Title:
CARBAMATE OF RAPAMYCIN
Document Type and Number:
Japanese Patent JP3909870
Kind Code:
B2
Abstract:
PURPOSE: To provide the novel compounds useful as immunosuppressants, anti- inflammatory agents, antifungal agents, antiproliferative agents and antitumor agents.
CONSTITUTION: By protecting an alcoholic site of paramycin with a protective group to convert carbonate and reacting the carbonate with amine or the like to remove the protection according to the scheme of formula IV, the aimed compound of formula I {wherein R1 and R2 are each a hydrogen, a -CONH-[(CR3R4)m(-A-(CR5R6)n]p}q-B, a -CONR9R10 or a group of formula II; R3, R4, R5 and R6 are each a hydrogen, a 1-6C alkyl, an Ar or the like; B represents a 2-7C alkenyl, 1-6C hydroxyalkyl or the like; R7 and R8 are each a 7-10C arylalkyl, 2-12C alkoxyalkyl, an Ar or the like; R9 and R10 are each 2-7C alkinyl, 3-8C cycloalkyl or the like; A represents a -CH2- or -NR-; Ar represents a naphthyl, a pyridyl or the like; a group of formula III represents a (un)saturated nitrogen containing heterocyclic ring or the like; m and n are each of from 0 to 6; p and q are each of 0 or 1}, for example 4-(2-hydroxyethyl) piperadine-1-carboxylic acid, is provided.
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Inventors:
Wenlin Kao
Majid A. Abo-Galvia
Robert El Vogel
Majid A. Abo-Galvia
Robert El Vogel
Application Number:
JP25413293A
Publication Date:
April 25, 2007
Filing Date:
October 12, 1993
Export Citation:
Assignee:
Wyeth
International Classes:
A61K31/435; A61K31/04; C07D498/18; A61K31/395; A61K31/436; A61K31/44; A61K31/675; A61K31/70; A61P9/00; A61P29/00; A61P37/06; C07D221/00; C07D273/00; C07D311/00; C07D487/18; C07D491/06; C07H19/01; C07J1/00; C07D; (IPC1-7): C07D498/18; A61K31/435; A61K31/435; A61K31/435
Domestic Patent References:
| JP62215592A |
Foreign References:
| US5118678 | ||||
| WO1992005179A1 |
Attorney, Agent or Firm:
Aoyama Aoi
Mitsuo Tanaka
Mitsuo Tanaka