- TISSUE FACTOR PRODUCTION INHIBITOR
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A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.
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Page/Page column 112
(2010/11/26)
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- BENZENE COMPOUND HAVING 2 OR MORE SUBSTITUENTS
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A superior LXR modulator is provided. A compound represented by the general formula (I): [wherein R1: -COR9 (wherein R9: alkyl, optionally substituted alkoxy or optionally substituted amino); R2: H, OH, alkoxy, optionally substituted amino, etc.; R3: H, optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, optionally substituted amino, halogeno, etc.; R4 and R5: H, optionally substituted alkyl, halogeno, etc.; R6 and R7: H, alkyl; R8: -X2R10 [wherein R10: -COR11 (wherein R11 : OH, optionally substituted alkoxy, optionally substituted amino, etc.), -SO2R12 (wherein R12: optionally substituted alkyl, optionally substituted amino, etc.), tetrazol-5-yl, etc.; X2: single bond, optionally substituted alkylene, etc.]; X1: -NH-, -O-, -S-, etc.; Y1: optionally substituted phenyl, optionally substituted 5- to 6-membered aromatic heterocyclyl; Y2: optionally substituted aryl, optionally substituted heterocyclyl, etc.] and the like is provided.
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- BENZENE COMPOUND HAVING 2 OR MORE SUBSTITUENTS
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Disclosed is an excellent LXR modulator. Specifically disclosed is a compound represented by the general formula (I) below or the like. (I) [In the formula, R1 represents a -COR9 (wherein R9 represents an alkyl, optionally substituted alkoxy or optionally substituted amino); R2 represents an H, OH, alkoxy, optionally substituted amino or the like; R3 represents an H, optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, optionally substituted amino, halogeno or the like; R4 and R5 respectively represent an H, optionally substituted alkyl, halogeno or the like; R6 and R7 respectively represent an H or alkyl; R8 represents a -X2R10 [wherein R10 represents a -COR11 (wherein R11 represents an OH, optionally substituted alkoxy, optionally substituted amino or the like), -SO2R12 (wherein R12 represents an optionally substituted alkyl, optionally substituted amino or the like), tetrazole-5-yl or the like; and X2 represents a single bond, optionally substituted alkylene or the like]; X1 represents an -NH-, -O-, -S- or the like; Y1 represents an optionally substituted phenyl or optionally substituted 5-membered or 6-membered aromatic heterocyclyl; and Y2 represents an optionally substituted aryl, substituted heterocyclyl or the like.]
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Page/Page column 231-232
(2010/11/08)
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- Approach to the synthesis of candelabrone and synthesis of 3,7-diketo-12-hydroxyabieta-8,11,13-triene
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An approach to the synthesis of aromatic diterpenes was tested for its generality.Phenylacetonitriles with increasing substitution on the aromatic ring were prepared and alkylated with geranyl bromide and the resulting dienes subjected to cationic cycliza
- Burnell, Robert H.,Caron, Stephane
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p. 1446 - 1454
(2007/10/02)
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- Synthesis of aromatic diterpenes synthesis of 12-hydroxy-abieta-8,11,13-trien-3,7-dione
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Model studies involving cationic cyclisation of suitable dienes have provided a synthesis of the title compound. Preparation of the dienes from available aromatic starting materials and the modification of the cyclised products are described.
- Burnell,Caron
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p. 127 - 132
(2007/10/02)
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- CARBAMYLPIPERAZINE COMPOUNDS
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4-(3-Aryloxy-2-hydroxypropyl)piperazines bearing a carbamyl group in the 1-position are β-adrenergic blockers. A typical example is 1-carbamyl-4-{3-2-allyl-3-(2-carbethoxyaminoethyl)phenoxy!-2-hydroxypropyl} piperazine.
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