KinasePro

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

Archive for the ‘Rigel’ Category

What do…

Posted by kinasepro on July 10, 2009

…the Bee Gee’s and R406 have in common?

R-788 (a prodrug of R-406) has shown promise in a Ph2b trial. Partner Plz?

riglstill no BMCL

Posted in Rigel, SYK | 2 Comments »

R788: Ruh Roh

Posted by kinasepro on April 9, 2009

The saga continues… So there’s some Shareholders alleging inappropriate behavior.  The short of their argument goes something like:

Dec 13, 07: Rigel: R788 is great!

rigl1

Feb 6, 08: Rigel sells 5,000,000 shares at $27

Oct 27, 08 Rigel presents full study details:

rigl2

And now there’s a lawsuit presumably claiming that Rigel didn’t share material data during the December 13 releases and 8k filing that when said data did finally come out, it dropped the stock considerably…

Read the rest of this entry »

Posted in Rigel, SYK | Leave a Comment »

R-343

Posted by kinasepro on March 24, 2009

Structure’s a guess from process app: WO/2009/031011

FC(C=N1)=C(NC2=CC3=C(OC(F)(C(N3)=O)F)C=C2)N=C1NC4=CC(OCC(NC)=O)=CC=C4.OC5=C(C(O)=O)C=CC6=CC=CC=C65

Posted in Pfizer, Rigel, SYK | 2 Comments »

R-406

Posted by kinasepro on March 10, 2009

3FQS is Roche dropping the dime on R-406

currently in Ph2 as R-788

O=C1NC2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC1(C)C

\ : still no BMCL, eh Rigel? : /

Posted in Rigel, Roche, SYK | Leave a Comment »

R-343

Posted by kinasepro on December 7, 2007

Rigel gets 5M & some good news from Pfizer:

Pfizer (NYSE: PFE), has begun a Phase 1 clinical trial of an inhaled formulation of Rigel’s small molecule syk kinase inhibitor, R343, for the treatment of allergic asthma

Posted in Pfizer, Rigel, SYK | 2 Comments »

News of the day

Posted by kinasepro on November 14, 2007

 O=C(N([H])C2=CC=C(C3=CN4C(SC5=CC(N6CCN(C)CC6)=CC=C45)=N3)C=C2)N([H])C1=NOC(C(C)(C)C)=C1

aetiology and limited data in: WO/2005/048953

Posted in Ambit, Aurora, Deals, Flt3, Rigel | 16 Comments »

R-788 (Fostamatinib disodium)

Posted by kinasepro on November 9, 2007

R-788 is Rigel’s SYK / Flt3 inhibiting prodrug of R-406, and despite a positive sounding press release on their Ph2 ITP study, the market is reacting negatively so far by knocking 20% off of the stock price.

r-788
the name suggests disodium.

Posted in Flt3, Rigel, SYK | 15 Comments »

R763

Posted by kinasepro on February 13, 2007

Rigel’s Aurora inhibitor R-763 going Ph1 for ‘Hematological Malignancies’. It’s in Ph1 for solid tumors already. hmm… I thought they had to call it ‘EMD Serono’ in USA.  Merck DE # is: AS703569

So it’s looking like: WO/2006/055561 and before that: WO/2005/118544

FC1=CN=C(NC2=CC(C)=C(N3CCN(C)CC3)C=C2)N=C1N[C@@H]4[C@H](C5)C=C[C@H]5[C@@H]4[C@@](N)=O

Neeto – looks like they resolve the enantiomers via:

Even neeter-0 they show a couple xenos

Posted in Aurora, clinical, Merck DE, Rigel | 2 Comments »

WO2006133426

Posted by kinasepro on December 20, 2006

Those artisans of the diaminopyrimidine are at it again: Rigel has another JAK application, they suggest these are JAK3 selective.

O=C1CSC2=CC=C(NC3=NC(NC4=CC=CC(S(=O)(N)=O)=C4)=NC=C3C)C=C2N1C

WO2006133426

Posted in JAK, Rigel | Leave a Comment »

US20060270694

Posted by kinasepro on December 2, 2006

Hey Rigel, What’s this I see about 10-250 fold selectivity Jak over Syk on compounds probably discovered during the SYK R406 exploratory / optimization campaign? Neet-O.

Selectivity within the JAKs?
not so much.

Posted in JAK, Rigel | Leave a Comment »