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Title:
THIENO(2,3-D)PYRIMIDIN-4-ONE DERIVATIVE
Document Type and Number:
Japanese Patent JP3760484
Kind Code:
B2
Abstract:

PURPOSE: To obtain a thieno[2,3-D]phrimidin-4-one derivative useful as treating hypertension, angina pectoris and cardiac insufficiency failure, having inhibitory action on strong cyclic GMP specific phosphodiesterase, comprising a prescribed one skeleton.
CONSTITUTION: This compound is shown by formula I [R1 is a 1-4C alkyl; X is phenoxy, morpholino, piperidino, pyrrolidino, 4-carbethoxypiperidino, 4-(2- hydroxyethyl)piperazino or R2R3N (R2 and R3 are each H, a 1-4C alkyl or a 2-4C hydroxyalkyl)] such as 4-methyl-2-(5-nitro-2-propoxybenzoylamido) thiophene-3-carboxamide. For example, the compound is preferably obtained by reacting a 2-aminothiophene-3-carboxamide of formula II with a compound of formula III in the presence of a base such as triethylamine in an organic solvent such as N,N-dimethylformamide at 0°C to the reflux temperature and treating the prepared compound of formula IV with a base such as NaOH.


Inventors:
Tomomi Ota
Minoru Taguchi
Yutaka Kawashima
Hatayama Katsuo
Application Number:
JP17974295A
Publication Date:
March 29, 2006
Filing Date:
July 17, 1995
Export Citation:
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Assignee:
Taisho Pharmaceutical Co., Ltd.
International Classes:
C07D495/04; A61K31/505; A61K31/519; A61K31/535; A61P3/00; A61P9/00; A61P9/04; A61P9/08; A61P9/10; A61P9/12; A61P11/00; A61P11/02; A61P11/06; A61P17/00; A61P27/16; A61P37/08; A61P43/00; (IPC1-7): C07D495/04; A61K31/505; A61K31/505; A61K31/505; A61K31/505; A61K31/505; A61K31/505; A61K31/505; A61K31/505; A61K31/535
Domestic Patent References:
JP2056484A
Attorney, Agent or Firm:
Tomizo Kitagawa