Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Takayuki Doi

Hideaki Natsugari

Takenori Ishimaru

Shigenori Ohkawa

Yuji Ishihara

Tetsuya Aono

Yoshinori Ikeura

Yuji Ishichi

Hiroshi Nagabukuro

Chiharu Kimura

Naoyuki Kanzaki

Motoki Ikeuchi

Hitoshi Ikeda

Mitsuo Yamamoto

Naoki Tarui

Kaneyoshi Kato

Tetsuo Miwa

Hideo Shirafuji

Agents for improving potency of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.

Agents and crystals for improving excretory potency of urinary bladder

Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an &#x3b1;1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

Preventives/remedies for urinary disturbance

Compounds of the formula wherein R, R, R, R, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

Pyrimidine 5-carboxamide compounds, process for producing the same and use thereof

Cyclic compounds, their production and use

Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC&lt;, --CO--N&lt; or --CS--N&lt; as the partial structure --X . . . . . Y&lt;; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C&lt;, --CO--N&lt; or --CS--N&lt; as the partial structure --X . . . Y&lt;; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C&lt;, --CO--N&lt; or --CS--N&lt; as the partial structure --X . . . Y&lt;; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Cyclic compounds, their prudiction and use

Disclosed are intermediates for the preparation of novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl, optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.

Intermediates for the preparation of aminocoumaran derivatives

Novel compound represented by the formula: ##STR1## wherein A', B, C, D, E, G, Ar, X, Y, and Z are defined herein or a salt thereof. The compounds have excellent activity of inhibiting ACAT, lowering Cholesterol in blood and inhibiting tachykinin receptor, or a salt thereof, their production and use.

Condensed heterocyclic compounds, their production and use

A novel aminocoumaran derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.

Intermediates for pharmaceutically useful aminocoumaran derivatives

A novel compound represented by the formula: ##STR1## wherein Ring A and Ring B respectively stands for an optionally substituted homo- or hetero-cyclic ring, and at least one of them stands for an optionally substituted heterocyclic ring stand; Ring C stands for an optionally substituted benzene ring; R stands for a hydrogen atom or an optionally substituted hydrocarbon residue; one of X and Y stands for --NR.sup.1 -- (R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue) or --O--, and the other stands for--CO-- or --CS--, or one of them stands for --N.dbd. and the other stands for .dbd.CR.sup.2 -- (R.sup.2 stands for a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon residue, an optionally substituted amino group or an optionally substituted hydroxyl group); n denotes 1 or 2 or salts thereof which have an excellent tachykinin receptor antagonistic action and inhibitory action on plasma extravasation.

Heterocyclic compounds, their production and use as tachykinin reactor

Novel composition represented by the formula: ##STR1## wherein ring A and ring B each means a benzene ring which may be substituted; R means a hydrogen atom or an alkyl group which may be substituted; R.sup.1 means a hydrogen atom or an alkyl group which may be substituted; R.sup.2 means a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted, or R.sup.1 and R.sup.2, taken together with the adjacent nitrogen atom, jointly form a ring which may be substituted, or a pharmaceutically acceptable salt thereof which is a useful tachykinin receptor antagonist.

Tachykinin receptor antagonists, isoquinolones and their production

Novel compound represented by the formula: ##STR1## such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3- acetamide: ##STR2## or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.

Growing community of inventors

Osaka, Japan

Takayuki Doi