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US 2003/0149024 A1Published application
Therapeutic compounds
AssigneePharmacia & Upjohn Company
InventorJian-Min Fu
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds of Formula I: 1 wherein X, R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula I.
Claims76
A compound of Formula I:
- 45
- wherein
- X is O, S, or N—Rb;
- R1 is —Y—Q—Z;
- Y is heterocycle, substituted heterocycle, heteroaryl, or substituted heteroaryl,
- Q is absent, —O—, —S(O)m—, —NRa—, or alkylene;
- Z is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl, or absent provided that Q is also absent;
- R2 is H, C1-8alkyl, or aryl(C1-8alkylene-);
- R3, R4, R5, and R6 are each independently H, hydroxy, nitro, halo, cyano, N3, amidine, guanidine, thioguanidine, cyanoguanidine, C1-8alkyl, C1-8haloalkyl, C1-8alkoxy, C1-8haloalkoxy, C3-8cycloalkyl, aryl, heteroaryl, substituted heteroaryl, —S(O)NRcRd, —S(O)2NRcRd, —NRcRd, —S(O)mRa, —C(═O)NRcRd, —C(═S)NRcRd, —N(Ra)—S(O)Ra, or —N(Ra)—S(O)2Ra;
- each Ra is independently H, C1-8alkyl, C1-8alkanoyl, C1-8alkoxycarbonyl, aryl, aryl(C1-8alkylene-), heteroaryl, heteroaryl(C1-8alkylene-), heterocycle, or heterocycle(C1-8alkylene-);
- Rb is hydrogen, C1-8alkyl, C1-8alkanoyl, C1-8alkoxycarbonyl, cyano, aryl, aryl(C1-8alkylene-), heteroaryl, heteroaryl(C1-8alkylene-), heterocycle, or heterocycle(C1-8alkylene-);
- each of Rc and Rd is independently H, C1-8alkyl, C1-8alkanoyl, C1-8alkoxycarbonyl, aryl, aryl(C1-8alkylene-), heteroaryl, heteroaryl(C1-8alkylene-), heterocycle, or heterocycle(C1-8alkylene-);
- or Rc and Rd together with the nitrogen to which they are attached form azepino, piperazino, pyrrolidino, piperidino, morpholino, or thiomorpholino ring;
- each m is independently 0, 1, or 2;
- or a pharmaceutically acceptable salt thereof.
12 more elements
Dependencies are inferred from the claim text.