- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
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Paragraph 0395-0396
(2021/11/13)
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- A aza indole compound and its preparation method (by machine translation)
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The invention relates to a aza indole compound and its preparation method, the compound is 6 - trifluoromethyl - 2, 3 - dihydro-pyrrolo [2, 3 - b] pyridine, is 2 - hydroxy - 5 - trifluoro methyl pyridine as the starting material, through the 9 step reaction of the synthesized compound; said compound is a novel phosphodiesterase inhibitors, in diseases such as asthma has wide application in the foreground; its preparation method of cheap raw material, the synthetic method is simple, it is a synthetic aza indole compound of the new method, is suitable for the needs of large-scale industrial production. (by machine translation)
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Paragraph 0029; 0036
(2017/08/25)
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- New tetracyclic 1,4-oxazepines constructed via practically simple tandem condensation strategy from readily available synthons
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A streamlined synthetic methodology towards novel tetracyclic 1,4-oxazepines from readily available precursors is described. The compounds, designed as more soluble version of the earlier described, poorly soluble dibenzo[b,f][1,4]oxazepines, were obtained in high yields and as a single regioisomer as a result of three tandem chemical events - nucleophilic aromatic substitution, Smiles rearrangement and denitrocyclization.
- Sapegin, Alexander V.,Kalinin, Stanislav A.,Smirnov, Alexey V.,Dorogov, Mikhail V.,Krasavin, Mikhail
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p. 1077 - 1083
(2014/01/23)
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- Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
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New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50 = 111 nM, EC50 = 1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
- Chun, Kwangwoo,Park, Ji-Seon,Lee, Han-Chang,Kim, Young-Ha,Ye, In-Hea,Kim, Kang-Jeon,Ku, Il-Whea,Noh, Min-Young,Cho, Goang-Won,Kim, Heejaung,Kim, Seung Hyun,Kim, Jeongmin
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p. 3983 - 3987
(2013/07/27)
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- HETEROCYCLIC COMPOUND AND ITS USE FOR CONTROL OF AN ARTHROPOD PEST
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A heterocyclic compound represented by formula (1): wherein A1, A2, R1, R2, R3, R4, n and so on are defined in that description, has an excellent control effect on arthropod pests and is useful for control of arthropod pests.
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Page/Page column 111-112
(2011/04/26)
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- NOVEL BRONCHODILATING ISOQUINOLINE AMIDES
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The invention relates to novel compounds having the general formula I, and which compounds are useful to manufacture a medicament to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma, and vasoconstriction, e.g. hypertension.
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Page/Page column 23
(2009/03/07)
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- 3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS
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The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
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Page/Page column 14; 35
(2008/06/13)
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- Chemical compounds
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Pesticidal compounds of formula (I) wherein R1, R2, R3 and R4 are independently selected from hydrogen, cyano, halogen, lower alkyl optionally substituted by halogen, lower alkoxy optionally substituted by halogen, lower alkenyl optionally substituted by halogen; amino and mono- or di-(lower alkyl) amino;, R6 is oxygen or sulphur;, R7, R8 and R10 are independently selected from hydrogen, halogen, cyano, lower alkyl optionally substituted by halogen, lower alkoxy optionally substituted by halogen, lower thioalkoxy optionally substituted by halo; and, R9 is lower alkyl substituted by halogen or lower alkenyl optionally substituted by halogen. The preparation of these compounds together with their use in combatting insect, acarine and nemotode pests is also described.
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- Anti-inflammatory oxazole[4,5-b]pyridines
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The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.
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