Taiho Pharmaceutical Company Limited

Other

Shigeo Okajima

Takahiro Asai

Masanori Asai

Kazuhisa Minamiguchi

Shinichi Aoki

Hiroyoshi Yamanaka

Suguru Dohi

Tetsuji Asao

Shozo Yamada

Kazuhiko Shigeno

Yoshio Ogino

Yukio Tada

Yoshimitsu Suda

Tomohiro Yamashita

Nobuhiko Katsunuma

Kazuhiro Kitagawa

Atsuhiko Uemura

To provide a compound having an inhibitory activity for an androgen receptor. A fused pyrimidine compound represented by the following formula (I) or a pharmaceutically acceptable thereof (in the formula, X, Y, Z, R, and Rare as defined in the specification). 

Fused pyrimidine compound or salt thereof

A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof 

Tetrahydropyridopyrimidine compound or salt thereof

A tetrahydropyridopyrimidine compound represented by formula (I) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition including the tetrahydropyridopyrimidine compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier: 

A method of manufacturing substance GM-95 having general formula &lsqb;I&rsqb;, comprising (a) deprotecting a macrocyclic compound having general formula &lsqb;II&rsqb; (wherein, R 's are the same or different and each represents a lower alkyl group, and R represents a thiol protecting group) by removing acetal protecting groups (the R 's) thereof, and forming an oxazole ring through an intramolecular cyclization reaction between produced formyl group and an amide group, and (b) deprotecting a resulting macrocyclic compound having general formula &lsqb;III&rsqb; (wherein, R is as mentioned above) by removing the thiol protecting group (R ) thereof, and forming a thiazoline ring through an intramolecular cyclization reaction between a thiol group thus produced and an amide group.

Process for preparing substance GM-95

Epoxysuccinamide derivative or salt thereof

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Tsukuba, Japan

Shigeo Okajima