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：US07501443B2

公开(公告)日：2009-03-10

申请号：US10540062

申请日：2002-12-23

申请人： Anita Mehta ,  Sanjay Kumar Srivastava ,  Jang Bahadur Gupta

发明人： Anita Mehta ,  Sanjay Kumar Srivastava ,  Jang Bahadur Gupta

IPC分类号： A61K31/46 ,  C07D211/18

CPC分类号： C07D209/52 ,  A61K31/352 ,  C07D405/12

摘要： This invention generally relates to the derivatives of 3.6-disubstituted azabicyclo [3.1.0] hexanes of the following formula [IA]. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the :h1ethods for treating the diseases mediated through muscarinic receptors.

摘要翻译： 本发明一般涉及下式[IA]的3.6-二取代的氮杂二环[3.1.0]己烷的衍生物。 本发明化合物可用作毒蕈碱受体拮抗剂，可用于治疗通过毒蕈碱受体介导的呼吸道，尿路和胃肠道系统的各种疾病。 本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和：用于治疗通过毒蕈碱受体介导的疾病的方法。