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2. 发明授权

US09266816B2 Fingolimod polymorphs and their processes 有权
标题翻译：芬戈莫德多晶型物及其工艺
公开(公告)号：US09266816B2
公开(公告)日：2016-02-23
申请号：US13635207
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Veereshappa , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Veereshappa , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07C213/10 , C07C215/10 , C07C215/28
CPC分类号： C07C213/10 , C07B2200/13 , C07C215/28
摘要： The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof.The application provides processes for preparation of crystalline polymorphic forms-α, β and μ substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which are useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment or prevention of autoimmune related disorder including multiple sclerosis.
摘要翻译：本发明提供了芬戈莫德HCl（I）的结晶多晶型物及其制备方法。该应用提供了制备结晶多晶型α-bgr的方法。并且μ基本上不含与工艺相关的杂质。通过根据本发明的方法获得的具有根据图1和2的XRDP图案的芬戈莫德HCl（I）的结晶多晶型物。 1,3和5，其可用作用于治疗或预防包括多发性硬化的自身免疫相关病症的药物组合物中的活性药物成分。

3. 发明授权

US07781464B2 Heterocyclic diphenyl ethers 有权
标题翻译：杂环二苯醚
公开(公告)号：US07781464B2
公开(公告)日：2010-08-24
申请号：US11359657
申请日：2006-02-21
申请人： Partha Neogi , Bishwajit Nag , Debendranath Dey , Abhijeet Nag , Birendra Kumar Bhattacharya , Vinod Kumar Singh , Surendradoss Jayakumar
发明人： Partha Neogi , Bishwajit Nag , Debendranath Dey , Abhijeet Nag , Birendra Kumar Bhattacharya , Vinod Kumar Singh , Surendradoss Jayakumar
IPC分类号： A61K31/426 , C07D277/04
CPC分类号： C07D277/34 , C07D209/34 , C07D277/36 , C07D401/12 , C07D417/12
摘要： The present invention relates to novel heterocyclic diphenyl ether and diphenyl amine compounds, derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable solvates thereof and pharmaceutically acceptable compositions containing these singly or in combination. The compounds of the present invention are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels and are useful in the treatment and/or prophylaxis of diabetes. The compounds of the present invention are effective in treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis and rheumatoid arthritis and immunological diseases, including the treatment of cancer. Furthermore, the compounds are useful for the treatment of disorders associated with insulin resistance.
摘要翻译：本发明涉及新颖的杂环二苯醚和二苯胺化合物，衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂化物，药学上可接受的盐和药学上可接受的溶剂合物以及含有这些单独或组合的药学上可接受的组合物。本发明的化合物可有效降低血糖，血清胰岛素，游离脂肪酸，胆固醇和甘油三酯水平，并且可用于治疗和/或预防糖尿病。本发明的化合物可有效治疗肥胖，炎症，自身免疫性疾病如多发性硬化和类风湿性关节炎以及免疫疾病，包括治疗癌症。此外，这些化合物可用于治疗与胰岛素抵抗相关的疾病。

4. 发明申请

US20130281739A1 FINGOLIMOD POLYMORPHS AND THEIR PROCESSES 有权
标题翻译： FINGOLIMOD POLYMORPHS及其方法
公开(公告)号：US20130281739A1
公开(公告)日：2013-10-24
申请号：US13635207
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Veereshappa N/A , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Veereshappa N/A , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07C215/28 , C07C213/10
CPC分类号： C07C213/10 , C07B2200/13 , C07C215/28
摘要： The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof.The application provides processes for preparation of crystalline polymorphic forms-α, β and μ substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which are useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment or prevention of autoimmune related disorder including multiple sclerosis.
摘要翻译：本发明提供了芬戈莫德HCl（I）的结晶多晶型物及其制备方法。该应用提供了制备基本上不含工艺相关杂质的结晶多晶型α，β和μ的方法。通过根据本发明的方法获得的具有根据图1和2的XRDP图案的芬戈莫德HCl（I）的结晶多晶型物。 1,3和5，其可用作用于治疗或预防包括多发性硬化的自身免疫相关病症的药物组合物中的活性药物成分。

5. 发明授权

US09278932B1 Process for preparation of 2-chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide solid forms 有权
标题翻译：制备2-氯-N-（4-氯-3-吡啶-2-基苯基）-4-甲基磺酰基苯甲酰胺固体形式的方法
公开(公告)号：US09278932B1
公开(公告)日：2016-03-08
申请号：US14773322
申请日：2014-03-05
申请人： Rafiuddin Dr , Vinod Kumar Singh , Nagnnath Kokare , Akshaykant Chaturvedi
发明人： Rafiuddin Dr , Vinod Kumar Singh , Nagnnath Kokare , Akshaykant Chaturvedi
IPC分类号： C07D213/38 , C07D213/40 , C07F5/04
CPC分类号： C07D213/40 , C07D213/38 , C07F5/04
摘要： The present invention relates to crystalline 2-Chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide (I) designated as Form-SV and process for preparation thereof. The invention further relates to pharmaceutical compositions comprising crystalline Form-SV or non-crystalline form of (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide, useful in the treatment of cancer.
摘要翻译：本发明涉及名为Form-SV的结晶2-氯-N-（4-氯-3-吡啶-2-基苯基）-4-甲基磺酰基苯甲酰胺（I）及其制备方法。本发明还涉及包含结晶形式SV或非结晶形式的（2-氯-N-（4-氯-3-（吡啶-2-基）苯基）-4-（甲基磺酰基）苯甲酰胺的药用组合物，其可用在治疗癌症。

6. 发明授权

US09217001B2 Crystalline bortezomib process 有权
标题翻译：结晶硼替佐米方法
公开(公告)号：US09217001B2
公开(公告)日：2015-12-22
申请号：US14434105
申请日：2013-11-12
申请人： Vimal Kumar Shrawat , Rafiuddin , Vinod Kumar Singh , Akshay Kant Chaturvedi
发明人： Vimal Kumar Shrawat , Rafiuddin , Vinod Kumar Singh , Akshay Kant Chaturvedi
IPC分类号： C07D241/12 , C07F5/02 , C07F5/04
CPC分类号： C07F5/025 , C07B2200/13 , C07D241/12
摘要： The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2θ° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±0.20 2θ°, wherein peaks at 9.8 and 11.39±0.20 2θ° are un-split and 100% intensity peak is present at 5.6±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 45 to 60° C. (Peak-1) and 175 to 185° C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm−1, 3304 cm−1, 2953 cm−1, 2927 cm−1, 2868 cm−1, 1627 cm−1, 1455 cm−1, 1400 cm−1, 1201 cm−1, 1150 cm−1, 1020 cm−1, 747 cm−1 and 702 cm−1 and Raman absorption spectra having characteristic peaks approximately at 3066 cm−1, 1583 cm−1, 1528 cm−1, 1281 cm−1, 1213 cm−1, 1035 cm−1, 1022 cm−1 and 1004 cm−1. The invention also provides the use of said crystalline Form-SB as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.
摘要翻译：本发明提供制备作为其一水合物的结晶硼替佐米（Ia）的方法，其被称为结晶形式-SB，其特征在于含水量在3.5-6.0％w / w之间; X射线粉末衍射图包含特征2＆amp; t s;峰值选自5.6,7.5,9.8,10.2,11.3,15.1,18.0,20.5,21.5和23.6±0.20 2的色度;°，其中9.8和11.39的峰 ±0.20 2＆amp; thetas;°是未分裂的，并且在5.6±0.20 2时存在100％强度峰值;°，DSC等温线包含在45至60℃（峰-1）和175至185℃之间的吸热峰。（峰-2）和IR吸收特征峰值大约在3387cm -1，3304cm -1，2953cm -1，2927cm -1，2868cm -1，1627cm -1，1455cm -1，1400cm -1，具有大约在3066cm-1,1583cm-1,1528cm -1的特征峰的拉曼吸收光谱的1,1201cm -1，1150cm -1，1020cm -1，747cm -1和702cm -1， 1281cm-1,1213cm-1,1035cm -1，1022cm -1和1004cm -1。本发明还提供所述结晶形式-SB作为药物组合物中的活性药物成分用于治疗癌症的用途。

7. 发明申请

US20130217888A1 PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE 审中-公开
标题翻译：制备丁二酸二氢马来酸单氯化物的方法
公开(公告)号：US20130217888A1
公开(公告)日：2013-08-22
申请号：US13635097
申请日：2011-08-29
申请人： Vimal Kumar Shrawat , Seshachalam Unnam , Vinod Kumar Singh , Prashant Purohit
发明人： Vimal Kumar Shrawat , Seshachalam Unnam , Vinod Kumar Singh , Prashant Purohit
IPC分类号： C07D235/16
CPC分类号： C07D235/16 , A61K31/4184 , C07B2200/13 , C07C209/10
摘要： The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) The present application also provides a process of purification of Bendamustine hydrochloride or monohydrate to get substantially pure Bendamustine hydrochloride monohydrate crystalline Form-SM. The said Bendamustine hydrochloride monohydrate crystalline Form-SM is characterized by X-ray powder diffraction pattern comprising at least 5 characteristic peaks selected from the XRPD 2 theta degrees peaks at 7.42, 10.60, 11.17, 16.43, 17.94, 22.89, 26.33, 28.77, 30.28, 31.92, 40.89±0.1 2θ°.The present application also provides a process for the preparation of Bendamustine hydrochloride monohydrate crystalline Form-SM useful in making pharmaceutical composition for the treatment of cancer or similar proliferative disorders.
摘要翻译：本发明提供了制备式（I）的盐酸苯达莫司汀一水合物的方法。本申请还提供了盐酸苯达莫司汀或一水合物的纯化方法，以获得基本上纯的盐酸苯达莫司汀一水合物结晶形式-SM。所述盐酸苯达莫司汀一水合物结晶形式SM的特征在于X射线粉末衍射图，其包含从7.42,10.60,11.17,16.43,17.94,22.89,26.33,28.77,30.28处选择的XRPD2θ度峰中的至少5个特征峰，31.92，40.89±0.12θ。本申请还提供了制备用于制备用于治疗癌症或类似增殖性疾病的药物组合物的盐酸苯达莫司汀一水合物结晶形式-SM的方法。

8. 发明授权

US07335686B2 Method and composition for treating osteoporosis 失效
标题翻译：治疗骨质疏松症的方法和组成
公开(公告)号：US07335686B2
公开(公告)日：2008-02-26
申请号：US10747671
申请日：2003-12-30
申请人： Kanury Venkata Subba Rao , Mohan Ramachandran Wani , Venkatasamy Manivel , Parameswaran Perunninakulath Subrayan , Vinod Kumar Singh , Ramasamy Vijaya Anand , Ehrlich Desa , Gyan Chandra Mishra , Anil Chatterji
发明人： Kanury Venkata Subba Rao , Mohan Ramachandran Wani , Venkatasamy Manivel , Parameswaran Perunninakulath Subrayan , Vinod Kumar Singh , Ramasamy Vijaya Anand , Ehrlich Desa , Gyan Chandra Mishra , Anil Chatterji
IPC分类号： A61K31/195
CPC分类号： A61K31/255 , A61K31/16 , A61K31/185 , A61K31/19 , A61K31/194 , A61K31/195 , C07C305/06 , C07C307/02 , C07C309/17 , C07C309/18
摘要： This invention relates to a novel class of acidic amino acid/dicarboxylic acid derivatives (sulfonic acid/sulfate derivatives of naturally occurring amino acids and their amides) useful as inhibitors of osteoclastogenesis. The invention also provides methods of using the novel class of acidic amino acid/dicarboxylic acid derivatives of the general formula ZOC—(CRR)m—COOH, wherein: m=2, 3 or 4; Z is OH or NH2; one R in the compound is from the group consisting of SO3H, OSO3H, CH2—SO3H, CH2—OSO3H, and NHSO3H, and the remaining Rs are H or NH2, for inhibition of osteoclastogenesis.
摘要翻译：本发明涉及可用作破骨细胞发生抑制剂的新型酸性氨基酸/二羧酸衍生物（天然氨基酸的磺酸/硫酸衍生物及其酰胺）。本发明还提供了使用通式为ZOC-（CRR）m -COOH的新型酸性氨基酸/二羧酸衍生物的方法，其中：m = 2,3或4; Z是OH或NH 2; 该化合物中的一个R是由SO 3 H，OSO 3 H，CH 2 -SO 3， H，CH 2 -SO 2 SO 3，NHSO 3 H，剩余的R 5是H或NH 2， / SUB>，用于抑制破骨细胞发生。

9. 发明授权

US06233149B1 High power inverter air cooling 失效
标题翻译：大功率变频器空气冷却
公开(公告)号：US06233149B1
公开(公告)日：2001-05-15
申请号：US08839113
申请日：1997-04-23
申请人： Ronald Barry Bailey , Vinod Kumar Singh , Wayne Alexander Kennedy , Eric Joseph Wildi
发明人： Ronald Barry Bailey , Vinod Kumar Singh , Wayne Alexander Kennedy , Eric Joseph Wildi
IPC分类号： H05K720
CPC分类号： H05K7/20918 , H01L25/115 , H01L2924/0002 , H02M7/003 , H01L2924/00
摘要： An electrically powered vehicle includes an inverter mounted in the vehicle, the inverter having a plurality of high power IGBT modules for converting DC power to AC power for application to a plurality of AC electric motors connected in driving relationship to wheels on the vehicle. Each of the IGBT modules is mounted in thermal transfer relationship to an electrically isolated base plate and each base plate has a plurality of closely spaced, parallel slots formed across one surface with a plurality of fins fitted into the slots and extending from the base plate. The system includes apparatus for mounting the IGBT modules to a wall separating an electronics compartment from an air supply and air exhaust compartment. Air from an air supply plenum in the air supply compartment is directed into the fins extending from the IGBT base plate and exhaust through an exhaust conduit. The vehicle includes a blower to force air to flow through the fins extending from the base plate.
摘要翻译：一种电动车辆包括安装在车辆中的逆变器，该逆变器具有多个用于将DC电力转换为AC电力的大功率IGBT模块，用于应用于与车辆上的车轮的驱动关系连接的多个AC电动机。每个IGBT模块以热传递关系安装到电隔离的基板，并且每个基板具有跨越一个表面形成的多个紧密间隔的平行的狭槽，其中多个翼片装配到槽中并从基板延伸。该系统包括用于将IGBT模块安装到将电子设备隔室与空气供应和排气隔间分隔开的壁的装置。空气供给室中的空气供给室的空气被引导到从IGBT基板延伸的散热片中，并通过排气导管排出。车辆包括鼓风机，以迫使空气流过从基板延伸的翅片。

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