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1. 发明申请

WO2018014829A1 AMINOPYRIDINE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS 审中-公开
标题翻译：氨基吡啶衍生物及其作为选择性ALK-2抑制剂的用途
公开(公告)号：WO2018014829A1
公开(公告)日：2018-01-25
申请号：PCT/CN2017/093385
申请日：2017-07-18
申请人： NOVARTIS AG
发明人： LI, Jialiang , ARISTA, Luca , BABU, Sreehari , BIAN, Jianwei , CUI, Kai , DILLON, Michael Patrick , LATTMANN, Rene , LIAO, Lv , LIZOS, Dimitrios , RAMOS, Rita , STIEFL, Nikolaus Johannes , ULLRICH, Thomas , USSELMANN, Peggy , WANG, Xiaoyang , WAYKOLE, Liladhar Murlidhar , WEILER, Sven , ZHANG, Yubo , ZHOU, Yizong , ZHU, Tingying
IPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/00 , C07D417/00 , C07D419/00 , A61K31/4427 , A61P19/00
摘要： 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.
摘要翻译：本发明涉及游离形式或药学上可接受的盐形式的式（I）化合物，涉及包含所述化合物的药物组合物以及涉及所述化合物在治疗异位骨化中的用途和纤维发育不良进行性骨化。

2. 发明申请

WO2015140709A1 SOLID PHARMACEUTICAL DOSAGE FORMS 审中-公开
标题翻译：固体药物剂型
公开(公告)号：WO2015140709A1
公开(公告)日：2015-09-24
申请号：PCT/IB2015/051944
申请日：2015-03-17
申请人： NOVARTIS AG , DEODHAR, Unmesh , ZHANG, Lei , BABU, Sreehari
发明人： DEODHAR, Unmesh , ZHANG, Lei , BABU, Sreehari
IPC分类号： A61K9/20 , A61K31/135 , A61K31/352
CPC分类号： A61K31/357 , A61K9/2077 , A61K31/137 , A61K31/366 , A61K45/06 , Y02A50/411 , A61K2300/00
摘要： The present invention relates to the use of active pharmaceutical ingredients (API) as lubricant and/or antiadherent in the manufacturing of solid pharmaceutical dosage forms. It further relates to solid pharmaceutical dosage forms the production of which involves a granulation process step followed by a capsule filling or tablet compression step. Said pharmaceutical dosage form is comprised of an intragranular phase and an extragranular phase wherein the latter is comprised of one or more active pharmaceutical ingredients (API) which functions as lubricants and/or antiadherents in the manufacturing of said solid dosage form. Specifically, the API Artemether with its endoperoxide structural element was surprisingly found to exhibit lubricant and/or antiadherent effects when used extragranularly. In further aspects, the present invention relates to the manufacturing process to produce said pharmaceutical dosage forms as well as to a test method to determine whether an API functions as lubricant and/or antiadherent.
摘要翻译：本发明涉及在制备固体药物剂型中使用活性药物成分（API）作为润滑剂和/或抗粘附剂。它还涉及固体药物剂型，其生产包括造粒工艺步骤，随后是胶囊填充或片剂压片步骤。所述药物剂型由晶内相和颗粒外晶相组成，其中后者由制备所述固体剂型的一种或多种活性药物成分（API）组成，其作为润滑剂和/或抗粘附剂起作用。具体地说，具有其内过氧化物结构元件的API蒿甲醚被惊奇地发现在粒子外使用时表现出润滑剂和/或抗附着效应。在其它方面，本发明涉及生产所述药物剂型的制备方法以及用于确定API是否用作润滑剂和/或抗粘附剂的测试方法。

3. 发明公开

EP4442317A2 AMINOPYRIDINE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS 审中-公开
公开(公告)号：EP4442317A2
公开(公告)日：2024-10-09
申请号：EP24183394.6
申请日：2017-07-18
申请人： Novartis AG
发明人： LI, Jialiang , ARISTA, Luca , BABU, Sreehari , BIAN, Jianwei , CUI, Kai , DILLON, Michael Patrick , LATTMANN, Rene , LIAO, Lv , RAMOS, Rita , STIEFL, Nikolaus Johannes , ULLRICH, Thomas , USSELMANN, Peggy , WANG, Xiaoyang , WAYKOLE, Liladhar Murlidhar , WEILER, Sven , ZHANG, Yubo , ZHOU, Yizong , ZHU, Tingying , LIZOS, Dimitrios
IPC分类号： A61P19/00
CPC分类号： C07D405/14 , C07D401/10 , A61P19/00 , C07D213/82 , C07D491/107 , C07D401/14 , A61P19/08 , C07D413/10 , C07D413/12 , C07D413/14 , C07D491/20 , Y02A50/30
摘要： 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.

4. 发明公开

EP3971177A1 AMINOPYRIDINE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS 有权
公开(公告)号：EP3971177A1
公开(公告)日：2022-03-23
申请号：EP21202619.9
申请日：2017-07-18
申请人： Novartis AG
发明人： LI, Jialiang , ARISTA, Luca , BABU, Sreehari , BIAN, Jianwei , CUI, Kai , DILLON, Michael Patrick , LATTMANN, Rene , LIAO, Lv , RAMOS, Rita , STIEFL, Nikolaus Johannes , ULLRICH, Thomas , USSELMANN, Peggy , WANG, Xiaoyang , WAYKOLE, Liladhar Murlidhar , WEILER, Sven , ZHANG, Yubo , ZHOU, Yizong , ZHU, Tingying , LIZOS, Dimitrios
IPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/00 , C07D417/00 , C07D419/00 , A61K31/4427 , A61P19/00
摘要： 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.

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