Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Hiroyuki Tawada

Kanji Meguro

Yutaka Kuwada

Hitoshi Ikeda

Hideaki Natsugari

Makoto Yamashita

Zen-ichi Terashita

Yoshiaki Sato

Isao Aoki

Hiroshi Banno

Keiji Kamiyama

Tsuneo Kanamaru

Masaki Ogino

Fumio Itoh

Masafumi Nakao

Mari Adachi

Misayo Sera

Yujiro Ono

Takashi Sohda

Kaneyoshi Kato

Yoshihiro Banno

Shogo Marui

Satoru Oi

Motoki Ikeuchi

Taihei Yamane

Norihiko Moriya

Koji Ikedou

Takao Matsuo

Koji Takeuchi

Osamu Yabe

Norihiko Ohashi

Fumio Ito

The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein Rand Rare each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like. 

Coumarin derivative and use thereof

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein Rand Rare each hydrogen or an optionally substituted hydrocarbon group; Ris an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Process for preparing optically active 2,3-dihydrobenzofuran compounds

A novel process for efficiently and easily producing a compound represented by the formula: wherein ring A is a benzene ring that may be optionally further substituted in addition to the group represented by W, or a salt thereof; which comprises reacting a compound represented by the formula: wherein Rand Rare the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, Y is a halogen atom, ring A is a benzene ring that may be optionally further substituted in addition to the group represented by Y and ring B is an optionally substituted benzene ring, or a salt thereof, with a compound represented by the formula:WHwherein W is wherein ring C is an optionally substituted benzene ring, ring D is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, Ris a hydrogen atom, an aliphatic hydrocarbon group containing an aromatic group or an acyl group, and Ris a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof and thereafter, if necessary, deprotecting the resultant product, which is suitable for industrial production.

Process for producing benzofuran derivative

The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; Rand Rare the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Fused heterocyclic compounds

A novel process for efficiently and easily producing a compound represented by the formula:wherein ring A is a benzene ring that may be optionally further substituted in addition to the group represented by W, or a salt thereof; which comprises reacting a compound represented by the formula:wherein Rand Rare the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, Y is a halogen atom, ring A is a benzene ring that may be optionally further substituted in addition to the group represented by Y and ring B is an optionally substituted benzene ring, or a salt thereof, with a compound represented by the formula:WHwherein W iswherein ring C is an optionally substituted benzene ring, ring D is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, Ris a hydrogen atom, an aliphatic hydrocarbon group containing an aromatic group or an acyl group, and Ris a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof and thereafter, if necessary, deprotecting the resultant product, which is suitable for industrial production.

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound:[wherein Rand Rare each hydrogen or an optionally substituted hydrocarbon group; Ris an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Process for producing amine derivatives

Process for the preparation of oxazole derivatives

Sulfonamide derivatives, their production and use

Oxazolone derivatives and their use as anti-helicobacter pylori agents

Sulfonamide derivatives, processes for producing the same and utilization thereof

An anti-,agent comprising a compound represented by the formula:

Oxazolone derivatives and their use as anti-Helicobacter pylori agent

Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

Tricyclic heterocyclic compounds, their production and use

A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Heterocyclic amine derivatives, their production and use

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Takatsuki, Japan

Hiroyuki Tawada