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：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：US06492330B1

公开(公告)日：2002-12-10

申请号：US09248381

申请日：1999-02-11

申请人： Rama Mukherjee ,  Manu Jaggi ,  Sudhanand Prasad ,  Anand C. Burman ,  Praveen Rajendran ,  Archana Mathur ,  Anu T. Singh

发明人： Rama Mukherjee ,  Manu Jaggi ,  Sudhanand Prasad ,  Anand C. Burman ,  Praveen Rajendran ,  Archana Mathur ,  Anu T. Singh

IPC分类号： A61K3800

CPC分类号： A61K38/31 ,  A61K38/08 ,  A61K38/10 ,  C07K7/086 ,  C07K7/22 ,  C07K14/57563 ,  C07K14/6555

摘要： The invention relates to the use of peptides individually or in combination, for treating and/or preventing angiogenesis. It also relates to the use of peptide analogs or a combination of peptides referred to as MuJ-7 as anticancer drugs in restricting the tumor growth and spread by inhibiting tumor angiogenesis. MuJ-7, in addition inhibits metastasis through its antiangiogenic activity in all cancers. The invention also relates to a pharmaceutical composition containing either individual peptides or in combination, and methods of treatment of human beings and animals for curing and/or preventing angiogenesis.

摘要翻译： 本发明涉及肽单独或组合用于治疗和/或预防血管生成的用途。 它还涉及肽类似物或被称为MuJ-7的肽的组合作为抗癌药物在限制肿瘤生长和通过抑制肿瘤血管生成而扩散的用途。 MuJ-7还通过其所有癌症中的抗血管生成活性抑制转移。 本发明还涉及含有单个肽或组合的药物组合物，以及用于治疗和/或预防血管生成的人和动物的治疗方法。

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：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：US20130274211A1

公开(公告)日：2013-10-17

申请号：US13633638

申请日：2012-10-02

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： A61K47/32

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-Vinylpyrrolidne (VP), N-Isopropylactylamide (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：US06828304B1

公开(公告)日：2004-12-07

申请号：US09630345

申请日：2000-07-31

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

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

IPC分类号： A61K3800

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

摘要： This invention relates to novel antiproliferative and anti secrectory peptides that are inhibitory to vasoactive intestinal peptide receptor and are useful in the treatment of cancer. The invention particularly relates to the synthesis of lipid-peptide conjugates containing fatty acids of different sizes, which inhibits the binding of VIP to its receptors. The invention encompasses methods for generation of these peptides, composition containing these peptides and the pharmacological applications of these peptides especially in the treatment and prevention of cancer.

摘要翻译： 本发明涉及抑制血管活性肠肽受体并可用于治疗癌症的新型抗增殖和抗分解肽。 本发明特别涉及含有不同大小的脂肪酸的脂质 - 肽缀合物的合成，其抑制VIP与其受体的结合。 本发明包括用于产生这些肽的方法，含有这些肽的组合物以及这些肽的药理学应用，特别是在治疗和预防癌症中。