ES2613716T3 - Formas cristalinas de un derivado de purina - Google Patents

Formas cristalinas de un derivado de purina Download PDF

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ES2613716T3
ES2613716T3 ES11701855.6T ES11701855T ES2613716T3 ES 2613716 T3 ES2613716 T3 ES 2613716T3 ES 11701855 T ES11701855 T ES 11701855T ES 2613716 T3 ES2613716 T3 ES 2613716T3
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theta
values
diffraction peaks
crystal forms
purine derivative
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Benjamin Mark Skead
Christopher Peter Worrall
Jonathan Charles Christian Atherton
Julian Scott Northen
Philippe Fernandes
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Cyclacel Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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Abstract

Una forma cristalina del compuesto (I), **Fórmula** en la que dicho compuesto está en forma de una sal L-tartrato o un solvato farmacéuticamente aceptable del mismo, que está caracterizada por: (i) un patrón de difracción de polvo de rayos X que tiene dos o más picos de difracción a valores de 2[theta] seleccionados entre 6,67 ± 0,2, 8,237 ± 0,2, 9,777 ± 0,2, 11,96 ± 0,2, 12,38 ± 0,2, 13,06 ± 0,2, 13,38 ± 0,2, 13,94 ± 0,2, 14,90 ± 0,2, 15,40 ± 0,2, 15,95 ± 0,2, 16,27 ± 0,2, 16,54 ± 0,2, 17,36 ± 0,2, 17,57 ± 0,2, 17,86 ± 0,2, 19,64 10 ± 0,2, 19,86 ± 0,2, 20,12 ± 0,2, 20,73 ± 0,2, 21,14 ± 0,2, 21,58 ± 0,2, 22,57 ± 0,2, 22,95 ± 0,2, 23,29 ± 0,2, 23,57 ± 0,2, 24,07 ± 0,2, 24,63 ± 0,2, 25,30 ± 0,2, 26,38 ± 0,2, 27,09 ± 0,2, 27,67 ± 0,2, 27,97 ± 0,2, 28,91 ± 0,2, 29,28 ± 0,2, 30,08 ± 0,2, 30,41 ± 0,2, 31,90 ± 0,2 y 34,49 ± 0,2, cuando se usa radiación de Cu Kα y una velocidad de exploración de 0,146 º/s (Forma E), más preferiblemente que tiene dos o más picos de difracción a valores de 2[theta] seleccionados entre 6,67 ± 0,2, 13,06 ± 0,2, 13,38 ± 0,2, 14,90 ± 0,2, 17,36 ± 0,2, 17,57 ± 0,2, 19,64 ± 15 0,2, 20,73 ± 0,2, 23,57 ± 0,2 y 25,30 ± 0,2 (Forma E); o (ii) una traza de calorimetría de exploración diferencial registrada a una tasa de calentamiento de 20 ºC por minuto que muestra un pico endotérmico máximo a una temperatura entre 176 ºC y 185 ºC; o (iii) un patrón de difracción de polvo de rayos X que tiene dos o más picos de difracción a valores de 2[theta] seleccionados entre 3,82 ± 0,2, 7,57 ± 0,2, 8,12 ± 0,2, 10,53 ± 0,2, 11,39 ± 0,2, 12,00 ± 0,2, 13,54 ± 0,2, 15,15 ± 20 0,2, 16,35 ± 0,2, 16,88 ± 0,2, 17,37 ± 0,2, 18,51 ± 0,2, 18,98 ± 0,2, 19,77 ± 0,2, 21,06 ± 0,2, 22,70 ± 0,2, 23,47 ± 0,2, 24,66 ± 0,2 y 28,73 ± 0,2, cuando se usa radiación de Cu Kα y una velocidad de exploración de 0,146 º/s [Forma D], más preferiblemente que tiene dos o más picos de difracción a valores de 2[theta] seleccionados entre 3,82 ± 0,2, 7,57 ± 0,2, 15,15 ± 0,2, 16,88 ± 0,2, 19,77 ± 0,2, 22,70 ± 0,2, 23,47 ± 0,2, 24,66 ± 0,2 y 28,73 ± 0,2 [Forma D]; o (iv) una traza de calorimetría de exploración diferencial registrada a una tasa de calentamiento de 10 ºC por minuto que muestra un pico endotérmico máximo a una temperatura entre 145 ºC y 154 ºC.
ES11701855.6T 2010-01-22 2011-01-24 Formas cristalinas de un derivado de purina Active ES2613716T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1001075.9A GB201001075D0 (en) 2010-01-22 2010-01-22 Crystalline forms
GB201001075 2010-01-22
PCT/GB2011/000087 WO2011089401A1 (en) 2010-01-22 2011-01-24 Crystalline forms of a purine derivative

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ES2613716T3 true ES2613716T3 (es) 2017-05-25

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CN107400134B (zh) 2020-09-29
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WO2011089401A1 (en) 2011-07-28
EP3150602A1 (en) 2017-04-05
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US8889861B2 (en) 2014-11-18
GB201001075D0 (en) 2010-03-10
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US20150148354A1 (en) 2015-05-28
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US9573951B2 (en) 2017-02-21
CN107400134A (zh) 2017-11-28
TR201816159T4 (tr) 2018-11-21
KR20180054933A (ko) 2018-05-24
KR20120124450A (ko) 2012-11-13
ES2694289T3 (es) 2018-12-19
KR101860806B1 (ko) 2018-05-24
US20130072504A1 (en) 2013-03-21
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