141699-55-0Relevant articles and documents
Reaction Rates of Various N-Acylenamines in the Inverse-Electron-Demand Diels–Alder Reaction
Engelsma, Sander B.,van den Ende, Thomas C.,Overkleeft, Hermen S.,van der Marel, Gijsbert A.,Filippov, Dmitri V.
, p. 2587 - 2591 (2018)
In light of the bioorthogonal inverse-electron-demand Diels–Alder strategy, an extended investigation into the effects of ring strain and electron inductive effects on the reactivity of the N-acylenamine core towards tetrazine has been carried out. Through a comparative study between N-acylazetines, N-vinylcarbamates and an N-vinylamide it was shown that ring strain has a more significant effect on reaction rate than electron donation. A significantly improved synthetic route is reported for the preparation of an N-acylazetine biorthogonal tag we have invented previously.
BROAD-SPECTRUM CARBAPENEMS
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Page/Page column 00167, (2021/05/29)
The present disclosure provides broad-spectrum carbapenem derivatives and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such derivatives and/or compositions.
PROCESSES OF PREPARING A JAK1 INHIBITOR
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, (2021/12/17)
The present application provides processes for preparing 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H, 1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide, and phosphoric acid salt thereof, which is useful as a selective (Janus kinase 1) JAK1 inhibitor, as well as salt forms and intermediates related thereto.
RET Inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0408-0411, (2021/10/27)
The invention belongs to the field of medicines, and relates to RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prophylaxis of diseases and disorders associated and RET.
A novel RET inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0312-0315, (2021/11/26)
The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. In particular, the invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I said compound and a pharmaceutical composition thereof for the manufacture of a medicament, in particular for the treatment and prophylaxis and RET of diseases and disorders associated with irritable bowel syndrome.
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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Paragraph 0122, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
PROTEIN KINASE INHIBITORS FOR PROMOTING LIVER REGENERATION OR REDUCING OR PREVENTING HEPATOCYTE DEATH
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Page/Page column 116, (2020/02/14)
The invention relates to compounds of formula (I) which are inhibitors of MKK4 (mitogen-activated protein kinase kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The compounds selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7. (I), wherein R x, R y , R z and R zz are selected from: a) R x and R y are F and R z and R zz are H; b) R x, R y and R zz are independently halogen and R z is H; c) R x R z and R zz are independently halogen and R y is H; and d) R x R y and R z are independently halogen and R zz is H
Compound as well as preparation method and medical application thereof
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Paragraph 0444-0446, (2020/02/14)
The invention provides a compound as well as a preparation method and medical application thereof, the compound has a structure as shown in a general formula (I), and can also be a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixture form thereof, or a pharmaceutically acceptable salt thereof. According to the compound with the structure as shown in the general formula (I)provided by the invention, a specific main chain structure and a corresponding substituent group are selected, so that the obtained compound can be used as an arginase inhibitor, is relatively high in activity, and has a potential treatment prospect in various diseases.
3-nitrile methylene azetidine-1-tert-butyl carbonate preparation method
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Page/Page column 8; 15-18, (2020/02/06)
The invention discloses a 3-nitrile methylene azetidine-1-tert-butyl carbonate preparation method, which specifically comprises: 1, synthesizing 1-tert-butyl-3-glycolate; 2, synthesizing N-Boc-3-hydroxy azetidine through the 1-tert-butyl-3-glycolate obtained in the step 1; 3, synthesizing N-Boc-3-azetidinone through the N-Boc-3-hydroxy azetidinone obtained in the step 2; and 4, synthesizing 3-nitrile methylene azetidine-1-tert-butyl carbonate through the N-Boc-3-azetidinone obtained in the step 3. According to the preparation method disclosed by the invention, the existing conventional five-step synthesis process of 3-nitrile methylene azetidine-1-tert-butyl carbonate is reduced into three steps, so that the synthesis time is greatly saved, the emission of three-waste is reduced, and the process cost is reduced.
MERTK DEGRADERS AND USES THEREOF
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Paragraph 00803; 00804, (2020/01/31)
The present invention provides compounds, compositions thereof, and methods of using the same.
