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).

  • Publication number: 20220024981
    Abstract: 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: Application
    Filed: November 26, 2019
    Publication date: January 27, 2022
    Inventors: 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
  • Publication number: 20210252103
    Abstract: 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: Application
    Filed: March 12, 2021
    Publication date: August 19, 2021
    Inventors: 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
  • Patent number: 11026993
    Abstract: 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: Grant
    Filed: November 26, 2019
    Date of Patent: June 8, 2021
    Assignee: Novartis AG
    Inventors: 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
  • Publication number: 20200164024
    Abstract: 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: Application
    Filed: November 26, 2019
    Publication date: May 28, 2020
    Inventors: 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
  • Patent number: 10005829
    Abstract: 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: Grant
    Filed: November 19, 2013
    Date of Patent: June 26, 2018
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Kayo Yasoshima, Philipp Grosche, Jun Yuan, Hongjuan Zhao
  • Patent number: 9982017
    Abstract: 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: Grant
    Filed: May 18, 2015
    Date of Patent: May 29, 2018
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Andrei Golosov, Philipp Grosche, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase
  • Patent number: 9908919
    Abstract: 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: Grant
    Filed: July 21, 2014
    Date of Patent: March 6, 2018
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan
  • Publication number: 20170233443
    Abstract: 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: Application
    Filed: April 25, 2017
    Publication date: August 17, 2017
    Inventors: Alexandra Marshall BRUCE, Philipp GROSCHE, Carla GUIMARAES, Aaron KANTER, Changgang LOU, Aimee Richardson USERA, Kayo YASOSHIMA, Jun YUAN, Frederic Zecri, Hongjuan ZHAO
  • Patent number: 9683018
    Abstract: 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: Grant
    Filed: July 21, 2014
    Date of Patent: June 20, 2017
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan
  • Patent number: 9683019
    Abstract: 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: Grant
    Filed: December 9, 2015
    Date of Patent: June 20, 2017
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan, Aimee Richardson Usera, Changgang Lou, Aaron Kanter, Alexandra Marshall Bruce, Carla Guimaraes
  • Publication number: 20160166634
    Abstract: 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: Application
    Filed: February 25, 2016
    Publication date: June 16, 2016
    Applicant: NOVARTIS AG
    Inventors: 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
  • Publication number: 20160159871
    Abstract: 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: Application
    Filed: July 21, 2014
    Publication date: June 9, 2016
    Applicant: Novartis AG
    Inventors: Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN
  • Publication number: 20160145309
    Abstract: 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: Application
    Filed: July 21, 2014
    Publication date: May 26, 2016
    Applicant: NOVARTIS AG
    Inventors: Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN
  • Patent number: 9340582
    Abstract: 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: Grant
    Filed: July 21, 2014
    Date of Patent: May 17, 2016
    Assignee: NOVARTIS AG
    Inventors: Jun Yuan, Frederic Zecri, Philipp Grosche, Hongjuan Zhao, Eric Peters, Shari Lynn Caplan, Changgang Lou
  • Publication number: 20160108091
    Abstract: 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: Application
    Filed: December 9, 2015
    Publication date: April 21, 2016
    Applicant: NOVARTIS AG
    Inventors: Frederic ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN, Aimee Richardson USERA, Changgang LOU, Aaron KANTER, Alexandra Marshall BRUCE, Carla GUIMARAES
  • Patent number: 9266925
    Abstract: 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: Grant
    Filed: July 21, 2014
    Date of Patent: February 23, 2016
    Assignee: NOVARTIS AG
    Inventors: Frederic Zecri, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Jun Yuan, Aimee Richardson Usera, Changgang Lou, Aaron Kanter, Alexandra Marshall Bruce, Carla Giumaraes
  • Publication number: 20150284446
    Abstract: 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: Application
    Filed: November 19, 2013
    Publication date: October 8, 2015
    Applicant: NOVARTIS AG
    Inventors: Frédéric ZECRI, Kayo YASOSHIMA, Philipp GROSCHE, Jun YUAN, Hongjuan ZHAO
  • Publication number: 20150252076
    Abstract: 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: Application
    Filed: May 18, 2015
    Publication date: September 10, 2015
    Applicant: NOVARTIS AG
    Inventors: Frederic ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE
  • Publication number: 20150030594
    Abstract: 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: Application
    Filed: July 21, 2014
    Publication date: January 29, 2015
    Applicant: NOVARTIS AG
    Inventors: Jun YUAN, Frederic ZECRI, Philipp GROSCHE, Hongjuan ZHAO, Andrei GOLOSOV, Kayo YASOSHIMA, David Thomas PARKER, Eric PETERS, Aimee Richardson USERA, Shari Lynn CAPLAN, Aaron KANTER, Changgang LOU, Carla Guimaraes
  • Publication number: 20150031604
    Abstract: 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: Application
    Filed: July 21, 2014
    Publication date: January 29, 2015
    Applicant: NOVARTIS AG
    Inventors: Frederic ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun Yuan, Aimee Richardson USERA, Changgang LOU, Aaron KANTER, Alexandra Marshall BRUCE, Carla Giumaraes