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Pub. No.:    WO/2005/123671    International Application No.:    PCT/JP2005/011343
Publication Date: 29.12.2005 International Filing Date: 21.06.2005
C07D 207/34 (2006.01), A61K 31/40 (2006.01), A61K 31/4025 (2006.01), A61K 31/422 (2006.01), A61K 31/435 (2006.01), A61K 31/439 (2006.01), A61K 31/4439 (2006.01), A61K 31/454 (2006.01), A61K 31/496 (2006.01), A61K 31/506 (2006.01), A61K 31/5377 (2006.01), A61K 31/55 (2006.01), A61P 11/06 (2006.01), A61P 17/04 (2006.01), A61P 37/00 (2006.01), A61P 37/06 (2006.01), A61P 43/00 (2006.01), C07D 401/12 (2006.01), C07D 403/12 (2006.01), C07D 405/06 (2006.01), C07D 409/06 (2006.01), C07D 413/06 (2006.01), C07D 453/02 (2006.01), C07D 455/02 (2006.01)
Applicants: TAISHO PHARMACEUTICAL CO., LTD. [JP/JP]; 24-1, Takada 3-chome, Toshima-ku Tokyo 1708633 (JP) (For All Designated States Except US).
UMEMIYA, Hiroki [JP/JP]; (JP) (For US Only).
TAKAYAMA, Tetsuo [JP/JP]; (JP) (For US Only).
AMADA, Hideaki [JP/JP]; (JP) (For US Only).
SHIOZAWA, Fumiyasu [JP/JP]; (JP) (For US Only).
SATO, Masakazu [JP/JP]; (JP) (For US Only).
YABUUCHI, Tetsuya [JP/JP]; (JP) (For US Only).
KATAKAI, Hironori [JP/JP]; (JP) (For US Only)
Inventors: UMEMIYA, Hiroki; (JP).
TAKAYAMA, Tetsuo; (JP).
AMADA, Hideaki; (JP).
SHIOZAWA, Fumiyasu; (JP).
SATO, Masakazu; (JP).
YABUUCHI, Tetsuya; (JP).
KATAKAI, Hironori; (JP)
Agent: SATORI, Soichi; c/o TAISHO PHARMACEUTICAL CO., LTD. INTELLECTUAL PROPERTY DIVISION 24-1, Takada 3-chome, Toshima-ku Tokyo 1708633 (JP)
Priority Data:
2004-183894 22.06.2004 JP
(JA) ピロール誘導体
Abstract: front page image
(EN)A pyrrole derivative represented by the general formula (1): (wherein R1 represents hydrogen or C1-4 alkyl; R2 represents C1-10 alkyl, C3-10 cycloalkyl, methylenedioxyphenyl, 1,2-ethylenedioxyphenyl, 1,3-propylenedioxyphenyl, etc.; R3 and R4 are the same or different and each represents hydrogen, halogeno, C1-6 alkyl, or C1-6 alkoxy; and R5 represents hydrogen, halogeno, nitro, amino, hydroxy, C1-6 alkyl, C1-6 alkoxy, etc.) or a pharmaceutically acceptable salt of the derivative. The compounds inhibit the enzymatic activity of LcK, which participates in the abnormal activation of immunocompetent cells, and are useful for rejection reactions in organ transplantation or immune/allergic diseases such as atopic dermatitis and asthma.
(FR)Dérivé du pyrrole représenté par la formule générale (1) : (1) (dans laquelle R1 représente un hydrogène ou un alkyle en C1-4 ; R2 représente un alkyle en C1-10, un cycloalkyle en C3-10, un méthylènedioxyphényle, un 1,2-éthylènedioxyphényle, un 1,3-propylènedioxyphényle, etc. ; R3 et R4 sont identiques ou différents et chacun représente un hydrogène, un halogéno, un alkyle en C1-6 ou un alcoxy en C1-6 ; et R5 représente un hydrogène, un halogéno, un nitro, un amino, un hydroxy, un alkyle en C1-6, un alcoxy en C1-6, etc.) ou un sel acceptable du point de vue pharmaceutique du dérivé. Les composés inhibent l'activité enzymatique de la LcK, laquelle participe à l'activation anormale de cellules immunocompétentes et sont utiles pour des réactions de rejet dans une greffe d'organes ou des maladies immunes/allergiques telles que la dermite atopique et l'asthme.
(JA)一般式(1) (式中、R1は、水素原子又はC1-4アルキル基を示し、 R2はC1-10アルキル基、C3-10シクロアルキル基、メチレンジオキシフェニル基、1,2-エチレンジオキシフェニル基、1,3-プロピレンジオキシフェニル基等を示し、 R3及びR4は、同一又は相異なって水素原子、ハロゲン原子、C1-6アルキル基又はC1-6アルコキシ基を示し、 R5は水素原子、ハロゲン原子、ニトロ基、アミノ基、ヒドロキシ基、C1-6アルキル基、C1-6アルコキシ基等を示す。)で表されるピロール誘導体又はその製薬学的に許容される塩であり、免疫担当細胞の異常な活性化に関与するLckの酵素活性を阻害し、臓器移植時の拒絶反応やアトピー性皮膚炎・喘息などの免疫・アレルギー疾患に対して有用な化合物である。
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)