Abstract: This invention is directed to novel benzoxazin-2-ones of the formula ##STR1## wherein A is a sulfur atom or an SO, SO.sub.2, R--N.dbd.S, or R--N.dbd.SO.sub.2 group where R is a hydrogen atom or an acyl group;D is an alkylene group;R.sub.1 is an alkyl, phenylalkyl, cycloalkyl, or phenyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a hydrogen or halogen atom or a nitro or alkyl group; andR.sub.6 is a hydrogen or halogen atom or an alkyl group,having valuable pharmacological properties, particularly an antithrombotic activity. The compounds of Formula I may be prepared by the methods used for analogous compounds.
Type:
Grant
Filed:
June 6, 1984
Date of Patent:
May 21, 1985
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Berthold Narr, Josef Nickl, Erich Muller, Josef Roch, Walter Haarmann, Johannes-Maximilian Weisenberger
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.
Type:
Grant
Filed:
January 31, 1984
Date of Patent:
May 21, 1985
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
Abstract: Compounds of the formula ##STR1## wherein A is phenyl, p=hydroxy-phenyl, 2-thienyl or 3-thienyl; andR represents substituents of various types;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antibiotics.
Type:
Grant
Filed:
August 20, 1982
Date of Patent:
June 12, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Bernd Wetzel, Wolfgang Eberlein, Gunter Trummlitz, Eberhard Woitun, Roland Maier, Wolfang Reuter, Uwe Lechner, Hanns Goeth
Abstract: The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydr o-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3, 2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds.The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.
Type:
Grant
Filed:
January 31, 1983
Date of Patent:
May 8, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gunter Trummlitz, Wolfhard Engel, Wolfgang Eberlein, Gunther Schmidt, Rudolf Hammer, Piero del Soldato
Abstract: This invention relates to compounds of the formula ##STR1## wherein X is oxygen, --NH--, or--NCH.sub.3 --andR is 1-methyl-4-piperidinyl, 4-methyl-1-piperazinyl, endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl, or exo-8-methyl-8-acabicyclo[3.2.1]oct-3-yl, each of which may optionally have an additional methyl substitutent,a diastereomer or enantiomer thereof, or a non-toxic, pharmacologically acceptable acid addition salt thereof with an inorganic or organic acid.
Type:
Grant
Filed:
January 31, 1983
Date of Patent:
April 17, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfhard Engel, Gunter Trummlitz, Gunther Schmidt, Wolfgang Eberlein, Rudolf Hammer, Piero del Soldato
Abstract: This invention relates to vehicles for the administration of bromhexine. More specifically, this invention relates to a composition for the delayed release of bromhexine which comprises (i) spheroid particles or tablets comprised of (a) bromhexine and/or acid addition salts thereof and (b) at least one pharmacologically acceptable acid or acidic substance, the total amount of acid substance from acid addition salts present and the acid or acidic substance being in a ratio of at least 2 mols to 1 mol of bromhexine, and (ii) a coating surrounding said spheroid particles or tablets, said coating being comprised of from about 50 to 100 percent by weight of acid-insoluble lacquers soluble in intestinal juices and from about 0 to 50 percent by weight of lacquers insoluble in gastric and intestinal juices and said coating being present in an amount of from about 2 to 30 percent by weight, based upon the weight of the spheroid particles or tablets.
Type:
Grant
Filed:
June 30, 1982
Date of Patent:
March 20, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Peter Gruber, Jochen Schmid, Horst Lechner, Eckhart Bauer
Abstract: A tridecadeoxynucleotide of the formuladCCTTCTGGAACTG,is useful as a primer in the enzymatic synthesis of deoxyribonucleic acid (DNA) on messenger ribonucleic acid (mRNA) matrices.The new tridecadeoxynucleotide is obtained by linking suitable partially protected oligonucleotide blocks, particularly two suitable oligonucleotide fragments, e.g. by linking a suitable tetramer to a suitable nomaer, using a condensing agent.
Type:
Grant
Filed:
February 24, 1982
Date of Patent:
February 21, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Hartmut Seliger, Eva Rastl, Peter Swetly
Abstract: This invention relates to vehicles for the administration of dipyridamole. More specifically, this invention relates to a method of treating cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of a composition comprised of (i) dipyridamole or an acid addition salt thereof and (ii) at least one pharmacologically acceptable acid or acid substance, the total amount of acid from acid addition salt present and acid or acid substance being in a ratio of at least about 5 acid equivalents to 1 mol of dipyridamole, preferably in the form of particles having particle sizes of from about 0.1 to 2.0 mm.
Type:
Grant
Filed:
June 17, 1982
Date of Patent:
January 24, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Rolf Brickl, Peter Gruber, Gottfried Schepky, Gerhard Bozler
Abstract: This invention relates to novel compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl having from 1 to 4 carbon atoms;R.sub.2 is halogen, hydrogen, or alkyl having from 1 to 4 carbon atoms; andR is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl, 1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)-methyl, or (8-methyl-8-azabicyclo?3.2.1!oct-3-yl)-methyl, each of which can optionally have an additional methyl substituent on the heterocyclic ring,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
Type:
Grant
Filed:
January 31, 1983
Date of Patent:
January 3, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gu/ nther Schmidt, Wolfgang Eberlein, Wolfhard Engel, Gu/ nter Trummlitz, Rudolf Hammer, Piero Del Soldato
Abstract: This invention relates to compounds of the formula ##STR1## wherein R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl, 1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl, 2,3-dehydro-8-methyl-8-azabicyclo?3.2.1!oct-3-yl methyl, endo-8-methyl-8-azabicyclo?3.2.1!oct-3-yl-methyl, or exo-8-methyl-8-azabicyclo?3.2.1!oct-3-yl-methyl, each of which may optionally have one or two methyl substituents on the six-membered heterocyclic ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
Type:
Grant
Filed:
January 31, 1983
Date of Patent:
January 3, 1984
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Gu/ nter Trummlitz, Gu/ nther Schmidt, Wolfhard Engel, Rudolf Hammer, Piero Del Soldato
Abstract: This invention relates to an apparatus for dispensing small quantities of fluid which comprises a hinged clamping member with a bellows attachment for receiving an elongated cylindrical tube containing fluid and having sealed ends, wherein the hinged clamping member consists of two half-shells which enclose an inner space; the two half-shells are enclosed by a retaining and supporting member; the retaining and supporting member consists of symmetrical halves which are connected to each other by a hinge; the inner diameter of the inner space corresponds to the outer diameter of the tube; the two halves of the retaining and supporting member have, adjacent to the hinge, recesses with stops and, on the side opposite the hinge, a locking or snap-fit member; the hinged half-shells comprise, at one end, a shaft whose outer diameter corresponds to the inner diameter of the cylindrical shaft of a bellows attachment; the bellows attachment is provided with an opening which permits the bellows attachment to be pushed u
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl, and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as sweetening agents.
Type:
Grant
Filed:
April 15, 1981
Date of Patent:
September 13, 1983
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gunter Trummlitz, Wolfgang Eberlein, Wolfhard Engel, Gunther Schmidt
Abstract: This invention is directed to the compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or an alkyl of from 1 to 6 carbon atoms;R.sub.2 is an alkyl of from 1 to 3 carbon atoms;R.sub.3 is hydrogen or an alkyl of from 1 to 3 carbon atoms; andR.sub.4 is hydrogen or an alkyl of from 1 to 4 carbon atoms.These compounds are useful in pharmaceutical compositions which serve as analgesics, antiphlogistics and antipyretics.
Abstract: Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.
Type:
Grant
Filed:
June 11, 1980
Date of Patent:
December 7, 1982
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Johannes Keck, Gerd Kruger, Helmut Pieper, Klaus Noll, Gunther Engelhardt, Norbert Promberger, Rainer Zimmermann