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AR052903A1 - Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. - Google Patents

Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno.

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Publication number
AR052903A1
AR052903A1 ARP060100467A ARP060100467A AR052903A1 AR 052903 A1 AR052903 A1 AR 052903A1 AR P060100467 A ARP060100467 A AR P060100467A AR P060100467 A ARP060100467 A AR P060100467A AR 052903 A1 AR052903 A1 AR 052903A1
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Argentina
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alkyl
heterocycle
heteroaryl
integer
aryl
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ARP060100467A
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Aventis Pharma Inc
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Publication of AR052903A1 publication Critical patent/AR052903A1/es

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
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Abstract

Estos compuestos son antagonistas selectivos de 5HT2a y, por lo tanto, son utiles en el tratamiento de una diversidad de enfermedades que incluyen, pero sin limitacion, una amplia diversidad de trastornos del sueno. Reivindicacion 1:Un compuesto, incluyendo enantiomeros, esteroisomeros y tautomeros de dicho compuesto y sus sales, solvatos o derivados farmacéuticamente aceptables teniendo dicho compuesto la estructura general mostrada en la formula 1 donde X=Y se refiere a un enlace sencillo o a un doble enlace entre X e Y; X es CR, CHR, CO, N, O o S; Y es CR, CHR, CO, S(O)2, N o NR; Z es NR, CO-NR, S(O)2-NR; A,B y E son iguales o diferentes y son independientemente entre sí CR o N; D es CH2 o CO; Ar es arilo o heteroarilo sustituido o sin sustituir; cada R se selecciona independientemente entre hidrogeno, halogeno, CN, C(O)NR3R4, alquilo C1-4, alcoxi C1-4, alquenilo C1-4, arilo, heteroarilo,aril-alquilo(C1-4), heteroaril-alquilo C1-4, fluoroalquilo o fluoroalcoxi de formula CnHxFy o OCnHxFy donde n es un numero entero de 1 a 4, x es un numero entero de 0 a 8, y es un numero entero de 1 a 9 y la suma de x e y es 2n+1; donde R3 y R4 son hidrogeno o alquilo C1-4; o R3 y R4 tomados con el átomo de nitrogeno al que están unidos forman un heterociclo sin sustituir o al menos monosustituido; R1 yR2 son iguales o diferentes y se seleccionan independientemente entre sí entre arilo sustituido o sin sustituir, heteroarilo, ariloílo, heteroariloílo, arilsulfonilo, heteroarilsulfonilo, aril-alquilo C1-4, heteroaril-alquilo C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, cicloalquilamino C3-8-alquilo C1-4, di-cicloalquilamino C3-8-alquilo C1-4, cicloalquil C3-8-alquilamino C1-4-alquilo C1-4, di- alquilaminoalquilo C1-4, heterociclo, heterociclo-alquilo C1-4, alquilheterociclo C1-4-alquilo C1-4; o R1 y R2 tomados juntos con el átomo de nitrogeno al que están unidos forman un heterociclo sin sustituir o al menos monosustituido; y donde los sustituyentes se seleccionan entre el grupo que consiste en arilo sustituido o sin sustituir, heteroarilo, aril-alquilo C1-4, heteroaril-alquilo C1-4, heterociclo, cicloalquilo C3-8 , alquilo C1-4, alcoxi C1-4, alquenilo C1-4, fluoroalquilo o fluoroalcoxi de formula CnHxFy o OCnHxFy donde n es un numero entero de 1 a 4, x es un numero entero de 0 a 8, y es un numero entero de 1 a 9 y la suma de x e y es 2n+1, - NO2, -NH2, -NH(alquilo C1-4), N-(alquilo C1-4)2, -CN, -C(O)R5, -NH(0)(alquilo C1-4), -SO2Cl, -SO2(alquilo C1-4), halogeno e hidroxi; donde R5 es hidroxi, alcoxi C1-3, -O-fenilo, -NH2, -NH(alquiloC1-3), -N(alquilo C1-3)2 o fenilo; heteroarilo es un heterociclo mono- o bicíclico, aromático de 5 a 10 miembros, que contiene uno o más heteroátomos seleccionados del grupo que consiste en N, O y S; arilo es un anillo mono- o bicíclico aromático de 6 a 10 miembros y heterociclo es un heterociclo mono- o bicíclico, no aromático de 3 a 10 miembros, que contiene uno o más heteroátomos seleccionados del grupo que consiste en N, O y S.
ARP060100467A 2005-02-10 2006-10-09 Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. AR052903A1 (es)

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EP (1) EP1851199B1 (es)
JP (1) JP5419355B2 (es)
KR (1) KR20070107037A (es)
CN (1) CN101115717A (es)
AR (1) AR052903A1 (es)
AU (1) AU2006213634A1 (es)
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SA05260357B1 (ar) 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
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EP2001870A2 (en) 2006-03-31 2008-12-17 Schering Corporation Kinase inhibitors
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