- Heterocyclic kinase inhibitor
-
The invention belongs to the technical field of medicines, and particularly relates to a heterocyclic DNA-PK kinase inhibitor compound shown as a general formula (I), a pharmaceutically acceptable salt and an isomer thereof, a pharmaceutical composition and preparation containing the compound, the pharmaceutically acceptable salt and the isomer thereof, a method for preparing the compound, the pharmaceutically acceptable salt and the isomer thereof, and application of the compound, the pharmaceutically acceptable salt and the isomer thereof.
- -
-
Paragraph 0499-0502
(2021/03/31)
-
- ARYL-BIPYRIDINE AMINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
-
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I): wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.
- -
-
-
- BENZENESULFONAMIDES USEFUL AS SODIUM CHANNEL INHIBITORS
-
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I), or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3a, R3b and R4 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
- -
-
-
- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
-
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
- -
-
Page/Page column 106
(2014/01/18)
-
- Human carbonic anhydrase II as host protein for the creation of artificial metalloenzymes: The asymmetric transfer hydrogenation of imines
-
In the presence of human carbonic anhydrase II, aryl-sulfonamide-bearing IrCp* pianostool complexes catalyze the asymmetric transfer hydrogenation of imines. Critical cofactor-protein interactions revealed by the X-ray structure of [(η5-Cp*)Ir(pico 4)Cl] 9 WT hCA II were genetically optimized to improve the catalytic performance of the artificial metalloenzyme (68% ee, kcat/KM 6.11 × 10 -3 min-1 mM-1).
- Monnard, Fabien W.,Nogueira, Elisa S.,Heinisch, Tillmann,Schirmer, Tilman,Ward, Thomas R.
-
p. 3269 - 3274
(2013/07/26)
-
- 7,9-Dihydro-Purin-8-One and Related Analogs as HSP90-Inhibitors
-
The invention relates in general to 7,9-dihydro-purin-8-one and related compounds that show broad utility, e.g., in inhibiting heat shock protein 90 (HSP90) to thereby treat or prevent HSP90-mediated diseases.
- -
-
Page/Page column 43-44
(2008/06/13)
-
- 5-AMINO-4-HYDROXY-7-(1H-INDOLMETHYL)-8-METHYLNONAMIDE DERIVATIVES AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION
-
The application relatés to novel alkanamides of the general formula (I) where X is -CH2- or >CH-OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4 is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted aryl-C1-C6-alkyl; R5 is Cl-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy- C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6-alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-Cl-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C-C1-C6-alkyl, C1-C6-alkyl-O-(O)C-C1-C6-alkyl, H2N-C(O)-C1-C6-alkyl, C1-C6-alkyl-HN-C(O)-C1-C6-alkyl, (C1,-C6-alkyl)2N-C(O)-C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-Cl-C6-alkyl, optionally substituted aryl--Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6-alkyl or optionally substituted heterocydyl-Co-C6-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.
- -
-
Page/Page column 30
(2008/06/13)
-
- ORGANIC COMPOUNDS
-
The invention relates to novel amino alcohols of the general formula (I) where X, R1, R2, R3, R4, R5 and R6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
- -
-
Page/Page column 38-39
(2010/02/14)
-