Abstract: The invention relates to new benzenesulphonamidoindanyl compounds having the following formula ##STR1## wherein the substituents are defined herein useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.
Type:
Grant
Filed:
July 16, 1987
Date of Patent:
April 11, 1989
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
Abstract: The present invention discloses 3-[2-(3',5'-di-tert-butyl-4'-hydroxyphenyl)ethenyl]pyridine and its use in treating inflammation, particularly chronic inflammatory diseases such as arthritis, and allergic disorders.
Type:
Grant
Filed:
December 21, 1987
Date of Patent:
March 14, 1989
Assignee:
Boehringer Ingelheim Pharmaceutical, Inc.
Abstract: The invention relates to the purification of polymers, particularly resorbable polyesters, using shear fields produced mechanically or by fluid dynamics.
Type:
Grant
Filed:
March 18, 1988
Date of Patent:
March 7, 1989
Assignee:
Boehringer Ingelheim KG
Inventors:
Dieter Bendix, Dieter Reichert, Michael Scharfe
Abstract: A charging valve consisting of a valve sleeve and a valve stem fixed in the interior thereof comprises a valve which acts by compression and tension, the tension or compression being exerted by resilient parts of the valve stem adjacent to both valves.
Abstract: Compounds of the formula ##STR1## R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.2 is hydrogen, methyl, hydroxyl, alkoxy of 1 to 4 carbon atoms, di(alkyl of 1 to 2 carbon atoms)amino-(alkoxy of 1 to 4 carbon atoms) or NHCOCOOR.sub.1 ;R.sub.3 is hydrogen or NHCOCOOR.sub.1 ;A is ##STR2## R.sub.4 is hydrogen, methyl, alkoxy of 1 to 4 carbon atoms, hydroxyl, amino, alkanoyloxy of 1 to 2 carbon atoms, di(alkyl of 1 to 2 carbon atoms)-amino-(alkoxy of 1 to 4 carbon atoms) or acetamido; andR.sub.5 is hydrogen, amino, alkoxy of 1 to 4 carbon atoms, halogen or NHCOCOOR.sub.1 ;and, when R.sub.1 is hydrogen, nontoxic, pharmaceutically acceptable salts thereof. The compounds as well as their salts are useful for the treatment of immunological, inflammatory and allergic disorders such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies and the like.
Type:
Grant
Filed:
April 27, 1987
Date of Patent:
November 29, 1988
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed is a method of treating cognitive decline in a normal aged primate by administering thereto a therapeutically effective amount of 2-[(2,6-dichlorophenyl)-amino]-2-imidazoline or a nontoxic, pharmaceutically acceptable salt thereof. Administration is preferably in amounts of at least about 0.001 mg/day.
Type:
Grant
Filed:
November 6, 1986
Date of Patent:
November 15, 1988
Assignee:
Yale University
Inventors:
Patricia S. Goldman-Rakic, Amy F. T. Arnsten
Abstract: The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.
Type:
Grant
Filed:
December 18, 1986
Date of Patent:
August 9, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Claus Schneider, Gerhard Walther, Dieter Hinzen, Franz J. Kuhn, Erich Lehr, Helmut Ensinger, Wolfgang Troger
Abstract: There is described a solid pharmaceutical preparation for oral administration which produces high and long-lasting blood and tissue levels, containing 9-deoxo-11-deoxy-9,11-[imino[2-(2-methoxyethoxy)-ethylidene]oxy]-(9S)-eryt hromycin as active substance, in which the active substance must be intimately mixed with a basic excipient in a ratio of 1 mol of active substance to at least 2 gram-equivalents of basic excipient, and the preparations are coated with a gastric juice-resistant lacquer which is soluble in a pH range of between 5.5 and 6.8, and processes for preparing them. The solid pharmaceutical preparations include tablets, pellets or granules and a syrup can be produced from the latter.
Type:
Grant
Filed:
July 8, 1986
Date of Patent:
July 5, 1988
Assignee:
Dr. Karl Thomae, GmbH
Inventors:
Alain Etienne, Peter Gruber, Ulrich Busch
Abstract: The present invention discloses 3-[2-(3',5'-di-tert-butyl-4'-hydroxyphenyl)ethenyl]pyridine and its use in treating inflammation, particularly chronic inflammatory diseases such as arthritis, and allergic disorders.
Type:
Grant
Filed:
March 25, 1986
Date of Patent:
May 10, 1988
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.
Type:
Grant
Filed:
May 30, 1986
Date of Patent:
April 12, 1988
Assignee:
Dr. Karl Tomae, GmbH
Inventors:
Andreas Bomhard, Manfred Psiorz, Joachim Heider, Norbert Hauel, Klaus Noll, Berthold Narr, Walter Kobinger, Christian Lillie
Abstract: New 1,2,4-triazolo-carbamates of general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the specification, are acetylcholinesterase inhibitors and may be used as drugs for the treatment of senile dementia.
Type:
Grant
Filed:
October 25, 1985
Date of Patent:
March 22, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Dieter Hinzen, Franz-Josef Kuhn, Erich Lehr, Wilhelm Frolke, Wolfgang Troger, Helmut Ensinger, Gerhard Walther, Albrecht Harreus
Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.
Type:
Grant
Filed:
December 19, 1985
Date of Patent:
March 15, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gerhart Griss, deceased, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
Abstract: Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.
Type:
Grant
Filed:
December 19, 1986
Date of Patent:
February 9, 1988
Assignee:
Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Gunter Trummlitz, Wolfhard Engel, Gerhard Mihm, Rudolf Hammer, Norbert Mayer, Antonio Giachetti, Adriaan de Jonge
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or ##STR2## A is alkyl of 1 to 8 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; phenyl; or phenyl mono-, di- or tri-substituted independently with alkyl of 1 to 4 carbon atoms, halogen, trihalomethyl, alkoxy of 1 to 3 carbon atoms, carboxylic acyl of 1 to 3 carbon atoms, carboxyl, (alkoxy of 1 to 3 carbon atoms)carbonyl, nitro, cyano or di(alkyl of 1 to 3 carbon atoms)amino;R.sub.1, R.sub.2 and R.sub.3, are independently hydrogen, halogen, alkyl of 1 to 4 carbon atoms, trihalomethyl, nitro, cyano, di(alkyl of 1 to 4 carbon atoms)amino, (alkoxy of 1 to 4 carbon atoms)carbonyl, alkoxy of 1 to 4 carbon atoms or hydroxyl;R.sub.4 and R.sub.5 are independently hydrogen, alkyl of 1 to 4 carbon atoms, or phenyl;R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently hydrogen or methyl;Y is --CH.sub.2 -- or --CH.sub.2 --CH.sub.
Type:
Grant
Filed:
July 23, 1986
Date of Patent:
February 2, 1988
Assignee:
Boehringer Ingelheim Limited
Inventors:
Karl D. Hargrave, John P. Devlin, Edward A. Barsumian
Abstract: The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.
Type:
Grant
Filed:
December 17, 1985
Date of Patent:
December 29, 1987
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Joachim Heider, Norbert Hauel, Volkhard Austel, Klaus Noll, Andreas Bomhard, Jacques van Meel, Willi Diederen
Abstract: Disclosed is a method of lowering the prolactin level in the blood or serum of a person which method comprises administering a therapeutically effective amount of 2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo-[5,4-d]azepine or a non-toxic, pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
January 23, 1986
Date of Patent:
November 17, 1987
Assignee:
Boehringer Ingelheim KG
Inventors:
Victor Brantl, Werner Bomann, Herbert Schill
Abstract: A new antibacterial agent designated LL-C19004 is described, which antibacterial agent is produced through microbiological fermentation, under controlled conditions using a new species of Saccharothrix, Saccharothrix espanaensis (NRRL 15764).
Type:
Grant
Filed:
September 13, 1985
Date of Patent:
October 13, 1987
Assignee:
American Cyanamid Company
Inventors:
Jane P. Kirby, Donald B. Borders, May D. Lee, William M. Maiese, Raymond T. Testa, David P. Labeda
Abstract: Vinylstannyl derivatives and the processes for their conversion to vinyliodides, vinylbromides and vinyllithium reagents. The vinylstannyl, vinyliodides, vinylbromide derivatives and vinyllithiums are useful as intermediates for the preparation of prostaglandin analogs.
Type:
Grant
Filed:
October 7, 1983
Date of Patent:
October 16, 1984
Assignee:
American Cyanamid Company
Inventors:
Middleton B. Floyd, Jr., Charles V. Grudzinskas, Sow-Mei L. Chen