372-37-2Relevant academic research and scientific papers
INHIBITORS OF LEUCINE RICH REPEAT KINASE 2
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Page/Page column 115, (2019/02/02)
The present invention relates to novel compounds that inhibit LRRK2 kinase activity, to processes for their preparation, to compositions containing them and to their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM
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Page/Page column 84-85, (2020/01/08)
The invention provides novel compounds having the general formula (I) or (II) wherein R2, R3, R5, R99, W, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.
Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
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Page/Page column 149; 150; 151; 152, (2016/09/26)
The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
Preparation of fluorine-containing methyl or aryl alkyl ketone method
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Paragraph 0094, (2016/10/07)
The invention discloses a method for preparing fluorine-containing methyl or alkylaryl ketones, belonging to an organic synthesis field. The method comprises two steps of: ester condensation: ester condensation reaction of an R1COOR2 compound represented by a formula A with a R2COOR2 compound represented by a formula B, is performed to form an R1COCH(R3)COOR2 intermediate represented by a formula C; and ester interchange: R1COCH(R3)COOR2 represented by the formula C is carried out ester interchange reaction with R2COOH under 100-110 DEG C and with catalysis of dilute H2SO4 or a cationic resin, and then decarboxylating to obtain R1COR2 fluorine-containing methyl or alkylaryl ketones represented by a formula D. The R1 group may be CF3-, CF2-, CF- or Ar-; the R2 group may be CH3-, Et- and n-Pr; and the R3 group may be CH3-, Et- and H-. Ester interchange in the invention avoids formation of HOR2 which has a nearly same boiling point with the compound represented by the formula D and is azeotropic with the compound represented by the formula D, enables the compound represented by the formula D to be purified without series rectification operation, and is suitable for large scale production. Simultaneously, ester interchange in the invention greatly raises cost. An ion exchange resin completes ester interchange in a waterless condition, which avoids a de-watering step, and simplifies technologies.
SUBSTITUTED 5-METHYL-[1, 2, 4] TRIAZOLO [1,5-A) PYRIMIDIN-2-AMINE COMPOUNDS AS PDE2 INHIBITORS
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Page/Page column 49, (2016/06/01)
The invention provides a chemical entity of Formula (I): (I), wherein R1, R2, R3, and R4, have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma- dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.
SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS
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Page/Page column 176, (2010/04/03)
The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
