公开(公告)号：WO2008001166A2

公开(公告)日：2008-01-03

申请号：PCT/IB2007/000281

申请日：2007-02-07

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH ,  MAHIDHAR, Yenugonda, Venkata ,  CHAUDHURI, Arabinda ,  MUKHERJEE, Rama

发明人： MAHIDHAR, Yenugonda, Venkata ,  CHAUDHURI, Arabinda ,  MUKHERJEE, Rama

CPC分类号： C07C235/40 ,  C07C2601/16

摘要： The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.

摘要翻译： 本发明提供了合成新颖的含有莽草酸头基的无毒阳离子两亲物的方法，所述无毒阳离子两亲物能够促进生物大分子向细胞中的转运。

公开(公告)号：WO2012035557A1

公开(公告)日：2012-03-22

申请号：PCT/IN2011/000629

申请日：2011-09-14

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH ,  SRINIVAS, Ramishetti ,  GARU, Arup ,  AGAWANE, Sachin, B. ,  CHAUDHURI, Arabinda

发明人： SRINIVAS, Ramishetti ,  GARU, Arup ,  AGAWANE, Sachin, B. ,  CHAUDHURI, Arabinda

IPC分类号： C07C237/10 ,  C07C231/02 ,  A61K31/16 ,  A61P43/00

CPC分类号： C07C237/24 ,  C07C231/12 ,  C07C237/22 ,  C07C2601/14 ,  C07C2601/16

摘要： The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.

摘要翻译： 本发明公开了含有甘露糖模拟莽草酸和奎尼酸头基的新型阳离子两亲物和用甘露糖模拟极性头基如莽草酸和奎尼酸制备阳离子两亲物的方法。 本文所述的发现还证明本发明的化合物可以通过在APC的细胞表面上表达的甘露糖受体将模拟DNA疫苗靶向抗原呈递细胞（APCs）如巨噬细胞和树突状细胞（DC）。 本文公开的阳离子两亲物与其在小鼠中的树突状细胞（DC，最专业的APC）基于遗传免疫的它们的甘露糖基配对相比显示出增强的细胞和体液免疫应答。 本发明描述的具有甘露糖模拟的奎尼酸和莽草酸头团的阳离子两亲物可能在将来在遗传免疫领域中的应用。

公开(公告)号：WO2014087429A1

公开(公告)日：2014-06-12

申请号：PCT/IN2013/000751

申请日：2013-12-06

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

发明人： GARU, Arup ,  MOKU, Gopikrishna ,  AGAWANE, Sachin, Barad ,  CHAUDHURI, Arabinda

IPC分类号： C07D233/64 ,  A61K31/4172 ,  A61P35/00

CPC分类号： C07D233/64 ,  A61K9/127 ,  A61K31/4172 ,  C07C227/18 ,  C07C269/06

摘要： Novel anti-cancer reagents capable of combating various types of tumors continue to be major research focus in many leading pharmaceutical companies round the globe. To this end, the present invention discloses processes for preparing a novel series of histidinylated cationic amphiphiles of formula I. The findings described herein also demonstrate that compounds of the present invention possess anti-proliferative activity such as anti" cancer activity and are useful in combating various types of cancer. The pharmaceutically active composition of cationic amphiphiles disclosed herein show enhanced cellular apoptosis through the Bax & Bcl-2 mediated signal transduction pathway. Cationic amphiphiles with histidine head-groups described in the present invention are likely to find future applications in the field of anti-cancer therapy.

摘要翻译： 能够抗击各种类型肿瘤的新型抗癌试剂继续成为全球许多领先制药公司的主要研究重点。 为此，本发明公开了制备式I的新一系列组氨酸化阳离子两亲物的方法。本文所述的发现还证明本发明的化合物具有抗增殖活性，例如抗癌活性，并且可用于对抗 本文公开的阳离子两亲物的药物活性组合物通过Bax和Bcl-2介导的信号转导途径显示增强的细胞凋亡。本发明中描述的具有组氨酸头基团的阳离子两亲物可能在未来的应用中发现 抗癌治疗领域。

公开(公告)号：WO2014115158A1

公开(公告)日：2014-07-31

申请号：PCT/IN2013/000054

申请日：2013-01-28

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

发明人： MUKHERJEE, Anubhab ,  BHATTACHARYYA, Jayanta ,  CHAUDHURI, Arabinda

IPC分类号： C12N15/113 ,  C12N15/11 ,  A61K48/00

CPC分类号： C12N15/113 ,  C12N15/111 ,  C12N15/1135 ,  C12N2310/14 ,  C12N2310/531 ,  C12N2320/32

摘要： Liposomal compositions comprising of liposomes of guanidinylated cationic amphiphiles as the main lipid and cholesterol/1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC)/aminopropyl polyethyleneglycol carbamyl-distearoylphosphatidyl-ethanolamine (DSPE-peg-NH2) as co-lipids are described. These liposomal compositions containing encapsulated or electrostatically complexed therapeutic small interfering RNAs (siRNAs) against Cdc20, a key cell cycle regulator, inhibit solid tumor growth and melanoma tumor growth on lung in C57BL/6J mice.

摘要翻译： 作为主要脂质的甘油基化阳离子两亲物的脂质体和胆固醇/ 1,2-二油酰-sn-甘油-3-磷酸胆碱（DOPC）/氨基丙基聚乙二醇氨基甲酰基 - 二硬脂酰磷脂酰乙醇胺（DSPE-peg-NH 2）的脂质体组合物， 描述脂质。 这些脂质体组合物含有针对Cdc20（一种关键细胞周期调节剂）的包封或静电复合治疗性小干扰RNA（siRNA），可抑制C57BL / 6J小鼠肺部的实体肿瘤生长和黑色素瘤肿瘤生长。

公开(公告)号：WO2014106856A1

公开(公告)日：2014-07-10

申请号：PCT/IN2013/000806

申请日：2013-12-27

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

发明人： GARU, Arup ,  MOKU, Gopikrishna ,  AGAWANE, Sachin Barad ,  CHAUDHURI, Arabinda

IPC分类号： C07H1/00 ,  C07H13/12 ,  C07C231/12 ,  C07C237/22 ,  C07C237/24 ,  A61K31/16 ,  A61K31/70

CPC分类号： C07H15/04 ,  A61K9/1271 ,  A61K31/166 ,  A61K31/351 ,  A61K31/7105 ,  A61K31/711 ,  A61K39/00 ,  A61K45/06 ,  A61K47/186 ,  A61K47/26 ,  C07C269/06 ,  C07C277/00 ,  C07C279/14 ,  C07C2601/14 ,  C07C2601/16 ,  C07H1/00 ,  C07H13/12 ,  A61K2300/00

摘要： The present invention relates to the mannose - receptor selective lysinylated cationic amphiphile and a process for preparation thereof. The compounds of the present invention can target DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterparts in genetic immunization in mice. The present invention discloses that immunization with electrostatic complexes (lipoplexes) of DNA vaccines encoding melanoma antigens (gp100 and tyrosinase) and liposome of the presently described novel lysinylated cationic amphiphiles with mannose-mimicking shikimoyl head-groups provides long-lasting (100 days post melanoma tumor challenge) protective immunity in all immunized mice. Cationic amphiphiles with mannose-mimicking shikimoyl head-groups described in the present invention are likely to find future applications in the field of genetic immunization.

摘要翻译： 本发明涉及甘露糖受体选择性赖氨酰化阳离子两亲物及其制备方法。 本发明的化合物可通过在APC的细胞表面上表达的甘露糖受体靶向抗原呈递细胞（APCs）如巨噬细胞和树突状细胞（DC）的DNA疫苗。 与其在小鼠的遗传免疫中的甘露糖基对应物相比，本文公开的阳离子两亲物显示增强的细胞和体液免疫应答。 本发明公开了用编码黑素瘤抗原（gp100和酪氨酸酶）的DNA疫苗的静电复合物（lipoplexes）和目前描述的具有甘露糖模仿的莽草酰基头基的新型赖氨酰化阳离子两亲物的脂质体进行免疫接种提供了持久的（黑素后100天） 肿瘤攻击）所有免疫小鼠的保护性免疫。 本发明中描述的具有甘露糖模拟的莽草酰基头基的阳离子两亲物可能会在遗传免疫领域中找到未来的应用。

公开(公告)号：WO2010113172A1

公开(公告)日：2010-10-07

申请号：PCT/IN2010/000164

申请日：2010-03-19

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH ,  BHATTACHARYYA, Jayanta ,  CHAUDHURI, Arabinda

发明人： BHATTACHARYYA, Jayanta ,  CHAUDHURI, Arabinda

IPC分类号： C12N15/11 ,  A61K48/00

CPC分类号： A61K48/0025 ,  A61K48/0033 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/32

摘要： The present invention provides method and pharmaceutical composition for efficient delivery of siRNA (small interfering ribonucleic acids) into cultured mammalian cells. In addition, the present invention provides methods and compositions for knocking down the expression of a specific target gene by treating cells with the formulations comprising cationic amphiphile, a neutral colipid and a small RNA molecule. We demonstrate that our method delivers siRNA efficaciously into animal cells for the purpose of RNA interference. The area of medical science that is likely to benefit most from the present invention is RNAi therapeutics.

摘要翻译： 本发明提供了将siRNA（小干扰核糖核酸）有效递送到培养的哺乳动物细胞中的方法和药物组合物。 此外，本发明提供了通过用包含阳离子两亲物，中性胶体和小RNA分子的制剂处理细胞来敲低特异性靶基因表达的方法和组合物。 我们证明我们的方法将siRNA有效地传递到动物细胞中，用于RNA干扰。 可能受益于本发明的医学领域是RNAi治疗剂。

公开(公告)号：WO2009109996A3

公开(公告)日：2009-09-11

申请号：PCT/IN2009/000119

申请日：2009-02-24

申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH ,  KARMALI, Priya, Prakash ,  PRAMANIK, Dipankar ,  MAJETI, Bharat, Kumar ,  CHAUDHURI, Arabinda ,  SISTLA, Ramakrishna

发明人： KARMALI, Priya, Prakash ,  PRAMANIK, Dipankar ,  MAJETI, Bharat, Kumar ,  CHAUDHURI, Arabinda ,  SISTLA, Ramakrishna

IPC分类号： C07C235/40 ,  A61K31/16 ,  A61K48/00

摘要： The present invention provides a novel series of glycomimicking cationic amphiphiles containing quinic acid head-groups and methods for preparing the said cationic amphiphiles. The invention provides novel compositions containing the said amphiphiles with remarkable gene transfer properties. Furthermore, the present invention provides methods for producing immune response in mice using the above-mentioned formulations containing the said cationic amphiphiles and genetic materials encoding immunogenic antigens. The area of medical science that is likely to benefit most from the present invention is genetic immunization.