Dainippon Pharmaceutical Company, Limited

Asahi Glass Company, Limited

Buichi Fujitani

Arata Yasuda

Tomoyuki Asai

Yasushi Matsumura

Robert George Boyle

Keiichi Uchida

Toshiaki Kadokawa

Fuminori Sato

Mitsue Notake

Takashi Deguchi

Ryotaro Shiratake

Kanoo Hosoki

Naonobu Hatano

Makoto Murata

Toshiyuki Negoro

Yoshiyuki Ono

Yayoi Honda

Shozo Ueda

Yoshitomo Morizawa

Akihiko Kiyoshi

Taku Yamamoto

Graham Andrew Showell

Sukhbinder Singh Klair

Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein Ris cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; Ris H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; Ris (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): Rand Rare independently H or OH, but Rand Rare not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.

Pyrrolidine derivatives and their use as chymase inhibitor

Prostaglandin I.sub.2 derivatives

Tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3'-pyrrolidine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, or nitro, and R.sup.3 is hydrogen, halogen or alkyl having 1 to 6 carbon atoms, and pharmaceutically acceptable salts thereof, processes for preparation thereof, and pharmaceutical composition containing the same. Said compounds and their salts show excellent aldose reductase inhibitory activity and are useful for the prevention and treatment of diabetic complications.

Tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3'-pyrrolidine derivatives,

A 6-fluoroprostaglandin having the formula: ##STR1## wherein A is a carbonyl group or a hydroxymethylene group, R.sup.1 is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl group or a substituted or unsubstituted 5- or 6-membered cycloalkyl group, R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group, each of R.sup.3 and R.sup.4 which may be the same or different is a hydrogen atom or a protecting group, R.sup.5 is a hydrogen atom or a hydroxyl group, and is a single bond or a double bond, and its salt when R.sup.2 is a hydrogen atom.

6-fluoroprostaglandins

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Sakai, Japan

Buichi Fujitani