公开(公告)号：US20210155606A1

公开(公告)日：2021-05-27

申请号：US17170690

申请日：2021-02-08

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D405/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (1) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

公开(公告)号：US20250101006A1

公开(公告)日：2025-03-27

申请号：US18834099

申请日：2023-01-30

Applicant: NOVARTIS AG

Inventor： Markus BAENZIGER ,  Fabrice GALLOU ,  Fengfeng GUO ,  Rudolf HÄNGGI ,  Enjian HAN ,  Guido JORDINE ,  Jialiang LI ,  Weipeng LIU ,  Bukeyan MIAO ,  Shaofeng RONG ,  Ernesto SANTANDREA ,  Paul Bernd SCHIRNER ,  Xiaodong SHEN ,  Can WANG ,  Hao ZHANG

IPC: C07D403/14 ,  B01J31/22 ,  B01J31/24

Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.

公开(公告)号：US20210299100A1

公开(公告)日：2021-09-30

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Cara BROCKLEHURST ,  Patrick CHENE ,  Zhongbo FEI ,  Pascal FURET ,  Vito GUAGNANO ,  Patricia IMBACH-WEESE ,  Joerg KALLEN ,  Mickael LE DOUGET ,  Jialiang LI ,  Wei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Joseph McKENNA ,  Bahaa SALEM ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K31/4155 ,  C07D307/81 ,  C07D405/12 ,  A61K31/343 ,  A61K31/443 ,  A61K31/426 ,  C07D417/04 ,  C07D407/04 ,  A61K31/357 ,  C07D405/04 ,  A61K31/403 ,  A61K31/4525 ,  A61K31/351 ,  C07D407/12 ,  A61K31/506 ,  A61K31/41 ,  A61K31/4025 ,  A61K31/4439 ,  C07D405/14 ,  A61P35/00

Abstract: The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US20200299265A1

公开(公告)日：2020-09-24

申请号：US16884666

申请日：2020-05-27

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D405/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

公开(公告)号：US20190161474A1

公开(公告)日：2019-05-30

申请号：US16318250

申请日：2017-07-18

Applicant: NOVARTIS AG

Inventor： Luca ARISTA ,  Sreehari BABU ,  Jianwei BIAN ,  Kai CUI ,  Michael Patrick DILLON ,  Rene LATTMANN ,  Jialiang LI ,  Lv LIAO ,  Dimitrios LIZOS ,  Rita RAMOS ,  Nikolaus Johannes STIEFL ,  Thomas ULLRICH ,  Peggy USSELMANN ,  Xiaoyang WANG ,  Liladhar Murlidhar WAYKOLE ,  Sven WEILER ,  Yubo ZHANG ,  Yizong ZHOU ,  Tingying ZHU

IPC: C07D401/14 ,  C07D401/10 ,  C07D401/12 ,  C07D491/20 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  A61P19/08

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.