Patents by Inventor Dirk Scharn

Dirk Scharn 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).

  • Publication number: 20220133734
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: October 29, 2021
    Publication date: May 5, 2022
    Inventors: Harald ENGELHARDT, Mark PETRONCZKI, Juergen RAMHARTER, Ulrich REISER, Heinz STADTMUELLER, Dirk SCHARN, Tobias WUNBERG
  • Patent number: 11261184
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: March 1, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Heribert Arnhof, Sebastian Carotta, Marco Hofmann, Marc Kerenyi, Dirk Scharn
  • Patent number: 11213520
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R2 to R5, A, X and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: January 4, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Heribert Arnhof, Sebastian Carotta, Marco Hans Hofmann, Marc Kerenyi, Dirk Scharn
  • Patent number: 11174245
    Abstract: The present invention encompasses compounds of formula (I) (I), wherein the groups R1 to R5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: November 16, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dietrich Boese, Georg Dahmann, Harald Engelhardt, Mark Petronczki, Dirk Scharn
  • Publication number: 20210332054
    Abstract: The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) wherein the groups R1, R2, R3 and R4 have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: April 6, 2021
    Publication date: October 28, 2021
    Inventors: Birgit WILDING, Dietrich BOESE, Harald ENGELHARDT, Julian FUCHS, Ralph NEUMUELLER, Mark PETRONCZKI, Dirk SCHARN, Matthias TREU
  • Publication number: 20200377476
    Abstract: The present invention encompasses compounds of formula (I) (I), wherein the groups R1 to R5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: February 20, 2019
    Publication date: December 3, 2020
    Inventors: Dietrich BOESE, Georg DAHMANN, Harald ENGELHARDT, Mark PETRONCZKI, Dirk SCHARN
  • Publication number: 20200291020
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: October 1, 2018
    Publication date: September 17, 2020
    Inventors: Harald ENGELHARDT, Heribert ARNHOF, Sebastian CAROTTA, Marco HOFMANN, Marc KERENYI, Dirk SCHARN
  • Publication number: 20190290637
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R2 to R5, A, X and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: May 19, 2017
    Publication date: September 26, 2019
    Inventors: Harald ENGELHARDT, Heribert ARNHOF, Sebastian CAROTTA, Marco Hans HOFMANN, Marc KERENYI, Dirk SCHARN
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8410134
    Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
    Type: Grant
    Filed: March 22, 2008
    Date of Patent: April 2, 2013
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Christoph Gibson, Thomas Tradler, Karsten Schnatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Matthias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
  • Patent number: 8309735
    Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: November 13, 2012
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8071810
    Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: December 6, 2011
    Assignee: Jerini AG
    Inventors: Karsten Schnatbaum, Dirk Scharn, Elsa Locardi, Thomas Polakowski, Uwe Richter, Ulrich Reineke, Gerd Hummel
  • Patent number: 8029979
    Abstract: The invention relates to a method for determining the substrate specificity of an enzymatic activity comprising the following steps: providing an assembly comprising a plurality of amino acid sequences on a planar surface of a support material, whereby the amino acids are directionally immobilized; contacting and/or incubating of an enzymatic activity with the assembly; and detection of a reaction between one of the amino acid sequences that are immobilized on the assembly and the enzymatic activity. According to the invention, during the reaction of the enzymatic activity with the assembly, a change in the molecular weight of at least one of the amino acid sequences takes place.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: October 4, 2011
    Assignee: JPT Peptide Technologies GmbH
    Inventors: Jens Schneider-Mergener, Mike Schutkowski, Ulf Reimer, Liying Dong, Soren Panse, Dirk Scharn, Frank Osterkamp, Gerd Hummel, Laurence Jobron
  • Publication number: 20110065760
    Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.
    Type: Application
    Filed: November 23, 2009
    Publication date: March 17, 2011
    Applicant: Jerini AG
    Inventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
  • Publication number: 20110003756
    Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure: whereby X1 is a radical with a mass of about 1-300, whereby X1 is preferably selected from the group comprising R5-, R5-CO—, R5-N(R6)-CO—, R5-O—CO—, R5-SO2—, R5-N(R6)-SO2—, R5-N(R6)-, R5-N(R6)-CS—, R5-N(R6)-C(NH)—, R5-CS—, R5-P(O)OH—, R5-B(OH)—, R5-CH?N—O—CH2—CO—, whereby R5 and R6 are individually and independently selected from the group comprising H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl and substituted aryloxyalkyl, X2 is a radical that mimics the biological binding characteristics of a phenylalanine unit, X3 and X4 are individually and independently a spacer, whereby the spacer is preferably selected from the group comprising amino a
    Type: Application
    Filed: March 29, 2010
    Publication date: January 6, 2011
    Applicant: Jerini AG
    Inventors: Gerd Hummel, Elsa Locardi, Thomas Polakowski, Dirk Scharn, Karsten Schnatbaum
  • Publication number: 20100234344
    Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
    Type: Application
    Filed: March 22, 2008
    Publication date: September 16, 2010
    Applicant: JERINI AG
    Inventors: Christoph Gibson, Thomas Tradler, Karsten Schinatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Mathias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
  • Patent number: 7727960
    Abstract: The invention relates to a C5a receptor antagonist of structure (I), wherein X1 is a radical having a mass of about 1-300 and stands for R5-, R5-CO—, R5-N(R6)-CO—, R5-O—CO—, R5-SO2—, R5-N(R6)-SO2—, R5-N(R6)-, R5-N(R6)-CS—, R5-N(R6)-C(NH)—, R5-CS—, R5-P(O)OH—, R5-B(OH)— or R5-CH?N—O—CH2—CO—, wherein R5/R6 represent H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl or substituted aryloxyalkyl; X2=radical (biological bonding properties of a mimicrying phenylalanine unit); X3/X4=spacer (amino acids, amino-acid analogs and amino-acid derivatives); X5=radical (biological bonding properties of a mimicrying cyclohexylalanine or homoleucine unit); X6=radical (biological bonding properties of a mimicrying tryptophan unit); X7=radical (biological bonding properties of a mimicrying
    Type: Grant
    Filed: July 19, 2004
    Date of Patent: June 1, 2010
    Assignee: Jerini AG
    Inventors: Gerd Hummel, Elsa Locardi, Thomas Polakowski, Dirk Scharn, Karsten Schnatbaum
  • Publication number: 20090203745
    Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.
    Type: Application
    Filed: May 14, 2007
    Publication date: August 13, 2009
    Applicant: Jerini AG
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20090104116
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Application
    Filed: January 31, 2007
    Publication date: April 23, 2009
    Applicant: JERINI AG
    Inventors: Gunter Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20080220003
    Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl
    Type: Application
    Filed: May 30, 2006
    Publication date: September 11, 2008
    Applicant: Jerini AG
    Inventors: Karsten Schnatbaum, Dirk Scharn, Elsa Locardi, Thomas Polakowski, Uwe Richter, Ulrich Reineke, Gerd Hummel