- Synthetic method 1 - methyl - 111H-indazole -6 - formic acid (by machine translation)
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The invention provides a synthetic method, 1 - methyl - 111H-indazole -6 - formic acid. The synthesis method comprises 2 - fluorine -4 - bromobenzaldehyde and methylhydrazine as a raw material, and after the cyclization reaction is carried out 6 - bromo -1 - methyl indazole, then formate esterification reaction and hydrolysis reaction, and the 1 - methyl - 111H (indazole -6 - formic acid; isomers, and the like 1 are avoided, and the problem that impurities are difficult to remove in follow-up separation is avoided. Not only is the product purity, the yield of ring-forming 85% reaction can also reach the unitunits ?, the yield is higher, the product is suitable for small-scale preparation in laboratories, production, reaction conditions are easy to operate, control, production cost, and large-scale industrial production are facilitated. (by machine translation)
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- HISTONE DEMETHYLASE INHIBITORS
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Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
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Paragraph 00477; 00478
(2014/06/24)
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- ORNITHINE DERIVATIVE
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Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.
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Page/Page column 24; 36
(2010/01/29)
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- SPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating mammals suffering from the condition of being overweight.
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Page/Page column 34
(2008/12/06)
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