AR061083A1 - Derivados de cicloalquilaminoacidos y composiciones farmaceuticas que los contienen - Google Patents

Derivados de cicloalquilaminoacidos y composiciones farmaceuticas que los contienen

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Publication number
AR061083A1
AR061083A1 ARP070102020A ARP070102020A AR061083A1 AR 061083 A1 AR061083 A1 AR 061083A1 AR P070102020 A ARP070102020 A AR P070102020A AR P070102020 A ARP070102020 A AR P070102020A AR 061083 A1 AR061083 A1 AR 061083A1
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Argentina
Prior art keywords
alkyl
group
heteroaryl
cycloalkyl
heterocyclyl
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ARP070102020A
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English (en)
Inventor
Samit K Bhattacharya
Peter H Dorff
Matthew Brown
Greca Susan D La
Robert J Maguire
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Pfizer Prod Inc
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Publication of AR061083A1 publication Critical patent/AR061083A1/es

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Abstract

Se refiere a compuestos de Formula 1 y a sales farmacéuticamente aceptables, profármacos, solvatos o hidratos de los mismos. También se refiere a un método de uso de tales compuestos en el tratamiento de enfermedades hiperproliferativas y enfermedades autoinmunes de mamíferos, especialmente en seres humanos, y a composiciones farmacéuticas que contienen tales compuestos. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, en la que B se selecciona entre el grupo que consiste en fenilo y un anillo heteroarilo (de 5 a 6 miembros); D se selecciona entre el grupo que consiste en fenilo y un anillo heteroarilo (de 5 a 6 miembros); E se selecciona entre el grupo que consiste en fenilo y un anillo heteroarilo (de 5 a 6 miembros); R1 es un radical seleccionado entre el grupo que consiste en hidrogeno, alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)-, heteroaril (C1-12)-, R7- SO2-, , R7-C(O)-, R7O-C(O)- y (R7)2N-C(O)-; donde cada uno de dichos radicales alquil (C1-6)-, alquenil C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)-, heteroaril (C1-12)-, R7-SO2-, R7-C(O)-, R7O-C(O)- y (R7)2N- C(O)-R1 puede estar opcionalmente sustituido con uno a tres restos seleccionados independientemente entre el grupo que consiste en hidrogeno, hidroxi, halogeno, -CN, alquil (C1-6)-, alcoxi (C1-6)-, perhaloalquil (C1-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)- y heteroaril (C1-12)-; cada R2 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, hidroxi, halogeno, -CN, alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3- 7)-, heterociclil (C2-9)-, aril (C6-10)- y heteroaril (C1-12)-; donde cada uno de dichos radicales alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)- y heteroaril (C1-12)- R2 puede estar opcionalmente sustituido con uno a tres restos seleccionados independientemente entre el grupo que consiste en hidrogeno, hidroxi, halogeno, -CN, alquil (C1-6)-, perhaloalquil (C1-4)-, perhaloalcoxi (C1-4)-, cicloalquil (C3-7)-, heterociclil (C2-9)- , aril (C6-10)- y heteroaril (C1-12)-; cada r3 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, halogeno, hidroxi, -CN, alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, alcoxi (C1-6)-, perhaloalquil (C1-6)- y perhaloalcoxi (C1-6)-; cada R4 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, halogeno, hidroxi, -CN, -N(R6)2, alquil (C1-6)-, alquenil (C2-6)-, alquinil (C3-6)-, alcoxi (C1-6)-, perhaloalquil (C1-6)-, alquil (C1-6)-S(O)k-, R10C(O)N(R10)-, (R10)2NC(O)-, R10C(O)-, R10OC(O)-, (R10)2NC(O)N(R10)-, (R10)2NS(O)-, (R10)2NS(O)2-, cicloalquil (C3-7)-, aril (C6-10)-, heterociclil (C2-9)- y heteroaril (C1-12)-; donde cada uno de dichos radicales alquil (C1-6)-, alquenil (C2-6)-, alquinil (C3-6)-, alcoxi (C1-6)-, alquil (C1-6)-S(O)k-, R10C(O)N(R10)-, (R10)2NC(O)-, R10C(O)-, R10OC(O)-, (R10)2NC(O)N(R10)-, (R10)2NS(O)-, (R10)2NS(O)2-, cicloalquil(C3-7)-, aril (C6-10)-, heterociclil (C2-9)- y heteroaril (C1-12)-R4 puede estar opcionalmente sustituido con uno a cinco restos seleccionados independientemente entre el grupo que consiste en halogeno, hidroxi, -CN, alquil (C1-6)-, cicloalquil (C3-7)-, alcoxi (C1-6)- y perhaloalcoxi (C1-6)-; R5 es un radical seleccionado entre el grupo que consiste en hidrogeno, halogeno, -CN, alquil (C1-10)-, alcoxi (C1-6)-, alquenil (C2-10)-, alquinil (C2-10)-, cicloalquil (C3-7)-, aril (C6-10)-, heterociclil (C2-9)-, heteroaril (C1-12)-, cicloalquil (C3-7)-O-, aril (C6-10)-O-, heterociclil (C2-9)-O-, heteroaril (C1-12)-O-, R7-S-, R7-SO-, R7-SO2-, R7-C(O)-, R7-C(O)-O-, R7O-C(O)- y (R7)2N-C(O)-; donde cada uno de dichos radicales alquil (C1-10)-, alcoxi (C1-6)- y alquinil (C2-10)-R5 puede estar opcionalmente sustituido con uno a cinco restos seleccionados independientemente entre el grupo que consiste en halogeno, hidroxi, -CN, alquil (C1-6), cicloalquil (C3-7)-, aril (C6-10)-, alcoxi (C1-6)-, heterociclil (C2-9)- y heteroaril (C1-12)-; donde cada uno de dichos radicales cicloalquil (C3-7)- y cicloalquil (C3-7)-O-R5 puede estar opcionalmente sustituido con uno a cinco restos seleccionados independientemente entre el grupo que consiste en halogeno, hidroxi, -CN, alquil (C1- 6)-, aril (C6-10)-, alcoxi (C1-6)-, heterociclil (C2-9)- y heteroaril (C1-12)-; donde cada uno de dichos radicales aril (C6-10)-, heterociclil (C2-9)-, heteroaril (C1-12)-, aril (C6-10)-O-, heterociclil (C2-9)-O- y heteroaril (C1-12)-O-R5 puede estar opcionalmente sustituido con uno a cinco restos seleccionados independientemente entre el grupo que consiste en halogeno, hidroxi, -CN, alquil (C1-6)- y alcoxi (C1-6)-; donde cada uno de dichos radicales R7-S-, R7-SO-, R7-SO2-, R7-C(O)-, R7- C(O)-O-, R7O-C(O)- y (R7)2N-C(O)-R5 puede estar opcionalmente sustituido con uno a cinco restos seleccionados independientemente entre el grupo que consiste en halogeno, hidroxi, -CN, alquil (C1-6)-, cicloalquil (C3-7)- y alcoxi (C1-6)-; donde cada uno de los restos alquil (C1-6)-, alcoxi (C1-6)-, aril (C6-10)-, alcoxi (C1-6)-, heterociclil (C2-9)- y heteroaril (C1-12)- mencionados anteriormente para cada uno de los radicales R5 mencionados anteriormente puede estar opcionalmente sustituido con uno a cinco grupos halogeno; opcionalmente dicho radical R5 y un radical R4 o dos radicales R4 pueden tomarse junto con E para formar un anillo bicíclico condensado (de 8 a 10 miembros) que contiene opcionalmente de 1 a 4 heteroátomos seleccionados entre el grupo que consiste en O, S o N(R6); donde dicho anillo bicíclico condensado (de 8 a 10 miembros) está opcionalmente sustituido adicionalmente con uno a dos grupos oxo (=O); cada R6 en un enlace o un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, alquil (C1-6)-, -CN y perhaloalquil (C1-6)-; cada R7 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, -CN, alquil (C1-6)-, perhaloalquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)- y heteroaril (C1-12)-; cada R8 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, hidroxi, halogeno, -CN, -NH(R)), alquil (C1-6)-, perhaloalquil (C1-6)- y alcoxi (C1-6)-; donde cada uno de dichos radicales alquil (c1-6)- y alcoxi (c1-6)-R8 está opcionalmente sustituido con uno a cinco restos seleccionados entre el grupo que consiste en perhaloalquil (C1-6)-, - O(R9) y -N(R9)2; cada R9 es un radical seleccionado independientemente entre el grupo que consiste en hidrogeno, alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)-, heteroaril (C1-12)-, R7-S- , R7-SO-, R7-SO2-, R7-C(O)-, R7-C(O)-O-, R7O-C(O)- y (R7)2N-C(O)-; donde cada uno de dichos radicales alquil (C1-6)-, alquenil (C2-6)-, alquinil (C2-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)-, heteroaril (C1-12)-R9 está opcionalmente sustituido con uno a tres restos seleccionados independientementes entre el grupo que consiste en hidrogeno, hidroxi, halogeno, -CN, alquil (C1-6)-, alcoxi (C1-6)-, perhaloalquil (C1-6)-, cicloalquil (C3-7)-, heterociclil (C2-9)-, aril (C6-10)- y heteroaril (C1-12)-; cada R10 es un radical seleccionado entre el grupo que consiste en hidrogeno y alquil (C1-6)-; k es un numero entero de 0 a 2; cada uno de m y n es independientemente un numero entero de 0 a 3; p es un numero entero de 1 a 2; q es un numero entero de 0 a 2; y cada uno de r, s, t y u es independientemente un numero entero de 0 a 4.
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ZA200809002B (en) 2009-12-30
IL194954A0 (en) 2009-08-03
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US20100120794A1 (en) 2010-05-13
US20070270438A1 (en) 2007-11-22
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AU2007251282A1 (en) 2007-11-22
CA2651629A1 (en) 2007-11-22
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