Patents by Inventor Ulrich Stache

Ulrich Stache has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 6835724
    Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III:  R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1)  III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: December 28, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Ulrich Stache, Hans-Georg Alpermann, Walter D├╝rckheimer, Manfred Bohn
  • Publication number: 20020103392
    Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds
    Type: Application
    Filed: July 22, 1997
    Publication date: August 1, 2002
    Inventors: ULRICH STACHE, HANS-GEORG ALPERMANN, WALTER DURCKHEIMER, MANFRED BOHN
  • Patent number: 6152404
    Abstract: An apparatus advantageously influences the wing root airflow along the wing root of an aircraft having a high lift system including leading edge slats provided on the main wings. The apparatus includes a respective vortex generator arranged on the inboard end of each leading edge slat in the area of the wing root, and further includes a respective transition fairing arranged on a separation edge that is let into the leading edge of the wing root and that borders along the inboard edge of the respective slat. The vortex generator is a rigid member fixed to the leading edge slat and may be in the shape of a horn, a disk, or a winglet. The transition fairing may be a rigid member fixed to the wing root along the separation edge, or may be a flexible elastic member that can be inflated to have a variable outer contour. The present system avoids the need of additional independently movable auxiliary flaps, and thus achieves a reduced weight, complexity, and maintenance requirement.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: November 28, 2000
    Assignee: DaimlerChrysler Aerospace Airbus GmbH
    Inventors: Axel Flaig, Detlev Schwetzler, Ulrich Stache, deceased
  • Patent number: 5824670
    Abstract: 17-Deoxycorticoid-21-carboxylic esters of the formula I ##STR1## are described, in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III.The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group.
    Type: Grant
    Filed: September 18, 1995
    Date of Patent: October 20, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Hans-Georg Alpermann, Manfred Bohn
  • Patent number: 5637721
    Abstract: The invention relates to a process which comprises a compound of the formula II ##STR1##
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 10, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Elisabeth Defossa, Gerd Fischer, Uwe Gerlach, Rolf Horlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann
  • Patent number: 5614623
    Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxyme thyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive steps.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: March 25, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Fischer, Elisabeth Defo.beta.a, Uwe Gerlach, Rolf H orlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann, Dieter Isert
  • Patent number: 5608093
    Abstract: Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.
    Type: Grant
    Filed: August 25, 1994
    Date of Patent: March 4, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Hans-Georg Alpermann, Walter D urckheimer, Manfred Bohn
  • Patent number: 5589594
    Abstract: The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R.sup.1 is C.sub.1 -C.sub.5 -alkanoyloxy-C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.5 -alkoxycarbonyloxy-C.sub.1 -C.sub.3 -alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form.
    Type: Grant
    Filed: December 30, 1993
    Date of Patent: December 31, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Elisabeth Defossa, Gerd Fischer, Uwe Gerlach, Rolf Horlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann
  • Patent number: 5550232
    Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Fischer, Elisabeth Defossa, Uwe Gerlach, Rolf H orlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann, Dieter Isert
  • Patent number: 5461043
    Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: October 24, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Fischer, Elisabeth Defossa, Uwe Gerlach, Rolf Horlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann, Dieter Isert
  • Patent number: 5410042
    Abstract: The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage.The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.
    Type: Grant
    Filed: May 19, 1993
    Date of Patent: April 25, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Norbert Krass, Elisabeth Defossa, Gerd Fischer, Uwe Gerlach, Rolf Hoerlein, Rudolf Lattrell, Adolf H. Linkies, Wolfgang Martin, Ulrich Stache, Theodor Wollmann
  • Patent number: 5362721
    Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.
    Type: Grant
    Filed: February 8, 1993
    Date of Patent: November 8, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Walter Durckheimer, Hans G. Alpermann, Walter Petri
  • Patent number: 5260425
    Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.
    Type: Grant
    Filed: June 2, 1989
    Date of Patent: November 9, 1993
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Peter Hermentin, Ernst Raab, Cenek Kolar, Manfred Gerken, Dieter Hoffmann, Hans P. Kraemer, Ulrich Stache
  • Patent number: 4762648
    Abstract: The present invention relates to a novel mono-functional and bis-functional anthraquinone-(oxy-2,3-oxido-propanes) and to a process for their preparation. The compounds according to the invention are useful as intermediates in the preparation of drugs possessing a .beta.-receptor blocker action and as crosslinking agents in the preparation of polymers, and moreover exhibit cytostatic activity.
    Type: Grant
    Filed: August 29, 1984
    Date of Patent: August 9, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Hans P. Kraemer, Hans-Harald Sedlacek
  • Patent number: 4377575
    Abstract: What is disclosed are steroid-21-halogeno-17-(alkyl carbonates), useful as medicaments for the treatment of inflammatory dermatoses, and a method for making them.
    Type: Grant
    Filed: December 15, 1980
    Date of Patent: March 22, 1983
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Werner Fritsch, Hans G. Alpermann, Jurgen K. Sandow
  • Patent number: 4242334
    Abstract: What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.
    Type: Grant
    Filed: August 2, 1978
    Date of Patent: December 30, 1980
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Werner Fritsch, Hans G. Alpermann
  • Patent number: 4191765
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.1' are identical or different and represent hydrogen, an alkyl radical or alkoxy radical having 1-4 carbon atoms, the allyl group, a halogen atom or the nitro group, R.sup.2 represents an acrylic acid radical or an acrylic acid nitrile radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, an alkyl radical having 1-5 carbon atoms, an aryl radical or aryl-lower alkyl radical either unsubstituted or substituted by lower alkyl or alkoxy, R.sup.6 represents hydrogen or an alkyl radical having 1-8 carbon atoms, R.sup.7 represents hydrogen, a lower alkyl radical or an aryl-lower alkyl radical, R.sup.3 and R.sup.4 represent together with the nitrogen atom a heterocyclic ring with 5-7 members being optionally substituted by C.sub.1 -C.sub.4 alkyl, in which ring one carbon atom may be replaced by one oxygen atom, sulfur atom or one further nitrogen atom, the latter may be substituted, or wherein R.sup.3 represents hydrogen and R.sup.
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: March 4, 1980
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Werner Fritsch, Ulrich Stache, Ernst Lindner
  • Patent number: 4003997
    Abstract: Cyclic 2',3'-ethers of 3-hydroxy-14,15.beta.-oxido-14.beta.-bufa-4,20,22-trienolide, 3.beta.-(.alpha.-L-rhamnopyranoside) and process for preparing them. The compounds have a strongly positive inotropic activity and may be used in the therapy of cardiac insufficiency.
    Type: Grant
    Filed: August 12, 1974
    Date of Patent: January 18, 1977
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Kurt Radscheit, Werner Fritsch, Werner Haede, Ernst Lindner
  • Patent number: 3950323
    Abstract: Digoxigenine-3-[2', 3'-didesoxy-glycosides] of the formula ##SPC1##In which R.sup.1 is the digoxigenine radical and R.sup.2 is hydrogen, methyl or --CH.sub.2 OH, which are prepared by a reaction of a digoxigenine-12-monoacylate with an acylated 1,2-glycal, a catalytic hydrogenation of the 12-acylates obtained and a subsequent hydrolysis. The products have a cardiotonic, diuretic and especially venotonic activity.
    Type: Grant
    Filed: November 16, 1973
    Date of Patent: April 13, 1976
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Werner Fritsch, Werner Haede, Ernst Lindner
  • Patent number: 3937697
    Abstract: 12-Dehydro digoxin mono-4'" and 3'"-alkyl ethers and a process for their manufacture.The compounds have a cardiotonic and diuretic activity.
    Type: Grant
    Filed: February 28, 1975
    Date of Patent: February 10, 1976
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Werner Fritsch, Werner Haede, Ernest Lindner