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The invention discloses a type of xanthine derivatives and isomers. Through tests about influences on normal mice sugar tolerance and in-vitro DPP-IV activity inhibiting tests, the compounds provided by the invention show excellent DPP-IV inhibiting activity, and can be used for preparation of medicines treating diseases related to dipeptidyl peptidase IV.

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The invention discloses a method for preparing advantage Geleg sandbank, comprising the following steps: the tert-butoxy-carbonyl-Leigh geleg sandbank (g) is added to the methanol aqueous solution, the stirring is then started, in an inert atmosphere and heating to reflux of the reaction is carried out under the state, get advantage Geleg sandbank, wherein the reaction temperature is 25-50C, the reaction time is 3-12h, tert-butoxy-carbonyl-Leigh geleg sandbank (g) with the weight proportion of the methanol water solution 100 : (400-550). Method for preparing advantage Geleg sandbank of this invention, is under the protection of inert gas and methanol aqueous solution Boc protecting group on the method, no longer need expensive trifluoro acetate-DCM Boc protecting group on the reaction, only use the cheap methanol-water systems can be, and after treatment is simple, and three suitable the reaction of acid-DCM system, generating a plurality of impurities, the after-treatment and purification process is extremely tedious. Furthermore, it is also possible to avoid the use of the strong acid intermediate (g) and row Gurley sandbank impurity such as in the breaking of amide linkage. (by machine translation)

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Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.

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The invention relates to a synthesis method of chiral aminopiperidine and derivatives thereof. 3 . The invention is carried out by R (or S) – piperidine -3 – ethyl ester – L (or D) – L (or D)-tartrate after benzyl protection followed by azide and Curtitius rearrangement to R or S -benzyl -3 -aminopiperidine. R or S – benzyl -3 – aminopiperidine undergoes debenzylation to give R or S -amino piperidine, R or S – benzyl -3 – aminopiperidine through 3 -t-butoxycarbonyl protection, for example. Of R or S – (3 – t-butoxycarbonyl amino) piperidine, R or S – (3 – t-butoxycarbonyl amino) piperidine under acidic conditions can give R or S – 3-aminopiperidine, corresponding salts. The synthesis method provides a low-cost, easily-industrialized chiral 3 -aminopiperidine with high optical purity and a method. (by machine translation)

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An efficient single step process for the construction of pharmaceutically relevant substituted aminobenzoxazoles have been described in this report. Various electrodes and electrolytes combinations have been carried out to harvest optimum coupling results. The presented C?N bond formation reaction methodology has applied for the synthesis of biologically active compounds. This methodology saves reaction steps over traditional functionalization reactions.

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Replacement of one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 (1) with sulfonamide containing substituents produced a new class of active and potent PI3Kalpha inhibitors. Solubility issues prevented all but the 6-amino derivative 17 from being evaluated in vivo, but the clear activity of this compound demonstrated that this class of PI3K inhibitor shows great promise.

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Molecular modeling of unbound tricyclic guanine scaffolds indicated that they can serve as effective bioisosteric replacements of xanthines. This notion was further confirmed by a combination of X-ray crystallography and SAR studies, indicating that tricyclic guanine DPP4 inhibitors mimic the binding mode of xanthine inhibitors, exemplified by linagliptin. Realization of the bioisosteric relationship between these scaffolds potentially will lead to a wider application of cyclic guanines as xanthine replacements in drug discovery programs for a variety of biological targets. Newly designed DPP4 inhibitors achieved sub-nanomolar potency range and demonstrated oral activity in vivo in mouse glucose tolerance test.

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The invention belongs to the technical field of preparing raw materials, in particular to a improved process for the preparation of advantage Geleg sandbank. The present invention provides a method for preparing advantage Geleg sandbank, in advantage Geleg sandbank two-step condensation reaction of the acid to be used in water-free controlled particle size of sodium carbonate is a micrometer range, the reaction does not need to use the iodide catalyst, the reducing reaction temperature, reaction time is shortened, and the two-step reaction is changed into “one-pot synthesis” preparation have high purity, high yield key intermediate of compound E. The preparation method of this invention is suitable for industrial mass production of advantage Geleg sandbank, and, ultimately, to obtain high-purity, advantage Geleg sandbank of high extraction rate. (by machine translation)

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The present invention discloses a xanthine derivative having the structure of the following general formula (I) or a pharmaceutically acceptable salt thereof; further discloses a preparation method for the xanthine derivative or a pharmaceutically acceptable salt thereof; and further discloses the use of the xanthine derivative or a pharmaceutically acceptable salt thereof. Through experiments of DPP-IV activity inhibition experiments in vitro, impact on glucose tolerance in normal mice and impact on blood glucose in spontaneous diabetic mice, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.

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The invention belongs to the technical field of pharmaceutical chemistry, and in particular discloses a of formula I shown advantage geleg sandbank impurity and its preparation method, and at the same time discloses the advantage geleg sandbank impurity in the relevant substance inspection when the use as the impurity of the reference substance, and can effectively control the advantage geleg sandbank of the quality of the product. (by machine translation)

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