DK2201018T3 - Faste former omfattende n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]-benzothiazol-2-yl]phenyl}urea, sammensætninger deraf og anvendelser dermed - Google Patents

Faste former omfattende n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]-benzothiazol-2-yl]phenyl}urea, sammensætninger deraf og anvendelser dermed Download PDF

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Publication number
DK2201018T3
DK2201018T3 DK08832577.4T DK08832577T DK2201018T3 DK 2201018 T3 DK2201018 T3 DK 2201018T3 DK 08832577 T DK08832577 T DK 08832577T DK 2201018 T3 DK2201018 T3 DK 2201018T3
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compound
certain embodiments
salt
hci
acid
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DK08832577.4T
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Shripad Bhagwat
Wei Lai
Stephan D Parent
Melanie J Roe
Alan Schwartz
Valeriya N Smolenskaya
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Ambit Biosciences Corp
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

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  • Pulmonology (AREA)
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Claims (10)

1. Fast form, der omfatter et salt
af forbindelsen med formlen (I): (i), hvor saltet er valgt fra gruppen bestående af: hydrobromid-, besylat-, esylat-, edisylat-, mesylat-, napsylat-, sulfat- og tosylatsalte.
2. Fast form, der omfatter
et bis-HCI-salt af forbindelsen med formlen (I): (i)·
3. Fast form ifølge krav 1 eller 2, der endvidere omfatter opløsningsmiddel, eller som endvidere omfatter vand.
4. Fast form ifølge krav 2, der er i det væsentlige fri for opløsningsmiddel, eller som er i det væsentlige fri for vand, eller som er vandfri.
5. Fast form ifølge krav 2, der er den krystallinske form af Form B af bis-HCI-saltet af forbindelsen med formlen (I); der har et XRPD-mønster, som omfatter peaks ved ca. 6,98, 10,7, 20,82 og 27,6 °2Θ ved analyse under anvendelse af kobber Κα-stråling, eventuelt omfattende yderligere peaks ved ca. 15,78, 18,48, 22,62 og 27,08 °20 ved analyse under anvendelse af kobber Κα-stråling, endvidere eventuelt omfattende yderligere peaks ved ca. 13,04, 18,8, 24,38 og 26,16 °2Θ ved analyse under anvendelse af kobber Ka-stråling.
6. Fast form ifølge krav 2 med et XRPD-mønster, der matcher XRPD-mønstrene i FIG. 13a; eller med et XRPD-mønster, der matcher XRPD-mønstret i FIG. 13b; eller med et DSC-termogram, der omfatter en endotermisk hændelse med en begyndelsestemperatur på ca. 260° C; eller med enhedscelleparametre, der er forenelige med de følgende omtrentlige enhedscelleparametre: a = 15,6089 Å, b = 11,9443 Å, c = 16,9448 Å, β = 101,249°, V= 3098,5 Å3 og Z = 4; eller der er fysisk stabile ved ca. 75% RH ved ca. omgivelsestemperatur.
7. Fast form ifølge et af kravene 1, 2, 3, 4, 5 eller 6, der er i det væsentlige ren, eller som er i det væsentlige fri for kemiske urenheder, eller som er i det væsentlige fri for fysiske urenheder.
8. Farmaceutisk sammensætning, der omfatter den faste form ifølge et af kravene 1,2, 3, 4, 5 eller 6.
9. Fast form ifølge et af kravene 1, 2, 3, 4, 5 eller 6 til anvendelse ved behandling af et karcinom, et sarkom, leukæmi, myelom, en inflammatorisk sygdom eller en infektionssygdom.
10. Amorf form, der omfatter forbindelsen med følgende formel eller et farmaceutisk acceptabelt salt deraf:
DK08832577.4T 2007-09-19 2008-09-19 Faste former omfattende n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]-benzothiazol-2-yl]phenyl}urea, sammensætninger deraf og anvendelser dermed DK2201018T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US99463507P 2007-09-19 2007-09-19
PCT/US2008/010884 WO2009038757A2 (en) 2007-09-19 2008-09-19 Solid forms comprising n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions thereof, and uses therewith

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DK2201018T3 true DK2201018T3 (da) 2016-05-17

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DK08832577.4T DK2201018T3 (da) 2007-09-19 2008-09-19 Faste former omfattende n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]-benzothiazol-2-yl]phenyl}urea, sammensætninger deraf og anvendelser dermed

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US (2) US8883783B2 (da)
EP (1) EP2201018B1 (da)
JP (1) JP5462168B2 (da)
KR (2) KR101572701B1 (da)
CN (1) CN101868465B (da)
AR (1) AR068528A1 (da)
AU (1) AU2008302744B2 (da)
BR (1) BRPI0816904B8 (da)
CA (1) CA2696776C (da)
CY (1) CY1117583T1 (da)
DK (1) DK2201018T3 (da)
ES (1) ES2573292T3 (da)
HR (1) HRP20160520T1 (da)
HU (1) HUE027982T2 (da)
IL (1) IL203926A (da)
MX (1) MX2010002295A (da)
PL (1) PL2201018T3 (da)
SI (1) SI2201018T1 (da)
TW (1) TWI437988B (da)
WO (1) WO2009038757A2 (da)

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EP2201018B1 (en) 2007-09-19 2016-03-16 Ambit Biosciences Corporation Solid forms comprising n-(5-tert-butyl-isoxazol-3-yl)-n'-{4-ý7-(2-morpholin-4-yl-ethoxy)imidazoý2,1-b¨ý1,3¨benzothiazol-2-yl¨phenyl}urea, compositions thereof, and uses therewith
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