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1. 发明授权

US08841466B2 Series of artemisinin derivatives and process for preparation thereof 有权
标题翻译：青蒿素衍生物系列及其制备方法
公开(公告)号：US08841466B2
公开(公告)日：2014-09-23
申请号：US13574440
申请日：2011-01-20
申请人： Gakul Baishya , Nabin Chandra Barua , Abhishek Goswami , Partha Pratim Saikia , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri , Madhunika Sharma
发明人： Gakul Baishya , Nabin Chandra Barua , Abhishek Goswami , Partha Pratim Saikia , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri , Madhunika Sharma
IPC分类号： C07D321/00
CPC分类号： C07D493/18
摘要： This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2-[10′β-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin. These highly functionalized artemisinin derivatives embodied in this document are found to be active against various cancer cell-lines.
摘要翻译：本发明涉及某些新颖的鸟氨酸衍生的醛2- [10'和bgr-脱氧生物素基] - 乙醛的Baylis-Hillman加合物的合成。使用Baylis-Hillman反应在一个步骤中将三个官能团引入分子的能力促使我们合成了一些高度官能化的青蒿素衍生物。发现本文件中体现的这些高度功能化的青蒿素衍生物对各种癌细胞系具有活性。

2. 发明申请

US20130030044A1 NEW SERIES OF ARTEMISININ DERIVATIVES AND PROCESS FOR PREPARATION THEREOF 有权
标题翻译：新系列的阿司匹林衍生物及其制备方法
公开(公告)号：US20130030044A1
公开(公告)日：2013-01-31
申请号：US13574440
申请日：2011-01-20
申请人： Gakul Baishya , Nabin Chandra Barua , Abhishek Goswami , Partha Pratim Saikia , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri , Madhunika Sharma
发明人： Gakul Baishya , Nabin Chandra Barua , Abhishek Goswami , Partha Pratim Saikia , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri , Madhunika Sharma
IPC分类号： C07D493/18 , A61P35/00 , A61K31/357
CPC分类号： C07D493/18
摘要： This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2[10′β-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin. These highly functionalized artemisinin derivatives embodied in this document are found to be active against various cancer cell-lines
摘要翻译：本发明涉及某些新颖的鸟氨酸衍生的醛2 [10'和bgr-脱氧生物素基] - 乙醛的Baylis-Hillman加合物的合成。使用Baylis-Hillman反应在一个步骤中将三个官能团引入分子的能力促使我们合成了一些高度官能化的青蒿素衍生物。发现本文件中体现的这些高度功能化的青蒿素衍生物对各种癌细胞系具有活性

3. 发明申请

US20130331581A1 1,2,3-TRIAZOLE CONTAINING ARTEMISININ COMPOUNDS AND PROCESS FOR PREPARATION THEREOF 有权
标题翻译：含有亚胺嘧啶的1,2,3-三唑化合物及其制备方法
公开(公告)号：US20130331581A1
公开(公告)日：2013-12-12
申请号：US13985527
申请日：2012-02-14
申请人： Bishwajit Saikia , Nabin Chandra Barua , Partha Pratim Saikia , Abhishek Goswami , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri
发明人： Bishwajit Saikia , Nabin Chandra Barua , Partha Pratim Saikia , Abhishek Goswami , Paruchuri Gangadhar Rao , Ajit Kumar Saxena , Nitasha Suri
IPC分类号： C07D493/18
CPC分类号： C07D493/18
摘要： The present invention relates to 1,2,3-triazole containing artemisinin compounds and process for preparation thereof. Described herein is the synthesis, bioassay results and usefulness of the artemisinin derived compounds resulting from 1,3-di-polar cycloaddition reaction of artemisinin derived azide or alkyne with aliphatic or aromatic diazides. These 1,2,3-triazole containing artemisinin derived compounds embodied in this document are found to be active against various cancer cell-lines.
摘要翻译：本发明涉及含有青蒿素的1,2,3-三唑化合物及其制备方法。本文描述了由青蒿素衍生的叠氮化物或炔烃与脂肪族或芳族二叠氮化物的1,3-二极性环加成反应产生的青蒿素衍生化合物的合成，生物测定结果和有用性。发现本文中实施的这些含有青蒿素的青蒿素衍生化合物的1,2,3-三唑对各种癌细胞系具有活性。

4. 发明申请

US20150328170A1 SYNERGISTIC PHARMACEUTICAL COMPOSITION USEFUL FOR THE TREATMENT OF LUNG CANCER 有权
标题翻译：用于治疗肺癌的协调药物组合物
公开(公告)号：US20150328170A1
公开(公告)日：2015-11-19
申请号：US14410844
申请日：2012-09-05
申请人： Mantu Bhuyan , Pranab Ram Bhattacharyya , Pranab Kumar Baruah , Nabin Chandra Barua , Paruchuri Gangadhar Rao , Sushmita Bhattacharya , Rakesh Kundu , Priyajit Chatterjee , Soma Seal , Sandeep Mukherjee , Suman Dasgupta , Sudipta Moitra , Shelley Bhattacharya , Samir Bhattacharya
发明人： Mantu Bhuyan , Pranab Ram Bhattacharyya , Pranab Kumar Baruah , Nabin Chandra Barua , Paruchuri Gangadhar Rao , Sushmita Bhattacharya , Rakesh Kundu , Priyajit Chatterjee , Soma Seal , Sandeep Mukherjee , Suman Dasgupta , Sudipta Moitra , Shelley Bhattacharya , Samir Bhattacharya
IPC分类号： A61K31/045 , A61K36/54
CPC分类号： A61K31/045 , A61K36/54 , A61K2300/00
摘要： The present invention relates to a synergistic pharmaceutical composition comprising Compound C2 (Neo-isopulegol), C3 (Iso-pulegol) and C4 (Citronellol) derived from herbal seed extract of Litsea cubeba useful for the treatment of lung cancer. The present invention also relates to the activity of compounds C2 or C3 or C4 either alone or in combination in killing of A549 lung cancer cells.
摘要翻译：本发明涉及一种协同药物组合物，其包含衍生自用于治疗肺癌的Litsea cubeba的草药种子提取物的化合物C2（新 - 异胡耳），C3（异丁胺）和C4（香茅醇））。本发明还涉及化合物C2或C3或C4单独或组合杀死A549肺癌细胞的活性。

5. 发明授权

US08513226B2 Simultaneous method for the preparation of a mixture of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene and 3-acetoxy-2'-chloro-5-androsteno[17,16-b]pyridine 有权
标题翻译：制备3-乙酰氧基-17-乙酰氨基-16-甲酰基 - 雄甾-5,17-二烯和3-乙酰氧基-2'-氯-5-雄甾烷[17,16-b]吡啶的混合物的同时方法
公开(公告)号：US08513226B2
公开(公告)日：2013-08-20
申请号：US12935877
申请日：2009-03-26
申请人： Romesh Chandra Boruah , Moyurima Borthakur , Madan Gopal Barthakur , Paruchuri Gangadhar Rao , Sudip Kumar Kar , Annalakshmi Chinniah , Suchandra Goswami , Pratap Kumar Das
发明人： Romesh Chandra Boruah , Moyurima Borthakur , Madan Gopal Barthakur , Paruchuri Gangadhar Rao , Sudip Kumar Kar , Annalakshmi Chinniah , Suchandra Goswami , Pratap Kumar Das
IPC分类号： A61K31/565
CPC分类号： C07J71/0052 , A61K31/568 , C07J13/005 , C07J41/0005 , C07J41/005
摘要： The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2′-chloro-5-androsteno[17,16-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1 g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.
摘要翻译：本发明涉及3-乙酰氧基-17-乙酰氨基-16-甲酰基 - 雄甾-5,17-二烯（4）和3-乙酰氧基-2'-氯-5-雄甾烷[17,16-b] 吡啶（5）作为胃质子泵抑制剂，与奥美拉唑相比较，临床上使用的抗胃溃疡药物。化合物（4）在胃壁细胞中显示剂量依赖性抑制组胺刺激的酸分泌，其IC50值与西咪替丁相当。在单剂量水平的1g / Kg体重的化合物（4）下，没有观察到瑞士白化病小鼠的死亡率或行为异常。化合物（4）在体内进一步表现出抗吲哚美辛诱导的溃疡的优异的抗溃疡活性。

6. 发明申请

US20130131350A1 PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF 失效
标题翻译：吡啶-2YL硫酸酯及其制备方法
公开(公告)号：US20130131350A1
公开(公告)日：2013-05-23
申请号：US13811090
申请日：2011-07-20
申请人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
发明人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
IPC分类号： C07D213/70
CPC分类号： C07D213/70
摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
摘要翻译：本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血，作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。

7. 发明授权

US06935144B2 Device for leather processing 失效
标题翻译：皮革加工设备
公开(公告)号：US06935144B2
公开(公告)日：2005-08-30
申请号：US10393388
申请日：2003-03-20
申请人： Duraiswamy Lakshmanan , Bommya Thangaraj , Subramaniyam Krishnan , Natesan Samivelu , Paruchuri Gangadhar Rao , Thirumalachari Ramasami
发明人： Duraiswamy Lakshmanan , Bommya Thangaraj , Subramaniyam Krishnan , Natesan Samivelu , Paruchuri Gangadhar Rao , Thirumalachari Ramasami
IPC分类号： C14C15/00 , C14C1/00
CPC分类号： C14C15/00
摘要： An improved device for leather processing comprising a vessel containing perforated dummy doors and compartments with pegs as well as friction disk fixed along the exterior periphery of the vessel. The leathers to be wet processed are subjected to mechanical action in terms of both rocking action as well as rotational movement simultaneously. The perpetual motion of the device help to create pressure generation for quickening the process and for addition of chemical solution continuously. The processing takes place under pressure generated inside the vessel and with the support of multiple mechanical actions, resulting in higher exhaustion of bath with less processing time and energy requirement and higher capacity utilization to produce good quality leather.
摘要翻译：一种用于皮革加工的改进装置，包括容纳穿孔假门的容器和具有钉的隔室以及沿着容器的外周固定的摩擦盘。要湿润处理的皮革在摇摆作用和旋转运动同时受到机械作用。该装置的永久运动有助于产生压力，以加快过程和不断添加化学溶液。该加工在容器内部产生的压力下进行，并具有多次机械作用的支撑，导致较少的浴槽耗尽，处理时间和能量需求较少，并且产生较高的产能利用率以生产出优质皮革。

8. 发明授权

US08912357B2 Method for the extraction of shikimic acid 有权
标题翻译：提取莽草酸的方法
公开(公告)号：US08912357B2
公开(公告)日：2014-12-16
申请号：US13583315
申请日：2011-03-09
申请人： Manobjyoti Bordoloi , Jayanta Borah , Dipak Kumar Roy , Subhash Chandra Dutta , Nabin Chandra Baruah , Paruchuri Gangadhar Rao
发明人： Manobjyoti Bordoloi , Jayanta Borah , Dipak Kumar Roy , Subhash Chandra Dutta , Nabin Chandra Baruah , Paruchuri Gangadhar Rao
IPC分类号： C07C51/47 , C07C51/43 , C07C51/44
CPC分类号： C07C51/44 , C07C51/43 , C07C51/47 , C07C57/04 , C07C62/32
摘要： This invention is directed to the production of shikimic acid from Illicium griffithii fruits. The method according to the invention is particularly applicable to the isolation of shikimic acid from Illicium griffithii fruits (seeds and pericarps). Yield is 12-18% w/w. Shikimic acid is useful as raw material for the production of oseltavir (Tamiflu) used against Avian Flu. It is also reported that its triacyl derivatives can inhibit blood platelet assembling and Thrombosis by affecting the metabolism of Arachidonic acid. Hitherto known commercial methods of production of shikimic acid from the fruits of star anise (Illicium verum) and sweet gum (Liquidambar styraciflua) gives only 3-7% and 1.5% respectively. The price of shikimic acid in the international market varies from US$ 45.00 to 1000.00 per Kg depending on demand. Further as per report published at the website www.livemint.com, China Government has imposed restriction on export of shikimic acid.
摘要翻译：本发明涉及从葛根果实生产莽草酸。根据本发明的方法特别适用于从sh藜果实（种子和浸膏）中分离莽草酸。产量为12-18％w / w。莽草酸可用作生产用于抗禽流感的奥司他唑（Tamiflu）的原料。据报道，其三酰基衍生物可通过影响花生四烯酸的代谢来抑制血小板聚集和血栓形成。迄今已知的从八角果实（Illicium verum）和甜口香糖（Liquidambar styraciflua）的果实生产莽草酸的商业方法分别仅分别为3-7％和1.5％。莽敌酸在国际市场的价格从45.00美元到1000.00 / Kg，取决于需求。进一步根据网站www.livemint.com发布的报告，中国政府对莽草酸出口实行限制。

9. 发明申请

US20110028440A1 Simultaneous Method for the Preparation of a Mixture of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene and 3-acetoxy-2'-chloro-5-androsteno[17,16-b]pyridine 有权
标题翻译：制备3-乙酰氧基-17-乙酰氨基-16-甲酰基 - 雄甾-5,17-二烯和3-乙酰氧基-2'-氯-5-雄甾烷[17,16-b]吡啶的混合物的同时方法
公开(公告)号：US20110028440A1
公开(公告)日：2011-02-03
申请号：US12935877
申请日：2009-03-26
申请人： Romesh Chandra Boruah , Moyurima Borthkur , Madan Gopal Barthakur , Paruchuri Gangadhar Rao , Sudip Kumar Kar , Annalaxmi Chinniah , Suchandra Goswami , Pratap Kumar Das
发明人： Romesh Chandra Boruah , Moyurima Borthkur , Madan Gopal Barthakur , Paruchuri Gangadhar Rao , Sudip Kumar Kar , Annalaxmi Chinniah , Suchandra Goswami , Pratap Kumar Das
IPC分类号： A61K31/568 , A61P1/04
CPC分类号： C07J71/0052 , A61K31/568 , C07J13/005 , C07J41/0005 , C07J41/005
摘要： The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2′-chloro-5-androsteno[17,16-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1 g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.
摘要翻译：本发明涉及3-乙酰氧基-17-乙酰氨基-16-甲酰基 - 雄甾-5,17-二烯（4）和3-乙酰氧基-2'-氯-5-雄甾烷[17,16-b] 吡啶（5）作为胃质子泵抑制剂，与奥美拉唑相比较，临床上使用的抗胃溃疡药物。化合物（4）在胃壁细胞中显示剂量依赖性抑制组胺刺激的酸分泌，其IC50值与西咪替丁相当。在单剂量水平的1g / Kg体重的化合物（4）下，没有观察到瑞士白化病小鼠的死亡率或行为异常。化合物（4）在体内进一步表现出抗吲哚美辛诱导的溃疡的优异的抗溃疡活性。

10. 发明授权

US08680288B2 Pyridin-2yl sulfanyl acid esters and process for the preparation thereof 失效
标题翻译：吡啶-2-基硫基酸酯及其制备方法
公开(公告)号：US08680288B2
公开(公告)日：2014-03-25
申请号：US13811090
申请日：2011-07-20
申请人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
发明人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
IPC分类号： C07D213/62 , A61K31/435
CPC分类号： C07D213/70
摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
摘要翻译：本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血，作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。

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