- Casein kinase 1 (CK1) inhibitor for plants (by machine translation)
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[Problem] to provide various lead compounds PHA derivatives, and/or circadian rhythm control agent having stronger CK1 inhibitor activity. [Solution] a compound represented by formula I, or a salt thereof or a solvate thereof. (R1 The, H or C1 - 5 A straight-chain, branched or cyclic alkyl group, alkenyl group or alkynyl group, R2 The, H, halogen (F, Cl, Br or I), or a C1 - 4 The alkyl group, the ring A, 5 - 8 membered lactam ring showing; however, R1 And R2 Except H together. )[Drawing] no (by machine translation)
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Paragraph 0053; 0104; 0109-0112; 0117
(2020/02/14)
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- ANTIBACTERIAL COMPOUNDS
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The present invention relates to compounds of general formula (II),to compositions comprising these compounds and to methods of treating Enterobacteriaceae bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Enterobacteriaceae.
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Page/Page column 83-84
(2019/05/22)
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- NOVEL GPR119 AGONIST COMPOUNDS
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The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
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- 18F LABELLED THIAZOLYLHYDRAZONE DERIVATIVES
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The present invention relates to compounds of Formula (I) wherein R1 and R2 are independently selected from 19F and 18F having selective binding for MAO-B as compared with MAO-A. The invention also provides radi
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- Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors
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The Rho kinases (ROCK1 and ROCK2) are highly homologous serine/threonine kinases that act on substrates associated with cellular motility, morphology, and contraction and are of therapeutic interest in diseases associated with cellular migration and contraction, such as hypertension, glaucoma, and erectile dysfunction. Beginning with compound 4, an inhibitor of ROCK1 identified through high-throughput screening, systematic exploration of SAR, and application of structure-based design, led to potent and selective ROCK inhibitors. Compound 37 represents significant improvements in inhibition potency, kinase selectivity, and CYP inhibition and possesses pharmacokinetics suitable for in vivo experimentation.
- Green, Jeremy,Cao, Jingrong,Bandarage, Upul K.,Gao, Huai,Court, John,Marhefka, Craig,Jacobs, Marc,Taslimi, Paul,Newsome, David,Nakayama, Tomoko,Shah, Sundeep,Rodems, Steve
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p. 5028 - 5037
(2015/07/02)
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- PTERIDINES AND THEIR USE AS AGROCHEMICALS
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The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products.
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- PTERIDINES AND THEIR USE AS AGROCHEMICALS
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The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products.
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- 5,8-DIFLUORO-4-(2-(4-(HETEROARYLOXY)-PHENYL)ETHYLAMINO)QUINAZOLINES AND THEIR USE AS AGROCHEMICALS
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The present disclosure relates to 5,8-difluoro-4-(2-(4-(heteroaryloxy)-phenyl)ethylamino)quinazolines and their use as agrochemicals and animal health products.
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Page/Page column 50-51
(2010/04/06)
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- 4-Pyridylanilinothiazoles that selectively target von Hippel - Lindau deficient renal cell carcinoma cells by inducing autophagic cell death
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Renal cell carcinomas (RCC) are refractory to standard therapy with advanced RCC having a poor prognosis; consequently treatment of advanced RCC represents an unmet clinical need. The von Hippel-Lindau (VHL) tumor suppressor gene is mutated or inactivated in a majority of RCCs. We recently identified a 4-pyridyl-2-anilinothiazole (PAT) with selective cytotoxicity against VHL-deficient renal cells mediated by induction of autophagy and increased acidification of autolysosomes. We report exploration of structure-activity relationships (SAR) around this PAT lead. Analogues with substituents on each of the three rings, and various linkers between rings, were synthesized and tested in vitro using paired RCC4 cell lines. A contour map describing the relative spatial contributions of different chemical features to potency illustrates a region, adjacent to the pyridyl ring, with potential for further development. Examples probing this domain validated this approach and may provide the opportunity to develop this novel chemotype as a targeted approach to the treatment of RCC. 2009 American Chemical Society.
- Hay, Michael P.,Turcotte, Sandra,Flanagan, Jack U.,Bonnet, Muriel,Chan, Denise A.,Sutphin, Patrick D.,Nguyen, Phuong,Giaccia, Amato J.,Denny, William A.
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supporting information; experimental part
p. 787 - 797
(2010/07/05)
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- HETEROARYL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE IN CANCER TREATMENT
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Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.
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- 2-PYRIDINYL[7-(SUBSTITUTED-PYRIDIN-4-YL) PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]METHANONES
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The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5--a]pyrimidin-3-yl]methanones with at least one substituent on the 4-pyridinyl ring having the chemical structure of formula (I): The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula: (I) in to modulate GABA and GABA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and/or GABA receptors.
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Page/Page column 33
(2010/02/14)
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- DIRECT FLUORINATION OF SUBSTITUTED PYRIDINES
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The direct fluorination of pyridines bearing alkyl, halogen, ester, or ketone functions has been employed to prepare the corresponding 2-fluoro-substituted pyridines.
- Puy, Michael Van Der
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p. 255 - 258
(2007/10/02)
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