AR082137A1 - Derivados de bisaril(tio)morfolina como modulares s1p y composiciones farmaceuticas que los contienen - Google Patents

Derivados de bisaril(tio)morfolina como modulares s1p y composiciones farmaceuticas que los contienen

Info

Publication number
AR082137A1
AR082137A1 ARP110102456A AR082137A1 AR 082137 A1 AR082137 A1 AR 082137A1 AR P110102456 A ARP110102456 A AR P110102456A AR 082137 A1 AR082137 A1 AR 082137A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
fluorine atoms
atoms
substituted
Prior art date
Application number
Other languages
English (en)
Inventor
Bakker Wouter I Iwema
Raymond Bronger
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 AR082137A1 publication Critical patent/AR082137A1/es

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Classifications

    • 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
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • 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
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

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

Abstract

La presente se relaciona con derivados de bisaril(tio)morfolina de la fórmula (1), en donde R1 es un sustituyente arilo se selecciona de fenilo, piridilo, pirimidinilo, bifenilo y naftilo, cada uno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, alquilo C1-6 opcionalmente sustituido con uno o más átomos de flúor, alcoxi C1-4 opcionalmente sustituido con uno o más átomos de flúor, amino, dialquilamino C1-4, -SO2-alquilo C1-4, -CO-alquilo C1-4, -CO-O-alquilo C1-4 y -NH-CO-alquilo C1-4, o sustituido con fenoxi, bencilo, benciloxi, feniletilo o morfolinilo, cada uno opcionalmente sustituido con alquilo C1-4, y grupo bicíclico C8-10, heterociclo bicíclico, cada uno opcionalmente sustituido con alquilo C1-4 opcionalmente sustituido con uno o más átomos de flúor o oxo; A se selecciona de -CO-, -NH-, -O-, -S-, -SO- o -SO2-; la estructura del anillo B contiene opcionalmente un átomo de nitrógeno; R2 es H, alquilo C1-4 opcionalmente sustituido con uno o más átomos de flúor, alcoxi C1-4 opcionalmente sustituido con uno o más átomos de flúor, o halógeno; y R3 es alquileno C1-4-R6 en donde el grupo alquileno se puede sustituir con (CH2)2 para formar un grupo funcional ciclopropilo o con uno o más átomos de halógeno, o R3 es cicloalquileno C3-6-R5 o -CO-CH2-R6, en donde R6 es -OH, -PO3H2, -OPO3H2, -COOH, -COO-alquilo C1-4 o tetrazol-5-ilo; R4 es H o alquilo C1-4; R5 es uno o más sustituyentes seleccionados independientemente de H, alquilo C1-4 o oxo; W es -O-, -S-, -SO- o -SO2-; o una sal farmacéuticamente aceptable, un solvato o hidrato del mismo, con la condición de que el derivado de la fórmula (1) no es 2-[4-(4-clorofenoxi)-2-cloro-fenil]-4-morfolinaetanol. Los compuestos de la presente tienen afinidad con los receptores S1P y se pueden utilizar en el tratamiento, alivio o prevención de enfermedades y afecciones mediadas por el receptor S1P.
ARP110102456 2010-07-09 2011-07-08 Derivados de bisaril(tio)morfolina como modulares s1p y composiciones farmaceuticas que los contienen AR082137A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10169108 2010-07-09
EP11158269 2011-03-15

Publications (1)

Publication Number Publication Date
AR082137A1 true AR082137A1 (es) 2012-11-14

Family

ID=44323383

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102456 AR082137A1 (es) 2010-07-09 2011-07-08 Derivados de bisaril(tio)morfolina como modulares s1p y composiciones farmaceuticas que los contienen

Country Status (13)

Country Link
US (3) US9029371B2 (es)
EP (1) EP2590954B1 (es)
JP (1) JP5841593B2 (es)
CN (1) CN103080096B (es)
AR (1) AR082137A1 (es)
CA (1) CA2804329C (es)
DK (1) DK2590954T3 (es)
ES (1) ES2570744T3 (es)
MX (1) MX338605B (es)
PL (1) PL2590954T3 (es)
TW (1) TW201206893A (es)
UY (1) UY33495A (es)
WO (1) WO2012004375A1 (es)

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Also Published As

Publication number Publication date
US20160151376A1 (en) 2016-06-02
US20130203745A1 (en) 2013-08-08
EP2590954B1 (en) 2016-04-13
US9029371B2 (en) 2015-05-12
US20150191457A1 (en) 2015-07-09
MX2013000361A (es) 2013-04-29
CA2804329A1 (en) 2012-01-12
DK2590954T3 (en) 2016-05-02
CN103080096A (zh) 2013-05-01
UY33495A (es) 2012-01-31
EP2590954A1 (en) 2013-05-15
US9227960B2 (en) 2016-01-05
MX338605B (es) 2016-04-22
US9662337B2 (en) 2017-05-30
CA2804329C (en) 2019-05-14
PL2590954T3 (pl) 2016-09-30
JP2013531003A (ja) 2013-08-01
TW201206893A (en) 2012-02-16
JP5841593B2 (ja) 2016-01-13
ES2570744T3 (es) 2016-05-20
CN103080096B (zh) 2015-12-09
WO2012004375A1 (en) 2012-01-12

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