AR096757A1 - Inhibidores de bromodominios - Google Patents
Inhibidores de bromodominiosInfo
- Publication number
- AR096757A1 AR096757A1 ARP140102430A ARP140102430A AR096757A1 AR 096757 A1 AR096757 A1 AR 096757A1 AR P140102430 A ARP140102430 A AR P140102430A AR P140102430 A ARP140102430 A AR P140102430A AR 096757 A1 AR096757 A1 AR 096757A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyleneyl
- alkylenyl
- alkyl
- nrjrk
- haloalkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005466 alkylenyl group Chemical group 0.000 abstract 25
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 24
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 18
- 229910052739 hydrogen Inorganic materials 0.000 abstract 15
- 239000001257 hydrogen Substances 0.000 abstract 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 15
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 12
- 125000001424 substituent group Chemical group 0.000 abstract 12
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical group 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical group O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 abstract 1
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 abstract 1
- 101710095156 E3 ubiquitin-protein ligase RBX1 Proteins 0.000 abstract 1
- 102100023877 E3 ubiquitin-protein ligase RBX1 Human genes 0.000 abstract 1
- 101710178916 RING-box protein 1 Proteins 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D471/02—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 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract
Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde Rˣ es hidrógeno o C₁₋₃ alquilo; Rʸ es hidrógeno o C₁₋₃ alquilo; A¹ es N o CR¹, A² es N o CR², A³ es N o CR³; y A⁴ es N o CR⁴; donde cero, uno, dos o tres de A¹, A², A³, y A⁴ son N; R¹ es hidrógeno, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, CN, NO₂; R² es hidrógeno, -S(O)₂R²ᵃ, -S(O)₂NR²ᵇR²ᶜ, -N(R²ᵇ)S(O)₂R²ᵃ, o -(C₁₋₆ alquilenil)-S(O)₂R²ᵃ; donde R²ᵃ es C₁₋₆ alquilo o C₁₋₆ haloalquilo; y R²ᵇ y R²ᶜ son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; L¹ es O, N(H), o OCH₂ donde la unidad CH₂ de OCH₂ se une a G¹; Rˣ¹, G¹, R³, y R⁴, se seleccionan entre (i), (ii), (iii), ó (iv); (i) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², -C(O)N(Rˣᵃ)(Rˣᵇ), C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᵇ, -SRˣᵇ, -S(O)Rˣᵇ, -S(O)₂Rˣᵇ, -NRˣᵃRˣᵇ, -C(O)Rˣᵇ, -C(O)ORˣᵇ, -C(O)NRˣᵃRˣᵇ, y -S(O)₂NRˣᵃRˣᵇ; C₂₋₆ alquenilo, o C₂₋₆ alquinilo; donde C₂₋₆ alquenilo y C₂₋₆ alquinilo están sustituidos en forma independiente entre sí con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ,-C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ, R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (ii) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², -C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ está sustituido con un grupo Rᵘ y además está opcionalmente sustituido con 1, 2, 3, 4, ó 5 grupos Rᵛ; R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (iii) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ; R³ es -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (iv) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ; R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es G⁴; Rˣᵃ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; Rˣᵇ, en cada caso, es en forma independiente C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en - CN, -ORᵃˣ¹, -SRᵃˣ¹, -S(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵃˣ¹, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, y -S(O)₂NRᵇˣ¹Rᶜˣ¹; Rˣᶜ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, -(C₁₋₆ alquilenil)-Gᵃ, o Rˣᵇ; Rᵃˣ¹, Rᵇˣ¹, y Rᶜˣ¹, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, o -(C₁₋₆ alquilenil)-Gᵃ; Rᵈˣ¹, en cada caso, es en forma independiente C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, o -(C₁₋₆ alquilenil)-Gᵃ; R¹ᵃ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, CN, o NO₂; R³ᵃ y R³ᵇ, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ, o C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORʰ, -SRʰ, -S(O)Rⁱ, -S(O)₂Rʰ, -NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, y -S(O)₂NRʲRᵏ; G⁴, en cada caso, es en forma independiente fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en C₁₋₆ alquilo, NO₂, halógeno, C₁₋₆ haloalquilo, -CN, oxo, -ORʰ, -SRʰ, -S(O)₂Rʰ, y -NRʲRᵏ; Rᵘ, en cada caso, es en forma independiente -(C₁₋₆ alquilenil)-Gᵘ, -(C₂₋₆ alquinilen)-Gᵘ, -(C₁₋₆ alquilenil)-SRʰ, -C(O)-Z¹, -C(O)-NZ¹Z², -S(O)₂-Z¹, -N(Z²)Z¹, o -N(Z²)S(O)₂-Z¹; donde Z¹ es Gᵘ, -(C₁₋₆ alquilenil)-Gᵘ, -(C₂₋₆ alquenilen)-Gᵘ, -(C₁₋₆ alquilenil)-CN, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-NRʲRᵏ, o -(C₁₋₆ alquilenil)-C₁₋₄ alcoxi-C₁₋₄ alcoxi, y Z² es hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; Gᵘ, en cada caso, es en forma independiente arilo, heteroarilo, heterociclo, cicloalquilo, o cicloalquenilo, donde cada Gᵘ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʰ, -O-(C₂₋₆ alquilenil)-NRʲRᵏ, -OC(O)Rⁱ, -OC(O)NRʲRᵏ, -O-(C₁₋₆ alquilenil)-NRʲRᵏ, -SRʰ, -S(O)₂Rʰ, -S(O)₂NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, -NRʲRᵏ, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)NRʲRᵏ, Gᵘᵃ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-OC(O)Rⁱ, -(C₁₋₆ alquilenil)-OC(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆ alquilenil)-S(O)₂Rʰ, -(C₁₋₆ alquilenil)-S(O)₂NRʲRᵏ, -(C₁₋₆ alquilenil)-C(O)Rʰ, -(C₁₋₆ alquilenil)-C(O)ORʰ, -(C₁₋₆ alquilenil)-C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-NRʲRᵏ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)Rⁱ, -(C₁₋₆ alquiIenil)-N(Rʰ)S(O)₂Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)O(Rⁱ), -(C₁₋₆ alquilenil)-N(Rʰ)C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-CN, y -(C₁₋₆ alquilenil)-Gᵘᵃ; Gᵃ, Gˣ¹, Gˣ², G³ᵃ, G³ᵇ, y Gᵘᵃ, en cada caso, son en forma independiente entre sí arilo, heteroarilo, heterociclo, cicloalquilo, o cicloalquenilo, cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, 4, ó 5 grupos Rᶻ; Rᶻ y Rᵛ, en cada caso, son en forma independiente entre sí C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʰ, -OC(O)Rⁱ, -OC(O)NRʲRᵏ, -SRʰ, -S(O)₂Rʰ, -S(O)₂NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, -NRʲRᵏ, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-OC(O)Rⁱ, -(C₁₋₆ alquilenil)-OC(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆alquilenil)-S(O)₂Rʰ, -(C₁₋₆ alquilenil)-S(O)₂NRʲRᵏ, -(C₁₋₆ alquilenil)-C(O)Rʰ, -(C₁₋₆ alquilenil)-C(O)ORʰ, -(C₁₋₆ alquilenil)-C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-NRʲRᵏ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)S(O)₂Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)O(Rⁱ), -(C₁₋₆ alquilenil)-N(Rʰ)C(O)NRʲRᵏ, o -(C₁₋₆ alquilenil)-CN; Rʰ, Rʲ, Rᵏ, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; y Rⁱ, en cada caso, es en forma independiente C₁₋₆ alquilo o C₁₋₆ haloalquilo.
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