- Azacyclic derivative as well as preparation method and medical use thereof
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The invention relates to an azacyclic derivative as well as a preparation method and medical use thereof and particularly relates to an azacyclic derivative represented by a general formula (I) (shownin the description), a preparation method thereof, a pharmaceutical composition containing the derivative and use of the derivative as an SMO antagonist, particularly in the treatment of diseases such as cancer related to Hedgehog signal channels. The definitions of groups in the general formula (I) are same as the definitions in the description.
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Paragraph 0376; 0377; 0378; 0382; 0383
(2019/02/04)
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- Preparation method of 1-aminoisoquinoline-6-methanol
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The invention relates to a synthesis method of 1-aminoisoquinoline-6-methanol. The synthesis method comprises the following steps: reacting 6-bromoisoquinoline used as a raw material to form 6-cyanoisoquinoline; adding a sulfuric acid solution to obtain isoquinoline-6-carboxylic acid; further obtaining isoquinoline-6-methyl formate under the action of absolute methanol and thionyl chloride; further adding m-chloroperoxybenzoic acid in batches in dichloromethane, and reacting to obtain a mixture isoquinoline-6-methyl formate oxynitride; adding into phosphorus oxychloride in batches, cooling after the reaction is completed, pouring into cracked ice, and precipitating a solid 1-chloroisoquinoline-6-methyl formate crude product; directly extracting the water phase with ethyl acetate, and performing centrifugal drying to obtain another 1-chloroisoquinoline-6-methyl formate crude product; merging the crude products of two batches, passing through a silica gel column, and eluting to obtain 1-chloroisoquinoline-6-methyl formate; adding into tetrahydrofuran, then cooling to -30 DEG C, and adding lithium aluminum hydride in batches to obtain a 1-(1-chloroisoquinoline-6-yl)methanol product; mixing with p-methoxybenzylamine, and heating to obtain (1-(4-methoxybenzylamino)isoquinoline-6-yl)methanol; and adding into trifluoroacetic acid, and refluxing to obtain the final product 1-aminoisoquinoline-6-methanol. The method is reasonable in route, low in waste, high in yield and easy to operate, and realizes raw material saving.
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Paragraph 0020; 0024
(2017/08/29)
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- NOVEL DIHYDROPYRIMIDIN-2(1H)-ONE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
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Page/Page column 157
(2011/04/24)
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- Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
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Provided herein are Heterocyclic Compounds having the following structure: wherein R1, R2, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.
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Page/Page column 33
(2008/12/07)
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- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 58
(2008/06/13)
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- NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
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Page/Page column 66
(2010/11/08)
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- Isoquinoline-6-carboxamides as potent and selective anti-human cytomegalovirus (HCMV) inhibitors
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Structure-activity relationship studies on our newly identified anti-HCMV compounds, the 1,6-naphthyridines led to the identification of isoquinoline-6-carboxamides as potent and selective anti-HCMV agents.
- Chan, Laval,Jin, Haolun,Stefanac, Tomislav,Wang, Wei,Lavallee, Jean-Francois,Bedard, Jean,May, Suzanne
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p. 2583 - 2586
(2007/10/03)
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