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1. 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。

2. 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。

3. 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。

4. 发明申请

WO2015121795A1 PHARMACEUTICAL COMBINATIONS COMPRISING A PI3K INHIBITOR FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：包含用于治疗癌症的PI3K抑制剂的药物组合
公开(公告)号：WO2015121795A1
公开(公告)日：2015-08-20
申请号：PCT/IB2015/050993
申请日：2015-02-10
申请人： NOVARTIS AG , MASSACESI, Cristian , GERMA, Marie - Caroline
发明人： MASSACESI, Cristian , GERMA, Marie - Caroline
IPC分类号： A61K45/06 , A61K31/436 , A61K31/4439 , A61K31/5685 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/436 , A61K31/5685 , A61K45/06 , A61K2121/00 , A61K2300/00
摘要： A pharmaceutical combination comprising: (a) an alpha-isoform specific phosphatidylinositol-3- kinase inhibitor (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, (b) an mTOR inhibitor and (c) exemestane or any pharmaceutically acceptable salt thereof, particularly for use in the treatment or prevention of a proliferative disease; uses of such a combination in the preparation of a medicament for the treatment or prevention of a proliferative disease; 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）α-异构体特异性磷脂酰肌醇-3-激酶抑制剂（S） - 吡咯烷-1,2-二羧酸2-酰胺1 - （{4-甲基-5- [2-（2， 2,2-二氟乙基） - 吡啶-4-基] - 噻唑-2-基} - 酰胺）或其任何药学上可接受的盐，（b）mTOR抑制剂和（c）依西美坦或其任何药学上可接受的盐，特别用于治疗或预防增殖性疾病; 在制备用于治疗或预防增殖性疾病的药物中的这种组合的用途; 所述治疗剂的组合的药物组合物和治疗受试者的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。

5. 发明申请

WO2013173283A1 DOSAGE REGIMEN FOR A PI-3 KINASE INHIBITOR 审中-公开
标题翻译：用于PI-3激酶抑制剂的剂量方案
公开(公告)号：WO2013173283A1
公开(公告)日：2013-11-21
申请号：PCT/US2013/040877
申请日：2013-05-14
申请人： NOVARTIS AG , HIRAWAT, Samit , MASSACESI, Cristian
发明人： HIRAWAT, Samit , MASSACESI, Cristian
IPC分类号： A61K31/5377
CPC分类号： A61K31/5377 , A61K31/4196
摘要： The present invention relates to a dosage regimen for a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a dosage regimen for the treatment of patients suffering from a proliferative disease, such as, for example, cancer, with a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（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的剂量方案。更具体地，本发明涉及用式（I）的磷脂酰肌醇3-激酶（PI3K）抑制剂化合物或药学上可接受的方法治疗患有增殖性疾病例如癌症的患者的剂量方案的盐。

6. 发明申请

WO2015107461A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2015107461A1
公开(公告)日：2015-07-23
申请号：PCT/IB2015/050260
申请日：2015-01-13
申请人： NOVARTIS AG , HIRAWAT, Samit , MASSACESI, Cristian
发明人： HIRAWAT, Samit , MASSACESI, Cristian
IPC分类号： A61K38/09 , A61K45/06 , A61K31/138 , A61K31/4439 , A61K31/4535 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/138 , A61K31/4439 , A61K31/4535 , A61K38/09 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical combination comprising: (a) a phosphatidylinositol-3-kinase inhibitor selected from 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) a gonadorelin agonist and, optionally, (c) an antiestrogen agent, particularly for use in the treatment or prevention of a cancer; uses of such a combination in the preparation of a medicament for the treatment or prevention of a cancer; pharmaceutical compositions of the combination of said therapeutic agents and methods of treating a cancer 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）选自5-（2,6-二吗啉-4-基 - 嘧啶-4-基）-4-三氟甲基 - 吡啶-2-基胺的磷脂酰肌醇-3-激酶抑制剂， 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-基 ] - 噻唑-2-基} - 酰胺）或其任何药学上可接受的盐和（b）促性腺激素和任选地（c）抗雌激素剂，特别是用于治疗或预防癌症; 在制备用于治疗或预防癌症的药物中的这种组合的用途; 所述治疗剂的组合的药物组合物和治疗受试者的癌症的方法包括向所述受试者施用治疗有效量的这种组合。

7. 发明申请

WO2017077445A1 DOSAGE REGIMEN FOR A PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR 审中-公开
标题翻译：用于磷脂酰肌醇3-激酶抑制剂的剂量方案
公开(公告)号：WO2017077445A1
公开(公告)日：2017-05-11
申请号：PCT/IB2016/056556
申请日：2016-10-31
申请人： NOVARTIS AG
发明人： SCHNELL, Christian , FRITSCH, Christine , DI TOMASO, Emmanuelle , MASSACESI, Cristian , BLUMENSTEIN, Lars
IPC分类号： A61K31/4196 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/553 , A61K9/00 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/4196 , A61K31/437 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/553
摘要： The present disclosure relates to methods of treating or preventing a proliferative disease in a patient in need thereof by orally administering a therapeutically effective amount of a phosphatidylinositol 3-kinase inhibitor compound or a pharmaceutically acceptable salt thereof once-per-day either on a continuous daily schedule or an intermittent schedule at about zero to about three hours prior to sleep; the use of said compound pharmaceutically acceptable salt thereof for the manufacture of a medicament for treating or preventing a proliferative disease administered in accordance with said dosage regimen; a therapeutic regimen comprising administration of said compound or a pharmaceutically acceptable salt thereof in accordance with said dosage regimen; and related pharmaceutical compositions and packages thereof.
摘要翻译：本公开涉及通过口服施用治疗有效量的磷脂酰肌醇3-激酶抑制剂化合物或其药学上可接受的盐来治疗或预防有需要的患者的增殖性疾病的方法，每天以连续的每日时间表或间歇时间表在睡眠前约零至约三小时进行; 所述化合物药学上可接受的盐在制备用于治疗或预防根据所述剂量方案施用的增殖性疾病的药物中的用途; 治疗方案，其包括根据所述剂量方案施用所述化合物或其药学上可接受的盐; 和相关的药物组合物及其包装。

8. 发明公开

EP3370719A1 DOSAGE REGIMEN FOR A PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR 审中-公开
公开(公告)号：EP3370719A1
公开(公告)日：2018-09-12
申请号：EP16794067.5
申请日：2016-10-31
申请人： Novartis AG
发明人： SCHNELL, Christian , FRITSCH, Christine , DI TOMASO, Emmanuelle , MASSACESI, Cristian , BLUMENSTEIN, Lars
IPC分类号： A61K31/4196 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/553 , A61K9/00 , A61P35/00
CPC分类号： A61K31/4439 , A61K9/0053 , A61K31/4196 , A61K31/437 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/553 , A61P35/00
摘要： A method of treating or preventing a proliferative disease in a patient in need thereof by orally administering a therapeutically effective amount of a phosphatidylinositol 3-kinase inhibitor compound or a pharmaceutically acceptable salt thereof once-per-day either on a continuous daily schedule or an intermittent schedule at about zero to about three hours prior to sleep; a therapeutic regimen comprising administration of said compound or a pharmaceutically acceptable salt thereof in accordance with said dosage regimen; and related pharmaceutical compositions and packages thereof.

9. 发明公开

EP3104890A1 PHARMACEUTICAL COMBINATIONS COMPRISING A PI3K INHIBITOR FOR THE TREATMENT OF CANCER 审中-公开
标题翻译： WITH A PI3K抑制剂用于治疗癌症的药物组合，
公开(公告)号：EP3104890A1
公开(公告)日：2016-12-21
申请号：EP15704384.5
申请日：2015-02-10
申请人： Novartis AG
发明人： MASSACESI, Cristian , GERMA, Marie - Caroline
IPC分类号： A61K45/06 , A61K31/436 , A61K31/4439 , A61K31/5685 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/436 , A61K31/5685 , A61K45/06 , A61K2121/00 , A61K2300/00
摘要： A pharmaceutical combination comprising: (a) an alpha-isoform specific phosphatidylinositol-3-kinase inhibitor (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, (b) an mTOR inhibitor and (c) exemestane or any pharmaceutically acceptable salt thereof, particularly for use in the treatment or prevention of a proliferative disease; uses of such a combination in the preparation of a medicament for the treatment or prevention of a proliferative disease; 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：的药物组合包括：（A）α-同工型特异性磷脂酰肌醇-3-激酶抑制剂（S）吡咯烷-1,2-二甲酸2-酰胺1 - （{4-甲基-5- [2-（2， 2,2,2-三氟-1,1-二甲基 - 乙基） - 吡啶-4-基] - 噻唑-2-基}酰胺）或其任何药学上可接受的盐，（b）中，在mTOR抑制剂和（c）依西美坦或其任意药学上可接受的盐，特别是用于治疗或预防增殖性疾病的用途; 寻求在制备用于治疗或预防增殖性疾病的药物的制备中的组合的用途; 所述治疗剂和在受试者中包括给予所述受试者治疗有效量求的组合的治疗增殖性疾病的方法中的药物组合的组合物。

10. 发明公开

EP3076969A1 DOSAGE REGIMEN FOR AN ALPHA-ISOFORM SELECTIVE PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR 有权
标题翻译： DOS UNÜMAÜÜER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER ER
公开(公告)号：EP3076969A1
公开(公告)日：2016-10-12
申请号：EP14812658.4
申请日：2014-12-03
申请人： Novartis AG
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 methods of treating or preventing a proliferative disease in a patient in need thereof by orally administering a therapeutically effective amount of an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof for at least two five-consecutive day cycle, 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; the use of said compound of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for treating or preventing a proliferative disease administered in accordance with said dosage regimen; therapeutic regimen comprising administration of said compound of formula (I) or a pharmaceutically acceptable salt thereof in accordance with said dosage regimen; and related pharmaceutical compositions and packages thereof.
摘要翻译：本发明涉及通过口服给予治疗有效量的式（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来治疗或预防有需要的患者中的增殖性疾病的方法或其药学上可接受的盐至少两个连续5天的周期，其中所述化合物在所述五个连续的第二个周期之间不给予患者约两天至约三天的时间; 所述式（I）化合物或其药学上可接受的盐在制备用于治疗或预防根据所述给药方案施用的增殖性疾病的药物中的用途; 包括根据所述剂量方案施用所述式（I）化合物或其药学上可接受的盐; 和相关的药物组合物及其包装。

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