Patents Assigned to Kali-Chemie Pharma GmbH
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Patent number: 5013852Abstract: Flavone-3-carboxylic acid compounds corresponding to the Formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, lower alkyl, halogen, hydroxy, or etherified or esterified hydroxy, and Z-R.sup.6 stands for a basically substituted alkoxy or amino group, as well as processes and intermediate products for their production. The compounds exhibit inflammation-inhibiting pharmacological activity.Type: GrantFiled: May 18, 1989Date of Patent: May 7, 1991Assignee: Kali-Chemie Pharma GmbHInventors: Rainer Walenta, Reiner Muller-Peddinghaus, Ivan Ban, Michael Wurl, Ulf Preuschoff
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Patent number: 5010076Abstract: Compounds corresponding to the formula I ##STR1## in which R.sup.1 represents hydrogen, lower alkyl or cycloalkylalkyl with 4-7 carbon atoms,R.sup.2 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andR.sup.3 represents hydrogen, halogen, lower alkyl or lower alkoxy, orR.sup.2 and R.sup.3 together denote an alkylenedioxy group,R.sup.4 represents cycloalkyl with 5 to 6 carbon atoms, thiophene or optionally substituted phenyl,R.sup.5 represents hydrogen or halogen,R.sup.6 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andZ represents an alkylene chain with 2-4 carbon atoms, which can optionally be mono- or disubstituted by lower alkyl or onto which a 5-6-membered carbocyclic ring can optionally be fused, or represents an --X--CH.sub.2 --CH.sub.2 -- chain,which have pharmacologically valuable properties, are described, together with a method for their preparation.Type: GrantFiled: March 7, 1990Date of Patent: April 23, 1991Assignee: Kali-Chemie Pharma GmbHInventors: Harald Waldeck, Werner Benson, Horst Zeugner, Klaus-Ullrich Wolf, Peter-Colin Gregory, Derk Hamminga, Ineke van Wijngaarden
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Patent number: 4983611Abstract: 3-sulfonyl-3,7-diazabicyclo[3,3,1]nonane compounds corresponding to the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen or lower alkyl orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents lower alkyl, thienyl, halogen substituted thienyl or a --(CH.sub.2).sub.n --R.sup.5 group, wherein n=0-3 andR.sup.5 is an optionally substituted phenyl group.The compounds are pharmacologically active, particularly in influencing the motility of the stomach.Type: GrantFiled: September 25, 1989Date of Patent: January 8, 1991Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schon, Wolfgang Kehrbach, Klaus-Ullrich Wolf
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Patent number: 4980487Abstract: The use of valepotriate hydrins in the prevention and treatment of disorders of the gastrointestinal tract is described, together with pharmaceutical compositions containing valepotriate hydrins and certain novel valepotriate hydrins per se.Type: GrantFiled: October 18, 1989Date of Patent: December 25, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Samuel David, Insa Hell, Klaus-Ulrich Wolf
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Patent number: 4976965Abstract: Coronary affecting medicinal compositions which in addition to a coronary affecting substance selected from the group consisting of isosorbide nitrates and dihydropyridines contain an alkylene glycol ether as a solvent.Type: GrantFiled: August 31, 1987Date of Patent: December 11, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Juergen Block, Lutz Feicho, Alwin Sobe, Martin Wischniewski
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Patent number: 4965369Abstract: A method of preparing indole carboxylic acid derivatives from aniline derivatives is described which can be carried out in a single reaction vessel without any isolation of intermediate products. The method involes reacting an aniline derivative with a soluble nitrite in an acid medium, reducing the resulting nitrosamine by treating the acidic nitrosamine containing reaction solution with zinc in the presence of sufficient acid, optionally with addition of additional acid and/or a solvent such as a lower alcohol, reacting the resulting hydrazine derivative containing solution with a lower alkyl ester of pyruvic acid to obtain a corresponding hydrazone which cyclizes to yield an indole carboxylic acid ester, and if desired, hydrolyzing the ester to obtain the corresponding carboxylic acid.Type: GrantFiled: March 7, 1990Date of Patent: October 23, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Maetzel, Walter Heitmann
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Patent number: 4924004Abstract: New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkyl or cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is a alkylene chain which is optionally substituted by hydroxyl.Type: GrantFiled: October 28, 1988Date of Patent: May 8, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuehl, Gerd Buschmann, Stephen Magda
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Patent number: 4912113Abstract: 3,7-Diazabicyclo[3,3,1]nonane compounds having valuable heart rate-affecting pharmacological properties corresponding to the Formula I: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is lower alkyl,R.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents a benzhydryl group, optionally substituted by halogen, lower alkoxy, lower alkyl, hydroxy or trifluoromethyl, or a cinnamyl group optionally substituted by halogen, lower alkyl, lower alkoxy, hydroxy, nitro or trifluoromethyl.Type: GrantFiled: September 2, 1988Date of Patent: March 27, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schon, Wolfgang Kehrbach, Gerd Buschmann, Ulrich Kuhl, Dieter Ziegler
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Patent number: 4906640Abstract: 3-sulfonyl-3,7-diazabicyclo[3,3,1]nonane compounds corresponding to the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen or lower alkyl orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents lower alkyl, thienyl, halogen substituted thienyl or a --(CH.sub.2).sub.n --R.sup.5 group, wherein n=0-3 andR.sup.5 is an optionally substituted phenyl group.The compounds are pharmacologically active, particularly in influencing the motility of the stomach.Type: GrantFiled: June 30, 1988Date of Patent: March 6, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Wolfgang Kehrbach, Klaus-Ullrich Wolf
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Patent number: 4886806Abstract: Falvone-3-carboxylic acid compounds corresponding to the Formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, lower alkyl, halogen, hydroxy, or etherified or esterified hydroxy, and Z--R.sup.6 stands for a basically substituted alkoxy or amino group, as well as processes and intermediate products for their production. The compounds exhibit inflammation-inhibiting pharmacological activity.Type: GrantFiled: May 5, 1988Date of Patent: December 12, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Rainer Walenta, Reiner Muller-Peddinghaus, Ivan Ban, Michael Wurl, Ulf Preuschoff
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Patent number: 4879299Abstract: Compounds of Formula (I)S--(CH2)n--Atm (I)in whichS is a 17-spartein nucleus,n is 0 or 1, andA is 2-furyl, 2-thienyl or 2-(N-loweralkyl)pyrrylwhen n=0, or3-furyl or 3-thienyl when n=1, or pyridyl, or a phenyl group of Formula (II) ##STR1## in which at least one of R.sub.1, R.sub.2 and R.sub.3 is a defined substituent other than hydrogen. Such compounds and corresponding compounds in which A is an unsubstituted phenyl group are useful in pharmaceutical compositions as heart affecting agents. Methods of preparing such compounds and pharmaceutical compositions are disclosed. Also described is the use of such compounds or compositions, particularly compounds or compositions with positive inotropic activity, to treat various heart conditions.Type: GrantFiled: December 18, 1987Date of Patent: November 7, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Wolfgang Kehrbach, Bernd Hachmeister, Gerd Buschmann, Ulrich G. Kuehl
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Patent number: 4831167Abstract: A process for producing cis-2,3,4,5-tetrahydro-3-amino-1-benzoxepin-5-ols in which 3-amino-1-benzoxepin-5(2H)-ones are diastereoselectively reduced in a single stage by catalytic hydrogenation in the presence of a platinum oxide catalyst and an equivalent amount of an acid in a polar protic solvent, or by reaction with a borane/amine complex in an aprotic solvent, optionally in the presence of an added lower aliphatic carboxylic acid.Type: GrantFiled: October 20, 1987Date of Patent: May 16, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich W. Ohlendorf, Uwe Maetzel
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Patent number: 4814345Abstract: Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.Type: GrantFiled: November 20, 1987Date of Patent: March 21, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuhl, Gerd Buschmann, Stephen J. Magda
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Patent number: 4803198Abstract: New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl.Type: GrantFiled: July 15, 1986Date of Patent: February 7, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuehl, Gerd Buschmann, Stephen J. Magda
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Patent number: 4771044Abstract: Tetraoxo compounds of the Formula (I) ##STR1## wherein R.sup.1 is an alkyl, alkenyl, phenylalkyl or cycloalkylalkyl group,R.sup.2 and R.sup.3 are each independently an alkyl or phenyl group or together denote an alkylene group,W is a (CH.sub.2).sub.n --Q group, in which n is 2 to 10 and Q is(a) a displaceable leaving group X, or(b) Z-R.sup.4, where Z is a 1-piperazinyl group, and R.sup.4 is in position 4, and is hydrogen or a phenyl, substituted phenyl, N-heteroaryl or substituted N-heteroaryl group;and salts and acid addition salts of said compound, and a method for their preparation. Selected compounds of Formula (I) have been found to have central nervous system affecting activity.Type: GrantFiled: August 19, 1986Date of Patent: September 13, 1988Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Wolfgang Kehrbach, Werner Benson, Andreas Fuchs, Michael Ruhland
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Patent number: 4755520Abstract: Compounds of Formula (I)S--(CH.sub.2).sub.n --A (I)in whichS is a 17-spartein nucleusn is 0 or 1and A is 2-furyl, 2-thienyl or 2-(N-alkyl)pyrryl when n=0, or 3-furyl or 3-thienyl when n=1, or pyridyl or a phenyl group of Formula (II) ##STR1## in which at least one of R.sub.1, R.sub.2 and R.sub.3 is a defined substituent other than hydrogen. Such compounds and corresponding compounds in which A is an unsubstituted phenyl group are useful in pharmaceutical compositions as heart affecting agents. Methods of preparing such compounds and pharmaceutical compositions are also disclosed.Type: GrantFiled: June 17, 1986Date of Patent: July 5, 1988Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schon, Wolfgang Kehrbach, Bernd Hachmeister, Gerd Buschmann, Ulrich G. Kuhl
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Patent number: 4742172Abstract: 3,7-diaza bicyclo-(3,3,1)-nonane compounds of the formula ##STR1## in which substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4, Z.sub.1, and Z.sub.2 indicate the substituents as they are given in the description of the invention, can be employed to produce certain pharmaceutically useful compounds.Type: GrantFiled: May 27, 1987Date of Patent: May 3, 1988Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Bernd Hachmeister, Wolfgang Kehrbach, Ulrich Kuehl, Gerd Buschmann
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Patent number: 4722941Abstract: A readily absorbable pharmaceutical composition of pharmacologically active agents, which per se are poorly absorbable, is disclosed which comprises a pharmacologically effective amount of at least one such pharmacologically active agent distributed in a vehicle comprising an absorption-enhancing amount of at least one fatty acid of medium chain length. The preparation is suited for formulating pharmacologically active bases, cardiac glycosides, steroids, antibiotics, sympathicomimetica, tranquilizing agents, or local anaesthetics.Type: GrantFiled: May 31, 1978Date of Patent: February 2, 1988Assignee: Kali-Chemie Pharma GmbHInventors: Theodor Eckert, Fritz H. Kemper, Martin Wischniewski, Reinhard Hempel
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Patent number: 4714709Abstract: N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.Type: GrantFiled: September 24, 1984Date of Patent: December 22, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Samuel David, Ulrich Kuehl, Gerd Buschmann, Peter Flecker
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Patent number: 4695566Abstract: 3-(aminoalkylaminocarbonylmethoxy)-5-phenylpyrazole compounds corresponding to the formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 and R.sub.9 may be hydrogen or lower alkyl groups, or R.sub.5 with R.sub.6 and/or R.sub.8 with R.sub.9 may also form specified cyclic groups, R.sub.3 and R.sub.4 may be hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro, hydroxy or alkylene dioxy, and Z represents an alkylene chain or the 2-hydroxypropylene chain. The compounds possess pharmacological, in particular antiarrhythmic, properties.Type: GrantFiled: July 2, 1985Date of Patent: September 22, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Henning Heinemann, Wolfgang Kehrbach, Uwe Schoen, Gerd Buschmann, Ulrich Kuhl