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DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA
专利权人:
RESPIVERT LIMITED
发明人:
KING-UNDERWOOD, JOHN,ITO, KAZUHIRO,MURRAY, PETER JOHN,HARDY, GEORGE,BROOKFIELD, FREDERICK ARTHUR,BROWNE, CHRISTOPHER JOHN
申请号:
PE0005062012
公开号:
PE13902012A1
申请日:
2010.10.19
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Refers to compounds derived from 2 - (1h pyrazolo [3,4-d] pyrimidine 1 - ylmethyl) quinazolin-4 (3H) - one of formula (i) wherein R1 is H, alkyl (C1 - C15) where one or more carbons can be replaced by a heteroatom such as o, N among others, and is optionally substituted aryl Halogen,, Heteroaryl is R3A, among others hydroxyl r3b is H, hydroxyl, Halo, NS,Among others, R4 and R5 are each H or alkyl (C1 - C3) X is aryl or heteroaryl (C6 C10) (c5-c9) replaced with 2A and R2B, where 2a is H, alkyl, Halo (C1 - C3), CN, among others R2B is H, alkyl (C1 - C3), Halo, haloalquilo (C1 - C3).Preferred compounds are: 2 - ((4 - (3 - amino - 4 - hydroxyphenyl) - 1H pyrazolo [3,4-d] pyrimidine 1 - yl) methyl) - 3 - (2 - clorobencil) - 5 - etinilquinazolin - 4 (3H) - One 6 - (2 - ((4 amino acid, 3 - (4-hydroxyphenyl) - 1H pyrazolo [3,4-d] - pyrimidine - 1 yl) methyl) - 3 - (2 - clorobencil) - 4 - oxo - 3.4 - dihidroquinazolin - 5 - yl) - 5 - inoico hex 2 - (N - (3 - (2 - ((4 - (3 - amino - 4 - hydroxyphenyl) - 1H pyrazolo [3,4 - d] pyrimidine 1 - yl) methyl) - 3 - (2 - clorobencil) - 4 - oxo - 3.4 - dihidroquinazolin - 5 - il) prop - 2 - in - 1 - il) acetamide among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of phosphoinositide 3 Kinase (PI3 kinase) to be useful in the treatment of cystic fibrosis, Asthma, sinusitis, Allergic dermatitisSE REFIERE A COMPUESTOS DERIVADOS DE 2-(1H-PIRAZOLO[3,4-d]PIRIMIDIN-1-ILMETIL)QUINAZOLIN-4(3H)-ONA DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C15) EN DONDE UNO O VARIOS CARBONOS PUEDEN SER REEMPLAZADOS POR UN HETEROATOMO TAL COMO O, N, ENTRE OTROS Y ESTA OPCIONALMENTE SUSTITUIDA CON HALOGENO, ARILO, HETEROARILO, ENTRE OTROS R3a ES HIDROXILO R3b ES H, HIDROXILO, HALO, CN, ENTRE OTROS R4 Y R5 SON CADA UNO H O ALQUILO(C1-C3) X ES ARILO(C6-C10) O HETEROARILO(C5-C9) SUSTITUIDO CON R2a Y R2b, EN DONDE R2a ES H, ALQUILO(C1-C3), HALO, CN, ENTRE OTROS R2b ES H, ALQUILO(C1-C3), HALO, HALOALQUILO(C1-C3). SON COMPUESTOS
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