| US 7,592,349 B2 | ||
| Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors | ||
| Valentina Molteni, San Diego, Calif. (US); Shuli You, Shanghai (China); Juliet Nabakka, Santee, Calif. (US); Yi Liu, San Diego, Calif. (US); Xiaolin Li, San Diego, Calif. (US); Donatella Chianelli, San Diego, Calif. (US); Jon Loren, San Diego, Calif. (US); Xiaodong Liu, San Diego, Calif. (US); Shifeng Pan, San Diego, Calif. (US); Donald S. Karanewsky, Escondido, Calif. (US); Pascal Furet, Thann (France); and Vito Guagnano, Basel (Switzerland) | ||
| Assigned to IRM LLC, Hamilton (Bermuda); and Novartis AG, Basel (Switzerland) | ||
| Filed on Oct. 31, 2007, as Appl. No. 11/933,056. | ||
| Application 11/933056 is a continuation of application No. 11/535455, filed on Sep. 26, 2006, granted, now 7,514,447. | ||
| Claims priority of provisional application 60/721015, filed on Sep. 27, 2005. | ||
| Prior Publication US 2008/0139559 A1, Jun. 12, 2008 | ||
| This patent is subject to a terminal disclaimer. | ||
| Int. Cl. A61K 31/505 (2006.01); A61K 31/506 (2006.01); C07D 239/42 (2006.01); C07D 403/04 (2006.01); C07D 403/14 (2006.01); A61P 35/00 (2006.01) | ||
| U.S. Cl. 514—275 [544/330; 544/331; 544/332] | 14 Claims |
1. A pharmaceutical composition comprising a therapeutically effective amount of a compound having the structure of Formula
(1) or Formula (46):
 Ar is a group comprising a moiety selected from an optionally substituted five-membered aromatic heterocycle, an optionally
substituted five-membered aromatic carbocycle, an optionally substituted six-membered aromatic heterocycle, and a substituted,
optionally further substituted phenyl;
Q is a group comprising a non-aromatic tertiary amine or a non-aromatic secondary amine, with the proviso that Q is not —NRaRb or —SO2NRaRb; wherein each of Ra and Rb is independently H or C1-6alkyl optionally substituted by mono- or di-alkyl (C1-6) amino;
each R1 is independently an optionally substituted moiety selected from -L1-H or -L1-C1-6alkyl; wherein L1 is selected from a bond, —O—, —NH—, —S—, —C(O)—, —C(S)—, —C(O)O—, —C(O)NH—, —S(O)—, —S(O)2—, —C(O)NH(CR″2)1-6C(O)O—, —C(O)NR″NR″C(O)O—, and —S(O)NH—;
each R″ is independently H, OH, halogen, C1-6alkyl, substituted C1-6alkyl, C1-6alkoxy, halo-C1-6alkyl, halo-C1-6alkoxy, aryl, haloaryl, or heteroaryl;
or any two adjacent R1 groups together may form an optionally substituted 5 to 8-membered heterocyclic, cycloalkyl, or aryl ring;
R5 is H or C1-6alkyl;
or a pharmaceutically acceptable salt, or pharmaceutically acceptable N-oxide thereof, in admixture with one or more pharmaceutically
acceptable excipients.
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