ES2527467T3 - Nuevas bencenosulfonamidas como bloqueantes de canales de calcio - Google Patents

Nuevas bencenosulfonamidas como bloqueantes de canales de calcio Download PDF

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ES2527467T3
ES2527467T3 ES10701070.4T ES10701070T ES2527467T3 ES 2527467 T3 ES2527467 T3 ES 2527467T3 ES 10701070 T ES10701070 T ES 10701070T ES 2527467 T3 ES2527467 T3 ES 2527467T3
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alkyl
nrc
heteroaryl
aryl
alkoxy
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Qingwei Zhang
Andrew O. Stewart
Zhiren Xia
Michael F. Jarvis
Victoria E. SCOTT
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AbbVie Bahamas Ltd
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Abstract

Un compuesto de fórmula (I) o (II),**Fórmula** o una sal farmacéuticamente aceptable del mismo, donde R1 es X y R2 es Y; X es (i) o (ii): m y n, en cada caso, son independientemente 1 o 2; G1 es azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tiomorfolinilo o azepanilo, donde G1 está conectado a través del átomo de nitrógeno de dicho azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tiomorfolinilo o azepanilo; Y es -NRcAr1, -NRcAr2-Ar1, -NRcCH(Ar1)2, -NRc(CRaRb)pAr1, -NRc(CRaRb)pCH(Ar1)2, -NRc-G2, -NRc-G2-Ar1, (iii), (iv), (v) o (vi): Ar1, en cada caso, es independientemente arilo o heteroarilo, donde dicho arilo y heteroarilo están sin sustituir o sustituidos con 1, 2, 3 o 4 o 5 sustituyentes seleccionados entre alcoxi, alquilo, ciano, haloalquilo, halógeno o -N(alquilo)2; Ar2 es arilo o heteroarilo, donde dicho arilo y heteroarilo están sin sustituir o sustituidos con 1, 2, 3 o 4 sustituyentes seleccionados entre alcoxi, alquilo, ciano, haloalquilo o halógeno; G2 es cicloalquilo; Ra y Rb son en cada caso independientemente hidrógeno, alquilo o hidroxialquilo; Rc es hidrógeno o alquilo; p es 1, 2, 3 o 4; y R3, R4, R5 y R6 son cada uno independientemente hidrógeno, alcoxi, alquilo o halógeno.

Description

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E10701070
07-01-2015
concentraciones en aumento de antagonista a las células individuales en un formato de multi-adición con 5 minutos en cada concentración de prueba. Para cada célula, las respuestas se normalizaron a control de vehículo de dimetil sulfóxido para generar curvas de respuesta a concentración.
La Tabla 1 lista los valores de CI50 para los compuestos 1-49, 57-59, 61-64, 66, 67, 70 y 74 de la presente invención; los demás compuestos en la tabla no forman parte de la presente invención.
Tabla 1. Determinación electrofisiológica para canales Cav3.2 humanos
Ejemplo
Calificador CI50 (μM) de Cav3.2 humana -77 mV GeoMean Ejemplo Calificador CI50 (μM) de Cav3.2 humana -77 mV GeoMean
1
> 10 43 4,9
2
10,6 44 4,9
3
5,9 45 > 10
4
7,7 46 1,8
5
1,8 47 3,8
6
1,9 48 > 10
7
6,5 49 1,3
8
2,1 50 0,6
9
7,3 51 0,9
10
1,5 52 0,6
11
6,6 53 0,5
12
4,7 54 1,2
13
5,6 55 1,8
14
3,7 56 4,1
15
> 10 57 48
16
6,0 58 4,6
17
> 10 59 9,0
18
9,3 60 5,0
19
2,4 61 > 10
20
6 62 > 10
21
5,9 63 > 10
22
1,4 64 1,7
23
2,5 65 1,84
24
1,0 66 5,9
25
8,9 67 3,18
26
1,5 68 10,9
27
> 10 69 > 10
28
1,9 70 7,2
29
2,1 71 10
30
1,8 72 > 10
31
3,3 73 1,8
32
8,4 74 2
33
5,7 75 6,5
34
6,2 76 6,4
35
4,8 77 > 10
36
4,7 78 > 10
37
1,1 79 8,5
38
4,6 80 2
39
4,1 81 > 10
40
4,1 82 2,6
41
5,0 83 > 10
42
5,8
15
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Claims (1)

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ES10701070.4T 2009-01-15 2010-01-14 Nuevas bencenosulfonamidas como bloqueantes de canales de calcio Active ES2527467T3 (es)

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US14489909P 2009-01-15 2009-01-15
US144899P 2009-01-15
PCT/US2010/020964 WO2010083264A1 (en) 2009-01-15 2010-01-14 Novel benzenesulfonamides as calcium channel blockers

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ES2527467T3 true ES2527467T3 (es) 2015-01-26

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EP (1) EP2382191B1 (es)
JP (1) JP5619773B2 (es)
KR (1) KR20110110299A (es)
CN (1) CN102282131B (es)
AR (1) AR077440A1 (es)
AU (1) AU2010204753A1 (es)
BR (1) BRPI1005675A2 (es)
CA (1) CA2747752A1 (es)
CL (1) CL2011001714A1 (es)
CO (1) CO6400194A2 (es)
DO (1) DOP2011000217A (es)
ES (1) ES2527467T3 (es)
IL (1) IL213500A0 (es)
MX (1) MX337190B (es)
PE (1) PE20120126A1 (es)
RU (1) RU2011134052A (es)
SG (1) SG172308A1 (es)
TW (1) TW201028421A (es)
UY (1) UY32384A (es)
WO (1) WO2010083264A1 (es)
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JP5501226B2 (ja) 2008-04-24 2014-05-21 Msd株式会社 アリールスルホニル誘導体を有効成分とする長鎖脂肪酸伸長酵素阻害剤
TW201028421A (en) * 2009-01-15 2010-08-01 Abbott Lab Novel benzenesulfonamides as calcium channel blockers
KR20140091522A (ko) * 2011-09-15 2014-07-21 타이페이 메디컬 유니이버시티 심부전증 또는 신경 손상을 치료하기 위한 인돌릴 및 인돌리닐 하이드록사메이트의 용도
US8648074B2 (en) 2011-09-29 2014-02-11 Abbvie Inc. Substituted octahydropyrrolo[1,2-a]pyrazine sulfonamides as calcium channel blockers
US8669255B2 (en) 2011-09-29 2014-03-11 Abbvie Inc. Substituted octahydropyrrolo[1,2-a]pyrazines as calcium channel blockers
WO2013103867A1 (en) 2012-01-05 2013-07-11 Abbvie Inc. Benzenesulfonamide derivative for use in the treatment of diabetic neuropathy
MX2015007460A (es) 2012-12-12 2015-09-04 Abbvie Inc Agentes para el tratamiento del dolor y usos de los mismos.
CN105873913B (zh) * 2013-09-10 2019-12-03 得克萨斯系统大学评议会 靶向截短的腺瘤性结肠息肉(apc)蛋白的治疗法
US9700549B2 (en) 2013-10-03 2017-07-11 David Wise Compositions and methods for treating pelvic pain and other conditions
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