereof, which have, inter alia, valuable pharmacological properties, particularly in chemotherapy a sensitizing effect on resistant tumors, the use thereof and processes for preparing them.
Abstract: Racemic mixtures of 1-(S,R)-(2-pyridyl)-2-cyclohexylethylamine are separated into (+)-(S)-1-(2-pyridyl)-2-cyclohexylethylamine or (-)-(R)-1-(2-pyridyl)-2-cyclohexylethylamine by admixture with (+)- or (-)-3-bromocamphor-8-sulfonic acid. 1-(S)-(2-pyridyl)-2-cyclohexylethylamine is an intermediate in the preparation of leukotriene biosynthesis inhibitors.
Type:
Grant
Filed:
April 20, 1995
Date of Patent:
April 1, 1997
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(1-(2-N-morpholinoethyl)-imidazol-4-yl)-benzimi dazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
March 25, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth