- Transition-Metal-Free Oxidation of Benzylic C-H Bonds of Six-Membered N-Heteroaromatic Compounds
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A novel oxidation of benzylic C-H bonds for the synthesis of diverse six-membered N-heteroaromatic aldehydes and ketones has been developed. The obvious advantages of this approach are the simple operation, mild reaction conditions, and without use of toxic reagent and transition metal. The present method should provide a useful access for the synthesis and modification of N-heterocycles.
- Gao, Xianying,Han, Shuaijun,Zheng, Maolin,Liang, Apeng,Zou, Dapeng,Wu, Yusheng,Wu, Yangjie,Li, Jingya
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p. 4040 - 4049
(2019/04/30)
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- NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
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There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)
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Paragraph 0942; 0943
(2016/07/05)
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- COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF
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The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.
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Paragraph 0103; 0104
(2015/05/05)
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- COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF
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The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.
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Paragraph 0152; 0153
(2015/06/24)
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- AROMATIC RING COMPOUND
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Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
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Paragraph 0458
(2015/01/18)
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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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- Isocytosine H2-receptor histamine antagonists. IV. The synthesis and biological activity of donetidine (SK and F 93574) and related compounds
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The synthesis and biological activity of some novel 2-amino-4-pyrimidone derivatives is described.Side-chains associated with H2 antagonist activity are attached through the 2-amino group, whilst a range of 2-hydroxypyridine containing moieties are substituted at the 5-position of the pyrimidone ring.Good H2-receptor histamine antagonist activity is observed with all the series and the majority of the compounds are selective for the H2-receptor.High aqueous solubility and iv potency coupled with an extended duration of biological activity in animal models ledto compound 16c, 2--5-(2-hydroxypyrid-4-ylmethyl)-4-pyrimidone (donetidine, SK and F 93574) being selected for clinical investigation as a potential parenterally administered therapeutic agent.H2-receptor antagonists / 2-amino-4-pyrimidones (isocytosines / imidazoles / thiazoles / pyridines / furans / 2-guanidinothiazoles / donetidine (SK and F 93574)
- Brown, T. H.,Blakemore, R. C.,Durant, G. J.,Ganellin, C. R.,Parsons, M. E.,et al.
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p. 601 - 608
(2007/10/02)
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- 5-(HYDROXYPYRIDYLALKYL)-4-PYRIMIDONES
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The compounds are substituted 2-amino-4-pyrimidones with a 5-(hydroxypyridylalkyl) substituent which are histamine H 2-antagonists. Two specific compounds are 2-2-(3-bromo-2-pyridylmethylthio) ethylamino!-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimidone and 2-4-(3-methoxy-2-pyridyl)butylamino!-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimido ne.
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- Pyrimidine compounds
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The compounds are substituted pyrimidine compounds which are histamine H2 -antagonists. A specific compound of the present invention is 2-[2-(5-dimethylaminomethyl)-2-furylmethylthio)ethylamino]-5-(3-pyridylmethyl)-4-pyrimidone.
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