320581-09-7Relevant academic research and scientific papers
Tricyclic compound, pharmaceutical composition and application thereof
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Paragraph 0135; 0140-0142, (2021/08/07)
The present invention provides a tricyclic compound, an isomer thereof, a pharmaceutically acceptable salt, a pharmaceutical composition and an application thereof. The tricyclic compound has a structure represented by formula I, has a significant effect of inhibiting RET kinase activity, can effectively inhibit cancer cell proliferation, can be used as an RET kinase inhibitor, can be used for preparing medicines for treating RET kinase-mediated diseases, has a good treatment effect on RET kinase-mediated cancers and other diseases, and has a wide application prospect.
ALKYLBORONIC ACIDS AS ARGINASE INHIBITORS
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, (2020/08/22)
Provided are alkylboronic acids as arginase inhibitors represented by formula (I), or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof and a pharmaceutical composition comprising said compounds.
HETEROCYCLIC COMPOUNDS AS ARGINASE INHIBITORS
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, (2019/07/13)
The present invention relates to heterocyclic compounds as arginase inhibitors, in particular to a compound represented by Formula (I), or a pharmaceutically acceptable salt, stereoisomer or tautomer, or prodrug thereof and a pharmaceutical composition comprising said compound.
allah Geleg sandbank method for the preparation of intermediates
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Paragraph 0030; 0031, (2017/02/24)
The invention relates to a preparation method of Anagliptin intermediates (2-amino-2-methyl-propyl)-benzyl carbamate and (2-amino-1, 1-dimethyl-ethyl)-tert-butyl carbamate, wherein the preparation method is short in reaction period, simple to operate, eas
Influence of achiral units with gem-dimethyl substituents on the helical character of aliphatic oligourea foldamers
Fremaux, Juliette,Dolain, Christel,Kauffmann, Brice,Clayden, Jonathan,Guichard, Gilles
, p. 7415 - 7417 (2013/09/23)
The structures of various urea oligomers incorporating one or two central achiral 1,2-diamino-1,1-dimethylethane (DADME) units have been investigated in solution and in the crystalline state. These diamine monomers are analogous to the achiral helicogenic
Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 2: α-Branched quaternary amines
Hunt, Thomas,Atherton-Watson, Hazel C.,Collingwood, Stephen P.,Coote, Kevin J.,Czarnecki, Sarah,Danahay, Henry,Howsham, Catherine,Hunt, Peter,Paisley, Derek,Young, Alice
, p. 2877 - 2879 (2012/05/20)
We report the synthesis and biological evaluation of a series of novel α-branched pyrazinoyl quaternary amines for their ability to block ion transport via the epithelial sodium channel (ENaC) in human bronchial epithelial cells (HBECs). Compound 12g has an IC50 of 30 nM and is highly efficacious in the Guinea-pig tracheal potential difference (TPD) model of ENaC blockade with an ED50 of 1 μg kg-1 at 1 h. In addition the SAR results demonstrate for the first time the chiral nature of the binding site of human ENaC. As such, pyrazinoyl quaternary amines represent a promising new class of ENaC blockers for the treatment of cystic fibrosis that are structurally distinct from the pyrazinoyl guanidine chemotype found in prototypical ENaC blockers such as amiloride.
A nonpeptidic reverse-turn scaffold stabilized by urea-based dual intramolecular hydrogen bonding
Medda, Amiya K.,Park, Chul Min,Jeon, Aram,Kim, Hyunwoo,Sohn, Jeong-Hun,Lee, Hee-Seung
supporting information; experimental part, p. 3486 - 3489 (2011/09/12)
A novel nonpeptidic reverse-turn scaffold containing urea fragments that are connected by a conformationally constrained d-prolyl-cis-1,2- diaminocyclohexane (d-Pro-DACH) linker is reported. The scaffold adopts a well-defined reverse-turn conformation tha
Isoselenocyanates derived from Boc/Z-amino acids: Synthesis, isolation, characterization, and application to the efficient synthesis of unsymmetrical selenoureas and selenoureidopeptidomimetics
Chennakrishnareddy, Gundala,Nagendra, Govindappa,Hemantha, Hosahalli P.,Das, Ushati,Guru Row, Tayur N.,Sureshbabu, Vommina V.
supporting information; experimental part, p. 6718 - 6724 (2010/09/30)
Isoselenocyanates derived from Boc/Z-amino acids are prepared by the reaction of the corresponding isonitriles with selenium powder in presence of triethylamine at reflux. The utility of these new classes of isoselenocyanates in the preparation of selenoureidodipeptidomimetics possessing both amino as well as carboxy termini has been accomplished. The 1H NMR analysis confirmed that the protocol involving the conversion of isonitriles to isoselenocyanates and their use as coupling agents in assembling selenoureido derivatives is free from racemization.
