PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION

WIPO Patent Application WO/1994/026721

A1

A pyrimidine derivative having an angiotensin (II) antagonism and represented by general formula (I), wherein A represents (I-1) or (I-2), R1 and R2 represent each hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, halogen or optionally substituted phenyl; R3 and R4 represent each hydrogen, alkyl, alkoxy, halogen, nitro, sulfone, carboxy, alkoxycarbonyl, cycloalkoxycarbonyloxyalkoxycarbonyl, alkanoyloxy alkoxycarbonyl or optionally protected tetrazolyl, or R3 and R4 may be combined together to form a fused 5- or 6-membered ring which may be substituted; X represents O, NH or S(O)p; p represents an integer of 0 to 2; m represents 1 or 2; B represents carboxy, alkoxycarbonyl or optionally protected tetrazolyl; and n represents 1 or 2.

MINEGISHI TORATARO (JP)
OHKUBO AKIHIRO (JP)
SHIMOYAMA IZUMI (JP)
NAGANO HIDEKI (JP)
IIDA SHIGEO (JP)
SATO HIROAKI (JP)
SHIRAKAMI YOSHIKO (JP)
MIZUTA TADASHI (JP)

PCT/JP1994/000764

November 24, 1994

May 12, 1994

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NIPPON KOKAN KK (JP)
MINEGISHI TORATARO (JP)
OHKUBO AKIHIRO (JP)
SHIMOYAMA IZUMI (JP)
NAGANO HIDEKI (JP)
IIDA SHIGEO (JP)
SATO HIROAKI (JP)
SHIRAKAMI YOSHIKO (JP)
MIZUTA TADASHI (JP)

C07D239/34; C07D239/36; C07D403/10; C07D403/12; C07D403/14; (IPC1-7): C07D239/36; A61K31/505; C07D239/40; C07D239/42

J. MED. CHEM., Vol. 35, No. 25, (1992), KARNAIL S. ATWAL et al., "Dihydropyrimidine Angiotensin II Receptor Antagonists", p. 4751-4763.
J. MED. CHEM., Vol. 35, No. 20, (1992), B. DE et al., "Discovery of a Novel Class of Orally Active, Non-Peptide Angiotensin II Antagonists", p. 3714-3717.

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