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1. 发明申请

WO2010130779A2 COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND 审中-公开
标题翻译： PBOSPBOINOSITKLE 3-KSpASE抑制剂和抗生素化合物的组合
公开(公告)号：WO2010130779A2
公开(公告)日：2010-11-18
申请号：PCT/EP2010/056538
申请日：2010-05-12
申请人： NOVARTIS AG , BASELGA, Jose , DI COSIMO, Serena , GARCIA-ECHEVERRIA, Carlos , HACKL, Wolfgang , MAIRA, Sauveur-Michel , RUSSILLO, Michelangelo , SERRA ELIZALDE, Violeta
发明人： BASELGA, Jose , DI COSIMO, Serena , GARCIA-ECHEVERRIA, Carlos , HACKL, Wolfgang , MAIRA, Sauveur-Michel , RUSSILLO, Michelangelo , SERRA ELIZALDE, Violeta
IPC分类号： A61K31/155 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P35/00 , A61P3/10
CPC分类号： A61K45/06 , A61K31/155 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphosnositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
摘要翻译：本发明涉及药物组合，其包含（a）磷酸肌醇3-激酶抑制剂化合物和（b）用于治疗增殖性疾病，特别是实体瘤疾病的胰岛素敏感性增强剂化合物; 包含这种组合的药物组合物; 使用这种组合来制备用于治疗增殖性疾病的药物; 包括作为用于同时，分开或顺序使用的组合制剂的组合的商业包装或产品; 以及治疗温血动物，特别是人的方法。

2. 发明申请

WO2012075253A3 PHARMACEUTICAL COMPOSITIONS 审中-公开
公开(公告)号：WO2012075253A3
公开(公告)日：2012-06-07
申请号：PCT/US2011/062837
申请日：2011-12-01
申请人： NOVARTIS AG , CAO, Yu , HACKL, Wolfgang , LI, Ping , LI, Shoufeng , MIRZA, Tahseen , ZEHENDER, Hartmut , ZHU, Jiahao
发明人： CAO, Yu , HACKL, Wolfgang , LI, Ping , LI, Shoufeng , MIRZA, Tahseen , ZEHENDER, Hartmut , ZHU, Jiahao
IPC分类号： A61K9/16 , A61P35/00
摘要： The present invention relates to a pharmaceutical composition for the oral administration of a therapeutic compound of formula (I), which comprises granules that comprise at least therapeutic compound of formula (I) (see below), particularly 2-Methyl-2-[4-(3-methyl-2-oxo-8- quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile or 8-(6-methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one, or a tautomer thereof, or a pharmaceutically acceptable salt, or a hydrate or solvate thereof; at least one non-ionic surfactant that is Vitamin E-TPGS in an amount ranging from about 15 to about 80% by weight of the composition; and at least one a dissolution enhancing agent selected from polyethylene glycol, polyethylene oxide, and any combination of the foregoing. The present invention also relates to processes for making such pharmaceutical compositions; a kit comprising such pharmaceutical composition and the instructions provide that the pharmaceutical composition may be taken immediately to about thirty minutes after the consumption of food; and related uses and methods of treatment.

3. 发明申请

WO2012075253A2 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2012075253A2
公开(公告)日：2012-06-07
申请号：PCT/US2011062837
申请日：2011-12-01
申请人： NOVARTIS AG , CAO YU , HACKL WOLFGANG , LI PING , LI SHOUFENG , MIRZA TAHSEEN , ZEHENDER HARTMUT , ZHU JIAHAO
发明人： CAO YU , HACKL WOLFGANG , LI PING , LI SHOUFENG , MIRZA TAHSEEN , ZEHENDER HARTMUT , ZHU JIAHAO
IPC分类号： A61K9/16 , A61P35/00
CPC分类号： C07D471/04 , A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1641 , A61K9/1694 , A61K31/00
摘要： The present invention relates to a pharmaceutical composition for the oral administration of a therapeutic compound of formula (I), which comprises granules that comprise at least therapeutic compound of formula (I) (see below), particularly 2-Methyl-2-[4-(3-methyl-2-oxo-8- quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile or 8-(6-methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one, or a tautomer thereof, or a pharmaceutically acceptable salt, or a hydrate or solvate thereof; at least one non-ionic surfactant that is Vitamin E-TPGS in an amount ranging from about 15 to about 80% by weight of the composition; and at least one a dissolution enhancing agent selected from polyethylene glycol, polyethylene oxide, and any combination of the foregoing. The present invention also relates to processes for making such pharmaceutical compositions; a kit comprising such pharmaceutical composition and the instructions provide that the pharmaceutical composition may be taken immediately to about thirty minutes after the consumption of food; and related uses and methods of treatment.
摘要翻译：本发明涉及用于口服施用式（I）的治疗性化合物的药物组合物，其包含至少包含式（I）的治疗性化合物（参见下文），尤其是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] - 丙腈或8-（6-甲氧基 - 吡啶-3-基）-3-甲基-1-（4-哌嗪-1-基-3-三氟甲基 - 苯基）-1,3-二氢 - 咪唑并[4,5-c]喹啉-2-酮，或其互变异构体，或其药学上可接受的盐或水合物或溶剂化物; 至少一种非离子表面活性剂，其量为组合物重量的约15至约80％的量的维生素E-TPGS; 和至少一种选自聚乙二醇，聚环氧乙烷和前述的任意组合的溶解增强剂。本发明还涉及制造这种药物组合物的方法; 包含此类药物组合物和说明书的试剂盒提供了可以立即在食物消耗后约三十分钟服用药物组合物; 以及相关的用途和治疗方法。

4. 发明申请

WO2016120828A1 TREATMENT OF BREAST CANCER BY M-CSF ANTAGONIST 审中-公开
标题翻译：通过M-CSF拮抗剂治疗乳腺癌
公开(公告)号：WO2016120828A1
公开(公告)日：2016-08-04
申请号：PCT/IB2016/050442
申请日：2016-01-28
申请人： NOVARTIS AG , HACKL, Wolfgang , MURAKAMI, Masato , WIESMANN, Marion , JI, Yan , FJAELLSKOG, Marie-Louise , WHARTON, Keith
发明人： HACKL, Wolfgang , MURAKAMI, Masato , WIESMANN, Marion , JI, Yan , FJAELLSKOG, Marie-Louise , WHARTON, Keith
IPC分类号： A61K39/395 , A61K31/00 , C07K16/24 , G01N33/574
CPC分类号： C07K16/243 , A61K31/555 , A61K31/7068 , A61K33/24 , A61K39/39558 , A61K2039/505 , A61K2039/55 , C07K2317/24 , G01N33/57415 , G01N2333/70596 , G01N2333/7153 , G01N2800/52 , A61K2300/00
摘要： The invention relates, in part, to a method of selectively treating a patient having breast cancer, comprising administering a therapeutically effective amount of a M-CSF antagonist to the patient on the basis of the patient having a level of CD 163 expression that is predictive that the patient will respond to an M-CSF antagonist. The invention relates, in part, to a method of treating a patient having triple negative breast cancer, comprising administering a therapeutically effective amount of an M-CSF antibody or fragment thereof to the patient, wherein the M-CSF antibody or fragment comprises 1, 2, 3, 4, 5, or 6 CDRs as shown in Table 1. The invention relates, in part, to a method of treating a patient having breast cancer, comprising administering a combination of a therapeutically effective amount of an M-CSF antagonist, a therapeutically effective amount of a second agent and a therapeutically effective amount of a third agent.
摘要翻译：本发明部分地涉及选择性治疗患有乳腺癌的患者的方法，其包括基于具有预测性的CD163表达水平的患者向患者施用治疗有效量的M-CSF拮抗剂患者将对M-CSF拮抗剂作出反应。本发明部分涉及治疗患有三阴性乳腺癌的患者的方法，包括向患者施用治疗有效量的M-CSF抗体或其片段，其中所述M-CSF抗体或片段包含1， 2,3,4,5或6个CDR。本发明部分涉及治疗患有乳腺癌的患者的方法，包括给予治疗有效量的M-CSF拮抗剂的组合，治疗有效量的第二药剂和治疗有效量的第三药剂。

5. 发明申请

WO2010130779A3 COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) AN ANTIDIABETIC COMPOUND FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：（A）磷酸三磷酸激酶抑制剂的组合和（B）用于治疗增殖性疾病的抗生素化合物
公开(公告)号：WO2010130779A3
公开(公告)日：2013-03-28
申请号：PCT/EP2010056538
申请日：2010-05-12
申请人： NOVARTIS AG , BASELGA JOSE , DI COSIMO SERENA , GARCIA-ECHEVERRIA CARLOS , HACKL WOLFGANG , MAIRA SAUVEUR-MICHEL , RUSSILLO MICHELANGELO , SERRA ELIZALDE VIOLETA
发明人： BASELGA JOSE , DI COSIMO SERENA , GARCIA-ECHEVERRIA CARLOS , HACKL WOLFGANG , MAIRA SAUVEUR-MICHEL , RUSSILLO MICHELANGELO , SERRA ELIZALDE VIOLETA
IPC分类号： A61K31/155 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P3/10 , A61P35/00
CPC分类号： A61K45/06 , A61K31/155 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphosnositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
摘要翻译：本发明涉及药物组合，其包含（a）磷酸肌醇3-激酶抑制剂化合物和（b）用于治疗增殖性疾病，特别是实体瘤疾病的胰岛素敏感性增强剂化合物; 包含这种组合的药物组合物; 使用这种组合来制备用于治疗增殖性疾病的药物; 商业包装或产品，其包含作为同时，分开或顺序使用的组合制剂的组合; 以及治疗温血动物，特别是人的方法。

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