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AR091962A1 - Compuesto antidiabeticos triciclicos - Google Patents

Compuesto antidiabeticos triciclicos

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Publication number
AR091962A1
AR091962A1 ARP130102739A ARP130102739A AR091962A1 AR 091962 A1 AR091962 A1 AR 091962A1 AR P130102739 A ARP130102739 A AR P130102739A AR P130102739 A ARP130102739 A AR P130102739A AR 091962 A1 AR091962 A1 AR 091962A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
substituted
halogen
Prior art date
Application number
ARP130102739A
Other languages
English (en)
Original Assignee
Merck Sharp & Dohme
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
Priority claimed from PCT/CN2012/079558 external-priority patent/WO2014019186A1/en
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of AR091962A1 publication Critical patent/AR091962A1/es

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    • 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
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine 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
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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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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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
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
    • A61K31/4427—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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505—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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/06—Antihyperlipidemics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • 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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    • C07D405/02—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 containing two hetero rings
    • C07D405/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula estructura [1] o a una sal farmacéuticamente aceptable del mismo; en la que X se elige de entre el grupo que consiste en: (1) oxígeno, y (2) NH; T se elige de entre el grupo que consiste en: CH, N y N-óxido; U se elige de entre el grupo que consiste en: CH, N y N-óxido; V se elige de entre el grupo que consiste en: CH, N y N-óxido; siempre que uno o dos de T, U y V sea N o N-óxido; A se elige de entre el grupo que consiste en: (1) arilo, y (2) heteroarilo, en la que A no está sustituido o está sustituido con de uno a cinco sustituyentes elegidos de entre Rᵃ; B se elige de entre el grupo que consiste en: (1) arilo, (2) aril-O, (3) cicloalquilo C₃₋₆, (4) cicloalquilo C₃₋₆alquilo C₁₋₁₀, (5) cicloalquilo C₃₋₆alquilo C₁₋₁₀-O, (6) cicloheteroalquilo C₂₋₅, (7) heteroarilo, (8) heteroaril-O, (9) alquilarilo C₁₋₁₀, y (10) heteroarilalquilo C₁₋₁₀; en los que B no está sustituido o está sustituido con de uno a cinco sustituyentes elegidos de entre Rᵇ; R¹ se elige de entre el grupo que consiste en: (1) halógeno, (2) -ORᵉ, (3) -CN, (4) alquilo C₁₋₆, y (5) cicloalquilo C₃₋₆, en los que cada alquilo C₁₋₆ y cicloalquilo C₃₋₆ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos de entre Rⁱ; R² se elige de entre el grupo que consiste en: (1) hidrógeno, (2) alquilo C₁₋₆, y (3) cicloalquilo C₃₋₆, en los que cada alquilo C₁₋₆ y cicloalquilo C₃₋₆ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos de entre Rʲ; R³ se elige de entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) -ORᵉ, (4) alquilo C₁₋₆, (5) alquenilo C₂₋₆, (6) alquinilo C₂₋₆, y (7) cicloalquilo C₃₋₆, en los que cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ y cicloalquilo C₃₋₆ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos de entre RL; R⁴ se elige de entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) -ORᵉ, (4) alquilo C₁₋₆, (5) alquenilo C₂₋₆, (6) alquinilo C₂₋₆, y (7) cicloalquilo C₃₋₆, en los que cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ y cicloalquilo C₃₋₆ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos de entre RL; R⁵ se elige de entre el grupo que consiste en: (1) hidrógeno, (2) alquilo C₁₋₃,y (3) halógeno; R⁶ se elige de entre el grupo que consiste en: (1) hidrógeno, (2) alquilo C₁₋₃, y (3) halógeno, o R⁵ y R⁶ pueden formar conjuntamente oxo; Rᵃ se elige de entre el grupo que consiste en: (1) alquilo C₁₋₆, (2) halógeno, (3) -ORᵉ, (4) -NRᶜS(O)ₘRᵉ, (5) -S(O)ₘRᵉ, (6) -S(O)ₘNRᶜRᵈ, (7) -NRᶜRᵈ, (8) -C(O)Rᵉ, (9) -OC(O)Rᵉ, (10) -CO₂Rᵉ, (11) -CN, (12) -C(O)NRᶜRᵈ, (13) -NRᶜC(O)Rᵉ, (14) -NRᶜC(O)ORᵉ, (15) -NRᶜC(O)NRᶜRᵈ, (16) -CF₃, (17) -OCF₃, (18) -OCHF₂, (19) cicloalquilo C₃₋₆, y (20) cicloheteroalquilo C₂₋₅; Rᵇ se elige independientemente de entre el grupo que consiste en: (1) alquilo C₁₋₁₀, (2) alquenilo C₂₋₁₀, (3) halógeno, (4) -OH, (5) -O-alquilo C₁₋₁₀, (6) -O-alquenilo C₂₋₁₀, (7) -O(CH₂)ₚO-alquilo C₁₋₁₀, (8) -O(CH₂)ₚ-cicloalquilo C₃₋₆, (9) -O(CH₂)ₚ-cicloalquilo C₃₋₆alquilo C₁₋₁₀, (10) -O(CH₂)ₚ-cicloheteroalquilo C₂₋₁₀, (11) -O(CH₂)ₚ-cicloheteroalquilo C₂₋₅alquilo C₁₋₁₀, (12) -O-arilo, (13) -O-heteroarilo, (14) -O-arilalquilo C₁₋₁₀, (15) -O-heteroarilalquilo C₁₋₁₀, (16) -NRᶜS(O)ₘRᵉ, (17) -S(O)ₘRᵉ, (18) -S(O)ₘNRᶜRᵈ, (19) -NRᶜRᵈ, (20) -C(O)Rᵉ, (21) -OC(O)Rᵉ, (22) CO₂Rᵉ, (23) -CN, (24) -C(O)NRᶜRᵈ, (25) -NRᶜC(O)Rᵉ, (26) -NRᶜC(O)ORᵉ, (27) -NRᶜC(O)NRᶜRᵈ, (28) -O(CH₂)ₚO-cicloalquilo C₃₋₆, (29) -O(CH₂)ₚO-cicloheteroalquilo C₂₋₁₀, (30) -CF₃, (31) -OCF₃, (32) -OCHF₂, (33) -(CH₂)ₚ-cicloalquilo C₃₋₆, (34) -(CH₂)ₚ-cicloheteroalquilo C₂₋₁₀, (35) arilo, (36) heteroarilo, (37) arilalquilo C₁₋₁₀, y (38) heteroarilalquilo C₁₋₁₀, en los que cada Rᵇ no está sustituido o está sustituido con de uno a cinco sustituyentes elegidos de entre Rᵏ; Rᶜ y Rᵈ se elige cada uno independientemente de entre el grupo que consiste en: (1) hidrógeno, (2) alquilo C₁₋₁₀, (3) alquenilo C₂₋₁₀, (4) cicloalquilo C₃₋₆, (5) cicloalquilo C₃₋₆alquilo C₁₋₁₀, (6) cicloheteroalquilo, (7) cicloheteroalquilalquilo C₁₋₁₀, (8) arilo, (9) heteroarilo, (10) arilalquilo C₁₋₁₀, y (11) heteroarilalquilo C₁₋₁₀, o Rᶜ y Rᵈ junto con el(los) átomo(s) al(los) que está(n) unidos forman un anillo cicloheteroalquilo de 4 a 7 miembros que contiene 0 - 2 heteroátomos adicionales elegidos independientemente de entre oxígeno, azufre y N-Rᵍ, y en los que cada Rᶜ y Rᵈ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos independientemente de entre Rᶠ; cada Rᵉ se elige independientemente de entre el grupo que consiste en: (1) hidrógeno, (2) alquilo C₁₋₁₀, (3) alquenilo C₂₋₁₀, (4) cicloalquilo C₃₋₆, (5) cicloalquilo C₃₋₆alquilo C₁₋₁₀, (6) cicloheteroalquilo C₂₋₅,(7) cicloheteroalquilo C₂₋₅alquilo C₁₋₁₀, (8) arilo, (9) heteroarilo, (10) arilalquilo C₁₋₁₀, y (11) heteroarilalquilo C₁₋₁₀, en los que cada Rᵉ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos de entre Rʰ; cada Rᶠ se elige de entre el grupo que consiste en: (1) halógeno, (2) alquilo C₁₋₁₀, (3) -OH, (4) -O-alquilo C₁₋₄, (5) -S(O)ₘ-alquilo C₁₋₄, (6) -CN, (7) -CF₃. (8) -OCHF₂, y (9) -OCF₃, en los que cada alquilo C₁₋₁₀ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos independientemente de entre: -OH, halógeno, ciano, y -S(O)₂CH₃; cada Rᵍ se elige de entre el grupo que consiste en: (1) hidrógeno, (2) -C(O)Rᵉ, y (3) alquilo C₁₋₁₀, en los que el alquilo C₁₋₁₀ no está sustituido o está sustituido con de uno a cinco flúor; cada Rʰ se elige de entre el grupo que consiste en: (1) halógeno, (2) alquilo C₁₋₁₀, (3) -OH, (4) -O-alquilo C₁₋₄, (5) -S(O)ₘ-alquilo C₁₋₄, (6) -CN, (7) -CF₃, (8) -OCHF₂, y (9) -OCF₃, en los que cada alquilo C₁₋₁₀ no está sustituido o está sustituido con de uno a tres sustituyentes elegidos independientemente de entre: -OH, halógeno, ciano, y -S(O)₂CH₃; Rⁱ se elige independientemente de entre el grupo que consiste en: (1) alquilo C₁₋₆, (2) -ORᵉ, (3) NRᶜS(O)ₘRᵉ, (4) halógeno, (5) -S(O)ₘRᵉ, (6) -S(O)ₘNRᶜRᵈ, (7) -NRᶜRᵈ, (8) -C(O)Rᵉ, (9) -OC(O)Rᵉ, (10) -CO₂Rᵉ, (11) -CN, (12) -C(O)NRᶜRᵈ, (13) -NRᶜC(O)Rᵉ, (14) -NRᶜC(O)ORᵉ, (15) -NRᶜC(O)NRᶜRᵈ, (16) -CF₃, (17) -OCF₃, (18) -OCHF₂, (19) cicloalquilo C₃₋₆, y (20) cicloheteroalquilo C₂₋₅; Rʲ se elige independientemente de entre el grupo que consiste en: (1) alquilo C₁₋₆, (2) -ORᵉ, (3) -NRᶜS(O)ₘRᵉ, (4) halógeno, (5) -S(O)ₘRᵉ, (6) -S(O)ₘNRᶜRᵈ, (7) -NRᶜRᵈ, (8) -C(O)Rᵉ, (9) -OC(O)Rᵉ, (10) -CO₂Rᵉ, (11) -CN, (12) -C(O)NRᶜRᵈ, (13) -NRᶜC(O)Rᵉ, (14) -NRᶜC(O)ORᵉ, (15) -NRᶜC(O)NRᶜRᵈ, (16) -CF₃, (17) -OCF₃, (18) -OCHF₂, (19) cicloalquilo C₃₋₆, y (20) cicloheteroalquilo C₂₋₅; cada Rᵏ se elige independiente
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US20150191495A1 (en) 2015-07-09
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RU2015106909A (ru) 2016-09-27
US20140045746A1 (en) 2014-02-13
AU2013296470A1 (en) 2015-02-05
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