US 5,045,541 AGranted

Fused pyridazine compounds and their pharmaceutical use

AssigneeYoshitomi Pharmaceutical Industries, Ltd.

InventorsToru Nakao, Minoru Kawakami, Masao Hisadome, Tetsuya Tahara

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Abstract

Fused pyridazine compounds ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, and alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula --O--Y--NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are the same or different and respectively hydrogen, an alkyl, a phenylalkyl or a substituted phenylalkyl or a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula --O--Y--NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are of the same meanings as defined above; W is .dbd.CH-- or .dbd.N; X is CH.sub.2, S, SO, SO.sub.2 or O; and the bond designated by a broken line in its part stands for a single bond or a double bond, or their pharmaceutically acceptable salts or hydrates and their pharmaceutical use. Said compounds possess stimulating effects on phagocytosis of leukocytes and macrophages, restorative effects on leukopenia, protective effects against infection, antitumor actions and the like and thus they are useable for the prophylaxis or therapy of human diseases accompanied by immunodeficiency.

Claims4

Dependent claims

A fused pyridazine compound of the formula ##STR13## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, a straight- or branched-chain C.sub.1-8 alkyl, a straight- or branched-chain C.sub.1-8 alkoxy or C.sub.2-5 alkanoylamino;

R.sub.a is a group of the formula
--O--Y--NR.sup.5 R.sup.6
wherein R.sup.5 and R.sup.6, the same or different, are respectively hydrogen, a straight- or branched-chain C.sub.1-8 alkyl or a phenyl-C.sub.1-4 alkyl in which the alkyl moiety is a straight- or branched-chain or a substituted phenyl-C.sub.1-4 alkyl having, on the phenyl ring, 1 to 3 substituent(s) selected from the group consisting of halogens, hydroxy, nitro, amino, cyano, trifluoromethyl, straight- or branched-chain C.sub.1-8 alkyls, straight- or branched-chain C.sub.1-8 alkoxys and C.sub.2-5 alkanoylaminos or a group forming a 5- or 6-membered saturated heterocycle together with the adjacent nitrogen atom selected from the group consisting of 1-pyrrolidinyl, piperidino, morpholino, 1-piperazinyl, 4-substituted-1-piperazinyl wherein the substituent is a straight- or branched-chain C.sub.1-8 alkyl, a hydroxy-C.sub.1-8 alkyl, phenyl, a phenyl-C.sub.1-4 alkyl, or a substituted phenyl-C.sub.1-4 alkyl having, on the phenyl ring, 1 to 3 substituent(s) selected from halogens, hydroxy, nitro, amino, cyano, trifluoromethyl, straight- or branched-chain C.sub.1-8 alkyls, straight- or branched-chain C.sub.1-8 alkoxys and C.sub.2-5 alkanoylaminos, and Y stands for a straight- or branched-chain C.sub.1-8 alkylene which may have a hydroxy group as a substituent on the chain, and;
W is .dbd.CH-- or .dbd.N--;
X is CH.sub.2, S, SO, SO.sub.2 or O;
and the bond designated by a broken line represents a single bond or a double bond, or a pharmaceutically acceptable salt or hydrate thereof.

3 more elements

Dependencies are inferred from the claim text.