Patents Assigned to Kali-Chemie Pharma GmbH
  • Patent number: 4391819
    Abstract: 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: Grant
    Filed: July 13, 1981
    Date of Patent: July 5, 1983
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Peter W. Thies, Samuel David
  • Patent number: 4382030
    Abstract: 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: Grant
    Filed: January 12, 1982
    Date of Patent: May 3, 1983
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Horst Zeugner, Dietmar Roemer, Hans Liepmann
  • Patent number: 4374846
    Abstract: 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: Grant
    Filed: July 24, 1980
    Date of Patent: February 22, 1983
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Henning Heinemann, Heinrich-Wilhelm Ohlendorf, Klaus-Ulrich Wolf
  • Patent number: 4367178
    Abstract: 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: Grant
    Filed: February 27, 1981
    Date of Patent: January 4, 1983
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Walter Heigel, Rolf Hueschens
  • Patent number: 4338314
    Abstract: 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: Grant
    Filed: August 16, 1979
    Date of Patent: July 6, 1982
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Insa Hell, Klaus-Ullrich Wolf
  • Patent number: 4325957
    Abstract: 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: Grant
    Filed: December 23, 1980
    Date of Patent: April 20, 1982
    Assignee: Kali-Chemie Pharma GmbH.
    Inventors: Horst Zeugner, Dietmar Roemer, Hans Liepmann, Wolfgang Milkowski
  • Patent number: 4320061
    Abstract: 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: Grant
    Filed: March 16, 1981
    Date of Patent: March 16, 1982
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann, Henning Heinemann
  • Patent number: 4313930
    Abstract: 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: Grant
    Filed: October 31, 1979
    Date of Patent: February 2, 1982
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Martin Wischniewski, Lutz Feicho, Werner Althaus
  • Patent number: 4280971
    Abstract: 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: Grant
    Filed: October 31, 1979
    Date of Patent: July 28, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Martin Wischniewski, Lutz Feicho, Gerhard Fischer, Guenter Peschke
  • Patent number: 4279904
    Abstract: 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: Grant
    Filed: July 28, 1980
    Date of Patent: July 21, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann, Henning Heinemann
  • Patent number: 4279905
    Abstract: 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: Grant
    Filed: July 28, 1980
    Date of Patent: July 21, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Klaus-Ullrich Wolf, Wilhelm Kaupmann
  • Patent number: 4271193
    Abstract: 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: Grant
    Filed: June 22, 1979
    Date of Patent: June 2, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Henning Heinemann, Klaus-Ulrich Wolf, Insa Hell, Reinhard Hempel
  • Patent number: 4263313
    Abstract: 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: Grant
    Filed: February 22, 1978
    Date of Patent: April 21, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Theodor Eckert, Fritz H. Kemper, Martin Wischniewski, Reinhard Hempel
  • Patent number: 4256642
    Abstract: 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: Grant
    Filed: June 25, 1979
    Date of Patent: March 17, 1981
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Peter Willibrord Thies, Akiji Asai
  • Patent number: 4242341
    Abstract: 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: Grant
    Filed: September 14, 1979
    Date of Patent: December 30, 1980
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Peter W. Thies, Akiji Asai, Samuell David
  • Patent number: 4237295
    Abstract: 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: Grant
    Filed: June 1, 1979
    Date of Patent: December 2, 1980
    Assignee: Kali-Chemie Pharma GmbH
    Inventor: Bernd Hachmeister
  • Patent number: 4230702
    Abstract: 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: Grant
    Filed: January 9, 1978
    Date of Patent: October 28, 1980
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Theodor Eckert, Fritz H. Kemper
  • Patent number: 4207331
    Abstract: 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: Grant
    Filed: May 11, 1978
    Date of Patent: June 10, 1980
    Assignee: Kali Chemie Pharma GmbH
    Inventors: Peter W. Thies, Akiji Asai, Samuel David
  • Patent number: 4202888
    Abstract: 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: Grant
    Filed: July 7, 1977
    Date of Patent: May 13, 1980
    Assignee: Kali-Chemie Pharma GmbH.
    Inventors: Theodor Eckert, Fritz H. Kemper, Martin Wischniewski, Reinhard Hempel
  • Patent number: 4191770
    Abstract: 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: Grant
    Filed: April 28, 1978
    Date of Patent: March 4, 1980
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Hans Liepmann, Rolf Hueschens, Wolfgang Milkowski, Horst Zeugner, Henning Heinemann, Klaus-Ullrich Wolf, Insa Hell, Reinhard Hempel