1207431-89-7Relevant academic research and scientific papers
Novel Compounds as Autotaxin Inhibitors and Pharmaceutical Compositions Comprising the Same
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Paragraph 1161-1162; 1167-1168, (2018/05/17)
The present invention relates to a novel autotaxin inhibitor compound for preventing and treating disease or symptoms due to an increase in concentration of lysophosphatidic acid or activation of autotaxin. The present invention further relates to a pharmaceutical composition containing the same. The novel compound of the present invention is an autotaxin inhibitor which inhibits production of lysophosphatidic acid, and thus is useful for treating or preventing cardiovascular disease, cancer, metabolic disease, kidney disease, liver disease, inflammatory diseases, nervous disease, respiratory disease, desmoid disease, eye disease, cholestatic symptoms, other types of chronic pruritus or acute, or chronic rejection of transplanted organs.COPYRIGHT KIPO 2017
Alkoxypyrazoles and the process for their preparation
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Page/Page column 8; 12, (2010/03/02)
The present invention relates to a process for the preparation of alkoxypyrazoles and new alkoxypyrazole compounds.
5-Iodo-3-ethoxypyrazoles: An entry point to new chemical entities
Guillou, Sandrine,Janin, Yves L.
experimental part, p. 4669 - 4677 (2010/08/06)
Our program, which has focused on the preparation of new pyrazole derivatives, has led us to report here an original and simplified preparation of ethyl 3-ethoxy-lW-pyrazole-4-carboxylate. This is based on the reaction of hydrazine monohydrochloride and diethyl 2-(ethoxymethylene)malonate. Further transformations of this key compound allowed the preparation of the two possible iodinated isomers, namely, 3-ethoxy-4-iodo- and 3-ethoxy-5-iodo-1H-pyrazole. These compounds have opened the way to a quick access to many original pyrazole series. As an illustration, we report here on the selectivity of N-arylation, by using the Lam and Cham method, the C4- and C5-arylation of some of these 3-ethoxy-pyrazole derivatives by using the Suzuki-Miyaura reaction, and C5-benzylation reactions by means of the Negishi reaction. This was followed by hydrolysis of the ethoxy group, which led to the corresponding pyrazol-3-one derivatives. As a conclusion of this work, we conducted an investigation into the regiochemistry of the condensation between diethyl 2-(ethoxymethylene) malonate and the hydrochloride salts of methyl, benzyl, or phenyl hydrazine.
