发明名称 CRYSTALLINE FORMS OF 1-(5'-(5-(3,5-DICHLORO-4-FLUOROPHENYL)-5-(TRIFLUORO-METHYL)-4,5-DIHYDROISOXAZOL-3-YL)-3'H-SPIRO[AZETIDINE-3,1'-ISOBENZOFURAN]-1-YL)-2-(METHYLSULFONYL)ETHANONE
摘要 The present invention relates to novel crystalline modifications of 1-(5′-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoro-methyl)-4,5-dihydroisoxazol-3-yl)-3′H-spiro[azetidine-3,1′-isobenzofuran]-1-yl)-2-(methylsulfonyl)ethanone. The present invention also describes compositions and methods of treating a parasitic infection or infestation in an animal in need thereof. The present invention also relates to processes for making the crystalline forms.
申请公布号 US2015183795(A1) 申请公布日期 2015.07.02
申请号 US201314422098 申请日期 2013.08.28
申请人 Zoetis LLC 发明人 Billen Denis;Birchmeier Matthew Joseph;VanderRoest Ronald J.
分类号 C07D491/107;A61K45/06;A61K31/422 主分类号 C07D491/107
代理机构 代理人
主权项 1. A crystalline Form A of 1-(5′-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3′H-spiro[azetidine-3,1′-isobenzofuran]-1-yl)-2-(methylsulfonyl)ethanone which exhibits at least one of the following properties: a) an X-ray diffraction pattern having characteristic peaks expressed in degrees 2θ (±0.2°) at about 17.18, 18.83, and 20.07; b) an X-ray diffraction pattern having characteristic peaks expressed in degrees 2θ (±0.2°) at about 17.18, 18.83, and 20.07, and further comprising at least one additional diffraction peak expressed in degrees 2θ (±0.2°) selected from the group consisting of peaks at about 4.70, 9.39, 14.10, 15.70, 19.12, 20.97, 21.42, 22.03, 22.54, 23.62, and 28.42; c) an X-ray diffraction pattern having characteristic peaks expressed in degrees 2θ (±0.2°) at about 17.18, 18.83, and 20.07, and further comprising at least one additional diffraction peak expressed in degrees 2θ (±0.2°) at about 21.42, 22.54, and 28.42; d) an X-ray diffraction pattern having characteristic peaks expressed in degrees 2θ (±0.2°) at about 17.18, 18.83, 20.07, 21.42, 22.54, and 28.42; e) a Fourier Transform infrared spectrum at the 1800 to 600 cm−1 range, substantially as shown in FIG. 2; f) a differential scanning calorimeter thermogram having a single predominant endotherm at about 145.53° C. at a scan rate of 10° C. per minute, substantially as shown in FIG. 3.1; and g) a differential scanning calorimeter thermogram having a single predominant endotherm within the range of 144.01 to 146.92° C. at a scan rate of 10° C. per minute, substantially as shown in FIG. 3.2.
地址 Florham Park NJ US