公开(公告)号：US08022055B2

公开(公告)日：2011-09-20

申请号：US11883753

申请日：2005-12-29

申请人： Rama Mukherjee ,  Sanjay Kumar Srivastava ,  Mohammad Jamshed Ahmed Siddiqui ,  Manu Jaggi ,  Anu T. Singh ,  Anand Vardhan ,  Manoj Kumar Singh ,  Praveen Rajendran ,  Hemant Kumar Jajoo ,  Anand C. Burman ,  Vivek Kumar ,  Nidhi Rani ,  Shiv Kumar Agarwal

发明人： Rama Mukherjee ,  Sanjay Kumar Srivastava ,  Mohammad Jamshed Ahmed Siddiqui ,  Manu Jaggi ,  Anu T. Singh ,  Anand Vardhan ,  Manoj Kumar Singh ,  Praveen Rajendran ,  Hemant Kumar Jajoo ,  Anand C. Burman ,  Vivek Kumar ,  Nidhi Rani ,  Shiv Kumar Agarwal

IPC分类号： A61K31/33 ,  A61K31/40 ,  A61K31/34

CPC分类号： C07J71/0005 ,  C07J71/0047

摘要： The invention relates to novel betulinic acid derivatives of formula (I), wherein R is C(═CH2)CH3 or CH(CH3)2; R2 together with the adjacent carbonyl group forms a carboxylic acid, carboxylic acid ester or amide or substituted amide; R3 or R4 are hydrogen or aryl with the proviso that both are not independently hydrogen or alkyl or R3 and R4 are combined together to form an aryl ring optionally substituted with a group X, wherein X is selected from halogen, alkyl, cyano, nitro, alkoxy, amino or substituted amine; Y is N or O; and R1 is zero when Y is O, and R1 is hydrogen, alkyl or aryl alkyl when Y is N, useful for inhibition of tumor cancer cells.

摘要翻译： 本发明涉及式（I）的新颖的桦木酸衍生物，其中R是C（= CH 2）CH 3或CH（CH 3）2; R2与相邻的羰基一起形成羧酸，羧酸酯或酰胺或取代的酰胺; R 3或R 4是氢或芳基，条件是两者不是独立地是氢或烷基，或者R 3和R 4结合在一起形成任选地被基团X取代的芳基，其中X选自卤素，烷基，氰基，硝基， 烷氧基，氨基或取代的胺; Y是N或O; 当Y为O时，R1为零，当Y为N时，R1为氢，烷基或芳基烷基，可用于抑制肿瘤细胞。

公开(公告)号：US20100184651A1

公开(公告)日：2010-07-22

申请号：US12093697

申请日：2006-11-16

申请人： Kapil Maithal ,  Dhatchana Moorthy Nachiappan ,  Rama Mukherjee

发明人： Kapil Maithal ,  Dhatchana Moorthy Nachiappan ,  Rama Mukherjee

IPC分类号： A61K38/17 ,  C07K14/435 ,  A61P35/00

CPC分类号： A61K38/1709

摘要： The invention relates to fusion proteins useful as therapeutics against cancer. The fusion protein comprises of cell-targeting moiety and apoptosis-inducing moiety. Cell-targeting moiety and apoptosis-inducing moiety are linked by a flexible linker, which are specifically recognized by cancer specific protease and cleaved in situ to release the apoptotic domain. In particular, the invention is illustrated by a recombinant fusion protein between human Vasoactive Intestinal Peptide (VIP) and BH3 domain of Bcl2 family protein, linked by a linker that has site for cancer specific proteases. The fusion protein specifically targets VIP receptor over-expressing cancer cells and induces cell-specific apoptosis after cleavage at the linker site by cancer specific proteases. Such fusion proteins are useful for the delivery of therapeutic/apoptotic moiety (peptides) to specific cells with perturbed expression of, but not limited to neuropeptide receptors.

摘要翻译： 本发明涉及可用作抗癌药物的融合蛋白。 融合蛋白包含细胞靶向部分和凋亡诱导部分。 细胞靶向部分和凋亡诱导部分通过柔性接头连接，柔性接头被癌特异性蛋白酶特异性识别并原位切割以释放凋亡结构域。 特别地，本发明通过人类血管活性肠肽（VIP）和Bcl2家族蛋白的BH3结构域之间的重组融合蛋白来说明，所述重组融合蛋白通过具有癌症特异性蛋白酶位点的接头连接。 融合蛋白特异性靶向VIP受体过表达癌细胞，并在癌症特异性蛋白酶在接头部位切割后诱导细胞特异性凋亡。 这种融合蛋白可用于将治疗性/凋亡部分（肽）递送至具有神经肽受体的扰动表达但不限于特异性细胞。

公开(公告)号：US20090318661A1

公开(公告)日：2009-12-24

申请号：US12159310

申请日：2006-12-26

申请人： Anand C. Burman ,  Rama Mukherjee ,  Dhiraj Khattar ,  Sanjoy Mullick ,  Manu Jaggi ,  Manoj Kumar Singh ,  Mukesh Kumar ,  Deepak Prusthy ,  Pawan Kumar Gupta ,  Rajendran Praveen ,  Shobhit Singh

发明人： Anand C. Burman ,  Rama Mukherjee ,  Dhiraj Khattar ,  Sanjoy Mullick ,  Manu Jaggi ,  Manoj Kumar Singh ,  Mukesh Kumar ,  Deepak Prusthy ,  Pawan Kumar Gupta ,  Rajendran Praveen ,  Shobhit Singh

IPC分类号： C08G61/04

CPC分类号： A61K47/32 ,  C08F220/56 ,  C08F222/12 ,  C08F222/385 ,  C08F226/10

摘要： The invention relates to a biocompatible, non-biodegradable, and non-toxic polymer of formula (I), comprising of three monomeric units, selected from 1-Vinylpyrrolidone (VP), N-Isopropylacrylamide (NIPAM), and ester of Maleic anhydride and Polyethylene glycol (MPEG), cross-linked with a bi-functional vinyl derivative, of high purity and substantially free of respective toxic monomeric contaminants, and a process for preparation thereof. The invention further relates to nanoparticulate pharmaceutical compositions of poorly water-soluble drugs or compounds comprising the polymer of the invention, which are safe, less-toxic and convenient for bedside administration to patients in need thereof. Furthermore, the invention relates to a highly selective method for preparation of nanoparticulate pharmaceutical compositions of poorly water-soluble drugs or compounds.

摘要翻译： 本发明涉及式（I）的生物相容性，不可生物降解的和无毒的聚合物，其包含三种单体单元，其选自1-乙烯基吡咯烷酮（VP），N-异丙基丙烯酰胺（NIPAM）和马来酸酐的酯和 与双官能乙烯基衍生物交联的聚乙二醇（MPEG），其纯度高，基本上不含有毒的单体污染物及其制备方法。 本发明还涉及难溶于水的药物或包含本发明聚合物的化合物的纳米颗粒药物组合物，其对于有需要的患者的床边给药是安全的，毒性较小且方便的。 此外，本发明涉及用于制备难溶于水的药物或化合物的纳米颗粒药物组合物的高选择性方法。

公开(公告)号：US20070149800A1

公开(公告)日：2007-06-28

申请号：US11582716

申请日：2006-10-17

申请人： Anil Kumar Shukla ,  Golak Chandra Maikap ,  Shiv Kumar Agarwal

发明人： Anil Kumar Shukla ,  Golak Chandra Maikap ,  Shiv Kumar Agarwal

IPC分类号： C07C317/28

CPC分类号： C07C315/02 ,  C07C317/46

摘要： A process for preparation of Bicalutamide of formula (I), comprising oxidation of compound of formula (II), with potassium permanganate in presence of water or a mixture of water and water miscible solvent and isolating Bicalutamide of formula (I) thereof.

摘要翻译： 一种制备式（I）的比卡鲁胺的方法，其包括用高锰酸钾在水或水和水混溶性溶剂的混合物中氧化式（II）化合物，并分离其式（I）的比卡鲁胺。

公开(公告)号：US20070054957A1

公开(公告)日：2007-03-08

申请号：US11515553

申请日：2006-09-05

申请人： Satish Upadhyay ,  Manoj Pananchukunnath ,  Ajeet Singh ,  Deepti Jain ,  Deepak Parshotamdas ,  Rama Mukharjee ,  Anand Burman

发明人： Satish Upadhyay ,  Manoj Pananchukunnath ,  Ajeet Singh ,  Deepti Jain ,  Deepak Parshotamdas ,  Rama Mukharjee ,  Anand Burman

IPC分类号： A61K31/282 ,  A61K31/70 ,  A61K31/7012

CPC分类号： A61K47/26 ,  A61K9/0019 ,  A61K31/282 ,  A61K31/70 ,  A61K31/7012

摘要： A storage stable pharmaceutical composition comprising a solution of Oxaliplatin in water and a catalytic amount of a carbohydrate. A process for forming such pharmaceutical composition comprising dissolving a known amount of Oxaliplatin in water; adding an amount of carbohydrate in the range of 0.0010% to 0.05% w/v with respect to such solution; agitating the mixture to get clear solution; filtering it through a filter membrane under aseptic conditions; and filling the solution resulting into glass vials sealed with elastomeric stoppers and aluminium flip-off seals.

摘要翻译： 一种储存稳定的药物组合物，其包含奥沙利铂在水中的溶液和催化量的碳水化合物。 一种形成这种药物组合物的方法，包括将已知量的奥沙利铂溶于水中; 相对于这种溶液加入0.001-0.05％w / v范围内的碳水化合物量; 搅拌混合物以得到澄清溶液; 在无菌条件下通过滤膜过滤; 并将溶液填充到用弹性塞子和铝翻盖密封件密封的玻璃小瓶中。

公开(公告)号：US20070208170A1

公开(公告)日：2007-09-06

申请号：US11678927

申请日：2007-02-26

申请人： Golak Maikap ,  Deependra Bhatt ,  Bijan Panda

发明人： Golak Maikap ,  Deependra Bhatt ,  Bijan Panda

IPC分类号： C07H19/06 ,  C07H5/06

CPC分类号： C07H19/073 ,  C07H13/08

摘要： The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the β-enriched anomer of gemcitabine hydrochloride of formula (IIb) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

摘要翻译： 本发明提供高度立体选择性，简单和经济的糖基化方法，其用于制备富含β-端基异构体的2-DIO-2 1，1/2 SUP 式（II）的-D-呋喃核糖二甲基二核苷酸及其生理学上可接受的片条，特别是纯度> 99％的式（IIb）的吉西他滨盐酸盐的β-富集的端基异构体是通过使用新的式（III）的三氯乙酰亚氨酸酯 （一世）。

公开(公告)号：US07544828B2

公开(公告)日：2009-06-09

申请号：US11582716

申请日：2006-10-17

申请人： Anil Kumar Shukla ,  Golak Chandra Maikap ,  Shiv Kumar Agarwal

发明人： Anil Kumar Shukla ,  Golak Chandra Maikap ,  Shiv Kumar Agarwal

IPC分类号： C07D255/00

CPC分类号： C07C315/02 ,  C07C317/46

摘要： A process for preparation of Bicalutamide of formula (I), comprising oxidation of compound of formula (II), with potassium permanganate in presence of water or a mixture of water and water miscible solvent and isolating Bicalutamide of formula (I) thereof.

摘要翻译： 一种制备式（I）的比卡鲁胺的方法，其包括用高锰酸钾在水或水和水混溶性溶剂的混合物中氧化式（II）化合物，并分离其式（I）的比卡鲁胺。

公开(公告)号：US07235647B2

公开(公告)日：2007-06-26

申请号：US11332830

申请日：2006-01-13

申请人： Golak Chandra Maikap ,  Deependra Bhatt ,  Bijan Kumar Panda

发明人： Golak Chandra Maikap ,  Deependra Bhatt ,  Bijan Kumar Panda

IPC分类号： C07H5/04 ,  C07H5/06 ,  C07H19/00

CPC分类号： C07H19/073 ,  C07H13/08

摘要： The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the β-enriched anomer of gemcitabine hydrochloride of formula (IIb) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

摘要翻译： 本发明提供高度立体选择性，简单和经济的糖基化方法，其用于制备富含β-端基异构体的2-DIO-2 1，1/2 SUP 式（II）的-D-呋喃核糖二基二氟核苷及其生理学上可接受的盐，特别是纯度> 99％的式（IIb）的吉西他滨盐酸盐的β-富集的端基异构体通过使用式（II）的新型三氯乙酰亚氨酸酯 （一世）。