- READ-THROUGH INDUCER AND PHARMACEUTICAL USE THEREOF
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PROBLEM TO BE SOLVED: To provide a novel read-through inducer. SOLUTION: The present invention relates to a compound represented by the general formula (I) [each symbol in the formula is as described in the specification] or a pharmaceutically acceptable
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Paragraph 0306-0310
(2020/08/04)
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- One pot synthesis of substituted imidazopyridines and thiazoles from styrenes in water assisted by NBS
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Heating of commercially available styrenes with NBS in water followed by reaction with 2-aminopyridines or thioamides afforded important heterocyclic scaffolds in a one pot procedure. The reaction proceeds via co-oxidant free, in situ formation of α-bromoketone using NBS as a bromine source as well as an oxidant followed by trapping with suitable nucleophiles to provide imidazopyridines and thiazoles.
- Shinde, Mahesh H.,Kshirsagar, Umesh A.
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supporting information
p. 1455 - 1458
(2016/04/04)
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- INDOLE DERIVATIVES AS CRAC MODULATORS
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Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
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Page/Page column 45
(2012/01/30)
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- An expedient protocol for conversion of olefins to α-bromo/iodoketones using IBX and NBS/NIS
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A variety of olefins have been shown to undergo conversion to the corresponding α-bromo/iodoketones when reacted with NBS/NIS and IBX in DMSO at room temperature. While the reaction is found to occur rapidly with e-rich arylolefins leading to the corresponding haloketones in 65-95% yields in 0.3-3.0 h, those containing e-withdrawing groups are found to yield diketones concomitantly, such that the latter are the exclusive products over extended duration of the reactions.
- Moorthy, Jarugu Narasimha,Senapati, Kalyan,Singhal, Nidhi
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experimental part
p. 2493 - 2496
(2009/08/17)
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- Kinase inhibitors
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The present application is directed to pyrazolopyrirnidine and furopyrimidine analogs of the formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors.
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- Kinase inhibitors
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The present application is directed to pyrazolopyrimidine and furopyrimnidine analogs of the formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors.
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- Studies on Cerebral Protective Agents. VIII. Synthesis of 2-Aminothiazoles and 2-Thiazolecarboxamides with Anti-anoxic Activity
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Various 2-aminothiazoles (2a-s and 3a-g) and 2-thiazolecarboxamides (4a-h), possessing a nitrogeneous basic moiety at the C-2 position of the thiazole ring, were prepared and tested for anti-anoxic (AA) activity in mice.Among them, N-4-(3-trifluoromethylphenyl)-2-thiazolecarbaxamide hydrochloride (4e, FR108143) (minimum effective doses of 3,2 mg/kg i.p. and 10 mg/kg p.o., respectively) exhibited more potent AA activity than either FK360 or compound 1, each of which has a nitrogeneous basic moiety at the C-5 position.The structure-activity relationship with regard to AA activity of this series of compounds are discussed, and the three-dimensional electrostatic potentials (3D-MEP) around the basic nitrogen atom of FK360 and the thiazole derivative (4e) are compared.Key words cerebral protective agent; anti-anoxia; 2-aminothiazole; 2-thiazolecarboxamide; structure-activity relationship; FK360
- Okhubo, Mitsuru,Kuno, Atsushi,Nakanishi,Isao,Takasugi, Hisashi
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p. 1497 - 1504
(2007/10/03)
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