Claims
- 1. A compound of the formula (Ic) ##STR467## wherein W is --O--, --S(O).sub.t --, --CR.sup.5 R.sup.6 --, --NR.sup.7 --, --NR.sup.7 CO--, --CONR.sup.7 --, --COO-- or --OCO--
- wherein
- R.sup.5 and R.sup.6 are the same or different and each is hydrogen atom or alkyl, R.sup.7 is hydrogen atom or alkyl, and t is 0, 1 or 2;
- R.sup.1 is an alkyl, an alkenyl, an alkynyl, an aryl, an arylalkyl, a heteroaryl, a heteroarylalkyl, a cycloalkyl or a cycloalkylalkyl
- wherein
- each group at R.sup.1 is optionally substituted by alkyl, alkylamino, amino, hydroxy, alkoxy, alkoxycarbonyl, acyl, acyloxy, acylthio, mercapto, alkylthio, alkylsulfinyl or alkylsulfonyl;
- R.sup.2 is a hydrogen atom, an alkyl, --OR.sup.15 wherein R.sup.15 is hydrogen atom, alkyl, alkenyl, alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or cycloalkylalkyl, --NR.sup.8 R.sup.9 wherein R.sup.8 and R.sup.9 are the same or different and each is hydrogen atom, alkyl, alkenyl, alkynyl, acyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or cycloalkylalkyl, or R.sup.8 and R.sup.9 optionally form heteroaryl together with the adjacent nitrogen atom, or --(CH.sub.2).sub.u, S(O).sub.u R.sup.12 wherein R.sup.12 is hydrogen atom, alkyl, alkenyl or alkynyl, u is 0, 1 or 2 and u' is 0, 1 or 2
- wherein
- each group at said R.sup.2 except hydrogen atom is optionally substituted by alkyl, alkylamino, amino, hydroxy, alkoxy, alkoxycarbonyl, acyl, acyloxy, acylthio, mercapto, alkylthio, alkylsulfinyl or alkylsulfonyl;
- Z is --CH.sub.2 -- or --CO--;
- Q is --NHCR.sup.28 (CH.sub.2).sub.v' --,
- wherein
- R.sup.28 is oxygen atom or sulfur atom, and v' is 0;
- Alk.sup.2 is an alkylene, --COCH.sub.2 -- or --CONH(H.sub.2).sub.v wherein v is 0, 1 or 2
- wherein
- alkylene and alkenylene at said Alk.sup.2 are each optionally substituted by hydroxy, carboxyl, alkoxycarbonyl, alkyl optionally substituted by hydroxy, alkoxy or alkylthio, or --CONR.sup.13 R.sup.14 wherein R.sup.13 and R.sup.14 are the same or different and each is hydrogen atom or alkyl, or R.sup.13 and R.sup.14 optionally form heteroaryl together with the adjacent nitrogen atom;
- R' is an aryl, a heteroaryl, a cycloalkyl or a benzene-condensed cycloalkyl
- wherein
- said aryl and heteroaryl are each optionally substituted by alkyl optionally substituted by hydroxy, hydroxyalkoxy, alkenyloxy, acyl, acyloxy, halogen atom, nitro, amino, sulfonamide, alkylamino, aralkyloxy, acylamino, piperidino or pyridyl, said cycloalkyl is optionally substituted by hydroxy, alkoxy or .dbd.O, and said benzene-condensed cycloalkyl is optionally substituted by hydroxy or alkoxy; and
- r is 0 or 1;
- provided that when Z is --CO-- and Q is --NHCR.sup.28 (CH.sub.2).sub.v' -- wherein R.sup.28 is oxygen atom and v' is 0, R.sup.2 is substituted at the i-position on the benzene ring, and --WR.sup.1 is substituted at the j-position on the benzene ring;
- or a pharmaceutically acceptable salt thereof.
- 2. The compound of claim 1, which is represented by the compound of the formula (Ic) ##STR468## wherein W is --O--, --S(O).sub.t --, --CR.sup.5 R.sup.6 --, --NR.sup.7 --, or --NR.sup.7 CO--,
- wherein
- R.sup.5 and R.sup.6 are the same or different and each is hydrogen atom or alkyl, R.sup.7 is hydrogen atom or alkyl, and t is 0, 1 or 2;
- R.sup.1 is an alkyl;
- R.sup.2 is a hydrogen atom, an alkyl, or --OR.sup.15 wherein R.sup.15 is hydrogen atom or alkyl;
- Z is --CH.sub.2 -- or --CO--;
- Q is --NHCR.sup.28 (CH.sub.2).sub.v' --,
- wherein
- R.sup.28 is oxygen atom or sulfur atom, and v' is 0 or 1;
- Alk.sub.2 is an alkylene, --COCH.sub.2 -- or --CONH(CH.sub.2).sub.v wherein v is 0, 2;
- R' is an aryl, a heteroaryl, or a cycloalkyl
- wherein
- said aryl and heteroaryl are each optionally substituted by alkyl, hydroxy, acyloxy, nitro, amino, alkylamino, aralkyloxy, acylamino, or piperidino, and said cycloalkyl is optionally substituted by .dbd.O;
- r is 0 or 1;
- provided that when Z is --CO-- and Q is --NHCR.sup.28 (CH.sub.2).sub.v' -- wherein R.sup.28 is oxygen atom and v' is 0, R.sup.2 is substituted at the i-position on the benzene ring, and --WR.sup.1 is substituted at the j-position on the benzene ring;
- or a pharmaceutically acceptable salt thereof.
- 3. The compound of claim 2, wherein Z is --CO--, Q is --NHCR.sup.28 (CH.sub.2).sub.v' --, wherein R.sup.28 is oxygen atom and v' is 0, R.sup.2 is --OR.sup.15, W is --O--, --NR.sup.7 -- or --NR.sup.7 CO--, R.sup.2 is substituted at the i-position on the benzene ring, and --WR.sup.1 is substituted at the j-position on the benzene ring, or a pharmaceutically acceptable salt thereof.
- 4. The compound of claim 3, wherein R.sup.1 is alkyl having 4 to 6 carbon atoms, or a pharmaceutically acceptable salt thereof.
- 5. The compound of claim 4, which is selected from the group consisting of
- 7-methoxy-3-[2-(4-nitrophenyl)ethyl]-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione,
- 7-methoxy-3-[2-(4-pyridyl)ethyl]-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione,
- 3-[2-(4-aminophenyl)ethyl]-7-methoxy-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione,
- 3-[2-(4-hydroxyphenyl)ethyl]-7-methoxy-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione,
- 3-[2-(4-methylaminophenyl)ethyl]-7-methoxy-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione and
- 3-[2-(4-dimethylaminophenyl)ethyl]-7-methoxy-8-pentyloxy-(1H,3H)-quinazoline-2,4-dione,
- or a pharmaceutically acceptable salt thereof.
- 6. A pharmaceutical composition comprising, as an active ingredient, a compound of claim 1, or a pharmaceutically acceptable salt thereof.
- 7. A pharmaceutical composition comprising, as an active ingredient, a compound of claim 2, or a pharmaceutically acceptable salt thereof.
- 8. A pharmaceutical composition comprising, as an active ingredient, a compound of claim 3, or a pharmaceutically acceptable salt thereof.
- 9. A pharmaceutical composition comprising, as an active ingredient, a compound of claim 4, or a pharmaceutically acceptable salt thereof.
- 10. A pharmaceutical composition comprising, as an active ingredient, a compound of claim 5, or a pharmaceutically acceptable salt thereof.
Priority Claims (2)
Number |
Date |
Country |
Kind |
8-020083 |
Feb 1996 |
JPX |
|
8-094989 |
Apr 1996 |
JPX |
|
CROSS REFERENCE
This application is a 371 of PCT/JP97/00291 filed Feb. 6, 1997.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/JP97/00291 |
2/6/1997 |
|
|
8/6/1998 |
8/6/1998 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO97/29079 |
8/14/1997 |
|
|
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5264438 |
Shimazaki et al. |
Nov 1993 |
|