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1. 发明申请

WO2013066483A1 SYNERGISTIC COMBINATIONS OF PI3K- AND MEK-INHIBITORS 审中-公开
标题翻译： PI3K和MEK-INHIBITORS的协同组合
公开(公告)号：WO2013066483A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/052955
申请日：2012-08-30
申请人： NOVARTIS AG , FRITSCH, Christine , HUANG, Xizhong , BOEHM, Markus , DI TOMASO, Emmanuelle , COSAERT, Jan GCE
发明人： FRITSCH, Christine , HUANG, Xizhong , BOEHM, Markus , DI TOMASO, Emmanuelle , COSAERT, Jan GCE
IPC分类号： A61K31/4184 , A61K31/4412 , A61K31/4439 , A61K45/06 , A61P35/00 , A61P43/00
CPC分类号： A61K31/4439 , A61K31/4184 , A61K31/4412 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical combination comprising (a) the phosphatidylinositol 3-kinase (PI3K) inhibitor compound (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) or a pharmaceutically acceptable salt thereof, and (b) at least one mitogen activated protein kinase (MEK) inhibitor or a pharmaceutically acceptable salt, and optionally at least one pharmaceutically acceptable carrier, for simultaneous, separate or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
摘要翻译：一种药物组合，其包含（a）磷脂酰肌醇3-激酶（PI3K）抑制剂化合物（S） - 吡咯烷-1,2-二羧酸2-酰胺1 - （{4-甲基-5- [2- 2-三氟-1,1-二甲基 - 乙基） - 吡啶-4-基] - 噻唑-2-基} - 酰胺）或其药学上可接受的盐，和（b）至少一种丝裂原活化蛋白激酶（MEK）抑制剂或药学上可接受的盐，以及任选的至少一种药学上可接受的载体，用于同时，分开或顺序施用; 这种组合在增殖性疾病治疗中的应用; 以及治疗患有增殖性疾病的受试者的方法，包括施用治疗有效量的这种组合。

2. 发明申请

WO2014203152A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2014203152A1
公开(公告)日：2014-12-24
申请号：PCT/IB2014/062271
申请日：2014-06-16
申请人： NOVARTIS AG , HIRAWAT, Samit , DI TOMASO, Emmanuelle
发明人： HIRAWAT, Samit , DI TOMASO, Emmanuelle
IPC分类号： A61K31/444 , A61K31/4745 , A61K31/506 , A61K45/06
CPC分类号： A61K31/506 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4745 , A61K31/5377 , A61K2300/00
摘要： A pharmaceutical combination comprising: (a) a phosphatidylinositol-3-kinase inhibitor selected from 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]- propionitrile, 5-(2,6-di-morpholin-4-yl-pyrimidin-4-yl)-4-trifluoromethyl-pyridin-2-ylamine, (S)- Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4- yl]-thiazol-2-yl}-amide) or any pharmaceutically acceptable salt thereof, and (b) an anaplastic lymphoma kinase inhibitor, particularly for use in the treatment or prevention of a proliferative disease; uses of such a combination in the treatment or prevention of proliferative diseases; to pharmaceutical compositions of the combination of said therapeutic agents and methods of treating a proliferative disease in a subject comprising administering to said subject a therapeutically effective amount of such a combination.
摘要翻译：一种药物组合，其包含：（a）磷脂酰肌醇-3-激酶抑制剂，其选自2-甲基-2- [4-（3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢咪唑并[ [4,5-c]喹啉-1-基） - 苯基] - 丙腈，5-（2,6-二吗啉-4-基 - 嘧啶-4-基）-4-三氟甲基 - 吡啶-2-基胺，（S） - 吡咯烷-1,2-二羧酸2-酰胺1 - （{4-甲基-5- [2-（2,2,2-三氟-1,1-二甲基 - 乙基） - 吡啶-4 噻唑-2-基} - 酰胺）或其任何药学上可接受的盐，和（b）间变性淋巴瘤激酶抑制剂，特别是用于治疗或预防增殖性疾病; 在治疗或预防增殖性疾病中使用这种组合; 涉及所述治疗剂的组合的药物组合物和治疗受试者中增殖性疾病的方法，包括向所述受试者施用治疗有效量的这种组合。

3. 发明申请

WO2015083101A1 DOSAGE REGIMEN FOR AN ALPHA-ISOFORM SELECTIVE PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR 审中-公开
标题翻译：用于ALPHA-ISOFORM选择性磷脂酰肌醇3激酶抑制剂的剂量
公开(公告)号：WO2015083101A1
公开(公告)日：2015-06-11
申请号：PCT/IB2014/066558
申请日：2014-12-03
申请人： NOVARTIS AG , DI TOMASO, Emmanuelle , GERMA, Marie-Caroline , MASSACESI, Cristian , FRITSCH, Christine , SCHNELL, Christian Rene , TAVORATH, Ranjana
发明人： DI TOMASO, Emmanuelle , GERMA, Marie-Caroline , MASSACESI, Cristian , FRITSCH, Christine , SCHNELL, Christian Rene , TAVORATH, Ranjana
IPC分类号： A61K31/4439 , A61P35/00
CPC分类号： A61K31/4439 , A61K9/0053
摘要： The present invention relates to an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof for use in methods of treating or preventing a proliferative disease in a patient in need thereof by orally administering a therapeutically effective amount of said compound for at least two five-consecutive day cycles, wherein said compound is not administered to the patient for a period of about two days to about three days between said five-consecutive day cycles.
摘要翻译：本发明涉及式（I）的α-同种型选择性磷脂酰肌醇3-激酶抑制剂化合物或其药学上可接受的盐，用于通过口服施用治疗有效的方法治疗或预防有需要的患者中的增殖性疾病的方法所述化合物的量至少两个连续5天的周期，其中所述化合物在所述五个连续的日期循环之间不向患者施用约两天至约三天的时间。

4. 发明申请

WO2015022657A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2015022657A1
公开(公告)日：2015-02-19
申请号：PCT/IB2014/063903
申请日：2014-08-13
申请人： NOVARTIS AG , HIRAWAT, Samit , MASSACESI, Cristian , DI TOMASO, Emmanuelle , TRANDAFIR, Lucia , VINCENT, Ghislaine
发明人： HIRAWAT, Samit , MASSACESI, Cristian , DI TOMASO, Emmanuelle , TRANDAFIR, Lucia , VINCENT, Ghislaine
IPC分类号： A61P35/00 , A61K31/175 , A61K31/506 , A61K31/5377
CPC分类号： A61K31/175 , A61K31/5377 , A61K2300/00
摘要： A pharmaceutical combination comprising (a) a phosphatidylinositol-3-kinase (PI3K) inhibitor compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof and (b) lomustine or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use, for the treatment of a brain tumor, particularly glioblastoma multiforme; a pharmaceutical composition comprising said combination; the use of said combination for the preparation of a medicament for the treatment of a brain tumor; a method of treating or preventing a brain tumor comprising administering a jointly therapeutically effective amount of such a combination to a subject in need thereof; and a commercial package thereof.
摘要翻译：一种药物组合，其包含（a）本文定义的式（I）的磷脂酰肌醇-3-激酶（PI3K）抑制剂化合物或其药学上可接受的盐和（b）洛莫司汀或其药学上可接受的盐，用于同时，分别或顺序使用，用于治疗脑肿瘤，特别是多形性成胶质细胞瘤; 包含所述组合的药物组合物; 所述组合用于制备用于治疗脑肿瘤的药物的用途; 治疗或预防脑肿瘤的方法包括向有需要的受试者施用联合治疗有效量的这种组合; 及其商业包装。

5. 发明申请

WO2014181252A1 COMBINATION OF A PI3 KINASE INHIBITOR WITH PACLITAXEL FOR USE IN THE TREATMENT OR PREVENTION OF A CANCER OF THE HEAD AND NECK 审中-公开
标题翻译： PI3激酶抑制剂与PACLITAXEL的组合用于治疗或预防头颈部癌症
公开(公告)号：WO2014181252A1
公开(公告)日：2014-11-13
申请号：PCT/IB2014/061239
申请日：2014-05-06
申请人： NOVARTIS AG , HIRAWAT, Samit , MASSACESI, Cristian , DI TOMASO, Emmanuelle
发明人： HIRAWAT, Samit , MASSACESI, Cristian , DI TOMASO, Emmanuelle
IPC分类号： A61K31/337 , A61K31/506 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/337 , A61K31/5395 , A61K2300/00
摘要： A pharmaceutical combination comprising (a) a phosphatidylinositol-3-kinase (PI3K) inhibitor compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof and (b) paclitaxel or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use, for the treatment of a cancer of the head and neck; a pharmaceutical composition comprising said combination; the use of said combination for the preparation of a medicament for the treatment of a cancer of the head and neck; a method of treating or preventing a cancer of the head and neck comprising administering a jointly therapeutically effective amount of such a combination to a subject in need thereof; and a commercial package thereof.
摘要翻译：一种药物组合，其包含（a）本文定义的式（I）的磷脂酰肌醇-3-激酶（PI3K）抑制剂化合物或其药学上可接受的盐和（b）紫杉醇或其药学上可接受的盐，用于同时，分别或顺序使用，用于治疗头颈部癌症; 包含所述组合的药物组合物; 所述组合用于制备用于治疗头颈部癌症的药物的用途; 治疗或预防头颈部癌症的方法包括向有需要的受试者施用联合治疗有效量的这种组合; 及其商业包装。

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