AR053832A1 - Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension - Google Patents

Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension

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Publication number
AR053832A1
AR053832A1 ARP060101103A ARP060101103A AR053832A1 AR 053832 A1 AR053832 A1 AR 053832A1 AR P060101103 A ARP060101103 A AR P060101103A AR P060101103 A ARP060101103 A AR P060101103A AR 053832 A1 AR053832 A1 AR 053832A1
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AR
Argentina
Prior art keywords
unsubstituted
substituted
mono
cyclic
alkyl
Prior art date
Application number
ARP060101103A
Other languages
English (en)
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR053832A1 publication Critical patent/AR053832A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • A61K31/33—Heterocyclic compounds
    • 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
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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/341—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 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
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    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—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
    • A61K31/351—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 not condensed with another ring
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    • A61K31/35—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
    • 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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    • A61K31/357—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
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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
    • A61K31/4025—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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    • A61K31/403—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
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    • 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
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    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
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Abstract

Se refiere al uso de compuestos de pirrolidina (3,4-di-, 3,3,4-tri-, 3,4,4-tri-, o 3,3,4,4-tetra-)-sustituidos, para la preparacion de una formulacion farmacéutica para el tratamiento de una enfermedad que dependa de la actividad de la renina; al uso de un compuesto de esta clase en el tratamiento de una enfermedad que dependa de la actividad de la renina; a compuestos que son parte de una sub-clase de estos compuestos de pirrolidina sustituida para utilizarse en el diagnostico y en el tratamiento terapéutico de un animal de sangre caliente, en especial para el tratamiento de una enfermedad (= trastorno) que dependa de la actividad de la renina; a compuestos que son parte de una sub-clase de estos compuestos de pirrolidina sustituida; a formulaciones farmacéuticas que comprenden a estos compuestos de pirrolidina sustituida, y/o a un método de tratamiento que comprende administrar estos compuestos de pirrolidina sustituida, a un método para la fabricacion en especial de estos compuestos de pirrolidina sustituida, así como a intermediarios, materiales de partida, y/o pasos parciales para su síntesis. Reivindicacion 1: El uso de un compuesto de la formula (1) en donde: R1 es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, o acilo; R2 es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, o acilo; R3 es una fraccion seleccionada a partir del grupo de fracciones de las formulas (a) a (g) en donde, en cualquiera de las fracciones de las formulas dadas anteriormente baja (a) a (g), el asterisco (*) muestra un enlace que enlaza a la fraccion R3 respectiva con el resto de la molécula en la formula (1); Ra es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, acilo, o H; Rb y Rc se seleccionan independientemente a partir de las fracciones dadas en Ra, con la condicion de que de preferencia no más de uno de Rb y Rc sea acilo; Rb y Rc pueden formar juntos un anillo de 3 a 7 miembros que contenga N, el cual puede estar insustituido o sustituido; Rd es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, o acilo, o puede tener uno de estos significados, o puede ser -N(Rb(Rc) si m es 1 o de preferencia 2; Re es H, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, o alquilo C1-7 sustituido o de preferencia insustituido; y Rf es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi- cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido; m es 0, 1 o 2; cada uno de R4 y R5 se selecciona, independientemente uno del otro, a partir de H, alquilo insustituido o sustituido, hidroxilo, o hidroxilo esterificado o eterificado; y T es metileno, metileno mono- sustituido por alquilo, o es carbonilo o tio-carbonilo; o una sal farmacéuticamente aceptable del mismo, en la preparacion de una formulacion farmacéutica para el tratamiento de una enfermedad que dependa de la actividad de la renina.
ARP060101103A 2005-03-23 2006-03-21 Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension AR053832A1 (es)

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