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НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ФОРМЫ ИНГИБИТОРОВ ДИПЕПТИДИЛПЕПТИДАЗЫ-IV
专利权人:
МЕРК ШАРП И ДОУМ КОРП. (US)
发明人:
АРРОЙО Ициа (US),КРЮГЕР Давида (US),ЧЭНЬ Пин (US),МОМЕНТ Аарон (US),БИФТУ Тесфайе (US),ШИН Фэй (GB),ЧЖАН Яньфын (CN)
申请号:
RU2014102773/04
公开号:
RU2014102773A
申请日:
2012.06.25
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. Crystalline (2R, 3S, 5R) -2- (2,5-difluorophenyl) -5- [2- (methylsulfonyl) -2,6-dihydro-pyrrolo [3,4-c] pyrazol-5 (4H) -yl ] tetrahydro-2H-pyran-3-amine compound I: 2. Crystalline (2 / R, 3S, 5R) -2- (2,5-difluorophenyl) -5- [2- (methylsulfonyl) -2,6-dihydro-pyrrolo [3,4-c] pyrazol-5 (4H) -yl ] tetrahydro-2H-pyran-3-amine (form I) according to claim. 1, characterized in that it has at least four peaks in its X-ray diffraction pattern from powders selected from the group consisting of 10.3 +0.1 2θ, 12.7 2θ ± 0.1, 14.6 ± 0.1 2θ, 16.1 2θ ± 0.1, 17.8 ± 0.1 2θ, 19.2 ± 0.1 2θ , 22.2 2θ ± 0.1, 24.1 ± 0.1 2θ and 26,9 ± 0,1 2θ.3. The crystalline form of claim 2 wherein the following four peaks in its X-ray diffraction pattern from powders:. 17.8 2θ ± 0.1, 19.2 ± 0.1 2θ, 22.2 ± 0.1 24,1 ± 2θ and 0,1 2θ.4. The crystalline form of claim. 2, further characterized in differential scanning calorimetry curve (DSC) or 3 further characterized curve of thermogravimetric analysis (TGA) on fig.2.5. The crystalline form of claim. 2, further otlichayuschayasyaspektrami nuclear magnetic resonance (NMR) or 4 further characterized in fig.5.6 IR spectra. The crystalline (2R, 3S, 5R) -2- (2,5-difluorophenyl) -5- [2- (methylsulfonyl) -2,6-dihydro-pyrrolo [3,4-c] pyrazol-5 (4H) -yl] tetrahydro -2H-pyran-3-amine (Form II) according to claim. 1, characterized in that it has at least four peaks in its X-ray diffraction pattern from powders selected from the group consisting of 7,5 ± 0 1 2θ, 15.0 2θ ± 0.1, 16.2 ± 0.1 2θ, 20.9 2θ ± 0.1, 22.0 ± 0.1 2θ, 27.0 ± 0.1 2θ, 27 , 6 ± 0,1 2θ, 33,3 + 0,1 2θ.7. The crystalline form of claim 6, wherein the following four peaks in its X-ray diffraction pattern from powders:. 20.9 2θ ± 0.1, 22.0 ± 0.1 2θ, 27.0 ± 0.1 and 27.6 2θ ± 0,1 2θ.8. The crystalline form of claim. 6, further wherein the differential curve1. Кристаллический (2R,3S,5R)-2-(2,5-дифторфенил)-5-[2-(метилсульфонил)-2,6-дигидропирроло[3,4-c]пиразол-5(4H)-ил]тетрагидро-2H-пиран-3-амин соединения I:
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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