Alkynyl pyrrolopyrimidines and related analogs as hsp90-inhibitors

A compound represented by Formula I, or a polymorph, solvate, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:

• wherein:
• R0 is selected from the group consisting of hydrogen, halogen, lower alkyl, —CN, —SR8, —OR8, and —NHR8;
• R1 is selected from the group consisting of halogen, —OR11, —SR11 and lower alkyl;
• R2 is —NHR8;
• R3 is selected from the group consisting of hydrogen, —CN, —C(O)OH, —OR11, —SR11, —C(O)R9, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower alkylsilyl, aryl, heteroaryl, alicyclyl and heterocyclyl, all optionally substituted, wherein:
• the aryl, heteroaryl, alicyclyl and heterocyclyl groups are mono-, bi- or tri-cyclic;
• R8 and R10 taken together with the N atom to which they are attached optionally form an optionally substituted ring comprising 3-7 ring atoms, wherein, in addition to said N atom, 0-3 of the ring atoms are heteroatoms selected from the group consisting of O, S and N;
• the optional substituents on R3 are selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, —CN, —C(O)OH, —NO2,—SR8, —OR8, —C(O)R9, —NR8R8, lower aryl, heteroaryl, alicyclyl, lower heterocyclyl, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, arylalkylamino, diarylamino, heteroarylamino, diheteroarylamino, arylheteroarylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, indazolyl, phosphonyl, phosphatidyl, phosphoramidyl, sulfanyl, sulfinyl, sulfonyl, sulphonamidyl, carbamyl, uryl, thiouryl and thioamidyl, wherein
• R8 and R8 taken together with the N atom to which they are attached optionally form an optionally substituted ring comprising 3-7 ring atoms, wherein, in addition to said N atom, 0-3 of the ring atoms are heteroatoms selected from the group consisting of O, S and N;
• R4 is selected from the group consisting of optionally substituted lower alkylene, —C(R12)2—, —C(O)—, —C(S)—, —S(O)— and —SO2—;
• R5 is selected from the group consisting of aryl, heteroaryl, alicyclyl and heterocyclyl, wherein:
• the aryl group is substituted with 2 to 5 substituents;
• the heteroaryl group is substituted with 2 to 5 substituents;
• the alicyclyl group is substituted with 3 to 5 substituents;
• the heterocyclyl group is substituted with 3 to 5 substituents;
• the substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —CN, —C(O)OH, —NO2, —SR8, —OR8, —C(O)R9, —NR8R10, lower aryl, lower heteroaryl, lower alicyclyl, lower heterocyclyl, arylalkyl, heteroarylalkyl, thioalkyl, amino, alkylamino, dialkylamino, arylalkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, indazolyl, phosphonyl, phosphatidyl, phosphoramidyl, sulfanyl, sulfinyl, sulfonyl, sulphonamidyl, carbamyl, uryl, thiouryl and thioamidyl, wherein
• R8 and R10 taken together with the N atom to which they are attached optionally form an optionally substituted ring comprising 3-7 ring atoms, wherein, in addition to said N atom, 0-3 of the ring atoms are heteroatoms selected from the group consisting of O, S and N;
• R8 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower heteroalkyl, lower heteroalkenyl, lower heteroalkynyl, lower aryl, lower heteroaryl and —C(O)R9;
• R9 is selected from the group consisting of H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR10R10 and —OR11, wherein
• R10 and R10 taken together with the N atom to which they are attached optionally form an optionally substituted ring comprising 3-7 ring atoms, wherein, in addition to said N atom, 0-3 of the ring atoms are heteroatoms selected from the group consisting of O, S and N;
• R10 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower heteroalkyl, lower heteroalkenyl, lower heteroalkynyl, lower aryl, lower heteroaryl and —C(O)R11;
• R11 is selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, lower aryl and lower heteroaryl;
• and
• R12 is selected from the group consisting of hydrogen and lower alkyl.