Patents by Inventor Bjoern Bartels
Bjoern Bartels 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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Publication number: 20240294543Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.Type: ApplicationFiled: April 4, 2024Publication date: September 5, 2024Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Giuseppe CECERE, Guido GALLEY, Luca GOBBI, Martin GOEBEL, Maria-Clemencia HERNANDEZ, Andrés Miguel OLIVARES MORALES, Hasane RATNI, Michael REUTLINGER, Valerie RUNTZ-SCHMITT
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Publication number: 20240217928Abstract: The invention relates to novel compounds having the general formula I wherein R1, R2, R3, R4, R5, R6, R7, W, m and n are as described herein, composition including the compounds and methods of using the compounds.Type: ApplicationFiled: January 25, 2024Publication date: July 4, 2024Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Karlheinz BAUMANN, Fiona GRUENINGER, Remo HOCHSTRASSER, Bernd KUHN, Federica MORANDI, Emmanuel PINARD
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Publication number: 20230142171Abstract: The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.Type: ApplicationFiled: October 4, 2022Publication date: May 11, 2023Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Roland HUMM, Andrés Miguel OLIVARES MORALES, Angélique PATINY-ADAM, Valerie RUNTZ-SCHMITT, Christian SCHNIDER
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Publication number: 20230136326Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.Type: ApplicationFiled: September 28, 2022Publication date: May 4, 2023Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Giuseppe CECERE, Guido GALLEY, Luca GOBBI, Maria-Clemencia HERNANDEZ, Andreas KOBLET, Andrés Miguel OLIVARES MORALES, Angélique PATINY-ADAM, Valerie RUNTZ-SCHMITT
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Publication number: 20220306607Abstract: The present invention provides compounds of formula I wherein R1, R2 or R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula I, pharmaceutical compositions comprising them and their use as medicaments.Type: ApplicationFiled: June 1, 2022Publication date: September 29, 2022Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Amanda Lee Dupont, Benjamin J. Hall, Jean-Yves Wach, Christian Schnider, Patrick Schnider, Michael Reutllinger, Eoin O'Connor, Eva Katrin Harde, Michael Weber
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Patent number: 11440915Abstract: The present invention relates to compounds of formula (I), wherein R is hydrogen or halogen, wherein R may be different if n=2 or 3; n is 1, 2 or 3; (II) is a disubstituted bicyclo[1,1,1]pentane or bicyclo[2,2,2]octane as defined below: (III) or (IV); or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: December 17, 2018Date of Patent: September 13, 2022Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Xinlan Aloise Ford Cook, Hasane Ratni, Michael Reutlinger, Walter Vifian
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Patent number: 11414420Abstract: The invention provides new pyrimidine compounds having the general formula (I), wherein R1, R2, R3, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.Type: GrantFiled: November 26, 2018Date of Patent: August 16, 2022Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Xinlan Aloise Ford Cook, Hasane Ratni, Michael Reutlinger, Walter Vifian
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Patent number: 11319314Abstract: The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two R1 occur; R2 is lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH2-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH2-heterocycloalkyl unsubstituted or substituted by lower alkyl; R3 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(O)2-lower alkyl; n is 1, 2 or 3; if n is >1, then R3 may be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof.Type: GrantFiled: November 6, 2017Date of Patent: May 3, 2022Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Stefan Berchtold, Guido Galley, Annick Goergler, Roland Jakob-Roetne, Daniela Krummenacher, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Rosa Maria Rodriguez Sarmiento, Christian Schnider
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Patent number: 11306093Abstract: A process for preparing the compound of formula I comprising: a) coupling a compound of formula 2 wherein a leaving group O—SO2—R is selected from the triflate group, the tosylate group, the mesylate group, the besylate group, the nosylate group or the brosylate group, with a suitable boronic acid, a trifluoroborate or a boronic acid ester under argon condition and in the presence of a catalyst and a base in a suitable solvent and then isolating the product as an acid addition salt to afford the compound of formula Ia and b) converting the acid addition salt of formula Ia wherein the acid HX comprises suitable organic or inorganic acids into the compound of formula I by treatment with at least a stoichiometric equivalent of a suitable base.Type: GrantFiled: March 6, 2019Date of Patent: April 19, 2022Assignee: Hoffmann-La Roche, Inc.Inventors: Bjoern Bartels, Philipp Cueni, Matthias Koerner, Dieter Muri
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Publication number: 20210309653Abstract: The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, i-f two R1 occur; R2 is lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH2-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH2-heterocycloalkyl unsubstituted or substituted by lower alkyl; R3 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(0)2-lower alkyl; n is 1, 2 or 3; if n is >1, then R3 may be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: November 6, 2017Publication date: October 7, 2021Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Stefan BERCHTOLD, Guido GALLEY, Annick GOERGLER, Roland JAKOB-ROETNE, Daniela KRUMMENACHER, Anja LIMBERG, Werner NEIDHART, Hasane RATNI, Michael REUTLINGER, Rosa Maria RODRIGUEZ SARMIENTO, Christian SCHNIDER
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Patent number: 11034687Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: GrantFiled: June 17, 2020Date of Patent: June 15, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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Patent number: 10941147Abstract: The present invention relates to a compound of formula I, 1-1 or 1-2 wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; R1 may be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; or to a pharmaceutically active acid addition salt thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: October 30, 2017Date of Patent: March 9, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Jérôme Charles Sarie, Greta Vastakaite
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Patent number: 10899766Abstract: The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; -( ) m-is —(CH2)m— or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-in-farct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: September 28, 2017Date of Patent: January 26, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Jérôme Charles Sarie, Greta Vastakaite
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Patent number: 10875854Abstract: The present invention relates to compounds of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R2 is lower alkyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is R4 is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: December 18, 2018Date of Patent: December 29, 2020Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Rosa Maria Rodriguez Sarmiento
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Patent number: 10829500Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: GrantFiled: July 31, 2019Date of Patent: November 10, 2020Assignee: Hoffmann-La Roche Inc.Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Andreas Kuglstatter, Ulrike Obst Sander, Jens-Uwe Peters, Mark Rogers-Evans, Thomas Woltering, Christian Schnider, Roger Wermuth
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Publication number: 20200317681Abstract: The present invention relates to compounds of formula (I), wherein R is hydrogen or halogen, wherein R may be different if n=2 or 3; n is 1, 2 or 3; (II) is a disubstitued bicyclo[1,1,1]pentane or bicyclo[2,2,2]octane as defined below: (III) or (IV); or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: ApplicationFiled: December 17, 2018Publication date: October 8, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Xinlan Aloise Ford COOK, Hasane RATNI, Michael REUTLINGER, Walter VIFIAN
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Publication number: 20200308166Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: ApplicationFiled: June 17, 2020Publication date: October 1, 2020Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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Publication number: 20200291032Abstract: The invention provides new pyrimidine compounds having the general formula (I), wherein R1, R2, R3, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.Type: ApplicationFiled: November 26, 2018Publication date: September 17, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Xinlan Aloise Ford COOK, Hasane RATNI, Michael REUTLINGER, Walter VIFIAN
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Publication number: 20200291034Abstract: The present invention relates to a compound of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, —CH2—C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n=2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: February 13, 2020Publication date: September 17, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Hasane RATNI, Karlheinz BAUMANN, Guido GALLEY, Georg JAESCHKE, Roland JAKOB-ROETNE, Anja LIMBERG, Werner NEIDHART, Rosa Maria RODRIGUEZ-SARMIENTO
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Patent number: 10730881Abstract: The present invention relates to a compound of formula I wherein R1 is phenyl, lower alkyl, C3-6-cycloalkyl, —CH2—C3-6-cycloalkyl or bridged C4-6-cycloalkyl, substituted by one, two or three halogen atoms, or by lower alkyl or lower alkyl substituted by halogen; R2 is a five or six membered heteroaryl group, selected from wherein R6 is hydrogen, lower alkyl, halogen or lower alkoxy; and R7 is hydrogen, lower alkoxy or halogen; R3 is lower alkyl or lower alkyl substituted by hydroxy: R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; n is 1 or 2; -( )n- is —CH2— or —CH2CH2— for n being 1 or 2; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndromType: GrantFiled: January 10, 2019Date of Patent: August 4, 2020Assignee: HOFFMANN-LA ROCHE, INC.Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Sandra Steiner