公开(公告)号：US20180290965A1

公开(公告)日：2018-10-11

申请号：US16013048

申请日：2018-06-20

Applicant: Novartis AG

Inventor： Luis Brito ,  Delai Chen ,  Gabriel Grant Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC: C07C229/12 ,  C07D211/44 ,  A61K39/39 ,  C07C271/22 ,  C07D211/06 ,  A61K31/713 ,  A61K31/7105 ,  A61K9/51 ,  A61K9/127 ,  A61K47/18 ,  C07C219/04 ,  C07C271/20 ,  C07D295/15 ,  C07D211/62 ,  C07D211/60 ,  C07D211/46 ,  C07D295/088 ,  C07D211/22 ,  C07D207/16 ,  C07D207/12 ,  C07D265/30 ,  C07D205/04 ,  C07C229/38 ,  C07D211/34

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US20170233443A1

公开(公告)日：2017-08-17

申请号：US15497135

申请日：2017-04-25

Applicant: NOVARTIS AG

Inventor： Alexandra Marshall BRUCE ,  Philipp GROSCHE ,  Carla GUIMARAES ,  Aaron KANTER ,  Changgang LOU ,  Aimee Richardson USERA ,  Kayo YASOSHIMA ,  Jun YUAN ,  Frederic Zecri ,  Hongjuan ZHAO

IPC: C07K14/47 ,  A61K45/06 ,  A61K38/17

CPC classification number: C07K14/47 ,  A61K38/12 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/542 ,  A61K47/60 ,  A61K47/643 ,  A61K47/6811 ,  C07K7/64 ,  C07K14/765 ,  C07K16/461 ,  C07K2319/30 ,  C07K2319/31

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. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their 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. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US09982017B2

公开(公告)日：2018-05-29

申请号：US14714914

申请日：2015-05-18

Applicant: Novartis AG

Inventor： Frederic Zecri ,  Andrei Golosov ,  Philipp Grosche ,  Hongjuan Zhao ,  Qi-Ying Hu ,  Hidetomo Imase

IPC: A61K38/10 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60 ,  A61K38/00

CPC classification number: A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

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. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20230183286A1

公开(公告)日：2023-06-15

申请号：US17820005

申请日：2022-08-16

Applicant: NOVARTIS AG

Inventor： David BARNES-SEEMAN ,  Scott Louis COHEN ,  John Louis DIENER ,  Christian GAMPE ,  James ROACHE ,  Amy White ,  Sarah Louise Williams ,  Jun Yuan ,  Frederic Zecri

IPC: C07H21/02 ,  C07F9/6561 ,  C07H19/167 ,  C07H19/207 ,  C07K14/575

CPC classification number: C07H21/02 ,  C07F9/65616 ,  C07H19/167 ,  C07H19/207 ,  C07K14/5759

Abstract: The disclosure relates to nucleic acids that contain modifications at the 5′-end, 3′-end or 5′-end and 3′-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.

公开(公告)号：US11466048B2

公开(公告)日：2022-10-11

申请号：US16802014

申请日：2020-02-26

Applicant: NOVARTIS AG

Inventor： David Barnes-Seeman ,  Scott Louis Cohen ,  John Louis Diener ,  Christian Gampe ,  James Roache ,  Amy White ,  Sarah Louise Williams ,  Jun Yuan ,  Frederic Zecri

IPC: C07H21/02 ,  C07F9/6561 ,  C07H19/167 ,  C07H19/207 ,  C07K14/575

Abstract: The disclosure relates to nucleic acids that contain modifications at the 5′-end, 3′-end or 5′-end and 3′-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.

公开(公告)号：US11420933B2

公开(公告)日：2022-08-23

申请号：US17104294

申请日：2020-11-25

Applicant: Novartis AG

Inventor： Luis Brito ,  Delai Chen ,  Gabriel Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC: C07C229/12 ,  A61K47/18 ,  C07C229/38 ,  C07D205/04 ,  C07D265/30 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D295/088 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D295/15 ,  C07C271/20 ,  C07C219/04 ,  A61K9/127 ,  A61K9/51 ,  A61K31/7105 ,  A61K31/713 ,  A61K39/12 ,  A61K39/39 ,  C07C271/22 ,  C07D211/06 ,  C07D211/34 ,  C07D211/44 ,  A61K39/00

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US10005829B2

公开(公告)日：2018-06-26

申请号：US14440198

申请日：2013-11-19

Applicant: Novartis AG

Inventor： Frederic Zecri ,  Kayo Yasoshima ,  Philipp Grosche ,  Jun Yuan ,  Hongjuan Zhao

IPC: A61K38/10 ,  C07K14/765 ,  C07K14/47 ,  A61K45/06 ,  A61K38/38

CPC classification number: C07K14/765 ,  A61K38/385 ,  A61K45/06 ,  C07K14/47 ,  A61K38/1709 ,  A61K2300/00

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.

公开(公告)号：US11752211B2

公开(公告)日：2023-09-12

申请号：US16889201

申请日：2020-06-01

Applicant: NOVARTIS AG

Inventor： Alexandra Marshall Bruce ,  Aaron Kanter ,  Aimee Richardson Usera ,  Jun Yuan ,  Frederic Zecri

IPC: A61K47/54 ,  A61K38/095 ,  A61K38/16 ,  A61K38/17 ,  A61K38/18 ,  A61K38/22 ,  A61K45/06 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113

CPC classification number: A61K47/543 ,  A61K38/095 ,  A61K38/164 ,  A61K38/1709 ,  A61K38/1825 ,  A61K38/1841 ,  A61K38/2221 ,  A61K45/06 ,  A61K47/542 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/351

Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:






wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20220267318A1

公开(公告)日：2022-08-25

申请号：US17399090

申请日：2021-08-11

Applicant: Novartis AG

Inventor： Nigel Graham Cooke ,  Paulo Fernandes Gomes Dos Santos ,  Nadege Graveleau ,  Christina Hebach ,  Klemens Hoegenauer ,  Gregory John Hollingworth ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Frank Stowasser ,  Ross Sinclair Strang ,  Nicola Tufilli ,  Anette von Matt ,  Romain Wolf ,  Frederic Zecri

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/519 ,  A61K31/5377

Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

公开(公告)号：US11013696B2

公开(公告)日：2021-05-25

申请号：US16537934

申请日：2019-08-12

Applicant: Novartis AG

Inventor： Luis Brito ,  Delai Chen ,  Gabriel Grant Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC: C07D319/06 ,  C07C219/06 ,  C07C229/12 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D211/62 ,  C07C323/52 ,  A61K31/7105 ,  A61K31/713 ,  C07C219/16 ,  C07D233/60 ,  C07D295/088 ,  C12N15/88 ,  A61K9/51 ,  A61K9/127 ,  A61K47/18 ,  A61K38/18 ,  A61K38/22 ,  A61K39/12 ,  C07C235/08 ,  C07D211/06 ,  C07D211/46 ,  C07D233/64 ,  C07D295/13 ,  C12N7/00 ,  C12N15/113 ,  A61K39/00

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.