Pyrimidine derivatives
DC CAFC
First Claim
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1. A compound represented by the formula (I):
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whereinR1 is (1) lower alkyl which may have 1 to 3 substitutents independently selected from the group consisting of halogen, amino, and cyano, (2) C6 to C12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano, or (3) C1 to C6 lower alkyl substituted by C6 to C12 aromatic group which may have 1 to 3 substituents independently sel-ected from the group consisting of lower alkyl, halo-gen, amino, and cyano;
R2 and R3 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) C6 to C12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano;
R4 is (1) hydro-gen, (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, vale-ryl, isovaleryl, amino substituted by sulfonyl or alkyl-sulfonyl, 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.
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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.
34 Citations
8 Claims
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1. A compound represented by the formula (I):
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wherein R1 is (1) lower alkyl which may have 1 to 3 substitutents independently selected from the group consisting of halogen, amino, and cyano, (2) C6 to C12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano, or (3) C1 to C6 lower alkyl substituted by C6 to C12 aromatic group which may have 1 to 3 substituents independently sel-ected from the group consisting of lower alkyl, halo-gen, amino, and cyano;
R2 and R3 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) C6 to C12 aromatic group which may have 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, amino, and cyano;
R4 is (1) hydro-gen, (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, vale-ryl, isovaleryl, amino substituted by sulfonyl or alkyl-sulfonyl, 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.- View Dependent Claims (2, 3, 4, 5)
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- 6. The compound 7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl)-(3R,5S)-dihydroxy-(E)-6-heptenoic acid in the form of a non-toxic pharmaceutically acceptable salt thereof.
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Litigation Data
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Current AssigneeShionogi Seiyaku Kabushiki Kaisha (Shionogi & Co., Ltd.)
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Original AssigneeShionogi Seiyaku Kabushiki Kaisha (Shionogi & Co., Ltd.)
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InventorsWatanabe, Masamichi, Koike, Haruo, Hirai, Kentaro, Ishiba, Teruyuki
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Primary Examiner(s)Raymond, Richard L.
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Application NumberUS09/141,731Time in Patent Office1,076 DaysField of Search514/756, 544/297US Class Current514/316CPC Class CodesC07D 239/34 One oxygen atomC07D 239/38 One sulfur atomC07D 239/42 One nitrogen atom nitro rad...
