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1. 发明授权

US07579491B2 Process for preparing brevifoliol 有权
标题翻译：短纤维酚的制备方法
公开(公告)号：US07579491B2
公开(公告)日：2009-08-25
申请号：US11548166
申请日：2006-10-10
申请人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Arvind Singh Negi , Ranganathan Santha Kumar Tirupadiripuliyur , Ankur Garg , Suman Preet Singh Khanuja
发明人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Arvind Singh Negi , Ranganathan Santha Kumar Tirupadiripuliyur , Ankur Garg , Suman Preet Singh Khanuja
IPC分类号： C07D305/00 , A61K36/13
CPC分类号： C07C67/56 , C07C2603/30 , C07C69/78
摘要： The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula I from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40° C. and then. concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50° C. for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.
摘要翻译：本发明提供了一种通过首先用醇优选在20-40℃的温度下提取植物的干燥和粉碎的叶来生产属于紫杉属的植物的式I的抗癌紫杉烷类短纤维醇的方法 C.然后。浓缩溶剂以获得醇提取物。然后将所得醇提物用吸附剂吸附，然后将所得吸附材料在20-50℃的温度范围内干燥4-48小时。然后将干燥的吸附材料用脂肪族溶剂和氯化溶剂的组合连续萃取并浓缩，得到残余物。使用柱色谱法如硅胶，佛罗里达和硅酸对残余物进行粗分馏，然后用合适的吸附剂进行色谱以得到短纤维醇。

2. 发明授权

US06437154B1 Process for the preparation of 10-deacetylbaccatin III 失效
标题翻译：制备10-脱乙酰基浆果赤霉素III的方法
公开(公告)号：US06437154B1
公开(公告)日：2002-08-20
申请号：US09963768
申请日：2001-09-28
申请人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Vijay Kumar Mehta
发明人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Vijay Kumar Mehta
IPC分类号： C07D30514
CPC分类号： C07D305/14
摘要： The present invention discloses a process for the conversion of a mixture of taxol analogues 7-xylosyl-10-deacetylbaccatin taxols of the formula 2 where R is C6H5, CH3C═CHCH3 or C5H11 into 10-deacetylbaccatin III of the formula 1 by dissolving the taxol analogue of formula 2 in a polar solvent, reacting the resultant solution with a base at a temperature of 20-50° C. for a time period in the range of 20-40 hours, and isolating 7-xyloxyl-10-deacetylbaccatin III, dissolving the 7-xylosyl-10-deacetylbaccatin III in a polar solvent, reacting the resultant solution with a periodate at 20-40° C. for a time period in the range of 20-40 hours to cleave the diol system of the xyloside into dialdehyde, treating the generated dialdehyde in an organic acid medium with salts of amine at 0-40° C. for 12-18 hours and isolating 10-deacetylbaccatin III of formula 1.
摘要翻译：本发明公开了一种将式2的紫杉醇类似物7-木糖基-10-脱乙酰基浆果赤霉素类紫杉醇的混合物，其中R为C6H5，CH3C = CHCH3或C5H11，转化为式1的10-脱乙酰基浆果赤霉素Ⅲ的方法，式2在极性溶剂中，使所得溶液与碱在20-50℃的温度下反应20-40小时的时间，并分离7-木糖基-10-脱乙酰基浆果赤霉素III，将 7-木糖基-10-脱乙酰基浆果赤霉素III在极性溶剂中，使所得溶液与20-40℃的高碘酸盐反应20-40小时的时间段，将木糖苷的二醇体系切割成二醛，在有机酸介质中用胺的盐在0-40℃处理生成的二醛12-18小时，并分离出式1的10-脱乙酰基浆果赤霉素III。

3. 发明申请

US20080039641A1 PROCESS FOR PREPARING BREVIFOLIOL 有权
标题翻译：制备BREVIFOLIOL的方法
公开(公告)号：US20080039641A1
公开(公告)日：2008-02-14
申请号：US11548166
申请日：2006-10-10
申请人： Sunil Chattopadhyay , Sachin Srivastava , Arvind Negi , Ranganathan Tirupadiripuliyur , Ankur Garg , Suman Khanuja
发明人： Sunil Chattopadhyay , Sachin Srivastava , Arvind Negi , Ranganathan Tirupadiripuliyur , Ankur Garg , Suman Khanuja
IPC分类号： C07D305/00
CPC分类号： C07C67/56 , C07C2603/30 , C07C69/78
摘要： The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula I from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40° C. and then. concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50° C. for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.
摘要翻译：本发明提供了一种通过首先用醇优选在20-40℃的温度下提取植物的干燥和粉碎的叶来生产属于紫杉属的植物的式I的抗癌紫杉烷类短纤维醇的方法 C.然后。浓缩溶剂以获得醇提取物。然后将所得醇提物用吸附剂吸附，然后将所得吸附材料在20-50℃的温度范围内干燥4-48小时。然后将干燥的吸附材料用脂肪族溶剂和氯化溶剂的组合连续萃取并浓缩，得到残余物。使用柱色谱法如硅胶，佛罗里达和硅酸对残余物进行粗分馏，然后用合适的吸附剂进行色谱以得到短纤维醇。

4. 发明授权

US06676976B2 Process for the production of vasicine 失效
标题翻译：生产vasicine的过程
公开(公告)号：US06676976B2
公开(公告)日：2004-01-13
申请号：US10104765
申请日：2002-03-21
申请人： Sunil Kumar Chattopadhyay , Guru Das Bagchi , Prem Dutt Dwivedi , Sachin Srivastava
发明人： Sunil Kumar Chattopadhyay , Guru Das Bagchi , Prem Dutt Dwivedi , Sachin Srivastava
IPC分类号： A61K3578
CPC分类号： C07D487/04
摘要： The present invention relates to an improved process for the production of vasicine of formula (1) from the Adhatoda vasica, said process comprising the steps of: extracting the dried and pulverized leaves with an alcoholic extract at an ambient temperature, concentrating the alcoholic extract to obtain a concentrated extract, treating and stirring extract with an aqueous organic acid for 2-24 hours, extracting the acid solution of with an organic solvent, separating the organic layer and aqueous acidic layer, basifying the aqueous acidic solution with a base, extracting the basified solution with an organic solvent, separating the organic layer, drying and filtering, evaporating the organic layer to obtain an amorphous residue, and treating the amorphous residue with an organic solvent or mixture of organic solvents to obtain vasicine.
摘要翻译：本发明涉及一种用于从Adhatoda vasica生产式（1）的维生素的改进方法，所述方法包括以下步骤：在室温下用醇提取物萃取干燥和粉碎的叶子，将醇提取物浓缩获得浓缩提取物，用有机酸水溶液处理和搅拌提取物2-24小时，用有机溶剂萃取酸溶液，分离有机层和酸性水层，用碱将酸性水溶液碱化，提取碱性溶液与有机溶剂分离，分离有机层，干燥和过滤，蒸发有机层，得到无定形残渣，用有机溶剂或有机溶剂混合物处理无定形残余物，得到vasicine。

5. 发明授权

US06384246B1 Process for the preparation of maltol from plants belonging to the genus Abies 失效
标题翻译：从属于Abies属的植物制备麦芽酚的方法
公开(公告)号：US06384246B1
公开(公告)日：2002-05-07
申请号：US09792030
申请日：2001-02-26
申请人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Koneni Venkata Sashidhara , Vinayah Tripathi , Sushil Kumar
发明人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Koneni Venkata Sashidhara , Vinayah Tripathi , Sushil Kumar
IPC分类号： C07D30940
CPC分类号： C07D309/40
摘要： A process has been developed for production of a food flavoring compound maltol which comprises (a) extracting the dried and pulverized leaves of the plants belonging to the genus Abies with an alcohol at 20-40° C. and concentrating the solvent to obtain an alcoholic extract, (b) adsorbing the alcoholic extract with an adsorbent and drying the adsorbed material at a temperature ranging between 20-50° C., (d) partitioning of the adsorbed material between selected solvents consisting of aliphatic hydrocarbon and chlorinated solvent successively, (d) concentrating the chlorinated solvent to a residue and crystallizing it from a suitable organic solvent or mixtures of such solvents to get pure maltol.
摘要翻译：已经开发了用于生产食品香料化合物麦芽酚的方法，其包括（a）在20-40℃下用醇在20-40℃下提取属于Abies属的植物的干燥和粉碎的叶子并浓缩溶剂以获得酒精提取物，（b）用吸附剂吸附醇提取物并在20-50℃的温度范围内干燥吸附的材料，（d）连续地将由脂族烃和氯化溶剂组成的选定溶剂之间的吸附材料分配（（ d）将氯化溶剂浓缩至残余物并将其从合适的有机溶剂或这些溶剂的混合物中结晶得到纯的麦芽酚。

6. 发明授权

US06372922B1 Process for the production of (−) 3,4-divanillyl tetrahydrofuran 失效
标题翻译：生产（ - ）3,4-二苯乙烯基四氢呋喃的方法
公开(公告)号：US06372922B1
公开(公告)日：2002-04-16
申请号：US09818278
申请日：2001-03-27
申请人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Vinayak Tripathi
发明人： Sunil Kumar Chattopadhyay , Sachin Srivastava , Vinayak Tripathi
IPC分类号： C07D30712
CPC分类号： C07D307/12
摘要： The present invention relates to a process for the production of (−)3,4-divanillyl tetrahydrofiran of formula (2) which comprises (a) isolating) (−) secoisolariciresinol of formula (1) from the heartwood and roots of Taxus wallichiana by an improved process which consists of partitioning of the alcoholic extract of the heartwood and roots of T. wallichiana between water and chlorinated solvent, (b) extracting the chlorinated solvent extract with alkali and (c) isolating (−) secoisolariciresinol from the alkali extract upon neutralization with mineral acid and extracting with organic solvent and (d) crystallizing it from suitable organic solvent, (e) dissolving the isolated (−) secoisolariciresinol in suitable organic solvent and (f) reacting with triphenyl phosphine halide at 0-80° C. for 1-10 hours and (g) isolating (−) 3,4-divanillyl tetrahydrofuran by column chromatography.
摘要翻译：本发明涉及一种制备式（2）的（ - ）3,4-二氢化茚基四氢呋喃的方法，其包括（a）从红豆杉的心材和根中分离出（ - ）式（1）的（ - ）间二异硫氰菊酯一种改进的方法，其包括在水和氯化溶剂之间分配心材的木材和根的酒精提取物，（b）用碱提取氯化溶剂提取物，和（c）从碱提取物中分离（ - ）二硫代亚铁氰菊酯，用无机酸中和并用有机溶剂萃取，（d）从合适的有机溶剂中结晶，（e）将分离的（ - ）二异硫氰酸酯溶解在合适的有机溶剂中，和（f）在0-80℃与三苯基膦卤化物反应（g）通过柱色谱法分离（ - ）3,4-二苯乙烯基四氢呋喃。

7. 发明申请

US20100310870A1 AMORPHOUS BAZEDOXIFENE ACETATE AND PREPARATION THEREOF 审中-公开
标题翻译：无定形乙酸异丙酯及其制备方法
公开(公告)号：US20100310870A1
公开(公告)日：2010-12-09
申请号：US12724432
申请日：2010-03-16
申请人： Shankar Sanganabhatla , Sachin Srivastava , Dinesh Bansilal Deore , Anthony Melvin Crasto , Mubeen Ahmed Khan
发明人： Shankar Sanganabhatla , Sachin Srivastava , Dinesh Bansilal Deore , Anthony Melvin Crasto , Mubeen Ahmed Khan
IPC分类号： B32B5/00 , C07D403/12
CPC分类号： C07D403/12 , Y10T428/2982
摘要： The present invention relates to amorphous form of bazedoxifene acetate and a process for the preparation thereof.
摘要翻译：本发明涉及无定形形式的巴多昔芬乙酸盐及其制备方法。

8. 发明申请

US20060052463A1 PROCESS FOR REGIOSELECTIVE DEMETHYLATION OF P-METHOXY GROUP IN PHENOLIC ESTER AND DIARYL KETONE MOIETIES 失效
标题翻译：酚羟基和二硫代酮酮中P-甲氧基的选择性脱乙酰化方法
公开(公告)号：US20060052463A1
公开(公告)日：2006-03-09
申请号：US10937096
申请日：2004-09-08
申请人： Arvind Negi , Sunil Chattopadhyay , Sachin Srivastava , Asish Bhattacharya
发明人： Arvind Negi , Sunil Chattopadhyay , Sachin Srivastava , Asish Bhattacharya
IPC分类号： C07D491/14 , C07C27/06 , C07C65/21 , C07C69/76
CPC分类号： C07D459/00 , C07C67/31 , C07C69/92
摘要： Demethylation of 3′,4′-dimethoxy or 3′,4′,5′-trimethoxy benzoic ester of a phenol is carried out in the presence of an excess of aluminum halide in an organic solvent to get 4′-Hydroxy, 3′-methoxy or 4′ hydroxy, 3′,5′-dimethoxy benzoic acid ester of a phenol. The reaction is also applicable to 3′,4′,5′-trimethoxy diaryl ketone and some natural products like reserpine.
摘要翻译：苯酚3'，4'-二甲氧基或3'，4'，5'-三甲氧基苯甲酸酯的脱甲基化在过量的卤化铝在有机溶剂中的存在下进行，得到4'-羟基，3' - 甲氧基或4'羟基，3'，5'-二甲氧基苯甲酸酯。该反应也适用于3'，4'，5'-三甲氧基二芳基酮和一些天然产物如利血平。

9. 发明授权

US09353114B2 Process for the preparation of dipeptidylpeptidase inhibitors 有权
标题翻译：二肽基肽酶抑制剂的制备方法
公开(公告)号：US09353114B2
公开(公告)日：2016-05-31
申请号：US14421896
申请日：2013-08-06
申请人： Sunil Kumar Singh , Sachin Srivastava , Shekhar Bhaskar Bhirud
发明人： Sunil Kumar Singh , Sachin Srivastava , Shekhar Bhaskar Bhirud
IPC分类号： C07D401/04 , C07D473/06 , C07D473/04
CPC分类号： C07D473/18 , C07C69/78 , C07D401/04 , C07D473/04 , C07D473/06
摘要： Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyi, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.
摘要翻译：本发明提供制备式I的利格列汀的方法，其包括使式II化合物脱保护，其中R 1和R 2与它们所连接的氮一起形成苯二甲酰亚氨基，其中苯二酰亚氨基的芳环被一个或更多选自卤素，烷基，硝基和氨基的R3取代基; 或R 1为H且R 2选自三烷基甲硅烷基，2-三烷基硅烷基乙氧基氨基甲酸酯，乙酰基，三卤代乙酰基，9-芴基甲氧基羰基，三苯甲基，烷基磺酰基，芳基磺酰基，二苯基膦和磺酰基乙氧基羰基。

10. 发明授权

US07196115B2 Pharmaceutical composition containing brevifoliol for use in chemotherapeutic treatment of human beings, method therefor 失效
标题翻译：含有短寿菌酚的药物组合物，用于化疗人类的治疗方法
公开(公告)号：US07196115B2
公开(公告)日：2007-03-27
申请号：US10334675
申请日：2002-12-30
申请人： Suman Preet Singh Khanuja , Ranganathan Santha Kumar Tirupadiripuliyur , Ankur Garg , Raghvendra Kumar Mishra , Sunil Kumar Chattopadhyay , Sachin Srivastava , Arvind Singh Negi
发明人： Suman Preet Singh Khanuja , Ranganathan Santha Kumar Tirupadiripuliyur , Ankur Garg , Raghvendra Kumar Mishra , Sunil Kumar Chattopadhyay , Sachin Srivastava , Arvind Singh Negi
IPC分类号： A61K3/21 , A61K31/335
CPC分类号： A61K31/235
摘要： The present invention relates to the bioactivity of taxanes isolated from the leaves of Himalayan Yew tree Taxus wallichiana against human cancer cell lines grown in-vitro and subsequent identification of brevifoliol [1] as anticancer agent useful in the treatment of various types of cancer in humans
摘要翻译：本发明涉及从喜马拉雅红豆杉红豆杉叶片分离出的紫杉醇对体外生长的人类癌细胞系的生物活性，随后鉴定了作为可用于治疗人类各种癌症的抗癌剂的短纤维酚[1]

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