JPWO2020167844A5 - - Google Patents

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JPWO2020167844A5
JPWO2020167844A5 JP2021547092A JP2021547092A JPWO2020167844A5 JP WO2020167844 A5 JPWO2020167844 A5 JP WO2020167844A5 JP 2021547092 A JP2021547092 A JP 2021547092A JP 2021547092 A JP2021547092 A JP 2021547092A JP WO2020167844 A5 JPWO2020167844 A5 JP WO2020167844A5
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crystal
diffraction pattern
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Priority claimed from FR1902018A external-priority patent/FR3092581A1/en
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Claims (42)

化合物１の結晶。
Figure 2020167844000001
 Crystals of compound 1.
Figure 2020167844000001
 前記結晶が水和物である、請求項１の結晶。 2. The crystal of claim 1, wherein said crystal is a hydrate. 前記結晶が、一水和物である、請求項２の結晶。 3. The crystal of claim 2, wherein said crystal is a monohydrate. 前記一水和物は、４．３、９．６、１０．０、１２．４、１２．７、及び１７．０±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項３の結晶。 The monohydrate has 1 4. The crystal of claim 3 characterized by one or more peaks. 前記一水和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項３の結晶。
Figure 2020167844000002
 4. The crystal of claim 3, wherein said monohydrate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000002
 前記結晶が三水和物である、請求項２の結晶。 3. The crystal of claim 2, wherein said crystal is a trihydrate. 前記三水和物は、５．４、６．２、１１．６、１３．９、１６．４、及び１６．７±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項６の結晶。 The trihydrate has a 1 in its X-ray powder diffraction pattern selected from 5.4, 6.2, 11.6, 13.9, 16.4, and 16.7 ± 0.2 degrees 2-theta. 7. The crystal of claim 6, characterized by one or more peaks. 前記三水和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項６の結晶。
Figure 2020167844000003
 7. The crystal of claim 6, wherein said trihydrate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000003
 前記結晶が無水物である、請求項１の結晶。 2. The crystal of claim 1, wherein said crystal is an anhydrate. 前記無水物は、４．３、６．２、８．６、９．７、１３．６、及び１７．３±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項９の結晶。 The anhydride has one or more in its X-ray powder diffraction pattern selected from 4.3, 6.2, 8.6, 9.7, 13.6, and 17.3 ± 0.2 degrees two-theta. 10. The crystal of claim 9, characterized by a peak of 前記無水物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項９の結晶。
Figure 2020167844000004
 10. The crystal of claim 9, wherein said anhydride is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000004
 前記無水物は、１２．８、１３．６、１４．９、１６．１、及び１７．２±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項９の結晶。 The anhydride is characterized by one or more peaks in its X-ray powder diffraction pattern selected from 12.8, 13.6, 14.9, 16.1, and 17.2 ± 0.2 degrees 2-theta. 10. The crystal of claim 9 attached. 前記無水物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項９の結晶。
Figure 2020167844000005
 10. The crystal of claim 9, wherein said anhydride is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000005
 前記結晶が溶媒和物である、請求項１の結晶。 2. The crystal of claim 1, wherein said crystal is a solvate. 前記結晶が、モノイソプロパノール溶媒和物である、請求項１４の結晶。 15. The crystal of claim 14, wherein said crystal is a monoisopropanol solvate. 前記モノイソプロパノール溶媒和物は、７．２、１０．４、１０．８、１３．２、及び１７．５±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項１５の結晶。 The monoisopropanol solvate has one or more 16. The crystal of claim 15 characterized by peaks. 前記モノイソプロパノール溶媒和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項１５の結晶。
Figure 2020167844000006
 16. The crystal of claim 15, wherein said monoisopropanol solvate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000006
 前記結晶が、テトライソプロパノール溶媒和物である、請求項１４の結晶。 15. The crystal of claim 14, wherein said crystal is a tetraisopropanol solvate. 前記テトライソプロパノール溶媒和物は、５．３、６．４、８．２、１０．５、１５．３、及び１５．７±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項１８の結晶。 The tetraisopropanol solvate has an X-ray powder diffraction pattern of 19. The crystal of claim 18, characterized by one or more peaks. 前記テトライソプロパノール溶媒和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項１８の結晶。
Figure 2020167844000007
 19. The crystal of claim 18, wherein said tetraisopropanol solvate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000007
 前記結晶がヘテロ溶媒和物である、請求項１の結晶。 2. The crystal of claim 1, wherein said crystal is a heterosolvate. 前記結晶が水－イソプロパノールヘテロ溶媒和物である、請求項２１の結晶。 22. The crystal of claim 21, wherein said crystal is a water-isopropanol heterosolvate. 前記水－イソプロパノールヘテロ溶媒和物は、７．３、７．６、１０．４、１０．８、及び１７．５±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項２２の結晶。 The water-isopropanol heterosolvate has one in its X-ray powder diffraction pattern selected from 7.3, 7.6, 10.4, 10.8, and 17.5 ± 0.2 degrees 2-theta. 23. The crystal of claim 22, characterized by the following peaks. 前記水－イソプロパノールヘテロ溶媒和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項２２の結晶。
Figure 2020167844000008
 23. The crystal of claim 22, wherein said water-isopropanol heterosolvate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000008
 前記結晶がヘキサフルオロイソプロパノール溶媒和物である、請求項１４の結晶。 15. The crystal of claim 14, wherein said crystal is a hexafluoroisopropanol solvate. 前記ヘキサフルオロイソプロパノール溶媒和物は、４．３、６．０、６．９、１０．９、１１．５、１４．７、及び１７．１±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項２５の結晶。 The hexafluoroisopropanol solvate has an X 26. The crystal of claim 25, characterized by one or more peaks in a line powder diffraction pattern. 前記ヘキサフルオロイソプロパノール溶媒和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項２５の結晶。
Figure 2020167844000009
 26. The crystal of claim 25, wherein said hexafluoroisopropanol solvate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000009
 前記結晶がエタノール溶媒和物である、請求項１４の結晶。 15. The crystal of claim 14, wherein said crystal is an ethanol solvate. 前記エタノール溶媒和物は、５．３、１０．６、及び１５．９±０．２度の２θから選択されるそのＸ線粉末回折パターンにおける１つ以上のピークによって特徴付けられる、請求項２８の結晶。 29. The ethanol solvate is characterized by one or more peaks in its X-ray powder diffraction pattern selected from 5.3, 10.6, and 15.9±0.2 degrees two-theta. crystals. 前記エタノール溶媒和物は、そのＸ線粉末回折パターンにおける以下のピークによって特徴付けられる、請求項２８の結晶。
Figure 2020167844000010
 29. The crystal of claim 28, wherein said ethanol solvate is characterized by the following peaks in its X-ray powder diffraction pattern.
Figure 2020167844000010
 請求項１～３０のいずれか１項の結晶を含む、実質的に不純物を含まないサンプル。 A substantially impurity-free sample comprising the crystals of any one of claims 1-30. 少なくとも約９０重量％の化合物１を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising at least about 90% by weight Compound 1. 少なくとも約９５重量％の化合物１を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising at least about 95% by weight Compound 1. 少なくとも約９９重量％の化合物１を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising at least about 99% by weight Compound 1. 約５．０％以下の全有機不純物を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising no more than about 5.0% total organic impurities. 約３．０％以下の全有機不純物を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising no more than about 3.0% total organic impurities. 約１．５％以下の全有機不純物を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising no more than about 1.5% total organic impurities. 約１．０％以下の全有機不純物を含む、請求項３１のサンプル。 32. The sample of claim 31, comprising no more than about 1.0% total organic impurities. 約０．５％以下の全有機不純物を含む、請求項３１のサンプル。 32. The sample of claim 31, containing no more than about 0.5% total organic impurities. インビトロ生物学的サンプルにおいてＪＡＫ２キナーゼまたはその変異体の活性を阻害する方法であって、前記インビトロ生物学的サンプルを請求項１～３０のいずれか１項の結晶またはその組成物と接触させるステップを含む、前記方法。 31. A method of inhibiting the activity of a JAK2 kinase or variant thereof in an in vitro biological sample, comprising the step of contacting said in vitro biological sample with a crystal or composition thereof of any one of claims 1-30. The method above. ＪＡＫ２キナーゼまたはその変異体の活性の阻害剤であって、請求項１～３０のいずれか１項の結晶またはその組成物を含む、阻害剤。 An inhibitor of the activity of JAK2 kinase or a variant thereof, comprising a crystal of any one of claims 1-30 or a composition thereof. ＪＡＫ２媒介性の疾患または障害の治療剤であって、請求項１～３０のいずれか１項の結晶またはその薬学的に許容される組成物を含む、治療剤。 A therapeutic agent for a JAK2-mediated disease or disorder, comprising the crystal of any one of claims 1-30 or a pharmaceutically acceptable composition thereof.
JP2021547092A 2019-02-12 2020-02-11 Crystal form of JAK2 inhibitor Pending JP2022520083A (en)

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FR1902018A FR3092581A1 (en) 2019-02-12 2019-02-12 CRYSTALLINE FORMS OF A JAK2 INHIBITOR
FR1902018 2019-02-12
PCT/US2020/017764 WO2020167844A1 (en) 2019-02-12 2020-02-11 Crystalline forms of a jak2 inhibitor

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