AR102492A1 - Cromanos sustituidos y métodos para su uso - Google Patents

Cromanos sustituidos y métodos para su uso

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Publication number
AR102492A1
AR102492A1 ARP150103536A ARP150103536A AR102492A1 AR 102492 A1 AR102492 A1 AR 102492A1 AR P150103536 A ARP150103536 A AR P150103536A AR P150103536 A ARP150103536 A AR P150103536A AR 102492 A1 AR102492 A1 AR 102492A1
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Argentina
Prior art keywords
alkyl
haloalkyl
alkylenyl
independently
case
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ARP150103536A
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English (en)
Inventor
R Koenig John
Bogdan Andrew
Voigth Eric
Liu Bo
J Altenbach Robert
C Yeung Ming
B Searle Xenia
Wang Xueqing
R Kym Philip
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Abbvie Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=55858309&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR102492(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbvie Inc filed Critical Abbvie Inc
Publication of AR102492A1 publication Critical patent/AR102492A1/es

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    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
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    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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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
    • A61K31/4353—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
    • A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • 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
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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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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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D405/14—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 three or more hetero rings
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    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
    • C07D491/04—Ortho-condensed systems
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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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Agentes en el tratamiento de enfermedades y condiciones mediadas y moduladas por CFTR, que incluyen fibrosis quística, síndrome de Sjögren, insuficiencia pancreática, enfermedad pulmonar obstructiva crónica y enfermedad obstructiva crónica del flujo aéreo. También se proveen composiciones farmacéuticas que comprenden uno o más de los compuestos de fórmula (1). Reivindicación 1: Un compuesto de fórmula (1) o una sal aceptable farmacéuticamente del mismo, donde X es CR² e Y es CR³; o X es N e Y es CR³; o X es CR² e Y es N; m es 0, 1, 2, ó 3; R son sustituyentes opcionales en el anillo ciclopropilo, y en cada caso, son en forma independiente entre sí halógeno, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R¹ y R², son en forma independiente entre sí hidrógeno, halógeno, C₁₋₆ haloalquilo, C₁₋₆ alquilo, -OR¹A, -C(O)OR¹B, -NR¹AR²A, o -C(O)NR¹AR²A; R¹A y R²A, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ haloalquilo, G¹A, o C₁₋₆ alquilo; donde el C₁₋₆ haloalquilo y el C₁₋₆ alquilo está cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre el grupo que consiste en -ORZA, -SRZA, -S(O)₂RZA, -C(O)RZA, -C(O)ORZA, -C(O)N(RZA)₂, -N(RZA)₂, -N(RZA)C(O)RZB, -N(RZA)S(O)₂RZB, -N(RZA)C(O)ORZB, -N(RZA)C(O)N(RZA), -CN, y G¹A; o R¹A y R²A junto con el átomo de nitrógeno al cual están unidos forman un heterociclo de 4 - 6 miembros donde el heterociclo de 4 - 6 miembros está opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre el grupo que consiste en halógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, -ORʲ, y N(Rʲ)₂; donde RZA, en cada caso, es en forma independiente hidrógeno, C₁₋₆, haloalquilo, C₁₋₆ alquilo, G¹A, o -(C₁₋₆ alquilenilo)-G¹A; y RZB, en cada caso, es en forma independiente C₁₋₆ haloalquilo, C₁₋₆ alquilo, G¹A, o -(C₁₋₆ alquilenilo)-G¹A; R¹B es hidrógeno, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R³ y R¹⁴, son en forma independiente entre sí hidrógeno, halógeno, C₁₋₆ haloalquilo, C₁₋₆ alquilo, -OH, o -O-(C₁₋₆ alquilo); R⁴ es hidrógeno, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R⁵ es hidrógeno, -C(O)Rⁱ, -C(O)OH, -C(O)O(C₁₋₆ alquilo), -C(O)N(Rʰ)₂, C₁₋₆ haloalquilo, C₁₋₆ alquilo, o G²A; donde el C₁₋₆ haloalquilo y el C₁₋₆ alquilo está cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre el grupo que consiste en -ORʰ, -OC(O)N(Rʰ)₂, -C(O)Rʰ, -C(O)ORʰ, -C(O)N(Rʰ)₂, -N(Rʰ)₂, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)N(Rʰ)₂, y G²A; o R⁴ y R⁵, junto con el átomo de carbono al cual se encuentran unidos, forman un cicloalquilo C₃₋₆ o un heterociclo de 4 - 6 miembros; donde el C₃₋₆ cicloalquilo y el heterociclo de 4 - 6 miembros está cada uno opcionalmente sustituido con 1, 2, ó 3 grupos Rᵖ seleccionados en forma independiente; G²A, en cada caso, es en forma independiente cicloalquilo, cicloalquenilo, heterociclo, arilo, o heteroarilo, cada uno de los cuales no está sustituido o está sustituido en forma independiente con 1, 2, ó 3 grupos Rq seleccionados en forma independiente; Rᵖ y Rq, en cada caso, son en forma independiente entre sí C₁₋₆ alquilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʰ, -OC(O)Rⁱ, -OC(O)N(Rʰ)₂, -SRʰ, -S(O)₂Rʰ, -S(O)₂N(Rʰ)₂, -C(O)Rʰ, -C(O)ORʰ, -C(O)N(Rʰ)₂, -C(O)N(Rʰ)S(O)₂Rʰ, -N(Rʰ)₂, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)N(Rʰ)₂, o GA, donde C₁₋₆, haloalquilo y el C₁₋₆ alquilo está cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre el grupo que consiste en -ORʰ, -OC(O)Rⁱ, -OC(O)N(Rʰ)₂, -SRʰ, -S(O)₂Rʰ, -S(O)₂N(Rʰ)₂, -C(O)Rʰ, -C(O)ORʰ, -C(O)N(Rʰ)₂, -C(O)N(Rʰ)S(O)₂Rʰ, -N(Rʰ)₂, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)N(Rʰ)₂, -CN, y GA; Rʰ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ haloalquilo, C₁₋₆ alquilo, o GA, donde el C₁₋₆ haloalquilo y el C₁₋₆ alquilo está cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre el grupo que consiste en -ORʲ, -OC(O)N(Rʲ)₂, -SRʲ, -C(O)ORʲ, -C(O)N(Rʲ)₂, -N(Rʲ)₂, -CN, y GA; Rⁱ, en cada caso, es en forma independiente C₁₋₆ haloalquilo, C₁₋₆ alquilo, o GA, donde el C₁₋₆ haloalquilo y el C₁₋₆ alquilo está cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre el grupo que consiste en -ORʲ, -OC(O)N(Rʲ)₂, -SRʲ, -C(O)ORʲ, -C(O)N(Rʲ)₂, -N(Rʲ)₂, -CN, y GA; R⁶ es hidrógeno, halógeno, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R⁷ es hidrógeno, halógeno, -ORʲ, -N(Rʲ)₂, -N(Rʲ)C(O)Rᵏ, C₁₋₆ haloalquilo, C₁₋₆ alquilo, C₂₋₆ alquenilo, o -(C₁₋₆ alquilenilo)-G³A; R⁸ es hidrógeno, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R⁹, R¹⁰, y R¹³, son en forma independiente entre sí hidrógeno, halógeno, -ORʲ, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; R¹¹ y R¹² son en forma independiente entre sí hidrógeno, C₁₋₃ alquilo, o halógeno; G¹A, G³A, y GA, en cada caso, son en forma independiente entre sí cicloalquilo, cicloalquenilo, heterociclo, arilo, o heteroarilo, cada uno de los cuales no está sustituido o está sustituido en forma independiente con 1, 2, ó 3 grupos Rˢ seleccionados en forma independiente; donde Rˢ, en cada caso, es en forma independiente C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʲ, -OC(O)Rᵏ, -OC(O)N(Rʲ)₂, -SRʲ, -S(O)₂Rʲ, -S(O)₂N(Rʲ)₂, -C(O)Rʲ, -C(O)ORʲ, -C(O)N(Rʲ)₂, -N(Rʲ)₂, -N(Rʲ)C(O)Rᵏ, -N(Rʲ)S(O)₂Rᵏ, -N(Rʲ)C(O)O(Rᵏ), -N(Rʲ)C(O)N(Rʲ)₂, -(C₁₋₆ alquilenilo)-ORʲ, -(C₁₋₆ alquilenilo)-OC(O)Rᵏ, -(C₁₋₆ alquilenilo)-OC(O)N(Rʲ)₂, -(C₁₋₆ alquilenilo)-SRʲ, -(C₁₋₆ alquilenilo)-S(O)₂Rʲ, -(C₁₋₆ alquilenilo)-S(O)₂N(Rʲ)₂, -(C₁₋₆ alquilenilo)-C(O)Rʲ, -(C₁₋₆ alquilenilo)-C(O)ORʲ, -(C₁₋₆ alquilenilo)-C(O)N(Rʲ)₂, -(C₁₋₆ alquilenilo)-N(Rʲ)₂, -(C₁₋₆ alquilenilo)-N(Rʲ)C(O)Rᵏ, -(C₁₋₆ alquilenilo)-N(Rʲ)S(O)₂Rᵏ, -(C₁₋₆ alquilenilo)-N(Rʲ)C(O)O(Rᵏ), -(C₁₋₆ alquilenilo)-N(Rʲ)C(O)N(Rʲ)₂, o -(C₁₋₆ alquilenilo)-CN; Rʲ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; y Rᵏ, en cada caso, es en forma independiente C₁₋₆ alquilo o C₁₋₆ haloalquilo.
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