Teva Pharmaceutical Industries Limited

Yigael Gozlan

Ben-Zion Dolitzky

Evgeny Shapiro

Ronit Yahalomi

Boaz Gome

Shlomit Wizel

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, &#x3b1;, &#x3b2;, &#x3b3;, &#x3b4;, &#x3b5;, &#x3c3;, &#x3b8; and &#x3a9;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Polymorphic forms of nateglinide

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, &#x3b1;, &#x3b2;, &#x3b3;, &#x3b4;, &#x3b5;, &#x3c3;, &#x3b8; and &#x3a9;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide. Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.

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Ramot Sapir, Israel

Yigael Gozlan