Patents by Inventor Michael D. Sintchak
Michael D. Sintchak 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: 20230149549Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/or polybromo-1 (PB-1) protein via ubiqitination and/or degradation by compounds. The compounds are bifunctional molecules that link a cereblon-binding moiety to a ligand that binds SMARCA and/or PB1 proteins.Type: ApplicationFiled: June 10, 2020Publication date: May 18, 2023Inventors: Nan JI, Yi ZHANG, Michael D. SINTCHAK, Paul R. FLEMING
-
Publication number: 20230132715Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 17, 2020Publication date: May 4, 2023Inventors: Nan JI, Michael D. SINTCHAK, Yi ZHANG, Xiaozhang ZHENG
-
Publication number: 20230093080Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.Type: ApplicationFiled: July 15, 2020Publication date: March 23, 2023Inventors: Nan JI, Michael D. SINTCHAK, Yi ZHANG, Xiaozhang ZHENG
-
Publication number: 20220324880Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/or polybromo-1 (PB-1) protein via ubiqitination and/or degradation by compounds. The compounds are useful in treatment of cancer.Type: ApplicationFiled: June 10, 2020Publication date: October 13, 2022Inventors: Nan JI, Yi ZHANG, Michael D. SINTCHAK
-
Publication number: 20220281831Abstract: The present invention provides compounds, compositions thereof, and methods of using the same. The present invention also relates to compounds and methods useful for binding and modulating the activity of cereblon (CRBN), especially for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.Type: ApplicationFiled: July 15, 2020Publication date: September 8, 2022Inventors: Nan JI, Michael d. SINTCHAK, Li ZHANG, Xiaozhang ZHENG
-
Patent number: 10538533Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 1, 2017Date of Patent: January 21, 2020Assignee: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
-
Patent number: 10202373Abstract: The present invention provides a compound of formula I: wherein R1, X1, X2, R2, R3, R4, R5, n, and m are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 13, 2015Date of Patent: February 12, 2019Assignee: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, He Xu, Yingchun Ye
-
Publication number: 20180118762Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 1, 2017Publication date: May 3, 2018Inventors: Indu T. BHARATHAN, Chris BLACKBURN, Jeffrey P. CIAVARRI, Jouhara CHOUITAR, Courtney A. CULLIS, Natalie D'AMORE, Paul E. FLEMING, Kenneth M. GIGSTAD, Krista E. GIPSON, Mario GIRARD, Yongbo HU, Janice LEE, Gang LI, Mansoureh REZAEI, Michael D. SINTCHAK, Francois SOUCY, Stephen G. STROUD, Tricia J. VOS, Tzu-Tshin WONG, He XU, Tianlin XU, Yingchun YE
-
Patent number: 9802960Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 13, 2015Date of Patent: October 31, 2017Assignee: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
-
Patent number: 9751854Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: November 9, 2016Date of Patent: September 5, 2017Assignee: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
-
Publication number: 20170107579Abstract: The invention provides isolated nucleic acids molecules, designated UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, which encode novel E1 enzyme variant proteins. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a UBA3, UAE, or UBA6, or other E1 enzyme variant gene has been introduced or disrupted. The invention still further provides isolated UBA3, UAE, or UBA6, or other E1 enzyme variant proteins, fusion proteins, antigenic peptides and anti-UBA3, UAE, or UBA6, or other E1 enzyme variant antibodies. The invention provides methods to identify agents that inhibit UBA3, UAE, or UBA6, or other E1 enzyme variant expression or activity. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.Type: ApplicationFiled: June 1, 2016Publication date: April 20, 2017Inventors: Benjamin Stone AMIDON, James E. BROWNELL, James M. GAVIN, Erik M. KOENIG, Michael D. SINTCHAK, Peter G. SMITH
-
Publication number: 20170073326Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: November 9, 2016Publication date: March 16, 2017Inventors: Indu T. BHARATHAN, Chris BLACKBURN, Jeffrey P. CIAVARRI, Jouhara CHOUITAR, Courtney A. CULLIS, Natalie D'AMORE, Paul E. FLEMING, Kenneth M. GIGSTAD, Krista E. GIPSON, Mario GIRARD, Yongbo HU, Janice LEE, Gang LI, Mansoureh REZAEI, Michael D. SINTCHAK, Francois SOUCY, Stephen G. STROUD, Tricia J. VOS, Tzu-Tshin WONG, He XU, Tianlin XU, Yingchun YE
-
Publication number: 20160333007Abstract: The present invention provides a compound of formula I: wherein R1, X1, X2, R2, R3, R4, R5, n, and m are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 13, 2015Publication date: November 17, 2016Inventors: INDU T. BHARATHAN, Chris BLACKBURN, Jeffrey P. CIAVARRI, Jouhara CHOUITAR, Courtney A. CILLIS, Natalie D'AMORE, Paul E. FLE,OMG, Kenneth M. GIGSTAD, Kirsta E. GIPSON, Mario GIRARD, Yongbo HU, Janice LEE, Gang LI, Mansoureh REZAEI, Michael D. SINTCHAK, Francois SOUCY, Stephen g. STROUD, Tricia J. VOS, He XU, Yingchun YE
-
Publication number: 20150225422Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 13, 2015Publication date: August 13, 2015Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
-
Publication number: 20150030601Abstract: The invention provides isolated nucleic acids molecules, designated UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, which encode novel E1 enzyme variant proteins. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a UBA3, UAE, or UBA6, or other E1 enzyme variant gene has been introduced or disrupted. The invention still further provides isolated UBA3, UAE, or UBA6, or other E1 enzyme variant proteins, fusion proteins, antigenic peptides and anti-UBA3, UAE, or UBA6, or other E1 enzyme variant antibodies. The invention provides methods to identify agents that inhibit UBA3, UAE, or UBA6, or other E1 enzyme variant expression or activity. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.Type: ApplicationFiled: October 5, 2012Publication date: January 29, 2015Applicant: Millennium Pharmaceuticals, Inc.Inventors: Benjamin Stone Amidon, James E. Brownell, James M. Gavin, Erik M. Koenig, Michael D. Sintchak, Peter G. Smith
-
Patent number: 7527952Abstract: The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.Type: GrantFiled: December 21, 2006Date of Patent: May 5, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Keith P. Wilson, Michael D. Sintchak, Mark Andrew Fleming, David M. Armistead
-
Patent number: 7216041Abstract: The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.Type: GrantFiled: October 2, 2000Date of Patent: May 8, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Keith P. Wilson, Michael D. Sintchak, Mark Andrew Fleming, David M. Armistead
-
Patent number: 7065452Abstract: The present invention relates to crystallized molecules and molecular complexes which comprise the active site binding pocket or the FKBP12/FK506 binding pocket of calcineurin or close structural homologues to either binding pocket. This invention also relates to a data storage material encoded with the corresponding structure coordinates of those crystallized molecules or molecular complexes. Such data storage material is capable of displaying such molecules and molecular complexes as a graphical three-dimensional representation on a computer screen. In addition, this invention relates to methods of using the structure coordinates of those molecules or molecular complexes to solve the structure of homologous proteins. This invention also relates to methods of using the structure coordinates to screen and design compounds that bind to calcineurin or homologues thereof.Type: GrantFiled: November 1, 1999Date of Patent: June 20, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Matthew James Fitzgibbon, Mark Andrew Fleming, James P. Griffith, Eunice E. Kim, Joseph L. Kim, Michael D. Sintchak, John Allan Thomson, Keith P. Wilson
-
Patent number: 6128582Abstract: The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.Type: GrantFiled: April 30, 1996Date of Patent: October 3, 2000Assignee: Vertex Pharmaceuticals IncorporatedInventors: Keith P. Wilson, Michael D. Sintchak, Mark Andrew Fleming, David M. Armistead
-
Patent number: 5978740Abstract: The present invention relates to crystallized molecules and molecular complexes which comprise the active site binding pocket or the FKBP12/FK506 binding pocket of calcineurin or close structural homologues to either binding pocket. This invention also relates to a data storage material encoded with the corresponding structure coordinates of those crystallized molecules or molecular complexes. Such data storage material is capable of displaying such molecules and molecular complexes as a graphical three-dimensional representation on a computer screen. In addition, this invention relates to methods of using the structure coordinates of those molecules or molecular complexes to solve the structure of homologous proteins. This invention also relates to methods of using the structure coordinates to screen and design compounds that bind to calcineurin or homologues thereof.Type: GrantFiled: August 9, 1995Date of Patent: November 2, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Matthew James Fitzgibbon, Mark Andrew Fleming, James P. Griffith, Eunice E. Kim, Joseph L. Kim, Michael D. Sintchak, John Allan Thomson, Keith P. Wilson