117411-40-2Relevant academic research and scientific papers
Asymmetric synthesis of a xanthine dehydrogenase inhibitor (S)-(-)-BOF-4272 : Mechanism of chiral diaryl sulfoxide formation
Hashimoto, Kinji,Matsugi, Masato,Fukuda, Norio,Kurogi, Yasuhisa
, p. 305 - 315 (2007/10/03)
A pyrazolotriazine derivative (BOF-4272), a potent xanthine dehydrogenase inhibitor, was synthesized in good yield via 9 steps from vanillin. The asymmetric synthesis was achieved effectively by a modified Oae's asymmetric oxidation of diaryl sulfide. A m
Pyrimidine derivatives, method of manufacturing the same, and androgen inhibitor
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, (2008/06/13)
The invention discloses a pyrimidien derivative expressed in Formula [I]: STR1 where R 1 denotes a hydrogen atom or hydroxyl group, R 2 denotes a hydrogen atom, lower alkoxycarbonyl group, lower alkoxy group, halogen atom, lower alkyl group, cycloalkyl group with 3 to 8 carbon atoms, lower alkoxycarbonyl lower alkyl group, carboxyl group, carboxy lower alkyl group, group: --CONHR 6 (R 6 represents a hydrogen atom, a phenyl group, which may possess halogen atom, or lower alkyl group), cyano group, phenyl group which may possess a group selected from the group consisting of hydroxyl group, halogen atom, lower alkyl group, lower alkoxy group and phenylthio group as a substituent, phenyl lower alkyl group which may possess a group selected from the group consisting of hydroxyl group and lower alkoxy group as a substituent on a phenyl ring, lower alkanoyloxy lower alkyl group, benzoyl group, lower alkanoyl group which may possess a halogen atom, or hydroxy lower alkyl group which may possess a group selected from the group consisting of phenyl group and halogen atom as a substituent, R 3 denotes a hydrogen atom, hydroxyl group, lower alkyl group, cycloalkyl group with 3 to 8 carbon atoms, halogen lower alkyl group, or phenyl group, R 4 denotes a hydrogen atom, lower alkyl group, or lower alkoxy group, and R 5 denotes a hydrogen atom, lower alkyl group, lower alkoxy lower alkyl group, or halogen lower alkyl group; provided that R 2 and R 3 may be bonded to each other to form a lower alkylene group with 3 to 5 carbon atoms, or its pharmaceutically available salt. This derivative is excellent in therapeutic effects of benign prostatic hypertrophy, prostatic carcinoma, female hairiness, male baldness or pimple as an androgen inhibitor.
Pyrazolotriazine compounds
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, (2008/06/13)
Pyrazolotriazine compounds of the formula: STR1 wherein R1 is OH or alkanoyloxy; R2 is H, OH, or SH; R3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) STR2 R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) STR3 or (xx) STR4 (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.
