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Title:
PI-3 KINASE INHIBITOR PRODRUG
Document Type and Number:
Japanese Patent JP2011057686
Kind Code:
A
Abstract:

To provide new prodrugs of inhibitors of PI-3 kinase.

The new compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine. A PI-3 kinase inhibitor of class I having an improved pharmacokinetics and pharmacodynamic characteristics is provided. The invention, in a specific embodiment, provides a pro-compound comprising a quaternary nitrogen, and a compound wherein one bond of the quaternary nitrogen is hydrolyzed. There are provided a method for producing these compounds and a method for treating a patient.


Inventors:
GARLICH JOSEPH R
DURDEN DONALD L
PATTERSON MARY
SU JINGDONG
SUHR ROBERT G
Application Number:
JP2010235985A
Publication Date:
March 24, 2011
Filing Date:
October 20, 2010
Export Citation:
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Assignee:
SEMAFORE PHARMACEUTICALS INC
International Classes:
C07D311/22; A61K9/127; A61K31/353; A61K31/395; A61K31/4025; A61K31/453; A61K31/47; A61K31/519; A61K31/535; A61K31/5377; A61K47/22; A61K47/26; A61K47/36; A61K47/42; A61K47/48; A61P1/04; A61P1/18; A61P9/00; A61P9/12; A61P25/00; A61P35/00; A61P35/02; A61P43/00; C07C381/00; C07D207/404; C07D257/02; C07D311/76; C07D405/04; C07D405/12; C07D407/12; C07D413/04; C07D475/04; C07D487/04; C07D207/40; C07K14/78
Domestic Patent References:
JPH05509302A1993-12-22
JPH05222092A1993-08-31
JPH04505330A1992-09-17
JP2000169372A2000-06-20
Foreign References:
WO2003024949A12003-03-27
WO2001053266A12001-07-26
WO2002042265A22002-05-30
Other References:
JPN6010028205; VLAHOS,C.J. et al: Journal of Biological Chemistry Vol.269, No.7, 1994, p.5241-5248
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita