| US 7,569,571 B2 | ||
| Substituted pyrazolo [3,4-d]pyrimidines as cytokine modulators | ||
| Qing Dong, San Diego, Calif. (US); Jianqiang Wang, Acton, Mass. (US); Hengyuan Lang, San Diego, Calif. (US); and Jiong Lan, Emeryville, Calif. (US) | ||
| Assigned to Novartis AG, Basel (Switzerland) | ||
| Appl. No. 10/584,076 PCT Filed Dec. 23, 2004, PCT No. PCT/US2004/043682 § 371(c)(1), (2), (4) Date Aug. 23, 2006, PCT Pub. No. WO2005/063766, PCT Pub. Date Jul. 14, 2005. |
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| Claims priority of provisional application 60/575113, filed on May 28, 2004. | ||
| Claims priority of provisional application 60/532529, filed on Dec. 23, 2003. | ||
| Prior Publication US 2007/0142405 A1, Jun. 21, 2007 | ||
| Int. Cl. C07D 487/04 (2006.01); A61K 31/519 (2006.01); A61P 35/04 (2006.01); A61P 25/02 (2006.01); A61P 25/06 (2006.01); A61P 19/02 (2006.01) | ||
| U.S. Cl. 514—262.1 [544/262] | 5 Claims |
1. A compound of formula
 wherein
R1 is methyl,
R2 is hydrogen,
n is 0, 1 or 2,
R3 is cyclopropyl,
X1 is a single bond or alkylene,
A, X2 and D are a pyrazolopyrimidine group of formula III
 k is an integer from 0 to 4,
w is an integer from 0 to 4,
R13 is hydrogen, alkyl, OH or NH2, and
(CR9R10)wE is alkyl, alkoxy, halo, —CH2-heterocyclyl, —CONH-cycloalkyl, alkylsulfonyl, alkylthio, alkylsulfonylamino, haloalkyl, aminocarbonyl, pseudohalo or heterocyclyl,
or two (CR9R10)wE groups, which substitute adjacent atoms on D, together form alkylenedioxy,
wherein
alkyl is lower alkyl having 1 to 6 carbon atoms,
alkylene is lower alkylene having 1 to 6 carbons,
haloalkyl is an alkyl group in which one or more of the hydrogen atoms are replaced by halogen
cycloalkyl is to a saturated mono- or multicyclic ring system of 3 to 10 carbon atoms,
alkoxy is RO—,
alkylthio is RS—,
R is lower alkyl having 1 to 6 carbon atoms
pseudohalo is cyanide, cyanate, thiocyanate, selenocyanate, trifluoromethoxy, or azido and
heterocyclyl is a monocyclic or multicyctic non-aromatic ring system of 3 to 10 members where 1 to 3, of the atoms in the
ring system is a heteroatom selected from nitrogen, oxygen or sulfur or a pharmaceutically acceptable salt thereof.
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