公开(公告)号：EP0841912A1

公开(公告)日：1998-05-20

申请号：EP96923609.0

申请日：1996-07-02

申请人： YALE UNIVERSITY

发明人： SARTORELLI, Alan, C. ,  SHYAM, Krishnamurthy ,  PENKETH, Philip, G.

IPC分类号： A61K31 ,  A61P35 ,  C07C311 ,  C07C317

CPC分类号： C07C311/55

摘要： The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhydrazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs roethylation or methylation and carbamoylation.

公开(公告)号：EP1028721A1

公开(公告)日：2000-08-23

申请号：EP98953830.1

申请日：1998-10-21

申请人： Yale University

发明人： SARTORELLI, Alan, C. ,  SHYAM, Krishnamruthy ,  PENKETH, Philip, G. ,  CHEN, Shu-Hui

IPC分类号： A61K31/325 ,  C07C271/44 ,  C07C271/48 ,  C07C271/58

CPC分类号： C07F9/12 ,  C07C311/61 ,  C07F9/091

摘要： The present invention relates to a compound of formula (I) wherein R?1 and R2¿ are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.

公开(公告)号：EP1028721B1

公开(公告)日：2003-06-04

申请号：EP98953830.1

申请日：1998-10-21

申请人： Yale University

发明人： SARTORELLI, Alan, C. ,  SHYAM, Krishnamruthy ,  PENKETH, Philip, G. ,  CHEN, Shu-Hui

IPC分类号： A61K31/325 ,  A61P35/00 ,  C07C271/44 ,  C07C271/48 ,  C07C271/58 ,  C07C311/61 ,  C07F9/09 ,  C07F9/12

CPC分类号： C07F9/12 ,  C07C311/61 ,  C07F9/091

摘要： The present invention relates to a compound of formula (I) wherein R?1 and R2¿ are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.

公开(公告)号：EP0841912B1

公开(公告)日：2002-09-25

申请号：EP96923609.0

申请日：1996-07-02

申请人： YALE UNIVERSITY

发明人： SARTORELLI, Alan, C. ,  SHYAM, Krishnamurthy ,  PENKETH, Philip, G.

IPC分类号： A61K31/22 ,  A61K31/18 ,  C07C311/55 ,  C07C317/50 ,  A61P35/00

CPC分类号： C07C311/55