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1.发明授权Pyrrolidine-substituted flavones as radio-sensitizers for use in the treatment of cancer 有权吡咯烷取代的黄酮作为用于治疗癌症的放射敏感剂公开(公告)号：US08895605B2
公开(公告)日：2014-11-25
申请号：US13318235
申请日：2010-05-03
IPC分类号： A61K31/4025 , C07D311/32 , A61P35/00 , A61K31/00
CPC分类号： A61K31/00 , A61K31/4025 , A61K2300/00
摘要： The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
摘要翻译： 本发明涉及用于治疗癌症的组合，其中组合表现出协同效应。 该组合包括辐射和至少一种选自式I化合物的细胞周期蛋白依赖性激酶（CDK）抑制剂或其药学上可接受的盐或溶剂合物。 本发明还涉及一种治疗癌症的方法，该方法包括向需要这种治疗的患者施用治疗有效量的组合。 本发明还涉及选自式I化合物的CDK抑制剂作为放射增敏剂的用途，其增强了放射治疗癌症尤其是头颈癌的疗效。
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2.发明申请PYRROLIDINE-SUBSTITUTED FLAVONES AS RADIO-SENSITIZERS FOR USE IN THE TREATMENT OF CANCER 有权用于治疗癌症的紫杉醇取代的氟喹诺酮类药物公开(公告)号：US20120046334A1
公开(公告)日：2012-02-23
申请号：US13318235
申请日：2010-05-03
IPC分类号： A61K31/4025 , A61P35/00 , C07D405/10
CPC分类号： A61K31/00 , A61K31/4025 , A61K2300/00
摘要： The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
摘要翻译： 本发明涉及用于治疗癌症的组合，其中组合表现出协同效应。 该组合包括辐射和至少一种选自式I化合物的细胞周期蛋白依赖性激酶（CDK）抑制剂或其药学上可接受的盐或溶剂合物。 本发明还涉及一种治疗癌症的方法，该方法包括向需要这种治疗的患者施用治疗有效量的组合。 本发明还涉及选自式I化合物的CDK抑制剂作为放射增敏剂的用途，其增强了放射治疗癌症尤其是头颈癌的疗效。
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公开(公告)号：US20130237582A1
公开(公告)日：2013-09-12
申请号：US13988240
申请日：2011-11-18
IPC分类号： A61K31/4025 , A61K31/337
CPC分类号： A61K31/4025 , A61K31/337 , A61K31/352
摘要： The present invention relates to a pharmaceutical combination comprising paclitaxel, or its pharmaceutically acceptable salt; and at least one cyclin dependent kinase (CDK) inhibitor represented by a compound of formula I (as described herein) or a pharmaceutically acceptable salt thereof, for use in the treatment of triple negative breast cancer (TNBC). The present invention relates to a method for the treatment of breast cancer, particularly triple negative breast cancer, by administration to a patient in need thereof, a therapeutically effective amount of a pharmaceutical combination comprising a cytotoxic antineoplastic agent, paclitaxel, and at least one cyclin dependent kinase (CDK) inhibitor; wherein said combination on administration exhibits synergistic effects.
摘要翻译： 本发明涉及包含紫杉醇或其药学上可接受的盐的药物组合; 和由式I化合物（如本文所述）或其药学上可接受的盐代表的至少一种用于治疗三阴性乳腺癌（TNBC）的细胞周期蛋白依赖性激酶（CDK）抑制剂。 本发明涉及通过给予有需要的患者的治疗乳腺癌特别是三阴性乳腺癌的方法，治疗有效量的包含细胞毒性抗肿瘤剂，紫杉醇和至少一种细胞周期蛋白的药物组合 依赖性激酶（CDK）抑制剂; 其中所述施用组合表现出协同效应。
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公开(公告)号：US08314103B2
公开(公告)日：2012-11-20
申请号：US12672485
申请日：2008-08-06
申请人： Sanjay Kumar , Kalpana Sanjay Joshi , Vijaykumar Deore , Mandar Ramesh Bhonde , Nilambari Nilkanth Yewalkar , Amol Arun Padgaonkar , Asha Adrian Kulkarni-Almeida , Maggie Joyce Rathos , Sapna Parikh , Nilesh Madhukar Dagia
发明人： Sanjay Kumar , Kalpana Sanjay Joshi , Vijaykumar Deore , Mandar Ramesh Bhonde , Nilambari Nilkanth Yewalkar , Amol Arun Padgaonkar , Asha Adrian Kulkarni-Almeida , Maggie Joyce Rathos , Sapna Parikh , Nilesh Madhukar Dagia
IPC分类号： A61K31/50 , C07D401/00
CPC分类号： C07D213/73 , C07D213/75 , C07D213/78 , C07D401/04 , C07D407/04 , C07D413/04
摘要： The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.
摘要翻译： 本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k），雷帕霉素哺乳动物靶（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号传导的吡啶衍生物。 还公开了制备吡啶基衍生物的方法及其在制备用于治疗由选自PI3K，mTOR和HIF-1α途径中的一种或多种的信号传导途径失调引起的临床病症的药物组合物中的用途。 吡啶基衍生物也可用于治疗由TNF-α介导的病症或病症。
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公开(公告)号：US20110077252A1
公开(公告)日：2011-03-31
申请号：US12672485
申请日：2008-08-06
申请人： Sanjay Kumar , Kalpana Sanjay Joshi , Vijaykumar Deore , Mandar Ramesh Bhonde , Nilambari Nilkanth Yewalkar , Amol Arun Padgaonkar , Asha Adrian Kulkarni-Almeida , Maggie Joyce Rathos , Sapna Parikh , Nilesh Madhukar Dagia
发明人： Sanjay Kumar , Kalpana Sanjay Joshi , Vijaykumar Deore , Mandar Ramesh Bhonde , Nilambari Nilkanth Yewalkar , Amol Arun Padgaonkar , Asha Adrian Kulkarni-Almeida , Maggie Joyce Rathos , Sapna Parikh , Nilesh Madhukar Dagia
IPC分类号： A61K31/501 , C07D403/04 , C07D239/34 , A61K31/505 , A61P35/00 , A61P31/14 , A61P31/18 , A61P3/10 , A61P25/28 , A61P37/00 , A61P19/02 , A61P19/10
CPC分类号： C07D213/73 , C07D213/75 , C07D213/78 , C07D401/04 , C07D407/04 , C07D413/04
摘要： The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.
摘要翻译： 本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k），雷帕霉素哺乳动物靶（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号传导的吡啶衍生物。 还公开了制备吡啶基衍生物的方法及其在制备用于治疗由选自PI3K，mTOR和HIF-1α途径中的一种或多种的信号传导途径失调引起的临床病症的药物组合物中的用途。 吡啶基衍生物也可用于治疗由TNF-α介导的病症或病症。
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公开(公告)号：US07915301B2
公开(公告)日：2011-03-29
申请号：US11779577
申请日：2007-07-18
申请人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
发明人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
IPC分类号： A61K31/4025 , A61K31/353 , C07D405/04 , C07D311/32
CPC分类号： A61K31/4025 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译： 本发明涉及用于抑制细胞周期蛋白依赖性激酶的新化合物，更具体地，涉及式（Ia）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有如 索赔。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以使用式（Ia）化合物在治疗和预防疾病中的用途 ，其可以通过抑制细胞周期蛋白依赖性激酶（例如癌症）来治疗或预防使用式（Ia）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ia）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ia）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。
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公开(公告)号：US08304449B2
公开(公告)日：2012-11-06
申请号：US13026503
申请日：2011-02-14
申请人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
发明人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
IPC分类号： A61K31/4025 , A61K31/353 , C07D405/04 , C07D311/32
CPC分类号： A61K31/4025 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译： 本发明涉及用于抑制细胞周期蛋白依赖性激酶的新化合物，更具体地，涉及式（Ia）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有如 索赔。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以使用式（Ia）化合物在治疗和预防疾病中的用途 ，其可以通过抑制细胞周期蛋白依赖性激酶（例如癌症）来治疗或预防使用式（Ia）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ia）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ia）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。
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公开(公告)号：US20130045993A1
公开(公告)日：2013-02-21
申请号：US13585006
申请日：2012-08-14
申请人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
发明人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
IPC分类号： A61K31/4025 , A61P35/02 , A61P35/00 , A61K31/4439 , A61K31/4178
CPC分类号： A61K31/4025 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel compounds for the inhibition of cyclindependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7, and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclindependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译： 本发明涉及用于抑制环有依赖性激酶的新化合物，更具体地说，涉及式（Ia）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有 声称。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以使用式（Ia）化合物在治疗和预防疾病中的用途 ，其可以通过抑制环己基依赖性激酶例如癌症来治疗或预防使用式（Ia）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ia）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ia）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。
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公开(公告)号：US20110136873A1
公开(公告)日：2011-06-09
申请号：US13026503
申请日：2011-02-14
申请人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
发明人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi
IPC分类号： A61K31/4439 , A61K31/4025 , A61K31/4178 , A61P35/00
CPC分类号： A61K31/4025 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译： 本发明涉及用于抑制细胞周期蛋白依赖性激酶的新化合物，更具体地，涉及式（Ia）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有如 索赔。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以使用式（Ia）化合物在治疗和预防疾病中的用途 ，其可以通过抑制细胞周期蛋白依赖性激酶（例如癌症）来治疗或预防使用式（Ia）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ia）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ia）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。
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公开(公告)号：US07884127B2
公开(公告)日：2011-02-08
申请号：US11530272
申请日：2006-09-08
申请人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi , Meenakshi Sivakumar
发明人： Bansi Lal , Kalpana Joshi , Sanjeev Kulkarni , Malcolm Mascarenhas , Shrikant Kamble , Maggie Joyce Rathos , Rajendrakumar Joshi , Meenakshi Sivakumar
IPC分类号： A61K31/4025 , A61K31/353 , C07D405/04 , C07D311/32
CPC分类号： C07D405/04 , C07D405/14
摘要： The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ic) wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ic) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ic) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ic) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ic) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译： 本发明涉及用于抑制细胞周期蛋白依赖性激酶的新化合物，更具体地说，涉及式（Ic）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有 声称。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，使用式（Ic）化合物在治疗和预防疾病中的用途 ，其可以通过抑制细胞周期蛋白依赖性激酶（例如癌症）来治疗或预防使用式（Ic）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ic）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ic）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。
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