40-O-(2-HYDROXY)ETHYLRAPAMYCIN IN CRYSTALLINE NONSOLVATED FORM, PHARMACEUTICAL COMPOSITION COMPRISING SUCH MACROLIDE AS ACTIVE SUBSTANCE AND METHOD FOR ITS PREPARING Russian patent published in 2005 - IPC

FIELD: organic chemistry, antibiotics, pharmacy.

SUBSTANCE: invention relates to a new crystalline nonsolvated form of 40-O-(2-hydroxy)-ethylrapamycin that shows crystalline lattice with the following parameters: a = 14.37Å; b = 11.24Å; c = 18.31 Å, and volume value is 2805Å. Also, invention relates to a method for preparing this crystalline form that involves crystallization of 40-O-(2-hydroxy)ethylrapamycin from a solvent with mixture with aliphatic hydrocarbon of the formula C_nH_2n+2 wherein n = 5, 6 or 7. Also, invention relates to a pharmaceutical composition based on thereof and its using in preparing medicinal agents used in treatment or prophylaxis of organ or tissue transplant rejection, autoimmune, inflammatory states, asthma, proliferative disorders, tumor or hyperproliferative vascular diseases. Invention provides preparing the novel crystalline nonsolvated form of 40-O-(2-hydroxy)ethylrapamycin possessing immunosuppressive properties.

EFFECT: improved preparing method, improved and valuable medicinal properties of compound and composition.

7 cl, 2 ex