Patents Assigned to Kali-Chemie Pharma GmbH
  • Patent number: 5712283
    Abstract: A method of using moxonidine or a physiologically acceptable acid addition salt thereof for the treatment and/or prophylaxis of hyperglycaemia, and pharmaceutical compositions for use therein.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: January 27, 1998
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Elbert Kaan, Dieter Ziegler, Reinhard Brueckner
  • Patent number: 5679699
    Abstract: 3-(Phenylalkylaminoalkyloxy)-heteroaryl compounds having heart rate lowering and/or anti-ischemic effects, methods for their preparation and pharmaceutical compositions containing them are described. The compounds correspond to the general formula I ##STR1## or to the general formula XXXI ##STR2## in which the substituents have the meanings given in the specification.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: October 21, 1997
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Wolfgang Kehrbach, Michael Mlinaric, Dieter Ziegler, Reinhard Brueckner, Willi Bielenberg
  • Patent number: 5635511
    Abstract: The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhytmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro, or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: June 3, 1997
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Arman Farjam, Reinhard Brueckner, Dieter Ziegler
  • Patent number: 5576327
    Abstract: The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhythmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4 ' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: November 19, 1996
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Arman Farjam, Reinhard Brueckner, Dieter Ziegler
  • Patent number: 5547967
    Abstract: 3-(Phenylalkylaminoalkylozy)-heteroaryl compounds having heart rate lowering and/or anti-ischemic effects, methods for their preparation and pharmaceutical compositions containing them are described. The compounds correspond to the general formula I ##STR1## or to the general formula XXXI ##STR2## in which the substituents have the meanings given the specification.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 20, 1996
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Wolfgang Kehrbach, Michael Mlinaric, Dieter Ziegler, Reinhard Brueckner, Willi Bielenberg
  • Patent number: 5532251
    Abstract: The use of 3-benzoyl-3,7-diazabicyclo[3.3.1]nonane compounds of the general formula I ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 and R.sup.3 are each individually lower alkyl or together form an alkylene chain having 3-6 carbon atoms,R.sup.4 is hydrogen, halogen, cyano, nitro, trifluoromethyl or a R.sup.6 --SO.sub.2 -- group, in which R.sup.6 is fluorine or lower alkyl, andR.sup.5 is hydrogen, halogen, trifluoromethyl or nitro, or their physiologically acceptable acid addition salts for the treatment of cardiac arrhythmias in larger mammals, including humans.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: July 2, 1996
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Reinhard Brueckner, Joerg Meil, Dirk Thormaehlen
  • Patent number: 5474988
    Abstract: Pharmacologically active compounds of formula I ##STR1## which can be substituted in the phenyl rings and in which R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 denotes hydrogen or lower alkyl,Y denotes oxygen or sulfurn represents an integer from 1 to 3Z represents a bond, a CO group or a CH.dbd. group,Q denotes nitrogen or the CH group andR.sup.7, if Q denotes nitrogen, represents an optionally substituted pyridyl or phenyl radical or, if Q denotes the CH group, represents the N-methyl-N-(4-oxo-3H-pyrimidin-2-yl)amino group,and their acid addition salts and processes and intermediates for their preparation.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: December 12, 1995
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Patrice Demonchaux, Patrick Lenoir
  • Patent number: 5418224
    Abstract: Ring-contracted N-demethyl-N-isopropylerythromycin A derivatives with gastrointestinally effective motilin-agonistic properties, a method for preparing such compounds, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: May 23, 1995
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Dagmar Hoeltje, Ulf Preuschoff, Christian Eeckhout
  • Patent number: 5378462
    Abstract: Pancreatin-containing micropellet cores which can be coated with a gastric juice-resistant film are prepared by extruding a mixture containing pancreatin, polyethylene glycol 4000 and a lower alcohol such as propan-2-ol to produce extrudates which break by themselves into fragments, rounding the fragments with the addition of highly liquid paraffin and drying. Propan-2-ol may be present with the paraffin during rounding. The micropellet cores contain 65-85% pancreatin, and have a bulk density of 0.6 g/ml to 0.85 g/ml, a spherical to ellipsoidal shape with a minor axis in the range of 0.7-1.4 mm and a particle size distribution in which at least 80% of the micropellet cores have a minor axis to major axis ratio in the range from 1:1 to 1:2.
    Type: Grant
    Filed: August 19, 1993
    Date of Patent: January 3, 1995
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Bernd Boedecker, Friederike Henninges, Klaus-Juergen Koelln, Guenther Kuhnow, Guenter-Josef Peschke, Manfred Rehburg, Alwin Sobe, Berthold Stemmle
  • Patent number: 5332733
    Abstract: Pharmacologically active compounds corresponding to the general formula I ##STR1## which are optionally substituted in the benzene ring and in which X denotes oxygen or sulfur,Y denotes oxygen or sulfur,R.sup.1 denotes hydrogen or lower alkyl,n is an integer from 0 to 4, andR.sup.4 is an optionally substituted 6-membered unsaturated heterocycle containing 1 or 2 nitrogen atoms not directly bonded to the piperazine ring,and physiologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: November 17, 1992
    Date of Patent: July 26, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Daniel Jasserand, Francois Floc'h, Richard White
  • Patent number: 5324725
    Abstract: Pharmacologically active compounds having anti-allergic properties corresponding to the formula I ##STR1## which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.
    Type: Grant
    Filed: August 21, 1992
    Date of Patent: June 28, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Daniel Jasserand, Dominique Paris, Patrice Demonchaux, Michel Cottin, Francois Floc'H, Pierre Dupassieux, Richard White
  • Patent number: 5324732
    Abstract: 1.5 Fumaric acid salts of N,N'-di-lower alkyl-substituted 9,9-alkylene-3,7-diazabicyclo[3.3.1 ]nonanes and a process for obtaining them in stoichiometrically pure and virtually non-hygroscopic form.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: June 28, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Walter Heitmann, Uwe Maetzel
  • Patent number: 5294638
    Abstract: Pharmacologically active compounds corresponding to the general formula I: ##STR1## wherein m represents 1-4,n represents 2-5,R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy or halogen, orR.sup.2 and R.sup.3 are linked to adjacent carbon atoms and together form an alkylenedioxy group with 1-2 carbon atoms,R.sup.4 represents a saturated monocyclic or bicyclic hydrocarbon radical derived from terpenes and having 10 or 11 hydrocarbon atoms, andZ represents oxygen, an N--R.sup.5 group, wherein R.sup.5 is lower alkyl, or if R.sup.4 is a dihydronopyl radical, Z may also be sulfur,and their acid addition salts.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: March 15, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Insa Hell, Ulf Preuschoff, Hermann Kraehling, Samuel David, Ivan Ban, Marie-Odile Christen
  • Patent number: 5283243
    Abstract: Pharmacologically active compounds corresponding to the formula I ##STR1## which are optionally substituted in the benzene ring and in which X denotes oxygen or sulfur,Y denotes oxygen or sulfur,R.sup.1 denotes hydrogen or lower alkyl,n is an integer from 0 to 4,R.sup.4 denotes hydrogen, andR.sup.5 denotes hydrogen, hydroxy or cyano, orR.sup.4 and R.sup.5 together form a bond,R.sup.6 denotes an A--R.sup.7 group in which R.sup.7 denotes an optionally substituted phenyl group, and A denotes a --CH.sub.2 -- group, a CO group or a bond, orR.sup.6 is a halogen-substituted 1-phenylmethyl-1H-benzimidazol-2-ylamino group,and physiologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: February 1, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Daniel Jasserand, Francois Floc', Richard White
  • Patent number: 5272143
    Abstract: Pharmacologically active compounds corresponding to the general formula I ##STR1## in which R.sup.1 represents hydrogen, a lower alkyl or cycloalkyl-alkyl group or an optionally substituted phenyl-lower alkyl group,R.sup.2 denotes hydrogen or a lower alkyl group optionally substituted in the .alpha.-position to the nitrogen atom by lower alkoxy,R.sup.3 denotes hydrogen, lower alkyl, lower alkoxy, halogen or hydroxyl,n represents 1 or, if the --(CH.sub.2).sub.n -- chain is in the 4-position of the ring structure, also represents 2,R.sup.4 denotes hydrogen, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl or an optionally substituted phenyl-lower alkyl group, andR.sup.5 denotes hydrogen, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl or an optionally substituted phenyl-lower alkyl group, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a heterocycle andD represents a bond, or, if R.sup.4 and R.sup.5 do not denote hydrogen, also represents the --N.dbd.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: December 21, 1993
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Werner Benson, Karin van Charldorp, Peter C. Gregory, Klaus-Ullrich Wolf, Ulf Preuschoff, Martin Tulp, Ton Hulkenberg, Ineke van Wijngaarden
  • Patent number: 5232686
    Abstract: A method of inhibiting peripheral blood circulation disorders or damage such as hemorrhagic lesions induced by gastrotoxic doses of substances such as alcohol or non-steroid, antiinflammatory medicaments in the gastrointestinal tract of a mammal comprising administering to said mammal an effective peripheral circulation disorder or gastrointestinal damage inhibiting amount of a quaternary N-benzyl-N-{2-[2-((1S,5S)-6,6-dimethylbicyclo[3,1,1]hept-2-yl)-ethoxy]-eth yl}-morpholinium salt, and pharmaceutical compositions comprising a substance having a tendency to induce a peripheral blood circulation disorder or damage such as a hemorrhagic lesion in the stomach and/or intestinal wall of a mammal and an effective peripheral circulation disorder or gastrointestinal damage inhibiting amount of a quaternary N-benzyl-N-{2-[2-((1S,5S)-6,6-dimethylbicyclo[3,1,1]hept-2-yl)-ethoxy]-eth yl}-morpholinium salt.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: August 3, 1993
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Marie-Odile Christen, Brigitte Noel, Ilse Philippi
  • Patent number: 5212173
    Abstract: Pharmacologically active compounds corresponding to the formula I ##STR1## in which n represents 2-5,m represents 2-6,R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 represents an OR.sup.4 group in which R.sup.4 denotes lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.2 represents a ##STR2## group in which R.sup.5 and R.sup.6 independently of one another each denote hydrogen, lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a saturated 5- or 6-membered heterocycle,R.sup.3 represents a saturated monocyclic or bicyclic hydrocarbon group which is derived from terpenes and has 10 or 11 carbon atoms, andZ represents oxygen or, if R.sup.3 is a dihydronopyl group, Z may also represent sulfur,and salts thereof.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: May 18, 1993
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Herman Kraehling, Samuel David, Insa Hell, Ulf Preuschoff, Ivan Ban, Marie-Odile Christen
  • Patent number: 5175347
    Abstract: A process for preparing cis-dihydronopol and esters thereof in which corresponding esters of (-)nopol are stereoselectively hydrogenated by heterogeneous hydrogenation in the presence of a platinum, platinum oxide or ruthenium/carbon catalyst, and the resulting cis-dihydronopyl esters optionally may be converted into corresponding alcohols by hydrolysis.
    Type: Grant
    Filed: December 2, 1991
    Date of Patent: December 29, 1992
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Walter Heitmann, Uwe Maetzel
  • Patent number: 5164401
    Abstract: A method of treating a mammal in need of diruetic treatment by administering an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound, diuretic pharmaceutical compositions containing an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound; and previously unknown diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compounds containing an optionally substituted phenylalkyl group in the 3-position.
    Type: Grant
    Filed: June 17, 1991
    Date of Patent: November 17, 1992
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Kurt Burow, Gerd Buschmann, Arman Farjam, Ulrich Kuehl, Gerda Varchmin, Deiter Ziegler, Uwe Schoen
  • Patent number: 5096920
    Abstract: The use of 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are optionally substituted in the phenyl ring as active substances in hepato-protective medicaments and new 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are substituted in the phenyl ring are described.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: March 17, 1992
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Dominique Biard, Marie-Odile Christen, Patrick Dansette, Daniel Jasserand, Daniel Mansuy, Amor Sassi