AR110796A2 - Derivados de bencilbenceno - Google Patents

Derivados de bencilbenceno

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AR110796A2
AR110796A2 ARP180100278A ARP180100278A AR110796A2 AR 110796 A2 AR110796 A2 AR 110796A2 AR P180100278 A ARP180100278 A AR P180100278A AR P180100278 A ARP180100278 A AR P180100278A AR 110796 A2 AR110796 A2 AR 110796A2
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Theracos Sub Llc
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    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Vascular Medicine (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto que es de la fórmula (1), en donde V es un miembro seleccionado del grupo formado por oxígeno; azufre; SO; SO₂; y un enlace simple; W es un miembro seleccionado del grupo formado por alquileno C₁₋₆, alquenileno C₂₋₆, alquinileno C₂₋₆, cicloalquileno C₃₋₁₀, cicloalquenileno C₅₋₁₀ y (cicloalquileno C₃₋₁₀)(alquileno C₁₋₆) donde la porción cicloalquileno C₃₋₁₀ se une a V y la porción alquileno C₁₋₆, se une a X, y donde los grupos o porciones alquileno, alquenileno, alquinileno, cicloalquileno y cicloalquenileno opcionalmente están parcial o totalmente fluorados y están opcionalmente mono- o disustituidos con sustituyentes independientemente seleccionados del grupo formado por cloro, hidroxi, alquilo C₁₋₃, alcoxi C₁₋₃, cicloalquilo C₃₋₆, cicloalquiloxi C₃₋₆, cicloalquenilo C₅₋₁₀ o cicloalqueniloxi C₅₋₁₀, y en los grupos o porciones cicloalquileno y cicloalquenileno, uno o dos grupos metileno están opcionalmente reemplazados, independientemente entre sí, por O, S, CO, SO, SO₂ o NRᵇ, y uno o dos grupos metino están opcionalmente reemplazados por N; X es un miembro seleccionado del grupo formado por oxígeno; azufre; SO; o SO₂; Y es un miembro seleccionado del grupo formado por hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₅₋₁₀, (cicloalquil C₃₋₁₀)alquilo C₁₋₄, (cicloalquenil C₅₋₁₀)alquilo C₁₋₃, (cicloalquil C₃₋₁₀)alquenilo C₂₋₄, cicloalquilidenmetilo C₃₋₆, (cicloalquenil C₅₋₁₀)alquenilo C₂₋₄, (alquiloxi C₁₋₄)alquilo C₁₋₃, (alqueniloxi C₂₋₄)alquilo C₁₋₃, (cicloalquiloxi C₃₋₁₀)alquilo C₁₋₃, (cicloalqueniloxi C₅₋₁₀)alquilo C₁₋₃, (amino)alquilo C₁₋₃, (alquilamino C₁₋₄)alquilo C₁₋₃, di-(alquilamino C₁₋₃)alquilo C₁₋₃, (alquil C₁₋₆)carbonilalquilo C₁₋₃, (alquenil C₂₋₆)carbonilalquilo C₁₋₃, (alquinil C₂₋₆)carbonilalquilo C₁₋₃, (arilcarbonil)alquilo C₁₋₃, (heteroarilcarbonil)alquilo C₁₋₃, (alquilsulfonil C₁₋₆)alquilo C₁₋₃, (alquenilsulfonil C₂₋₆)alquilo C₁₋₃, (alquinilsulfonil C₂₋₆)alquilo C₁₋₃, (arilsulfonil)alquilo C₁₋₃, (heteroarilsulfonil)alquilo C₁₋₃, (alquil C₁₋₆)aminocarbonilalquilo C₁₋₃, (alquenil C₂₋₆)aminocarbonilalquilo C₁₋₃, (alquinil C₂₋₆)aminocarbonilalquilo C₁₋₃, (arilaminocarbonil)alquilo C₁₋₃, (heteroarilaminocarbonil)alquilo C₁₋₃, (alquil C₁₋₆)carbonilo, (alquenil C₂₋₆)carbonilo, (alquinil C₂₋₆)carbonilo, arilcarbonilo, heteroarilcarbonilo, (alquil C₁₋₆)sulfonilo, (alquenil C₂₋₆)sulfonilo, (alquinil C₂₋₆)sulfonilo, arilsulfonilo o heteroarilsulfonilo; donde los grupos o porciones alquilo, alquenilo, alquinilo, cicloalquilo y cicloalquenilo opcionalmente están parcial o totalmente fluorados y opcionalmente están mono- o disustituidos con sustituyentes independientemente seleccionados del grupo formado por cloro, hidroxi, alquilo C₁₋₃, alcoxi C₁₋₃, cicloalquilo C₃₋₆, cicloalquiloxi C₃₋₆, cicloalquenilo C₅₋₁₀, cicloalqueniloxi C₅₋₁₀, y NRᵇRᶜ, y en los grupos o porciones cicloalquilo y cicloalquenilo uno o dos grupos metileno están opcionalmente reemplazados, independientemente entre sí, por O, S, CO, SO, SO₂ o NRᵇ, y uno o dos grupos metino están opcionalmente reemplazados por N, donde el heterociclo formado por dicho reemplazo opcional no es heteroarilo, y donde cuando V es un miembro seleccionado del grupo formado por oxígeno, azufre o un enlace simple y W es alquileno C₁₋₆, entonces Y no es hidrógeno, o alquilo C₁₋₆, y cuando V es oxígeno, W es cicloalquileno C₃₋₁₀ y X es oxígeno, entonces Y es diferente de hidrógeno, alquilo C₁₋₆, o trifluorometilo, y cuando V es un enlace simple y W es un miembro seleccionado a partir del grupo formado por alquenileno C₂₋₆, alquinileno C₂₋₆, cicloalquileno C₃₋₁₀ y cicloalquenileno C₅₋₁₀, entonces Y no es hidrógeno, alquilo C₁₋₆ o (cicloalquil C₃₋₁₀)alquilo C₁₋₄; y cuando V es un miembro seleccionado del grupo formado por oxígeno, azufre, SO o SO₂, W es un miembro seleccionado a partir del grupo formado por alquenileno C₂₋₆ o alquinileno C₂₋₆, e Y es un miembro seleccionado a parir del grupo formado por cicloalquilo C₃₋₁₀ o cicloalquenilo C₅₋₁₀, entonces X también puede representar un enlace simple; u opcionalmente X es NRᵃ e Y es un miembro seleccionado a partir del grupo formado por alquilsulfonilo C₁₋₆, alquenilsulfonilo C₂₋₆, alquinilsulfonilo C₂₋₆, arilsulfonilo, heteroarilsulfonilo, alquilsulfinilo C₁₋₆, arilsulfinilo, heteroarilsulfinilo, (alquil C₁₋₆)carbonilo, (alquenil C₂₋₆)carbonilo, (alquinil C₂₋₆)carbonilo, arilcarbonilo, heteroarilcarbonilo, (alquil C₁₋₆)aminocarbonilo, (alquenil C₂₋₆)aminocarbonilo, (alquinil C₂₋₆)aminocarbonilo, arilaminocarbonilo, heteroarilaminocarbonilo, (alquilsulfonil C₁₋₆)alquilo C₁₋₃, (alquenilsulfonil C₂₋₆)alquilo C₁₋₃, (alquinilsulfonil C₂₋₆)alquilo C₁₋₃, (arilsulfonil)alquilo C₁₋₃, (heteroarilsulfonil)alquilo C₁₋₃, (alquilsulfinil C₁₋₆)alquilo C₁₋₃, (arilsulfinil)alquilo C₁₋₃, (heteroarilsulfinil)alquilo C₁₋₃, (alquil C₁₋₆)aminocarbonilalquilo C₁₋₃, (alquenil C₂₋₆)aminocarbonilalquilo C₁₋₃, (alquinil C₂₋₆)aminocarbonilalquilo C₁₋₃, (arilaminocarbonil)alquilo C₁₋₃ o (heteroarilaminocarbonil)alquilo C₁₋₃; donde las porciones alquilo, alquenilo y alquinilo opcionalmente están parcial o totalmente fluoradas, y cuando Rᵃ es un miembro seleccionado del grupo formado por H y (alquil C₁₋₄)carbonilo, entonces Y no es (alquil C₁₋₆)carbonilo ni arilcarbonilo; Z es un miembro seleccionado del grupo formado por oxígeno; azufre; SO; SO₂; 1,1-ciclopropileno; carbonilo; o metileno opcionalmente sustituido con uno a dos sustituyentes independientemente seleccionados entre halo, hidroxi, alquilo C₁₋₆, alcoxi C₁₋₆, cicloalquilo C₃₋₆ y cicloalquiloxi C₃₋₆; R¹, R² y R³ son cada uno miembros independientemente seleccionados del grupo formado por hidrógeno, halo, hidroxi, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₅₋₁₀, alquiloxi C₁₋₆, cicloalquiloxi C₃₋₁₀, ciano y nitro, donde los grupos o porciones alquilo y cicloalquilo están opcionalmente mono- o polisustituidos con flúor, o cuando R¹ y R² están unidos a dos átomos de C adyacentes, R¹ y R² están opcionalmente unidos para formar un puente de alquileno C₃₋₅, alquenileno C₃₋₅ o butadienileno, que opcionalmente está parcial o totalmente fluorado y esta opcionalmente mono- o disustituido con sustituyentes idénticos o diferentes seleccionados entre cloro, hidroxi, alcoxi C₁₋₃ y alquilo C₁₋₃, y en donde uno o dos grupos metileno están opcionalmente reemplazados independientemente entre sí, por O, S, CO, SO, SO₂ o NRᵇ, y en donde uno o dos grupos metino están opcionalmente reemplazados por N; R⁴ y R⁵ son cada uno independientemente miembros seleccionados del grupo formado por hidrógeno, halo, ciano, nitro, hidroxi, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, alquiloxi C₁₋₃ o cicloalquiloxi C₃₋₁₀, donde los grupos o porciones alquilo y cicloalquilo opcionalmente están mono- o polisustituidos con flúor, o cuando R⁴ y R⁵ están unidos a dos átomos de C adyacentes, R⁴ y R⁵ están opcionalmente unidos para formar un puente de alquileno C₃₋₅, alquenileno C₃₋₅ o butadienileno, que opcionalmente está parcial o totalmente fluorado y opcionalmente está mono- o disustituido con sustituyentes idénticos o diferentes seleccionados entre cloro, hidroxi, alcoxi C₁₋₆ y alquilo C₁₋₆, y donde uno o dos grupos metileno están opcionalmente reemplazados independientemente entre sí, por O, S, CO, SO, SO₂ o NRᵇ, y en donde uno o dos grupos metino están opcionalmente reemplazados por N; R⁶, R⁷, R⁸ y R⁹ son cada uno miembros independientemente seleccionados del grupo formado por hidroxi, (alquil C₁₋₁₈)carboniloxi, (alquil C₁₋₁₈)oxicarboniloxi, arilcarboniloxi, aril-(alquil C₁₋₃)carboniloxi, (cicloalquil C₃₋₁₀)carboniloxi, hidrógeno, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquil C₃₋₁₀-alquilo C₁₋₃, cicloalquenil C₅₋₇-alquilo C₁₋₃, arilalquilo C₁₋₃, heteroaril-alquilo C₁₋₃, alquiloxi C₁₋₆, alqueniloxi C₂₋₆, alquiniloxi C₂₋₆, cicloalquiloxi C₃₋₇, cicloalqueniloxi C₅₋₇, ariloxi, heteroariloxi, cicloalquil C₃₋₇-alquiloxi C₁₋₃, cicloalquenil C₅₋₇-alquiloxi C₁₋₃, aril-alquiloxi C₁₋₃, heteroaril-alquiloxi C₁₋₃, aminocarbonilo, hidroxicarbonilo, (alquil C₁₋₄)aminocarbonilo, di-(alquil C₁₋₃)aminocarbonilo, (alquiloxi C₁₋₄)carbonilo, aminocarbonil-alquilo C₁₋₃, (alquil C₁₋₄)aminocarbonil-alquilo C₁₋₃, di-(alquil C₁₋₃)aminocarbonil-alquilo C₁₋₃, hidroxicarbonil-alquilo C₁₋₃, (alquiloxi C₁₋₄)carbonil-alquilo C₁₋₃, cicloalquiloxi C₃₋₇-alquilo C₁₋₃, cicloalqueniloxi C₅₋₇-alquilo C₁₋₃, ariloxi-alquilo C₁₋₃, heteroariloxi-alquilo C₁₋₃, alquilsulfoniloxi C₁₋₄, arilsulfoniloxi, aril-alquil C₁₋₃-sulfoniloxi, trimetilsililoxi, t-butildimetilsililoxi, o ciano; donde los grupos o porciones alquilo, alquenilo, alquinilo, cicloalquilo y cicloalquenilo opcionalmente están parcial o totalmente fluorados y opcionalmente están mono- o disustituidos con sustituyentes independientemente seleccionados entre cloro, hidroxi, alcoxi C₁₋₃ y alquilo C₁₋₃, y en los grupos o porciones cicloalquilo y cicloalquenilo uno o dos grupos metileno están opcionalmente reemplazados independientemente entre sí, por NRᵇ, O, S, CO, SO o SO₂, y cuando Y es hidrógeno o alquilo C₁₋₆, entonces R⁸ y R⁹ son hidroxi; cada Rᵃ es un miembro independientemente seleccionado del grupo formado por H, alquilo C₁₋₆, cicloalquilo C₃₋₆ o (alquil C₁₋₄)carbonilo, donde los grupos o porciones alquilo y cicloalquilo opcionalmente están parcial o totalmente fluorados; cada Rᵇ es un miembro independientemente seleccionado del grupo formado por H, alquilo C₁₋₄ o (alquil C₁₋₄)carbonilo, donde los grupos o porciones alquilo opcionalmente están parcial o totalmente fluorados; cada Rᶜ es un miembro independientemente seleccionado del grupo formado por H, alquilo C₁₋₄, cicloalquilo C₃₋₆, CHRᵈRᵉ, SO₂Rᵈ, C(O)ORᵈ o C(O)NRᵈRᵉ, en donde los grupos alquilo y cicloalquilo opcionalmente están parcial o totalmente fluorados; y Rᵈ y Rᵉ cada uno independientemente representan H o alquilo C₁₋₆, en donde los grupos alquilo opcionalmente están parcial o totalmente fluorados; y sales farmacéuticamente aceptables del mismo.
ARP180100278A 2007-08-23 2018-02-06 Derivados de bencilbenceno AR110796A2 (es)

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