公开(公告)号：US20210000964A1

公开(公告)日：2021-01-07

申请号：US16889201

申请日：2020-06-01

Applicant: NOVARTIS AG

Inventor： David Weninger BARNES ,  Avirup BOSE ,  Alexandra Marshall BRUCE ,  Alokesh DUTTAROY ,  Chikwendu IBEBUNJO ,  Aaron KANTER ,  Louise Clare KIRMAN ,  Changgang LOU ,  Aimee Richardson USERA ,  Ken YAMADA ,  Jun YUAN ,  Frederic ZECRI

IPC: A61K47/54 ,  A61K38/095 ,  A61K38/08 ,  A61K38/16 ,  A61K38/17 ,  A61K38/18 ,  A61K38/22 ,  A61K45/06 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113

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：US20180326079A1

公开(公告)日：2018-11-15

申请号：US15985060

申请日：2018-05-21

Applicant: NOVARTIS AG

Inventor： David Weninger BARNES ,  Avirup BOSE ,  Alexandra Marshall BRUCE ,  Alokesh DUTTAROY ,  Chikwendu IBEBUNJO ,  Aaron KANTER ,  Louise Clare KIRMAN ,  Changgang LOU ,  Aimee Richardson USERA ,  Ken YAMADA ,  Jun YUAN ,  Frederic ZECRI

IPC: A61K47/54 ,  C07C55/02 ,  A61K38/08 ,  C12N15/113 ,  C07C59/245 ,  C07C57/18 ,  C07C57/02 ,  C07C55/22 ,  A61K45/06 ,  A61K38/22 ,  A61K38/18 ,  A61K38/17 ,  A61K38/16

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：US20150342951A1

公开(公告)日：2015-12-03

申请号：US14365512

申请日：2012-12-14

Applicant: NOVARTIS AG

Inventor： Nigel Graham COOKE ,  Paulo Antonio FERNANDES GOMES DOS SANTOS ,  Pascal FURET ,  Christina HEBACH ,  Klemens HOGENAUER ,  Gregory HOLLINGWORTH ,  Christoph KALIS ,  Ian LEWIS ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Frederic STAUFFER ,  Ross STRANG ,  Frank STOWASSER ,  Nicola TUFFILLI ,  Anette VON MATT ,  Romain WOLF ,  Frederic ZECRI

IPC: A61K31/519 ,  A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/517

CPC classification number: A61K31/519 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D239/74 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D487/08 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414

Abstract: The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.

Abstract translation: 本发明涉及PI3K抑制剂的新用途，其中所述抑制剂对PI3K同种型δ具有抑制作用，用于治疗患有选自疟疾，利什曼病，锥虫病，弓形虫病和/或神经囊尾erc病的疾病或病症的受试者的免疫病理学， 通过功能抑制受感染受试者的TLR9。

公开(公告)号：US20240066132A1

公开(公告)日：2024-02-29

申请号：US18352345

申请日：2023-07-14

Applicant: NOVARTIS AG

Inventor： David Weninger BARNES ,  Avirup BOSE ,  Alexandra Marshall BRUCE ,  Alokesh DUTTAROY ,  Chikwendu IBEBUNJO ,  Aaron KANTER ,  Louise Clare KIRMAN ,  Changgang LOU ,  Aimee Richardson USERA ,  Ken YAMADA ,  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 ,  A61K47/542 ,  A61K38/095 ,  A61K38/164 ,  A61K38/1709 ,  A61K38/1825 ,  A61K38/1841 ,  A61K38/2221 ,  A61K45/06 ,  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：US20210078936A1

公开(公告)日：2021-03-18

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 ,  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 ,  A61K47/18 ,  A61K9/127 ,  A61K9/51 ,  A61K31/7105 ,  A61K31/713 ,  A61K39/12 ,  A61K39/39 ,  C07C271/22 ,  C07D211/06 ,  C07D211/34 ,  C07D211/44

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：US20180002368A1

公开(公告)日：2018-01-04

申请号：US15536516

申请日：2015-12-16

Applicant: NOVARTIS AG

Inventor： David BARNES-SEEMAN ,  Scott Louis COHEN ,  John Louis DIENER ,  Christian GAMPE ,  James ROACHE ,  Amy WHITE ,  Sarah WILLIAMS ,  Jun YUAN ,  Frederic ZECRI

IPC: C07H21/02 ,  C07F9/6561 ,  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 arc disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.

公开(公告)号：US20130165436A1

公开(公告)日：2013-06-27

申请号：US13721805

申请日：2012-12-20

Applicant: Novartis AG

Inventor： Giorgio CARAVATTI ,  Sylvie CHAMOIN ,  Pascal FURET ,  Klemens HOGENAUER ,  Konstanze HURTH ,  Christoph KALIS ,  Karen KAMMERTOENS ,  Ian LEWIS ,  Henrik MOEBITZ ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Romain WOLF ,  Frederic ZECRI

IPC: A61K31/538 ,  C07D413/14

CPC classification number: A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 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.

Abstract translation: 本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。