- HERBICIDAL COMPOUNDS
-
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
- -
-
Page/Page column 101-102
(2021/04/02)
-
- tele-Substitution Reactions in the Synthesis of a Promising Class of 1,2,4-Triazolo[4,3- a]pyrazine-Based Antimalarials
-
We have discovered and studied a tele-substitution reaction in a biologically important heterocyclic ring system. Conditions that favor the tele-substitution pathway were identified: the use of increased equivalents of the nucleophile or decreased equivalents of base or the use of softer nucleophiles, less polar solvents, and larger halogens on the electrophile. Using results from X-ray crystallographic and isotope labeling experiments, a mechanism for this unusual transformation is proposed. We focused on this triazolopyrazine as it is the core structure of the in vivo active antiplasmodium compounds of Series 4 of the Open Source Malaria consortium.
- Korsik, Marat,Tse, Edwin G.,Smith, David G.,Lewis, William,Rutledge, Peter J.,Todd, Matthew H.
-
p. 13438 - 13452
(2020/12/15)
-
- Discovery of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing a 4-oxo-pyridazinone moiety as potential c-Met kinase inhibitors
-
Two series of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing 4-oxo-pyridazinone moieties (compounds21a-land22a-l) were designed and their IC50values were evaluated against three cancer cell lines (A549, MCF-7 and HeLa) and c-Met kinase. Among them, the compound with most potential,22i,exhibited excellent anti-tumor activity against A549, MCF-7 and HeLa cancer cell lines with IC50values of 0.83 ± 0.07 μM, 0.15 ± 0.08 μM and 2.85 ± 0.74 μM, respectively, and it also possessed superior c-Met kinase inhibition ability at the nanomolar level (IC50= 48 nM). Moreover, dose-dependent experiments, AO fluorescence staining, cell cycle assay, Annexin V-FITC/PI staining and docking studies were carried out in this study. The results demonstrated that compound22icould be a potential c-Met kinase inhibitor.
- Liu, Xiaobo,Sun, Xin,Xiong, Hehua,Xu, Shan,Yang, Zunhua,Zhang, Binliang,Zhang, Qian,Zheng, Pengwu,Zhu, Wufu
-
p. 9053 - 9063
(2020/06/08)
-
- Preparation and application of triazole heterocyclic compound containing heteroaryl amide structure
-
The invention discloses a triazole heterocyclic compound containing a heteroaryl amide structure, a geometrical isomer of triazole heterocyclic compound containing the heteroaryl amide structure and pharmacologically acceptable salt, hydrate, solvate or p
- -
-
Paragraph 0085; 0089; 0090
(2019/11/14)
-
- Triazolo pyrazine compound containing heteroaryl substituted pyridazinone structure, and preparation method and applications thereof
-
The invention relates to a triazolo pyrazine compound containing a heteroaryl substituted pyridazinone structure, and pharmaceutically acceptable salts, hydrates, solvates, and a prodrug thereof, wherein the triazolo pyrazine compound containing a heteroa
- -
-
Paragraph 0076; 0080-0081
(2019/11/29)
-
- Compound as potassium channel modulator
-
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
- -
-
Paragraph 0775; 0777; 0780; 0781
(2018/07/30)
-
- New tetrahydropyrido pyrimidinecarboxylic compound or salt thereof
-
To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).
- -
-
Paragraph 0301
(2016/10/08)
-
- Synthesis and studies on anticonvulsant activity of 8-alkoxy-[1,2,4] triazolo[4,3-a]pyrazine
-
In this study, a series of new 8-alkoxy-[1,2,4]triazolo[4,3-a]pyrazine derivatives were synthesized and their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock test and the rotarod test, respectively. The most promising compounds 3d (8-butoxy-[1,2,4]triazolo[4,3-a] pyrazine) and 3f (8-hexyloxy-[1,2,4]triazolo[4,3-a]pyrazine) showed a median effective dose of 44 and 35.3 mg/kg and had protective index value of 3.2 and 4.8, respectively. To explain the possible mechanism of anticonvulsant activity, all compounds were tested in chemical induced model in anti pentylenetetrazol test.
- Guan, Li-Ping,Zhang, Rui-Peng,Chang, Yue,Gan, Xi-Xi
-
p. 3660 - 3664
(2013/04/24)
-
- Substituted Pyrano [2,3-b] Pyridinamine compounds as beta-secretase modulators and methods of use
-
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
- -
-
Page/Page column 37-38
(2010/06/11)
-
- SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
-
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I) I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
- -
-
Page/Page column 85
(2009/06/27)
-
- (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a] pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
A novel series of β-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H) -yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC50 = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo efficacy in animal models. MK-0431, the phosphate salt of compound 1, was selected for development as a potential new treatment for type 2 diabetes.
- Kim, Dooseop,Wang, Liping,Beconi, Maria,Eiermann, George J.,Fisher, Michael H.,He, Huaibing,Hickey, Gerard J.,Kowalchick, Jennifer E.,Leiting, Barbara,Lyons, Kathryn,Marsilio, Frank,McCann, Margaret E.,Patel, Reshma A.,Petrov, Aleksandr,Scapin, Giovanna,Patel, Sangita B.,Roy, Ranabir Sinha,Wu, Joseph K.,Wyvratt, Matthew J.,Zhang, Bei B.,Zhu, Lan,Thornberry, Nancy A.,Weber, Ann E.
-
p. 141 - 151
(2007/10/03)
-
