MX338605B - Derivados de bisaril (tio)morfolina como moduladores s1p. - Google Patents

Derivados de bisaril (tio)morfolina como moduladores s1p.

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Publication number
MX338605B
MX338605B MX2013000361A MX2013000361A MX338605B MX 338605 B MX338605 B MX 338605B MX 2013000361 A MX2013000361 A MX 2013000361A MX 2013000361 A MX2013000361 A MX 2013000361A MX 338605 B MX338605 B MX 338605B
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MX
Mexico
Prior art keywords
alkyl
optionally substituted
fluoro atoms
halogen
substituted
Prior art date
Application number
MX2013000361A
Other languages
English (en)
Other versions
MX2013000361A (es
Inventor
Bakker Wouter I Iwema
Raymond Bronger
Original Assignee
Abbvie 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 Abbvie Bv filed Critical Abbvie Bv
Publication of MX2013000361A publication Critical patent/MX2013000361A/es
Publication of MX338605B publication Critical patent/MX338605B/es

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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
    • A61K31/535—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)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (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 invención se relaciona con derivados de bisaril (tio) morfolina de la fórmula (I) (Ver Formula) 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 (C 1-6) opcionalmente sustituido con uno o más átomos de flúor, alcoxi (C 1-4) opcionalmente sustituido con uno o más átomos de flúor, amino, dialquilamino (C 1-4), -S02-alquilo (C 1-4), -CO-alquilo (C 1-4), -CO-O-alquilo (C 1-4) y -NHCO-alquilo (C 1-4), o sustituido con fenoxi, bencilo, benciloxi, feniletilo o morfolinilo, cada uno opcionalmente sustituido con alquilo (C 1-4), y grupo bicíclico (C 8-10), heterociclo bicíclico, cada uno opcionalmente sustituido con alquilo (C 1-4) 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 (C 1-4) opcionalmente sustituido con uno o más átomos de flúor, alcoxi (C 1-4) opcionalmente sustituido con uno o más átomos de flúor, o halógeno; y R3 es alquileno (C 1-4)-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 (C 3-6)-R5 o -CO-CH2-R6, en donde R6 es - OH, -P03H2, -0P03H2, -COOH, -COOalquilo (C 1-4) o tetrazol -5- ilo; R4 es H o alquilo (C 1-4); R5 es uno o más sustituyentes seleccionados independientemente de H, alquilo (C 1-4) 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 (I) no es 2-[4-(4-cborofenoxi) -2- cloro -fenil]-4-morfolinaetanol; los compuestos de la invención 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.
MX2013000361A 2010-07-09 2011-07-08 Derivados de bisaril (tio)morfolina como moduladores s1p. MX338605B (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US36278510P 2010-07-09 2010-07-09
EP10169108 2010-07-09
US201161452977P 2011-03-15 2011-03-15
EP11158269 2011-03-15
PCT/EP2011/061590 WO2012004375A1 (en) 2010-07-09 2011-07-08 Bisaryl (thio)morpholine derivatives as s1p modulators

Publications (2)

Publication Number Publication Date
MX2013000361A MX2013000361A (es) 2013-04-29
MX338605B true MX338605B (es) 2016-04-22

Family

ID=44323383

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013000361A MX338605B (es) 2010-07-09 2011-07-08 Derivados de bisaril (tio)morfolina como moduladores s1p.

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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WO2021087299A1 (en) 2019-10-31 2021-05-06 E-Scape Bio, Inc. Solid forms of an s1p-receptor modulator

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Also Published As

Publication number Publication date
CA2804329C (en) 2019-05-14
EP2590954A1 (en) 2013-05-15
TW201206893A (en) 2012-02-16
ES2570744T3 (es) 2016-05-20
US20130203745A1 (en) 2013-08-08
JP2013531003A (ja) 2013-08-01
US9227960B2 (en) 2016-01-05
US20160151376A1 (en) 2016-06-02
UY33495A (es) 2012-01-31
WO2012004375A1 (en) 2012-01-12
JP5841593B2 (ja) 2016-01-13
DK2590954T3 (en) 2016-05-02
PL2590954T3 (pl) 2016-09-30
MX2013000361A (es) 2013-04-29
US20150191457A1 (en) 2015-07-09
US9029371B2 (en) 2015-05-12
US9662337B2 (en) 2017-05-30
AR082137A1 (es) 2012-11-14
CN103080096A (zh) 2013-05-01
CA2804329A1 (en) 2012-01-12
CN103080096B (zh) 2015-12-09
EP2590954B1 (en) 2016-04-13

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