Eisai Company, Limited

Genox Research, Inc.

Japan As Represented by General Director of Agency of National Center for Child Health & Development

Takeshi Nagasu

Kentaro Yoshimatsu

Nozomu Koyanagi

Hiroshi Yoshino

Yoshihiko Kotake

Kyosuke Kitoh

Jun Niijima

Norihiro Ueda

Tatsuo Watanabe

Toshimi Okada

Kappei Tsukahara

Hiroyuki Sugumi

Makoto Asada

Atsumi Iijima

Takashi Owa

Kyosuke Kito

Toru Haneda

Yoichi Ozawa

Naoko Tsukahara

Tatsuo Okauchi

Kaoru Ogawa

Yuji Sugita

Tomoko Fujishima

Naoko Sugi

Yoshimasa Machida

Shigeto Negi

Isao Saito

Seiichiro Nomoto

Ieharu Hishinuma

Takayuki Hida

Kanemasa Katsu

Norimasa Miyamoto

Michael D Lewis

Ryoichi Hashida

James J Kowalczyk

Hu Yang

Naoko Hata

Toshimitsu Uenaka

Takeo Kanai

Takatoshi Kawai

Atsumi Yamaguchi

Yukio Ohya

Yukiho Imai

Ana Maria Garcia

Katsuji Nakamura

Hiroyuki Kato

Keiko Matsui

Nei Yoshida

Tadahiro Oshida

Masaya Obayashi

Shigemichi Gunji

Izumi Obayashi

Akira Yokoi

Junro Kuromitsu

Hirovuki Sugumi

Rulin Fan

Edmund M Harrington

Amy E Christuk

Xiaoning C Sheng

Gozoh Tsujimoto

Jun-ichi Kamata

Eiki Takahashi

Susceptibility of a tumor cell to an anticancer agent is tested by measuring an expression level or levels of a gene or genes selected from the group consisting of the genes listed in Tables 3 and 4 in a tumor cell collected from a cancer patient treated with an anticancer agent (E7070 and related compounds thereof), or causing the anticancer agent to act on a tumor cell collected from a cancer patient and measuring an expression level or levels of a gene or genes selected from the group consisting of the genes listed in Tables 3 and 4 in the tumor cell, and determining that the tumor cell is susceptible to the anticancer agent when the expression level or levels of the gene or genes listed in Table 3 increase, or the expression level or levels of the gene or genes listed in Table 4 decrease.

Method of testing anticancer agent-sensitivity of tumor cells

The differential display method was used to search for a gene whose expression level in eosinophils collected from patients with atopic dermatitis differs in the exacerbation stage and in the remission stage. As a result, gene '2090-05' showing a significant increase in expression in eosinophils of patients in the remission stage was isolated. This gene is usable in testing for an allergic disease and screening for a candidate compound for a therapeutic agent therefor an allergic disease.

Method of testing for allergic diseases

An appetite-stimulating agent and a therapeutic agent for anorexia, each comprising, as an active ingredient, a sulfonamide derivative or sulfonic acid ester derivative represented by the following general formula (I):

Appetite-stimulating agents and remedies for anorexia

T cells from multiple subjects who showed different cedar pollen specific IgE titers were prepared before and after cedar pollen dispersal, and differential display analysis was performed to screen for pollen antigen responsive genes. As a result, a novel gene was successfully isolated whose expression is significantly higher in subjects with high cedar pollen specific IgE titer. The inventors have found that it is possible to use this gene to test for an allergic disease and to screen for candidate compounds for therapeutic drugs for an allergic disease.

Pollen allergy-related gene 513

Fused polycyclic heterocycle derivatives

Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16); and n represents 0, 1 or 2, R.sup.3 to R.sub.13, R.sup.15 and R.sup.16 each represent hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lower acyl.

Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives

A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).

Isoprenyl transferase inhibitors

Novel heterobicyclic sulfonamide and sulfonic ester derivatives represented by the following general formula (I), which exhibit an antitumor activity and are lowly toxic, and processes for the preparation thereof. A sulfonamide derivative and a sulfonic ester derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein variables A, W, X, B, C, Y, Z are as defined in the specification.

7-Amino-1H-indoles

Heterobicyclic sulfonamide and sulfonic ester derivatives

Sulfonamide compounds of formula (I) or a pharmacologically acceptable salt thereof: ##STR1## exhibit excellent antitumor activity and low toxicity.

Pyrimidinyl or pyridinyl sulfonamide substituted compounds

Sulfonamide compounds of the formula or pharmacologically acceptable salts thereof: ##STR1## wherein: R.sup.1 is a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, nitro group, phenoxy group, cyano group, acetyl group, amino group or a protected amino group; R.sup.2 and R.sup.3 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group; R.sup.4 and R.sup.7 may be the same or different from each other and each is a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkoxy group, amino group or amino group substituted with a lower alkyl or a phenyl group; A is .dbd.CH--; B is .dbd.CH--; and E is selected from the group consisting of ##STR2## in which Q is an oxygen atom or a sulfur atom; and R.sup.11 is a hydrogen atom, a lower alkyl group, an amino group which may be substituted with a lower alkyl group, a lower alkoxy group, a 2-thienyl group, a 2-furyl group, phenyl group or a phenyl group having from 1 to 3 substituents, said substituents being the same or different from one another and selected from the group consisting of a halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, carboxyl group, esterified carboxyl group, amidated carboxyl group, lower alkylthio group and phenoxy group; and (b) a phenyl group or a phenyl group having from 1 to 3 substituents.

Sulfonamide phenyl substituted compounds

Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them, have an excellent antitumo-activity.

Sulfonamide derivatives

Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptable salts of them, have an excellent antitumor activity.

Pyridine carboxamide compounds which have useful as pharmaceutical

Growing community of inventors

Ibaraki, Japan

Takeshi Nagasu