Rapamycin carbonate esters as immunosuppressant agents

Details Rapamycin carbonate esters as immunosuppressant agents Rapamycin carbonate esters as immunosuppressant agents

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/445 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2149669

2149669 9411380 PCTABS00032 Carbonate esters with rapamycin at position 42 or positions 31 and 42 have immunosuppressant properties and are useful in the treatment of transplant rejections and autoimmune diseases. These esters are represented by formula (I), wherein R1 and R2 are independently H or -COOR3 but both R1 and R2 cannot be H, and R3 is C1-C6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C3-C8 cycloalkyl, C2-C6 alkenyl, or Ar-(CH2)n- where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C1-C6 alkyl or C1-C6 alkoxy; pyridinyl, indolyl, quinolyl or furanyl; or a pharmaceutically acceptable salt thereof.

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