- ROCK INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
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The invention relates to a ROCK inhibitor represented by formula (I), its preparation method and its use. The ROCK inhibitor has excellent ROCK inhibition activity, in particular good selective inhibition on ROCK2 kinase, has good safety and metabolic stability, and has high bioavailability. The process of preparing the ROCK inhibitor is simple, and the ROCK inhibitor is easy to purify, and therefore offers good prospects for application.
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Page/Page column 65
(2022/01/24)
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- Trizaine-based dehydrative condensation reagents bearing carbon-substituents
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Herein, we report on the synthesis of alkyl-, aryl-, and alkynyl-substituted chlorotriazines and their ammonium salts, and demonstrate their utility in dehydrative condensation reactions. Although the electrophilicity of these reagents is mainly dependent on the hybridization of the carbon-substituents, it was found that bulky 2,6-dimethylphenyl group-substituted reagents resulted in the highest product yields because of a slight increase in reagent electrophilicity and/or steric hindrance favorable for desired dehydrative condensation reactions.
- Kitamura, Masanori,Komine, Sayaka,Kunishima, Munetaka,Yamada, Kohei
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- Glass engineering of aminotriazine-based materials with sub-ambient: T gand high kinetic stability
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A challenge in glass engineering is the design of molecular glasses combining a high glass kinetic stability (GS) of the amorphous phase with a low (sub-ambient) glass transition temperature (Tg). Triazine derivatives with arylamino substituents readily form glassy phases that can show outstanding resistance to crystallization. In the present study, a series of 12 analogous compounds incorporating phenylamino and cyclohexylamino groups was synthesized, and their thermal properties and intermolecular interactions were studied. All compounds possess an excellent glass-forming ability, a low Tg ranging from 32 °C to as low as -19 °C, and a high GS. While the cyclohexyl derivatives show higher Tg, the phenyl derivatives possess a higher GS with some compounds remaining completely amorphous for over three years despite their sub-ambient Tg. X-ray diffraction, infrared spectroscopy and DFT calculations reveal that the higher volume occupancy and rotational energy barrier of cyclohexyl groups are the main factors responsible for the compounds' higher Tg values but that they also contribute to their higher propensity to crystallize. In counterpart, the planarity of phenyl groups leads to poorer packing and enhances their GS while keeping their Tg well below ambient. The formation of hydrogen bonds or competing interactions provides an additional handle to tune the Tg of the compounds. Taken together, these studies provide guidelines for the design of molecular glasses with readily tunable thermal properties in view of their functionalization. This journal is
- Iankovitch, Anna,Jokar, Mahboubeh,Kara Ali, Zeinab,Lebel, Olivier,Maris, Thierry,Pellerin, Christian
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p. 4275 - 4288
(2020/07/10)
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- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.
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Page/Page column 74
(2010/12/29)
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- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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The invention provides Triazine derivatives and further provides methods of using these compounds to modulate protein kinases and for treating diseases and conditions mediated by protein kinases.
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Page/Page column 64-65
(2010/12/29)
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- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof.
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Page/Page column 92
(2010/12/29)
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- TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.
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Page/Page column 66
(2010/12/29)
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- UREIDOPHENYL SUBSTITUTED TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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The present invention provides Uredophenyl substituted triazine derivatives and provides methods of using these compounds to modulate protein kinases and methods of using these compounds to treat protein kinase mediated diseases and conditions.
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Page/Page column 67
(2010/12/29)
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- Anarchy in the solid state: structural dependence on glass-forming ability in triazine-based molecular glasses
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We have recently shown that molecular glasses, small molecules capable of readily forming glassy solids as opposed to crystals, can be designed by exploiting molecular association through strong and directional intermolecular interactions, as exemplified by several members of the bis(mexylamino)triazine family. Herein, 43 new bis(mexylamino)triazine derivatives were synthesized, 31 of which have been found to spontaneously form glassy phases and did not crystallize upon heating. Crown Copyright
- Wuest, James D.,Lebel, Olivier
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experimental part
p. 7393 - 7402
(2009/12/06)
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- PREVENTIVES OR REMEDIES FOR ALZHEIMER'S DISEASE OR AMYLOID PROTEIN FIBROSIS INHIBITORS CONTAINING NITROGEN-CONTAINING HETEROARYL COMPOUNDS
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The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereo
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- Substituted cyclopropylamino-1,3,5-triazines
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New substituted cyclopropylamino-1,3,5-triazines having the formula STR1 wherein R1 is C1 -C3 -alkyl, C3 -C5 -cycloalkyl or C1 -C3 -alkyl-C3 -C5 -cycloalkyl R2 is bis(2-hydroxyethyl)amino, 3-hydroxy-1-azetidinyl, 3-methoxy-1-azetidinyl, 3-oxo-1-azetidinyl, morpholino, 4-hydroxypiperidino, thiomorpholino, thiomorpholino S-oxide, thiomorpholino S,S-dioxide, 3-thiazolidinyl, 3-thiazolidinyl S-oxide, 3-thiazolidinyl S,S-dioxide or 8-oxa-3-azabicyclo[3,2,1]oct-3-yl. Processes for the preparation thereof and pharmaceutical composition containing them are also given. The compounds are useful for the treatment of disorders associated with Alzheimer's disease, senile dementia, Alzheimer's type and with any evolutive cognitive pathology, and also for the treatment of depression, anxiety, mood disturbances, inflammatory phenomena and asthma.
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