ARMANI, ELISABETTA,GHIDINI, ELONORA,PERETTO, ILARIA,VIRDIS, ANDREA
申请号：
PE0003032012
公开号：
PE08942012A1
申请日:
2010.09.01
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Isoxazolidina refers to compounds of formula (i) wherein R1 is - (CH2) n Z - n - (CH2) R4, where N and N are each from 0 to 2 Z is a Union simple, S, o, co, among others R4 is H, halogen Oh, CN, arylalkyl (C1 - C6), among others R2 is H, alkyl (C2 - C6), (CH2) MR5, among others, where R5 is optionally substituted heteroaryl and with OXO, Oh, halogen, NS,Among others M is 0 to 6 X and y are each H or Halogen.Preferred compounds are: (4aR, 5S, 4BS, 6aS, 6BR, 9aS, 10aS, 10bS) - 8 - furan - 3 - methyl - 5 - hydroxy - 6B - (2 - hydroxy Acetyl) - 4a, 6a - dimethyl - 5,6,6a, 4a, 4b, 6B, 8,9,9a, 10,10a, 10b 11,12 - tetradecahidro - 7 - 8 - aza oxa - pentaleno [2,1-a] fenantren - 2 - One (4aS, 4bR, 5S, 6aS, 6BR, 9aS, 10aS, 10bS, 12S) - 4b, 12 - difluoro - 8 - 2 - methyl - 5 - Furan Hydroxy 6B - (2 - hydroxy Acetyl) - 4a, 6a - dimethyl - 5,6,6a, 4a, 4b, 6B, 8,9,9a, 10,10a, 10B, 11Tetradecahidro - 12 - 7 - 8 - aza oxa - pentaleno [2,1-a] fenantren - 2 - One among others. It also relates to a preparation method and a Pharmaceutical composition. These compounds are useful in the treatment of glucocorticoids in asthma, chronic bronchitis, chronic obstructive pulmonary diseaseSE REFIERE A COMPUESTOS DERIVADOS DE ISOXAZOLIDINA DE FORMULA (I) DONDE R1 ES (CH2)n-Z-(CH2)n-R4, EN DONDE n Y n SON CADA UNO DE 0 A 2 Z ES UNA UNION SIMPLE, S, O, CO, ENTRE OTROS R4 ES H, HALOGENO, OH, CN, ARILALQUILO(C1-C6), ENTRE OTROS R2 ES H, ALQUILO(C2-C6), (CH2)mR5, ENTRE OTROS, EN DONDE R5 ES HETEROARILO OPCIONALMENTE SUSTITUIDO CON OXO, OH, HALOGENO, CN, ENTRE OTROS m ES DE 0 A 6 X E Y SON CADA UNO H O HALOGENO. SON COMPUESTOS PREFERIDOS: (4aR,4bS,5S,6aS,6bR,9aS,10aS,10bS)-8-FURAN-3-ILMETIL-5-HIDROXI-6b-(2-HIDROXI-ACETIL)-4a,6a-DIMETIL-4a,4b,5,6,6a,6b,8,9,9a,10,10a,10b,11,12-TETRADECAHIDRO-7-OXA-8-AZA-PENTALENO[2,1-a]FENANTREN-2-ONA (4aS,4bR,5S,6aS,6bR,9aS,10aS,10bS,12S)-4b,12-DIFLUORO-8-FURAN-2-ILMETIL-5-HIDROXI-6b-(2-HIDROXI-ACETIL)-4a,6a-DIMETIL-4a,4b,5,6,6a,6b,8,9,9a,10,10a,10b,11,12-TETRADECAHID
