Patents by Inventor Paul Hebeisen

Paul Hebeisen 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: 11918586
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1 X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substitu
    Type: Grant
    Filed: March 26, 2021
    Date of Patent: March 5, 2024
    Assignees: TORQUR AG, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Doriano Fabbro, Paul Hebeisen, Petra Hillmann-Wuellner, Anton Stuetz, John T. Seykora, Florent Beaufils
  • Patent number: 11878972
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; R1 and R2 are independently of each other (iii) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalk
    Type: Grant
    Filed: December 17, 2020
    Date of Patent: January 23, 2024
    Assignees: TORQUR AG, UNIVERSITÄT BASEL
    Inventors: Denise Rageot, Paul Hebeisen, Florent Beaufils, Doriano Fabbro, Petra Hillmann-Wüllner, Hoa Huu Phuc Nguyen, Wolfgang Löscher, Claudia Brandt, Alexander Markus Sele
  • Publication number: 20220153752
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR) and PI3K-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Application
    Filed: October 12, 2021
    Publication date: May 19, 2022
    Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
  • Publication number: 20220135551
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; R1 and R2 are independently of each other (iii) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl,
    Type: Application
    Filed: December 17, 2020
    Publication date: May 5, 2022
    Inventors: Denise RAGEOT, Paul HEBEISEN, Florent BEAUFILS, Doriano FABBRO, Petra HILLMANN-WÜLLNER, Hoa Huu Phuc NGUYEN, Wolfgang LÖSCHER, Claudia BRANDT, Alexander Markus SELE
  • Patent number: 11186591
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR) and PI3K-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: November 30, 2021
    Assignees: UNIVERSITÄT BASEL, TORQUR AG
    Inventors: Vladimir Cmiljanovic, Paul Hebeisen, Florent Beaufils, Thomas Bohnacker, Denise Rageot, Alexander Sele, Matthias Wymann, Jean-Baptiste Langlois
  • Publication number: 20210361665
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1 X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, ClalkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substitu
    Type: Application
    Filed: March 26, 2021
    Publication date: November 25, 2021
    Inventors: Doriano FABBRO, Paul HEBEISEN, Petra HILLMANN-WUELLNER, Anton STUETZ, John T. SEYKORA, Florent BEAUFILS
  • Patent number: 10993947
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: May 4, 2021
    Assignee: TORQUR
    Inventors: Doriano Fabbro, Paul Hebeisen, Petra Hillmann-Wuellner, Anton Stuetz, John T. Seykora, Florent Beaufils
  • Patent number: 10766874
    Abstract: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: September 8, 2020
    Assignees: UNIVERSITAET BASEL, PIQUR THERAPEUTICS AG
    Inventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
  • Publication number: 20200277304
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR) and PI3K-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Application
    Filed: March 13, 2020
    Publication date: September 3, 2020
    Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
  • Patent number: 10640516
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3k), mammalian target of rapamycin (mTOR) and PI3k-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: May 5, 2020
    Assignees: PIQUR THERAPEUTICS AG, UNIVERSITÄT BASEL
    Inventors: Vladimir Cmiljanovic, Paul Hebeisen, Florent Beaufils, Thomas Bohnacker, Denise Rageot, Alexander Sele, Matthias Wymann, Jean-Baptiste Langlois
  • Publication number: 20190290653
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrenc
    Type: Application
    Filed: May 17, 2017
    Publication date: September 26, 2019
    Inventors: Doriano FABBRO, Paul HEBEISEN, Petra HILLMANN-WUELLNER, Anton STUETZ, John T. SEYKORA, Florent BEAUFILS
  • Publication number: 20190284178
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; R1 and R2 are independently of each other (iii) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-
    Type: Application
    Filed: May 17, 2017
    Publication date: September 19, 2019
    Inventors: Denise RAGEOT, Paul HEBEISEN, Florent BEAUFILS, Doriano FABBRO, Petra HILLMANN-WÜLLNER, Hoa Huu Phuc NGUYEN, Wolfgang LÖSCHER, Claudia BRANDT, Alexander Markus SELE
  • Publication number: 20190031682
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3k), mammalian target of rapamycin (mTOR) and PI3k-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Application
    Filed: November 10, 2015
    Publication date: January 31, 2019
    Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
  • Publication number: 20190016698
    Abstract: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
    Type: Application
    Filed: July 25, 2018
    Publication date: January 17, 2019
    Inventors: Paul HEBEISEN, Florent BEAUFILS, Jean-Baptiste LANGLOIS
  • Patent number: 10100031
    Abstract: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: October 16, 2018
    Assignees: UNIVERSITAET BASEL, PIQUR THERAPEUTICS AG
    Inventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
  • Publication number: 20170037027
    Abstract: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
    Type: Application
    Filed: April 20, 2015
    Publication date: February 9, 2017
    Inventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
  • Patent number: 9556203
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor compounds of formula (I) and (II), which are conformationally restricted, and for which the meaning of the substituents are listed in the description. Preferred compounds are those wherein X isoxygen, R1 is morpholino and R2 is substituted phenyl or heteroaryl. These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: January 31, 2017
    Assignees: PIQUR THERAPEUTICS AG, UNIVERSITAET BASEL
    Inventors: Vladimir Cmiljanovic, Paul Hebeisen, Eileen Jackson, Florent Beaufils, Thomas Bohnacker, Matthias Wymann
  • Publication number: 20160244463
    Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor compounds of formula (I) and (II), which are conformationally restricted, and for which the meaning of the substituents are listed in the description. Preferred compounds are those wherein X isoxygen, R1 is morpholino and R2 is substituted phenyl or heteroaryl. These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.
    Type: Application
    Filed: October 3, 2014
    Publication date: August 25, 2016
    Inventors: Vladimir Cmiljanovic, Paul Hebeisen, Eileen Jackson, Florent Beaufils, Thomas Bohnacker, Matthias Wymann
  • Patent number: 9403808
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. In particular, the compound may be used as a preferential agonist of Cannabinoid Receptor 2.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: August 2, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Baledi Dhurwasulu, Uwe Grether, Anindya Hazra, Paul Hebeisen, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20160137606
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: January 21, 2016
    Publication date: May 19, 2016
    Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang