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Inhibitors of the tyrosine kinase Bruton
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
SAUL JAIME-FIGUEROA,YAN LOU,TIMOTHY D. OWENS,CHRISTINE BROTHERTON-PLEISS,FRANCISCO JAVIER LOPEZ-TAPIA
申请号:
ARP120102984
公开号:
AR087543A1
申请日:
2012.08.15
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
These compounds help regulate Btk activity and treat diseases related to Btk overactivity. These compounds also contribute to the treatment of inflammatory and autoimmune diseases, such as rheumatoid arthritis, associated with the abnormal spread of B cells. It also describes a compound containing formula (1) and at least one vehicle, diluent or precursor compound. 1. Claim 1: a formula compound (1),Where: - 8315; - 8315; - 8315; - 8315; - 8315; - 8315; is a simple or double link; each x is an independent ch, ch8322;CHX or N; X is the asphalt at the bottom; R is h, R1,-R1-R2-R3-R¹-R³ or -R²-R³;R1 is arilo, heteromorphic, bicyclic isoarilo, cyclopentyl, isocyclopropylene or bicyclic heterocycle, each of which can be selected from one or more of the following asphalts, hydroxyl, low hydroxyl, suboxidation, halogen, nitrogen, amine, cyanogen, oxo or halo groups; R2 es-c (= O),-C (3DO) O -C (3DO) NR-NHC (3DO) O -C (R)-O -S -C (3DNH) NR o -S (3DO)Each square kilometer is independent h or lower asphalt; R3 is h or r83088;R⁴ is lower alkyl, halo lower alkyl, lower alkoxy, amino, (lower alkyl) -amino, cycloalkylamino, di- (lower alkyl) -amino, aryl, arylalkyl, alkylaryl, heteroaryl, (lower alkyl) -heteroaryl, heteroaryl-lower alkyl , cycloalkyl, (lower alkyl) -cycloalkyl, cycloalkyl-lower alkyl, heterocycloalkyl, (lower alkyl) -heterocycloalkyl, heterocycloalkyl-lower alkyl, cycloalkyl bicyclic, heterocyclo-bicyclic alkyl, spirocycloalkyl, spiroheterocycloalkyl or (spiroheterocycloalkyl). each of which is optionally substituted by one or more lower alkyl, halogen, (lower alkyl) -amino,Bis - (lower pitch) - amino, hydrogen, hydroxy low pitch, low alkane, halogen, nitrogen, amino, acylamine, acylamine, acid, cyanogen, oxo, sulfuric acid (lower pitch) - sulfur, guandino, hydroxy amino, carboxi, carbamoi, carbamato, haloxysub, isocyclopentyl or lower halogen; a. Ey1 is ch or N, if there is at least one a, ey1 must be n; Y2 is ch or N; Y3 is h or F; ys is y8308; y is y749191;Y⁴ᵇ
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