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.
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
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.
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.
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
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.
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.
Abstract: Use of imidazol-1-yl compounds of the general formula I ##STR1## wherein R.sup.1 denotes lower alkyl or hydrogen;m represents 2 or 3, andn represents 2 or 3;or a physiologically acceptable acid addition salt thereof for treating functional disturbances of the lower intestinal tract in larger mammals and humans associated with increased pain sensitivity and/or anomalies in stool passage in the colon region.
Type:
Grant
Filed:
November 3, 1993
Date of Patent:
August 1, 1995
Assignee:
Kali-Chemie Pharma
Inventors:
Christian Eeckhout, Ulf Preuschoff, Samuel David
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
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.
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
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
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
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
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
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
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.
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
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.
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.