Patents by Inventor Hans-Georg Alpermann

Hans-Georg Alpermann 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 Dürckheimer, 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: 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: 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: 5597803
    Abstract: Peptides of the formula IZ-P-A-B-C-E-F-K-(D)Q-G-M-F'-I (I)and the physiologically tolerated salts thereof, are described.They have an excellent bradykinin-antagonistic action.They are obtained by reacting reacting a fragment with a C-terminal free carboxyl group or its activated derivative with a corresponding fragment with an N-terminal free amino group or assembling the peptide stepwise, where appropriate eliminating in the compound obtained in this way one or more protective groups introduced temporarily to protect other functionalities, and where appropriate converting the compounds of the formula I obtained in this way into the physiologically tolerated salt thereof.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: January 28, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Stephan Henke, Jochen Knolle, Bernward Scholkens, Hans-Georg Alpermann, Hermann Gerhards, Klaus Wirth
  • Patent number: 5100890
    Abstract: Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a--(CH.sub.2).sub.2-11 chain or a bridged--(CH.sub.2).sub.4-5 chain,and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III O.dbd.CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomes are resolved.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: March 31, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Herbert Siegel, Klaus-Dieter Kampe, Hans-Georg Alpermann, Hermann J. Gerhards, Patricia Usinger, Ulrich Schacht, Margret Leven, Wolfgang Raether, Walter Dittmar, Burkhard Sachse
  • Patent number: 5023357
    Abstract: Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 l and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a --(CH.sub.2).sub.2-11 chain or a bridged --(CH.sub.2).sub.4-5 chain,and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III 0=CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.
    Type: Grant
    Filed: September 21, 1989
    Date of Patent: June 11, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Herbert Siegel, Klaus-Dieter Kampe, Hans-Georg Alpermann, Hermann J. Gerhards, Patricia Usinger, Ulrich Schacht, Margret Leven, Wolfgang Raether, Walter Dittmar, Burkhard Sachse