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21. 发明申请

US20050256336A1 Crystal forms of n-(trans-4-isopropylcyclohexylcarbonyl)-d-phenylalanine 失效
标题翻译： n-（反式-4-异丙基环己基羰基）-d-苯丙氨酸的晶型
公开(公告)号：US20050256336A1
公开(公告)日：2005-11-17
申请号：US10510927
申请日：2003-04-14
申请人： Paul Sutton
发明人： Paul Sutton
IPC分类号： A61P3/10 , A61K31/195 , A61K31/198 , C07C231/22 , C07C231/24 , C07C233/63 , C07C235/70
CPC分类号： C07C233/63 , C07B2200/13 , C07C231/22 , C07C2601/14
摘要： New crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine, also known as nateglinide, may be produced by dissolving nateglinide in any of its forms, including solvates, in an organic solvent to form a solution followed by precipitation of nateglinide from the solution, and isolating and drying the precipitated crystal form of nateglinide. The precipitation of nateglinide may be induced either by cooling the solution, or by addition of another solvent which is miscible with the first solvent but in which nateglinide is only poorly soluble, or by combination of the two. Depending on the solvent a specific crystal form of nateglinide may be obtained, e.g., the R′-type crystal form of nateglinide produced by the described method has a different melting point, infra red spectra and X-ray diffraction patterns from the previously known crystal forms of nateglinide.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（也称为那格列奈）的新结晶形式可以通过将那格列奈以任何形式（包括溶剂化物）溶解在有机溶剂中来形成溶液，然后沉淀那格列奈，并分离和干燥那格列奈沉淀的晶体形式。那格列奈的沉淀可以通过冷却溶液，或通过加入与第一溶剂混溶但其中那格列奈仅溶于难溶性的另外的溶剂，或通过两者的组合来诱导。取决于溶剂，可以获得那格列奈的特定结晶形式，例如，通过所述方法制备的那格列奈的R'型晶型具有不同的熔点，红外光谱和来自先前已知的晶体的X射线衍射图那格列奈的形式

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