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Polymorphic forms of acid 5 - (3,3 - dimethyl - but - 1 - inil) - 3 - (trans-4 - [Cyclohexyl (Hydroxy) - trans - 4 - methyl - ciclohexancarbonil) - amino] - 2 - tiofen - carboxylic acid and its use in the treatment of hepatitis C
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
LUONG HOA Q.,HU KAN,NIAN - LUISI BRIAN,WILLCOX DAVID,ROEPER STEFANIE
申请号:
ARP120102726
公开号:
AR087344A1
申请日:
2012.07.26
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
A method for preparing the polymetallic form of formula compound m (1) comprises stirring a mixture of formula compound (1) and a solvent system, including isopropanol, ethyl acetate, n-butyl acetate, methylacetic acid, acetone, 2-butanone (MEK)),o heptano o una combinaci n de los mismos a una temperatura comprendida entre 10 C y 47 C para formar la Forma M del compuesto de f rmula (1) Un m todo para preparar la Forma polim rfica H del compuesto de f rmula (1) and 70 ° C to form Form H of the compound of formula (1). A method for preparing Form P of the compound of formula (1) includes stirring a mixture of the compound of formula (1) and a solvent system that includes a solvent selected from the group consisting of dichloromethane and tetrahydrofuran (THF)And the P shape of a formula compound (1) is formed by mixing it at ambient temperature. The X-type method for preparing the formula compound (1) includes removing the solution GDE acetate from the formula compound (1). One methodTo prepare the form (1) of formula compound ZA, including the removal of n-butil acetic acid from solvato a of formula compound (1): requirement 1: a structural formula compound (1).wherein the polymorphic form is the polymorphic form M, polymorphic form H, polymorphic form P, polymorphic form X or polymorphic form ZA. Claim 4: The polymorphic form according to claim 2, wherein the polymorphic form M is characterized by having an X-ray powder diffraction pattern with characteristic peaks expressed in 2-q ± 0.2 in the following positions: 19 , 6, 16.6, 18.1, 9.0, 22.2 and 11.4, where the X-ray powder diffraction pattern is obtained at room temperature using CuKa radiation. Claim 11: The polymorphic form according to claim 9,where the polymorphic form H is characterized by having an X-ray powder diffraction pattern with characteristic peaks expressed in 2-q ± 0.2 in the following positions: 6.6, 18.7, 8.5, 17, 3, 15.8 and 19.4, where the X-ray powder diffraction pattern is obtained at room
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