148214-90-8Relevant articles and documents
Guanidine derivative and application thereof
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Paragraph 0307; 0309-0312, (2020/06/09)
The invention relates to a guanidine derivative serving as a VAP-1 inhibitor and application of the guanidine derivative, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be us
FGFR4 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0412-0413, (2019/10/10)
Provided are a class of compounds as shown in formula (I) as FGFR4 inhibitors, and pharmaceutically acceptable salts thereof, preparation methods therefor and the use thereof in the preparation of drugs for treating FGFR4-related diseases.
NOVEL HETEROCYCLIC COMPOUNDS AS IRAK4 INHIBITORS
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Page/Page column 33, (2019/06/23)
The present invention relates to novel compounds of the general formula (I) their tautomeric forms, their enantiomers, their diastereoisomers, their pharmaceutically accepted salts, or pro-drugs thereof, which are useful for the treatment or prevention of cancer and inflammatory diseases associated with Interleukin-1 Receptor Associated Kinase (IRAK), and more particularly compounds that modulate the function of IRAK4.
Tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use
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Paragraph 0210; 0212, (2018/03/24)
The invention relates to a tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use. The tetrahydroisoquinoline compound is shown by the general formula (1). In the general formula (1), the symbols have the same definitions as in the specification.
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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Page/Page column 157, (2018/06/30)
Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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Page/Page column 157, (2017/09/02)
The present disclosure is directed to compounds of formula I and methods of their use and preparation, as well as compositions comprising compounds of formula I.
Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core
Jin, Yonghao,Roycik, Mark D.,Bosco, Dale B.,Cao, Qiang,Constantino, Manuel H.,Schwartz, Martin A.,Sang, Qing-Xiang Amy
, p. 4357 - 4373 (2013/07/19)
New series of pyrrolidine mercaptosulfide, 2-mercaptocyclopentane arylsulfonamide, and 3-mercapto-4-arylsulfonamidopyrrolidine matrix metalloproteinase inhibitors (MMPIs) were designed, synthesized, and evaluated. Exhibiting unique properties over other MMPIs (e.g., hydroxamates), these newly reported compounds are capable of modulating activities of several MMPs in the low nanomolar range, including MMP-2 (~2 to 50 nM), MMP-13 (~2 to 50 nM), and MMP-14 (~4 to 60 nM). Additionally these compounds are selective to intermediate- and deep-pocket MMPs but not shallow-pocketed MMPs (e.g., MMP-1, ~850 to >50 000 nM; MMP-7, ~4000 to >25 000 nM). Our previous work with the mercaptosulfide functionality attached to both cyclopentane and pyrrolidine frameworks demonstrated that the cis-(3S,4R)-stereochemistry was optimal for all of the MMPs tested. However, in our newest compounds an interesting shift of preference to the trans form of the mercaptosulfonamides was observed with increased oxidative stability and biological compatibility. We also report several kinetic and biological characteristics showing that these compounds may be used to probe the mechanistic activities of MMPs in disease.
N -phosphonocarbonylpyrrolidine derivatives of guanine: A new class of Bi-substrate inhibitors of human purine nucleoside phosphorylase
Rejman, Dominik,Panova, Natalya,Klener, Pavel,Maswabi, Bokang,Pohl, Radek,Rosenberg, Ivan
experimental part, p. 1612 - 1621 (2012/05/05)
A complete series of pyrrolidine nucleotides, (3R)- and (3S)-3-(guanin-9-yl)pyrrolidin-1-N-ylcarbonylphosphonic acids and (3S,4R)-, (3R,4S)-, (3S,4S)-, and (3R,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N- ylcarbonylphosphonic acids, were synthesized and e
FUSED HETEROCYCLIC COMPOUND
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, (2011/07/29)
The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.
Highly active organocatalysts for asymmetric anti-mannich reactions
Martín-Rapún, Rafael,Fan, Xinyuan,Sayalero, Sonia,Bahramnejad, Mahboubeh,Cuevas, Félix,Pericàs, Miquel A.
supporting information; scheme or table, p. 8780 - 8783 (2011/09/15)
Lighten the load! A family of enantiopure 4-oxy-substituted 3-aminopyrrolidines arising from the enantioselective ring-opening of meso-3-pyrroline oxide have been developed as catalysts for the asymmetric, anti-selective Mannich reaction (see scheme; PMP=