- HETEROCYCLIC COMPOUNDS AS BET INHIBITORS
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Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.
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Paragraph 0316
(2021/01/23)
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- Organic metal compound and organic light-emitting device
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Organic metal compounds and organic light-emitting devices employing the same are provided. The organic metal compound has a chemical structure of Formula (I) or Formula (II): In particular, one of the following two conditions (1) and (2) is met: (1) R1 is deuterium or C1-6 deuterated alkyl group, when R3 and R4 are independently hydrogen, halogen, C1-6 alkyl group, C1-6 fluoroalkyl or C3-12 heteroaryl group; and (2) R1 is hydrogen, deuterium, C1-6 alkyl group, C1-6 deuterated alkyl group, C3-12 heteroaryl group, or C6-12 aryl group, when at least one of R3 and R4 is C6-12 aryl group or C6-12 fluoroaryl group.
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Paragraph 0041; 0063
(2020/02/10)
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- EZH2 Inhibitors
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The present invention relates to compounds that inhibit EZH2 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0168
(2018/11/02)
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- One-pot synthesis of fused 2-pyridones from heteroarylacrylic acid via curtius rearrangement & microwave-assisted thermal electrocyclization
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We investigated the one-pot synthesis of several fused 2-pyridone ring systems based on a Curtius rearrangement, followed by a microwave-assisted thermal electrocyclization of a 2-aza-6?-electron system including isocyanate. We synthesized seven heterocyclic compounds containing a fused 2-pyridone ring. In these results, the one-pot synthesis of fused 2-pyridone ring system 5 from (E)-acrylic acids 1 under microwave irradiation conditions was more effective than the conventional reaction conditions in terms of the yield and the reaction time.
- Nishiyama, Takashi,Hatae, Noriyuki,Hayashi, Kaori,Obata, Manami,Taninaka, Kimiko,Yamane, Masahiro,Oda, Shota,Abe, Takumi,Ishikura, Minoru,Hibino, Satoshi,Choshi, Tominari
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p. 251 - 267
(2017/07/28)
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- Design and synthesis of piperazinylpyridine derivatives as novel 5-HT 1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS)
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We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT 1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piper-azine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure-activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.
- Asagarasu, Akira,Matsui, Teruaki,Hayashi, Hiroyuki,Tamaoki, Satoru,Yamauchi, Yukinao,Sato, Michitaka
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experimental part
p. 34 - 42
(2009/07/18)
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- Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors
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Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioavailability.
- Rewinkel,Lucas,Smit,Noach,Van Dinther,Rood,Jenneboer,Van Boeckel
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p. 2837 - 2842
(2007/10/03)
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- SUBSTITUTED SULFONIC ACID N-[(AMINOIMINOMETHYL)PHENYLALKYL]-AZAHETEROCYCLAMIDE COMPOUNDS
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The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
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- The Thienopyridine and Furopyridine Rings: New Pharmacophores with Potential Antipsychotic Activity
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Two new arylpiperazine derivatives, the 4-(1-piperazinyl)thieno- and -furopyridine ring systems, have been synthesized and appended via tetramethylene chains to various imide rings.Target compounds from each series were found to have significant activity in the blockade of apomorphine stereotypy and apomorphine-induced climbing, the Sidman avoidance response, and the conditioned avoidance response.In addition, while potent affinity for serotonin 5-HT1 and 5-HT2 receptors was observed for both the thieno- and furopyridine derivatives,the interaction of these molecules with the dopamine D2 receptor was weak.Electrophysiological studies of the lead prototypes from each series, involving compounds 22 and 33, indicate these two molecules have distinctively different effects on dopamine neurons in areas A9 and A10.Despite the similarity these molecules share in their behavioral indices of antipsychotic acivity, it is likely that the thieno- and furopyridine rings employ different mechanisms to achieve this convergence of biological effects.
- New, James S.,Christopher, William L.,Yevich, Joseph P.,Butler, Rhett,Schlemmer, R. Francis,et al.
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p. 1147 - 1156
(2007/10/02)
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- Antipsychotic fused-ring pyridinylpiperazine derivatives
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Disubstituted 1,4-piperazinyl derivatives are disclosed wherein one substituent is a bicyclic fused-ring furo-, pyrrolo-, cyclopentadieno-, or thieno-pyridine heterocyclic system and the second substituent is an alkylene chain attached to cyclic imide heterocycles, such as azaspiro[4.5]decanediones, dialkylglutarimides, thiazolidinediones, succinimides, and morpholine-2,6-diones; or a benzylic carbinol moiety. These compounds have potent antipsychotic and serotonin antagonist activities. 4-[4-[4-(4-Furo[3,2-c]pyridinyl)-1-piperazinyl]butyl]-3,5-morpholinedione is an example of a typical embodiment having selective antipsychotic activity.
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