AR076755A1 - Compuestos carboxamida y su uso como inhibidores de calpaina - Google Patents

Compuestos carboxamida y su uso como inhibidores de calpaina

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Publication number
AR076755A1
AR076755A1 ARP100101566A AR076755A1 AR 076755 A1 AR076755 A1 AR 076755A1 AR P100101566 A ARP100101566 A AR P100101566A AR 076755 A1 AR076755 A1 AR 076755A1
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Argentina
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alkyl
aryl
cycloalkyl
radicals
substituents
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Andreas Kling
Helmut Mack
Moeller
Jantos
Wilfried Hornberger
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Abbott Gmbh & Co Kg
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Application filed by Abbott Gmbh & Co Kg filed Critical Abbott Gmbh & Co Kg
Publication of AR076755A1 publication Critical patent/AR076755A1/es

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Abstract

Su uso para la fabricacion de un medicamento. Los compuestos carboxamida son inhibidores de calpaína (cisteína proteasas dependientes del calcio). Por lo tanto, la presente también se refiere al uso de dichos compuestos carboxamida para tratar un trastorno asociado con una alta actividad de calpaína. Reivindicacion 1: Un compuesto de carboxamida caracterizado porque es de la formula (1) en donde - - - - - indica una union simple o, si R4 se encuentra ausente, indica una union doble; R1 es hidrogeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, donde los ultimos 3 radiales mencionados pueden estar parcial o totalmente halogenados y/o tener 1, 2 o 3 sustituyentes R1a, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, donde un grupo CH2 en la porcion cicloalquilo de los ultimos dos radicales mencionados puede reemplazarse por O, NH, o S, o dos átomos de C adyacentes pueden formar una union doble, donde la porcion cicloalquilo además puede tener 1, 2, 3 o 4 radicales R1b, arilo, hetarilo, aril-alquilo C1-6, aril-alquenilo C2-6, hetaril-alquilo C1-4 o hetaril-alquenilo C2-6, donde los grupos arilo y hetarilo en los ultimos 6 radicales mencionados pueden no estar sustituidos o llevar 1, 2, 3 o 4 radicales R1c idénticos o diferentes; donde R1a se selecciona en forma independiente entre sí entre OH, SH, COOH, CN, OCH2COOH, alcoxi C1-6, haloalcoxi C1-6, cicloalquiloxi C3-7, alquiltio C1-6, haloalquiltio C1-6, COORa1, CONRa2Ra3, SO2NRa2Ra3, -NRa2SO2Ra4, NRa2-CO-Ra5, SO2-Ra4 y NRa6Ra7; R1b se selecciona en forma independiente entre si entre OH, SH, COOH, CN, OCH2COOH, halogeno, fenilo que tiene opcionalmente 1, 2 o 3 sustituyentes R1d, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, donde las porciones alquilo en los ultimos 3 sustituyentes mencionados pueden estar parcial o totalmente halogenadas y/o tener 1, 2 o 3 sustituyentes R1a, COORb1, CONRb2Rb3, SO2NRb2Rb3, NRb2-SO2-Rb4, NRb2-CO-Rb5, SO2-Rb4 y NRb6Rb7, además los radicales R1b pueden formar juntos un grupo alquileno C1-4, o 2 radicales R1b unidos a átomos de C de cicloalquilo adyacentes también pueden formar junto con los átomos de carbono a los cuales están unidos un anillo benceno; R1c se selecciona en forma independiente entre sí entre OH, SH, halogeno, NO2, NH2, CN, COOH, OCH2COOH, alquilo C1-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-4, alquiltio C1-6, donde las porciones alquilo en los ultimos 4 sustituyentes mencionados pueden estar parcial o totalmente halogenadas y/o tener 1, 2 o 3 sustituyentes R1a, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, cicloalquiloxi C3-7, donde la porcion cicloalquilo de los ultimos tres radicales mencionados puede tener 1, 2, 3 o 4 radicales R1b, y donde 1 o 2 grupos CH2 en la porcion cicloalquilo pueden reemplazarse por O, NH o S, arilo, hetarilo, O-arilo, O-CH2-arilo, donde los ultimos tres radicales mencionados no están sustituidos en la porcion arilo o pueden llevar 1, 2, 3 o 4 radicales R1d, COORc1, CONRc2Rc3, SO2NRc2Rc3, NRc2-SO2-Rc4, NRc2-CO-Rc5, SO2-Rc4, (CH2)pNRc6Rc7 con p = 0, 1, 2, 3, 4, 5 o 6 y O(CH2)q-NRc6Rc7 con q = 2, 3, 4, 5 o 6; donde Ra1, Rb1 y Rc1 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, Ra2, Rb2 y Rc2 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyente R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y Ra3, Rb3 y Rc3 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, o los dos radicales Ra2 y Ra3, o Rb2 y Rb3 o Rc2 y Rc3 forman junto con el átomo de N un heterociclo con nitrogeno opcionalmente sustituido de entre 3 y 7 miembros que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales iguales o diferentes seleccionados entre O, N, S como miembros del anillo, Ra4, Rb4 y Rc4 son en forma independiente entre sí alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y Ra5, Rb5 y Rc5 tienen en forma independiente entre sí uno de los significados mencionados para Ra1, Rb1 y Rc1, Ra6, Rb6 y Rc6 son en forma independiente entre sí H, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, CO-alquilo C1-6, CO-O-alquilo C1-6, SO2-alquilo C1-6, arilo, hetarilo, O-arilo, OCH2-arilo, aril-alquilo C1-4, hetaril-alquilo C1-4, CO-arilo, CO-hetarilo, CO-(aril-alquilo C1-4), CO-(hetaril-alquilo C1-4), CO-O-arilo, CO-O-hetarilo, CO-O-(aril-alquilo C1-4), CO-O-(hetaril-alquilo C1-4), SO2-arilo, SO2-hetarilo, SO2-(aril-alquilo C1-4) o SO2-(hetaril-alquilo C1-4), donde los grupos arilo y hetarilo en los ultimos 18 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y Ra7, Rb7 y Rc7 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, o los dos radicales Ra6 y Ra7, o Rb6 y Rb7 o Rc6 y Rc7 forman junto con el átomo de N un heterociclo con nitrogeno opcionalmente sustituido de entre 3 y 7 miembros que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales iguales o diferentes seleccionados entre O, N y S como miembros del anillo, o dos radicales R1b o R1c unidos a átomos de C adyacentes forman junto con los átomos de C a los cuales están unidos un carbociclo opcionalmente sustituido de 4, 5, 6 o 7 miembros o un heterociclo opcionalmente sustituido que tiene 1, 2 o 3 heteroátomos iguales o diferentes seleccionados entre O, N y S como miembros del anillo; R1d se selecciona entre halogeno, OH, SH, NO2, COOH, C(O)NH2, CHO, CN, NH2, OCH2COOH, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquiltio C1-6, haloalquiltio C1-6, CO-alquilo C1-6, CO-O-alquilo C1-6, NH-alquilo C1-6, NHCHO, NH-C(O)alquilo C1-6, y SO2-alquilo C1-6 o dos radicales R1d unidos a átomos de carbono adyacentes pueden formar juntos una porcion -O-Alk''-O-, donde Alk'' es alcandiilo C1-2 lineal, que no está sustituido o donde 1 o 2 átomos de hidrogeno pueden reemplazarse por fluor, cloro o metilo; R2 es cicloalquilo C3-7, donde un grupo CH2 en la porcion cicloalquilo puede reemplazarse por O, NH, o S, o dos átomos de C adyacentes pueden formar una union doble, donde la porcion cicloalquilo puede tener adicionalmente 1, 2, 3 o 4 radicales Ra2, arilo, o hetarilo, donde los grupos arilo y hetarilo pueden no estar sustituidos o llevar 1, 2, 3 o 4 radicales R2b iguales o diferentes, donde R2a tiene uno de los significados indicados para R1b, y R2b tiene uno de los significados indicados para R1c; R3a y R3b son en forma independiente entre sí hidroxi o alcoxi C1-4, o junto con el átomo de carbono al cual están unidos son C=O o C=NR3; o R3a y R3b juntos forman una porcion S-Alk-S, O-Alk-S o O-Alk-O, donde Alk es alcandiilo C2-5 lineal, que puede no estar sustituido o estar sustituido con 1, 2, 3 o 4 radicales seleccionados entre alquilo C1-4 o halogeno; R3 es H, alquilo C1-6, alcoxi C1-6, alquenilo C2-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-4, alqueniloxi C2-6, cicloalquiloxi C3-6 o cicloalquil C3-6-alquiloxi C1-4; R4 se encuentra ausente o indica hidrogeno; A es C=O, S(=O) o S(=O)2; Q es una union simple o una porcion Alk'-Z, donde Z está unido a R2 y se selecciona entre una union simple, O, S, S(=O), S(=O)2 y NRq, donde Rq se selecciona entre hidrogeno, alquilo C1-4 y haloalquilo C1-4; Alk' es alcandiilo C1-3 lineal, donde 1, 2 o 3 átomos de hidrogeno pueden reemplazarse por alquilo C1-4, haloalquilo C1-4 o halogeno; X es hidrogeno o un radical de las formulas C(=O)-O-Rx1, C(=O)-NRx2Rx3, C(=O)-N(Rx4)-alquilen C1-6-NRx2Rx3 o C(=O)N(Rx4)NRx2Rx3, en donde Rx1 es hidrogeno, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes Rxa, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, donde los grupos alquilo, alquenilo, alcoxi, alquinilo, cicloalquilo, heterocicloalquilo en los ultimos 6 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes Rxa, o arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no
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