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AR129910A1 - Inhibidores de tirosina cinasa 2 y usos de estos - Google Patents

Inhibidores de tirosina cinasa 2 y usos de estos

Info

Publication number
AR129910A1
AR129910A1 ARP230101832A ARP230101832A AR129910A1 AR 129910 A1 AR129910 A1 AR 129910A1 AR P230101832 A ARP230101832 A AR P230101832A AR P230101832 A ARP230101832 A AR P230101832A AR 129910 A1 AR129910 A1 AR 129910A1
Authority
AR
Argentina
Prior art keywords
membered monocyclic
alkyl
heterocyclyl
cycloalkyl
membered
Prior art date
Application number
ARP230101832A
Other languages
English (en)
Inventor
Jeffrey Vessels
Tamara Halkina Levin
Harold George Vandeveer
Lopez De Turiso Felix Gonzalez
Zhili Xin
Edward Yin Shiang Lin
Soma Maitra
Vatee Pattaropong
Simone Sciabola
Christopher HELAL
Kevin M Guckian
Original Assignee
Biogen Ma Inc
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 Biogen Ma Inc filed Critical Biogen Ma Inc
Publication of AR129910A1 publication Critical patent/AR129910A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
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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
    • A—HUMAN NECESSITIES
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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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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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
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
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Abstract

La presente descripción se refiere a compuestos de fórmula (1), o sales farmacéuticamente aceptables de estos, en donde todas las variables de la fórmula (1) son como se definen en la solicitud. Los compuestos de la presente descripción son capaces de inhibir la actividad de la tirosina cinasa 2 (TYK2). La descripción proporciona además métodos para preparar los compuestos de la descripción y métodos para su uso terapéutico. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable de este, en donde: R¹ es H, alquilo C₁₋₆, -OR¹ᵃ, -NR¹ᵇR¹ᶜ, carbociclilo monocíclico de 3 a 7 miembros, o heterociclilo monocíclico de 4 a 7 miembros, en donde el alquilo C₁₋₆, el carbociclilo monocíclico de 3 a 7 miembros y el heterociclilo monocíclico de 4 a 7 miembros representado por R¹ están cada uno opcionalmente sustituidos con uno o más R¹ᵈ; cada uno de R¹ᵃ, R¹ᵇ y R¹ᶜ es independientemente H, alquilo C₁₋₄ o carbociclilo monocíclico de 3 a 4 miembros; cada R¹ᵈ es independientemente halo, oxo, -CN, -OR¹ᵃ, -NR¹ᵇR¹ᶜ, alquilo C₁₋₆, haloalquilo C₁₋₄, fenilo, heteroarilo de 5 a 6 miembros, carbociclilo monocíclico de 3 a 7 miembros o heterociclilo monocíclico de 4 a 7 miembros; R² se selecciona de H, halo, alquilo C₁₋₆, cicloalquilo C₃₋₇, -OR²ᵃ, -N(R²ᵇ)₂, heterociclilo monocíclico o bicíclico de 4 a 11 miembros que tiene de 1 a 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, y heteroarilo monocíclico de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, en donde el alquilo C₁₋₆, el cicloalquilo C₃₋₇, el heterociclilo monocíclico o bicíclico de 5 a 11 miembros y el heteroarilo monocíclico de 5 a 6 miembros representado por R² están opcionalmente sustituidos con 1 a 3 R²⁰; R²ᵃ se selecciona de H, alquilo C₁₋₆, cicloalquilo C₃₋₇, heteroarilo de 5 o 6 miembros, y heterociclilo monocíclico de 4 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, en donde el alquilo C₁₋₆, cicloalquilo C₃₋₇, heteroarilo de 5 o 6 miembros, y heterociclilo monocíclico de 4 a 7 miembros representado por R²ᵃ están opcionalmente sustituidos con 1 a 3 R²⁰; cada R²ᵇ es independientemente H, alquilo C₁₋₄, alquilo C₁₋₃-alcoxi C₁₋₃, alcoxi C₁₋₄ o heterociclilo monocíclico de 4 a 6 miembros; R²⁰, para cada aparición, se selecciona independientemente de halo, -CN, alquilo C₁₋₄, haloalquilo C₁₋₄, -OR²⁰ᶜ-C(O)R²⁰ᵇ, -C(O)N(R²⁰ᵇ)₂, -N(R²⁰ᵇ)₂, -SO₂R²⁰ᵇ, -P(O)(alquilo C₁₋₃)₂, fenilo, cicloalquilo C₃₋₇, carbociclo bicíclico de 5 a 10 miembros, heterociclilo monocíclico o bicíclico de 4 a 10 miembros con 1 a 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, y heteroarilo monocíclico de 5 a 6 miembros con 1 a 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, en donde el alquilo C₁₋₄, el fenilo, el cicloalquilo C₃₋₇, el carbociclo bicíclico de 5 a 10 miembros, el heterociclilo monocíclico o bicíclico de 4 a 10 miembros y el heteroarilo monocíclico de 5 a 6 miembros representados por R²⁰ están cada uno opcionalmente sustituidos con 1 a 3 R²⁰⁰; cada R²⁰ᵇ es independientemente H, alquilo C₁₋₄ o alcoxi C₁₋₄; R²⁰ᶜ es H, alquilo C₁₋₄, haloalquilo C₁₋₄, cicloalquilo C₃₋₆, o heterociclo monocíclico de 4 a 6 miembros, en donde el alquilo C₁₋₄ está opcionalmente sustituido por alcoxi C₁₋₃; R²⁰⁰, para cada aparición, se selecciona independientemente de halo, -CN, alquilo C₁₋₄, alquilo C₁₋₃-alcoxi C₁₋₃, haloalquilo C₁₋₄, -OH, -N(R²⁰ᵇ)₂, alcoxi C₁₋₃, haloalcoxi C₁₋₃, cicloalquilo C₃₋₇ y heterociclilo monocíclico o bicíclico de 5 a 10 miembros opcionalmente sustituido con 1 a 3 alquilo C₁₋₃ o alcoxi C₁₋₃; el anillo B es fenilo, heteroarilo monocíclico o bicíclico de 5 a 10 miembros, carbociclilo monocíclico de 3 a 7 miembros o heterociclilo monocíclico de 4 a 7 miembros, cada uno de los cuales está opcionalmente sustituido con uno o más RB; cada RB se selecciona independientemente de halo, -CN, -ORBᵃ, -N(RBᵇ)₂, -C(O)RBᶜ, -C(O)ORBᵃ, -SO₂RBᶜ, alquilo C₁₋₆, alquenilo C₂₋₆, fenilo, carbociclilo monocíclico de 3 a 7 miembros, heterociclilo monocíclico o bicíclico de 4 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, y heteroarilo monocíclico o bicíclico de 5 a 10 miembros que tiene de 1 a 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno y azufre, en donde el alquilo C₁₋₆, el alquenilo C₂₋₆, el fenilo, el carbociclilo monocíclico de 3 a 7 miembros, el heterociclilo monocíclico de 4 a 7 miembros y el heteroarilo monocíclico o bicíclico de 5 a 10 miembros representados por RB están opcionalmente sustituidos con uno o más RB¹; cada RB¹ se selecciona independientemente de halo, oxo, -CN, -ORBᵃ, -N(RBᵇ)₂, alquilo C₁₋₄, alquilo C₁₋₄-RBᵈ, haloalquilo C₁₋₄, -C(O)ORBᵃ, fenilo, heteroarilo de 5 a 6 miembros, carbociclilo monocíclico de 3 a 7 miembros y heterociclilo monocíclico de 4 a 8 miembros; RBᵃ es independientemente H, alquilo C₁₋₄, cicloalquilo C₃₋₇, o heterociclilo monocíclico o bicíclico de 4 a 8 miembros, en donde el alquilo C₁₋₄, el cicloalquilo C₃₋₇ y el heterociclilo monocíclico o bicíclico de 4 a 8 miembros representados por RBᵃ están opcionalmente sustituidos con 1 o 2 RB⁰; cada RB⁰ es independientemente halo, -CN, -OH, alquilo C₁₋₄ o alcoxi C₁₋₄; cada RBᵇ es independientemente H, alquilo C₁₋₄, alcoxi C₁₋₄ o cicloalquilo C₃₋₇; RBᶜ es alquilo C₁₋₆ o cicloalquilo C₃₋₇; RBᵈ es -C(O)ORBᵃ, -N(RBᵇ)₂, -ORBᵃ, carbociclilo monocíclico de 3 a 7 miembros, o heterociclilo monocíclico de 4 a 8 miembros; y RN¹ y RN² son cada uno independientemente H o alquilo C₁₋₄.
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