发明名称 Apoptosis inducing adamantyl derivatives and pharmaceutical uses
摘要 In the adamantyl group derivatives of formula I to IV; W is CH2, O, S, SO or SO2; X is a radical selected from optionally substituted naphthalene, benzofuran, indazole or other group; R1 and R'1 is H, halogen or a lower alkyl radical; R2 is a hydroxyl radical, an optionally substituted alkyl radical, an optionally substituted alkoxyl radical, an acyl radical, an aminocarbonyl radical or a halogen; R3 is H, a hydroxyl, alkyl or alkoxyl radical; or R2 and R3 can form together a radical O-CH2-O; R4 is H, an alkyl or alkoxyl radical or a halogen; R5 is COR10, a halogen or an optionally substituted alkyl radical (wherein R10 is a hydroxyl radical, an alkoxy radical or a radical of formula Nr'r" (wherein r' and r' represent H, optionally substituted aminoalkyl, mono or polyhydroxyalkyl, optionally substituted aryl radical or an amino acid or sugar residue); R6 is H, halogen, a hydroxyl group or an alkoxyl radical; and R7 is H or a halogen. These adamantyl retinoid derivatives induce apoptosis of cancer cells and may be used for the treatment of cancers and solid tumors. The compounds may also be used as active agents for the treatment or prevention of keratinization disorders, dermatological conditions, osteoporosis, arteriosclerosis, myocardial infarction, arthritis or alopecia.
申请公布号 NZ333800(A) 申请公布日期 2000.08.25
申请号 NZ19970333800 申请日期 1997.07.08
申请人 GALDERMA RESEARCH & DEVELOPMENT SOCIETE EN NOM COLLECTIF 发明人 PFAHL, MAGNUS;LU, XIAN-PING;RIDEOUT, DARRYL;ZHANG, HONGYUE
分类号 C07D243/08;A61K8/00;A61K8/11;A61K8/14;A61K8/30;A61K8/36;A61K8/368;A61K8/37;A61K8/42;A61K8/49;A61K31/05;A61K31/085;A61K31/166;A61K31/167;A61K31/192;A61K31/216;A61K31/235;A61K31/34;A61K31/343;A61K31/36;A61K31/4166;A61K31/495;A61K31/496;A61K31/5375;A61K31/551;A61K31/7048;A61P35/00;A61Q5/02;A61Q19/00;C07C65/17;C07C65/26;C07C69/157;C07C69/94;C07C235/66;C07D235/12;C07D295/18;C07D317/60;C07D405/10;C07D493/08;C07H17/08;(IPC1-7):A61K31/36;C07D307/79;C07D265/30;C07C63/66;C07C233/64;A61K31/41;C07D241/04;C07D317/46;C07D235/08 主分类号 C07D243/08
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