Nippon Kayaku Kabushiki Kaisha

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Mercian Corporation

Tetsuya Someno

Tomio Takeuchi

Hamao Umezawa

Shinichi Ishii

Takaaki Aoyagi

Tetsushi Saino

Kazuo Kato

Masaaki Ishizuka

Yasuhiko Muraoka

Hideo Sugimura

Kunio Isshiki

Makoto Tsuda

Yasushi Takahashi

Naoto Kawamura

Hiroyuki Inoue

Tomohiro Sameshima

Hiroyuki Kumagai

Motoko Matsufuji

Fumika Yamada

A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents &#x2014;O&#x2014; and R represents a hydroxyl group, by using a microorganism belonging to the genus; and asp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents &#x2014;O&#x2014; or &#x2014;CH&#x2014;, and R represents a hydroxyl group when X represents &#x2014;O&#x2014;, or a hydrogen atom when X represents &#x2014;CH&#x2014;.

Osteoclast differentiation inhibitors

The present invention discloses a new .alpha.-keto amide derivative or a salt thereof represented by the formula (1): ##STR1## wherein X represents (1) a peptide residue or amino acid residue in which the functional group may be protected, (2) a hydrogen atom or (3) an amino-protective group, Y represents a peptide residue or amino acid residue in which the functional group may be protected, E represents a substituent on the alkylene (C.sub.n H.sub.2n-1) and is a halogen, lower alkoxy or hydrogen, A represents a carbonyl group or mono- or di-substituted methylene (the substituent being a hydroxy, lower alkoxy, phenylimino or benzylimino), and n represents an integer of 2 to 6. The compound of the present invention is effective in inhibiting prolyl endopeptidase activity and useful as an active ingredient of an enzyme inhibitor.

.alpha.-keto amide derivatives

A protease adsorbent wherein valyl-glycyl-argininal is bound to a water-insoluble carrier and a process for purifying TPA utilizing the same.

Protease adsorbent and process for purifying TPA utilizing the same

A biospecific adsorbent comprising pyroglutamyl-lysyl-leucyl-argininal combined with a water-insoluble support is provided. This biospecific adsorbent is useful as an adsorbent for use in affinity chromatography and can be utilized for the purification of proteases such as urokinase.

Water-insoluble biospecific absorbent containing argininal derivative

L-Argininal derivatives of the general formula: ##STR1## are disclosed. A method of manufacturing any such derivative is also disclosed. The L-argininal derivative of this invention has a strong inhibitory activity on proteases, such as serine and thiol proteases, and is expected to provide useful medicines, including those which are effective for diseases caused by abnormal elevation of protease activity.

L-Argininal derivatives and a method of manufacturing the same

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Saitama, Japan

Tetsuya Someno