Pirido - pyrimidine Derivatives of tetrahydro -, a Pharmaceutical composition based on the compound and a process for its preparation

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专利权人:

NOVARTIS AG

发明人:

申请号：

ARP110102390

公开号：

AR084970A1

申请日:

2011.07.04

申请国别(地区):

AR

年份:

2013

代理人:

摘要：

These compounds are suitable for treating a disorder or disease that is mediated by the Enzyme activity of PI3K, and Autoimmune disorders.Inflammatory and allergic diseases.Claim 1: a Derivative of pirido - tetrahydro - pyrimidine of formula (1),And / or taut u00f3meros and / or N - Oxides and / or pharmaceutically acceptable salts thereof； wherein: and select from or or NR1； r1 is selected from piridilo, pirimidinilo, phenylPirazinilo, piridazinilo, 1,2,3 - triazinilo, 1,2,4 - triazinilo triazinilo 1,3,5, -, or - C (o) - Where: R4 R4 is selected from alkyl of C1 - 8 8 -, Halo - C1 alkyl, Hydroxy alkyl C1 - 8Alkoxyl alkyl C1 C1 - 8 - 8 - 8 - C1 alkyl sulfonyl alkyl C1 - 8, heterociclilo, heterocicliloxilo heterociclil alkyl, cycloalkyl C1 - C3 - 12 8, 12 alkyl, cycloalkyl C1 - C3 - heteroaryl, 8Heteroariloxilo heteroaryl alkyl, hydroxyl, alkoxyl - 8 C1, C1 - 8 n - alkyl, amino, C1 - 8 or - amino - n, N - alkyl of C1 - 8 - amino alkyl, where C1 C1 - 8 - 8 - N - alkyl Amine and N,Di - N - alkyl amino C1 - 8 - can be replaced by insustituido or Halogen, alkoxyl, hydroxyl, or C1 - 4； where cycloalkyl C3 C3 - 12 - 12 in cycloalkyl alkyl and cycloalkyl C1 - C3 - 12 8Insustituido or can be replaced by 1 to 5 substituents selected independently from oxo Halogen, alkyl, Halo - C1 - 8 - 8 - hydroxy alkyl C1, C1 hydroxyl, alkyl - 8C1 - 8 alkoxyl alkyl, alkoxyl C1 C1 - 8 - 8 - N - alkyl, amino, C1 - 8 - amino - n, N - alkyl of C1 - 8 - 8 - C1 - amino alkyl carbonyl alkyl, Halo - C1 - 8 - carbonylC1 - 8 - hydroxy alkyl carbonyl alkyl or alkoxyl C1 C1 - 8 - 8 - carbonyl； where heterociclilo is selected from oxiranilo, AZIRIDINYL, oxetanilo, tietanilo, acetitinilo, pirrolidinilo,Furanilo tetrahydro - tetrahydro -, tiofenilo, 2,3 dihydro - furanilo, 2.5 - dihydro - furanilo, 2,3 dihydro - 1 - tiofenilo, pirrolinilo pirrolinilo, 2 -, 3 - pirrolinilo piranilo, tetrahydro -, piperidinilo,Tiopiranilo morfolinilo, tetrahydro -, tiomorfolinilo, piperazinilo, azepanilo,Tiepanilo or oxe

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