Patents Assigned to 4SC AG
  • Patent number: 7365094
    Abstract: The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, for the use as a medicament.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: April 29, 2008
    Assignee: 4SC AG
    Inventors: Johann Leban, Stefan Tasler
  • Patent number: 7317030
    Abstract: The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or CH2 if Y is SO2 Y is C?O, C?S, or SO2 if Z is CH2; A is phenyl or indolyl, N-methyl-indolyl R1 is —CN, wherein the bond between CR3 and CR7 is a single or double bond; m is 0 or 1; n is 0 or 1; p is 0 or 1; and to their use as medicaments.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: January 8, 2008
    Assignee: 4SC AG
    Inventors: Johann Leban, Harald Schmitt
  • Patent number: 7276606
    Abstract: The present invention relates to compounds of the general formula (IV) and (II) and salts and physiologically functional derivatives thereof, wherein X is C—R8 or N; and Z is independently one of the following groups:
    Type: Grant
    Filed: May 2, 2005
    Date of Patent: October 2, 2007
    Assignee: 4SC AG
    Inventors: Stefano Pegoraro, Martin Lang, Juliane Feurle, Juergen Kraus
  • Publication number: 20070219190
    Abstract: The present invention relates to compounds of the general formula(Ig) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R1 independently represents H, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, or heteroaryl; R2 independently represents NR3R5, R3 independently represents H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 independently represents H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 independently represents H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 independently represents H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is
    Type: Application
    Filed: March 14, 2007
    Publication date: September 20, 2007
    Applicant: 4SC AG
    Inventors: Johann Leban, Daniel Vitt
  • Patent number: 7247736
    Abstract: The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.
    Type: Grant
    Filed: November 10, 2004
    Date of Patent: July 24, 2007
    Assignee: 4SC AG
    Inventors: Johann Leban, Bernd Kramer, Roland Baumgartner, Katharina Aulinger-Fuchs, Stefan Tasler
  • Patent number: 7176241
    Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).
    Type: Grant
    Filed: July 9, 2002
    Date of Patent: February 13, 2007
    Assignee: 4SC AG
    Inventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
  • Publication number: 20070027193
    Abstract: The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.
    Type: Application
    Filed: November 10, 2004
    Publication date: February 1, 2007
    Applicant: 4SC AG
    Inventors: Johann Leban, Bernd Kramer, Roland Baugartner, Katharina Aulinger-Fuchs, Stefan Tasler
  • Publication number: 20070021446
    Abstract: The present invention relates to compounds of the general formula (I) and salts, prodrugs, and stereoisomers thereof, wherein Y independently represents S, O, NR2, SO, SO2; A independently represents a fife- or six-membered aromatic carbocycle or heterocycle and wherein R1 to R20 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
    Type: Application
    Filed: May 16, 2006
    Publication date: January 25, 2007
    Applicant: 4SC AG
    Inventors: Jan Ehlert, Thomas Herz, Rolf Krauss, Michael Kubbutat, Martin Lang, Wael Saeb, Christoph Schaechtele, Stefan Tasler, Frank Totzke, Ute Zirrgiebel
  • Publication number: 20060247253
    Abstract: The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.
    Type: Application
    Filed: March 15, 2006
    Publication date: November 2, 2006
    Applicant: 4 SC AG
    Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
  • Publication number: 20060199856
    Abstract: The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehyrogenase (DHODH).
    Type: Application
    Filed: February 17, 2006
    Publication date: September 7, 2006
    Applicant: 4 SC AG
    Inventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
  • Patent number: 7071355
    Abstract: The present invention relates to compounds of the general formula (I) and salt and physiologically functional derivatives thereof, wherein A is a non-aromatic ring system containing 4 to 8 carbon atoms, wherein the ring system comprises at least one double bond and wherein one or more of the carbon atoms in the ring can be replaced by a group X, wherein X is selected from the group consisting of S, O, N, NR4, SO, CO or SO2; D is O, S, SO2, NR4 or CH2; Z1 and Z2 are independent from each other O, S, or NR5; R2 is H, OR6, or NHR7; E is an alkyl or cycloalkyl group or a monocyclic or polycyclic substituted or unsubstituted ring system which may contain one or more groups X and which contains at least one aromatic ring; Y is hydrogen, halogen, haloalkyl, haloalkyloxy, alkyl, cycloalkyl, a monocyclic or polycyclic substituted or unsubstituted ring system for the use as a medicament.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: July 4, 2006
    Assignee: 4 SC AG
    Inventors: Johann Leban, Martin Kralik
  • Publication number: 20060142570
    Abstract: The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.
    Type: Application
    Filed: December 22, 2005
    Publication date: June 29, 2006
    Applicant: 4SC AG
    Inventors: Thomas Herz, Rolf Krauss, Michael Kubbutat, Martin Lang, Christoph Schaechtele, Stefan Tasler, Frank Totzke
  • Publication number: 20060135782
    Abstract: The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
    Type: Application
    Filed: December 15, 2005
    Publication date: June 22, 2006
    Applicant: 4SC AG
    Inventors: Thomas Herz, Rolf Krauss, Michael Kubbutat, Martin Lang, Christoph Schaechtele, Stefan Tasler, Frank Totzke
  • Publication number: 20060069102
    Abstract: The present invention relates to compounds of the general formula (1) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or
    Type: Application
    Filed: July 29, 2005
    Publication date: March 30, 2006
    Applicant: 4 SC AG
    Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
  • Patent number: 6949567
    Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: September 27, 2005
    Assignee: 4SC AG
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
  • Publication number: 20050197368
    Abstract: The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or CH2 if Y is SO2 Y is C?O, C?S, or SO2 if Z is CH2; A is phenyl or indolyl, N-methyl-indolyl R1 is —CN, wherein the bond between CR3 and CR7 is a single or double bond; m is 0 or 1; n is 0 or 1; p is 0 or 1; and to their use as medicaments.
    Type: Application
    Filed: February 28, 2005
    Publication date: September 8, 2005
    Applicant: 4SC AG
    Inventors: Johann Leban, Harald Schmitt
  • Publication number: 20050176686
    Abstract: The present invention is directed to compounds of the general formula (I) or pharmaceutical acceptable salts or physiologically functional derivatives thereof wherein: n is a non-aromatic ring system containing two to seven carbon atoms, wherein the ring system can contain one ore two double bonds; X is C, CH or CH2; Y is selected from C, CH, CH2, S, NR, CH2-CH2, H2C—CH, HC—CH2, C—CH2, H2C—C, or C—C; one or more of the hydrogen atoms can optionally be substituted by one or more substituents R?; each of the dotted lines means a single, a double or triple bond with the exclusion of a combination of a triple with triple bond and a double with a triple bond; R? is independently H, —CN, alkyl, cycloalkyl, aminoalkyl, alkylamino, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, hydroxyalkylamino, halogene, haloalkyl, haloalkyloxy; R is H, an alkyl or cycloalkyl group; Z is CH, C, or P; p is 0 or 1.
    Type: Application
    Filed: July 23, 2003
    Publication date: August 11, 2005
    Applicants: 4SC AG, G2M Cancer Drugs AG
    Inventors: Alexander Maurer, Sascha Hoevelmann, Elke Martin, Bernd Hentsch, Michael Gassen, Juergen Kraus, Rolf Krauss, Adam-Spencer Vincek
  • Publication number: 20050143382
    Abstract: The present invention relates to furazanopyrazine derivatives of the general formula (I): wherein: R? represents —NR1R2 or —OR9 R? represents —NR5—NR3R4, —NR5—ORb, —O—NR3R4; wherein R1 to R9 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
    Type: Application
    Filed: November 2, 2004
    Publication date: June 30, 2005
    Applicant: 4SC AG
    Inventors: Katharina Aulinger-Fuchs, Thomas Herz, Rolf Krauss, Michael Kubbatat, Martin Lang, Christoph Schachtele, Frank Totzke
  • Publication number: 20050070570
    Abstract: The invention relates to compounds having the Formula (I) or a salt, or a physiologically functional derivative, or a prodrug thereof, wherein Z is carbonyl or sulfonyl; R1 is alkyl, alkenyl, alkynyl, aryl, H, halogen, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl or heteroaryl; R2 is H, OH, —CH2—SO2-alkyl, —CH2—SO2-cycloalkyl, —CH2—SO2-aryl, —CH2—SO2-heteroaryl, alkylamine, alkenylamine, alkynylamine, cycloalkylamine, arylamine, heteroarylamine, aryl, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl, heteroaryl or a linear or branched alkyl, alkenyl, alkynyl, which can optionally be substituted by one or more substituents R3; R3 is H, alkyl, alkenyl, alkynyl, cycloalkyl, —CO2R4, —CONHR4, —CONR4R4, —CR4O, —SO2R4, —NR4—CO—R4, alkoxy, alkylthio, —OH, —SH, —O-aryl, —O-cycloalkyl, —S-aryl, —S-cycloalkyl, hydroxyalkyl, halogen, haloalkyl, haloalkoxy, CN, NO2, hydroxyalkylamine, aminoalkyl, alkylamine, aryl or heteroaryl; R4 is H, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, —O-aryl,
    Type: Application
    Filed: June 18, 2004
    Publication date: March 31, 2005
    Applicant: 4SC AG
    Inventors: Gabriel Garcia, Wael Saeb, Bernd Kramer
  • Publication number: 20040235914
    Abstract: The present invention relates to the use of compounds of the general Formula (XIII): 1
    Type: Application
    Filed: May 6, 2004
    Publication date: November 25, 2004
    Applicant: 4 SC AG
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik