Title:
【発明の名称】免疫抑制剤としてのラパマイシンの炭酸エステル
Document Type and Number:
Japanese Patent JPH08503210
Kind Code:
A
Abstract:
Carbonate esters with rapamycin at position 42 or positions 31 and 42 have been shown to have immunosuppressant properties and are useful in the treatment of transplant rejections and autoimmune diseases. These esters are represented by the formula below: 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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Inventors:
Hugh, David Chen
Application Number:
JP51207393A
Publication Date:
April 09, 1996
Filing Date:
October 06, 1993
Export Citation:
Assignee:
American Home Products Corporation
International Classes:
A61K31/435; A61K31/445; A61P37/06; C07D498/18; (IPC1-7): C07D498/18; A61K31/435
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)