公开(公告)号：EP1341745A1

公开(公告)日：2003-09-10

申请号：EP01982482.0

申请日：2001-11-13

申请人： F.HOFFMANN-LA ROCHE AG

发明人： BARBIER, Pierre ,  BAUER, Franz, W. ,  MOHR, Peter ,  MULLER, Marc ,  PIRSON, Wolfgang

IPC分类号： C07C43/178 ,  C07C35/17 ,  C07C235/08 ,  C07C233/18 ,  C07C49/242 ,  C07C69/30

CPC分类号： C07C235/08 ,  C07B2200/07 ,  C07B2200/09 ,  C07C35/21 ,  C07C45/29 ,  C07C47/27 ,  C07C233/18 ,  C07C403/04 ,  C07C403/08 ,  C07C403/10 ,  C07C403/12 ,  C07C403/16 ,  C07C403/18 ,  C07C2601/14

摘要： Disclosed are retiferol derivatives of formula (I): wherein X is > C=CH2 or -CH2-; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is -O(CH2)3-, -(CH2)2-(1,2-C6H4)-, -CH=CH-(1,2-C6H4)-, -C=C-(1,2-C6H4)-, -(CH2)2-CO-, -CH2-O-CO-, -CH2NHCO-, or -CH2NHCOCH2-; R1 is C1-C5-alkyl; R?2 and R3¿ are independently of each other alkyl or perfluoroalkyl; and R4 is hydrogen, hydroxy, C1-C5-alkyl or C1-C5-alkyl or C1-C5-alkoxy; the use of such compounds to treat or present hyperproliferative skin diseases such as psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; neoplastic diseases; disorders of the sebaceous glands such as acne and seborrhoic dermatitis; the use of these compounds in reversing the conditions associated with photodamage, particularly for the oral or topical treatment of the skin damaged through sun exposure, the effects of wrinkling, elastosis and premature ageing, furthermore a process for the manufacture of such compounds as well as pharmaceutical compositions containing such compounds.

摘要翻译： 本发明公开了式retiferol衍生物（I）：worin X是> C = CH 2或-CH 2 - ; Y和Z是unabhängig海誓山盟氢，氟或羟基的; A是-O（CH 2）3 - ， - （CH2）2-（1,2C6H4） - ， - CH = CH-（1,2C6H4） - ，-C = C-（1,2C6H4） - ， - （CH 2）2 CO-，-CH2-O-CO-，-CH2NHCO-，或-CH2NHCOCH2-; [R <1>是C1-C5烷基; [R <2>和R <3>是unabhängig海誓山盟烷基或全氟烷基的; 且R <4>是氢，羟基，<1> C5烷基或C1-C5烷基或C1-C5烷氧基C。; 使用寻求化合物治疗或本过度增生的皮肤病：如牛皮癣，基底细胞癌，角质化和角化的障碍; 肿瘤性疾病; 皮脂腺的障碍：如痤疮和脂溢性皮炎; 逆转与光伤害有关的病况，特别是用于由阳光曝晒引起的皮肤伤害的口服或局部治疗，起皱，弹性组织变性和早衰，进一步更寻求化合物的制造方法的效果以及使用合成的化合物的 药物组合物含有测试化合物。