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：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。