AR114421A1 - Piperidinil-3-(ariloxi)-propanamidas y propanoatos - Google Patents

Piperidinil-3-(ariloxi)-propanamidas y propanoatos

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Publication number
AR114421A1
AR114421A1 ARP190100507A ARP190100507A AR114421A1 AR 114421 A1 AR114421 A1 AR 114421A1 AR P190100507 A ARP190100507 A AR P190100507A AR P190100507 A ARP190100507 A AR P190100507A AR 114421 A1 AR114421 A1 AR 114421A1
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Argentina
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halo
independently selected
alkyl
substituted
optional substituents
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ARP190100507A
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Takeda Pharmaceuticals Co
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Publication of AR114421A1 publication Critical patent/AR114421A1/es

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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • A61K31/40Heterocyclic 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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    • A61K31/4353Heterocyclic 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
    • A61K31/4355Heterocyclic 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 oxygen as a ring hetero atom
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    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61K31/33Heterocyclic compounds
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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 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
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
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    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Abstract

Se describen compuestos de fórmula (1), estereoisómeros de estos, y sales farmacéuticamente aceptables de estos, donde L, r, s, R⁵, R⁶, R⁷, R⁹, R¹⁰, R¹¹, R¹², X¹, X², X³, X⁴, X¹³, y X¹⁴ se definen en la memoria descriptiva. Esta descripción también se refiere a materiales y métodos para preparar compuestos de fórmula (1), a composiciones farmacéuticas que los contienen, y a su uso para tratar enfermedades, trastornos y afecciones asociados con SSTR4. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable este donde: X¹ se selecciona de N y CR¹; X² se selecciona de N y CR²; X³ se selecciona de N y CR³; y X⁴ se selecciona de N y CR⁴, con la condición de que no más de dos de X¹, X², X³, y X⁴ sean N; X¹³ es NR¹³ y X¹⁴ es CR¹⁵R¹⁶ o X¹³ es CH₂ y X¹⁴ es NR¹⁴; L se selecciona de NR⁸ y O; r se selecciona de 0 y 1; s se selecciona de 0 y 1; R¹, R² y R³ se seleccionan independientemente de (a) hidrógeno, halo, hidroxi y ciano; y (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; R⁴ se selecciona de (a) hidrógeno, halo, hidroxi y ciano; y (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; R⁵ se selecciona de (a) hidrógeno, halo, hidroxi y ciano; y (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, oxo y fenilo que está sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; o R⁴ y R⁵, junto con el átomo de carbono al que están unidos, forman un ciclopent-1-en-1,2-diilo o un furan-2,3-diilo; cada R⁶ y R⁷ se selecciona independientemente halo y alquilo C₁₋₃, o R⁶ y R⁷, junto con el átomo de carbono al que están unidos, forman un cicloalcan-C₃₋₄-1,1-diilo; R⁸ se selecciona de H y alquilo C₁₋₄; R⁹ y R¹⁰ se seleccionan cada uno independientemente de (a) hidrógeno, halo, hidroxi y ciano; (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; y (c) fenilo y heteroarilo C₁₋₅, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, alquilo C₁₋₄ y alcoxi C₁₋₄, donde el sustituyente de C₁₋₅ heteroarilo es un anillo monocíclico con 5 a 6 miembros del anillo donde 1 a 4 miembros del anillo son heteroátomos, cada uno de los heteroátomos se selecciona independientemente de N, O y S, con la condición de que no más de uno de los miembros del anillo sea O ó S y donde cada uno de los sustituyentes opcionales alquilo C₁₋₄ y alcoxi C₁₋₄ de fenilo y heteroarilo C₁₋₅ está sustituido independientemente con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; o R⁹ y R¹⁰, junto con el átomo de carbono al que están unidos, forman un grupo cicloalcan-C₃₋₄-1,1-diilo; R¹¹ y R¹² se seleccionan cada uno independientemente de (a) hidrógeno, halo, hidroxi y ciano; y (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; o R¹¹ y R¹², junto con el átomo de carbono al que están unidos, forman un grupo cicloalcan-C₃₋₄-1,1-diilo; R¹³ y R¹⁴ se seleccionan cada uno independientemente de (a) hidrógeno, y (b) alquilo C₁₋₄, que está sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de ciano, oxo y fenilo que está sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; y R¹⁵ y R¹⁶ se seleccionan cada uno independientemente de (a) hidrógeno, halo, hidroxi y ciano; y (b) alquilo C₁₋₄, cicloalquilo C₃₋₆ y alcoxi C₁₋₄, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; o R¹⁵ y R¹⁶, junto con el átomo de carbono al que están unidos, forman un grupo cicloalcan-C₃₋₄-1,1-diilo.
ARP190100507A 2018-03-01 2019-02-28 Piperidinil-3-(ariloxi)-propanamidas y propanoatos AR114421A1 (es)

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