US 7,531,531 B2
Method of treating diseases associated with altered kinase activity with bicyclo-pyrazoles
Daniele Fancelli, Milan (Italy); Valeria Pittalà, Catania (Italy); and Mario Varasi, Milan (Italy)
Assigned to Pfizer Italia S.r.l., Rome (Italy)
Filed on Apr. 10, 2007, as Appl. No. 11/784,980.
Application 11/784980 is a division of application No. 10/344480, previously published as PCT/EP01/08639, filed on Jul. 25, 2001.
Application 10/344480 is a continuation in part of application No. 09/635914, filed on Aug. 10, 2000, abandoned.
Prior Publication US 2007/0191386 A1, Aug. 16, 2007
Int. Cl. A61K 31/55 (2006.01); A61K 31/501 (2006.01); A61K 31/437 (2006.01); A61K 31/426 (2006.01)
U.S. Cl. 514—215  [514/252.06; 514/303; 514/365] 1 Claim
 
1. A method for treating a mammal, including humans, suffering from a disease caused by and/or associated with an altered protein kinase activity, by administering to said mammal in need thereof a therapeutically effective amount of a bicyclo-pyrazole compound of formula (I):

OG Complex Work Unit Drawing
wherein
R is an optionally further substituted group selected from the group consisting of —COR′, —COOR′, —CONHR′, —CONR′R″, —NH—C(═NH)NHR′, —C(═NH)NHR′, —SO2R′, —SO2NHR′ and —SO2NR′R″;
R1 is a hydrogen atom or an optionally further substituted group selected from the group consisting of R′, —COR′, —COOR′, —CONHR′, —CONR′R″, —NH—C(═NH)NHR′, —C(═NH)NHR′, —SO2R′, —SO2NHR′ and —SO2NR′R″; wherein R′ and R″ are the same or different and are independently hydrogen, straight or branched C1-C6 alkyl, aryl, C3-C6 cycloalkyl or aryl C1-C6 alkyl or R′ and R″ taken together form a C4-C6 alkylene chain;
Ra, Rb, Rc and Rd, being the same or different, are independently selected among hydrogen, optionally further substituted straight or branched C1-C6 alkyl, aryl, aryl C1-C6 alkyl or —CH2OR′ groups, wherein R′ is as above defined, or Ra and Rb and/or Rc and Rd, taken together with the carbon atom to which they are bonded, form an optionally substituted C3-C6 cycloalkyl group;
m and n, each independently, represents 0 or an integer from 1 to 2, provided that m+n is lower than, or equal to, 2 (m+n≤2);
or a pharmaceutically acceptable salt thereof, and wherein said disease caused by and/or associated with an altered protein kinase activity is selected from the group consisting of cancer and cell proliferative disorders wherein the cancer is selected from the group consisting of leukemia, ovary, colon, breast, lung, and pancreas.