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DK2614058T3 - Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. - Google Patents

Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. Download PDF

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Publication number
DK2614058T3
DK2614058T3 DK11755311.5T DK11755311T DK2614058T3 DK 2614058 T3 DK2614058 T3 DK 2614058T3 DK 11755311 T DK11755311 T DK 11755311T DK 2614058 T3 DK2614058 T3 DK 2614058T3
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Denmark
Prior art keywords
salt
polymorph
methyl
dimethyl
added
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DK11755311.5T
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English (en)
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Robert David Willacy
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Glaxosmithkline Ip Dev Ltd
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    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (14)

1. Polymorf (Form II) af /V-[5-[4-(5-{[(2Æ,6S)-2,6-dimethyl-4-nnorpholinyl]nnethyl}- 1.3- oxazol-2-yl)-l/-/-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 9,2 ± 0,1.
2. Polymorf ifølge krav 1, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 1 Tabel 1
3. Polymorf ifølge krav 1 eller krav 2 i at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 1.
4. Polymorf (Form III) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl)·- 1.3- oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, k e n d e t egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 6,7 ± 0,1.
5. Polymorf ifølge krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 2 Tabel 2
6. Polymorf ifølge krav 4 eller krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 2.
7. Polymorf (Form IV) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl>- l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved omkring 5,8.
8. Polymorf ifølge krav 7, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 3 Tabel 3
9. Polymorf ifølge krav 7 eller krav 8, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 3.
10. Salt af /V-[5-[4-(5-{[(2/?,6S)-2,6-dimethyl-4-morpholinyl]methyl>-l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid som er natrium-, tosy-lat-, maleat-, hemipamoat-, heminaphthalendisulfonat-, mesitylensulfonat-, hemibiphenyl-disulfonat-, 2-naphthalensulfonat- (napsylat-), hemicinnamat-, hemisebacat-, hemipyro-mellitat- eller hemibenzendiacrylatsaltet.
11. Farmaceutisk sammensætning omfattende en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 og én eller flere farmaceutisk acceptable excipien-ser.
12. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i medicinsk terapi.
13. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
14. Anvendelse af en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 til fremstilling af et lægemiddel til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
DK11755311.5T 2010-09-08 2011-09-06 Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. DK2614058T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38074810P 2010-09-08 2010-09-08
PCT/EP2011/065419 WO2012032067A1 (en) 2010-09-08 2011-09-06 Polymorphs and salts of n- [5- [4- (5- { [(2r,6s) -2, 6 - dimethyl - 4 -morpholinyl] methyl} - 1, 3 - oxazol - 2 - yl) - 1h- inda zol-6-yl] -2- (methyloxy) - 3 - pyridinyl] methanesulfonamide

Publications (1)

Publication Number Publication Date
DK2614058T3 true DK2614058T3 (da) 2015-09-28

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Country Link
US (1) US8735390B2 (da)
EP (1) EP2614058B1 (da)
JP (1) JP5965402B2 (da)
DK (1) DK2614058T3 (da)
ES (1) ES2548036T3 (da)
HR (1) HRP20151017T1 (da)
HU (1) HUE026059T2 (da)
PL (1) PL2614058T3 (da)
PT (1) PT2614058E (da)
RS (1) RS54286B1 (da)
SI (1) SI2614058T1 (da)
SM (1) SMT201500223B (da)
WO (1) WO2012032067A1 (da)

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SI2614058T1 (sl) 2015-10-30
SMT201500223B (it) 2015-10-30
RS54286B1 (sr) 2016-02-29
PT2614058E (pt) 2015-10-27
HUE026059T2 (en) 2016-05-30
US8735390B2 (en) 2014-05-27
EP2614058B1 (en) 2015-07-08
US20130165441A1 (en) 2013-06-27
JP5965402B2 (ja) 2016-08-03
PL2614058T3 (pl) 2015-12-31
JP2013537175A (ja) 2013-09-30

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