Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immuno-suppressant/immunomodulating actions.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
July 19, 2005
Assignee:
ASTA MEDICA, Aktiengesellschaft
Inventors:
Guillaume Lebaut, Cécilia Menciu, Bernhard Kutscher, Peter Emig, Stefan Szelenyi, Kay Brune
Abstract: The invention relates to novel modifications of the compound 2-amino-4-(4-fluorobenzylamino)-1-ethoxy-carbonylaminobenzene of the
processes for their preparation and their use in pharmaceutical compositions.
Type:
Grant
Filed:
October 29, 1998
Date of Patent:
March 25, 2003
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Peter Meisel, Karl-Friedrich Landgraf, Jürgen Schäfer, Wilfried Thiel, Matthias Rischer, Alfred Olbrich, Bernhard Kutscher
Abstract: A method of treating protozoal and fungal diseases is described, in which an effective amount of a compound of formula I is administered to a host having a protozoal or fungal disease.
Type:
Grant
Filed:
September 29, 2000
Date of Patent:
November 12, 2002
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Gerhard Nössner, Bernhard Kutscher, Jürgen Engel, Wolfgang Schumacher, Jurij Stekar, Peter Hilgard
Abstract: Novel, advantageous dosage forms of thioctic acid and the enantiomers thereof together with thioctic acid salts are described. The pharmaceutical formulations according to the invention are used for the production of pharmaceutical dosage forms which release the active ingredient more rapidly and have greater bioavailability than previous forms.
Type:
Grant
Filed:
August 20, 1999
Date of Patent:
February 19, 2002
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Helmut Hettche, Matthias Rischer, Werner Sarlikiotis
Abstract: A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with &agr;-reductase inhibitors or &agr;-receptor blocking agents. The regiment reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0.5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0.30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with &agr;-reductase inhibitors or a &agr;-receptor blocking agents.
Type:
Grant
Filed:
September 22, 1999
Date of Patent:
October 9, 2001
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Jürgen Engel, Thomas Reissmann, Hilde Riethmüller-Winzen, Jürgen Rawert
Abstract: Camomile oil having a high cis- and trans-spiroether content is produced in a process which includes steam distillation or aqueous distillation of fresh camomile or an extraction residue of camomile.
Abstract: The invention relates to the use of R-(+)-&agr;-lipoic acid, R-(−)-dihydrolipoic acid or their metabolites, salts, esters and amides for the synthesis of drugs for the treatment of diabetes mellitus of types I and II, compensated and decompensated insulin resistance and sequelae or late complications of diabetes mellitus, such as cataracts, polyneuropathy, nephropathy, as well as sequelae or late complications of insulin resistance. These drugs mentioned can also be used advantageously in combination with other antidiabetic drugs, particularly with insulin, and/or other additives or stabilizers or adjuvants, such as vitamin B, vitamin C, NADH, NADPH and ubiquinone.
The invention furthermore relates to the use of R-(+)-&agr;-lipoic acid, R-(−)-dihydrolipoic acid or their metabolites, as well as their salts, esters and amides for the preparation of drugs for the treatment of diseases with limited function of or a lowered content of the glucose transporters.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
September 4, 2001
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Klaus Wessel, Harald Borbe, Heinz Ulrich, Helmut Hettche, Hans Bisswanger, Lester Packer, Amira Klip
Abstract: The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
July 10, 2001
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Dietmar Reichert, Bernhard Kutscher, Holger Bang, Kay Brune, Gerhard Quinkert, Hans-Günter Schaible
Abstract: The invention relates to the use of racemic &agr;-lipoic acid or its enantiomers or pharmaceutically acceptable salts, amides, esters or thioesters thereof, in reduced or oxidized form, as active ingredient in the prevention or the acute or chronic treatment of migraine.
Type:
Grant
Filed:
August 15, 2000
Date of Patent:
June 26, 2001
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Jean Schoenen, Jürgen Engel, Klaus Wessel, Manfred Peukert, Michael Lobisch, Harald Borbe
Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents
and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.
Type:
Grant
Filed:
April 2, 1999
Date of Patent:
May 15, 2001
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Bernd Nickel, Istvan Szelenyi, Jürgen Schmidt, Peter Emig, Dietmar Reichert, Eckhard Günther, Kay Brune
Abstract: The invention relates to a process for the preparation of compounds of the general formula I
in which R1 and R2 are identical or different and are a C1-C20-alkyl group, C3-C12-cycloalkyl group, C7-C12-aralkyl group or a mono- or binuclear aryl group, in which a ketone of the formula III or IV
in which R1 and R2 have the above meaning, is asymmetrically hydrogenated.
Abstract: A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme
in which R1 is H, 2-bromoethyl, 2-chloroethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl; R2 is H or 2-chloroethyl; R3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; and R4 is H; or R1 and R2, and also R3 and R4, together with the linked N atom, form an aziridide ring, where R1, R2 and R3 are not simultaneously H, and R1 and R3 are not simultaneously 1-phenylethyl; and Y, which is optionally present, is hydrogen chloride or hydrogen bromide. The reaction is carried out in a single vessel with phosphoryl chloride and an auxiliary base as an acid-binding agent with minimization of the effect of water and without isolation of an intermediate compound.
Type:
Grant
Filed:
September 8, 1998
Date of Patent:
February 13, 2001
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Ulf Niemeyer, Harald Niegel, Bernard Kutscher, Ion Neda
Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with 5-azaquinoxaline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to 5-azaquinoxaline compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
January 30, 2001
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
Abstract: Phospholipid derivatives of Formula X:
wherein A is the ring system
in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.
Type:
Grant
Filed:
August 4, 1997
Date of Patent:
January 9, 2001
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Gerhard Nössner, Bernhard Kutscher, J{umlaut over (u)}rgen Engel, Wolfgang Schumacher, Jurij Stekar, Peter Hilgard
Abstract: A process for the preparation of lipolic acid (thioctic acid), or a derivative thereof, is one in which a 2-substituted cyclohexanone is transformed in an oxidation reaction to a lactone having formula (I), wherein X is a heteroatom substituent.
Type:
Grant
Filed:
May 12, 1999
Date of Patent:
October 31, 2000
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Brian Michael Adger, Raymond McCague, Stanley Michael Roberts
Abstract: The invention relates to the use of flupirtine or its salts for the production of a medicament for the prophylaxis and therapy of disorders which accompany an unphysiologically high cell death rate. Of particular importance here is the treatment of organ disorders with cell-destroying processes, such as myocardial infarct, shock kidney, shock lung, senile macular degeneration or traumas as a result of mechanical, thermal, radiation or toxic influences.
Type:
Grant
Filed:
June 11, 1997
Date of Patent:
September 26, 2000
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Gabriele Pergande, Werner E. Muller, Neville Osborne, Heinz Ulrich
Abstract: The invention relates to the use of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene of formula I ##STR1## or its pharmaceutically utilizable salts, for the prophylaxis and treatment of neuropathic pain.
Type:
Grant
Filed:
September 27, 1999
Date of Patent:
September 12, 2000
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Chris Rundfeldt, Reni Bartsch, Angelika Rostock, Christine Tober, Rita Dost