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Details for Patent: 5,260,440

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Details for Patent: 5,260,440

Title: Pyrimidine derivatives
Abstract:The compounds of the present invention inhibit the HMG-CoA reductase, and subsequently suppress the biosynthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.
Inventor(s): Hirai; Kentaro (Kyoto, JP), Ishiba; Teruyuki (Osaka, JP), Koike; Haruo (Kyoto, JP), Watanabe; Masamichi (Shiga, JP)
Assignee: Shionogi Seiyaku Kabushiki Kaisha (Osaka, JP)
Filing Date:Jun 12, 1992
Application Number:07/897,793
Claims:1. A compound represented by the formula (I): ##STR17## wherein R.sup.1 is (1) lower alkyl which may have 1 to 3 substitutents independently selected from the group consisting of halogen, amino, and cyano, (2) C.sub.6 to C.sub.12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano, or (3) C.sub.1 to C.sub.6 lower alkyl substituted by C.sub.6 to C.sub.12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano; R.sup.2 and R.sup.3 each is independently (1) hydrogen, (2) lower alkyl which may have 1 to 3 substituents independently selected from the group consisting of halogen, amino, and cyano, or (3) C.sub.6 to C.sub.12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano; R.sup.4 is (1) hydrogen, (2) lower alkyl, or a cation capable of forming a non-toxic pharmaceutically acceptable salt; X is sulfur, oxygen, or sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino; the dotted line represents the presence or absence of a double bond, or the corresponding ring-closed lactone.

2. The compound claimed in claim 1, wherein X is imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, or sulfonyl substituted by alkyl, amino or alkylamino.

3. The compound claimed in claim 2, wherein X is imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, alkylsulfonylamino, or alkylsulfonyl.

4. The compound claimed in claim 1 having the (3R, 5S)-dihydroxy configuration.

5. A pharmaceutical composition comprising an effective amount of the compound claimed in claim 1 as an active ingredient, in combination with a pharmaceutical excipient.
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