公开(公告)号：US08609858B2

公开(公告)日：2013-12-17

申请号：US12921061

申请日：2009-03-05

申请人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

发明人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

IPC分类号： C07D498/10 ,  C07D491/107

CPC分类号： C07D491/107 ,  C07D498/10

摘要： The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (α-methylene-γ-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 μM to 93 μM. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the α,β-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.

摘要翻译： 本发明涉及通过各种偶极子，苄腈氧化物，硝酮，叠氮化物，腈基内鎓，重氮烷，腈酰亚胺，臭氧，偶氮甲碱酰亚胺，偶氮甲碱基内鎓等与环C的环外双键的偶极环加成制备的新戊二烯衍生物 （α-亚甲基-γ-丁内酯）。 已经筛选了代表性化合物对抗不同癌细胞系的抗癌活性。 这些类似物的ICs0值在4.3μM至93μM之间变化。 已经描述了其抗癌活性的机械相关性。 化合物研究的细胞毒性试验的结果表明，单分散素中的α，β-不饱和酮部分在维持高水平的细胞毒性中起重要作用。

公开(公告)号：US20110201661A1

公开(公告)日：2011-08-18

申请号：US12921061

申请日：2009-03-05

申请人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

发明人： Mahabalarao Sampath Kumar Halmuthur ,  Ajit Kumar Saxena ,  Subhash Chandra Taneja ,  Shashank Kumar Singh ,  Vijay Kumar Sethi ,  Naveed Ahmed Qazi ,  Sanghapal Damodhar Sawant ,  Mahendhar Reddy Doma ,  Abid Hussain Banday ,  Monika Verma ,  Ghularn Nabi Qazi

IPC分类号： A61K31/424 ,  C07D498/10 ,  C07D491/107 ,  A61K31/396 ,  A61P35/00

CPC分类号： C07D491/107 ,  C07D498/10

摘要： The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (α-methylene-γ-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 μM to 93 μM. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the α,β-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.

摘要翻译： 本发明涉及通过各种偶极子，苄腈氧化物，硝酮，叠氮化物，腈基内鎓，重氮烷，腈酰亚胺，臭氧，偶氮甲碱酰亚胺，偶氮甲碱基内鎓等与环C的环外双键的偶极环加成制备的新戊二烯衍生物 （α-亚甲基-γ-丁内酯）。 已经筛选了代表性化合物对抗不同癌细胞系的抗癌活性。 这些类似物的ICs0值在4.3μM至93μM之间变化。 已经描述了其抗癌活性的机械相关性。 化合物研究的细胞毒性试验结果表明，在维持高水平的细胞毒性方面，单分散素中α，bgr-不饱和酮部分起重要作用。

公开(公告)号：US20090298938A1

公开(公告)日：2009-12-03

申请号：US12401337

申请日：2009-03-10

申请人： Ghulam Nabi Qazi ,  Subhash Chandra Taneja ,  Jaswant Singh ,  Ajit Kumar Saxena ,  Vijay Kumar Sethi ,  Bhahwal Ali Shah ,  Bal Krishan Kapahi ,  Samar Singh Andotra ,  Ajay Kumar ,  Shashi Bhushan ,  Fayaz Malik ,  Dilip Manikrao Mondhe ,  Shanmugavel Muthiah ,  Surjeet Singh ,  Monika Verma ,  Shashank Kumar Singh

发明人： Ghulam Nabi Qazi ,  Subhash Chandra Taneja ,  Jaswant Singh ,  Ajit Kumar Saxena ,  Vijay Kumar Sethi ,  Bhahwal Ali Shah ,  Bal Krishan Kapahi ,  Samar Singh Andotra ,  Ajay Kumar ,  Shashi Bhushan ,  Fayaz Malik ,  Dilip Manikrao Mondhe ,  Shanmugavel Muthiah ,  Surjeet Singh ,  Monika Verma ,  Shashank Kumar Singh

IPC分类号： A61K31/19 ,  C07C62/30

CPC分类号： A61K31/19

摘要： The present invention relates to use of compounds of general formula 1 for anticancerous activity, wherein the said compound being derived semi-synthetically from natural triterpenoic acids known as boswellic acids by the induction of apoptosis thereof cytotoxicity and anti-cancer activity displayed by semi-synthetic analogues of natural triterpenes, known as Boswellic acids. These compounds may be used for the treatment of cancer, alone or in combination with pharmaceutically acceptable or other carriers, displaying cytotoxicity and anti-cancer activity for colon, prostrate, liver, breast, central nervous system (CNS), leukemia and malignancy of other tissues, including ascites and solid tumors. The cancer cell death is mediated by induction of apoptosis and inhibition of cell proliferation at specific doses.

摘要翻译： 本发明涉及通式1的化合物用于抗癌活性的用途，其中所述化合物通过诱导其细胞凋亡的细胞毒性和半合成显示的抗癌活性而被天然三萜烯酸被称为保乳酸半合成衍生 天然三萜类似物，称为乳香酸。 这些化合物可以单独使用或与药学上可接受的或其它载体组合用于治疗癌症，显示对结肠，前列腺癌，肝癌，乳腺癌，中枢神经系统（CNS），白血病和其他恶性肿瘤的细胞毒性和抗癌活性 组织，包括腹水和实体瘤。 癌细胞死亡是通过细胞凋亡的诱导和特定剂量的细胞增殖抑制来介导的。

公开(公告)号：US08445700B2

公开(公告)日：2013-05-21

申请号：US13130702

申请日：2009-11-24

申请人： Subhash Chandra Taneja ,  Mushtaq Ahmad Aga ,  Brijesh Kumar ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

发明人： Subhash Chandra Taneja ,  Mushtaq Ahmad Aga ,  Brijesh Kumar ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

IPC分类号： C07D207/12 ,  C07D471/02

CPC分类号： C07D207/12

摘要： The present invention relates to a facile, highly efficient and economical process for the preparation of optically active N-benzyl-3-hydroxypyrrolidine in high yield from a naturally occurring alkaloid vasicine. The natural alkaloid vasicine is used as a precursor of (S)—N-benzyl-3-hydroxypyrrolidine and (R)—N-benzyl-3-hydroxypyrrolidines which can easily be sourced from the medicinal plant Adatoda vasica by the method known in the art and transformed to optical isomers (R) and (S)—N-benzyl-3-hydroxypyrrolidine by the method described in the present invention.

摘要翻译： 本发明涉及从天然存在的生物碱催化剂以高产率制备光学活性N-苄基-3-羟基吡咯烷的简便，高效和经济的方法。 使用天然生物碱维生素作为（S）-N-苄基-3-羟基吡咯烷和（R）-N-苄基-3-羟基吡咯烷的前体，其可以通过以下方法容易地从药用植物金丝桃源中获得 并通过本发明所述的方法转化成光学异构体（R）和（S）-N-苄基-3-羟基吡咯烷。

公开(公告)号：US20120101285A1

公开(公告)日：2012-04-26

申请号：US13130702

申请日：2009-11-24

申请人： Subhash Chandra Taneja ,  Mushtaq Ahmad Aga ,  Brijesh Kumar ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

发明人： Subhash Chandra Taneja ,  Mushtaq Ahmad Aga ,  Brijesh Kumar ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

IPC分类号： C07D207/12

CPC分类号： C07D207/12

摘要： The present invention relates to a facile, highly efficient and economical process for the preparation of optically active N-benzyl-3-hydroxypyrrolidine in high yield from a naturally occurring alkaloid vasicine. The natural alkaloid vasicine is used as a precursor of (S)—N-benzyl-3-hydroxypyrrolidine and (R)—N-benzyl-3-hydroxypyrrolidines which can easily be sourced from the medicinal plant Adatoda vasica by the method known in the art and transformed to optical isomers (R) and (S)—N-benzyl-3-hydroxypyrrolidine by the method described in the present invention.

摘要翻译： 本发明涉及从天然存在的生物碱催化剂以高产率制备光学活性N-苄基-3-羟基吡咯烷的简便，高效和经济的方法。 使用天然生物碱维生素作为（S）-N-苄基-3-羟基吡咯烷和（R）-N-苄基-3-羟基吡咯烷的前体，其可以通过以下方法容易地从药用植物金丝桃源中获得 并通过本发明所述的方法转化成光学异构体（R）和（S）-N-苄基-3-羟基吡咯烷。

公开(公告)号：US07166728B2

公开(公告)日：2007-01-23

申请号：US11023904

申请日：2004-12-28

申请人： Vijay Kumar Sethi ,  Samar Singh Andotra ,  Subhash Chandra Taneja ,  Pankaj Gupta ,  Ghulam Nabi Qazi

发明人： Vijay Kumar Sethi ,  Samar Singh Andotra ,  Subhash Chandra Taneja ,  Pankaj Gupta ,  Ghulam Nabi Qazi

IPC分类号： C07D309/18

CPC分类号： C08K5/1545

摘要： The present invention relates to a process for the synthesis of racemic nerol oxide i.e. 3,6-dihydro-4-methyl-2-[2-methyl-1-propenyl)-2H-pyran from monoterpene alcohol nerol i.e. cis-3,7-dimethylocta-2,6-diene-1-ol.

摘要翻译： 本发明涉及从单萜醇橙花醇合成外消旋橙花蜜的方法，即3,6-二氢-4-甲基-2- [2-甲基-1-丙烯基）-2H-吡喃，即顺式-3,7 - 二甲基-2,6-二烯-1-醇。

公开(公告)号：US06787674B1

公开(公告)日：2004-09-07

申请号：US10401128

申请日：2003-03-27

申请人： Subhash Chandra Taneja ,  Ashok Kumar Shahi ,  Vijeshwar Verma ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Abid Zaffar Hashmi ,  Prabhu Dutt ,  Sanotosh Kumar Bakshi ,  Maharaj Krishan Koul ,  Satya Narayan Sharma ,  Suresh Chandra ,  Ghulam Nabi Qazi

发明人： Subhash Chandra Taneja ,  Ashok Kumar Shahi ,  Vijeshwar Verma ,  Vijay Kumar Sethi ,  Samar Singh Andotra ,  Abid Zaffar Hashmi ,  Prabhu Dutt ,  Sanotosh Kumar Bakshi ,  Maharaj Krishan Koul ,  Satya Narayan Sharma ,  Suresh Chandra ,  Ghulam Nabi Qazi

IPC分类号： C07C4500

CPC分类号： C07C403/02 ,  A23L3/3499 ,  C07B2200/07 ,  C07C2601/16 ,  C11B9/0034

摘要： The present invention relates to anti-microbial activity of the essential oil of Cymbopogon flexuosus (Nees ex Steud) Wats and the process of isolation of novel sesquiterpene compound which is mainly responsible for the strong anti-microbial/anti-bacterial activity. The present invention particularly relates to anti-bacterial activity of the essential oil and a pure isolate identified as (+)-1-bisabolone of formula 1 against gram positive bacteria from a strain of a grass identified as Cymbopogon flexuosus.

摘要翻译： 本发明涉及Cymbopogon flexuosus（Nees ex Steud）Wats的精油的抗微生物活性和主要负责强抗微生物/抗菌活性的新型倍半萜烯化合物的分离过程。 本发明特别涉及精油的抗细菌活性，以及​​鉴定为式（1）的（+） - 1 - 双代谢素的革兰氏阳性细菌的鉴定为Cymbopogon flexuosus的草的菌株的抗菌活性。

公开(公告)号：US06692944B2

公开(公告)日：2004-02-17

申请号：US10109369

申请日：2002-03-29

申请人： Shubash Chandra Taneja ,  Vijay Kumar Sethi ,  Surrinder Koul ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

发明人： Shubash Chandra Taneja ,  Vijay Kumar Sethi ,  Surrinder Koul ,  Samar Singh Andotra ,  Ghulam Nabi Qazi

IPC分类号： C12P1706

CPC分类号： C12P17/06 ,  C07D307/02 ,  C12P7/62 ,  C12P41/003

摘要： The present invention relates to a process for the systhesis of optically enriched dextro- and laevo-rotatory isomers of rose oxide from racemic citronellol. The invention particularly relates to the preparation of optically enriched (−)-(2 S, 4 R)-rose oxide and its isomer (+)-(2 R, 4 S)-rose oxide torn racemic citronellol.

摘要翻译： 本发明涉及从外消旋香茅醇合成玫瑰氧化物的光学富集的右旋和右旋旋光异构体的方法。 本发明特别涉及光学富集的（ - ） - （2 S，4 R） - 葡萄糖氧化物及其异构体（+） - （2 R，4 S） - 葡萄糖氧化物的外消旋香茅醇的制备。