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: An improved bio-reactor with spiral or coil-shaped filling bodies is disclosed, the improvement comprising use of a gas diffusion tube through which air, oxygen or other gases can be bubbled through the fermentation medium.
Type:
Grant
Filed:
February 24, 1995
Date of Patent:
September 30, 1997
Assignee:
Boehringer Ingelheim Animal Health, Inc.
Abstract: A process for the preparation of a 3-amino-2-chloro-4-alkylpyridine of the formula: ##STR1## wherein R is alkyl of from one to three carbon atoms, an intermediate in the preparation of certain 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine compounds useful in the prevention and treatment of HIV infection.
Type:
Grant
Filed:
August 14, 1995
Date of Patent:
September 16, 1997
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Karl G. Grozinger, Karl D. Hargrave, Julian Adams
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: Disclosed herein are pentapeptide derivatives of the formula (SEQ ID NO: 24) XNR.sup.1 --CH(R.sup.2)--C(O)--NH--CH(R.sup.3 --C(O)--NR.sup.4 --CH(CH.sub.2 Y)--CO--NH--CH[CR.sup.5 (R.sup.6)--COOH]--C(W)--NH--CH(R.sup.7)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is alkyl or phenylalkyl, R.sup.2, R.sup.3 and R.sup.7 are selected from the side chains of amino acid or derived amino acid residues, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or lower alkyl, W is oxo or thioxo, Y is carboxy, carbamyl or 5-1H-tetrazolyl and Z is carboxy or 5-1H-tetrazolyl. The derivatives are useful for treating herpes infections.
Type:
Grant
Filed:
July 13, 1993
Date of Patent:
July 15, 1997
Assignee:
Bio-Mega/Boehringer Ingelheim Research Inc.
Inventors:
Julian Adams, Pierre Louis Beaulieu, Pierre Lavallee, Raymond Plante, Sumanas Rakhit
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: The invention relates to a process and apparatus for the controlled release of metered quantities of finely divided solids with one or more regulated venturi nozzles for the purpose of applying lubricant or separating compound to the stressed surfaces of pressing tools in tablet making machines or for applying finely divided solids to solid carrier materials particularly in the fields of pharmaceuticals, foodstuffs or catalysts.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
April 29, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Boldis, Volker I. Glasel, Ekkehard Flaischlen, Gunther M. Voss
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: The invention relates to cyclic derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined in claim 1, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing the compounds and processes for preparing them.
Type:
Grant
Filed:
May 2, 1995
Date of Patent:
March 18, 1997
Assignee:
Karl Thomae GmbH
Inventors:
F. Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Brian Guth, Thomas Muller, Johannes Weisenberger
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: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
Type:
Grant
Filed:
May 16, 1994
Date of Patent:
January 28, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
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 cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
January 7, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Volkhard Austel, Helmut Pieper, Wolfgang Eisert, Thomas Mueller, Johannes Weisenberger, Guenter Linz, Gerd Krueger
Abstract: Pharmacologically active benzimidazolone derivatives as 5-HT.sub.1A and 5-HT.sub.2 receptors, useful in the treatment of CNS disorders, of formula: ##STR1## wherein the substituents are defined herein.
Type:
Grant
Filed:
March 23, 1994
Date of Patent:
November 19, 1996
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Giuseppe Bietti, Franco Borsini, Marco Turconi, Ettore Giraldo, Maura Bignotti
Abstract: Disclosed herein are peptide derivatives of the formula A-B-D-CH.sub.2 CH{CH.sub.2 C(O)R.sup.1 }C(O)-NHCH{CR.sup.2 (R.sup.3)COOH}C(O)-E wherein A is a terminal group, for example an optionally substituted phenylalkanoyl, and B is a N-methyl amino acid residue; or A and B together form a saturated or unsaturated alkylaminocarbonyl; D is an amino acid residue; R.sup.1 is alkyl, cycloalkyl, a monosubstituted or a disubstituted amino; R.sup.2 is hydrogen or alkyl and R.sup.3 is alkyl, or R.sup.2 is hydrogen and R.sup.3 is phenylalkyl, or R.sup.2 and R.sup.3 are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.
Type:
Grant
Filed:
October 17, 1994
Date of Patent:
November 12, 1996
Assignee:
Bio-Mega/Boehringer Ingelheim Research Inc.
Inventors:
Pierre L. Beaulieu, Robert D eziel, Neil Moss, Raymond Plante
Abstract: Disclosed are novel pyridodiazepines. These compounds, as well certain known 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.
Type:
Grant
Filed:
August 17, 1994
Date of Patent:
November 5, 1996
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Karl D. Hargrave, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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