Takeda Chemical Industries, Inc.

Yasuko Ashida

Akio Miyake

Yasuhiko Kawano

Tatsumi Matsumoto

Mitsuru Shiraishi

Masahiro Kajino

A method for treating allergic rhinitis by administrating to a subject in need thereof an effective amount of a compound of the formula: ##STR1## wherein R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.4a and R.sup.5a independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or a pharmaceutically acceptable salt thereof.

Method for treating allergic rhinitis

A method for inhibiting eosinophil infiltration by administrating to a subject in need thereof an effective amount of a compound of the formula: ##STR1## wherein R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-4 group, and R.sup.4a and R.sup.5a independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or a pharmaceutically acceptable salt thereof.

Eosinophil chemotaxis inhibitor

There is disclosed a pharmaceutical composition for treating or preventing allergic rhinitis which comprises a quinone or hydroquinone derivative having thromboxane A.sub.2 receptor antagonism. This compound is hardly inactivated by in vivo metabolism and can maintain its effective blood level for a long term and exhibit excellent pharmacological activity in a low dose.

Pharmaceutical composition for treating or preventing allergic rhinitis

A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent --C.dbd.C--; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R.sup.6 and R.sup.7 are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together With the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.

Triazolopyridazine derivatives, their production and use

Novel compound of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R.sup.2 or R.sup.3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O).sub.p (p stands for an integer from 0 to 2; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for a hydrogen atom, an optionally substituted lower lakyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.7 may, taken together with the adjacent nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group; m stands for an integer from 0 to 4; and n stands for an integer from 0 to 4, or a salt thereof, which has excellent anti-PAF activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.

Imidazopyridazines, their production and use

Novel compound represented by the formula: ##STR1## wherein R.sup.1 stands for H, an optionally substituted lower alkyl group or a halogen; R.sup.2 and R.sup.3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C.dbd.C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO.sub.2 ; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.7 may, taken together with the adjacent N, form an optionally substituted N-containing heterocyclic group; m stands for 0 to 4; n stands for 0 to 4, or a salt thereof, which has excellent anti-PAF activities anti-LTC.sub.4 activities and anti-ET-1 activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.

Triazolopyridazine compounds, their production and use

Novel compound represented by the formula: ##STR1## wherein R.sup.1 stands for H, an optionally substituted lower alkyl group or a halogen; R.sup.2 and R.sup.3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C.dbd.C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO.sub.2 ; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.6 and R.sup.7 may, taken together with the adjacent N, form an optionally substituted N-containing heterocyclic group; m stands for 0 to 4; n stands for 0 to 4, or a salt thereof, which has excellent anti-PAF activities anti-LTC.sub.4 activities and anti-ET-1 activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmasceutical compositions.

Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.

Pyridazine compounds, their production and use

An imidazo [1,2-b]pyridazine compound of the formula (I): ##STR1## wherein R.sub.1 is a halogen atom or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.k (k is zero to two), a group --.circle.A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m.sup.1 and m.sup.2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.

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Takatsuki, Japan

Yasuko Ashida