公开(公告)号：US08338562B2

公开(公告)日：2012-12-25

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： C08F26/00

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：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：US20090017105A1

公开(公告)日：2009-01-15

申请号：US12045958

申请日：2008-03-11

申请人： Dhiraj Khattar ,  Mukesh Kumar ,  Rama Mukherjee ,  Anand C. Burman ,  Minakshi Garg ,  Manu Jaggi ,  Anu T. Singh ,  Anshumali Awasthi

发明人： Dhiraj Khattar ,  Mukesh Kumar ,  Rama Mukherjee ,  Anand C. Burman ,  Minakshi Garg ,  Manu Jaggi ,  Anu T. Singh ,  Anshumali Awasthi

IPC分类号： A61K9/127 ,  A61P35/00

CPC分类号： A61K31/337 ,  A61K9/0019 ,  A61K9/1271 ,  A61K9/1277

摘要： Concentrates or proliposomal compositions of poorly water-soluble drugs and compounds, comprising of one or more membrane forming lipids, a membrane stabilizing agent, in a suitable vehicle, and optionally containing a Polyethylene Glycol (PEG)-coupled phospholipid or a mixture thereof and further, optionally containing pharmaceutically acceptable excipients such as antioxidants, buffering agents, acidifying agents etc. are provided, which have superior long term stability. The concentrates of proliposomal compositions instantly form liposomes of the said poorly water-soluble drugs and compounds on rapid injection to a diluting fluid, the liposomal composition so obtained, characterized by a physical stability more than 24 hours, ≧95% drug encapsulation and having a particle size diameter of less than 100 nm. The liposomal compositions so obtained can further be directly administered to patients in need of treatment of the poorly water-soluble drugs and compounds.

摘要翻译： 水溶性差的药物和化合物的浓缩物或前体组合物，包含一种或多种形成膜的脂质，膜稳定剂，在合适的载体中，并且任选地含有聚乙二醇（PEG） - 偶联的磷脂或其混合物 ，任选地含有药学上可接受的赋形剂如抗氧化剂，缓冲剂，酸化剂等，其具有优异的长期稳定性。 促乳素体组合物的浓缩物立即形成所述水难溶性药物和化合物的脂质体，其快速注射至稀释液体，如此获得的脂质体组合物，其特征在于物理稳定性超过24小时，> = 95％药物包封并具有 粒度直径小于100nm。 如此获得的脂质体组合物可以进一步直接施用于需要治疗不良水溶性药物和化合物的患者。

公开(公告)号：US07173006B2

公开(公告)日：2007-02-06

申请号：US10329321

申请日：2002-12-23

申请人： Rama Mukherjee ,  Anand C. Burman ,  Anu T. Singh ,  Manu Jaggi ,  Sudhanand Prasad ,  Sarjana Dutt

发明人： Rama Mukherjee ,  Anand C. Burman ,  Anu T. Singh ,  Manu Jaggi ,  Sudhanand Prasad ,  Sarjana Dutt

IPC分类号： A61K38/00

CPC分类号： A61K38/08 ,  A61K2300/00

摘要： The present invention relates to a combination of peptides that may be used for treatment of cancer. The peptide combination competes for the binding of specific neuropeptides at the plasma membrane and thereby alters the levels of key intracellular molecules implicated in cell proliferation, resulting in a broad spectrum of anticancer activity. The invention also relates to pharmaceutical compositions containing a combination of such peptide analogs.

公开(公告)号：US06489297B1

公开(公告)日：2002-12-03

申请号：US09630335

申请日：2000-07-31

申请人： Anand C. Burman ,  Sudhanand Prasad ,  Rama Mukherjee ,  Anu T. Singh ,  Archna Mathur ,  Neena Gupta

发明人： Anand C. Burman ,  Sudhanand Prasad ,  Rama Mukherjee ,  Anu T. Singh ,  Archna Mathur ,  Neena Gupta

IPC分类号： A61K3816

CPC分类号： C07K14/57563 ,  A61K38/00 ,  Y10S930/17

摘要： The present invention encompasses novel analogs of vasoactive intestinal peptide (VIP), containing substitutions at appropriately selected amino acids. The invention particularly relates to the design and synthesis of novel biologically active VIP analogs containing &agr;,&agr;-dialkylated amino acids in a site-specific manner. Specifically, the invention relates to the synthesis of VIP peptide derivatives, which bind selectively to VIP receptors on target cells. The invention encompasses methods for the generation of these peptides, compositions containing the peptides and the pharmacological applications of these peptides especially in the treatment and prevention of cancer,

摘要翻译： 本发明包括血管活性肠肽（VIP）的新类似物，其在适当选择的氨基酸处含有取代。 本发明特别涉及以位点特异性方式设计和合成含有α，α-二烷基化氨基酸的新型生物活性VIP类似物。 具体而言，本发明涉及VIP靶衍生物的合成，VIP衍生物选择性结合靶细胞上的VIP受体。 本发明包括产生这些肽的方法，含有肽的组合物和这些肽的药理学应用，特别是在治疗和预防癌症中，

公开(公告)号：US07781398B2

公开(公告)日：2010-08-24

申请号：US11643342

申请日：2006-12-21

申请人： Rama Mukherjee ,  Anand C. Burman ,  Anu T. Singh ,  Manu Jaggi ,  Sudhanand Prasad ,  Sarjana Dutt

发明人： Rama Mukherjee ,  Anand C. Burman ,  Anu T. Singh ,  Manu Jaggi ,  Sudhanand Prasad ,  Sarjana Dutt

IPC分类号： A01N37/10 ,  A61K38/00

CPC分类号： A61K38/08 ,  A61K2300/00

摘要： The present invention relates to a combination of peptides that may be used for treatment of cancer. The peptide combination competes for the binding of specific neuropeptides at the plasma membrane and thereby alters the levels of key intracellular molecules implicated in cell proliferation, resulting in a broad spectrum of anticancer activity. The invention also relates to pharmaceutical compositions containing a combination of such peptide analogs.

摘要翻译： 本发明涉及可用于治疗癌症的肽的组合。 肽组合竞争在质膜上特异性神经肽的结合，从而改变涉及细胞增殖的关键细胞内分子的水平，导致广谱的抗癌活性。 本发明还涉及含有这些肽类似物的组合的药物组合物。

公开(公告)号：US07699987B2

公开(公告)日：2010-04-20

申请号：US11449476

申请日：2006-06-08

申请人： Anand C. Burman ,  Rama Mukherjee ,  Dinesh Kumar ,  Dhiraj Khattar ,  Mukesh Kumar ,  Praveen Khullar ,  Perundurai S. Srinivasan ,  Rajesh Srivastava

发明人： Anand C. Burman ,  Rama Mukherjee ,  Dinesh Kumar ,  Dhiraj Khattar ,  Mukesh Kumar ,  Praveen Khullar ,  Perundurai S. Srinivasan ,  Rajesh Srivastava

IPC分类号： B01D15/08

CPC分类号： C07D305/14 ,  A61K47/44 ,  B01D15/325 ,  B01J20/287

摘要： A stabilized pharmaceutical composition of anticancer drug and a solvent like Polyethoxylated castor oil (cremophor) also containing any other suitable solubilizer suitable for human administration like dehydrated alcohol, is disclosed. Compositions prepared using this purified polyethoxylated castor oil enhance the stability of paclitaxel in such compositions.

摘要翻译： 公开了一种稳定的抗癌药物和溶剂，如聚乙氧基化蓖麻油（cremophor）的药物组合物，其也含有适于人类给药的任何其它合适的增溶剂如脱水醇。 使用该纯化的聚乙氧基化蓖麻油制备的组合物增强紫杉醇在这些组合物中的稳定性。

公开(公告)号：US07674824B2

公开(公告)日：2010-03-09

申请号：US11515553

申请日：2006-09-05

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

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

IPC分类号： A61K31/282

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：US20080293682A1

公开(公告)日：2008-11-27

申请号：US11883753

申请日：2005-12-29

申请人： Rama Mukherjee ,  Kumar Srivastava ,  Mohammad Jamshed Ahmed Siddioui ,  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 ,  Kumar Srivastava ,  Mohammad Jamshed Ahmed Siddioui ,  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： A61K31/58 ,  A61P35/04

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）的新型桦木酸衍生物，其中R为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：US07060678B2

公开(公告)日：2006-06-13

申请号：US10638107

申请日：2003-08-08

申请人： Sudhanand Prasad ,  Tushar Kanti Chakraborty ,  Archna Mathur ,  Manu Jaggi ,  Ajit Chand Kunwar ,  Rama Mukherjee ,  Anand C. Burman

发明人： Sudhanand Prasad ,  Tushar Kanti Chakraborty ,  Archna Mathur ,  Manu Jaggi ,  Ajit Chand Kunwar ,  Rama Mukherjee ,  Anand C. Burman

IPC分类号： A61K38/07 ,  A61K38/08 ,  C07K5/02 ,  C07K7/02 ,  C07K9/00

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1013 ,  C07K14/57563

摘要： Anticancer peptides which incorporate furanoid sugar amino acids and compositions made using these peptides are described. Methods for synthesis of the peptides and for preparing the furanoid sugar amino acids are disclosed. The peptides and compositions made using the peptides have pharmacological applications of these peptides especially in the treatment and prevention of cancer and tumors.

摘要翻译： 描述了掺入呋喃糖类氨基酸的抗癌肽和使用这些肽制备的组合物。 公开了合成肽和制备呋喃糖基氨基酸的方法。 使用肽制备的肽和组合物具有这些肽的药理学应用，特别是在治疗和预防癌症和肿瘤中。