Abstract: The invention relates to a method for the production of substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acids, i.e. 7,9-dichlor-3a,4,5,9b-tetrahydro-3H-cyclopental[c]quinoline-4-carboxylic acid.
Abstract: The invention relates to methods for producing substituted acrylic acid esters and to the use of the latter for producing substituted ?-amino acids, such as gabapentin and pregabalin. The substituted acrylic acid esters are produced by Wadsworth-Emmons olefination with trialkyl phosphonoacetate in the presence of alkali carbonate as the base, in an aqueous solvent.
Abstract: The present invention relates to substituted cyclopentene compounds of the general formula I, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use thereof for the production of pharmaceutical preparations.
Type:
Grant
Filed:
November 19, 2004
Date of Patent:
September 19, 2006
Assignee:
Grunenthal GmbH
Inventors:
Oswald Zimmer, Michael Haurand, Klaus Schiene, Clemens Gillen, Johannes Schneider, Gregor Bahrenberg
Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.
Type:
Grant
Filed:
January 5, 2004
Date of Patent:
June 20, 2006
Assignee:
Grunenthal GmbH
Inventors:
Bernd Sundermann, Corinna Sundermann, Helmut Buschmann, Babette-Yvonne Koegel
Abstract: The invention relates to substituted benzo[b]azepin-2-one compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
Type:
Grant
Filed:
April 14, 2004
Date of Patent:
May 9, 2006
Assignee:
Grunenthal GmbH
Inventors:
Michael Sattlegger, Helmut Buschmann, Michael Przewosny, Werner Englberger, Babette-Yvonne Koegel, Hans Schick
Abstract: The invention relates to substituted ?-lactone compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
Type:
Grant
Filed:
January 5, 2004
Date of Patent:
October 18, 2005
Assignee:
Grunenthal GmbH
Inventors:
Corinna Sundermann, Michael Przewosny, Werner Englberger
Abstract: The invention relates to the use of substituted gamma-lactone compounds in the production of medicines for treating migraines, septic shock, neurodegenerative diseases, such as multiple sclerosis, Parkinsons, Alzheimers or Huntingtons disease, inflammations and related pain, cerebral ischaemia, diabetes, meningitis, arteriosclerosis, cancer, mycosis, or for healing wounds.
Type:
Grant
Filed:
January 5, 2004
Date of Patent:
September 13, 2005
Assignee:
Grunenthal GmbH
Inventors:
Corinna Sundermann, Bernd Sundermann, Michael Przewosny, Hagen-Heinrich Hennies
Abstract: The invention relates to a method for isolating and purifying (1RS,2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol as a saccharinate from a mixture of the diastereomers (1SR,2)RS-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and (1SR-2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and optionally impurities.
Abstract: The invention relates to parenteral dosage forms of administration that comprise a suspension of the salt of the active substances tramadol and diclofenac.
Type:
Grant
Filed:
May 21, 2003
Date of Patent:
April 5, 2005
Assignee:
Grunenthal GmbH
Inventors:
Johannes Bartholomäus, Heinrich Kugelmann
Abstract: A pharmaceutical formulation for delayed release of the active ingredient 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol or a pharmaceutically acceptable salt thereof in a matrix containing between 1 and 80 wt. % of at least one pharmaceutically acceptable hydrophilic or hydrophobic polymer as a matrix forming agent and exhibiting in vivo the following release rate: 3 to 35% by weight (based on 100% by weight active ingredient) 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 0.
Abstract: There are described DNA sequences from the genome of mammals, in particular from the human genome, coding for proteins having the biological activity of HUSI-type I inhibitors. There are further described biotechnological methods of the preparation of proteins having the biological activity of HUSI-type I inhibitors as well as pharmaceutical compositions containing said proteins.
Type:
Grant
Filed:
January 9, 1987
Date of Patent:
July 4, 1989
Assignee:
Grunenthal GmbH
Inventors:
Regina Heinzel, Heribert Appelhans, Hans G. Gassen, Werner Machleidt, Ursula Seemuller
Abstract: The invention relates to new lactam compounds, pharmaceutical compositions containing them (especially those for oral or rectal application) and to processes for the preparation of these compounds and compositions. The new compounds have the general formula ##STR1## wherein X represents a straight or branched alkyl radical with 1 to 4 carbon atoms, preferably a methyl group. The new compounds of formula (I) have sedating-tranquilizing properties. In higher dosages some of them also act as hypno-anesthetics. Moreover the derivative in which X represents the methyl group has anticonvulsant activities. The valuable compounds of formula (I) are prepared in a manner known per se e.g. by reacting an 3-alkyl-3-halogen-2-oxopiperidine (the alkyl having 1-4 carbon atoms) with a metal derivative of 2,3-dihydro-3-oxo-1,2-benzisothiazoldioxid-(1,1) or by reacting an 3-alkyl-3-amino-2-oxopiperidine with o-sulfobenzoic acid dichloride or dibromide or with an o-halomercaptobenzoylhalide, followed by oxydation.
Abstract: Derivative of 1-hydroxy-benzo-2,3,1-diazaborines which are substituted in the 2-position by a sulfo group linked to a defined aliphatic radical like alkyl or alkenyl and which may be substituted on the benzene ring by one or more lower alkyl radicals and/or halogen atoms and salts of such compounds. The pharmaceutical compositions containing these diazaborines are highly effective against gram-negative bacteria. The new compounds are prepared by reacting o-formyl phenyl boric acid, which may be substituted, with the respective aliphatic sulfonic acid hydrazide or by reacting the respective (substituted) benzaldehyde sulfonylhydrazone with a boron trihalogenide.
Type:
Grant
Filed:
July 27, 1978
Date of Patent:
April 22, 1980
Assignee:
Grunenthal GmbH
Inventors:
Hubert M. A. van Wersch, Siegfried Herrling, Heinrich Muckter
Abstract: The invention relates to new cephalosporin derivatives, which are effective as antibacterial agents, methods for their production, and medicines containing these products. These compounds have high effectiveness against numerous pathogenic microorganisms, and particularly against gram negative bacilli. Beyond that, the compounds according to the invention are also suitable as intermediate products for the production of further .beta.-lactam antibiotics.
Abstract: Drug compositions including a lactam of the substituted ortho-sulfobenzoic acid imido pyrrolidone-2, piperidone-2, or caprolactam type.The drug compositions have valuable therapeutic properties: they are immunouppressive, sedative and have antitumor activity. The method of inducing sedation in warmblooded animals.
Type:
Grant
Filed:
December 12, 1975
Date of Patent:
January 10, 1978
Assignee:
Chemie Grunenthal GmbH
Inventors:
Ivars Graudums, Heinrich Muckter, Ernst Frankus
Abstract: A process for the manufacture of 2,4-diamino-5-(substituted benzyl)pyrimidines from the corresponding 6-hydroxy-derivatives or the hydrochloride thereof by (a) chlorinating with phosphoryl chloride in presence of a considerable excess of hydrogen chloride and (b) hydrogenation of the thus easily in practically pure form and with high yields obtained 6-chloro derivatives.
Abstract: Lactams of the substituted ortho-sulfobenzoic acid imido pyrrolidone-2, piperidone-2, or caprolactam type. The compounds are useful drugs having therapeutical properties. They are immunosuppressive, sedative, and have antitumor activity. They are produced, for instance, by reacting bromo-lactams with a metal salt of o-sulfobenzoic acid imide.
Type:
Grant
Filed:
February 27, 1973
Date of Patent:
April 20, 1976
Assignee:
Chemie Grunenthal GmbH
Inventors:
Ivars Graudums, Heinrich Muckter, Ernst Frankus