Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Yoshinori Ikeura

Hideaki Natsugari

Takayuki Doi

Takenori Ishimaru

Chiharu Kimura

Junya Shirai

Yasuo Sugiyama

Naoki Tarui

Hideyuki Sugiyama

Taku Kamei

Nobuki Sakauchi

Tadatoshi Hashimoto

Yuji Nishikimi

The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), Ris an optionally halogenated Calkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, andis a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

Nitrogen-containing heterocyclic compound and use thereof

The present invention provides a compound represented by the formula:  wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, Ris a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, Ris not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

Piperidine derivative, process for producing the same, and use

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 compound represented by the formula: ##STR1## wherein ring A, ring B and ring C each stands for an optionally substituted benzene ring; X stands for --NR-- wherein R stands for hydrogen atom or an optionally substituted hydrocarbon group, --O-- or --S--; Y stands for --(CH.sub.2)n-- wherein n denotes 1 or 2 or --NH--; and R.sup.a stands for a hydrogen atom or an optionally substituted hydrocarbon group, provided that when ring C is unsubstituted or substituted only at para-position, ring B is substituted at least at ortho-position or a salt thereof which have an excellent acyl-CoA: cholesterol acyltransferase inhibiting action and cholesterol-lowering activity, their production and medicinal use.

Condensed heterocyclic 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.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.

Growing community of inventors

Nara, Japan

Yoshinori Ikeura