Patents Assigned to 4SC AG
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Novel calcium salts of Compound as Anti-Inflammatory, Immunomodulatory and Anti-Proliferatory Agents
Publication number: 20120029034Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 2, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT -
Publication number: 20120028985Abstract: The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,Type: ApplicationFiled: November 6, 2009Publication date: February 2, 2012Applicant: 4SC AGInventors: Manfred Gröppel, Johann Leban
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Patent number: 8106048Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) 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, SO2R6, 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;Type: GrantFiled: July 29, 2005Date of Patent: January 31, 2012Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzík
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Publication number: 20120022068Abstract: The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2?, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7?R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2?, O, or S; Z is N or CR2?.Type: ApplicationFiled: September 2, 2011Publication date: January 26, 2012Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Patent number: 8067615Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: GrantFiled: June 24, 2010Date of Patent: November 29, 2011Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
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Publication number: 20110263486Abstract: The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRc?ONRaRb, —NRcC?SNRaRb, —NRcC?NRdNaRb, heterocycle, —C?ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C?O, C?S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occurring amino acid; Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occurring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occurring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.Type: ApplicationFiled: March 11, 2011Publication date: October 27, 2011Applicant: 4SC AGInventors: Johann LEBAN, Martin KRALIK
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Publication number: 20110245289Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.Type: ApplicationFiled: March 23, 2009Publication date: October 6, 2011Applicant: 4SC AGInventors: Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev Kulkarni, Anil Jagtap, Ganesh Chaure
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Publication number: 20110201643Abstract: Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.Type: ApplicationFiled: March 12, 2009Publication date: August 18, 2011Applicant: 4SC AGInventors: Thomas Maier, Thomas Beckers, Christian Hesslinger
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Publication number: 20110172241Abstract: 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: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Applicant: 4SC AGInventors: Thomas HERZ, Rolf KRAUSS, Michael KUBBUTAT, Martin LANG, Christoph SCHAECHTELE, Stefan TASLER, Frank TOTZKE
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Publication number: 20110105568Abstract: Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II?): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof.Type: ApplicationFiled: March 11, 2009Publication date: May 5, 2011Applicant: 4SC AGInventors: Matthias Muller, Bernd Muller, Thomas Maier
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Publication number: 20110091889Abstract: The present invention provides a centrosome assay for the identification of preferably, Eg5 inhibitors.Type: ApplicationFiled: March 24, 2009Publication date: April 21, 2011Applicant: 4SC AGInventors: Claudia Diefenbach, Matthias Vennemann, Astrid Grunwald
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Publication number: 20110086897Abstract: A salt of (E)-N-{2-amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-be?zenesulfonyl]-1H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicant: 4SC AGInventors: Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Muller, Thomas Maier, Bernd Muller
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Publication number: 20110077404Abstract: The invention relates to a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-?-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitor, with very high overall chemical yield and enantiomeric purity.Type: ApplicationFiled: March 5, 2009Publication date: March 31, 2011Applicant: 4SC AGInventors: Bernd Muller, Helmut Schlemper
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Publication number: 20110065734Abstract: The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth.Type: ApplicationFiled: November 14, 2008Publication date: March 17, 2011Applicant: 4SC AGInventors: Thomas Bar, Thomas Maier, Thomas Beckers, Thomas Clossek, Siavosh Mahboobi, Andreas Sellmer
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Publication number: 20110027226Abstract: Compounds of a certain formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: August 22, 2007Publication date: February 3, 2011Applicant: 4SC AGInventors: Matthias Vennemann, Juergen Braugner, Petra Gimmnich, Thomas Baer
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Publication number: 20110021494Abstract: The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.Type: ApplicationFiled: September 19, 2008Publication date: January 27, 2011Applicant: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Matthias Vennemann, Volker Gekeler, Astrid Zimmermann, Petra Gimmnich, Kamlesh Padiya, Hemant Joshi, Uday Joshi, Mahindra Makhija, Dipak Harel
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Patent number: 7842820Abstract: Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective HDAC inhibitors.Type: GrantFiled: March 10, 2005Date of Patent: November 30, 2010Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
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Publication number: 20100280081Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: ApplicationFiled: May 3, 2010Publication date: November 4, 2010Applicant: 4SC AGInventors: Daniel VITT, Manfred GROEPPEL, Roland BAUMGARTNER, Johann LEBAN
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Publication number: 20100267717Abstract: The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2?, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7?R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2?, O, or S; Z is N or CR2?.Type: ApplicationFiled: March 14, 2007Publication date: October 21, 2010Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Patent number: 7812041Abstract: The present invention relates to compounds of the general formula (I) 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 1;Type: GrantFiled: July 29, 2005Date of Patent: October 12, 2010Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik