Patents Assigned to Dr. Karl Thomae GmbH
  • Patent number: 4707309
    Abstract: The invention is directed to a process for dotting molding tools with droplets of liquid or suspended lubricant in the production of shaped articles in the pharmaceutical, food, or catalyst fields. Pressurized lubricant solutions or suspensions and pressurized gas are alternately passed through capillaries, in conjunction with alternating single-substance nozzles, in such a way that drops are formed on the nozzle surface, in between the jets of gas, and are then detached form this surface and directed to specific zones of pressing tools. The apparatus comprises fast-acting valves for the brief release of pressurized gases and lubricant liquids or suspensions. The delivery lines of a gas valve and a liquid valve combine upstream of a capillary, and single-substance nozzles are mounted at the end of the capillaries.
    Type: Grant
    Filed: March 27, 1984
    Date of Patent: November 17, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gunther M. Voss, Volker I. Glasel, Peter Gruber, Walter Bubeck
  • Patent number: 4699909
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methypyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; andR.sub.
    Type: Grant
    Filed: July 24, 1986
    Date of Patent: October 13, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen, Walter Haarman
  • Patent number: 4696931
    Abstract: There are disclosed novel imidazole derivatives of the formula. ##STR1## and derivatives of the formula ##STR2## the tautomers thereof, and non-toxic, pharmacologically acceptable addition salts thereof with inorganic or organic acids. The compounds described herein are useful in treating cardiac insufficiency.
    Type: Grant
    Filed: April 30, 1985
    Date of Patent: September 29, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen
  • Patent number: 4678792
    Abstract: This invention relates to a compound of formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; and R.sub.3 is a C.sub.7 -C.sub.9 aralkyl, the phenyl nucleus of which can be mono-, di-, or trisubstituted by halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, and nontoxic, pharmaceutically acceptable salts thereof. The compounds have useful antithrombic properties.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: July 7, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Josef Nickl, Erich Muller, Benthold Narr, Helmut Ballhause, Walter Haarmann
  • Patent number: 4670438
    Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are --N.dbd., HN.dbd., R.sub.3 N.dbd., O.dbd.C.dbd., HC.tbd., HO--C.tbd. or R.sub.3 SO.sub.2 --O--C.tbd.; andR.sub.1 and R.sub.2 are substituents of various types.The compounds are useful as hypotensives and cardiotonics.
    Type: Grant
    Filed: June 22, 1984
    Date of Patent: June 2, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Volkhard Austel, Joachim Heider, Norbert Hauel, Manfred Reiffen, Jacobus C. A. van Meel, Willi Diederen
  • Patent number: 4668674
    Abstract: There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a pharmaceutical material.The compound is characterized by a powerful activity against ulcers of the gastro-intestinal tract.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: May 26, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: G/u/ nter Trummlitz, Wolfhard Engel, Wolfgang Eberlein, Gerhard Mihm, Antonio Giachetti
  • Patent number: 4659584
    Abstract: The specification describes a process and apparatus for charging eye rods with solutions or suspensions of active substance. The latter are applied dropwise, by means of a micrometering device, to specific points on the eye rods which are set in rotation, and simultaneously or subsequently the solvent or suspension agent is removed.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 21, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventor: Leonhard Schilk
  • Patent number: 4656171
    Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
    Type: Grant
    Filed: November 27, 1984
    Date of Patent: April 7, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Volkhard Austel, Norbert Hauel, Joachim Heider, Manfred Reiffen, Jacobus C. A. Van Meel, Willi Diederen
  • Patent number: 4650664
    Abstract: This invention relates to vehicles for the administration of mopidamol. More specifically, this invention relates to a method of treating cardiovascular disorders, malignancy, or thrombosis in a host in need of such treatment which comprises administering to said host a cardiovascularly, antimetastic, or antithrombotic effective amount of a composition comprised of (i) mopidamol 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 1 acid equivalent to 1 mol of mopidamol or its acid addition salt.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: March 17, 1987
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gottfried Schepky, Rolf Brickl, Peter Gruber, Jochen Schmid, Ursula Springmeier
  • Patent number: 4629733
    Abstract: The present invention relates to novel indolinones of the general formula ##STR1## wherein R represents an aryl group having from 6 to 10 carbon atoms, unsubstituted or mono- or disubstituted by alkyl groups having from 1 to 5 carbon atoms, hydroxyl groups, alkoxy groups having from 1 to 3 carbon atoms, or halogen atoms, whereby the substituents may be the same or different and whereby the phenyl nucleus of the aryl group may also be substituted by an amino group, a hydroxyl group, or an alkanoylamino group with altogether from 1 to 3 carbon atoms; an aryl group having from 6 to 10 carbon atoms, substituted by 3 or 4 alkyl groups having from 1 to 5 carbon atoms each; a phenyl group substituted by a phenyl, halogenphenyl, or cycloalkyl group with 5 to 7 carbon atoms; an aralkyl group having from 7 to 11 carbon atoms; or a pentamethylphenyl, pyridyl, or quinolyl group; m represents the number 0, 1, or 2; and n represents the number 2, 3, 4, 5, or 6.
    Type: Grant
    Filed: July 27, 1984
    Date of Patent: December 16, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Erich Muller, Josef Nickl, Josef Roch, Berthold Narr
  • Patent number: 4616011
    Abstract: This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##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, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.
    Type: Grant
    Filed: November 26, 1984
    Date of Patent: October 7, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Joachim Heider, Volkhard Austel, Norbert Hauel, Walter Kobinger, Christian Lillie
  • Patent number: 4604389
    Abstract: This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: May 8, 1985
    Date of Patent: August 5, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Klaus Noll, Joachim Heider, Volkhard Austel, Norbert Hauel, Walter Kobinger, Christian Lillie
  • Patent number: 4596705
    Abstract: This invention relates to vehicles for the administration of mopidamol. More specifically, this invention relates to a method of treating cardiovascular disorders, malignancy, or thrombosis in a host in need of such treatment which comprises administering to said host a cardiovascularly, antimetastic, or antithrombotic effective amount of a composition comprised of (i) mopidamol 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 1 acid equivalent to 1 mol of mopidamol.
    Type: Grant
    Filed: October 7, 1983
    Date of Patent: June 24, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gottfried Schepky, Rolf Brickl, Peter Gruber, Jochen Schmid, Ursula Springmeier
  • Patent number: 4584293
    Abstract: This invention related to new aminotetralin derivatives of formula I ##STR1## wherein ##STR2## B is methylene or, when A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO-- or --CH.sub.2 --CO--, B can also be carbonyl or thiocarbonyl;E is a C.sub.2 -C.sub.4 straight-chain alkylene, optionally substituted by a C.sub.1 -C.sub.3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;R.sub.1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylthio, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkoxy phenyl C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkyl or, together with R.sub.1, can be a C.sub.1 -C.sub.2 alkylenedioxy;R.sub.3 and R.sub.4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, hydroxy, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 8, 1985
    Date of Patent: April 22, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Joachim Heider, Volkhard Austel, Norbert Hauel, Walter Kobinger, Christian Lillie
  • Patent number: 4582837
    Abstract: There are disclosed novel imidazole derivatives of the formula ##STR1## and derivatives of the formula ##STR2## the tautomers thereof, and non-toxic, pharmacologically acceptable addition salts thereof with inorganic or organic acids. The compounds described herein are useful in treating cardiac insufficiency.
    Type: Grant
    Filed: June 21, 1983
    Date of Patent: April 15, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen
  • Patent number: 4581177
    Abstract: A new process is disclosed for preparing 3-cyano-4-aminoacetophenone which, starting from 3-cyano-4-acetamidoacetophenone, enables this compound to be produced on an industrial scale in high yields.3-Cyano-4-aminoacetophenone is an intermediate product for the preparation of 2-amino-5-[1-hydroxy-2-(alkyl- or dialkyl-amino)ethyl]benzonitriles which show .beta..sub.2 -mimetic activities and may be used as feed additives.
    Type: Grant
    Filed: April 17, 1985
    Date of Patent: April 8, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Resemann, Ferdinand Fraunberger
  • Patent number: 4575504
    Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## and R is hydrogen, alkyl of 1 to 5 carbon atoms, alkanoyl of 1 to 5 carbon atoms, alkenyl of 3 to 5 carbon atoms, (alkoxy of 1 to 4 carbon atoms)carbonyl, or aralkyl of 7 to 11 carbon atoms optionally halo-substituted,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: March 11, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Robert Sauter, Gerhart Griss, deceased, Wolfgang Grell, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler
  • Patent number: 4568680
    Abstract: Compounds of the formula ##STR1## wherein one of A and B is methenyl (--CH.dbd.) and the other is carbonyl; R.sub.1 is (alkyl of 1 to 3 carbon atoms)mercapto, (alkyl of 1 to 3 carbon atoms)sulfinyl or (alkyl of 1 to 3 carbon atoms)sulfonyl; andR.sub.2 is alkoxy of 1 to 3 carbon atoms;tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
    Type: Grant
    Filed: December 5, 1984
    Date of Patent: February 4, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Volkhard Austel, Norbert Hauel, Joachim Heider, Manfred Reiffen, Jacobus C. A. Van Meel, Willi Diederen
  • Patent number: 4567178
    Abstract: The invention relates to novel substituted 5,11-dihydro-6H-dibenz[b,e]azepin-6-one of the formula ##STR1## wherein A represents a (1-methyl-4-piperidinyl)-acetyl, (4-methyl-1-piperazinyl)-acetyl, or [(1-methyl-4-piperidinyl)-amino]-carbonyl group,and the acid addition salts thereof, which have valuable pharmacological properties, particularly an ulcer-inhibiting and secretion-inhibiting activity. The compounds of Formula I may be prepared using methods conventionally used for analogous compounds.
    Type: Grant
    Filed: January 7, 1985
    Date of Patent: January 28, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gunter Trummlitz, Wolfhard Engel, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti
  • Patent number: 4550107
    Abstract: Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 14, 1985
    Date of Patent: October 29, 1985
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfhard Engel, Gunter Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti