Takeda Chemical Industries, Inc.

Yasuhiko Kawano

Akio Miyake

Yasuko Ashida

Hideaki Nagaya

Michiyo Gyoten

Kouichi Yoshioka

Shunsaku Noguchi

Saburo Takei

Akira Morimoto

Hideaki Natsugari

Tetsuya Aono

Osamu Uchikawa

Toshihiro Ishiguro

Naoki Tarui

Motoki Ikeuchi

Nobuhiro Fujii

Tohru Sugawara

Tatsumi Matsumoto

Takahiro Saraie

Kenya Kawashima

Yukio Hara

A compound having a partial structure represented by Formula:or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory diseases, for example, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, autoimmune disease, diabetes and the like.

Furoisoquinoline derivatives, process for producing the same and use thereof

A condensed pyridazine derivative which is useful as a pharmaceutical composition for preventing or treating allergic skin diseases such as contact dermatitis, pruritus, dried dermatitis, acute urticaria and prurigo.

Condensed pyridazine derivatives, their production and use

A condensed pyridazine derivative which exhibits anti-allergic activity, anti-histaminic activity and/or eosinophil chemotaxis-inhibiting activity, anti-inflammatory activity, anti-PAF (platelet-activating factor) activity, and the like, and is useful as an agent for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis, and the like.

Condensed pyridazine compounds, their production and use

The present invention provides a compound represented by the formula:

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

The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.

Antibiotic

Optically active .beta.-lactams of the general formula ##STR1## wherein R.sup.1 is an amino or protected amino group, R.sup.2 is an organic residue bonding through a carbon atom thereof and R.sup.3 is the residue remaining after removal of the .alpha.-amino group from an optically active .alpha.-amino acid or a derivative thereof as well as a method of producing the same.

Optically active .beta.-lactams and method of their production

Compounds of formula: ##STR1## wherein R is hydroxyl, lower alkoxy having 1 to 4 carbon atoms or amino and R.sup.1 is hydrogen or lower alkyl having 1 to 4 carbon atoms, are useful as medicines such as antipyretics, analgesics and antiinflammatory agents.

Thenoylindan derivatives

Spiro[cyclopropane-1,2'-indolin]-3'-ones of the general formula: ##STR1## wherein the ring A is a substituted or unsubstituted phenyl ring and Z is hydrogen, a substituted or unsubstituted alkyl group or a substituted or unsubstituted acyl group and their pharmaceutically acceptable salts have gastric acid secretion suppressing activity, antiinflammatory activity and analgesic activity.

Spiro[cyclopropane-1,2'-indolin]-3'-ones

1,1-Dichloro-1a, 10b-dihydrodibenzo(b,f)cycloprop(d)azepine-6(1H)-carboxaldehyde is produced in good yield through a reaction between a compound of the general formula ##SPC1## Wherein R stands for hydrogen or formyl group and chloroform. Thus obtained product can be used as a valuable intermediate for synthesizing medicines and is further convertible to known drugs, e.g. 6-(3-dimethylamino)propyl)-1, 1a, 6, 10b-tetrahydrodibenzo(b,f)cycloprop(d)azepine.

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Suita, Japan

Yasuhiko Kawano