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Last Updated: April 25, 2024

Details for Patent: 8,415,469


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Title:Compounds and methods for kinase modulation, and indications therefor
Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
Inventor(s): Ibrahim; Prabha N. (Mountain View, CA), Artis; Dean R. (Kensington, CA), Bremer; Ryan (Oakland, CA), Habets; Gaston (Pleasant Hill, CA), Mamo; Shumeye (Oakland, CA), Nespi; Marika (Berkeley, CA), Zhang; Chao (Moraga, CA), Zhang; Jiazhong (Foster City, CA), Zhu; Yong-Liang (Fremont, CA), Zuckerman; Rebecca (Alameda, CA), West; Brian (San Francisco, CA), Suzuki; Yoshisa (El Sobrante, CA), Tsai; Jianming (Vallejo, CA), Hirth; Klaus-Peter (San Francisco, CA), Bollag; Gideon (Orinda, CA), Spevak; Wayne (Berkeley, CA), Cho; Hanna (Oakland, CA), Gillette; Samuel J. (Oakland, CA), Wu; Guoxian (Palo Alto, CA), Zhu; Hongyao (Berkeley, CA), Shi; Shenghua (San Diego, CA)
Assignee: Plexxikon Inc. (Berkeley, CA)
Filing Date:Nov 10, 2009
Application Number:12/616,079
Claims:1. A compound having the structure of Formula VIIa: ##STR03436## wherein: R.sup.84 is selected from the group consisting of hydrogen, lower alkoxy, and --Cl; R.sup.94, R.sup.95, and R.sup.96 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, fluoro substituted lower alkyl, lower alkoxy, and fluoro substituted lower alkoxy; R.sup.92 is fluoro; R.sup.99 is selected from the group consisting of optionally substituted C.sub.2-6 alkyl and --NR.sup.79R.sup.80; wherein, when R.sup.99 is substituted C.sub.2-6alkyl, R.sup.84 is hydrogen or --Cl; and R.sup.79 and R.sup.80 combine with the nitrogen to which they are attached to form optionally substituted 5-7 membered heterocycloalkyl.

2. The compound of claim 1 wherein R.sup.94 and R.sup.95 are hydrogen.

3. The compound of claim 1 wherein R.sup.96 is selected from the group consisting of hydrogen, fluoro and chloro.

4. The compound of claim 3 wherein R.sup.96 is hydrogen.

5. The compound of claim 3 wherein R.sup.96 is fluoro.

6. The compound of claim 3 wherein R.sup.96 is chloro.

7. The compound of claim 1 wherein R.sup.99 is optionally substituted C.sub.2-6alkyl.

8. The compound of claim 1 wherein R.sup.99 is n-propyl.

9. The compound of claim 1 wherein R.sup.99 is optionally substituted aryl.

10. The compound of claim 1 wherein R.sup.99 is optionally substituted heteroaryl.

11. The compound of claim 1 wherein R.sup.99 is --NR.sup.79R.sup.80.

12. The compound of claim 11 wherein R.sup.79 and R.sup.80 are independently hydrogen or optionally substituted lower alkyl.

13. The compound of claim 11 wherein R.sup.79 and R.sup.80 combine with the nitrogen to which they are attached to form optionally substituted 5-7 membered heterocycloalkyl.

14. The compound of claim 1 wherein R.sup.92 and R.sup.96 are fluoro, R.sup.94 and R.sup.95 are hydrogen, and R.sup.99 is n-propyl.

15. The compound of claim 14 wherein R.sup.84 is hydrogen.

16. The compound of claim 14 wherein R.sup.84 is --Cl.

17. The compound of claim 13, wherein R.sup.92 and R.sup.96 are fluoro and R.sup.94 and R.sup.95 are hydrogen.

18. The compound of claim 17, wherein R.sup.84 is hydrogen or --Cl.

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