Nippon Chemiphar Co., Ltd.

Suntory Limited

Other

Michiko Ishida

Haruhiko Shinozaki

Mitsuo Masaki

Atsushi Tendo

Norihisa Miyake

Keiko Shimamoto

Hiromitsu Takeda

Yasufumi Ohfune

Yutaka Nomura

Yasunori Goto

Takeo Taguchi

A cyclopropylglycine derivative having the following formula:

Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors

Disclosed are new alkylenediamine derivatives of the following formula which are effective for treatment of dysuria are disclosed: ##STR1## wherein R.sup.1 is hydrogen, alkyl, or a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.2 is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.3 and R.sup.4 represent hydrogen, alkyl, aralkyl or aryl; or R.sup.3 and R.sup.4 are combined to form one of substituted or unsubstituted 5- to 7-membered heterocyclic groups; X is oxygen, sulfur or imino; Y is oxygen or sulfur; Z is --CH.sub.2 --, --CO-- or --CS--; m is an integer of 0-4; n is an integer of 0-4; r is 0 or 1; and p and q represent an integer of 0-5 provided that p plus q is 1-5.

N-aminoalkyl-substituted nitrogen-containing six membered heterocyclic

Alkylenediamine derivatives

N-aminoalkyl-substituted nitrogen-containing five membered heterocyclic

(2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)-glycine (DCG-I) and (2S,1'S,2'S,3'S)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-II), as well as methods for synthesizing these compounds are provided. Studies on L-glutamate receptors with the use of DCG-I and DCG-II, which are agonists for NMDA receptors, contribute to the development of remedies for various nervous disorders. Further, DCG-I and DCG-II selectively inhibit monosynaptic reflex even at a low concentration, which makes them useful as a remedy for spastic palsy, an anesthetic and an analgesic.

2-(2,3-dicarboxycyclopropyl) glycine and method for producing the same

(2R,3S,4S)-.alpha.-(carboxycyclopropyl)glycine of the formula (1) and salts thereof are disclosed. ##STR1## The compound (1) exhibits most potent depolarizing activities among the known NMDA agonists and will be a useful tool to investigate various neuronal functions related to the excitatory amino acid receptors.

(2R,3S,4S)-.alpha.-(carboxycyclopropyl)glycine

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Saitama, Japan

Michiko Ishida