- TRIAZOLE ANTIMICROBIAL DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof: The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.
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Paragraph 0213-0214
(2020/01/04)
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- Posaconazole derivative, pharmaceutical composition and use thereof
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The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof: The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl-β-cyclodextrin, sulfobutyl ether-β-cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.
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Page/Page column 247
(2020/01/22)
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- HYDROXYL PURINE COMPOUNDS AND USE THEREOF
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Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers thereof or pharmaceutically acceptable salts thereof.
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Paragraph 0528; 0529
(2018/04/05)
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- HYDROXYL PURINE COMPOUNDS AND USE THEREOF
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Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.
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Paragraph 0267; 0268
(2018/06/09)
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- A simple synthesis of aminopyridines: Use of amides as amine source
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A transition metal/microwave irradiation (or base) free synthesis of aminopyridines has been accomplished via C-N bond forming reaction between chloropyridine and a variety of simple amides under refuxing conditions.
- Kodimuthali, Arumugam,Mungara, Anitha,Prasunamba, Padala Lakshmi,Pal, Manojit
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experimental part
p. 1439 - 1445
(2010/11/04)
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- Pyrido[2,3-d]pyrimidinone and imidazo[4,5-b]pyrimidinone
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Compounds useful for increasing cardiotonic contractility in humans or other animals and pharmaceutical compositions including these compounds are disclosed. The compounds have the general structure STR1 wherein: A is STR2 and R1, R2, R3, R4, R8, R10, R11, R12, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23 and R24 are H, lower alkyl of 1-4 carbon atoms, phenyl, substituted phenyl, phenyl lower alkyl of 1-4 carbon atoms or substituted phenyl lower alkyl of 1-4 carbon atoms; wherein the substituted phenyl group is substituted by one or more of lower alkyl, lower alkoxy, amino, lower alkyl amino, lower alkyl mercapto, hydroxy, hydroxy lower alkyl, acetoxy, benzyloxy, phenoxy, lower alkyl sulfinyl or lower alkyl sulfonyl; R13 is H, lower alkyl of 1-4 carbon atoms, alkoxy lower alkyl of 1-4 carbon atoms, hydroxy lower alkyl of 1-5 carbon atoms, amino, carbamoyl, cyano, lower alkyl carbamoyl of 1-4 carbon atoms, formyl, amino lower alkyl of 1-4 carbon atoms, carboxy, carbalkoxy, or tetrazolyl; R3 and R4 together may form =O; R16 and R17 together may form a carbon-carbon bond; n is 0 or 1; and O is 0 or 1.
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- 2-Oxo-1,8-naphthyridine-3-carboxylic Acid Derivatives with Potent Gastric Antisecretory Properties
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The syntheses of 2-oxo-1,8-naphthyridine-3-carboxylic acid derivatives having potent gastric antisecretory properties in the pyloric-ligated (Shay) rat model are described.Two of the more potent compounds tested that were selected for more detailed dose-r
- Santilli, Arthur A.,Scotese, Anthony C.,Bauer, Raymond F.,Bell, Stanley C.
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p. 2270 - 2277
(2007/10/02)
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- NOVEL HETEROCYCLES. 12. SYNTHESIS OF THE IMIDAZOPYRIDOTHIADIAZINE RING SYSTEM
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The synthesis of 2,6-dihydro-6-methyl-3H-imidazopyrido thiadiazine 5-oxide (4), a new ring system, is accomplished in three steps from 2-chloronicotinonitrile.
- Coppola, Gary M.
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p. 1013 - 1018
(2007/10/02)
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