Claims
- 1. A compound having the formula: wherein X is a member selected from the group consisting of —NR3R4, —OR3, —SR3, aryl, alkyl and arylalkyl; Y is a member selected from the group consisting of a covalent bond, —NR6)—, —O—, —S—, —C(═O)— and alkylene; R1 and R2 are members independently selected from the group consisting of hydrogen, alkyl, —O-alkyl, —S-alkyl, aryl, arylalkyl, —O-aryl, —S-aryl, —NO2, —NR7R8, —C(O)R9, —CO2R10, —C(O)NR7R8, —N(R7)C(O)R9, —N(R7)CO2R11, —N(R9)C(O)NR7R8, —S(O)mNR7R8, —S(O)nR9, —CN, halogen, and —N(R7)S(O)mR11; R3 and R4 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl, or taken together with the nitrogen atom to which each is attached form a 5-, 6- or 7-membered aromatic or non-aromatic ring containing from one to three heteroatoms selected from the group consisting of N, O and S; R5 is a member selected from the group consisting of alkyl, aryl, arylalkyl and bicyclic fused aryl-cycloalkyl; R6 is a member selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; or is combined with R5 and the nitrogen atom to which R5 and R6 are attached to form a 5-, 6-, 7- or 8-membered aromatic or non-aromatic ring containing one to three heteroatoms selected from the group consisting of N, O or S; R7 and R8 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; R9 and R10 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; R11 is a member selected from the group consisting of alkyl, aryl and arylalkyl; m is an integer of from 1 to 2; n is an integer of from 1 to 3; and wherein R1 and R3, R5 and N1, or R2 and N1 are joined to form a 5-, 6-, 7-, or 8- membered aromatic or non-aromatic ring containing one to three heteroatoms selected from the group consisting of N, O and S; said compound having a molecular weight of from about 150 to about 750, with the proviso that when Y is a bond, then R5 is other than an imidazole ring.
- 2. A compound in accordance with claim 1, wherein R1 is selected from the group consisting of —NO2, —S(O)mNR7R8, —S(O)nR9, —CN, fluoroalkyl, —C(O)R9, —CO2R10 and —C(O)NR7R8 and R2 is selected from the group consisting of hydrogen, alkyl, —O-alkyl, —S-alkyl, aryl, arylalkyl, —O-aryl and —S-aryl.
- 3. A compound in accordance with claim 2, wherein X is —NR3R4, Y is selected from the group consisting of —N(R6)—, —O— and —S—, R2 is a member selected from the group consisting of hydrogen, alkyl, —O-alkyl and halogen.
- 4. A compound in accordance with claim 3, wherein R1 is selected from the group consisting of —CF3, —S(O)mNR7R8, —CO2R10, —CN and —NO2, and R2 is selected from the group consisting of hydrogen, (lower)alkyl, —O—(lower)alkyl and —S—(lower)alkyl.
- 5. A compound in accordance with claim 4, wherein Y is —N(R6)— or —O—, R1 is —NO2, and R2 is hydrogen or (C1-C4)alkyl.
- 6. A compound in accordance with claim 1, wherein R3 is joined to R4 form a 5-membered ring, together with the nitrogen to which both radicals are attached.
- 7. A pharmaceutical composition comprising a pharmaceutically or diagnostically acceptable compound having the formula: wherein X is a member selected from the group consisting of —NR3R4, —OR3, —SR3, aryl, alkyl and arylalkyl; Y is a member selected from the group consisting of a covalent bond, —N(R6)—, —O—, —S—, —C(O))— and alkylene; R1 and R2 are members independently selected from the group consisting of hydrogen, alkyl, —O-alkyl, —S-alkyl, aryl, arylalkyl, —O-aryl, —S-aryl, —NO2, —NR7R8, —C(O)R9, —CO2R10, —C(O)NR7R8, —N(R7)C(O)R9, —N(R7)CO2R11, —N(R9)C(O)NR7R8, —S(O)mNR7R8, —S(O)nR9, —CN, halogen, and —N(R7)S(O)mR11; R3 and R4 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl, or taken together with the nitrogen atom to which each is attached form a 5-, 6- or 7-membered aromatic or non-aromatic ring containing from one to three heteroatoms selected from the group consisting of N, O and S; R5 is a member selected from the group consisting of alkyl, aryl, arylalkyl and bicyclic fused aryl-cycloalkyl; R6 is a member selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; or is combined with R5 and the nitrogen atom to which R5 and R6 are attached to form a 5-, 6-, 7- or 8-membered aromatic or non-aromatic ring containing one to three heteroatoms selected from the group consisting of N, O or S; R7 and R8 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; R9 and R10 are members independently selected from the group consisting of hydrogen, alkyl, aryl and arylalkyl; R11 is a member selected from the group consisting of alkyl, aryl and arylalkyl; m is an integer of from 1 to 2; n is an integer of from1 to 3; and wherein R1 and R3, R5 and N1, or R2 and N1 are joined to form a 5-, 6-, 7-, or 8- membered aromatic or non-aromatic ring containing one to three heteroatoms selected from the group consisting of N, O and S; said compound having a molecular weight of from about 150 to about 750, with the proviso that when Y is a bond, then R5 is other than an imidazole ring.
- 8. A composition in accordance with claim 7, wherein R1 is selected from the group consisting of —NO2, —S(O)mNR7R8, —S(O)nR9, —CN, fluoroalkyl, —C(O)R9, —CO2R10 and —C(O)NR7R8 and R2 is selected from the group consisting of hydrogen, alkyl, —O-alkyl, —S-alkyl, aryl, arylalkyl, —O-aryl and —S-aryl.
- 9. A composition in accordance with claim 8, wherein X is —NR3R4, Y is selected from the group consisting of —N(R6)—, —O— and —S—, R2 is a member selected from the group consisting of hydrogen, alkyl, —O-alkyl and halogen.
- 10. A composition in accordance with claim 9, wherein R1 is selected from the group consisting of —CF3, —S(O)mNR7R8, —CO2R10, —CN and —NO2, and R2 is selected from the group consisting of hydrogen, (lower)alkyl, —O—(lower)alkyl and —S—(lower)alkyl.
- 11. A composition in accordance with claim 10, wherein Y is —N(R6)— or —O—, R1 is —NO2, and R2 is hydrogen or (C1-C4)alkyl.
- 12. A compound in accordance with claim 7, wherein R3 is joined to R4 to form a 5-membered ring, together with the nitrogen to which both radicals are attached.
CROSS-REFERENCE TO RELATED APPLICATION
This application is a continuation of U.S. application Ser. No. 09/737,983, filed Dec. 15, 2000, now issued as U.S. Pat. No. 6,528,513, which is a continuation of U.S. application Ser. No. 09/249,641, filed Feb. 12, 1999, now issued as U.S. Pat. No. 6,200,977, which is related to PCT/US99/03136, and also claims benefit of priority to U.S. Provisional Application No. 60/075,005, filed Feb. 17, 1998, the disclosure of each being incorporated by reference.
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|
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|
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Continuations (2)
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Number |
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US |
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10/350801 |
|
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09/249641 |
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09/737983 |
|
US |