- MICROBIOCIDAL DERIVATIVES
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Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, and especially fungicides.
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Page/Page column 49
(2020/12/11)
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- COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND PYRIDOPYRIMIDINE DERIVATIVES
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Therapeutic combinations of hepatitis B virus (HBV) vaccines and a pyridopyrimidine derivative are described. Methods of inducing an immune response against HBV or treating an HBV-induced disease, particularly in individuals having chronic HBV infection, using the disclosed therapeutic combinations are also described. The invention provides therapeutic combinations or compositions and methods for inducing an immune response against hepatitis B viruses (HBV) infection.
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Page/Page column 303
(2021/01/22)
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- Synthesis, docking study and kinase inhibitory activity of a number of new substituted pyrazolo[3,4-c]pyridines
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A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against glycogen synthase kinase 3 (GSK3)α/β as well as against cdc2-like kinases 1 (CLK1) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with good selectivity and remarkable structure-activity relationships (SARs), without being cytotoxic. Molecular simulations in correlation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent.
- Sklepari, Meropi,Lougiakis, Nikolaos,Papastathopoulos, Athanasios,Pouli, Nicole,Marakos, Panagiotis,Myrianthopoulos, Vassilios,Robert, Thomas,Bach, Stéphane,Mikros, Emmanuel,Ruchaud, Sandrine
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- Novel pyrazolopyridine derivatives as potential angiogenesis inhibitors: Synthesis, biological evaluation and transcriptome-based mechanistic analysis
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Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed and synthesized a new series of substituted pyrazolopyridines and explored their ability to influence crucial pro-angiogenic attributes of endothelial cells. Four of the synthesized compounds, possessing analogous substitution pattern, were found able to inhibit at low micromolar concentrations endothelial cell proliferation, migration and differentiation, constitutively or in response to Vascular Endothelial Growth Factor (VEGF) and to attenuate VEGF-induced phosphorylation of VEGF receptor-2 and downstream kinases AKT and ERK1/2. Administration of effective compounds in mice delayed the growth of syngeneic Lewis lung carcinoma transplants and reduced tumor microvessel density, without causing toxicity. Genome-wide microarray and gene ontology analyses of treated endothelial cells revealed derivative 18c as the most efficient modulator of gene expression and mitotic cell cycle/cell divisiong along with ? cholesterol biosynthesis? as the most significantly altered biological processes.
- Michailidou, Maria,Giannouli, Vassiliki,Kotsikoris, Vasilios,Papadodima, Olga,Kontogianni, Georgia,Kostakis, Ioannis K.,Lougiakis, Nikolaos,Chatziioannou, Aristotelis,Kolisis, Fragiskos N.,Marakos, Panagiotis,Pouli, Nicole,Loutrari, Heleni
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p. 143 - 157
(2016/06/09)
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- ERK INHIBITORS
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The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
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Page/Page column 40
(2016/07/05)
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- ERK INHIBITORS
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The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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Page/Page column 73; 74
(2016/07/05)
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- TOLL LIKE RECEPTOR MODULATOR COMPOUNDS
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The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.
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Paragraph 0753; 0754
(2016/10/27)
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- Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt
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Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.
- Zhu, Gui-Dong,Gong, Jianchun,Gandhi, Viraj B.,Woods, Keith,Luo, Yan,Liu, Xuesong,Guan, Ran,Klinghofer, Vered,Johnson, Eric F.,Stoll, Vincent S.,Mamo, Mulugeta,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
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p. 2441 - 2452
(2007/10/03)
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- Diamine derivatives
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A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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- DIAMINE DERIVATIVES
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A compound represented by the general formula (1):Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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Page 244-245
(2008/06/13)
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- SULFONYLQUINOXALONE ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ ANTAGONISTS
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Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists to relieve symptons, associated with bradykinin including pain, inflammation, bronchoconstriction, cerebral edema, etc.
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Page/Page column 204-205
(2010/02/07)
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- REDUCTION OF HETERO-AROMATIC NITRO COMPOUNDS WITH BAKER'S YEAST
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Reduction of nitro group on hetero-aromatics with baker's yeast has been examined.
- Takeshita, Mitsuhiro,Yoshida, Sachiko
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p. 2201 - 2204
(2007/10/02)
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- Pyrazolopyridines. Part 5. Preparation and Reactions of Pyrazolopyridines
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A series of pyrazolopyridines has been prepared by nitrosation of 3-acetamido-4-methylpyridines and subsequent rearrangement and cyclisation of the N-acetyl-N-nitroso-compounds produced.The reactions of the pyrazolopyridines have been investigated. 1- and 2-Acetyl and 1- and 2-benzyl compounds were obtained and their structures elucidated spectroscopically.The ring system readily undergoes electrophilic substitution in the 3-position. 7-Chloropyrazolopyridine has been shown to be more susceptible to nucleophilic substitution than the isomeric 5-chloro-compound.
- Chapman, David,Hurst, Jim
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p. 2398 - 2404
(2007/10/02)
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