AR044770A1 - Derivados de piridina como inhibidores de caspasa y sus usos - Google Patents

Derivados de piridina como inhibidores de caspasa y sus usos

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Publication number
AR044770A1
AR044770A1 ARP040101830A ARP040101830A AR044770A1 AR 044770 A1 AR044770 A1 AR 044770A1 AR P040101830 A ARP040101830 A AR P040101830A AR P040101830 A ARP040101830 A AR P040101830A AR 044770 A1 AR044770 A1 AR 044770A1
Authority
AR
Argentina
Prior art keywords
aliphatic
heterocyclyl
heteroaryl
aryl
cor7
Prior art date
Application number
ARP040101830A
Other languages
English (en)
Inventor
Guy Brenchley
Jean-Damien Charrier
Steven Durrant
Ronald Knegtel
Michael Mortimore
John Studley
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR044770A1 publication Critical patent/AR044770A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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Abstract

La presente provee composiciones farmacéuticas y métodos para utilizar dichas composiciones para el tratamiento de enfermedades mediadas por la caspasa y los procesos para preparar dichos compuestos. Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque: R1 es R6C(O)-, HC(O)-, R6SO2-, R6OC(O)-, (R6)2NC(O)-, (R6)(H)NC(O)-, R6C(O)C(O)-, R6-, (R6)2NC(O)C(O)-, (R6)(H)NC(O)C(O)-, o R6OC(O)C(O)-; R2 es hidrógeno, -CF3, halo, -OR7, -NO2, -OCF3, -CN, o R8; R3 es hidrógeno o alifático-(C1-4)-; R4 es -COOH o -COOR8; R5 es -CH2F o -CH2O-2,3,5,6-tetrafluorofenilo; R6 es alifático-(C1-12)-cicloalifático-(C3-10)-, arilo-(C6-10)-, heterociclilo-(C3-10)-, heteroarilo-(C5-10)-, cicloalifático-(C3-10)-alifático-(C1-12)-, aril-(C6-10)-alifático-(C1-12)-, heterociclil-(C3-10)-alifático-(C1-12)-, heteroaril-(C5-10)-alifático(C1-12)-, o dos grupos R6 enlazados al mismo átomo forman junto con dicho átomo un anillo aromático o no aromático de 3 a 10 miembros; donde el anillo está opcionalmente fusionado a arilo-(C6-10), heteroarilo-(C5-10), cicloalquilo-(C3-10), o heterociclilo-(C3-10); donde hasta 3 átomos de carbono alifáticos pueden ser reemplazados por un grupo seleccionado entre O, N(H), N(R), S, SO, y SO2; y donde R6 está sustituido con hasta 6 sustituyentes seleccionados de manera independiente de R; R es halógeno, -OR7, -OC(O)N(R7)2, -NO2, -CN, -CF3, -OCF3, -R7, oxo, =NR7, =N(OR7), tioxo, 1,2-metilendioxi, 1,2-etilendioxi, -N(R7)2, -SR7, -SOR7, -SO2R7, -SO2N(R7)2, -SO3R7, -C(O)R7, -C(O)C(O)R7, -C(O)C(O)OR7, -C(O)C(O)N(R7)2, -C(O)CH2C(O)R7, -C(S)R7, -C(S)OR7, -C(O)OR7, -OC(O)R7, -C(O)N(R7)2, -OC(O)N(R7)2, -C(S)N(R7)2, -(CH2)0-2NHC(O)R7, -N(R7)N(R7)COR7, -N(R7)N(R7)C(O)OR7, -N(R7)N(R7)CON(R7)2, -N(R7)SO2R7, -N(R7)SO2N(R7)2, -N(R7)C(O)OR7, -N(R7)C(O)R7, -N(R7)C(S)R7, -N(R7)C(O)N(R7)2, -N(R7)C(S)N(R7)2, -N(COR7)COR7, -N(OR7)R7, -C(=NH)N(R7)2, -C(O)N(OR7)R7, -C(=NOR7)R7, -OP(O)(OR7)2, -P(O)(R7)2, -P(O)(OR7)2, o -P(O)(H)(OR7); dos grupos R7 junto con los átomos a los cuales están enlazados forman un anillo aromático o no aromático de 3 a 10 miembros que tienen hasta 3 heteroátomos seleccionados independientemente entre N(H), N(R), O, S, SO, o SO2, donde el anillo está opcionalmente fusionado a arilo (C6-10), heteroarilo (C5-10), cicloalquilo (C3-10), o heterociclilo (C3-10), y donde cualquier anillo tiene hasta 3 sustituyentes seleccionados de manera independiente de J2; o cada R7 se selecciona, de manera independiente, de: hidrógeno-, alifático-(C1-12)-; cicloalifático-(C3-10)-; cicloalifático-(C3-10)-alifático-(C1-12)-; arilo-(C6-10)-; aril-(C6-10)-alifático-(C1-12)-; heterociclilo-(C3-10)-; heterociclil-(C6-10)-alifático-(C1-12)-; heteroarilo-(C5-10)-, o heteroaril-(C5-10)-alifático-(C1-12)-; donde R7 tiene hasta 3 sustituyentes seleccionados, de manera independiente, de J2; y J2 es halógeno, -OR7, -OC(O)N(R7)2, -NO2, -CN, -CF3, -OCF3, -R7, oxo, tioxo, =NR7, =NOR7, 1,2-metilendioxi, 1,2-etilendioxi, -N(R7)2, -SR7, -SOR7, -SO2R7, -SO2N(R7)2, -SO3R7, -C(O)R7, -C(O)C(O)R7, -C(O)C(O)OR7, -C(O)CH2C(O)R7, -C(S)R2, -C(S)OR7, -OC(O)R7, -C(O)N(R7)2, -OC(O)N(R7)2, -C(S)N(R7)2, -(CH2)0-2NHC(O)R7, -N(R7)N(R7)COR7, -N(R7)N(R7)C(O)OR7, -N(R7)N(R7)CON(R7)2, -N(R7)SO2R7, -N(R7)SO2N(R7)2, -N(R7)C(O)OR7, -N(R7)C(O)R7, -N(R7)C(S)R7, -N(R7)C(O)N(R7)2, -N(R7)C(S)N(R7)2, -N(COR7)COR7, -N(OR7)R7, -CN, -C(=NH)N(R7)2, -C(O)N(OR7)R7, -C(=NOR7)R7, -OP(O)(OR7)2, -P(O)(R7)2, -P(O)(OR7)2, o -P(O)(H)(OR7); y R8 es alifático-(C1-12)-cicloalifático (C3-10)-, (C6-10)-arilo-, heterociclilo-(C3-10)-, heteroarilo-(C5-10)-, cicloalifático-(C3-10)-alifático-(C1-12)-, aril-(C6-10)-alifático-(C1-12)-, heterociclil-(C3-10)-alifático-(C1-12), heteroaril-(C5-10)-alifático-(C1-12)-, donde hasta 3 átomos de carbono alifáticos pueden estar reemplazados con un grupo seleccionado entre O, N(H), N(R), S, SO, y SO2; y donde R8 está opcionalmente sustituido con hasta 6 sustituyentes seleccionados independientemente de R.
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