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AR059037A1 - Compuestos para el tratamiento de trastornos inflamatorios - Google Patents

Compuestos para el tratamiento de trastornos inflamatorios

Info

Publication number
AR059037A1
AR059037A1 ARP070100164A ARP070100164A AR059037A1 AR 059037 A1 AR059037 A1 AR 059037A1 AR P070100164 A ARP070100164 A AR P070100164A AR P070100164 A ARP070100164 A AR P070100164A AR 059037 A1 AR059037 A1 AR 059037A1
Authority
AR
Argentina
Prior art keywords
aryl
heteroaryl
heterocyclyl
alkyl
cycloalkyl
Prior art date
Application number
ARP070100164A
Other languages
English (en)
Original Assignee
Schering Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38038495&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR059037(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR059037A1 publication Critical patent/AR059037A1/es

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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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Abstract

Estos compuestos pueden ser utiles para el tratamiento de enfermedades o afecciones mediadas por las MMP, ADAM, TACE, agrecanasa, TNF-a o combinaciones de las mismas. Reivindicacion 1: Un compuesto representado por la formula (1), o una de sus sales, solvatos, o ésteres aceptables para uso farmacéutico, donde: el anillo A se selecciona del grupo que consiste en arilo y heteroarilo, estando cada uno ellos substituido con -Y-R1 y -Z-R2 como se muestra; X se selecciona del grupo que consiste en of -S-, -O-, -S(O)2-, S(O)-, -(C(R3)2)m- y -N(R3)-; T está ausente o presente y, si está presente se selecciona del grupo que consiste en alquilo; arilo y heteroarilo, en donde cuando cada uno de dichos T arilo y heteroarilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden opcionalmente tomarse junto con los átomos de carbono a los cuales están unidos para formar un anillo arilo o heteroarilo de cinco a ocho miembros, en donde cada uno de los antes mencionados T arilo y heteroarilo, opcionalmente con dicho arilo o heteroarilo de cinco a ocho miembros está independientemente no substitutido o substituido con uno a cuatro restos R10 que pueden ser iguales o diferentes; U está ausente o presente y, si está presente se selecciona del grupo que consiste en -O-, -O-C(O)NH-, -OC(O)N(alquilo)-, -C(O)-, -C(O)O-, -C(O)NH-, -C(O)N(alquilo)-, -C(=N-OH)-alquilo-, y -C(=N-O-alquil)-alquilo-; V está ausente o presente y, si está presente, V se selecciona del grupo que consiste en alquilo, alquinilo, cicloalquilo, heterociclilo, arilo, heteroarilo y N-oxidos de dicho heterociclilo y heteroarilo, en donde cuando cada uno de dichos V cicloalquilo, heterociclilo, arilo, heteroarilo y N-oxidos de dicho heterociclilo y heteroarilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden estar opcionalmente tomados conjuntamente con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros, donde cada uno de dichos V alquilo, alquinilo, cicloalquilo, heterociclilo, arilo, heteroarilo y heterociclilo, opcionalmente con dichos cicloalquilo, arilo, heterociclilo, o heteroarilo de cinco a ocho miembros independientemente no substitutido o substituido con uno a cuatro restos R10 que pueden ser iguales o diferentes; Y se selecciona del grupo que consiste en una union covalente, -(C(R4)2)n-, -N(R4)-, -C(O)N(R4)-, -N(R4)C(O)-, -N(R4)C(O)N(R4)-, -S(O)2N(R4)-, -N(R4)-S(O)2-, -O-, -S-, -C(O)-, -S(O)-, y -S(O)2-; Z se selecciona del grupo que consiste en una union covalente, -(C(R4)2)n-, -N(R4)-, -C(O)N(R4)-, -N(R4)C(O)-, -N(R4)C(O)N(R4)-, -S(O)2N(R4)-, -N(R4)-S(O)2-, -O-, -S- , -C(O)-, -S(O)-, y -S(O)2-; m es 1 a 3: n es 1 a 3; R1 está seleccionado del grupo que consiste en H, ciano, -C(O)OH, -C(O)O-alquilo, -C(O)NH2, -C(O)NH(alquilo), -C(O)N(alquilo)2, -alquinilo, halogeno, alquilo, cicloalquilo, haloalquilo, arilo, heteroarilo, y heterociclilo, en donde cuando cada uno de dichos cicloalquilo, heterociclilo, arilo y heteroarilo contienen dos radicales en átomos de carbono adyacentes, dichos radicales pueden estar opcionalmente tomados conjuntamente con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros; donde cada uno de los R1 alquilo, alquinilo, arilo, heteroarilo, y heterociclilo, opcionalmente con el anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco o seis miembros no substitutido o en forma opcional está substituido independientemente con uno a cuatro restos R20 los cuales pueden ser iguales o diferentes; con la salvedad de que cuando Y es -N(R4)-, -S- o -O-, entonces R1 no es halogeno o ciano; R2 se selecciona del grupo que consiste en H, ciano, -C(O)OH, -C(O)O-alquilo, -C(O)NH2, -C(O)NH(alquilo), -C(O)N(alquilo)2, alquinilo, halogeno, alquilo, cicloalquilo, haloalquilo, arilo, heteroarilo, y heterociclilo, donde cuando cada uno de dichos cicloalquilo, heterociclilo, arilo y heteroarilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden opcionalmente tomarse junto con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros; en donde cada uno de los R2 alquilo, cicloalquilo, arilo, heteroarilo, y heterociclilo, en forma opcional con el anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a seis miembros no substitutido o en forma opcional está substituido independientemente con uno a cuatro restos R20 que pueden ser iguales o diferentes; con la salvedad de que cuando Y es -N(R4)-, -S- o -O-, entonces R2 no es halogeno o ciano; cada R3 es igual o diferente y seleccionado en forma independiente del grupo que consiste en H, alquilo, y arilo; cada R4 es igual o diferente y seleccionado en forma independiente del grupo que consiste en H, alquilo, cicloalquilo, haloalquilo, hidroxi, -alquilcicloalquilo, -alquil-N(alquil)2, heterociclilo, arilo, y heteroarilo en donde cuando cada uno de dichos cicloalquilo, heterociclilo, arilo, y heteroarilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden opcionalmente tomarse junto con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros; R10 se selecciona del grupo que consiste en hidrogeno, ciano, nitro, -C(R4)=N-OR4, -OR4, -SR4, -N(R4)2, -S(O)R4, -S(O)2R4, -N(R4)S(O)2R4, -N(R4)-C(O)-R4, -N(R4)-C(O)-N(R4)2, -N(R4)-C(O)-OR4, -OC(O)N(R4)2, -C(O)N(R4)-S(O)2R4, -S(O)2N(R4)-C(O)-R4, - C(O)N(R4)C(O)R4, -C(O)N(R4)C(O)NR4, -S(O)2N(R4)2, -N(R4)-C(=NR4)-N(R4)2, -N(R4)-C(=N-CN)-N(R4)2, -haloalcoxi, -C(O)OR4, -C(O)R4, -C(O)N(R4)2, halogeno, alquilo, haloalquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo, donde cada uno alquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo, en donde cada uno de los R10 alquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo no está substitutido o en forma opcional está substituido independientemente con uno a cuatro restos R30 que pueden ser iguales o diferentes; o donde dos restos R10, cuando están unidos al mismo átomo de carbono o átomos de carbono adyacentes pueden en forma opcional tomarse junto con el/los átomo(s) de carbono a los cuales están unidos para formar un anillo cicloalquilo, cicloalquenilo, heterociclilo, arilo, o heteroarilo; R20 se selecciona del grupo que consiste en of ciano, nitro, -C(R4)=N-OR4, -OR4, -SR4, -N(R4)2, -S(O)R4, -S(O)2R4, -N(R4)S(O)2R4, -N(R4)-C(O)-R4, -N(R4)-C(O)-N(R4)2, -N(R4)- C(O)-OR4, -OC(O)N(R4)2, -C(O)N(R4)-S(O)2R4, -S(O)2N(R4)-C(O)-R4, -C(O)N(R4)C(O)R4, -C(O)N(R4)C(O)NR4, -S(O)2N(R4)2, -N(R4)-C(=NR4)-N(R4)2, -N(R4)-C(=N-CN)-N(R4)2, -haloalcoxi, -C(O)OR4, -C(O)R4, -C(O)N(R4)2, halogeno, alquilo, haloalquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo; en donde cuando cada uno de dichos R20 arilo, heteroarilo, heterociclilo y cicloalquilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden opcionalmente tomarse junto con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros; en donde cada uno dichos R20 alquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo, en forma opcional con dicho anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros no substitutido o está substituido con uno a cuatro restos seleccionados independientemente del grupo que consiste en alquilo, halo, haloalquilo, hidroxi, alcoxi, haloalcoxi, hidroxialquilo, ciano, nitro, -NH2, -NH(alquil), y -N(alquil)2; o cuando dos restos R20 cuando están unidos al mismo átomo de carbono o átomos de carbono adyacentes pueden tomarse opcionalmente en forma conjunta con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, cicloalquenilo, heterociclilo, arilo, o heteroarilo; R30 se selecciona del grupo que consiste en of ciano, nitro, -C(R4)=N-OR4, -OR4, -SR4, -N(R4)2, -S(O)R4, -S(O)2R4, - N(R4)S(O)2R4, -N(R4)-C(O)-R4, -N(R4)-C(O)-N(R4)2, -N(R4)-C(O)-OR4, -OC(O)N(R4)2, -C(O)N(R4)-S(O)2R4, -S(O)2N(R4)-C(O)-R4, -C(O)N(R4)C(O)R4, -C(O)N(R4)C(O)NR4, -S(O)2N(R4)2, -N(R4)-C(=NR4)-N(R4)2, -N(R4)-C(=N-CN)-N(R4)2, -haloalcoxi, -C(O)OR4, - C(O)R4, -C(O)N(R4)2, halogeno, alquilo, haloalquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo; en donde cuando cada uno de dichos R30 arilo, heteroarilo, heterociclilo y cicloalquilo contiene dos radicales en átomos de carbono adyacentes, dichos radicales pueden opcionalmente tomarse junto con los átomos de carbono a los cuales están unidos para formar un anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros; en donde cada uno dichos R30 alquilo, arilo, heteroarilo, heterociclilo, y cicloalquilo, en forma opcional con dicho anillo cicloalquilo, arilo, heterociclilo o heteroarilo de cinco a ocho miembros no está substitutido o está substituido con uno a cuatro restos seleccionados independientemente del grupo que consiste en alquilo, halo, haloalquilo, hidroxi, alcoxi, haloalcoxi, ciano, nitro, -NH2, -NH(alquilo), y -N(alquilo)2; o cuando dos restos R30 cuando están unidos al mismo átomo de carbono o átomos de carbono adyacentes pueden en forma opcional tomarse junto con el/los átomo(s) de carbono a los cuales están unidos para formar un anillo cicloalquilo, cicloalquenilo, heterociclilo, arilo, o heteroarilo; con la salvedad de que al menos uno de T, U, y V debe estar presente; y además que se hayan cumplido al menos una de las condiciones (a) - (e): (a) al menos uno de T y V está presente, y V es diferente de alquinilo; en donde dicho T o V está substituido con al menos un resto R10 seleccionado del grupo que consiste en ciano, - C(O)OR4, -C(O)R4, -C(O)N(R4)2, -C(O)N(R4)C(O)R4, -C(O)N(R4)C(O)NR4, -SR4, -S(O)2R4, -N(R4)-C(O)OR4, -OC(O)N(R4)2, -N(R4)C(O)N(R
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EP1973901B1 (en) 2014-12-17
US7683088B2 (en) 2010-03-23
KR20080085222A (ko) 2008-09-23
CN101405286A (zh) 2009-04-08
IL192690A0 (en) 2009-02-11
NO20083568L (no) 2008-10-16
AR059036A1 (es) 2008-03-12
US7524842B2 (en) 2009-04-28
RU2008133383A (ru) 2010-02-27
WO2007084451A1 (en) 2007-07-26
PE20071240A1 (es) 2008-01-14
TW200736247A (en) 2007-10-01
US20090156586A1 (en) 2009-06-18
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KR20080085221A (ko) 2008-09-23
ZA200806072B (en) 2009-04-29
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US20070197564A1 (en) 2007-08-23
BRPI0706599A2 (pt) 2011-03-29
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US20070265299A1 (en) 2007-11-15
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