AR082135A1 - Derivados de espiro-piperidina como moduladores s1p - Google Patents

Derivados de espiro-piperidina como moduladores s1p

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Publication number
AR082135A1
AR082135A1 ARP110102454A ARP110102454A AR082135A1 AR 082135 A1 AR082135 A1 AR 082135A1 AR P110102454 A ARP110102454 A AR P110102454A AR P110102454 A ARP110102454 A AR P110102454A AR 082135 A1 AR082135 A1 AR 082135A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
halogen
fluorine atoms
substituted
Prior art date
Application number
ARP110102454A
Other languages
English (en)
Inventor
Axel Stoit
Bakker Wouter I Iwema
Hein K A C Coolen
Dongen Maria J P Van
Nicolas J-L D Leflemme
Original Assignee
Abbott Healthcare Products Bv
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.)
Filing date
Publication date
Application filed by Abbott Healthcare Products Bv filed Critical Abbott Healthcare Products Bv
Publication of AR082135A1 publication Critical patent/AR082135A1/es

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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Derivados de espiro-amina cíclica de la fórmula (1) en donde R1 se selecciona de ciano, alquenilo C2-4, alquinilo C2-4alquilo C1-4 cada uno sustituido opcionalmente con CN o uno o más átomos de flúor; cicloalquilo C3-6, cicloalquenilo C4-6 o un grupo bicíclico C8-10, cada uno sustituido opcionalmente con halógeno o alquilo C1-4; fenilo, bifenilo, naftilo, cada uno sustituido opcionalmente con uno o más sustituyentes seleccionados independiente de halógeno, ciano, alquilo C1-6 opcionalmente sustituido con uno o más átomos de flúor, alcoxi C1-6 opcionalmente sustituido con uno o más átomos de flúor, amino, dialquil C1-4amino y cicloalquilo C3-6 opcionalmente sustituido con fenilo que se puede sustituir con alquilo C1-4 o halógeno; fenilo sustituido con fenoxi, bencilo, benciloxi, feniletilo o heterociclo monocíclico, cada uno sustituido opcionalmente con alquilo C1-4 opcionalmente sustituido con uno o más átomos de flúor; heterociclo monocíclico opcionalmente independientemente sustituido con halógeno, alquilo C1-6 opcionalmente sustituido con uno o más átomos de flúor, cicloalquilo C3-6, o fenilo opcionalmente sustituido con alquilo C1-4 o halógeno, y heterociclo bicíclico opcionalmente sustituido con halógeno o alquilo C1-4 opcionalmente sustituido con uno o más átomos de flúor; -Y-(Cn-alquileno)-X- es un grupo ligador en donde Y se adhiere a R1 y se selecciona de un enlace, -O-, -CO-, -S-, -SO-, -SO2-, -NH-, -CH=CH-, -C(CF3)=CH-, -CºC-, -CH2-O-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, y trans-ciclopropileno; n es un entero de 0 a 10; y X se adhiere al grupo funcional fenileno/piridilo y se selecciona de un enlace, -O-, -S-, -SO-, -SO2-, -NH-, -CO-, -CH=CH-, y trans-ciclopropileno; R2 es H o independientemente seleccionado de uno o más sustituyentes seleccionados de halógeno, alcoxi C1-4 y alquilo C1-4 opcionalmente sustituido con uno o más átomos de flúor; y R3 es alquileno C1-4-R4 en donde el grupo alquileno se puede sustituir con uno o más átomos de halógeno o con (CH2)2 para formar un grupo funcional ciclopropilo, o R3 es cicloalquileno C3-6-R4, -CH2-cicloalquileno C3-6-R4, cicloalquileno C3-6-CH2-R4 o -CO-CH2-R4, en donde R4 es -OH, -PO3H2, -OPO3H2, -COOH, -COO-alquilo C1-4 o tetrazol-5-ilo; Q es un enlace ó -O-; -W-T- se selecciona de -CH=CH-, -CH2-CH2-, -CH2-O-, -O-CH2-, -O-CH2-CH2- y -CO-O-; R5 es H o seleccionado independientemente de uno o más halógenos; Z es CH, CR2 o N; y A representa una estructura de anillo morfolino o una amina cíclica de 5, 6 ó 7 miembros; o una sal, un solvato, un hidrato farmacéuticamente aceptable de los mismos o uno o más óxidos N de los mismos. Estos compuestos tienen afinidad a los receptores S1P y se pueden utilizar en el tratamiento, alivio o prevención de enfermedades o afecciones en las que se involucran (a) los receptores S1P. Se proveen además, intermediarios de síntesis de los mismos y un proceso para su obtención.Reivindicación 18: Un compuesto de la fórmula (2) en donde Br se une en uno de los sitios indicados con un asterisco. Reivindicación 19: Un compuesto de la fórmula (3) en donde OH se une en uno de los sitios indicados con #, y en donde, si OH está en la posición indicada con 1, el compuesto se puede sustituir independientemente con alquilo C1-4 o halógeno seleccionado de F o Cl en una o ambas posiciones indicadas con 2; y -W-T es -O-CH2- o -CH2-CH2-; y A representa una estructura de anillo morfolino o una amina cíclica de 5, 6 ó 7 miembros.
ARP110102454A 2010-07-09 2011-07-08 Derivados de espiro-piperidina como moduladores s1p AR082135A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10169104 2010-07-09
EP11154961 2011-02-18

Publications (1)

Publication Number Publication Date
AR082135A1 true AR082135A1 (es) 2012-11-14

Family

ID=44315247

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102454A AR082135A1 (es) 2010-07-09 2011-07-08 Derivados de espiro-piperidina como moduladores s1p

Country Status (23)

Country Link
US (4) US10179791B2 (es)
EP (2) EP2590955B9 (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) TWI543984B (es)
UY (1) UY33497A (es)
WO (1) WO2012004378A1 (es)
ZA (1) ZA201300153B (es)

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