- Pyridine N-oxidation derivative as well as preparation method and application thereof
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The invention relates to a pyridine N-oxidation derivative as well as a preparation method and an application thereof, in particular to a compound shown in a general formula (I), a preparation methodof the compound, pharmaceutical composition containing the compound and an application of the compound as a BRD4 inhibitor in treating related diseases such as cancer, inflammation, chronic liver diseases, diabetes, cardiovascular diseases, AIDS and the like, wherein in the general formula (I), all substituent groups are the same as definitions in the description.
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Paragraph 1273-1279
(2019/08/06)
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- 2 - - 2, 3 - Dihydrobenzofuran compounds 3 - halomethyl [...] compound and method of manufacturing (by machine translation)
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[Problem] under mild conditions (temperature, such as reagents and solvents), reaction can be effectively suppressed, and the reagent and the solvent to be used can be also suppressed, the safety can be enhanced and increased productivity in industrial production, production of compound 2 - [...], and excellent in the manufacturing and 3 - halomethyl - 2, 3 - dihydrobenzofuran compound. (2) A compound represented by the following formula [a], metal M1 , Metal M1 Metal salt, or an organic metal compound M2 The reaction, (1) a compound represented by formula a, - 2, 3 - dihydrobenzofuran (2) is represented by formula 2 - production of compound 3 - halomethyl [...] and compound. [1 A] In the formulas, R1 - R4 Each independently represents a substituent, X is a chlorine atom, a bromine atom or an iodine atom. [Drawing] no (by machine translation)
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Paragraph 0146-0148
(2018/04/11)
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- 5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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Page/Page column 45-46
(2011/02/24)
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- NEW COMPOUNDS 574
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome,
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Page/Page column 25
(2010/06/13)
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- PROCESS FOR PRODUCING CYCLOPROPYLPHENOL DERIVATIVE
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A method of easily synthesizing a cyclopropylphenol derivative. The method, which is a process for producing a cyclopropylphenol derivative represented by the general formula (10): [wherein R1, R2, R3, and R4 each independently is hydrogen, etc.; Z is hydrogen, etc.; and Y1, Y2, and Y3 each independently is hydrogen, etc.], comprises reacting a compound represented by the general formula (7): [wherein the symbols have the same meanings as defined above; X is halogeno; and V is hydrogen, etc.] with a metal, metal salt, or organometallic compound represented by the general formula M2 (8) to obtain a compound represented by the general formula (9): [wherein the symbols have the same meanings as defined above]. When V is a -W-R5 group, hydrolysis is further conducted. Thus, a compound of the general formula (10) is obtained.
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Page/Page column 84
(2008/06/13)
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