Quinazoline derivatives and their preparation
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsNorihiko Shimazaki, Hitoshi Yamazaki, Takumi Yatabe, Hirokazu Tanaka, Yoshikuni Itoh, Masashi Hashimoto
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Abstract
A compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, optionally substituted heterocyclic-carbonyl, optionally substituted heterocyclic-(lower)alkyl, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R.sup.3 is aryl which may have suitable substituent(s), and A is lower alkylene, or pharmaceutically acceptable salts thereof.
Claims13
A compound of the formula:
- ##STR5## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, ureido, N'-(lower)alkylureido, lower alkylsulfonylamino, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, optionally substituted heterocyclic-carbonyl or optionally substituted heterocyclic(lower)alkyl, wherein said heterocyclic group is selected from the group consisting of unsaturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s), saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s), unsaturated 3 to 8-membered heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), and unsaturated condensed 7 to 12-membered heterocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), and wherein said heterocyclic group may be optionally substituted by at least one lower alkyl,
- R.sup.3 is aryl which may have suitable substituent(s), and
- A is lower alkylene,
- or pharmaceutically acceptable salts thereof.
A compound of the formula:
- ##STR6## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, amino, ureido, N'-(lower)alkylureido, lower alkylsulfonylamino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, optionally substituted heterocyclic-carbonyl or optionally substituted heterocyclic(lower)alkyl wherein said heterocyclic is selected from the group consisting of pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, and its N-oxide, pyrimidyl, pyrazinyl, pyrazolyl, triazolyl, tetrazolyl, dihydrotriazinyl, acetidinyl, pyrrolidinyl, imidazolidinyl, piperidinyl, pyrazolidinyl, piperazinyl, indolyl, isoindolyl, indolizinyl, benzimidazolyl, quinolyl, isoquinolyl, indazolyl, benzotriazolyl, tetrazolopyridyl, tetrazolopyridazinyl, dihydrotriazolopyridazinyl, oxazolyl, isoxazolyl, oxadiazolyl, mopholinyl, benzoxazolyl and benzoxadiazolyl, and wherein said heterocyclic group may be optionally substituted by at least one lower alkyl;
- and
- R.sup.3 is aryl which may have suitable substituent(s), and
- A is lower alkylene,
- or pharmaceutically acceptable salts thereof.
A compound of the formula:
- ##STR7## in which R.sup.1 is hydrogen,
- R.sup.2 is lower alkyl piperazinyl(lower)alkyl,
- R.sup.3 is phenyl, and
- A is lower alkylene,
- or pharmaceutically acceptable salts thereof.
A compound, which is
- 7-(4-methylpiperazin-1-ylmethyl)-3-[4-(4-phenyl-1,2,3,6-tetrahydropyridin-1 -yl)butyl]-1,2,3,4-tetrahydroquinazoline-2,4-dione
- or its acid addition salt.
Dependencies are inferred from the claim text.