公开(公告)号：US20070015802A1

公开(公告)日：2007-01-18

申请号：US11530272

申请日：2006-09-08

申请人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Rathos ,  Rajendrakumar Joshi ,  Meenakashi Sivakumar

发明人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Rathos ,  Rajendrakumar Joshi ,  Meenakashi Sivakumar

IPC分类号： A61K31/427 ,  A61K31/422 ,  A61K31/4178 ,  C07D417/02 ,  C07D413/02 ,  C07D405/02

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，涉及其中R 1，R 2，R 2， R 3，R 4，R 5，R 6，R 7和A 具有权利要求中所示的含义。 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。

公开(公告)号：US20080108690A1

公开(公告)日：2008-05-08

申请号：US11779577

申请日：2007-07-18

申请人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Rathos ,  Rajendrakumar Joshi

发明人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Rathos ,  Rajendrakumar Joshi

IPC分类号： A61K31/4025 ,  A61P35/00 ,  A61P35/04 ,  C07D405/04

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R 7， A具有权利要求中所示的含义。 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。

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。

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。

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。

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。

公开(公告)号：US07271193B2

公开(公告)日：2007-09-18

申请号：US10611539

申请日：2003-07-01

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： 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R 7， A具有权利要求中所示的含义。 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。

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。

公开(公告)号：US20100179210A1

公开(公告)日：2010-07-15

申请号：US12305815

申请日：2006-06-21

申请人： Meenakshi Sivakumar ,  Malcolm Mascarenhas ,  Ankush Sarde ,  Pramod Kumar Jadhav ,  Manoj Shukla ,  Kalpana Joshi ,  Maggie Rathos

发明人： Meenakshi Sivakumar ,  Malcolm Mascarenhas ,  Ankush Sarde ,  Pramod Kumar Jadhav ,  Manoj Shukla ,  Kalpana Joshi ,  Maggie Rathos

IPC分类号： A61K31/4025 ,  C07D405/00 ,  C07D207/04 ,  A61P35/00

CPC分类号： C07D405/04 ,  C07D207/08

摘要： The present invention relates to an enantiomerically pure (+)-trans-enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.

摘要翻译： 本发明涉及由下式（I）表示的化合物的对映体纯的（+） - 反式对映异构体：其中R1，R2，R3，R4和R9如说明书中所定义; 对映体纯的中间体，用于制备对映体纯的化合物及其中间体的方法，以及包含对映体纯的化合物的药物组合物。 式（I）化合物可用于治疗由抑制细胞周期蛋白依赖性激酶（例如癌症）介导的疾病或病症。

公开(公告)号：US08563596B2

公开(公告)日：2013-10-22

申请号：US12305815

申请日：2006-06-21

申请人： Meenakshi Sivakumar ,  Malcolm Mascarenhas ,  Ankush Sarde ,  Pramod Kumar Jadhav ,  Manoj Shukla ,  Kalpana Joshi ,  Maggie Rathos

发明人： Meenakshi Sivakumar ,  Malcolm Mascarenhas ,  Ankush Sarde ,  Pramod Kumar Jadhav ,  Manoj Shukla ,  Kalpana Joshi ,  Maggie Rathos

IPC分类号： A01N43/36 ,  A61K31/40 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D207/00

CPC分类号： C07D405/04 ,  C07D207/08

摘要： The present invention relates to an enantiomerically pure (+)-trans enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.

摘要翻译： 本发明涉及由下式（I）表示的化合物的对映体纯的（+） - 反式对映异构体：其中R1，R2，R3，R4和R9如说明书中所定义; 对映体纯的中间体，用于制备对映体纯的化合物及其中间体的方法，以及包含对映体纯的化合物的药物组合物。 式（I）化合物可用于治疗由抑制细胞周期蛋白依赖性激酶（例如癌症）介导的疾病或病症。