- ACSS2 INHIBITORS AND METHODS OF USE THEREOF
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The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoho
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Paragraph 0033
(2019/06/09)
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- Alkoxypyrazoles and the process for their preparation
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The present invention relates to a process for the preparation of alkoxypyrazoles and new alkoxypyrazole compounds.
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Page/Page column 15; 17
(2010/03/02)
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- 5-Iodo-3-ethoxypyrazoles: An entry point to new chemical entities
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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.
- Guillou, Sandrine,Janin, Yves L.
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experimental part
p. 4669 - 4677
(2010/08/06)
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- PYRAZOLE DERIVATIVES AS ANTI-PLATELET AND ANTI-THROMBOTIC AGENTS
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This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.
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Page/Page column 30
(2010/11/30)
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- DRUGS COMPRISING COMBINATION OF ANTITHROMBOTIC AGENT WITH PYRAZOLONE DERIVATIVE
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It is intended to provide drugs for treating and/or preventing ischemic diseases which are safe and have little side effects. Namely, drugs comprising a combination of an antithrombotic agent and a pyrazolone derivative defined in the description or its pharmaceutically acceptable salt.
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- Solid-phase synthesis of substituted pyrazolones from polymer-bound β-keto esters
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Polymer-bound acetoacetate 3 was γ-mono- and γ-dialkylated, as well as α-monoalkylated, to give 6, 9, and 13, respectively. Treatment with hydrazine or substituted hydrazines followed by thermal or acidic cyclizing cleavage yielded the pyrazolones 17a-dd in a purity of >90%.
- Tietze, Lutz F.,Evers, Holger,Hippe, Thomas,Steinmetz, Adrian,T?pken, Enno
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p. 1631 - 1634
(2007/10/03)
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- 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof
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2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
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