Title:
抗腫瘍および神経保護活性を有する、アミノアルキルステロール化合物
Document Type and Number:
Japanese Patent JP4601297
Kind Code:
B2
Abstract:
Sterol derivatives (I) are new. Sterol derivatives of formula (I) are new. T1, T2 = H or Me, Me being in alpha- or beta-configuration; T4 = H, Me or Et; T3 = H or beta-Me; dotted line = optional additional 5(6) or 6(7) bond; Z = H or OH in the 5- or 8-position; R = -Q0-Q1 in the 6- or 7-position; Q0 = -X-(CH2)n-(Y1-(CH2)n)p-(Y2-(CH2)n)p-(Y3-(CH2)n)p-(Y4-(CH2)n)p-(Y5-(CH2)n)p-; each p = 0 or 1; each n = 0-4; X = S, O, CH2, NR3 or imidazole-1,5-diyl; R3 = H or 1-4C alkyl; Y1 - Y5 = S, O, C or NR3; Q1 = indolyl, morpholino, thiomorpholino, 1-(R1)-imidazol-5-yl, NR1R2 or pyrrole or pyrrolidine ring; R1 = H, COMe or 1-4C alkyl; R2 = H or 1-4C alkyl; or NR1R2 = piperidine, pyridine or piperazine ring (optionally substituted by 1-4C alkyl); and provided that: (1) if X = NH and Q1 = dialkylamino, then at least one p is other than 0; (2) if X(CH2)n = CH2CH2 and all p = 0, then Q1 is other than NH2; (3) in Z, OH is not bonded to an atom carrying a double bond; (4) R is not bonded to an atom carrying a double; and (5) n is not 0 in the (CH2)n bonded to X. An Independent claim is included for the preparation of (I).
Inventors:
Poor Arrow, Mark
De Medina, Philip
Poireau, Sandrine
De Medina, Philip
Poireau, Sandrine
Application Number:
JP2003586169A
Publication Date:
December 22, 2010
Filing Date:
April 18, 2003
Export Citation:
Assignee:
Institut National de la Saint ed Lar Surche Medical
International Classes:
A61K31/575; C07J41/00; A61K31/58; A61P25/00; A61P25/16; A61P25/28; A61P35/00; A61P37/04; C07J43/00
Domestic Patent References:
| JP62501446A |
Foreign References:
| FR2047880B1 | ||||
| WO1997010836A1 |
Other References:
ELKIHEL,L. et al.,Synthesis and preliminary in vitro evaluation of antitumor nitrosoureido cholesterol derivatives ,Arzneim.-Forsch./Drug Res.,1995年,Vol.45(I),No.2,p.190-194
EL KIHEL, L.,ANTICANCER RESEARCH,1999年,V19 N2A,P1229-1234
PINHAS,H. et al,6-Amino derivatives of stigmastanol and cholestanol,Journal of Medicinal Chemistry,1971年,Vol.14, No.11,p.1048-1049
EL KIHEL, L.,ANTICANCER RESEARCH,1999年,V19 N2A,P1229-1234
PINHAS,H. et al,6-Amino derivatives of stigmastanol and cholestanol,Journal of Medicinal Chemistry,1971年,Vol.14, No.11,p.1048-1049
Attorney, Agent or Firm:
Yuzo Sanada
Ohara Shizuo
Ohara Shizuo