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1. 发明申请

US20130245259A1 PROCESS FOR THE PREPARATION OF BOSENTAN MONOHYDRATE 审中-公开
标题翻译：制备硼酸单硬脂酸酯的方法
公开(公告)号：US20130245259A1
公开(公告)日：2013-09-19
申请号：US13422491
申请日：2012-03-16
申请人： Amala Kishan Kompella , Srinivasu Kasa , Veera Swamy Balina , Subhash Kusumba , Kali Satya Bhujanga Rao Adibhatla , Venkaiah Chowdary Nannapaneni
发明人： Amala Kishan Kompella , Srinivasu Kasa , Veera Swamy Balina , Subhash Kusumba , Kali Satya Bhujanga Rao Adibhatla , Venkaiah Chowdary Nannapaneni
IPC分类号： C07D403/04
CPC分类号： C07D239/52
摘要： The invention relates to improved processes for the preparation of bosentan monohydrate which provide higher yield and purity.
摘要翻译：本发明涉及提供更高产率和纯度的改进的制备波生坦一水合物的方法。

2. 发明授权

US08067422B2 Crystal form of phenylamino pyrimidine derivatives 有权
标题翻译：苯基氨基嘧啶衍生物的晶型
公开(公告)号：US08067422B2
公开(公告)日：2011-11-29
申请号：US12042247
申请日：2008-03-04
申请人： Amala Kishan Kompella , Bhujanga Rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
发明人： Amala Kishan Kompella , Bhujanga Rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
IPC分类号： A01N43/54 , C07D239/00 , C07D239/02
CPC分类号： C07D401/04 , A61K31/506
摘要： The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN-019, is:
摘要翻译：本发明涉及（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（式I）的具体形式，方法用于制备它们，含有这种晶形的药物组合物，以及它们在人体中作为抗肿瘤剂的用途。式I化合物，也称为AN-019，是：

3. 发明申请

US20080306100A1 PHENYLAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF BCR-ABL KINASE 有权
标题翻译：作为BCR-ABL激酶的抑制剂的苯甲酰胺嘧啶衍生物
公开(公告)号：US20080306100A1
公开(公告)日：2008-12-11
申请号：US12042235
申请日：2008-03-04
申请人： Amala Kishan KOMPELLA , Bhujanga Rao ADIBHATLA KALI SATYA , Sreenivas RACHAKONDA , Nannapaneni VENKAIAH CHOWDARY
发明人： Amala Kishan KOMPELLA , Bhujanga Rao ADIBHATLA KALI SATYA , Sreenivas RACHAKONDA , Nannapaneni VENKAIAH CHOWDARY
IPC分类号： C07D401/04 , A61K31/506 , C07C381/00 , A61P35/00
CPC分类号： C07C323/62 , C07C233/66 , C07C279/18 , C07C317/44 , C07D213/82 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC50; 191 values of these molecules are in the range 0.1 to 10.0 nm, these novel compounds are potentially useful for the treatment of CML.The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN-019, is: This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates. The compound of formula (I), also known as AN-024, is:
摘要翻译：本发明涉及可用于制备新型苯基氨基嘧啶衍生物，新型苯基氨基嘧啶衍生物的新中间体。含有新型苯基氨基嘧啶衍生物的药物组合物及其制备方法。本发明特别涉及通式（I）的新型苯基嘧啶胺衍生物。式1的新化合物可用于治疗慢性骨髓性白血病（CML）。由于IC50; 这些分子的191个值在0.1至10.0nm的范围内，这些新化合物潜在地可用于治疗CML。本发明涉及（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（式I）的具体形式，方法用于制备它们，含有这种晶形的药物组合物，以及它们在人体中作为抗肿瘤剂的用途。式I化合物，也称为AN-019，是：本发明涉及制备（3-三氟甲基磺酰基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基（3-三氟甲基磺酰基）-N- [4-甲基-3-硝基苯基] - 苯甲酰胺，由4-甲基-2-硝基 - 苯胺（式（II））开始制备） - 苯基] - 苯甲酰胺（式（III）），（3-三氟甲基磺酰基）-N- [3-氨基-4-甲基苯基] - 苯甲酰胺（式（IV））和（3-三氟甲基磺酰基）-N- [3-胍基-4-甲基苯基] - 苯甲酰胺（式（V））。本发明还涉及制备这些中间体的方法。式（I）化合物，也称为AN-024，为：

4. 发明申请

US20080249121A1 INTERMEDIATES AND A PROCESS EMPLOYING THE INTERMEDIATES FOR THE PREPARATION OF (3-TRIFLUOROMETHYLSULFONYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]-BENZAMIDE 有权
标题翻译：中间体和使用制备（3-三氟甲磺酰基）-N- [4-甲基-3-（4-吡啶-3-基 - 吡咯烷-2-基氨基）苯基] - 苯甲酰胺的中间体的方法
公开(公告)号：US20080249121A1
公开(公告)日：2008-10-09
申请号：US12042240
申请日：2008-03-04
申请人： Amala Kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
发明人： Amala Kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/506 , C07D401/04 , C07C233/66 , C07C279/18 , A61P35/00
CPC分类号： C07C317/44 , C07D213/82 , C07D401/04 , C07D401/14
摘要： This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates. The compound of formula (I), also known as AN-024, is:
摘要翻译：本发明涉及从4开始制备（3-三氟甲基磺酰基）-N- [4-甲基-3-（4-吡啶基-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（式（I））的方法（3-三氟甲磺酰基）-N- [4-甲基-3-硝基苯基] - 苯甲酰胺（式（III）），（3-三氟甲基磺酰基）-N-甲基-2-硝基 - 苯胺（式（II） [3-氨基-4-甲基苯基] - 苯甲酰胺（式（IV））和（3-三氟甲基磺酰基）-N- [3-胍基-4-甲基苯基] - 苯甲酰胺（式（Ⅴ））。本发明还涉及制备这些中间体的方法。式（I）化合物，也称为AN-024，为：

5. 发明授权

US07910598B2 Phenylaminopyrimidine derivatives as inhibitors of BCR-ABL kinase 有权
标题翻译：苯基氨基嘧啶衍生物作为BCR-ABL激酶的抑制剂
公开(公告)号：US07910598B2
公开(公告)日：2011-03-22
申请号：US11714565
申请日：2007-03-05
申请人： Amala kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Khadgapathi Podili , Nannapaneni Venkaiah Chowdary
发明人： Amala kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Khadgapathi Podili , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D401/04 , C07D401/14 , A61K31/506
CPC分类号： C07C323/62 , C07C233/66 , C07C279/18 , C07C317/44 , C07D213/82 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC50; 191 values of these molecules are in the range 0.1 to 10.0 nm, these novel compounds are potentially useful for the treatment of CML.
摘要翻译：本发明涉及可用于制备新型苯基氨基嘧啶衍生物，新型苯基氨基嘧啶衍生物的新中间体。含有新型苯基氨基嘧啶衍生物的药物组合物及其制备方法。本发明特别涉及通式（I）的新型苯基嘧啶胺衍生物。式1的新化合物可用于治疗慢性骨髓性白血病（CML）。由于IC50; 这些分子的191个值在0.1至10.0nm的范围内，这些新化合物潜在地可用于治疗CML。

6. 发明申请

US20090227611A1 CRYSTAL FORM OF PHENYLAMINO PYRIMIDINE DERIVATIVES 有权
标题翻译：苯甲酰基吡嗪衍生物的晶体形式
公开(公告)号：US20090227611A1
公开(公告)日：2009-09-10
申请号：US12042247
申请日：2008-03-04
申请人： Amala kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
发明人： Amala kishan Kompella , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/506 , C07D401/04
CPC分类号： C07D401/04 , A61K31/506
摘要： The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN-019, is:
摘要翻译：本发明涉及（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（式I）的具体形式，方法用于制备它们，含有这种晶形的药物组合物，以及它们在人体中作为抗肿瘤剂的用途。式I化合物，也称为AN-019，是：

7. 发明授权

US08735415B2 Acid addition salts of (3,5-Bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide 有权
标题翻译：（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺的酸加成盐
公开(公告)号：US08735415B2
公开(公告)日：2014-05-27
申请号：US13289762
申请日：2011-11-04
申请人： Amala Kishan Kompella , Sreenivas Rachakonda , Bhujanga rao Adibhatla Kali Satya , Venkaiah Chowdary Nannapaneni
发明人： Amala Kishan Kompella , Sreenivas Rachakonda , Bhujanga rao Adibhatla Kali Satya , Venkaiah Chowdary Nannapaneni
IPC分类号： C07D401/04 , A61K31/506
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): Development Code—AN019 The invention also relates to processes for the preparation these acid addition salts and to their use as anti tumor agent in humans.
摘要翻译：本发明涉及药物活性化合物（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（I）的酸加成盐：发明代码AN019本发明还涉及制备这些酸加成盐的方法及其在人体中作为抗肿瘤剂的用途。

8. 发明授权

US08183253B2 Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase 有权
标题翻译：作为bcr-abl激酶抑制剂的苯基氨基嘧啶衍生物
公开(公告)号：US08183253B2
公开(公告)日：2012-05-22
申请号：US12042235
申请日：2008-03-04
申请人： Amala Kishan Kompella , Bhujanga Rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
发明人： Amala Kishan Kompella , Bhujanga Rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary
IPC分类号： A01N43/54 , A61K31/505 , C07D401/00
CPC分类号： C07C323/62 , C07C233/66 , C07C279/18 , C07C317/44 , C07D213/82 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel phenylaminopyrimidine derivatives, pharmaceutical compositions containing the novel phenylaminopyrimidine derivatives, and processes for their preparation. These compounds are candidates for the treatment of chronic myeloid leukemia.
摘要翻译：本发明涉及新的苯基氨基嘧啶衍生物，含有新的苯基氨基嘧啶衍生物的药物组合物及其制备方法。这些化合物是治疗慢性骨髓性白血病的候选药物。

9. 发明申请

US20120077833A1 ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]-BENZAMIDE 有权
标题翻译：（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 吡啶基-2亚氨基） - 苯基] - 苯甲酰胺的添加量
公开(公告)号：US20120077833A1
公开(公告)日：2012-03-29
申请号：US13289762
申请日：2011-11-04
申请人： Amala Kishan KOMPELLA , Sreenivas Rachakonda , Bhujanga rao Adibhatla Kali Satya , Venkaiah Chowdary Nannapaneni
发明人： Amala Kishan KOMPELLA , Sreenivas Rachakonda , Bhujanga rao Adibhatla Kali Satya , Venkaiah Chowdary Nannapaneni
IPC分类号： A61K31/506 , A61P35/02 , A61P35/00 , C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): Development Code—AN019 The invention also relates to processes for the preparation these acid addition salts and to their use as anti tumor agent in humans.
摘要翻译：本发明涉及药物活性化合物（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（I）的酸加成盐：发明代码AN019本发明还涉及制备这些酸加成盐的方法及其在人体中作为抗肿瘤剂的用途。

10. 发明申请

US20110190328A1 ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]-BENZAMIDE 审中-公开
标题翻译：（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 吡啶基-2亚氨基） - 苯基] - 苯甲酰胺的添加量
公开(公告)号：US20110190328A1
公开(公告)日：2011-08-04
申请号：US13053908
申请日：2011-03-22
申请人： Amala Kishan Kompella , Sreenivas Rachakonda , Kali Satya Bhujanga Rao ADIBHATLA , Venkaiah Chowdary Nannapaneni
发明人： Amala Kishan Kompella , Sreenivas Rachakonda , Kali Satya Bhujanga Rao ADIBHATLA , Venkaiah Chowdary Nannapaneni
IPC分类号： A61K31/506 , C07D401/04 , A61P35/02 , A61P35/04
CPC分类号： A61K31/506 , C07D401/04
摘要： The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I): The invention also relates to processes for the preparation these acid addition salts and to their use as anti tumor agent in humans.
摘要翻译：本发明涉及药物活性化合物（3,5-双三氟甲基）-N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺（I）的酸加成盐：本发明还涉及制备这些酸加成盐的方法及其在人体中作为抗肿瘤剂的用途。

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