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US 2007/0191376 A1Published application
Bicyclic heteroaryl compounds
AssigneeARIAD Pharmaceuticals, Inc.
InventorsDong Zou, Wei-Sheng Huang, R. Thomas, Jan Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William Shakespeare, Rajeswari Sundaramoorthi, Chester Metcalf,, David Dalgarno, Tomi Sawyer
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Abstract
This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Claims22
A compound of the Formula I:
- or a tautomer, or an individual isomer or a mixture of isomers thereof wherein:
- Ring T is a 5-membered heteroaryl ring containing 1 or 2 nitrogens with the remaining ring atoms being carbon, substituted on at least two ring atoms with Rt groups, at least two of which being located on adjacent ring atoms, and, together with the atoms to which they are attached, forming a saturated, partially saturated or unsaturated 5- or 6-membered ring (Ring E), containing 0-3 heteroatoms selected from O, N, and S and being optionally substituted with 1-4 Re groups;
- Ring B represents a 5- or 6-membered aryl or heteroaryl ring;
- L1 is selected from NR1C(O), C(O)NR1, NR1C(O)O, NR1C(O)NR1, and OC(O)NR1;
- each occurrence of Ra, Rb and Rt is independently selected from the group consisting of halo, —CN, —NO2, —R4, —OR2, —NR2R3, —C(O)YR2, —OC(O)YR2, —NR2C(O)YR2, —SC(O)YR2, —NR2C(═S)YR2, —OC(═S)YR2, —C(═S)YR2, —YC(═NR3)YR2, —YP(═O)(YR4)(YR4), —Si(R2)3, —NR2SO2R2, —S(O)rR2, —SO2NR2R3 and —NR2SO2NR2R3, wherein each Y is independently a bond, —O—, —S— or —NR3—;
- Re, at each occurrence, is independently selected from the group consisting of halo, ═O, —CN, —NO2, —R4, —OR2, —NR2R3, —C(O)YR2, —OC(O)YR2, —NR2C(O)YR2, —SC(O)YR2, —NR2C(═S)YR2, —OC(═S)YR2, —C(═S)YR2, —YC(═NR3)YR2, —YP(═O)(YR4)(YR4), —Si(R2)3, —NR2SO2R2, —S(O)rR2, —SO2NR2R3 and —NR2SO2NR2R3, wherein each Y is independently a bond, —O—, —S— or —NR3—;
- R1, R2 and R3 are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclic and heteroaryl;
- alternatively, R2 and R3, taken together with the atom to which they are attached, form a 5- or 6-membered saturated, partially saturated or unsaturated ring, which can be optionally substituted and which contains 0-2 heteroatoms selected from N, O and S(O)r;
- each occurrence of R4 is independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclic and heteroaryl;
- each of the alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclic and heteroaryl moieties is optionally substituted;
- m is 0, 1, 2, 3 or 4;
- n is 2 or 3;
- p is 0, 1, 2, 3, 4 or 5;
- and,
- r is 0, 1 or 2;
- or a pharmaceutically acceptable salt, solvate or hydrate thereof.
13 more elements
Dependencies are inferred from the claim text.