AR087853A1 - Inhibidores del canal de potasio medular externo renal - Google Patents

Inhibidores del canal de potasio medular externo renal

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AR087853A1
AR087853A1 ARP120103364A ARP120103364A AR087853A1 AR 087853 A1 AR087853 A1 AR 087853A1 AR P120103364 A ARP120103364 A AR P120103364A AR P120103364 A ARP120103364 A AR P120103364A AR 087853 A1 AR087853 A1 AR 087853A1
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alkyl
carbon atoms
ring
cycloalkyl
attached
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Merck Sharp & Dohme
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C07D211/28—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/48—Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Urology & Nephrology (AREA)
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Abstract

La presente se refiere a los compuestos que tienen la fórmula estructural (1) y a las sales farmacéuticamente aceptables de los mismos que son inhibidores del canal (Kir1,1) de Potasio Medular Externo Renal (ROMK). Los compuestos de fórmula (1) actúan como diuréticos y natriuréticos y por lo tanto son útiles para la terapia y la profilaxis de los trastornos que resultan de una retención excesiva de sal y de agua, que incluye las enfermedades cardiovasculares tales como la hipertensión y el fallo cardíaco crónico y agudo. Reivindicación 1: Un compuesto que tiene la fórmula (1) estructural, o una sal farmacéuticamente aceptable del mismo, en la que: B¹-ZB- es B¹-CHR¹CH₂-, B¹-CHR¹C(O)-, B¹-C(O)-, B¹-CHR¹CH₂C(O)-, B¹-OCH₂C(O)- o B¹-CH(CH₂OH)-; ZA-A¹ es -CHR²¹CR²R²²-A¹, -CH=CR²-A¹, -CºC-A¹, -S-A¹, -CH₂O-A¹, -C(O)CHR²-A¹, -O-A¹, -NHCHR²-A¹, -CH₂N(CH₃)CH₂CH(OH)-A¹, -CH₂N(CH₃)CH(CH₂OH)-A¹, -CH₂N(CH₃)-A¹, -CH₂S-A¹, -CH₂O-A¹, CH₂S(O)-A¹, -CH₂S(O₂)-A¹ o -NH-A¹; A¹ es un compuesto seleccionado del grupo de formulas (2); B¹ es un compuesto del grupo de formulas (3); X es O ó S; R¹ es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, CF₃, -OH, F, -CH₂OH, -C(O)OH, -C(O)O-alquilo C₁₋₆ o R¹ se puede unir a R¹³ᵇ mediante 2 - 3 átomos de carbono ó 1 - 2 átomos de carbono y un heteroátomo para formar un anillo; R² es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, CF₃, -OH, F, -CH₂OH, -C(O)OH, -C(O)O-alquilo C₁₋₆ ó R² se puede unir a R¹³ᵃ mediante 2 - 3 átomos de carbono ó 1 - 2 átomos de carbono y un heteroátomo para formar un anillo; R⁴ es H, -OH, F, -O-alquilo C₁₋₆ ó alquilo C₁₋₆ o se puede unir a R⁵ mediante un enlace o mediante 1 - 4 átomos de carbono, para formar un anillo; R⁵ es H, -OH, F, -O-alquilo C₁₋₆ o alquilo C₁₋₆ o se puede unir a R⁴ mediante un enlace o mediante 1 - 4 átomos de carbono para formar un anillo; R⁶ es -H, alquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, -OH, halógeno, -OC(O)alquilo C₁₋₆, -CH₂OH, -CHF₂, -N(alquilo C₁₋₆)₂, -C₆H₅, -CF₃ o un anillo heteroarilo de 5 ó 6 miembros con 1, 2, 3 ó 4 heteroátomos; R¹³ᵃ es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, -halógeno, CF₃, -CH₂OH, CO₂R¹⁶ᵃ, -OR¹⁶ᵃ, -SR¹⁶ᵃ, -CN, -arilo, -heterociclo, -NR¹⁶ᵃR¹⁸ᵃ ó R¹³ᵃ se puede unir a R² mediante 2 - 3 átomos de carbono ó 1 - 2 átomos de carbono y un heteroátomo para formar un anillo ó R¹³ᵃ se puede unir a R¹⁴ᵃ mediante 3 - 4 átomos de carbono ó 2 - 3 átomos de carbono y un heteroátomo para formar un anillo; R¹³ᵇ es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, -halógeno, CF₃, -CH₂OH, CO₂R¹⁶ᵇ, -OR¹⁶ᵇ, -SR¹⁶ᵇ, -CN, -arilo, -heterociclo, -NR¹⁶ᵇR¹⁸ᵇ o R¹³ᵇ se puede unir a R¹ mediante 2 - 3 átomos de carbono ó 1 - 2 átomos de carbono y un heteroátomo para formar un anillo ó R¹³ᵇ se puede unir a R¹⁴ᵇ mediante 3 - 4 átomos de carbono ó 2 - 3 átomos de carbono y un heteroátomo para formar un anillo; R¹⁴ᵃ es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, -halógeno, CF₃, -CH₂OH, CO₂R¹⁷ᵃ, -OR¹⁷ᵃ, -SR¹⁷ᵃ, CN, -arilo, -heterociclo ó R¹⁴ᵃ se puede unir a R¹³ᵃ mediante 3 - 4 átomos de carbono ó 2 - 3 átomos de carbono y un heteroátomo para formar un anillo; R¹⁴ᵇ es -H, alquilo C₁₋₆, cicloalquilo C₃₋₆, -halógeno, CF₃, -CH₂OH, -CO₂R¹⁷ᵇ, -OR¹⁷ᵇ, -SR¹⁷ᵇ, -CN, -arilo, -heterociclo ó R¹⁴ᵇ se puede unir a R¹³ᵇ mediante 3 - 4 átomos de carbono ó 2 - 3 átomos de carbono y un heteroátomo para formar un anillo; R¹⁵ᵃ es -H, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, alquilo -O-C₁₋₆ ó -CF₃; R¹⁵ᵇ es -H, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, alquilo -O-C₁₋₆ ó -CF₃; R¹⁶ᵃ, R¹⁶ᵇ, R¹⁷ᵃ, R¹⁷ᵇ, R¹⁸ᵃ y R¹⁸ᵇ son independientemente -H, alquilo C₁₋₆, cicloalquilo C₃₋₆; R¹⁹ y R²⁰ son H o se pueden unir mediante un enlace ó 1 - 2 átomos de carbono para formar un anillo de 4 - 5 miembros; y R²¹ y R²² son H o, junto con un átomo de carbono al que se unen, forman un cicloalquilo C₃₋₆.
ARP120103364A 2011-09-16 2012-09-13 Inhibidores del canal de potasio medular externo renal AR087853A1 (es)

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EP (1) EP2755656B1 (es)
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