Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
Type:
Grant
Filed:
October 14, 1992
Date of Patent:
May 23, 1995
Assignee:
Karl Thomae GmbH
Inventors:
Guenter Linz, Helmut Pieper, Frank Himmelsbach, Austel: Volkhard, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
Abstract: The invention relates to phenylethanolamines of general formula ##STR1## wherein R.sub.1 and R.sub.2 are defined as in claim 1, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, not only analgesic, antiphlogistic, broncholytic, uterus-spasmolytic, lipolytic effects and an antispastic effect on the cross-striped muscle, but also .beta..sub.2 -mimetic and/or .beta..sub.1 -blocking effects, the use thereof as pharmaceuticals and as performance enhancers and processes for preparing them.
Abstract: The invention includes a mouse erythroblastoid cell line whose growth is responsive to levels of erythropoietin present in the cell line's growth medium. Also disclosed are methods of using the mouse erythroblastoid cell line to assay the amount of erythropoietin that is present in a sample.
Type:
Grant
Filed:
February 18, 1993
Date of Patent:
February 14, 1995
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Gordon Keller, Harmut Beug, Erwin Wagner
Abstract: Disclosed herein is a combination of an antiviral nucleoside analog and a ribonucleotide reductase inhibiting peptide derivative. The combination is useful for treating herpes infections.
Abstract: Pharmaceutical forms of pimobendan for oral administration comprising citric acid, whereby a constant, satisfactory resorption is ensured even when there are major pH fluctuations in the gastrointestinal tract.
Type:
Grant
Filed:
March 16, 1993
Date of Patent:
November 15, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Peter Gruber, Willy Roth, Gottfried Schepky
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:
May 21, 1993
Date of Patent:
October 18, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Boldis, Volker I. Glasel, Ekkehard Flaischlen, Gunther M. Voss
Abstract: Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration.
Type:
Grant
Filed:
December 10, 1992
Date of Patent:
October 11, 1994
Assignee:
Bio-Mega, Inc.
Inventors:
Paul C. Anderson, Gary W. Bantle, Grace L. Jung, Pierre Lavallee, Bruno Simoneau
Abstract: The present invention relates to a process for preparing 3-amino-9,13b-dihydro-1H-dibenz[c,f]-imidazo[1,5-a]azepine-hydrochloride, as follows:a) hydrogenating 6-phthalimidomethyl-5H-dibenz[b,e]-azepine, to produce 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine;b) reacting the 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine with hydrazine, to produce 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine;c) reacting the 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine with bromooyanogen, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine; andd) precipitating the 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine in the presence of DMF and HCl, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine-hydrochloride.
Abstract: Various substituted benzoxazoles, benzothiazoles, oxazolopyridines and thiazolopyridines are described and disclosed, compounds that are potent inhibitors of leukotriene synthesis in warm-blooded animals.
Type:
Grant
Filed:
September 4, 1992
Date of Patent:
March 22, 1994
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Edward S. Lazer, Julian Adams, Clara K. Miao, Peter Farina
Abstract: The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH) They also have an effect on PGE.sub.2 production.
Type:
Grant
Filed:
May 14, 1990
Date of Patent:
March 15, 1994
Assignee:
Dr. Karl Thomas GmbH
Inventors:
Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
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:
March 11, 1992
Date of Patent:
January 4, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
Abstract: Disclosed herein are cyclic peptide derivatives of the formula ##STR1## wherein A is absent or the tripeptide radical Thr.rarw.Gly.rarw.Ala, R.sup.1 is benzyl or benzyl monosubstituted at position 4 of the aromatic ring with halo, hydroxy, lower alkyl or lower alkoxy, R.sup.2 and R.sup.4 each independently is hydrogen or lower alkyl, R.sup.3 is lower alkyl or lower alkyl monosubstituted with a hydroxy, R.sup.5 is lower alkyl, Y is oxo or thioxo and Z is hydroxy or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 each independently is hydrogen or lower alkyl. The derivatives are useful for treating herpes infections.
Type:
Grant
Filed:
March 16, 1992
Date of Patent:
November 2, 1993
Assignee:
Bio-Mega/Boehringer Ingelheim Research Inc.
Inventors:
Julian Adams, John DiMaio, Raymond Plante
Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
Type:
Grant
Filed:
May 30, 1991
Date of Patent:
October 12, 1993
Assignee:
B.I. Italia
Inventors:
Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
Abstract: The present invention relates to 14-hydroxy-N-(2-methoxyethyl)-7,8-dihydromorphine and -norisomorphine, processes for preparing them and their use as pharmaceutical compositions.
Type:
Grant
Filed:
September 25, 1992
Date of Patent:
August 31, 1993
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Herbert Merz, Ingrid Wiedemann, Helmut Ensinger, Klaus Stockhaus, Matthias Grauert
Abstract: Tetrahydroisoquinoline amides having the general structure ##STR1## are disclosed, the substituents defined hereinbelow, which amides are useful in inhibiting human leukocyte and neutrophil elastaes.
Type:
Grant
Filed:
November 14, 1991
Date of Patent:
August 3, 1993
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: A new polycyclic peptide antibiotic termed gallidermin is disclosed and described, together with a process for producing such antibiotic by fermination of a new microorganism, Staphylococcus gallinarum (DSM 4616).
Type:
Grant
Filed:
May 18, 1989
Date of Patent:
July 27, 1993
Inventors:
Gunther Jung, Roland Kellner, Hans Zahner, Friedrich Gotz, Thomas Horner, Rolf G. Werner, Hermann Allgaier
Abstract: The invention relates to new nucleating agents for the preparation of directly gassed thermoplastic foams. The new agents comprise a combination of citric acid, the salts or esters thereof and carbonate or bicarbonate and talc.