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1.发明公开PROGESTERONE-CATIONIC LIPID HYBRID AS ANTICANCER AGENT AND THE PROCESS OF SYNTHESIS THEREOF 审中-公开抗肿瘤药物孕酮 - 阳离子脂质混合物及其合成方法
公开(公告)号：EP3275888A1
公开(公告)日：2018-01-31
申请号：EP17179456.3
申请日：2017-07-04
CPC分类号： C07J41/005 , A61P35/00 , C07J41/0033
摘要： The present invention relates to the development of the cationic progesterone compounds of formula 6 as a novel anti-tumor agent. The present invention provides a method for the preparation of novel series of progesterone derivatives of formula 6. The invention also provides information related to highly selective anti-cancer activities of these compounds in wide range of cancer cell irrespective of their progesterone receptor status. Thus, the presently disclosed cationic progesterone compounds offer a viable option as anti-cancer therapeutics.
摘要翻译： 本发明涉及作为新型抗肿瘤剂的式6的阳离子黄体酮化合物的开发。 本发明提供了制备式6的新一系列黄体酮衍生物的方法。本发明还提供了与这些化合物在广泛癌细胞中的高度选择性抗癌活性有关的信息，而不管它们的孕酮受体状态如何。 因此，目前公开的阳离子黄体酮化合物作为抗癌治疗剂提供了可行的选择。
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公开(公告)号：EP4346902A1
公开(公告)日：2024-04-10
申请号：EP22741839.9
申请日：2022-06-03
发明人： KOTAMRAJU, Srigiridhar , BATHULA, Surendar Reddy , SHAIKH, Altab , NEELI, Praveen Kumar , SRAVYA, Panangipalli , BANERJEE, Rajkumar , THENNATI, Rajamannar , GAJALAKSHMI, Singuru
IPC分类号： A61K47/54 , A61P35/00 , C12N15/113 , C07F9/54 , A61K31/37
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3.发明公开NOVEL CATIONIC 17 ALPHA- SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT 有权新型阳离子17α被取代的雌二醇为手段对抗癌症
公开(公告)号：EP2111409A1
公开(公告)日：2009-10-28
申请号：EP07859632.7
申请日：2007-12-31
IPC分类号： C07J41/00 , A61K31/565 , A61P35/00
CPC分类号： C07J41/0044
摘要： The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
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4.发明公开AN AQUEOUS FORMULATION FOR SELECTIVE TARGETING AND DELIVERING GENE TO CANCER CELLS 有权用于可能的选择性靶向和基因递送到癌细胞中的含水制剂
公开(公告)号：EP2061514A2
公开(公告)日：2009-05-27
申请号：EP07827543.5
申请日：2007-08-27
CPC分类号： A61K48/0025 , A61K9/0019 , A61K9/1272
摘要： The present invention relates to a cationic lipid based aqueous formulation comprising cationic lipid, dexamethasone and a neutral co-lipid, wherein the said formulation is useful for selective targeting and delivering gene to glucocorticoid receptor expressing cancer cells. Glucorticoid receptors (GR) express in various normal and cancer cells. A lot of ligand activated physiological functions are known involving GR but its role in cancer progression (if any) is not clearly understood. Synthetic GR antagonist, dexamethasone (Dex) finds use as anti-inflammatory drug and is known to induce apoptosis in cancer cells. This Dex is included in a cationic lipid-based formulation as a co-lipid to deliver to and express genes specifically in cancer cells possibly through expressed GR. Gene delivery to cancer cells is independent of the gene construct, and tumor cell line. Normal transformed cells expressing GR but with no cancer lineage show much smaller level of transfection. The composition of the formulation is optimized. The formulation may have particular application to the enhanced delivery of anticancer genetic constructs to cancer, with the synergistic effect of Dex in inducing apoptosis as such.
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公开(公告)号：EP4313005A1
公开(公告)日：2024-02-07
申请号：EP22779330.4
申请日：2022-03-29
申请人： Council Of Scientific & Industrial Research , Jawaharlal Nehru Centre For Advanced Scientific Research
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6.发明授权An aqueous formulation for possible selective targeting and delivering gene to cancer cells 有权用于可能的选择性靶向和基因递送到癌细胞中的含水制剂
公开(公告)号：EP2061514B1
公开(公告)日：2014-11-26
申请号：EP07827543.5
申请日：2007-08-27
CPC分类号： A61K48/0025 , A61K9/0019 , A61K9/1272
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7.发明授权NOVEL CATIONIC 17 ALPHA- SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT 有权新型阳离子17α被取代的雌二醇为手段对抗癌症
公开(公告)号：EP2111409B1
公开(公告)日：2012-06-27
申请号：EP07859632.7
申请日：2007-12-31
IPC分类号： C07J41/00 , A61K31/565 , A61P35/00
CPC分类号： C07J41/0044
摘要： The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
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