Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Takashi Kosasa

Yoshiharu Yamanishi

Hachiro Sugimoto

Kiyomi Yamatsu

Norio Karibe

Atsushi Sasaki

Hiroo Ogura

Youichi Iimura

Satoshi Nagato

Masahiro Yonaga

Yoichi Iimura

Kumi Uchikoshi

Atsuhiko Kubota

Yutaka Tsuchiya

Shin Araki

Kunizou Higurashi

Michiko Kosasa

Yoshio Takeuchi

Emiko Suzuki

Toshiaki Tanaka

Toru Watanabe

Yoichi Kita

Keiichi Sorimachi

Yuji Kazuta

Takahisa Hanada

Hiroyuki Higashiyama

Yukio Ishikawa

Minako Saito

Tetsuyuki Teramoto

Tetsuo Shibata

Norio Shibata

Novel indansulfamide derivatives or a pharmaceutically acceptable salt thereof such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (+)-N-(2,2,4,6,7-pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, have an action of improving Seizure Severity Index (Score) in mice kindling model. Thus the compounds or the salt thereof are expected as a drug for treating epilepsy.

Indanesulfamide derivatives

The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof:  In the formula (I), R, R, Rand Rare the same as or different from each other.

(1-Indanone)-(1,2,3,6-tetrahydropyridine) compounds

The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a compound represented by formula: (wherein Rand Rrepresent substituents), a pharmacologically acceptable salt thereof or hydrates thereof.

4-substituted piperidine compound

The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action. It provides a compound represented by the formula:(In the formula, Rrepresents a group represented by the formula:(wherein, R, R, Rand Rare the same as or different from each other and each represents a hydrogen atom, an optionally substituted Calkoxy group and the like; and m represents an integer from 0 to 6) and the like; and Rrepresents a hydrogen atom, an optionally substituted Calkyl group, an optionally substituted Calkenyl group or an optionally substituted Calkynyl group), a salt thereof or a hydrate of them.

Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts

Fluorides of 4-substituted piperidine derivatives

The present invention provides a novel compound useful as a medicament, an acetylcholinesterase inhibitor, and an agent for preventing, treating and improving various kinds of senile dementia, Alzheimer-type senile dementia, cerebrovascular dementia or attention deficit hyperactivity disorder, namely, 1-benzyl-4-&lsqb;(5,6-dimethoxy-2-fluoro-1-indanone)-2-yl&rsqb;methylpiperidine represented by the following formula:

1-benzyl-4&lsqb;(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl&rsqb;methylpiperidine

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Cyclic amide derivatives

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH.sub.2)n-Z in which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R.sup.2 and R.sup.4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Bicyclic amide derivatives, compositions and methods of treatment

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH2)n--Z in which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Benzoxazine derivatives

The cyclic amide derivative is defined by the formula (I) or a salt thereof:

1,2,3,4 tetrahydropteridinone cyclic amide derivatives

2H-3,4-tetrahydroquinazoline-2-one and

The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1--(CH2)n-z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22) r--, R22 being H or methyl, --CO-- (CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.

Cyclic amine compounds and pharmaceutical use

A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22)r--, R22 being H or methyl, --CO--(CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.

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Ibaraki, Japan

Takashi Kosasa