Patents by Inventor Rosa Maria Rodriguez-Sarmiento
Rosa Maria Rodriguez-Sarmiento 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: 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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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: 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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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: 10604517Abstract: The present invention relates to compounds of formula hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing —O—CH2—O—; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers 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: March 6, 2018Date of Patent: March 31, 2020Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Guido Galley, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Rosa Maria Rodriguez Sarmiento, Björn Bartels, Hasane Ratni
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Patent number: 10562903Abstract: 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: GrantFiled: June 8, 2018Date of Patent: February 18, 2020Assignee: 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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Publication number: 20190194183Abstract: 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: ApplicationFiled: December 18, 2018Publication date: June 27, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Bjoern BARTELS, Roland JAKOB-ROETNE, Anja LIMBERG, Werner NEIDHART, Hasane RATNI, Rosa Maria RODRIGUEZ SARMIENTO
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Publication number: 20190010156Abstract: 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: June 8, 2018Publication date: January 10, 2019Applicant: 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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Publication number: 20180237432Abstract: The present invention relates to compounds of formula hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing —O—CH2—O—; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers 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: ApplicationFiled: March 6, 2018Publication date: August 23, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Guido Galley, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Rosa Maria Rodriguez Sarmiento, Björn Bartels, Hasane Ratni
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Patent number: 9187455Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: GrantFiled: February 16, 2010Date of Patent: November 17, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
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Patent number: 8921397Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: April 27, 2012Date of Patent: December 30, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20140350051Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: July 24, 2014Publication date: November 27, 2014Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 8877778Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: December 7, 2011Date of Patent: November 4, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8829029Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: GrantFiled: February 21, 2013Date of Patent: September 9, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 8722683Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 10, 2012Date of Patent: May 13, 2014Assignee: Hoffmann LA-Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8703768Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: April 22, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
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Patent number: 8623866Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: January 7, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
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Patent number: 8598357Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: February 27, 2012Date of Patent: December 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8586579Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: GrantFiled: June 16, 2011Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8470820Abstract: The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: GrantFiled: January 13, 2011Date of Patent: June 25, 2013Assignee: Hoffman-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Eric Vieira