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公开(公告)号：US09370508B2
公开(公告)日：2016-06-21
申请号：US12525333
申请日：2008-02-19
申请人： Carlos Garcia-Echeverria , Paul Leslie Nicklin , Leon Murphy , Sauveur-Michel Maira , Peter Finan , Christine Fritsch , Saskia Maria Brachmann
发明人： Carlos Garcia-Echeverria , Paul Leslie Nicklin , Leon Murphy , Sauveur-Michel Maira , Peter Finan , Christine Fritsch , Saskia Maria Brachmann
IPC分类号： A61K31/4745
CPC分类号： A61K31/4745
摘要： The invention relates to the use of compounds of formula (I) in the treatment of mammalian target of rapamycin (mTOR) kinase dependent diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
摘要翻译： 本发明涉及式（I）化合物在治疗雷帕霉素（mTOR）激酶依赖性疾病的哺乳动物靶标中的用途，所述化合物在温血动物，特别是人类的治疗所述疾病中的应用方法 ，包含用于治疗所述疾病的所述化合物的药物制剂和用于治疗所述疾病的所述化合物。
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公开(公告)号：US20100105696A1
公开(公告)日：2010-04-29
申请号：US12525333
申请日：2008-02-19
申请人： Carlos Garcia-Echeverria , Paul Leslie Nicklin , Leon Murphy , Sauveur-Michel Maira , Peter Finan , Christine Fritsch , Saskia Maria Brachmann
发明人： Carlos Garcia-Echeverria , Paul Leslie Nicklin , Leon Murphy , Sauveur-Michel Maira , Peter Finan , Christine Fritsch , Saskia Maria Brachmann
IPC分类号： A61K31/4745 , A61K31/496 , A61P37/00 , A61P31/04 , A61P31/12 , A61P25/28
CPC分类号： A61K31/4745
摘要： The invention relates to the use of compounds of formula (I) in the treatment of mammalian target of rapamycin (mTOR) kinase dependent diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
摘要翻译： 本发明涉及式（I）化合物在治疗雷帕霉素（mTOR）激酶依赖性疾病的哺乳动物靶标中的用途，所述化合物在温血动物，特别是人类的治疗所述疾病中的应用方法 ，包含用于治疗所述疾病的所述化合物的药物制剂和用于治疗所述疾病的所述化合物。
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3.发明申请Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members 审中-公开使用2-甲酰胺环氨基脲衍生物治疗EGFR依赖性疾病或已获得耐药性靶向EGFR家族成员的疾病公开(公告)号：US20150250778A1
公开(公告)日：2015-09-10
申请号：US14721064
申请日：2015-05-26
申请人： Saskia Maria Brachmann , Christine Fritsch , Sauveur-Michel Maira , Christian Schnell , Carlos Garcia-Echeverria
发明人： Saskia Maria Brachmann , Christine Fritsch , Sauveur-Michel Maira , Christian Schnell , Carlos Garcia-Echeverria
IPC分类号： A61K31/4439 , A61K31/517 , A61K39/395 , A61K45/06
CPC分类号： A61K31/4439 , A61K31/517 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2300/00 , C07K16/32 , C07K2317/24
摘要： The use of compounds of formula (I) in the treatment of Epidermal Growth Factor Receptor (EGFR) dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.
摘要翻译： 使用式（I）化合物在治疗表皮生长因子受体（EGFR）依赖性疾病或具有获得对靶向EGFR家族成员的药物的抗性的疾病中的用途，所述化合物用于制备药物组合物用于治疗 所述疾病，所述化合物与所述用途的EGFR调节剂的组合，用所述化合物治疗所述疾病的方法和用于治疗所述疾病的药物制剂，所述疾病包括单独或组合的所述化合物，特别是与EGFR调节剂组合。
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4.发明申请Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members 审中-公开使用2-甲酰胺环氨基脲衍生物治疗EGFR依赖性疾病或已获得耐药性靶向EGFR家族成员的疾病公开(公告)号：US20130209461A1
公开(公告)日：2013-08-15
申请号：US13879644
申请日：2011-11-07
申请人： Saskia Maria Brachmann , Christine Fritsch , Sauveur-Michel Maira , Christian Rene Schnell , Carlos Garcia-Echeverria
发明人： Saskia Maria Brachmann , Christine Fritsch , Sauveur-Michel Maira , Christian Rene Schnell , Carlos Garcia-Echeverria
IPC分类号： A61K31/4439 , A61K31/517 , A61K39/395
CPC分类号： A61K31/4439 , A61K31/517 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2300/00 , C07K16/32 , C07K2317/24
摘要： A method for treating an Epidermal Growth Factor Receptor (EGFR) dependent diseases or diseases that have acquired resistance to agents that target EGFR family members comprising administering a therapeutically effective amount of a compound of formula (I) alone or in combination with an EGFR modulator, to a warm-blooded animal in need thereof; combinations comprising the compound of formula (I) and an EGFR modulator for the treatment of said diseases; and pharmaceutical preparations for the treatment of said diseases comprising the compound of formula (I), alone or in combination with an EGFR modulator.
摘要翻译： 一种用于治疗具有针对EGFR家族成员的药物获得抗性的表皮生长因子受体（EGFR）依赖性疾病或疾病的方法，包括单独或与EGFR调节剂组合施用治疗有效量的式（I）化合物， 到有需要的温血动物; 包含式（I）化合物和用于治疗所述疾病的EGFR调节剂的组合; 和用于治疗包含式（I）化合物的所述疾病的药物制剂，其单独或与EGFR调节剂组合。
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5.发明授权公开(公告)号：US09241939B2
公开(公告)日：2016-01-26
申请号：US14576314
申请日：2014-12-19
申请人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
发明人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
IPC分类号： A61K31/497 , A61K31/4745 , A61K31/4188 , A61K45/06 , A61K31/166 , A61K31/437 , A61K31/4439 , A61K31/5377
CPC分类号： A61K31/4745 , A61K31/166 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway 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.
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6.发明申请COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) A MODULATOR OF RAS/RAF/MEK PATHWAY 审中-公开（A）磷酸三磷酸激酶抑制剂的组合和（B）RAS / RAF / MEK途径的调节剂公开(公告)号：US20110105521A1
公开(公告)日：2011-05-05
申请号：US13003581
申请日：2009-07-10
申请人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
发明人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
IPC分类号： A61K31/496 , A61K31/4745 , A61P35/00 , A61P35/02
CPC分类号： A61K31/4745 , A61K31/166 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway 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）调节Ras / Raf / Mek途径用于治疗增殖性疾病，特别是实体瘤疾病的化合物; 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。
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7.发明申请Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of RAS/RAF/MEK pathway 审中-公开（a）磷酸肌醇3-激酶抑制剂和（b）RAS / RAF / MEK途径的调节剂的组合公开(公告)号：US20150105417A1
公开(公告)日：2015-04-16
申请号：US14576314
申请日：2014-12-19
申请人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
发明人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
IPC分类号： A61K31/4745 , A61K31/166
CPC分类号： A61K31/4745 , A61K31/166 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway 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）调节Ras / Raf / Mek途径用于治疗增殖性疾病，特别是实体瘤疾病的化合物; 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。
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8.发明申请COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND A MTOR INHIBITOR 审中-公开磷脂酰肌醇三激酶（PI3K）抑制剂和MTOR抑制剂的组合公开(公告)号：US20140066474A1
公开(公告)日：2014-03-06
申请号：US14113316
申请日：2012-04-23
IPC分类号： A61K31/4439 , A61K31/439
CPC分类号： A61K31/4439 , A61K31/427 , A61K31/436 , A61K31/439 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical combination comprising a phosphatidylinositol-3-kinase (PI3K) inhibitor compound which is a 2-carboxamide cycloamino urea derivative or a pharmaceutically acceptable salt thereof and at least one mammalian target of rapamycin (mTOR) inhibitor or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising such a combination; and the uses of such a combination in the treatment proliferative diseases, more specifically of mammalian target of rapamycin (mTOR) kinase dependent diseases.
摘要翻译： 本发明涉及药物组合，其包含磷酰肌醇-3-激酶（PI3K）抑制剂化合物，其是2-甲酰胺环氨基脲衍生物或其药学上可接受的盐和至少一种哺乳动物雷帕霉素靶（mTOR）抑制剂或药学上可接受的盐 其可接受的盐; 包含这种组合的药物组合物; 以及这种组合在治疗增殖性疾病中的用途，更具体地涉及雷帕霉素（mTOR）激酶依赖性疾病的哺乳动物靶标。
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公开(公告)号：US20170095463A1
公开(公告)日：2017-04-06
申请号：US15335957
申请日：2016-10-27
IPC分类号： A61K31/4439 , A61K45/06 , A61K31/436
CPC分类号： A61K31/4439 , A61K31/427 , A61K31/436 , A61K31/439 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical combination comprising a phosphatidylinositol-3-kinase (PI3K) inhibitor compound which is a 2-carboxamide cycloamino urea derivative or a pharmaceutically acceptable salt thereof and at least one mammalian target of rapamycin (mTOR) inhibitor or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising such a combination; and the uses of such a combination in the treatment proliferative diseases, more specifically of mammalian target of rapamycin (mTOR) kinase dependent diseases.
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10.发明申请Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of RAS/RAF/MEK pathway 审中-公开（a）磷酸肌醇3-激酶抑制剂和（b）RAS / RAF / MEK途径的调节剂的组合公开(公告)号：US20140057904A1
公开(公告)日：2014-02-27
申请号：US14066734
申请日：2013-10-30
申请人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
发明人： Carlos Garcia-Echeverria , Sauveur-Michel Maira , Darrin Stuart , Susan Wee , Christine Fritsch , Tobi Nagel
IPC分类号： A61K31/5377 , A61K45/06 , A61K31/437 , A61K31/166 , A61K31/4439
CPC分类号： A61K31/4745 , A61K31/166 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway 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）调节Ras / Raf / Mek途径用于治疗增殖性疾病，特别是实体瘤疾病的化合物; 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。
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