KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘Schering-Plough’ Category

SCH-727965

Posted by kinasepro on March 27, 2009

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:

O=N1=CC=CC(CNC2=CC(N3CCCC[C@H]3CCO)=NC4=C(CC)C=NN42)=C1

WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

Advertisements

Posted in CDK, Schering-Plough | 5 Comments »

SGP’s CDK CIPs

Posted by kinasepro on April 4, 2007

‘Nother set of light reading galloping down the hill from Schering-Plough on CDK. 3 continuations: 20070072882, 20070072881, and from 20070072880:

ClC1=C(S(=O)(N(C)C)=O)C=C(NC2=CC(C3CNCCC3)=NC4=C(C5=CN(C)N=C5)C=NN24)C=C1

Posted in CDK2, Schering-Plough | Leave a Comment »

Schering’s latest CDK stuff

Posted by kinasepro on March 27, 2007

Schering-Plough has a series of CDK inhibitors of which the latest installment is: US20070066621. Earlier app’s in this series appear as a combined effort via SP and PCOP, and Pharmacopeia has a press release suggesting that the collaboration has an oncology candidate in Ph1. Hrmph, No ph1 oncology trials via ScheringP in the US and the press on this stuff is a little thin.

NCC1=C(C2=CC=CC=C2Cl)C(C#N)=C(NCC3=CN=CC=C3)C4=NNC(Br)=C14

Vernalis described related series’ in Bioorg Med Chem Lett ’05, 863; 1Y8Y 1Y91 and Bioorg Med Chem Lett ’06, 1353; 2C68, 2C69, 2C6T, 2C6O, 2C6M, 2C6L, 2C6K, 2C6I

Posted in CDK2, Pharmacopeia, Schering-Plough | Leave a Comment »

US20060235025

Posted by kinasepro on October 24, 2006

How now Schering-Plough, Nice purvalanol analogs as CDK2 inhibitors.

Anything earthshaking here? Hmm… Not really, but look hard enough, and KP always learns something.

Yep, hadn’t noticed the bromide as an isopropyl isostere before, but this is a continuation from US2006041131, WO2004022559. Schering has been beating on this and other 6-5 purine isosteres for some time (WO2004026877). There’s been plenty of Biotech sniffing around here. Vernalis has a similar CDK series (WO2004087707), and a Bioorg. Med. Chem. Lett. 2005, 863 (appears they’ve dropped the series).  Ono has some c-Jun (WO2005035516) inhibitors on the scafford. So whats new here? Vernalis describes selectivity issues.  Maybe they cracked that nut, otherwise its not obvious to me.
BrC2=C1N(N=C2)C(NC3=CC=NC=C3)=CC(C4CCCNC4)=N1 BrC2=C1N(N=C2)C(NC3=CC=CN=C3)=CC(N4CCC[C@@H]4CO)=N1 CC(C)N2C=NC1=C(NC3=CC(Cl)=CC=C3)N=C(N[C@H]([C@H](C)C)CO)N=C12

Posted in CDK2, Schering-Plough | Leave a Comment »