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AR099768A1 - Inhibidores de diacilglicerol aciltransferasa 2 - Google Patents

Inhibidores de diacilglicerol aciltransferasa 2

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Publication number
AR099768A1
AR099768A1 ARP150100790A ARP150100790A AR099768A1 AR 099768 A1 AR099768 A1 AR 099768A1 AR P150100790 A ARP150100790 A AR P150100790A AR P150100790 A ARP150100790 A AR P150100790A AR 099768 A1 AR099768 A1 AR 099768A1
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AR
Argentina
Prior art keywords
alkyl
cooh
heteroaryl
aryl
cycloalkyl
Prior art date
Application number
ARP150100790A
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English (en)
Inventor
Cabral Shawn
Futatsugi Kentaro
Hepworth David
Huard Kim
Wei Kung Daniel
Tuula Marjukka Shung - Orr Suvi
Song Kun
Original Assignee
Pfizer
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Application filed by Pfizer filed Critical Pfizer
Publication of AR099768A1 publication Critical patent/AR099768A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D491/02—Heterocyclic 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
    • C07D491/08—Bridged systems

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Abstract

Compuestos que inhiben la actividad de la diacilglicerol aciltransferasa 2 (DGAT2) y sus usos en el tratamiento de enfermedades relacionadas con estos en animales. Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1) en donde D es N, CH o CF; R¹ es C₁₋₄ alquilo opcionalmente sustituido con 1, 2 ó 3 sustituyentes cada uno seleccionado independientemente de fluoro y C₃₋₆ cicloalquilo; R² es fluoro o C₁₋₄ alquilo; R³ es H, C₁₋₄ alquilo o C₃₋₆ cicloalquilo; R⁴ es H, -C₁₋₄ alquilo, -(C₁₋₄ alquil)ₚ-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)ₚ-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)ₚ-arilo o -(C₁₋₄ alquil)ₚ-heteroarilo, en donde R⁴ se sustituye opcionalmente con 1, 2, 3 ó 4 sustituyentes seleccionados de halo, ciano, oxo, aminilo, iminilo, -OH, -C₁₋₄ alquilo, -C₁₋₄ fluoroalquilo, -C₁₋₄ alcoxi, -C₃₋₆ cicloalcoxi, -C₁₋₄ fluoroalcoxi, -(C₁₋₄ alquil)q-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquil-COOH, -(C₁₋₄ alquil)q-C₃₋₆ heterociclil-COOH, -(C₁₋₄ alquil)q-aril-COOH, -(C₁₋₄ alquil)q-heteroaril-COOH, -O-(C₁₋₄ alquil)q-COOH, -O-(C₁₋₄ alquil)q-aril-COOH, -O-(C₁₋₄ alquil)q-heteroaril-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)q-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)q-arilo, -(C₁₋₄ alquil)q-heteroarilo, -C(O)-C₁₋₄ alquilo, -C(O)-C₁₋₄ alcoxi, -C(O)-C₃₋₆ cicloalquilo, -C(O)-C₃₋₆ heterociclilo, -C(O)-NR⁶R⁷, -C(O)-(C₁₋₄ alquil)q-arilo, -C(O)-(C₁₋₄ alquil)q-heteroarilo, -NR⁶R⁷, -NR⁶-C(O)-R⁷, -(C₁₋₄ alquil)q-O-arilo, -(C₁₋₄ alquil)q-O-heteroarilo, -S(O)₂-R⁷ y -S(O)₂-NR⁶R⁷; o R³ y R⁴ juntos se pueden unir para formar un sistema de anillos totalmente saturados o parcialmente saturados de 4 a 10 miembros opcionalmente sustituidos con 1, 2, 3 ó 4 sustituyentes seleccionados de halo, ciano, -OH, -C₁₋₄ alquilo, -C₁₋₄ fluoroalquilo, -C₁₋₄ alcoxi, -C₃₋₆ cicloalcoxi, -C₁₋₄ fluoroalcoxi, -(C₁₋₄ alquil)q-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquil-COOH, -(C₁₋₄ alquil)q-C₃₋₆ heterociclil-COOH, -(C₁₋₄ alquil)q-aril-COOH, -(C₁₋₄ alquil)q-heteroaril-COOH, -O-(C₁₋₄ alquil)q-COOH, -O-(C₁₋₄ alquil)q-aril-COOH, -O-(C₁₋₄ alquil)q-heteroaril-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)q-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)q-arilo, -(C₁₋₄ alquil)q-heteroarilo, -C(O)-C₁₋₄ alquilo, -C(O)-C₃₋₆ cicloalquilo, -C(O)-C₃₋₆ heterociclilo, -C(O)-arilo, -C(O)-heteroarilo, -C(O)-NR⁶R⁷, -C(O)-C₁₋₄ alquil-arilo, -C(O)-C₁₋₄ alquil-heteroarilo, -NR⁶R⁷, -NR⁶-C(O)-R⁷, -O-arilo, -O-heteroarilo, -C₁₋₄ alquil-O-arilo, -C₁₋₄ alquil-O-heteroarilo, -O-C₁₋₄ alquil-arilo y -O-C₁₋₄ alquil-heteroarilo; R⁵ es H, F o ciano; R⁶ es H, C₁₋₄ alquilo o -S(O)₂-R⁷; R⁷ es H, C₁₋₄ alquilo, -C₃₋₆ cicloalquilo, -C₃₋₆ heterociclilo, arilo o heteroarilo; n es 0, 1, 2 ó 3; p es 0 ó 1; y q es 0 ó 1; o una sal de aquel aceptable desde el punto de vista farmacéutico.
ARP150100790A 2014-03-17 2015-03-16 Inhibidores de diacilglicerol aciltransferasa 2 AR099768A1 (es)

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