Shionogi Company Limited

Shionigi & Co., Ltd.

Hiroshi Hashizume

Hiromu Matsumura

Masami Eigyo

Akira Matsushita

Toshisada Yano

Masahiro Sakagami

Jun Sato

Hideaki Watanabe

Masanao Inagaki

Yoshiharu Hiramatsu

Takashi Sasatani

Kenji Takaya

Natsuki Ishizuka

Satoru Tanaka

Yasuhiko Fujii

Susumu Mitsumori

Yoshikazu Fukui

Nobuhiro Ibii

Hitomi Araki

Teruo Shiomi

Hiroshi Yari

Masahide Odan

The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: whereinA is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(&#x2550;O); Y is a single bond, CRRNRor C(&#x2550;O)NR; Rand Rare independently hydrogen or substituted or unsubstituted alkyl; Ris substituted or unsubstituted aryl or heterocyclyl; Ris halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.

Piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonism

This invention provides a compound of the formula (I): 

Compounds having NPY Y5 receptor antagonistic activity

The compounds of the present invention relates to tetrahydropyridine derivatives and have high affinity and specificity to .sigma. receptors, whereby these are thought to be effective for some psychoses.

Tetrahydropyridine derivatives

A compound of the formula: ##STR1## wherein n is an integer of from 2 to 6; and p and q each is an integer of 0 or 1, excluding the case where p is 0 when q is 1; or a pharmaceutically acceptable acid addition salt thereof. This compound has a high affinity and specificity to .sigma. receptors, and is thought to be effective for treatment of some psychoses.

A compound of the formula (I): ##STR1## wherein X.sup.1 nd X.sup.2 each independently represents lower alkyl, lower alkoxy or halogen or a pharmaceutically acceptable salt thereof, which is useful as an active ingredient for a pharmaceutical composition for treating antidepressant or aftereffects of cerebrovascular impairments.

Piperidine derivatives and process for preparation thereof

The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.

Teirahydropyridine derivatives

A compound of the formula: ##STR1## wherein Y is ##STR2## R is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkanoyl, or C.sub.7 -C.sub.9 phenylalkyl, and X is hydrogen, C.sub.1 -C.sub.5 alkoxy, or halogen being useful for the treatment of senile dementia, psychoneurosis, and/or amnesia.

Pyrrolo(1,4)benzodiazepine derivatives

A compound of the formula: ##STR1## (wherein R is --SO.sub.2 R.sup.1 or --CONHR.sup.2 ; R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.8 -C.sub.12 phenylalkenyl, amino, dimethylamino, optionally substituted C.sub.8 -C.sub.12 aryl, or 5- or 6-membered heterocyclic group including at least one hetero atom selected from the group consisting of N, S, and O; R.sup.2 is amino, C.sub.1 -C.sub.8 alkylamino, C.sub.1 -C.sub.8 alkyl, or optionally substituted C.sub.8 -C.sub.12 aryl) or its pharmaceutically acceptable acid-addition salt, being useful as a drug for senile dementia, psychotropic, or antiamnesia agent is provided through several routes.

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Osaka, Japan

Hiroshi Hashizume