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US20090281075: ISOMERIC PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS

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Filing Information

Inventor(s) Andrew L. Roughton · Yajing Rong · Koc-Kan Ho · Michael J. Ohlmeyer · David Diller · Ray Jui-Hsiang Chan · Gaifa Lai ·
Assignee(s) PHARMACOPEIA, INC. ·
Correspondent KNOBBE MARTENS OLSON & BEAR LLP ·
Application Number US12267271
Filing date 11/07/2008
Publication date 11/12/2009
Predicted expiration date 02/02/2027
U.S. Classifications 514/210.21  · 546/118  · 514/263.2  · 514/252.16  · 514/263.37  · 514/303  · 544/118  · 514/234.2  · 544/276  ·
International Classifications A61K31397  · A61K31437  · A61K31496  · A61K31522  · A61K315377  · A61P2900  · A61P310  · A61P3500  · A61P3706  · C07D41314  · C07D47102  · C07D47318  ·
Kind CodeA1
53 Claims, No Drawings


Abstract

A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ inhibitors, and their methods of use are disclosed. The genus is represented by the formula I:

Independent Claims | See all claims (53)

  1. 1. A compound represented by Formula I, wherein: X1 and X2 are independently chosen from N and CH, with the proviso that both X1 and X2 are not CH; R1 is chosen from and —NHR4; R4 is chosen from -M-NR7R8 and M is C2-C10 alkyl optionally substituted with —OH, with a proviso that —OH cannot be bonded to a carbon atom that is also bonded to N; R7 and R8 are independently chosen from —H and C1-C4 alkyl; A is chosen from carbocycle, substituted carbocycle, heterocycle and substituted heterocycle; and L1 is a C1-C10 alkyl optionally substituted with —OH, with the proviso that —OH cannot be bonded to a carbon atom that is also bonded to N; R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl; and Z is chosen from hydrogen, C1-C6 alkyl, cyano, hydroxyalkyl, carboxamido and haloalkyl; with the provisos that, when Z is carboxamido, only one of X1 or X2 can be nitrogen; and that 8H-Purin-8-one, 2-[[2-(2-fluorophenyl)ethyl]amino]-7,9-dihydro-9-(3-methoxyphenyl) and 8H-Purin-8-one, 9-[(2,6-difluorophenyl)methyl]-2-[[(2,4-dimethoxyphenyl)methyl]amino]-7,9-dihydro are excluded compounds.

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