AR105893A1 - Derivados del anillo (hetero) aromático sustituidos con carboxi como inhibidores de xantina oxidasa y del transportador 1 del anión urato - Google Patents

Derivados del anillo (hetero) aromático sustituidos con carboxi como inhibidores de xantina oxidasa y del transportador 1 del anión urato

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Publication number
AR105893A1
AR105893A1 ARP160102677A ARP160102677A AR105893A1 AR 105893 A1 AR105893 A1 AR 105893A1 AR P160102677 A ARP160102677 A AR P160102677A AR P160102677 A ARP160102677 A AR P160102677A AR 105893 A1 AR105893 A1 AR 105893A1
Authority
AR
Argentina
Prior art keywords
alkyl
haloalkyl
amino
membered
independently
Prior art date
Application number
ARP160102677A
Other languages
English (en)
Inventor
Zhang Yingjun
Wang Xiaojun
Zhang Ji
Ma Facheng
Huang Changwei
Yang Xinye
Original Assignee
Sunshine Lake Pharma Co Ltd
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 Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Publication of AR105893A1 publication Critical patent/AR105893A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
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    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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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
    • A61K31/437—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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Derivados de (hetero) arilo sustituidos con carboxi y composiciones farmacéuticas que comprenden estos compuestos. Los compuestos o composiciones farmacéuticas son de utilidad en la inhibición de xantina oxidasa y transportador 1 del anión urato. Composiciones farmacéuticas, así como usos de tales compuestos y composiciones farmacéuticas en el tratamiento o la prevención de enfermedades asociadas con un alto nivel de ácido úrico en sangre en mamíferos, en especial seres humanos. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) o uno de sus estereoisómeros, isómeros geométricos, tautómeros, N-óxidos, hidratos, solvatos, metabolitos, ésteres, sales farmacéuticamente aceptables o profármacos, en donde: U es fenilo o heteroarilo de 5 a 6 miembros; cada R¹ y R² es, de modo independiente, H, D, halógeno, OH, NH₂, NO₂, CN, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquil C₁₋₆-amino, haloalquil C₁₋₆-amino, cicloalquilo de 3 a 8 miembros o heterociclilo de 3 a 8 miembros, en donde cada uno del alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquil C₁₋₆-amino, haloalquil C₁₋₆-amino, cicloalquilo de 3 a 8 miembros o heterociclilo de 3 a 8 miembros es, de modo independiente, y está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados de OH, oxo (=O), NH₂, NO₂ o CN; T es H, D, F, Cl, Br, NO₂, CN o CF₃; X es CR⁴ o N; R⁴ es H, D, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, alquil C₁₋₆-amino o haloalcoxi C₁₋₆; cada uno de Y y Z es, de modo independiente, C, CH o N; “⁻ ⁻ ⁻ ⁻ ⁻” se refiere a un enlace simple o un enlace doble; Q es feno, carbociclo C₄₋₇, heterociclo de 4 a 7 miembros o anillo heteroaromático de 5 a 6 miembros; cada R³ es, de modo independiente, H, D, halógeno, oxo (=O), OH, NH₂, NO₂, CN, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquil C₁₋₆-amino, haloalquil C₁₋₆-amino, cicloalquilo de 3 a 8 miembros, heterociclilo de 3 a 8 miembros, heteroarilo de 5 a 10 miembros, fenilo, naftilo o G, en donde cada uno del alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquil C₁₋₆-amino, haloalquil C₁₋₆-amino, cicloalquilo de 3 a 8 miembros, heterociclilo de 3 a 8 miembros o heteroarilo de 5 a 10 miembros es, de modo independiente, y está opcionalmente sustituido con 1, 2, 3, 4 ó 5 sustituyentes seleccionados de OH, oxo (=O), NH₂, NO₂, CN o G; G es hidrocarburo alifático C₁₋₆ sustituido, en donde cada uno de los grupos de metileno del hidrocarburo alifático C₁₋₆ está sustituido, de modo opcional e independiente, con J; J es -NH-, -S-, -O-, -C(=O)-, -C(=O)NH-, -SO-, -SO₂-, -NHC(=O)-, -C(=O)O-, -SO₂NH- o NHC(=O)NH; m es 0, 1, 2 ó 3; y n es 0, 1, 2, 3 ó 4; con la condición de que: (i) cuando T es F, Cl, Br o CF₃, R¹ sea OH; (ii) cuando T es H, el resto de fórmula (2) sea de fórmula (3) y Q no sea feno; (iii) cuando T es NO₂, R¹ no sea H.
ARP160102677A 2015-09-02 2016-09-01 Derivados del anillo (hetero) aromático sustituidos con carboxi como inhibidores de xantina oxidasa y del transportador 1 del anión urato AR105893A1 (es)

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