ES2606137T3 - Derivados de aminas espirocíclicas como moduladores de S1P - Google Patents

Derivados de aminas espirocíclicas como moduladores de S1P Download PDF

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Publication number
ES2606137T3
ES2606137T3 ES11730314.9T ES11730314T ES2606137T3 ES 2606137 T3 ES2606137 T3 ES 2606137T3 ES 11730314 T ES11730314 T ES 11730314T ES 2606137 T3 ES2606137 T3 ES 2606137T3
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optionally substituted
alkyl
halogen
substituted
fluoro atoms
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Axel Stoit
Wouter I. Iwema Bakker
Hein K.A.C. Coolen
Maria J.P. Van Dongen
Nicolas J.-L.D. Leflemme
Adrian D. Hobson
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AbbVie BV
AbbVie Inc
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AbbVie Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4427—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Abstract

Un derivado de amina espiro-cíclica de la fórmula (I)**Fórmula** en donde R1 se selecciona de ciano, (2-4C)alquenilo, (2-4C)alquinilo, (1-4C)alquilo cada uno opcionalmente sustituido con CN o uno o más átomos de fluoro, (3-6C)cicloalquilo, (4-6C)cicloalquenilo o un grupo (8-10C)bicíclico, cada uno opcionalmente sustituido con halógeno o (1-4C)alquilo, fenilo, bifenilo, naftilo, cada uno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, ciano, (1-6C)alquilo opcionalmente sustituido con uno o más átomos de fluoro, (1-6C)alcoxi opcionalmente sustituido con uno o más átomos de fluoro, amino, di(1-4C)alquilamino y (3- 6C)cicloalquilo opcionalmente sustituido con fenilo que puede estar sustituido con (1-4C)alquilo o halógeno, fenilo sustituido con fenoxi, bencilo, benciloxi, feniletilo o heterociclo monocíclico, cada uno opcionalmente sustituido con (1-4C)alquilo opcionalmente sustituido con uno o más átomos de fluoro, heterociclo monocíclico opcionalmente independientemente sustituido con halógeno, (1-6C)alquilo opcionalmente sustituido con uno o más átomos de fluoro, (3-6C)cicloalquilo, o fenilo opcionalmente sustituido con (1-4C)alquilo o halógeno, y heterociclo bicíclico opcionalmente sustituido con halógeno o (1-4C)alquilo opcionalmente sustituido con uno o más átomos de fluoro; -Y-(Cn-alquilen)-X- es un grupo enlazante en donde Y está unido a R1 y seleccionado de un enlace, -O-, -CO-, -S-, -SO-, -SO2-, -NH-, -CH>=CH-, -C(CF3)>=CH-, - C≡C-, -CH2-O-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, y trans-ciclopropileno; n es un entero de 0 a 10; y X está unido a la unidad estructural fenileno/piridilo y seleccionado de un enlace, -O-, -S-, -SO-,-SO2-, -NH-, - CO-, -CH>=CH-, y trans-ciclopropileno; R2 es H o seleccionados independientemente de uno o más sustituyentes seleccionados de halógeno, (1-4C)alcoxi y (1-4C)alquilo opcionalmente sustituido con uno o más átomos de flúor; y R3 es (1-4C)alquilen-R4 en donde el grupo alquileno puede estar sustituido con uno o más átomos de halógeno o con (CH2)2 para formar una unidad estructural ciclopropilo, o R3 es (3-6C)cicloalquilen-R4, -CH2-(3- 6C)cicloalquilen-R4, (3-6C)cicloalquilen-CH2-R4 o -CO-CH2-R4, en donde R4 es -PO3H2, -OPO3H2, -COOH, - COO(1-4C)alquilo o tetrazol-5-ilo; Q es un enlace; -W-T- se selecciona de -CH>=CH-, -O-CH2-CH2-, -CO-O-, -CH2-CH2-, -CH2-O- y -O-CH2-; R5 es H o independientemente seleccionado de uno o más halógenos; Z es CH, CR2 o N; y A representa una estructura de anillo de morfolina o una amina cíclica de 5, 6 o 7 miembros; o una sal, un solvato o hidrato farmacéuticamente aceptable del mismo o uno o más N-óxidos del mismo
ES11730314.9T 2010-07-09 2011-07-08 Derivados de aminas espirocíclicas como moduladores de S1P Active ES2606137T3 (es)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US36278210P 2010-07-09 2010-07-09
EP10169104 2010-07-09
EP10169104 2010-07-09
US362782P 2010-07-09
US201161444186P 2011-02-18 2011-02-18
US201161444186P 2011-02-18
EP11154961 2011-02-18
EP11154961 2011-02-18
PCT/EP2011/061599 WO2012004378A1 (en) 2010-07-09 2011-07-08 Spiro-cyclic amine derivatives as s1p modulators

Publications (1)

Publication Number Publication Date
ES2606137T3 true ES2606137T3 (es) 2017-03-22

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ES11730314.9T Active ES2606137T3 (es) 2010-07-09 2011-07-08 Derivados de aminas espirocíclicas como moduladores de S1P

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US (4) US10179791B2 (es)
EP (2) EP3144312A1 (es)
JP (1) JP5922115B2 (es)
KR (1) KR101889695B1 (es)
CN (1) CN103097364B (es)
AR (1) AR082135A1 (es)
AU (1) AU2011275760B2 (es)
BR (1) BR112013000629B1 (es)
CA (1) CA2804143C (es)
DK (1) DK2590955T3 (es)
ES (1) ES2606137T3 (es)
HK (1) HK1184153A1 (es)
IL (1) IL224049B (es)
MX (1) MX347423B (es)
NZ (1) NZ605486A (es)
PL (1) PL2590955T3 (es)
PT (1) PT2590955T (es)
RU (2) RU2016140266A (es)
SG (1) SG186926A1 (es)
TW (2) TW201643169A (es)
UY (1) UY33497A (es)
WO (1) WO2012004378A1 (es)
ZA (1) ZA201300153B (es)

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