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).
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Patent number: 11918586Abstract: 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 substituType: GrantFiled: March 26, 2021Date of Patent: March 5, 2024Assignees: TORQUR AG, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Doriano Fabbro, Paul Hebeisen, Petra Hillmann-Wuellner, Anton Stuetz, John T. Seykora, Florent Beaufils
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Patent number: 11878972Abstract: 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-C2fluoroalkType: GrantFiled: December 17, 2020Date of Patent: January 23, 2024Assignees: TORQUR AG, UNIVERSITÄT BASELInventors: Denise Rageot, Paul Hebeisen, Florent Beaufils, Doriano Fabbro, Petra Hillmann-Wüllner, Hoa Huu Phuc Nguyen, Wolfgang Löscher, Claudia Brandt, Alexander Markus Sele
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Publication number: 20220153752Abstract: 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: ApplicationFiled: October 12, 2021Publication date: May 19, 2022Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
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Publication number: 20220135551Abstract: 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: ApplicationFiled: December 17, 2020Publication date: May 5, 2022Inventors: Denise RAGEOT, Paul HEBEISEN, Florent BEAUFILS, Doriano FABBRO, Petra HILLMANN-WÜLLNER, Hoa Huu Phuc NGUYEN, Wolfgang LÖSCHER, Claudia BRANDT, Alexander Markus SELE
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Patent number: 11186591Abstract: 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: GrantFiled: March 13, 2020Date of Patent: November 30, 2021Assignees: UNIVERSITÄT BASEL, TORQUR AGInventors: Vladimir Cmiljanovic, Paul Hebeisen, Florent Beaufils, Thomas Bohnacker, Denise Rageot, Alexander Sele, Matthias Wymann, Jean-Baptiste Langlois
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Publication number: 20210361665Abstract: 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 substituType: ApplicationFiled: March 26, 2021Publication date: November 25, 2021Inventors: Doriano FABBRO, Paul HEBEISEN, Petra HILLMANN-WUELLNER, Anton STUETZ, John T. SEYKORA, Florent BEAUFILS
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Patent number: 10993947Abstract: 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: GrantFiled: May 17, 2017Date of Patent: May 4, 2021Assignee: TORQURInventors: Doriano Fabbro, Paul Hebeisen, Petra Hillmann-Wuellner, Anton Stuetz, John T. Seykora, Florent Beaufils
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Patent number: 10766874Abstract: 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: GrantFiled: July 25, 2018Date of Patent: September 8, 2020Assignees: UNIVERSITAET BASEL, PIQUR THERAPEUTICS AGInventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
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Publication number: 20200277304Abstract: 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: ApplicationFiled: March 13, 2020Publication date: September 3, 2020Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
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Patent number: 10640516Abstract: 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: GrantFiled: November 10, 2015Date of Patent: May 5, 2020Assignees: PIQUR THERAPEUTICS AG, UNIVERSITÄT BASELInventors: Vladimir Cmiljanovic, Paul Hebeisen, Florent Beaufils, Thomas Bohnacker, Denise Rageot, Alexander Sele, Matthias Wymann, Jean-Baptiste Langlois
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Publication number: 20190290653Abstract: 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 occurrencType: ApplicationFiled: May 17, 2017Publication date: September 26, 2019Inventors: Doriano FABBRO, Paul HEBEISEN, Petra HILLMANN-WUELLNER, Anton STUETZ, John T. SEYKORA, Florent BEAUFILS
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Publication number: 20190284178Abstract: 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: ApplicationFiled: May 17, 2017Publication date: September 19, 2019Inventors: Denise RAGEOT, Paul HEBEISEN, Florent BEAUFILS, Doriano FABBRO, Petra HILLMANN-WÜLLNER, Hoa Huu Phuc NGUYEN, Wolfgang LÖSCHER, Claudia BRANDT, Alexander Markus SELE
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Publication number: 20190031682Abstract: 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: ApplicationFiled: November 10, 2015Publication date: January 31, 2019Inventors: Vladimir CMILJANOVIC, Paul HEBEISEN, Florent BEAUFILS, Thomas BOHNACKER, Denise RAGEOT, Alexander SELE, Matthias WYMANN, Jean-Baptiste LANGLOIS
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Publication number: 20190016698Abstract: 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: ApplicationFiled: July 25, 2018Publication date: January 17, 2019Inventors: Paul HEBEISEN, Florent BEAUFILS, Jean-Baptiste LANGLOIS
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Patent number: 10100031Abstract: 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: GrantFiled: April 20, 2015Date of Patent: October 16, 2018Assignees: UNIVERSITAET BASEL, PIQUR THERAPEUTICS AGInventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
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Publication number: 20170037027Abstract: 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: ApplicationFiled: April 20, 2015Publication date: February 9, 2017Inventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
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Patent number: 9556203Abstract: 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: GrantFiled: October 3, 2014Date of Patent: January 31, 2017Assignees: PIQUR THERAPEUTICS AG, UNIVERSITAET BASELInventors: Vladimir Cmiljanovic, Paul Hebeisen, Eileen Jackson, Florent Beaufils, Thomas Bohnacker, Matthias Wymann
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Publication number: 20160244463Abstract: 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: ApplicationFiled: October 3, 2014Publication date: August 25, 2016Inventors: Vladimir Cmiljanovic, Paul Hebeisen, Eileen Jackson, Florent Beaufils, Thomas Bohnacker, Matthias Wymann
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Patent number: 9403808Abstract: 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: GrantFiled: October 24, 2012Date of Patent: August 2, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Baledi Dhurwasulu, Uwe Grether, Anindya Hazra, Paul Hebeisen, Stephan Roever, Mark Rogers-Evans
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Publication number: 20160137606Abstract: 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: ApplicationFiled: January 21, 2016Publication date: May 19, 2016Inventors: 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