Takeda Chemical Industries, Inc.

Koichiro Ootsu

Hiroshi Akimoto

Kazuyoshi Aso

Fumio Itoh

Yukimasa Nozaki

Tsuneaki Hida

Takafumi Ishii

This invention provides a novel compound TAN-1813 having farnesyltransferase-inhibitory, cell growth-inhibitory, and anti-tumor activities; its production; farnesyltransferase-inhibiting agent; anti-tumor agent; pharmaceutical composition comprising a compound TAN-1813; and a novel microorganism capable of producing said compound.

Octahydro-2-naphthalenecarboxylic acid derivative, its production and use

A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, 0 or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.

Condensed heterocyclic compounds, their production and use

A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.

Pyrrolopyrimidinyalglutaminate derivatives and their use

A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, O or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.

Disclosed is an immunostimulant agent containing interleukin-2 and 5'-deoxy-5-fluorouridine or a salt thereof in combination, which shows a strong therapeutic effect by synergistic action and weak side effects. The immunostimulant agent may further contain another chemotherapeutic agent and/or another immunotherapeutic agent.

Growing community of inventors

Mishima, Japan

Koichiro Ootsu