15450-69-8Relevant articles and documents
Carbon transfer reactions of functionalized oxazolidines and their open chain enamine tautomers to enamine nucleophiles. A facile synthesis of substituted pyridines and ring annulated derivatives
Singh, Kamaljit,Singh, Jasbir,Singh, Harjit
, p. 935 - 942 (1998)
Oxazolidines substituted at C-2 with -CH2-EW(-CO-, etc.) and capable of existing as ring-chain (enamine) tautomers react with cyclic, acyclic and heterocyclic enamine derivatives in a 1:1 stoi-chiometric manner to provide a versatile synthesis of substituted pyridines and their ring annulated derivatives.
TRICYCLIC SULFONES AS ROR GAMMA MODULATORS
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Page/Page column 16, (2021/07/31)
There are described ROR? modulators of the formula (I), or stereoisomers, pharmaceutically acceptable salts thereof, wherein all substituents are defined herein.
SHP2 INHIBITORS, COMPOSITIONS AND USES THEREOF
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Page/Page column 108-109, (2021/12/30)
Provided are compounds of Formula (I), methods of using the compounds as SHP2 inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating SHP2-mediated diseases.
Preparation method and intermediate of hexahydroquinolinedione compound
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Paragraph 0054; 0062-0065, (2020/02/29)
The invention discloses a preparation method and an intermediate of a hexahydroquinolinedione compound. A compound represented by formula I undergoes a hydrolysis reaction shown in the description inthe presence of an acid to obtain the compound represent
Preparation method of 2-chloro-7, 8-dihydro-6H-quinolin-5-ketone
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Paragraph 0056; 0066-0072, (2018/07/30)
The invention relates to a preparation method of 2-chloro-7, 8-dihydro-6H-quinolin-5-ketone. 2-chloro-7, 8-dihydro-6H-quinolin-5-ketone comprises preparation components of a component as shown in thedescription, anhydrous ethanol, anhydrous ammonium acetate, anhydrous sodium carbonate, methyl acrylate, DMF, acetonitrile, phosphorus oxychloride and ethyl acetate, and by adopting the preparation method, the existing situation of g-class production is overcome, so that the technical level reaches the industry leading position. Furthermore, the optimized process enables the order batch output ofa project to reach 15 kg, the product quality is improved obviously, the product purity reaches 99.5%, single impurities are lower than 0.1%, and heavy metal, burning residues and residual solvents meet the standards of pharmacopoeia. Technically, the process is optimized, therefore the overall yield of the process is increased by 30%, and the discharge of three wastes (waste water, waste gas andwaste residues) is reduced through the recovery of the solvents.
HETEROARYLCARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
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Page/Page column 65, (2017/05/21)
The present invention relates to compounds of general formula I, wherein D1 to D3, A, R1, R2, Y and n are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of pl
SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS
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Page/Page column 52; 53, (2016/12/07)
The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These co
Novel 5-aminotetrahydroquinoline-2-carboxylic acids and their use
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Paragraph 0365; 0366; 0367, (2014/02/16)
The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.
HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS
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Page/Page column 75, (2012/04/05)
The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency
Stachel, Shawn J.,Steele, Thomas G.,Petrocchi, Alessia,Haugabook, Sharie J.,McGaughey, Georgia,Katharine Holloway,Allison, Timothy,Munshi, Sanjeev,Zuck, Paul,Colussi, Dennis,Tugasheva, Katherine,Wolfe, Abigail,Graham, Samuel L.,Vacca, Joseph P.
scheme or table, p. 240 - 244 (2012/03/10)
We have developed a novel series of pyrrolidine derived BACE-1 inhibitors. The potency of the weak initial lead structure was enhanced using library-based SAR methods. The series was then further advanced by rational design while maintaining a minimal ligand binding efficiency threshold. Ultimately, the co-crystal structure was obtained revealing that these inhibitors interacted with the enzyme in a unique fashion. In all, the potency of the series was enhanced by 4 orders of magnitude from the HTS lead with concomitant increases in physical properties needed for series advancement. The progression of these developments in a systematic fashion is described.