Otsuka Pharmaceutical Company, Limited

Otsuka Pharmaceutical Factory, Inc.

Yoshihito Yamamoto

Mitsuru Hirohashi

Setsuro Fujii

Yutaka Kojima

Masatoshi Inai

Fumio Shimizu

Takashi Sakamoto

Makoto Sakamoto

Kazuhiko Tsutsumi

Tetsuhiko Shirasaka

Hideki Takasu

Shizuo Nakamura

Masaaki Motoyama

Setsuro Fujii, Deceased

Naosumi Kinoshita

Takeshi Imaoka

By Shinichiro Fujii, Successor

By Keiko Fujii, Successor

By Kaoruko Takada, Successor

This invention provides a carbostyril derivative of the formula (1): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined, or its salt. This carbostyril derivative or its salt possess an excellent matrix metalloproteinases inhibitory action.

Carbostyril derivatives as matrix metalloproteinases inhibitors

Novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, having the activities for inhibiting bone calcium absorption, for lowering the blood level of calcium, as analgesics, for inhibiting secretion of the gastric juice. Pharmaceutical composition can be prepared by formulating, at least one of the novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, together with a proteolytic enzyme inhibitors and/or pharmaceutically acceptable acids. The pharmaceutical composition are quite effective as agents for curing hypercalcemia, for curing Peget's disease, for curing osteoporosis, analgetic agent, anti-ulcerative agent and the like.

Polypeptide derivatives and calcium metabolism improving agent

Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.

Polypeptide derivatives

5-fluorouracil derivatives

Derivatives of 5-deoxy-fluorouridine are disclosed of formula (1) ##STR1## in which one of R and R is a substituted furanylmethyl or thienylmethyl group; and the other R and R is a lower alkanoyl group with one free amino substituent or a salt thereof.

3'-O-,5'-O-derivatives of 2'-deoxy-5-fluorouridine

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Otsu, Japan

Yoshihito Yamamoto