Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Rogyo Kabushiki Kaisha

Satoshi Nakanishi

Hiroshi Sano

Hiroshi Kase

Isao Kawamoto

Toru Yasuzawa

Katsuhiko Ando

Koji Yamada

Noriaki Hirayama

Joji Goto

Etsuyo Shimizu

Hideaki Kusaka

Kimihisa Ueno

Yoshihisa Ohta

Kotaro Takasaki

Hiroshi Yano

Yutaka Saito

Chikara Murakata

Junichi Shimada

Etsuo Ohshima

Yuji Nomoto

Yuzuru Matsuda

Ichiro Miki

Shizuo Shiozaki

Hitoshi Arai

Seiji Aratake

Koji Suzuki

Koji Yanagawa

Tohru Yasuzawa

Hiroshi Ishida

Tsutomu Matsumura

Motoki Miyama

Katsuya Kobayashi

Miho Suda

Yosuke Yamaura

Keiko Ohsawa

Ari Kawabe

Katsuichi Shutoh

Takashi Sato

Shinya Fujii

Miho Iwase

Akira Ogawa

Chiharu Nakagawa

[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; Rrepresents &#x2014;NRR(wherein Rand Rmay be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); Rrepresents the above Formula (II), Formula (IV) or the like; A represents a single bond, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;SO&#x2014;, &#x2014;OC(&#x2550;O)&#x2014; or the like; and Rrepresents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.

Bicyclic pyrimidine derivatives

A condensed purine derivative represented by Formula (I):wherein X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O or N&#x2550;C&#x2014;W, Rrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, Vrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, Vrepresents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when Vrepresents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O and Rrepresents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, &#x2014;NRR, &#x2014;COH, a lower alkoxycarbonyl group, &#x2014;COHal, &#x2014;CONRRor &#x2014;CHO, Vmay represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.

Fused purine derivatives

Remedies for diabetes

A new compound designated KS-505 having amnesia-inhibiting activity may be prepared by fermentation of a suitable strain of Streptomyces, preferably Streptomyces argenteolus A-2 (FERM BP-2065). The compound is thought to have the structure: ##STR1##

Compound KS-505 useful for improving cerebral function

Disclosed are KS-501 derivatives represented by the formula (I) ##STR1## wherein X represents a hydrogen atom or COOR.sub.3, Y represents hydroxy or ##STR2## and R.sub.1, R.sub.2 and R.sub.3 are the same or different and represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, provided that when R.sub.1, R.sub.2 and R.sub.3 are simultaneously hydrogen atoms, and when R.sub.1, R.sub.2 and X are simultaneously hydrogen atoms, Y does not represent ##STR3## and a pharmaceutically acceptable acid addition salt thereof. The KS-501 derivatives have a platelet aggregation-inhibiting property, and are expected to be useful as antithrombotic agent.

KS-501 derivatives

Novel physiologically active substances KS-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.

Novel substances KS-504a, KS-504b, KS-504d and KS-504e and process for

Novel physiologically active substances Ks-504a, KS-504b and KS-504d having a vasodilative activity and a novel physiologically active substance KS-504e having an activity to inhibit histamine secretion are produced by culturing a microorganism of the genus Mollisia.

Novel physiologically active substances KS-501 and KS-502 having inhibitory activity on serotonin release from platelets and/or platelet aggregation are produced by culturing a microorganism of the genus Sporothrix.

Novel substances KS-501 and KS-502 and process for their preparation

Growing community of inventors

Machida, Japan

Satoshi Nakanishi