1046478-89-0Relevant academic research and scientific papers
NEW HETEROCYCLIC COMPOUNDS AS MONOACYLGLYCEROL LIPASE INHIBITORS
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Page/Page column 64; 227, (2020/03/05)
The invention provides new heterocyclic compounds having the general formula (I) wherein A, L, X, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds, methods of using the compounds and methods of determining the monoacylglycerol lipase (MAGL) inhibitory activity of the compounds.
NEW HETEROCYCLIC COMPOUNDS AS MONOACYLGLYCEROL LIPASE INHIBITORS
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Page/Page column 235, (2020/03/05)
The invention provides new heterocyclic compounds having the general formula (I) wherein A, L, X, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
4-HETEROARYLCARBONYL-N-(PHENYL OR HETEROARYL) PIPERIDINE-1-CARBOXAMIDES AS INHIBITORS OF TANKYRASES
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Page/Page column 38-39, (2020/07/06)
Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.
Umpolung Difunctionalization of Carbonyls via Visible-Light Photoredox Catalytic Radical-Carbanion Relay
Wang, Shun,Cheng, Bei-Yi,Sr?en, Matea,K?nig, Burkhard
supporting information, p. 7524 - 7531 (2020/08/05)
The combination of photoredox catalysis with the Wolff-Kishner (WK) reaction allows the difunctionalization of carbonyl groups by a radical-carbanion relay sequence (photo-Wolff-Kishner reaction). Photoredox initiated radical addition to N-sulfonylhydrazones yields α-functionalized carbanions following the WK-type mechanism. With sulfur-centered radicals, the carbanions are further functionalized by reaction with electrophiles including CO2 and aldehydes, whereas CF3 radical addition furnishes a wide range of gem-difluoroalkenes through β-fluoride elimination of the generated α-CF3 carbanions. More than 80 substrate examples demonstrate the broad applicability of this reaction sequence. A series of investigations including radical inhibition, deuterium labeling, fluorescence quenching, cyclic voltammetry, and control experiments support the proposed radical-carbanion relay mechanism.
FUSED GLYCOSIDASE INHIBITORS
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Page/Page column 128-129, (2020/09/08)
Compounds of formula (I), wherein A, Z, E, R1, R2, m and n have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
A N - Boc - 4 - piperidine formaldehyde preparation method (by machine translation)
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Paragraph 0019; 0030; 0034-0035; 0039; 0043, (2018/03/26)
The invention discloses a N - Boc - 4 - piperidine formaldehyde preparation method, which belongs to the technical field of organic chemistry. From the N - Boc - 4 - piperidone as the starting point, and the toluene shPs reaction generating diethylketohydrazone, then add the butyl lithium/tetramethyl ethylenediamine/formylation reagent reaction to obtain the 1 - Boc - 4 - formyl - 3, 6 - dihydro - 2 H - pyridine, then palladium carbon to catalyze hydrogenation to obtain N - Boc - 4 - piperidine formaldehyde. The invention has simple operation, higher yield, use of the starting raw material is cheap, is preparing N - Boc - 4 - piperidine formaldehyde suitable method. (by machine translation)
IMIDAZO ISOINDOLE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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Paragraph 0097; 0104; 105; 0116; 0117, (2018/03/25)
The present invention relates to an imidazo isoindole derivative, a preparation method therefor and a medical use thereof. In particular, the present invention relates to the imidazo isoindole derivative as shown in the formula (I), a preparation method and pharmaceutical composition containing the derivative, and a use thereof for treating diseases with the pathological characteristic of IDO-mediated tryptophan metabolic pathways. The diseases comprise cancers, Alzheimer's disease, autoimmune diseases, depression, anxiety disorders, cataracts, psychological disorders and AIDS, wherein the substituents in the formula (I) are the same as those defined in the description.
1,4-DICARBONYL-PIPERIDYL DERIVATIVES
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Page/Page column 58, (2017/07/01)
Compounds of the formula I in which Z, W, Q, R and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
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Paragraph 0297, (2017/09/15)
The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).
Pyrimidine derivative, preparation method therefor and application thereof in medicine
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Paragraph 0204; 0205; 0206; 0207; 0208, (2016/10/07)
The invention relates to a pyrimidine derivative, a preparation method therefor and an application thereof in medicine. Particularly, the invention relates to a compound as shown in general formula (M) or a stereisomer, an aquo-complex, a metabolic product, a solvate, a pharmaceutically acceptable salt, a co-crystallization or a prodrug thereof; the preparation method thereof; and the application of the medicine composition thereof and the compound medicine compound in the medicine, particularly the application as an EGFR target spot inhibitor, wherein the definition of each substituent group in the general formula (M) is the same as that of the specification.
