Claims
- 1. A compound of the general formula (I) wherein A is hydrogen or (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, —N═CHR′ (wherein R′ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (wherein R″ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkylcarboxy, and m and n are independently an integer of 0, 1 or 2) or its pharmaceutically acceptable salt, wherein A and Y are not H at the same time, and when Y is amino group, A is not H.
- 2. A process for the preparation of a compound of the following formula (I) or pharmaceutically acceptable acid addition salt thereof, comprising reacting a compound of the formula (a) with a —C═X-providing agent selected from the group consisting of 1,1-carbonyldiimidazol, 1,1-carbonylthiodiimidazol, phosgene, thiophosgene, carbonyldiphenoxide, and phenylchloroformate to give a compound of the formula (b), reacting the compound of the formula (b) with a compound of the formula (c) to give a compound of the formula (I), and optionally converting it to an acid addition salt therof wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R′ and Y are as defined in claim 1, and Y′ is H or —NH2.
- 3. A process for the preparation of a compound of the following formula (I) of claim 1 wherein Y is —N═CHR′ or a pharmaceutically acceptable salt thereof, comprising reacting a compound of the general formula (d) with HCOR′ in the presence of a base and an organic solvent to give a compound of the general formula (I) wherein, R6, R7, R8, R9, R′, and A are as defined in claim 1.
- 4. A process for the preparation of a compound of the following formula (I) of claim 1 wherein Y is —NHC(O)CHR″NHR′″ or a pharmaceutically acceptable addition salt thereof, comprising reacting a compound of the general formula (d) with in the presence of a base and an organic solvent to give a compound of the general formula (I) wherein, R6, R7, R8, R9, R″, R′″, and A are as defined in claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
98-56185 |
Dec 1998 |
KR |
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CROSS REFERENCE TO RELATED APPLICATIONS
This application is a continuation of U.S. Ser. No. 09/640/400, filed Aug. 17, 2000, which is the national phase of International Application No. PCT/KR99/00787, filed Dec. 17, 1999, which claims priority from Korean Application No. 1998/56185, filed Dec. 18, 1998, the contents of which are incorporated herein by reference in their entirety.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
5229395 |
Watanabe et al. |
Jul 1993 |
A |
5354864 |
Watanabe et al. |
Oct 1994 |
A |
Continuations (1)
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Number |
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Parent |
09/640400 |
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US |
Child |
09/855530 |
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US |