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1. 发明申请

WO2008102374A1 AMORPHOUS FORM OF DOCETAXEL 审中-公开
标题翻译： DOCETAXEL的不规则形式
公开(公告)号：WO2008102374A1
公开(公告)日：2008-08-28
申请号：PCT/IN2008/000098
申请日：2008-02-19
申请人： DABUR PHARMA LIMITED , MISHRA, Bhuwan, Bhaskar , VARDHAN, Anand , AGARWAL, Shiv, Kumar
发明人： MISHRA, Bhuwan, Bhaskar , VARDHAN, Anand , AGARWAL, Shiv, Kumar
IPC分类号： C07D305/14 , A61K31/337 , A61P35/00
CPC分类号： C07D305/14
摘要： A process for preparation of Amorphous Form of Docetaxel comprising: i. preparation of a solution or suspension of Docetaxel in an organic solvent or mixtures thereof; ii. evaporation of the solvent or mixtures thereof from the solution or suspension of step i ) under reduced pressure to obtain a solid substance; iii. optionally further dissolving or suspending the solid substance of step ii) in an organic solvent or mixtures thereof and evaporation of the solvent or mixtures thereof from the solution or suspension under reduced pressure to obtain a solid substance; iv. further optionally repeating step iii) one or more times; v. drying the solid substance obtained from step ii), iii) or iv) to give the amorphous form of Docetaxel. An amorphous form of docetaxel obtained by the process. A composition comprising amorphous form of Docetaxel along with pharmaceutically acceptable excipients adapted for therapy for cancer of various origins.
摘要翻译：一种制备多西紫杉醇无定型形式的方法，包括：i。多烯紫杉醇在有机溶剂或其混合物中的溶液或悬浮液的制备; II。将溶剂或其混合物从步骤i）的溶液或悬浮液中减压蒸发得到固体物质; III。任选地将步骤ii）的固体物质进一步溶解或悬浮在有机溶剂或其混合物中，并在减压下从溶液或悬浮液中蒸发溶剂或其混合物以获得固体物质; IV。进一步任选地重复步骤iii）一次或多次; v。干燥从步骤ii）获得的固体物质，iii）或iv）得到无定形形式的多西他赛。通过该方法获得的多西紫杉醇的无定形形式。包含无定形形式的多西他赛的组合物以及适于治疗各种癌症的药学上可接受的赋形剂。

2. 发明申请

WO2016199076A2 POLYMORPHIC FORMS OF AFATINIB FREE BASE AND AFATINIB DIMALEATE 审中-公开
标题翻译： AFATINIB自由基和AFATINIB DIMALEATE的多形态
公开(公告)号：WO2016199076A2
公开(公告)日：2016-12-15
申请号：PCT/IB2016/053420
申请日：2016-06-10
申请人： FRESENIUS KABI ONCOLOGY LTD. , CABRI, Walter , LAHIRI, Saswata , MISHRA, Bhuwan Bhaskar , AZIM, Abul , PANDA, Nilendu , BHAVANAM, Poli Reddy , RAY, Krishanu , KACHHADIA, Nikunj , SINGH, Kumber
发明人： CABRI, Walter , LAHIRI, Saswata , MISHRA, Bhuwan Bhaskar , AZIM, Abul , PANDA, Nilendu , BHAVANAM, Poli Reddy , RAY, Krishanu , KACHHADIA, Nikunj , SINGH, Kumber
IPC分类号： C07D407/12 , A61K31/517 , A61P35/00
CPC分类号： C07D407/12
摘要： The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
摘要翻译：本发明涉及阿片素及其二马来酸盐的结晶形式。本发明还涉及制备阿拉非尼及其二马来酸盐的结晶形式的方法。本发明进一步涉及这种阿伐他汀二马来酸的结晶形式的药物组合物及其在治疗有需要的患者中的用途。

3. 发明申请

WO2013065070A8 AMORPHOUS FORM OF CABAZITAXEL AND PROCESS FOR ITS PREPARATION 审中-公开
标题翻译： CABAZITAXEL的非晶形式及其制备方法
公开(公告)号：WO2013065070A8
公开(公告)日：2014-03-13
申请号：PCT/IN2012000706
申请日：2012-10-26
申请人： FRESENIUS KABI ONCOLOGY LTD , LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , OJHA VIJAY , PANDA NILENDU , SHUKLA SONU PRASAD
发明人： LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , OJHA VIJAY , PANDA NILENDU , SHUKLA SONU PRASAD
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： An Amorphous Form of Cabazitaxel is disclosed. It is preferably characterized by an X-ray powder diffraction (XRD) pattern as depicted in Fig-1. It is prepared by (a) preparing a solution of Cabazitaxel in a suitable solvent and mixture thereof; and (b) recovering the Amorphous Forms of Cabazitaxel from the solution thereof by removal of the solvent.
摘要翻译：公开了一种无定形形式的卡巴他赛。其优选特征在于如图1所示的X射线粉末衍射（XRD）图案。其制备方法是（a）将卡巴他赛的溶液制备在合适的溶剂及其混合物中; 和（b）通过除去溶剂从其溶液中回收无定形形式的卡巴他赛。

4. 发明申请

WO2013046223A1 AN IMPROVED PROCESS FOR THE PREPARATION OF BENDAMUSTINE HYDROCHLORIDE 审中-公开
标题翻译：一种改进溴苯菌胺氢氯化物制剂的改进方法
公开(公告)号：WO2013046223A1
公开(公告)日：2013-04-04
申请号：PCT/IN2012/000534
申请日：2012-07-31
申请人： FRESENIUS KABI ONCOLOGY LTD. , MISHRA, Bhuwan Bhaskar , KACHHADIA, Nikunj Shambhubhai , TOMAR, Vinod Singh , LAHIRI, Saswata
发明人： MISHRA, Bhuwan Bhaskar , KACHHADIA, Nikunj Shambhubhai , TOMAR, Vinod Singh , LAHIRI, Saswata
IPC分类号： C07D235/16 , A61K31/4184 , A61P35/00
CPC分类号： C07D235/16
摘要： The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1 -Methyl-5-[bis(2-chloroethyl)amino]- 1H-benzimidazol-2-yl]lithium butanoate of formula(V), both having a purity of ≥99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.
摘要翻译：本发明涉及一种用于合成苯达莫司汀的改进方法，特别是式（VI）的盐酸苯达莫司汀及其中间体1-甲基-5- [双（2-氯乙基）氨基] -1H-苯并咪唑-2-酮（V）的丁酸锂，其纯度> 99％，简单，方便，经济，不使用危险化学品和工业上可行的。

5. 发明申请

WO2016199076A3 POLYMORPHIC FORMS OF AFATINIB FREE BASE AND AFATINIB DIMALEATE 审中-公开
标题翻译： AFATINIB自由基和AFATINIB DIMALEATE的多形态
公开(公告)号：WO2016199076A3
公开(公告)日：2017-03-09
申请号：PCT/IB2016053420
申请日：2016-06-10
申请人： FRESENIUS KABI ONCOLOGY LTD , CABRI WALTER , LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , AZIM ABUL , PANDA NILENDU , BHAVANAM POLI REDDY , RAY KRISHANU , KACHHADIA NIKUNJ , SINGH KUMBER
发明人： CABRI WALTER , LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , AZIM ABUL , PANDA NILENDU , BHAVANAM POLI REDDY , RAY KRISHANU , KACHHADIA NIKUNJ , SINGH KUMBER
IPC分类号： C07D407/12 , A61K31/517 , A61P35/00
CPC分类号： C07D407/12
摘要： The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
摘要翻译：本发明涉及阿片素及其二马来酸盐的结晶形式。本发明还涉及制备阿拉非尼及其二马来酸盐的结晶形式的方法。本发明还涉及此类结晶形式的阿片素二马来酸二乙酯的药物组合物及其在治疗有需要的患者中的用途。

6. 发明申请

WO2013065070A1 AMORPHOUS FORM OF CABAZITAXEL AND PROCESS FOR ITS PREPARATION 审中-公开
标题翻译： CABAZITAXEL的非晶形式及其制备方法
公开(公告)号：WO2013065070A1
公开(公告)日：2013-05-10
申请号：PCT/IN2012/000706
申请日：2012-10-26
申请人： FRESENIUS KABI ENCOLOGY LTD. , LAHIRI, Saswata , MISHRA, Bhuwan Bhaskar , OJHA, Vijay , PANDA, Nilendu , SHUKLA, Sona Prasad
发明人： LAHIRI, Saswata , MISHRA, Bhuwan Bhaskar , OJHA, Vijay , PANDA, Nilendu , SHUKLA, Sona Prasad
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： An Amorphous Form of Cabazitaxel is disclosed. It is preferably characterized by an X-ray powder diffraction (XRD) pattern as depicted in Fig-1. It is prepared by (a) preparing a solution of Cabazitaxel in a suitable solvent and mixture thereof; and (b) recovering the Amorphous Forms of Cabazitaxel from the solution thereof by removal of the solvent.
摘要翻译：公开了一种无定形形式的卡巴他赛。其优选特征在于如图1所示的X射线粉末衍射（XRD）图案。其制备方法是（a）将卡巴他赛的溶液制备在合适的溶剂及其混合物中; 和（b）通过除去溶剂从其溶液中回收无定形形式的卡巴他赛。

7. 发明申请

WO2013069027A9 PROCESSES FOR THE PREPARATION OF CABAZITAXEL INVOLVING C(7) -OH AND C(13) -OH SILYLATION OR JUST C(7) -OH SILYLATION 审中-公开
标题翻译：制备涉及C（7）-OH和C（13）-OH苯甲酰化或仅C（7）-OH苯甲酰化的卡巴他赛的方法
公开(公告)号：WO2013069027A9
公开(公告)日：2013-10-17
申请号：PCT/IN2012000630
申请日：2012-09-21
申请人： FRESENIUS KABI ONCOLOGY LTD , LAHIRI SASWATA , GUPTA NITIN , AZIM ABUL , PANDA NILENDU , MISHRA BHUWAN BHASKAR , SANGHANI SUNIL
发明人： LAHIRI SASWATA , GUPTA NITIN , AZIM ABUL , PANDA NILENDU , MISHRA BHUWAN BHASKAR , SANGHANI SUNIL
IPC分类号： C07D305/14 , A61K31/335
CPC分类号： C07F7/1856 , C07D305/14
摘要： Disclosed are processes towards Cabazitaxel (I) starting from 10-Deacetylbaccatin (III) that involve steps of either 7-OH monosilylation (passing through formula V) or 7,13-disilylation (passing through formulae XI, XII). Isopropanol Solvates of Cabazitaxel and processes to make this are also described.
摘要翻译：公开了从10-脱乙酰浆果赤霉素（III）开始的涉及卡巴他赛（I）的方法，其涉及7-OH单甲硅烷基化（通过式V）或7,13-二甲硅烷基化（通过式XI，XII）的步骤。也描述了卡巴他赛的异丙醇溶剂化物和制备它的方法。

8. 发明申请

WO2013069027A1 PROCESSES FOR THE PREPARATION OF CABAZITAXEL INVOLVING C(7) -OH AND C(13) -OH SILYLATION OR JUST C(7) -OH SILYLATION 审中-公开
标题翻译：涉及C（7）-OH和C（13）-OH硅烷的CABAZITAXEL的制备方法或者只是C（7）-OH硅烷化
公开(公告)号：WO2013069027A1
公开(公告)日：2013-05-16
申请号：PCT/IN2012/000630
申请日：2012-09-21
申请人： FRESENIUS KABI ONCOLOGY LTD. , LAHIRI, Saswata , GUPTA, Nitin , AZIM, Abul , PANDA, Nilendu , MISHRA, Bhuwan Bhaskar , SANGHANI, Sunil
发明人： LAHIRI, Saswata , GUPTA, Nitin , AZIM, Abul , PANDA, Nilendu , MISHRA, Bhuwan Bhaskar , SANGHANI, Sunil
IPC分类号： C07D305/14 , A61K31/335
CPC分类号： C07F7/1856 , C07D305/14
摘要： Disclosed are processes towards Cabazitaxel (I) starting from 10-Deacetylbaccatin (III) that involve steps of either 7-OH monosilylation (passing through formula V) or 7,13-disilylation (passing through formulae XI, XII). Isopropanol Solvates of Cabazitaxel and processes to make this are also described.
摘要翻译：公开了从10-脱乙酰基浆果赤霉素（III）开始的涉及卡巴他昔（I）的方法，其涉及7-OH单甲硅烷基化（通过式V）或7,13-二甲硅烷基化（通过式XI，XII）的步骤。异丙醇卡巴他赛的溶剂化物及其制备方法也被描述。

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