Abstract: A compound of formula I ##STR1## wherein A denotes a benzo, indolo or thieno group;R.sup.1 denotes thienyl or the group ##STR2## whereinR.sup.7, R.sup.8 and R.sup.9 independently of one another may represent methyl, ethyl, propyl, phenyl or benzyl, whilst not more than 2 of the substituents can simultaneously represent phenyl or benzyl;R.sup.2, m, R.sup.3 and R.sup.4 are defined as in the specification, as well as pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
Type:
Grant
Filed:
December 21, 1994
Date of Patent:
March 4, 1997
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Walter L osel, Otto Roos, Dietrich Arndts
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-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-2-carboxylic acid.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
February 11, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
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: 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 compound is:4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-ben zimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
January 14, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
Abstract: Disclosed herein are 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:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
January 7, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
Abstract: Cyclic imino derivatives of the formulaB--X.sub.2 --X.sub.1 --A--Y--E (I)wherein A, B, E, X.sub.1, X.sub.2 and Y are as defined herein, the stereoisomers, tautomers, mixtures and addition salts thereof, pharmaceutical compositions containing these compounds and processes for preparing them. The cyclic imino derivatives are useful as inhibitors of cell-cell and cell-matrix interactions, e.g., thrombocyte aggregation.
Type:
Grant
Filed:
April 26, 1993
Date of Patent:
November 19, 1996
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Austel Volkhard, Helmut Pieper, Guenter Linz, Johannes Weisenberger, Thomas Mueller
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
Abstract: The present invention relates to an improved process for preparing 1,2-5,6-diacetone-D-glucose from D-glucose and diketene or the adduct of diketene with acetone.
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: Xanthines of the formula I ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group:R.sub.2 is a C.sub.1 -C.sub.4 alkyl group;R.sub.3 tetrahydropyran-4-yl or 1,3-dithiolan or;R.sub.3 represents one of the groups of formula ##STR2## and pharmaceutically acceptable acid addition salts thereof. These are adenosine antagonists, capable of acting as cholinomimetics, useful for the treatment of CNS disorders such as senile dementia and Alzheimer's disease.
Type:
Grant
Filed:
July 27, 1993
Date of Patent:
July 2, 1996
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Ulrike Kufner-Muhl, Karl-Heinz Weber, Gerhard Walther, Werner Stransky, Helmut Ensinger, Gunter Schingnitz, Franz J. Kuhn, Erich Lehr
Abstract: The invention relates to an ophthalmic solution for topical application to the eye in order to lower increased intraocular pressure of the aqueous humor, containing a quantity of a polyhydroxyalcohol such as sorbitol, mannitol, inositol or xylitol or mixtures thereof, effective for lowering the intraocular pressure of aqueous humor, in a carrier tolerated by the eye, the use thereof and the preparation thereof.
Type:
Grant
Filed:
August 19, 1993
Date of Patent:
June 18, 1996
Assignee:
Basotherm GmbH
Inventors:
Helmut Franz, Hannes E. Kompa, Tibor Rozman
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: The present invention relates to a novel class of benzoylecgonine, ecgonine and ecgonidine derivatives which are useful for preventing and treating immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. The compounds of this invention are conveniently obtained by chemical synthesis. Accordingly, this invention also relates to methods for preparing the benzoylecgonine, ecgonine and ecgonidine derivatives and to pharmaceutical compositions containing these derivatives.
Abstract: This invention relates to 1-amino thioacylbenzimidazoyl-2-one derivatives having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined herein. These compounds are useful as thioacylating reagents. This invention also relates to a process for producing cyclic and linear thiopeptides using the thioacylating reagents of this invention. This invention further relates to intermediate anilide compounds, which are produced by reacting an ortho phenylene diamine with an amino acid chain or peptide. This invention also relates to intermediate thioanilide compounds, which are produced by thionating the intermediate anilide compounds. This invention further relates to a process for producing the thioacylating reagents of this invention by cyclizing the intermediate thioanilide compounds.
Type:
Grant
Filed:
February 21, 1992
Date of Patent:
December 6, 1994
Assignee:
Biochem Pharma Inc.
Inventors:
Bernard Belleau, Denis Brillon, Gilles Sauve, Boulos Zacharie