AR090602A1 - AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2 - Google Patents

AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2

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Publication number
AR090602A1
AR090602A1 ARP130101102A ARP130101102A AR090602A1 AR 090602 A1 AR090602 A1 AR 090602A1 AR P130101102 A ARP130101102 A AR P130101102A AR P130101102 A ARP130101102 A AR P130101102A AR 090602 A1 AR090602 A1 AR 090602A1
Authority
AR
Argentina
Prior art keywords
atoms
mono
unsubstituted
cooa
hal
Prior art date
Application number
ARP130101102A
Other languages
English (en)
Inventor
Dr Zenke Frank
Dr Heinrich Timo
Dra Krier Mireille
Dra Friese-Hamim Manja
Seenisamy Jeyaprakashnarayanan
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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 Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR090602A1 publication Critical patent/AR090602A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/402—1-aryl substituted, e.g. piretanide
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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Abstract

Los compuestos de la fórmula (1) en donde R es NR²R⁴, Alk, C(=CH₂)[C(R⁴)₂]ₙAr², Het², O[C(R⁴)₂]ₙAr² u OA; X es CO o CH₂; Y es CO o CH₂; R¹ es H, [C(R⁴)₂]ₙAr¹, (CH₂)ₙHet, (CH₂)ₙCyc, [C(R⁴)₂]ₙCOOH, [C(R⁴)₂]ₙCONHAr¹, [C(R⁴)₂]ₙCONH₂, [C(R⁴)₂]ₙNHA, [C(R⁴)₂]ₙNA₂, O[C(R⁴)₂]ₙAr¹, [C(R⁴)₂]ₙOR⁷, [C(R⁴)₂]ₙCOO(CH₂)ₙAr¹, [C(R⁴)₂]ₙCOOA, [C(R⁴)₂]ₙCONH[C(R⁴)₂]ₚCON(R⁴)₂ o [C(R⁴)₂]ₙCONHCR⁴[(CH₂)ₙN(R⁴)₂]CON(R⁴)₂; R² es H, [C(R⁴)₂]ₙAr², (CH₂)ₙCOHet¹, (CH₂)ₙCOAr², (CH₂)ₘNA₂ O (CH₂)ₙHet; R³ es OH u OCOA; R⁴ es H o alquilo con 1, 2, 3 ó 4 átomos de C; R² y R⁴ también son juntos alquileno con 2, 3, 4 ó 5 átomos de C, en donde un grupo CH₂ también puede esta reemplazado por N(CH₂)ₘOH ó SO₂; R⁵, R⁶ son cada uno, de modo independiente entre sí, H, F o A; R⁵ y R⁶ también son juntos alquileno con 2, 3, 4 ó 5 átomos de C, en donde un grupo CH₂ también puede estar reemplazado por NCOA u O; R⁷ es H o A; Ar¹ es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, OH, OA, CONH₂, CONHA, CONA₂, NHSO₂A, CONHCyc, NHSO₂Cyc, CONHAr², COHet¹ y/o NASO₂A; Ar² es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, CONH₂, y/u OAr³; Ar³ es fenilo no sustituido o monosustituido con NH₂; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático no sustituido o mono-, di- o trisustituido con Hal, A, OA, CN, NH₂, NHA, NA₂, NO₂, CN, COOH, COOA, (CH₂)ₙCONH₂, (CH₂)ₙCONHA, (CH₂)ₙCONA₂, NHCOA, COA, CHO, Het¹, SO₂A, SO₂NH₂, SO₂NHA, SO₂NA₂, CONHNH₂, CONHAr³, =O y/o Ar³ con 1 a 4 átomos de N y/u O y/o S; Het¹ es un heterociclo monocíclico saturado no sustituido o mono-, di- o trisustituido con =O y/o COOA con 1 a 4 átomos de N y/u O y/o S; Het² es isoindolilo; A es alquilo no ramificado o ramificado con 1 - 10 átomos de C, en donde 1 - 7 átomos de H pueden estar reemplazados por F, Cl, Br, OH, CHO, COA, COOA, CN, CONA₂, CONHA y/o CONH₂, y/o en donde uno o dos grupos no adyacentes CH y/o CH₂ pueden estar reemplazados por O, o Cyc; Alk es alquenilo con 2, 3, 4, 5 ó 6 átomos de C; Cyc es alquilo cíclico no sustituido o mono-, di- o trisustituido con NHCOA, NHSO₂, OH, OA, A, NH₂, NHA, NA₂, COOA, COOH y/o CONHA con 3 - 7 átomos de C; Hal es F, Cl, Br o I; m es 1, 2, 3 ó 4; n es 0, 1, 2, 3 ó 4; p es 1, 2 ó 3; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la metionina-amino-peptidasa y se pueden usar para el tratamiento de tumores.
ARP130101102A 2012-04-04 2013-04-04 AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2 AR090602A1 (es)

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