PE20141686A1 - Compuestos de piperazina alquilados como inhibidores de actividad btk - Google Patents

Compuestos de piperazina alquilados como inhibidores de actividad btk

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Publication number
PE20141686A1
PE20141686A1 PE2014000639A PE2014000639A PE20141686A1 PE 20141686 A1 PE20141686 A1 PE 20141686A1 PE 2014000639 A PE2014000639 A PE 2014000639A PE 2014000639 A PE2014000639 A PE 2014000639A PE 20141686 A1 PE20141686 A1 PE 20141686A1
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PE
Peru
Prior art keywords
methyl
rented
btk activity
piperazine compounds
activity inhibitors
Prior art date
Application number
PE2014000639A
Other languages
English (en)
Inventor
James John Crawford
Wendy B Young
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20141686A1 publication Critical patent/PE20141686A1/es

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    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE: R1, R2 Y R3 SE SELECCIONAN INDEPENDIENTEMENTE DE H, F, CL, -NH2, ENTRE OTROS; R4 ES H, F, CL, CN, CICLOPROPILO, ENTRE OTROS; R5 ES -CH3, -CH2CH3, -CH2OH, ENTRE OTROS; R6 ES H, F, -CH3, ENTRE OTROS; R7 SE SELECCIONA DE A, ENTRE OTROS; R8 ES -CH3, -S(O)2CH3, CICLOPROPILO, ENTRE OTROS; X1 ES CR9 O N DONDE R9 ES H, F, CH3, ENTRE OTROS; X2 ES CR10 O N, DONDE R10 ES H, CH3, CH2CH3, ENTRE OTROS;Y1 Y Y2 SON INDEPENDIENTEMENTE ENTRE SI CH Y N. SON COMPUESTOS PREFERIDOS: (S)-2-(5-FLUORO-2-(HIDROXIMETIL)-3-(1-METIL-5-(5-(2-METIL-4-(OXETAN-3-IL)PIPERAZIN-1-IL)PIRIDIN-2-ILAMINO)-6-OXO-1,6-DIHIDROPIRIDIN-3-IL)FENIL)-3,4,6,7,8,9-HEXAHIDROPIRIDO[3,4-B]INDOLIZIN-1(2H)-ONA; (S)-5-[5-FLUORO-2-HIDROXIMETIL)-3-(1-METIL-5-(5-(2-METIL-4-(OXETAN-3-IL)PIPERAZIN-1-IL)PIRIDIN-2-ILAMINO)-6-OXO-1,6-DIHIDROPIRIDIN-3-IL)FENIL]-8-TIA-4,5-DIAZATRICICLO[7.4.0.02,7]TRIDECA-1(9),2(7),3-TRIEN-6-ONA. DICHO COMPUESTO ES UN INHIBIDOR DE BTK (TIROSIN QUINASA DE BRUTON). TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y METODOS PARA SU OBTENCION SIENDO UTIL EN EL TRATAMIENTO DE TRANSTORNOS INMUNES.
PE2014000639A 2011-11-03 2012-11-02 Compuestos de piperazina alquilados como inhibidores de actividad btk PE20141686A1 (es)

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US201161555395P 2011-11-03 2011-11-03

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US (3) US8729072B2 (es)
EP (1) EP2773639B1 (es)
JP (2) JP5976828B2 (es)
KR (1) KR101716011B1 (es)
CN (1) CN104024255B (es)
AR (1) AR088642A1 (es)
AU (1) AU2012332368A1 (es)
BR (1) BR112014010439A2 (es)
CA (1) CA2853970A1 (es)
CL (1) CL2014001158A1 (es)
CO (1) CO6950475A2 (es)
CR (1) CR20140187A (es)
EA (1) EA027561B1 (es)
IL (1) IL232280A0 (es)
IN (1) IN2014CN03265A (es)
MA (1) MA35725B1 (es)
MX (1) MX2014005289A (es)
PE (1) PE20141686A1 (es)
SG (1) SG11201401993RA (es)
TW (1) TW201326171A (es)
WO (1) WO2013067277A1 (es)
ZA (1) ZA201403158B (es)

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