124467-36-3Relevant articles and documents
SHP2 INHIBITORS, COMPOSITIONS AND USES THEREOF
-
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 of 2-chloro-7, 8-dihydro-6H-quinolin-5-ketone
-
, (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
-
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
-
, (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
-
, (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
-
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.
SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF
-
Page/Page column 30, (2009/03/07)
Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5a receptor modulators, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, immune and inflammatory diseases and conditions, are disclosed.
Positive and negative modulation of group I metabotropic glutamate receptors
Vanejevs, Maksims,Jatzke, Claudia,Renner, Steffen,Müller, Sibylle,Hechenberger, Mirko,Bauer, Tanja,Klochkova, Anna,Pyatkin, Ilya,Kazyulkin, Denis,Aksenova, Elena,Shulepin, Sergey,Timonina, Olga,Haasis, Ariane,Gutcaits, Aleksandrs,Parsons, Christopher G.,Kauss, Valerjans,Weil, Tanja
, p. 634 - 647 (2008/09/19)
A discriminating pharmacophore model for noncompetitive metabotropic glutamate receptor antagonists of subtype 1 (mGluR1) was developed that facilitated the discovery of moderately active mGluR1 antagonists. One scaffold was selected for the design of sev
Substituted diazepan orexin receptor antagonists
-
Page/Page column 21, (2008/12/05)
The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.