- IMIDAZOPYRIMIDINES AS EED INHIBITORS AND THE USE THEREOF
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The present disclosure provides compounds represented by Formula (I) wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula (I) are FED inhibitors. FED inhibitors are useful for the treatment of cancer and other diseases.
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- ANTIMALARIAL HEXAHYDROPYRIMIDINE ANALOGUES
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The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-l,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted by an arylaminophenyl or heteroarylaminophenyl moiety. The compounds a
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Page/Page column 55
(2019/10/30)
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- FUSED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION METHODS THEREOF AND MEDICAL USES THEREOF
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The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I′), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I′) is the same as defined in the specification.
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- Full synthesis of natural-product (+/-)-cananga odorata alkali and separation method of enantiomers
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The invention discloses full synthesis of natural-product (+/-)-cananga odorata alkali and a chiral separation method of enantiomers thereof and belongs to the technical field of organic synthesis. The chiral separation method comprises the following steps of: adopting natural-product (+/-)-anthorine G as a substrate, carrying out tetrahydrofuran/methyl lithium reaction to obtain the natural-product (+/-)-cananga odorata alkali and the enantiomers thereof; then using a chiral semi-preparative type high-performance liquid chromatograph to carry out separation on the enantiomers, and obtaining the cananga odorata alkali and the enantiomers with the total yield being 17.9%. The full synthesis and the chiral separation method disclosed by the invention have the beneficial effects that the synthesis method is simplified, the total yield of full synthesis is increased, the structure identification is carried out, and not only is the divergence on the specific rotation of the cananga odorataalkali solved, but also basis and powerful guarantee are provided for further study on the compounds.
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- Method for totally synthesizing natural product (+/-)-rupestine G and resolving enantiomers
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The invention relates to a method for totally synthesizing a natural product (+/-)-rupestine G and resolving enantiomers. The method comprises the following steps: oxidizing the raw material 2-methyl-5-bromopyridine (1) by m-chloroperoxybenzoic acid to obtain a nitrogen oxidation product compound 2, carrying out a Reissert-Henze reaction to perform cyano substitution so as to obtain a compound 3, carrying out a decarboxylation reaction on the compound 3 and potassium monoethyl malonate to obtain beta-ketoester 4, carrying out alkylation under the condition of sodium ethylate to obtain a compound 5, carrying out a coupling reaction to obtain a compound 6, carrying out an intramolecular olefin double replacement reaction on the compound 6 to obtain a key intermediate compound 7, carrying out reduction with sodium borohydride to obtain a compound 8, carrying out a reaction under the condition of pyridine/MsCl to obtain a compound 9, hydrolyzing the compound 9 under the action of lithium hydroxide, carrying out methyl esterification by using iodomethane to obtain a compound 10, carrying out palladium-carbon catalytic hydrogenation to obtain a pair of diastereoisomers 11 and 12, and carrying out resolution by a semi-preparative high performance liquid chromatograph to obtain the natural product rupestine G and three stereoisomers, namely a compound 13, a compound 14 and a compound 15.
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- Homogenous suspension of immunopotentiating compounds and uses thereof
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The present invention generally relates to homogeneous suspensions of small molecule immune potentiators (SMIPs) that are capable of stimulating or modulating an immune response in a subject in need thereof. The homogeneous suspensions may be used in combinations with various antigens or adjuvants for vaccine therapies.
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- Preparation method of 3-bromo-6-methyl-2-pyridylaldehyde
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The invention relates to a preparation method of 3-bromo-6-methyl-2-pyridylaldehyde. The 3-bromo-6-methyl-2-pyridylaldehyde is an important medical intermediate and has wide market prospects. The 3-bromo-6-methyl-2-pyridylaldehyde can be condensed with amino groups to form an N-containing Schiff alkali conjugated system; and both N atoms on the pyridine ring and N atoms on imino C=N outside the ring can be coordinated with metal ions to form functional complexes. The preparation method comprises the following step: by using 5-bromo-2-methylpyridine as an initial raw material, carrying out N-oxidation, cyanation, acidification, esterification, reduction and aldehyde reaction to obtain the product 3-bromo-6-methyl-2-pyridylaldehyde. The 3-bromo-6-methyl-2-pyridylaldehyde synthesized by the method has the advantages of high purity, high yield and lower production cost. The synthesis method is simple and easy to implement, is green and environment-friendly, and provides theoretical and experimental references for industrial production.
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- COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
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The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is -CR4=CR5.
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