Patents Assigned to Kali-Chemie Pharma GmbH
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Patent number: 4391819Abstract: Novel and highly effective sleep inducing 3.beta.-hydroxy methyl-4.alpha.-hydroxy-8.beta.-alkoxy-2,9-dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds of the following Formula: ##STR1## in which R.sub.1 indicates an alkoxy group and preferably a lower alkoxy group, such as the methoxy group, the ethoxy group, or the n-butoxy group, whileR.sub.2 indicates the 10-methylene group or the 10.beta.-methyl group, are produced from didrovaltratum, i.e., 1-isovaleroxy-4-isovaleroxy methyl-7-acetoxy-spiro-oxirano-1,9-dihydrocyclopenta(c)pyrane or from extracts of plants of the genus Valerianaceae which contain about 70% of didrovaltratum. The novel compounds have a surprisingly low toxicity.Type: GrantFiled: July 13, 1981Date of Patent: July 5, 1983Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Samuel David
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Patent number: 4382030Abstract: Novel 2-acylaminomethyl-1H-2,3-dihydro-1,4-benzodiazepine derivatives are disclosed which possess the Formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, lower alkenyl or cyclopropylmethyl;R.sub.2 represents hydrogen, lower alkyl or lower alkenyl;R.sub.3 represents a group of the formula a, b, c or d; ##STR2## wherein R is hydrogen or C.sub.1 -C.sub.3 -alkyl;R.sub.4 is hydrogen, lower alkyl, lower alkoxy, nitro or halogen, andR.sub.4 ' is hydrogen or C.sub.1 -C.sub.4 -alkyl and the aromatic groups A and B may be unsubstituted or substituted by 1 to 3 substituents such as halogen, lower alkylthio, lower alkoxy, lower alkyl, hydroxy, nitro, trifluoromethyl or methylenedioxy or ethylenedioxy and optical isomers and acid addition salts of the compounds. In addition to psycho pharmacological, diuretic and antiarrhythmic properties, the novel compounds of Formula I possess primarily outstanding analgesic activities and are low in toxicity.Type: GrantFiled: January 12, 1982Date of Patent: May 3, 1983Assignee: Kali-Chemie Pharma GmbHInventors: Horst Zeugner, Dietmar Roemer, Hans Liepmann
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Patent number: 4374846Abstract: Novel N-amino alkyl indole compounds are disclosed. These compounds correspond to the Formula I ##STR1## In said Formula R.sub.1 indicates the hydrogen atom, an alkyl group with 1 to 4 carbon atoms, which may be substituted by a phenyl group, or the acetyl group;R.sub.2 indicates the hydroxy carbonyl group, an alkoxy carbonyl group with 1 to 4 alkyl carbon atoms, the cyano group, the amino carbonyl group, a mono-alkyl amino carbonyl group with 1 to 4 alkyl carbon atoms, or a di-alkyl amino carbonyl group with 1 to 4 alkyl carbon atoms, with the proviso that, when R.sub.2 is the hydroxy carbonyl group, then R.sub.1 is other than the hydrogen atom;A indicates an alkylene group with 2 to 5 carbon atoms;R.sub.3 and R.sub.4 are the same or different substituents and indicate the hydrogen atom, an alkyl group with 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 are an alkylene group forming, together with the nitrogen atom to which they are attached, a heterocyclic ring with 5 to 7 ring members; andR.sub.5 and R.sub.Type: GrantFiled: July 24, 1980Date of Patent: February 22, 1983Assignee: Kali-Chemie Pharma GmbHInventors: Henning Heinemann, Heinrich-Wilhelm Ohlendorf, Klaus-Ulrich Wolf
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Patent number: 4367178Abstract: Disclosed is a process for the production from raw lecithin of pure lecithin directly usable for physiological purposes, comprising the steps of contacting raw lecithin with gas as the extraction medium under supercritical conditions with respect to pressure and temperature in an extraction stage to produce a gas containing an extract; passing the gas containing the extract from the extraction stage into a separation stage; varying at least one of the pressure and the temperature of the gas in the separation stage to separate the extract-containing gas into the gas and the extract; recycling the gas after the step of varying the pressure and/or temperature; and removing pure lecithin from the extraction stage.Type: GrantFiled: February 27, 1981Date of Patent: January 4, 1983Assignee: Kali-Chemie Pharma GmbHInventors: Walter Heigel, Rolf Hueschens
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Patent number: 4338314Abstract: Compounds of [1,2]anellated-7-phenyl-1,4-benzodiazepines having the formula I ##STR1## wherein X is oxygen, sulfur or NR;R is H,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl, substituted with a terminal phenyl group, which is unsubstituted or substituted by one or 2 methoxy groups, a 3,4-methylene dioxy or 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl, substituted with terminal halogen, hydroxy or methoxy or,C.sub.3 -C.sub.5 alkenylR.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are H, halogen, trifluoromethyl, nitro, alkyl, alkoxy, or alkylthio wherein alkyl is C.sub.1 -C.sub.4 alkyl or two neighboring groups represent a methylenedioxy or ethylenedioxy group and the acid addition salts thereof, ulcer treating pharmaceutical compositions containing these compounds and a method of medical treatment using same.Type: GrantFiled: August 16, 1979Date of Patent: July 6, 1982Assignee: Kali-Chemie Pharma GmbHInventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Insa Hell, Klaus-Ullrich Wolf
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Patent number: 4325957Abstract: Novel 2-acylaminomethyl-1H-2,3-dihydro-1,4-benzodiazepine derivatives are disclosed which possess the Formula I ##STR1## wherein R.sub.1 represents hydrogen, lower akyl, lower alkenyl or cyclopropylmethyl;R.sub.2 represents hydrogen, lower alkyl or lower alkenyl;R.sub.3 represents a group of the formula a, b, c or d; ##STR2## wherein R is hydrogen or C.sub.1 -C.sub.3 - alkyl;R.sub.4 is hydrogen, lower alkyl, lower alkoxy, nitro or halogen, andR.sub.4 ' is hydrogen or C.sub.1 -C.sub.4 - alkyl and the aromatic groups A and B may be unsubstituted or substituted by 1 to 3 substituents such as halogen, lower alkylthio, lower alkoxy, lower alkyl, hydroxy, nitro, trifluoromethyl or methylenedioxy or ethylenedioxy and optical isomers and acid addition salts of the compounds. In addition to psycho pharmacological, diuretic and antiarrhythmic properties, the novel compounds of Formula I possess primarily outstanding analgesic activities and are low in toxicity.Type: GrantFiled: December 23, 1980Date of Patent: April 20, 1982Assignee: Kali-Chemie Pharma GmbH.Inventors: Horst Zeugner, Dietmar Roemer, Hans Liepmann, Wolfgang Milkowski
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Patent number: 4320061Abstract: Novel, 3-amino-1-benzoxepin-5(2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another are hydrogen,C.sub.1 -C.sub.3 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4 -ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 or 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.Type: GrantFiled: March 16, 1981Date of Patent: March 16, 1982Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann, Henning Heinemann
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Patent number: 4313930Abstract: Stable valepotriate compositions are produced by a process wherein impurities are removed from the pharmaceutically active extract of the valerianacea fruits, followed by a mixing with pharmaceutically acceptable sheathing materials and the formation of microspheres therefrom.Type: GrantFiled: October 31, 1979Date of Patent: February 2, 1982Assignee: Kali-Chemie Pharma GmbHInventors: Martin Wischniewski, Lutz Feicho, Werner Althaus
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Patent number: 4280971Abstract: Pancreatin pellets are produced by a process employing extrusion techniques. In the process, a mixture of pancreatin powder and selected solvent is formed into a pliable mass suitable for extrusion. The extrusion is conducted followed by a cutting, shaping or forming of the extruded mass into pre-pellet like forms. Further drying and mechanical working of the pre-pellet forms results in the final pancreatin pellet of improved pharmaceutical and mechanical stability. A special aspect of the process is the selection of a solvent for mixing with pancreatin powder that is harmless to enzymes. Such solvents typically include isopropanol and acetone.Type: GrantFiled: October 31, 1979Date of Patent: July 28, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Martin Wischniewski, Lutz Feicho, Gerhard Fischer, Guenter Peschke
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Patent number: 4279904Abstract: Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.7 R.sub.8 ;R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.7 and R.sub.8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR.sub.9 ;R.sub.Type: GrantFiled: July 28, 1980Date of Patent: July 21, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann, Henning Heinemann
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Patent number: 4279905Abstract: Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 to 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.Type: GrantFiled: July 28, 1980Date of Patent: July 21, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann
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Patent number: 4271193Abstract: N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which exhibit a stabilizing effect on the gastric mucosa and enhance the stability and resistance of the gastic mucosa against harmful effects caused by, e.g., excessive alcohol consumption or drugs. The compounds are useful in the prophylaxis and treatment of gastritis.Further disclosed are pharmaceutical compositions which are effective in stabilizing the gastric mucosa and in the treatment and proplylaxis of gastritis and which comprise as a pharmacologically active ingredient N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent. Further disclosed are processes for the preparation of the N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.Type: GrantFiled: June 22, 1979Date of Patent: June 2, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Henning Heinemann, Klaus-Ulrich Wolf, Insa Hell, Reinhard Hempel
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Patent number: 4263313Abstract: A carrier composition for cutaneously absorbable topical pharmaceutical formulations of pharmacologically active agents is disclosed which comprises at least one partial glyceride of a fatty acid of medium chain length. This vehicle enhances the permeation of the topical formulation through the skin. A topical formulation which comprises this permeation enhancing vehicle is suitable for cutaneously applying pharmacologically active agents which are locally and/or systematically effective in the body.Type: GrantFiled: February 22, 1978Date of Patent: April 21, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Theodor Eckert, Fritz H. Kemper, Martin Wischniewski, Reinhard Hempel
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Patent number: 4256642Abstract: Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes and the process for their production and the production of various intermediates are disclosed. Pharmaceutical compositions containing an effective amount of the novel compounds and a pharmaceutically acceptable carrier are also disclosed.Type: GrantFiled: June 25, 1979Date of Patent: March 17, 1981Assignee: Kali-Chemie Pharma GmbHInventors: Peter Willibrord Thies, Akiji Asai
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Patent number: 4242341Abstract: New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino groupone of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygenone of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.Type: GrantFiled: September 14, 1979Date of Patent: December 30, 1980Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Akiji Asai, Samuell David
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Patent number: 4237295Abstract: Disclosed is the preparation of 17-hydroxysparteine by means of the oxidation of sparteine with permanganate in an aqueous acid solution. The oxidation is highly selective and produces the 17-hydroxysparteine in a high yield of more than 90%. The oxidizing agent may be readily separated from the reaction mixture after the reaction in the form of insoluble manganese ammonium phosphate.Type: GrantFiled: June 1, 1979Date of Patent: December 2, 1980Assignee: Kali-Chemie Pharma GmbHInventor: Bernd Hachmeister
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Patent number: 4230702Abstract: A readily enterally absorbable pharmaceutical composition of pharmacologically active agents, which per se are poorly enterally 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 partial glyceride of a fatty acid of long chain length. The preparation is suited for formulating cardiac glycosides, steroids, or anti-capillary fragility agents.Type: GrantFiled: January 9, 1978Date of Patent: October 28, 1980Assignee: Kali-Chemie Pharma GmbHInventors: Theodor Eckert, Fritz H. Kemper
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Patent number: 4207331Abstract: New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group one of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen one of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.Type: GrantFiled: May 11, 1978Date of Patent: June 10, 1980Assignee: Kali Chemie Pharma GmbHInventors: Peter W. Thies, Akiji Asai, Samuel David
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Patent number: 4202888Abstract: A readily enterally absorbable pharmaceutical composition of cardiac glycosides is disclosed which comprises a therapeutically-effective amount of at least one cardiac glycoside distributed in a vehicle comprising an absorption-enhancing amount of at least one partial glyceride of a fatty acid of medium chain length. The preparation is suited for formulating cardiac glycosides which per se are poorly enterally absorbable, in particular, k-strophanthin, g-strophanthin, and proscillaridin.Type: GrantFiled: July 7, 1977Date of Patent: May 13, 1980Assignee: Kali-Chemie Pharma GmbH.Inventors: Theodor Eckert, Fritz H. Kemper, Martin Wischniewski, Reinhard Hempel
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Patent number: 4191770Abstract: N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which possess ulcer-inhibiting activities.Further disclosed are pharmaceutical compositions which are effective in the treatment and prophylaxis of ulcers and which comprise as a pharmacologically active ulcus-inhibiting ingredient N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent.Further disclosed are processes for the preparation of the N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.Type: GrantFiled: April 28, 1978Date of Patent: March 4, 1980Assignee: Kali-Chemie Pharma GmbHInventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Henning Heinemann, Klaus-Ullrich Wolf, Insa Hell, Reinhard Hempel