- SUBSTITUENT-INCLUDING UREA COMPOUND
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An object of the present invention is to provide a compound that has a specific chemical structure having an activation effect on SIRT6 and is useful as an active component for preventing and treating inflammatory diseases. The present invention relates to a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. (Each symbol in Formula (1) has the same definition as that described in the specification.)
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Paragraph 0923-0925
(2021/12/03)
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- Palladium-Catalyzed Reductive Carbonylation of (Hetero) Aryl Halides and Triflates Using Cobalt Carbonyl as CO Source
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An efficient protocol for the reductive carbonylation of (hetero) aryl halides and triflates under CO gas-free conditions using Pd/Co2(CO)8 and triethylsilane has been developed. The mild reaction conditions, enhanced chemoselectivity and, easy access to heterocyclic and vinyl carboxaldehydes highlights its importance in organic synthesis.
- Dogga, Bhushanarao,Joseph, Jayan T.,Kumar, C. S. Ananda
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supporting information
p. 309 - 313
(2020/12/23)
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- Noncryogenic synthesis of functionalized 2-methoxypyridines by halogen-magnesium exchange using lithium dibutyl(isopropyl)magnesate(1-) and lithium chloride
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2-Methoxypyridines functionalized in the 3-, 5-, or 6-position and 2,6-dimethoxypyridines functionalized in the 3-position were prepared from the corresponding bromo or iodo analogues by using lithium dibutyl(isopropyl) magnesate(1-) and lithium chloride
- Struk, Lukasz,Sosnicki, Jacek G.
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experimental part
p. 735 - 746
(2012/04/04)
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- Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists
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A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure-activity relationships were examined in order to identify potent and selective arginine vasopressin V2 receptor agonists. Attempts to substitute other chemical groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V2 binding affinity could be obtained with a wide range of functional groups. This structural tolerance allowed for the manipulation of other attributes, such as selectivity against V1a receptor affinity or avoidance of the undesirable inhibition of cytochrome P450 (CYP), without losing potent affinity for the V2 receptor. Some representative compounds obtained in this study were also found to decrease urine volume in awake rats.
- Tsukamoto, Issei,Koshio, Hiroyuki,Kuramochi, Takahiro,Saitoh, Chikashi,Yanai-Inamura, Hiroko,Kitada-Nozawa, Chika,Yamamoto, Eisaku,Yatsu, Takeyuki,Shimada, Yoshiaki,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
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experimental part
p. 3130 - 3141
(2009/09/30)
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- BENZAZEPIN-2(1H)-ONE DERIVATIVES
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.
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Page/Page column 50
(2008/06/13)
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- TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE
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Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
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Page/Page column 90
(2010/11/28)
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- Preparation and antioxidant activity of α-pyridoin and its derivatives
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Focusing on α-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) as the lead compound of the novel antioxidative enediol, we synthesized 5,5′- or 6,6′-bis-substituted derivatives of 1 from disubstituted pyridines. The antioxidant activity of 1 and its synthetic derivatives 2-7 was evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl radical) scavenging assay and inhibition of lipid peroxidation. In the DPPH assay, 1 exhibited an activity stronger than that of ascorbic acid, and 5,5′-dimethyl-(5) or 5,5′-dimethoxy- substituted derivatives (6) exhibited more potent activity than 1. The DPPH scavenging activities of α-pyridoins were correlated with their oxidation potential and thus the electron density of enediol. 5 and 6 effectively inhibited lipid peroxidation in the rat liver microsome/tert-butyl hydroperoxide system. Therefore, 5 and 6 serve as good candidates for a pharmacologically useful enediol antioxidant.
- Hatanaka, Masashi,Takahashi, Kyoko,Nakamura, Shigeo,Mashino, Tadahiko
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p. 6763 - 6770
(2007/10/03)
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- Imidazo[1,5-a]pyridine-3-ylidenes - Pyridine derived N-heterocyclic carbene ligands
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The ready synthesis of differently substituted 2H-imidazo[1,5-a]pyridin-4- ium bromides is reported. These salts are precursors for a new class of N-heterocyclic carbene ligands. As a consequence of their bicyclic geometry, these ligands are capable of in
- Burstein, Christian,Lehmann, Christian W.,Glorius, Frank
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p. 6207 - 6217
(2007/10/03)
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- A simple route to new phenanthro- and phenanthroid-fused thiazoles by a PIFA-mediated (hetero)biaryl coupling reaction
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An application of the PIFA-mediated [PIFA: phenyliodine(III) bis(trifluoroacetate) biaryl coupling reaction is presented and extended to the formation of heterobiaryl connections. A preliminary study of the scope and limitations of this procedure was carried out in the synthesis of phenanthroids 11 from a series of phenethyl-substituted heterocycles 10, It was observed that in some cases a competitive dimerization process took place. It was also found that the coupling step could be efficiently extended to a larger number of examples if an aromatic ring were situated fused to the 1,2-diarylethane skeleton, as in 23 and 30. The synthesis of a series of 4,5-diarylthiazoles 23a-g was therefore carried out to explore the electronic requirements and the regioselectivity of the PIFA-mediated non-phenolic coupling reaction. When the same procedure was applied to aryl-heteroarylthiazoles 30, a series of phenanthroid-fused thiazoles 31 was obtained in good overall yields. To the best of our knowledge, no oxidative aryl-heteroaryl coupling reaction of this type had previously been reported. Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
- Moreno, Isabel,Tellitu, Imanol,Dominguez, Esther,SanMartin, Raul
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p. 2126 - 2135
(2007/10/03)
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- Substituted piperidine derivatives as muscarinic M3 receptor antagonists
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PCT No. PCT/JP96/02904 Sec. 371 Date Apr. 9, 1998 Sec. 102(e) Date Apr. 9, 1998 PCT Filed Oct. 7, 1996 PCT Pub. No. WO97/13766 PCT Pub. Date Apr. 17, 1997This invention provides substituted heteroaromatic ring derivatives which are represented by a genera
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- Lithiation of Methoxypyridines Directed by α-Amino Alkoxides
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The addition of methoxypyridinecarboxaldehydes to certain lithium dialkylamides gave α-amino alkoxides in situ that were ring-lithiated with alkyllithium bases.Alkylation and hydrolysis on workup provided ring-substituted methoxypyridinecarboxaldehydes via a one-pot reaction.The one-pot methylation of isomeric methoxypyridinecarboxaldehydes was examined.The regioselectivity of the lithiation-methylation was dependent on the aldehyde, the amine component of the α-amino alkoxide, and the metalation conditions.When lithiated N,N,N'-trimethylethylenediamine was used as the amine component of the α-amino alkoxide, methylation generally occured ortho to the aldehyde function.The analogous reactions using lithium N-methylpiperazide as the amine component gave substitution next to the methoxy group.Several new methylated methoxypyridinecarboxaldehydes were prepared in a regioselective manner by using this one-pot procedure.
- Comins, Daniel L.,Killpack, Michael O.
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