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AR088359A1 - FORMAS POLIMORFICAS DEL (1,1-DIOXO-l-4-TIOMORFOLINIL)-{6-[3-(4-FLUOROFENIL)-5-METIL-ISOXAZOL-4-ILMETOXI]-PIRIDIN-3-IL}-METANONA Y SU USO EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS - Google Patents

FORMAS POLIMORFICAS DEL (1,1-DIOXO-l-4-TIOMORFOLINIL)-{6-[3-(4-FLUOROFENIL)-5-METIL-ISOXAZOL-4-ILMETOXI]-PIRIDIN-3-IL}-METANONA Y SU USO EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS

Info

Publication number
AR088359A1
AR088359A1 ARP120103860A ARP120103860A AR088359A1 AR 088359 A1 AR088359 A1 AR 088359A1 AR P120103860 A ARP120103860 A AR P120103860A AR P120103860 A ARP120103860 A AR P120103860A AR 088359 A1 AR088359 A1 AR 088359A1
Authority
AR
Argentina
Prior art keywords
isoxazol
dioxo
methyl
xrpd
thiomorpholin
Prior art date
Application number
ARP120103860A
Other languages
English (en)
Inventor
Dott Pascal
Grassmann Olaf
Kammerer Michael
Manns Joachim
Schwitter Urs
Thomas Andrew
Wyttenbach Nicole
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR088359A1 publication Critical patent/AR088359A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • A61P25/28Drugs 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
    • 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
    • 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
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Formas sólidas del compuesto de la fórmula (1), así como a solvatos, complejos de inclusión con otros compuestos idóneos, a procesos de obtención, a composiciones farmacéuticas que contienen estas formas sólidas y a su utilización como medicamentos. Reivindicación 2: La (1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxi]-piridin-3-il}-metanona monohidratada cristalina de la forma polimórfica B según la reivindicación 1, caracterizada por un diagrama de difracción XRPD que contiene picos XRPD en los ángulos de difracción 2-q de aproximadamente 13,3º, 20,6º, 22,5º. Reivindicación 6: La 1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxi]-piridin-3-il}-metanona cristalina de la forma polimórfica anhidra C según la reivindicación 1, caracterizada por un diagrama de difracción XRPD que contiene picos XRPD en los ángulos de difracción 2-q de aproximadamente 17,4º, 23,4º. Reivindicación 10: La (1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxi]-piridin-3-il}-metanona cristalina monosolvatada con trifluoroetanol de la forma polimórfica D según la reivindicación 1, caracterizada por un diagrama de difracción XRPD que contiene picos XRPD en los ángulos de difracción 2-q de aproximadamente 6,1º, 16,8º, 22,6º. Reivindicación 13: La (1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxi]-piridin-3-il}-metanona cristalina de la forma polimórfica anhidra E según la reivindicación 1, caracterizada por un diagrama de difracción XRPD que contiene picos XRPD en los ángulos de difracción 2-q de aproximadamente 16,5º, 20,8º. Reivindicación 16: Un complejo de inclusión 1:1 de la (1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxi]-piridin-3-il}-metanona con la g-ciclodextrina según la reivindicación 1. Reivindicación 17: El complejo de inclusión según la reivindicación 16, caracterizado por un diagrama de difracción XRPD que contiene picos XRPD en los ángulos de difracción 2-q de aproximadamente 7,4º, 14,9º, 16,7º, 21,8º. Reivindicación 22: La (1,1-dioxo-1l⁶-tiomorfolin-4-il)-{6-[3-(4-fluoro-fenil)-5-metil-isoxazol-4-ilmetoxil-piridin-3-il}-metanona amorfa, caracterizada por lo menos por un halo amorfo y la falta de un pico agudo de difracción de Bragg en el diagrama de difracción XRPD. Reivindicación 26: La forma amorfa según una cualquiera de las reivindicaciones de 22 a 25, caracterizada por una temperatura de transición vítrea Tg de 60ºC a 70ºC.
ARP120103860A 2011-10-20 2012-10-17 FORMAS POLIMORFICAS DEL (1,1-DIOXO-l-4-TIOMORFOLINIL)-{6-[3-(4-FLUOROFENIL)-5-METIL-ISOXAZOL-4-ILMETOXI]-PIRIDIN-3-IL}-METANONA Y SU USO EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS AR088359A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11185993 2011-10-20

Publications (1)

Publication Number Publication Date
AR088359A1 true AR088359A1 (es) 2014-05-28

Family

ID=47019027

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120103860A AR088359A1 (es) 2011-10-20 2012-10-17 FORMAS POLIMORFICAS DEL (1,1-DIOXO-l-4-TIOMORFOLINIL)-{6-[3-(4-FLUOROFENIL)-5-METIL-ISOXAZOL-4-ILMETOXI]-PIRIDIN-3-IL}-METANONA Y SU USO EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS

Country Status (19)

Country Link
US (2) US8785435B2 (es)
EP (1) EP2768821B1 (es)
JP (1) JP5918856B2 (es)
KR (1) KR20140079503A (es)
CN (1) CN103889971B (es)
AR (1) AR088359A1 (es)
AU (1) AU2012318294B2 (es)
BR (1) BR112014009288A8 (es)
CA (1) CA2850441A1 (es)
DK (1) DK2768821T3 (es)
ES (1) ES2606547T3 (es)
HU (1) HUE030298T2 (es)
IL (1) IL231532A0 (es)
MX (1) MX341492B (es)
PL (1) PL2768821T3 (es)
RU (1) RU2618524C2 (es)
SG (1) SG11201401591WA (es)
SI (1) SI2768821T1 (es)
WO (1) WO2013057124A1 (es)

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EP2792360A1 (en) 2013-04-18 2014-10-22 IP Gesellschaft für Management mbH (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,2b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide for use in treating HCV
EA202090521A1 (ru) * 2017-08-28 2020-06-10 Юниверсити Оф Мэриленд, Балтимор Новые модуляторы рецептора гамма-аминомасляной кислоты типа a против расстройств настроения
CR20200610A (es) 2018-06-13 2021-02-05 Hoffmann La Roche Nuevos derivados de isoxazolit éter como pan de gaba a alfa 5
MX2023004293A (es) 2020-10-13 2023-05-03 Boehringer Ingelheim Int Proceso de reelaboracion.

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Also Published As

Publication number Publication date
JP2014530832A (ja) 2014-11-20
EP2768821B1 (en) 2016-11-16
CN103889971B (zh) 2016-08-31
MX341492B (es) 2016-08-23
US20130172329A1 (en) 2013-07-04
WO2013057124A1 (en) 2013-04-25
NZ622215A (en) 2016-06-24
IL231532A0 (en) 2014-04-30
BR112014009288A8 (pt) 2020-04-22
HUE030298T2 (en) 2017-04-28
AU2012318294B2 (en) 2015-10-01
MX2014004678A (es) 2014-05-28
SG11201401591WA (en) 2014-05-29
RU2618524C2 (ru) 2017-05-04
PL2768821T3 (pl) 2017-05-31
CA2850441A1 (en) 2013-04-25
CN103889971A (zh) 2014-06-25
US20140329806A1 (en) 2014-11-06
RU2014118968A (ru) 2015-11-27
DK2768821T3 (en) 2017-01-23
SI2768821T1 (sl) 2017-01-31
JP5918856B2 (ja) 2016-05-18
US8975397B2 (en) 2015-03-10
EP2768821A1 (en) 2014-08-27
AU2012318294A1 (en) 2013-05-09
ES2606547T3 (es) 2017-03-24
KR20140079503A (ko) 2014-06-26
HK1193611A1 (zh) 2014-09-26
US8785435B2 (en) 2014-07-22
BR112014009288A2 (pt) 2017-06-13

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