Patents by Inventor Cenek Kolar

Cenek Kolar 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: 7241595
    Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: July 10, 2007
    Assignee: sanofi-aventis Pharma Deutschland GmbH
    Inventors: Cenek Kolar, Jörg Czech, Klaus Bosslet, Gerhard Seemann, Hans-Harald Sedlacek
  • Patent number: 6610299
    Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
    Type: Grant
    Filed: October 19, 1994
    Date of Patent: August 26, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Cenek Kolar, Jörg Czech, Klaus Bosslet, Gerhard Seemann, Hans-Harald Sedlacek, Dieter Hoffmann
  • Publication number: 20030064482
    Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
    Type: Application
    Filed: April 24, 2002
    Publication date: April 3, 2003
    Applicant: Hoechst Aktiengesellschaft
    Inventors: Cenek Kolar, Jorg Czech, Klaus Bosslet, Gerhard Seemann, Hans-Harald Sedlacek, Dieter Hoffman
  • Patent number: 6475486
    Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: November 5, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Cenek Kolar, Jörg Czech, Klaus Bosslet, Gerhard Seemann, Hans-Harald Sedlacek, Dieter Hoffman
  • Patent number: 6146658
    Abstract: Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: November 14, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Bosslet, Jorg Czech, Dieter Hoffmann, Cenek Kolar, Fran.cedilla.ois Tillequin, Jean-Claude Florent, Michel Azoulay, Claude Monneret, Jean-Claude Jacquesy, Jean-Pierre Gesson, Michel Koch
  • Patent number: 5955100
    Abstract: Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: September 21, 1999
    Assignees: Behringwerke Aktiengesellschaft, Laboratories Hoechst S/A
    Inventors: Klaus Bosslet, Jorg Czech, Dieter Hoffmann, Cenek Kolar, Fran.cedilla.ois Tillequin, Jean-Claude Florent, Michel Azoulay, Claude Monneret, Jean-Claude Jacquesy, Jean-Pierre Gesson, Michel Koch
  • Patent number: 5627283
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 6, 1997
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5561119
    Abstract: Glycosylated prodrugs, a preparation method therefor, and their use with tumor-specific immunoenzymatic conjugates for the treatment of cancer, are described. These anthracycline prodrugs have formula (I).
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: October 1, 1996
    Assignees: Laboratoires Hoechst, Behringwerke A.G.
    Inventors: Jean-Claude Jacquesy, Jean-Pierre Gesson, Claude Monneret, Martine Mondon, Brigitte Renoux, Jean-Claude Florent, Michel Koch, Fran.cedilla.ois Tillequin, Hans H. Sedlacek, Manfred Gerken, Cenek Kolar, Gilbert Gaudel, Klaus Bosslet, J org Czech, Dieter Hoffman, Gerhard Seemann, Hans-Ulrich Schorlemmer, Gerhard Dickneite
  • Patent number: 5556941
    Abstract: Glycopeptide derivatives, a process for their preparation and pharmaceutical agents containing these compounds N-Glycopeptide derivatives of the formula I ##STR1## where aromatic is an unsubstituted or substituted benzene residue, naphthalene residue, chroman residue, chromene residue or coumarone residue,a is 0 to 5, b is 0 to 4, c is 0 or 1, d is 1 or 2R.sup.1 is (C.sub.1 -C.sub.3)-alkyl,R.sup.2 is (C.sub.1 -C.sub.3)-alkyl or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.3 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, NH.sub.2, NH-(C.sub.1 -C.sub.6)-alkanoyl, NH-benzoyl, NH--SO.sub.3 H or NH-acyl radical of a natural N-acetylated amino acid,R.sup.4 is H, OH, or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.5 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, fluorine, chlorine or bromine,R.sup.6 is H, CH.sub.3, CH.sub.2 OH, CH.sub.2 O--(C.sub.1 -C.sub.6), CH.sub.2 NHCOCH.sub.3 or CH.sub.2 NH--SO.sub.3 H,R.sup.5 and R.sup.6 are together O--CH.sub.2 --O--CH.sub.2, --O--CH(CH.sub.3)--O--CH.sub.2 or O--C(CH.sub.3).sub.2 --O--CH.sub.2,R.sup.
    Type: Grant
    Filed: August 16, 1994
    Date of Patent: September 17, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Cenek Kolar, Werner Stuber
  • Patent number: 5457114
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: October 10, 1995
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner Stuber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5434138
    Abstract: Peptides of the formula ##STR1## in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R.sup.1), F is Leu, Trp or Phe, G is L-Ser(R.sup.1), H is Gly-NH.sub.2, D-Ala-NH.sub.2 or Azagly-NH.sub.2 and R.sup.1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Konig, Jurgen Sandow, Cenek Kolar
  • 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: 5091367
    Abstract: The invention relates to peptides of the formula ##STR1## in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl.The invention also relates to methods for the preparation of these peptides, agents containing them and their use.
    Type: Grant
    Filed: June 28, 1991
    Date of Patent: February 25, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Konig, Jurgen K. Sandow, Cenek Kolar
  • Patent number: 5091521
    Abstract: Compounds of the general formula I ##STR1## in which R.sup.1 represents a hydrogen atom or an alkyl group of the formula CH.sub.3 (CH.sub.2).sub.n --where n=0 to 5,R.sup.2 represents a hydrogen atom when X is a carbamoyl group, an alkyl group having 1 to 6 carbon atoms, a group, bonded in an ether-like fashion, of the formula R.sup.3 --O--CH.sub.2 --(CHR.sup.4).sub.m --CH.sub.2 -- in whichR.sup.3 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms,R.sup.4 is a hydroxyl group or an alkyloxy group having 1 to 3 carbon atoms, and m is 0 to 2, represents a group, bonded in an ether-like fashion, of the formula H--(CH.sub.2).sub.a --(O--(CH.sub.2).sub.b).sub.c -- where a=0 to 4, b=1 to 4 and c=1 to 7, orR.sup.2 represents a radical, bonded in a O-glycoside fashion of the formula ##STR2## in whichR.sup.5, R.sup.6 and R.sup.7, independently of one another, are a hydrogen atom or a hydroxyl group, andR.sup.
    Type: Grant
    Filed: August 28, 1990
    Date of Patent: February 25, 1992
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Cenek Kolar, Konrad Dehmel, Hans Peter Kraemer
  • Patent number: 5071836
    Abstract: Peptides of the formulaAc-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Yin which X represents Tyr or His and Y represents Gly-NH.sub.2, D-Ala-NH.sub.2, Azgly-NH.sub.2 or NH--C.sub.2 H.sub.5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.
    Type: Grant
    Filed: December 12, 1989
    Date of Patent: December 10, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Cenek Kolar, Wolfgang Konig, Jurgen K. Sandow
  • Patent number: 5049549
    Abstract: 7-O-Glycosyl-rhodomycins which correspond to the general formula I below ##STR1## in which the radicals have the following meaning: R.sup.1 is a hydrogen atom or a hydroxyl group,R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 a hydroxyl group, an O-acyl protective group or the methyloxycarbonyl group,R.sup.4 is a hydrogen atom, an O-acyl protective group, an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group andR.sup.5 is an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group,where acyl protective group denotes an acetyl, mono-, di- or trihalogenoacetyl group with fluorine or chlorine as halogen or the p-nitrobenzoyl group, and a process for the preparation thereof and the use thereof as pharmaceuticals, are described.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: September 17, 1991
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Cenek Kolar, Hans P. Kraemer, Konrad Dehmel
  • Patent number: 4965352
    Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## wherein R.sup.1 is a CH.sub.3 (CH.sub.2).sub.n group with n=0 to 3,R.sup.2 is a hydrogen atom or a methyl group,R.sup.3 is a hydrogen atom, a methyl group or an acyl protective group, andR.sup.4 is a hydrogen atom or an acyl protective group,and which are optionally in the form of a salt of an inorganic or organic acid, to a process for their preparation and to their use in pharmaceuticals.
    Type: Grant
    Filed: June 12, 1989
    Date of Patent: October 23, 1990
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Cenek Kolar, Michael Paal, Peter Hermentin, Hans P. Kraemer
  • Patent number: 4948880
    Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, which are optionally in the form of a salt of an inorganic or organic acid, ##STR1## in which the substituents have the following meaning: R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen or 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 is hydrogen, a hydroxyl or a methoxycarbonyl group, or a substituent of the general formula II, ##STR2## in which R.sup.8a has the meaning indicated for R.sup.8, or a substituent of the formula III, ##STR3## R.sup.6 is ethyl, methylcarbonyl, hydroxymethylcarbonyl, hydroxyalkyl or a dihydroxyalkyl,R.sup.7 is hydrogen or a substituent of the general formula IV, ##STR4## and R.sup.8 is hydrogen or a cyanomethyl group or a substituent of the general formula COR.sup.9 or CH.sub.2 R.sup.10, R.sup.9 being hydrogen, CH.sub.3, CF.sub.3 or CCl.sub.3, and R.sup.10 being C.sub.1 - to C.sub.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: August 14, 1990
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Peter Hermentin, Michael Paal, Hans P. Kraemer, Cenek Kolar, Dieter Hoffmann, Manfred Gerken, Hans G. Berscheid, Dirk Bottger
  • Patent number: 4914191
    Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## in which the radicals R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen or a hydroxyl group or a structure of the formula II, and R.sup.3 is a hydroxyl group or a structure of the formula II ##STR2## in which R.sup.4 is an aliphatic or aromatic acyl group, with the proviso that at least one of the radicals R.sup.2 and R.sup.3 has a structure of the formula II, which are optionally in the form of a salt of an inorganic or organic acid, as well as to the process for the preparation thereof, and to the use thereof in pharmaceuticals.
    Type: Grant
    Filed: July 7, 1988
    Date of Patent: April 3, 1990
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Peter Hermentin, Michael Paal, Cenek Kolar, Hans P. Kraemer, Dieter Hoffmann, Hans G. Berscheid, Dirk Bottger
  • Patent number: 4730069
    Abstract: Compounds of the general formulae I and II ##STR1## in which R.sup.1 and R.sup.2 independently of one another represent H--(CH.sub.2).sub.a --(O--(CH.sub.2).sub.b).sub.c --O, where a=0 to 4, b=1 to 4 and c=1 to 7, an alkoxy or arylalkoxy group with 1 to 20 carbon atoms, an alkane- or aralkanesulfonyloxy group with 1 to 7 carbon atoms or a tetrahydropyranyloxy radical, orR.sup.1 and R.sup.2 together represent an oxygen atom bonded in an ether-like manner or an acetal or ketal radical ##STR2## where R.sup.3 and R.sup.4 independently of one another represent a hydrogen atom, an alkyl group with 1 to 20 carbon atoms of a phenyl group,A.sup.1 and A.sup.2 are identical and represent a hydroxyl group, chloride, bromide, iodide, nitrate, acetate, trifluoroacetate, trifluorosulfonate or perchlorate, orA.sup.1 represents sulfate or carbonate ion and A.sup.2 represents H.sub.2 O, orA.sup.1 A.sup.
    Type: Grant
    Filed: August 30, 1985
    Date of Patent: March 8, 1988
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Cenek Kolar, Hans P. Kraemer, Konrad Dehmel