- HERBICIDAL COMPOUNDS
-
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
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Page/Page column 101
(2021/04/02)
-
- 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
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p. 9053 - 9063
(2020/06/08)
-
- 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.
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p. 13438 - 13452
(2020/12/15)
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- PYRIDAZINIUM COMPOUNDS FOR USE IN CONTROLLING UNWANTED PLANT GROWTH
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Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, especially as herbicides.
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Page/Page column 57
(2020/08/22)
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- An original class of small sized molecules as versatile fluorescent probes for cellular imaging
-
An unusual class, compact in size, of fluorescent probes based on pyridazino-1,3a,6a-triazapentalene scaffolds exhibits promising fluorescent properties (quantum yield values up to 73%, large Stokes shifts, emission wavelengths located in the green-yellow
- Sirbu, Doina,Diharce, Julien,Martini?, Ivana,Chopin, Nicolas,Eliseeva, Svetlana V.,Guillaumet, Gérald,Petoud, Stéphane,Bonnet, Pascal,Suzenet, Franck
-
supporting information
p. 7776 - 7779
(2019/07/08)
-
- COMBINATION TREATMENT OF ACUTE MYELOID LEUKEMIA
-
The present invention relates to the use of volasertib, or a pharmaceutically acceptable salt thereof or a hydrate thereof, in combination with a BET inhibitor, or a pharmaceutically acceptable salt thereof or a hydrate thereof for treating patients suffering from acute myeloid leukemia (AML).
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Page/Page column 20; 34
(2019/08/12)
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- Preparation and application of triazole heterocyclic compound containing heteroaryl amide structure
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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 0085-0088
(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; 0078-0079
(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; 0778; 0779
(2018/07/30)
-
- Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment
-
Bromodomain and extra-terminal (BET) proteins, a class of epigenetic reader domains has emerged as a promising new target class for small molecule drug discovery for the treatment of cancer, inflammatory, and autoimmune diseases. Starting from in silico screening campaign, herein we report the discovery of novel BET inhibitors based on [1,2,4]triazolo[4,3-a]quinoxaline scaffold and their biological evaluation. The hit compound was optimized using the medicinal chemistry approach to the lead compound with excellent inhibitory activities against BRD4 in the binding assay. The substantial antiproliferative activities in human cancer cell lines, promising drug-like properties, and the selectivity for the BET family make the lead compound (13) as a novel BRD4 inhibitor motif for anti-cancer drug discovery.
- Ali, Imran,Lee, Jooyun,Go, Areum,Choi, Gildon,Lee, Kwangho
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p. 4606 - 4613
(2017/09/29)
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- COMPOUNDS ANTAGONIZING A3 ADENOSINE RECEPTOR, METHOD FOR PREPARING THEM, AND MEDICAL-USE THEREOF
-
The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed
- -
-
Paragraph 0397; 0398
(2017/08/07)
-
- Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
-
This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
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Paragraph 0708
(2017/01/23)
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- TRIAZOLOPYRAZINONES AS PDE1 INHIBITORS
-
The present invention provides triazolopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
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Page/Page column 64
(2016/05/02)
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- 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 0300
(2016/10/08)
-
- Molecular structure, NMR, UV-Visible, vibrational spectroscopic and HOMO, LUMO analysis of (E)-1-(2, 6-bis (4-methoxyphenyl)-3, 3-dimethylpiperidine-4-ylidene)-2-(3-(3, 5-dimethyl-1H-pyrazol-1-yl) pyrazin-2-yl) hydrazine by DFT method
-
We have synthesized (E)-1-(2, 6-bis (4-methoxyphenyl)-3, 3-dimethylpiperidine-4-ylidene)-2-(3-(3, 5-dimethyl-1H-pyrazol-1-yl) pyrazin-2-yl) hydrazine (PM6). It was characterized using FT-IR, FT-Raman, 1H NMR, 13C NMR techniques. To i
- Alphonsa, A.Therasa,Loganathan,Anand, S.Athavan Alias,Kabilan
-
p. 277 - 285
(2015/11/18)
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- BICYCLIC AZAHETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
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Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
- -
-
Paragraph 0196; 0258
(2016/07/05)
-
- Triazolopyrazine
-
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitabl
- -
-
Paragraph 0287; 0288; 0289
(2015/05/26)
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- TRIAZOLOPYRAZINE DERIVATIVES AS BRD4 INHIBITORS
-
The present invention encompasses compounds of general formula (I), wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitab
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-
Page/Page column 40
(2015/05/26)
-
- FT-IR, FT-Raman, UV, NMR spectra and molecular structure investigation of (E)-2-(3-chloropyrazin-2-yl)-1-(3-ethyl-2, 6-diphenyl piperidin-4-ylidene) hydrazine: A combined experimental and theoretical study
-
This work presents the characterization of (E)-2-(3-chloropyrazin-2-yl)-1-(3-ethyl-2, 6-diphenyl piperidin-4-ylidene) hydrazine (HDE) by quantum chemical calculations and spectral techniques. The structure was investigated by FT-IR, FT-Raman, UV-vis and NMR techniques. The geometrical parameters and energies have been obtained from Density functional theory (DFT) B3LYP (6-31G (d, p)) basis set calculations. The geometry of the molecule was fully optimized, vibrational spectra were calculated and fundamental vibrations were assigned on the basis of total energy distribution (TED) of the vibrational modes, calculated with scaled quantum mechanics (SQM) method. 1H and 13C NMR chemical shifts of the molecule were calculated using Gauge-independent atomic orbital method (GIAO). The electronic properties such as excitation energies, wavelength, HOMO, LUMO energies performed by Time dependent density functional theory (TD-DFT) results complements with the experimental findings. NBO analysis has been performed for analyzing charge delocalization throughout the molecule. The calculation results were applied to simulate spectra of the title compound, which show excellent agreement with observed spectra. To provide information about the interactions between human cytochrome protein and the novel compound theoretically, docking studies were carried out using Schr?dinger software.
- Therasa Alphonsa,Loganathan,Athavan Alias Anand,Kabilan
-
p. 137 - 144
(2015/08/06)
-
- TRIAZOLOPYRAZINE
-
Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
- -
-
Paragraph 0233 - 0236
(2014/05/25)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
-
The present invention relates to salts, hydrates, and polymorphs of bicyclic heteroaryl compounds, and pharmaceutical compositions thereof, which may be useful as inhibitors of H4R for the treatment or prevention of diseases including allergic rhinitis
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-
Page/Page column 80; 81
(2013/03/28)
-
- 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)
-
- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
-
The present invention relates to compounds and methods which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
- -
-
Page/Page column 78
(2011/10/05)
-
- 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.
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-
Page/Page column 37
(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.
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-
Page/Page column 85
(2009/06/27)
-
- FUSED HETEROCYCLIC 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
-
Novel compounds are provided which are 1 1 -beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxys
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-
Page/Page column 60
(2008/12/08)
-
- 3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
-
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
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-
Page/Page column 42
(2010/02/07)
-
