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: 12209144Abstract: 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: GrantFiled: November 26, 2019Date of Patent: January 28, 2025Assignee: Novartis AGInventors: 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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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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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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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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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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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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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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Patent number: 8921307Abstract: The invention provides a synthetic polypeptide of Formula I? (SEQ ID NO: 1): X1-X2-X3-R—X5-X6-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, wherein X1, X2, X3, 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: November 18, 2013Date of Patent: December 30, 2014Assignee: Novartis AGInventors: Frédéric Zecri, Kayo Yasoshima, Philipp Grosche, Jun Yuan, Hongjuan Zhao
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Publication number: 20140155315Abstract: The invention provides a synthetic polypeptide of Formula I? (SEQ ID NO: 1): X1-X2-X3-R—X5-X6-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, wherein X1, X2, X3, 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: November 18, 2013Publication date: June 5, 2014Applicant: NOVARTIS AGInventors: Frédéric Zecri, Kayo Yasoshima, Philipp Grosche, Jun Yuan, Hongjuan Zhao
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Patent number: 8673848Abstract: 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: January 23, 2013Date of Patent: March 18, 2014Assignee: Novartis AGInventors: Frédéric Zecri, Andrei Golosov, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase, David Thomas Parker
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Patent number: 8178559Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.Type: GrantFiled: July 6, 2011Date of Patent: May 15, 2012Assignee: Novartis AGInventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen Klaus Maibaum, Keiichi Masuya, Atsuko Iwasaki, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
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Patent number: 8163773Abstract: The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1, R2, T, R3 and R4 are as defined in the specification.Type: GrantFiled: July 10, 2006Date of Patent: April 24, 2012Assignee: Novartis AGInventors: Werner Breitenstein, Claus Erhardt, Juergen Klaus Maibaum, Nils Ostermann, Juerg Zimmermann, Keiichi Masuya, Kazuhide Konishi, Fumiaki Yokokawa, Takanori Kanazawa, Edgar Jacoby, Andreas Marzinzik, Philipp Grosche, Shimpei Kawakami
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Patent number: 8129411Abstract: The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds have the formula I? wherein R1, R2, T, R3 and R4 are as defined in the specification.Type: GrantFiled: December 28, 2006Date of Patent: March 6, 2012Assignee: Novartis AGInventors: Takeru Ehara, Philipp Grosche, Osamu Irie, Yuki Iwaki, Takanori Kanazawa, Shimpei Kawakami, Kazuhide Konishi, Muneto Mogi, Masaki Suzuki, Fumiaki Yokokawa
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Patent number: 8084450Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.Type: GrantFiled: December 28, 2005Date of Patent: December 27, 2011Assignee: Novartis AGInventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen Klaus Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
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Publication number: 20100029609Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R5, R10 and X1-X7 are as defined in the specification.Type: ApplicationFiled: September 6, 2007Publication date: February 4, 2010Inventors: Frederic Berst, Philipp Grosche, Philipp Janser, Frederic Zecri, Birgit Bollbuck
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Publication number: 20090312304Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.Type: ApplicationFiled: December 28, 2005Publication date: December 17, 2009Inventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen K. Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
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Publication number: 20090233920Abstract: The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1, R2, T, R3 and R4 are as defined in the specification.Type: ApplicationFiled: July 10, 2006Publication date: September 17, 2009Inventors: Werner Breitenstein, Claus Erhardt, Juergen Klaus Maibaum, Nils Ostermann, Juerg Zimmermann, Keiichi Masuya, Kazuhide Konishi, Fumiaki Yokokawa, Takanori Kanazawa, Edgar Jacoby, Andreas Marzinzik, Philipp Grosche, Shimpei Kawakami