公开(公告)号：US20210363254A1

公开(公告)日：2021-11-25

申请号：US16981828

申请日：2019-03-18

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Nelson GUERREIRO ,  Ensar HALILOVIC ,  Sebastien JEAY ,  Astrid JULLION ,  Jinsheng LIANG ,  Christophe MEILLE ,  Hui-Qin WANG ,  Jens WUERTHNER

IPC分类号： C07K16/28 ,  A61P35/00 ,  C07D487/04

摘要： The present invention relates to a pharmaceutical combination which comprises (a) at least one antibody molecule (e.g., humanized antibody molecules) that bind to Programmed Death 1 (PD-1), and (b) a HDM2-p53 interaction inhibitor, said combination for simultaneous, separate or sequential administration for use in the treatment of a proliferative disease, a pharmaceutical composition comprising such combination; a method of treating a subject having a proliferative disease comprising administration of said combination to a subject in need thereof; use of such combination for the treatment of proliferative disease; and a commercial package comprising such combination; said proliferative disease being a TP53 wildtype tumor, in particular TP53 wildtype renal cell carcinoma (RCC) or TP53 wildtype colorectal cancer (CRC).

公开(公告)号：US20220233530A9

公开(公告)日：2022-07-28

申请号：US16898886

申请日：2020-06-11

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K9/00 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20200281925A1

公开(公告)日：2020-09-10

申请号：US16494927

申请日：2018-03-29

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Nesol GURREIO ,  Senastien JEAY ,  Astrid JULLION ,  Christophe MEILLE ,  Jens WUERTHNER

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61K31/553 ,  A61K31/706 ,  A61K31/7068 ,  A61P35/00

摘要： The present invention relates to the HDM2-p53 interaction inhibitors (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one (HDM201), or a pharmaceutically acceptable non-covalent derivative thereof, for use in the treatment of patients with hematological tumors, wherein the drug is administered by an extended low dose dosing regimen.

公开(公告)号：US20240261284A1

公开(公告)日：2024-08-08

申请号：US18632528

申请日：2024-04-11

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K9/00 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

CPC分类号： A61K31/506 ,  A61K9/0019 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20210000824A1

公开(公告)日：2021-01-07

申请号：US16898886

申请日：2020-06-11

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K9/00 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20190209561A1

公开(公告)日：2019-07-11

申请号：US16221650

申请日：2018-12-17

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61K9/00 ,  A61K31/496 ,  A61K31/472 ,  A61K31/402 ,  A61K31/4439 ,  A61K31/4418 ,  A61K31/4178 ,  A61K31/404 ,  A61K31/47

CPC分类号： A61K31/506 ,  A61K9/0019 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20170196866A1

公开(公告)日：2017-07-13

申请号：US15321042

申请日：2015-06-25

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61K9/00

CPC分类号： A61K31/506 ,  A61K9/0019 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20240197715A1

公开(公告)日：2024-06-20

申请号：US18510836

申请日：2023-11-16

申请人： NOVARTIS AG

发明人： Rita ANDRAOS-REY ,  Sandra BLUM-KALLERT ,  Marta CORTES-CROS ,  Ruben DE KANTER ,  Stephane FERRETTI ,  Isabel Cristina Colaco Farias JACO ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Laurent LABORDE ,  Henrik MOEBITZ ,  Michele MOSCHETTA ,  Joseph SCHOEPFER ,  Ross Sinclair STRANG

IPC分类号： A61K31/4745 ,  A61K31/4535 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7048 ,  A61K33/243 ,  A61P35/00

CPC分类号： A61K31/4745 ,  A61K31/4535 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7048 ,  A61K33/243 ,  A61P35/00

摘要： The present invention provides a pharmaceutical combination comprising a WRN inhibitor in combination with at least one additional therapeutically active agent. It also provides a method of treating cancer, involving administering to a subject in need thereof the WRN inhibitor in combination with the at least one additional therapeutically active agent. For example, the WRN inhibitor compound, or a pharmaceutically acceptable salt thereof, is of formula (I):




wherein R1, R2, R3, R4, R5, R28, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein.

公开(公告)号：US20230092181A1

公开(公告)日：2023-03-23

申请号：US17814599

申请日：2022-07-25

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K9/00 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US20220031697A1

公开(公告)日：2022-02-03

申请号：US17401600

申请日：2021-08-13

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Nelson GUERREIRO ,  Sebastien JEAY ,  Astrid JULLION ,  Christophe MEILLE ,  Jens WUERTHNER ,  Claire Fabre

IPC分类号： A61K31/506 ,  A61P35/00 ,  A61K31/553 ,  A61K31/706 ,  A61K31/7068 ,  A61K45/06

摘要： The present invention relates to the HDM2-p53 interaction inhibitors (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one (HDM201), or a pharmaceutically acceptable non-covalent derivative thereof, for use in the treatment of patients with hematological tumors, wherein the drug is administered by an extended low dose dosing regimen.