Patents by Inventor Philipp Grosche
Philipp Grosche 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: 11813306Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.Type: GrantFiled: March 12, 2021Date of Patent: November 14, 2023Assignee: Novartis AGInventors: Karin Briner, Brian Addison Dechristopher, Alec Nathanson Flyer, Andrei Alexandrovich Golosov, Philipp Grosche, Eugene Yuejin Liu, Justin Yik Ching Mao, Lauren Gilchrist Monovich, Tajesh Jayprakash Patel, Liansheng Su, Lihua Yang, Rui Zheng
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Publication number: 20230089867Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein X1, R1, R2, R3, R4, R5, R6, R6?, R7, R7?, R8, R9, R9?, R10, R11, R12, and n are described herein.Type: ApplicationFiled: November 26, 2019Publication date: March 23, 2023Inventors: Christopher BECKER, Brian Addison DECHRISTOPHER, Alec Nathanson FLYER, Adam FRIEDMAN, Christian GAMPE, Andrei Alexandrovich GOLOSOV, Philipp GROSCHE, Tyler HARRISON, Qian LIU, Eugene Yuejin LIU, I, Justin Yik Ching MAO, Lauren Gilchrist MONOVICH, Tajesh Jayprakash PATEL, Carina Cristina SANCHEZ, Liansheng SU, Lihua YANG, Rui ZHENG
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Publication number: 20220024981Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R1, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, and X13 are described herein.Type: ApplicationFiled: November 26, 2019Publication date: January 27, 2022Inventors: Alec Nathanson FLYER, Andrei Alexandrovich GOLOSOV, Philipp GROSCHE, Ian LEWIS, Eugene Yuejin LIU, Andreas MARZINZIK, Lauren Gilchrist MONOVICH, Johannes OTTL, Tajesh Jayprakash PATEL, Patrick Crawford REID, Mohindra SEEPERSAUD
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Publication number: 20210252103Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.Type: ApplicationFiled: March 12, 2021Publication date: August 19, 2021Inventors: Karin BRINER, Brian Addison DECHRISTOPHER, Alec Nathanson FLYER, Andrei Alexandrovich GOLOSOV, Philipp GROSCHE, Eugene Yuejin LIU, Justin Yik Ching MAO, Lauren Gilchrist MONOVICH, Tajesh Jayprakash PATEL, Liansheng SU, Lihua YANG, Rui ZHENG
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Patent number: 11026993Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.Type: GrantFiled: November 26, 2019Date of Patent: June 8, 2021Assignee: Novartis AGInventors: Karin Briner, Brian Addison Dechristopher, Alec Nathanson Flyer, Andrei Alexandrovich Golosov, Philipp Grosche, Eugene Yuejin Liu, Justin Yik Ching Mao, Lauren Gilchrist Monovich, Tajesh Jayprakash Patel, Carina Cristina Sanchez, Liansheng Su, Lihua Yang, Rui Zheng
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Publication number: 20200164024Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.Type: ApplicationFiled: November 26, 2019Publication date: May 28, 2020Inventors: Karin BRINER, Brian Addison DECHRISTOPHER, Alec Nathanson FLYER, Andrei Alexandrovich GOLOSOV, Philipp GROSCHE, Eugene Yuejin LIU, Justin Yik Ching MAO, Lauren Gilchrist MONOVICH, Tajesh Jayprakash PATEL, Carina Cristina SANCHEZ, Liansheng SU, Lihua YANG, Rui ZHENG
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Patent number: 10005829Abstract: The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.Type: GrantFiled: November 19, 2013Date of Patent: June 26, 2018Assignee: NOVARTIS AGInventors: Frederic Zecri, Kayo Yasoshima, Philipp Grosche, Jun Yuan, Hongjuan Zhao
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Patent number: 9982017Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: GrantFiled: May 18, 2015Date of Patent: May 29, 2018Assignee: NOVARTIS AGInventors: Frederic Zecri, Andrei Golosov, Philipp Grosche, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase
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Patent number: 9908919Abstract: The invention provides a synthetic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13??I or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor.Type: GrantFiled: July 21, 2014Date of Patent: March 6, 2018Assignee: NOVARTIS AGInventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan
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Publication number: 20170233443Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor.Type: ApplicationFiled: April 25, 2017Publication date: August 17, 2017Inventors: Alexandra Marshall BRUCE, Philipp GROSCHE, Carla GUIMARAES, Aaron KANTER, Changgang LOU, Aimee Richardson USERA, Kayo YASOSHIMA, Jun YUAN, Frederic Zecri, Hongjuan ZHAO
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Patent number: 9683018Abstract: The invention provides a synthetic polypeptide of Formula I?: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: GrantFiled: July 21, 2014Date of Patent: June 20, 2017Assignee: NOVARTIS AGInventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan
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Patent number: 9683019Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor.Type: GrantFiled: December 9, 2015Date of Patent: June 20, 2017Assignee: NOVARTIS AGInventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan, Aimee Richardson Usera, Changgang Lou, Aaron Kanter, Alexandra Marshall Bruce, Carla Guimaraes
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Publication number: 20160166634Abstract: The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I? (SEQ ID NO: 1): or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor.Type: ApplicationFiled: February 25, 2016Publication date: June 16, 2016Applicant: NOVARTIS AGInventors: Shari Lynn CAPLAN, Andrei GOLOSOV, Philipp GROSCHE, Carla GUIMARAES, Aaron KANTER, Changgang LOU, David Thomas PARKER, Eric C. Peters, Aimee Richardson USERA, Kayo YASOSHIMA, Jun YUAN, Federic ZECRI, Hongjuan ZHAO
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Publication number: 20160159871Abstract: The invention provides a synthetic polypeptide of Formula I?: X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: July 21, 2014Publication date: June 9, 2016Applicant: Novartis AGInventors: Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN
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Publication number: 20160145309Abstract: The invention provides a synthetic polypeptide of Formula I?: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: July 21, 2014Publication date: May 26, 2016Applicant: NOVARTIS AGInventors: Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN
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Patent number: 9340582Abstract: The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I? (SEQ ID NO: 1): or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor.Type: GrantFiled: July 21, 2014Date of Patent: May 17, 2016Assignee: NOVARTIS AGInventors: Jun Yuan, Frederic Zecri, Philipp Grosche, Hongjuan Zhao, Eric Peters, Shari Lynn Caplan, Changgang Lou
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Publication number: 20160108091Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor.Type: ApplicationFiled: December 9, 2015Publication date: April 21, 2016Applicant: NOVARTIS AGInventors: Frederic ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN, Aimee Richardson USERA, Changgang LOU, Aaron KANTER, Alexandra Marshall BRUCE, Carla GUIMARAES
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Patent number: 9266925Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor.Type: GrantFiled: July 21, 2014Date of Patent: February 23, 2016Assignee: NOVARTIS AGInventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan, Aimee Richardson Usera, Changgang Lou, Aaron Kanter, Alexandra Marshall Bruce, Carla Giumaraes
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Publication number: 20150284446Abstract: The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.Type: ApplicationFiled: November 19, 2013Publication date: October 8, 2015Applicant: NOVARTIS AGInventors: Frédéric ZECRI, Kayo YASOSHIMA, Philipp GROSCHE, Jun YUAN, Hongjuan ZHAO
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Publication number: 20150252076Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: May 18, 2015Publication date: September 10, 2015Applicant: NOVARTIS AGInventors: Frederic ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE