AR074755A1 - QUATERNARY DERIVATIVES OF PIPERIDINE AND ITS USES - Google Patents

QUATERNARY DERIVATIVES OF PIPERIDINE AND ITS USES

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Publication number
AR074755A1
AR074755A1 ARP090104875A ARP090104875A AR074755A1 AR 074755 A1 AR074755 A1 AR 074755A1 AR P090104875 A ARP090104875 A AR P090104875A AR P090104875 A ARP090104875 A AR P090104875A AR 074755 A1 AR074755 A1 AR 074755A1
Authority
AR
Argentina
Prior art keywords
nr7r8
alkyl
compounds
nr7c
attached
Prior art date
Application number
ARP090104875A
Other languages
Spanish (es)
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Astrazeneca Ab
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.)
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Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR074755A1 publication Critical patent/AR074755A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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 singly bound oxygen or sulphur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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 singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic 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 singly bound oxygen or sulphur atoms by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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 singly bound oxygen or sulphur atoms
    • C07D211/24Heterocyclic 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 singly bound oxygen or sulphur atoms by sulfur atoms to which a second hetero atom is attached
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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
    • C07D211/28Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/34Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se refiere en general a compuestos de piperidina cuaternarios, en particular a compuestos de 3-fenilpiperidina sustituidos y sales de dichos compuestos, a composiciones farmacéuticas que comprenden dichos compuestos, a usos de dichos compuestos en trastornos depresivos, deficit de atención, conducta disruptiva y trastornos relacionados con la cocaína. Reivindicación 1: Un compuesto de fórmula 1 o una sal farmacéuticamente aceptable de dicho compuesto, donde: fórmula (1); R1 y R2 se seleccionan, cada uno independientemente, de halógeno; como a R3 y R4: R3 y R4 se seleccionan, cada uno independientemente, de H, -OH y alquiIoC1-3, o R3 y R4, junto con el carbono al cual están ambos unidos, forman cicloalquiloC3-6; R5 se selecciona de -CN, -CF3, -alqueniloC2-6, -OR7, S(=O)R6, -S(=O)R6, -SR6, -S(=O)2NR7R8, -C(=O)NR7R8, -NR7C(=O)R12, -NR7R8, -NR7C(=O)OR8, -NR7S(=O)2R9, -NR7(C=O)NR7R8 y -O(C=O)NR7R8; R6 es alquiloC1-6; como a R7 y R8; R7 y R8 se seleccionan, cada uno independientemente, de H y alquiloC1-6, donde: el alquiloC1-6 está opcionalmente sustituido con 1 o 2 sustituyentes seleccionados de haloalquilo, alquiloC1-3, -C(=O)NR10R11, -OH, -CN y alcoxiC1-3, o cuando R5 es -C(=O)NR7R8, -NR7R8, -NR7C(=O)OR8 o -S(=O)2NR7R8, R7 y R8, junto con los átomos a los cuales están ambos unidos, pueden formar un heterocicloalquilo de 3, 4, 5 o 6 miembros, donde: el heterocicloalquilo de 3, 4, 5 o 6 miembros opcionalmente contiene al menos un heteroátomo anular seleccionado de O y N además de: el N al cual ambos R7 y R8 están unidos, donde R5 es -C(=O)NR7R8, -NR7R8 o -S(=O)2NR7R8, o el N al cual R7 está unido y el O al cual R8 está unido, donde R5 es -NR7C(=O)OR8; R9 se selecciona de H, alquiloC1-6, -NR7R8 y haloalquilo; R10 y R11 se seleccionan, cada uno independientemente, de H y aIquiloC1-6; R12 se selecciona de H, alquiloC1-6 y haloalquilo; n se selecciona de 0 y 1; p se selecciona de 0, 1, 2 y 3; p no es 0 cuando R5 es -OR7; y el compuesto de fórmula (1) no es 2-(3-(3,4-dicIorofenil)piperidin-3-il)etanol.It refers generally to quaternary piperidine compounds, in particular to substituted 3-phenylpiperidine compounds and salts of said compounds, to pharmaceutical compositions comprising said compounds, to uses of said compounds in depressive disorders, attention deficit, disruptive behavior and disorders Cocaine related. Claim 1: A compound of formula 1 or a pharmaceutically acceptable salt of said compound, wherein: formula (1); R1 and R2 are each independently selected from halogen; as at R3 and R4: R3 and R4 are each independently selected from H, -OH and C1-3 alkyl, or R3 and R4, together with the carbon to which they are both attached, form C3-6 cycloalkyl; R5 is selected from -CN, -CF3, -C2-6 alkenyl, -OR7, S (= O) R6, -S (= O) R6, -SR6, -S (= O) 2NR7R8, -C (= O) NR7R8, -NR7C (= O) R12, -NR7R8, -NR7C (= O) OR8, -NR7S (= O) 2R9, -NR7 (C = O) NR7R8 and -O (C = O) NR7R8; R6 is C1-6 alkyl; as to R7 and R8; R7 and R8 are each independently selected from H and C1-6 alkyl, where: C1-6 alkyl is optionally substituted with 1 or 2 substituents selected from haloalkyl, C1-3 alkyl, -C (= O) NR10R11, -OH, -CN and C1-3 alkoxy, or when R5 is -C (= O) NR7R8, -NR7R8, -NR7C (= O) OR8 or -S (= O) 2NR7R8, R7 and R8, together with the atoms to which they are both together, they can form a 3, 4, 5 or 6-membered heterocycloalkyl, where: the 3, 4, 5 or 6-membered heterocycloalkyl optionally contains at least one annular heteroatom selected from O and N in addition to: the N to which both R7 and R8 are attached, where R5 is -C (= O) NR7R8, -NR7R8 or -S (= O) 2NR7R8, or the N to which R7 is attached and the O to which R8 is attached, where R5 is -NR7C (= O) OR8; R9 is selected from H, C1-6 alkyl, -NR7R8 and haloalkyl; R10 and R11 are each independently selected from H and C1-6 alkyl; R12 is selected from H, C1-6 alkyl and haloalkyl; n is selected from 0 and 1; p is selected from 0, 1, 2 and 3; p is not 0 when R5 is -OR7; and the compound of formula (1) is not 2- (3- (3,4-dicIorophenyl) piperidin-3-yl) ethanol.

ARP090104875A 2008-12-16 2009-12-15 QUATERNARY DERIVATIVES OF PIPERIDINE AND ITS USES AR074755A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12291208P 2008-12-16 2008-12-16
US22638909P 2009-07-17 2009-07-17
US22907309P 2009-07-28 2009-07-28

Publications (1)

Publication Number Publication Date
AR074755A1 true AR074755A1 (en) 2011-02-09

Family

ID=42269030

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104875A AR074755A1 (en) 2008-12-16 2009-12-15 QUATERNARY DERIVATIVES OF PIPERIDINE AND ITS USES

Country Status (4)

Country Link
AR (1) AR074755A1 (en)
TW (1) TW201026666A (en)
UY (1) UY32333A (en)
WO (1) WO2010071575A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011075470A1 (en) * 2009-12-15 2011-06-23 Astrazeneca Pharmaceuticals Lp Quaternary piperidine compounds and uses thereof
CN105017244A (en) * 2014-04-16 2015-11-04 上海药明康德新药开发有限公司 Cis/trans-tert-butyl-4-O-hexahydro-1H-pyrrole[3,4-c]pyridine-2(3H)-tert-butyl carboxylate synthesis method
CN116462607B (en) * 2023-02-06 2024-09-03 中山大学 Cyano compound and preparation method and application thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5607939A (en) * 1994-04-28 1997-03-04 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use
GB9600235D0 (en) * 1996-01-05 1996-03-06 Pfizer Ltd Therapeutic agents
GB9601202D0 (en) * 1996-01-22 1996-03-20 Pfizer Ltd Piperidones
SE0401465D0 (en) * 2004-06-08 2004-06-08 Carlsson A Research Ab New substituted piperdines as modulators of dopamine neurotransmission
MX2009012787A (en) * 2007-06-05 2009-12-15 Nsab Af Neurosearch Sweden Ab Disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission.

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Publication number Publication date
TW201026666A (en) 2010-07-16
WO2010071575A1 (en) 2010-06-24
UY32333A (en) 2010-07-30

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