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Method for synthesizing tert-2-(3- (2S)-4- butyl)-1- ester of n-oxo-isothiazole alkyloxycarbonylpyrrolidinecarboxylic acid (by machine translation)

The technical scheme of the present (2S) – 4 – invention is that the following) – 1 – technical scheme of the present invention, is that the compound is obtained. by the continuous production of the: compound having L – the following beneficial, effects: the Boc compound is obtained II, from the following technical scheme III, No.No. STR3, No.No. IV; The technical proposal of the present invention is the following technical proposal: II No.No. STR3 III. No., No. The following technical II, proposal III Boc – L – of the present, N – Boc – 4 – IV invention is the following (2S) – 4 -) – 1 – technical proposal: No.No. STR8. No. II No.No. :(1) STR8 III, No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR2, No.No.No. STR8No.No.No.No. .(2) STR8No., No.No.No.. STR8No., No.No.No., STR2No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR8No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR7No.No.No.No. STR2No.No.No. STR7No.No.No.No. ST (by machine translation)

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Facile new industrial process for synthesis of teneligliptin through new intermediates and its optimization with control of impurities

Abstract: The present study is related to a commercially practicable new synthetic process for production of teneligliptin hydrobromide hydrate (1), a dipeptidyl peptidase-4 (DPP-4) inhibitor. Key strategies in the new process include preparation and isolation of new intermediates such as a better reactive nosyl derivative (3c) of l-proline methyl ester (2), its stereoselective substituted intermediate (5) with 1-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazine (4) through SN2-type nucleophilic substitution, and isolation of carboxylic acid derivative 6 by deesterification of intermediate 5. The reaction conditions for preparation of new intermediates, and the additionally used coupling reaction for amidation and deprotection of N-Boc were optimized with control of impurities to improve the quality of drug molecule 1 with good yield. The developed synthetic strategy offers significant advantages over existing synthetic approaches, avoiding use of expensive reagents, long time consumption, and laborious procedures involving isolation of intermediates. The developed process for drug molecule 1, achieving overall yield of 37?39% over six sequential chemical transformations, enables rapid delivery of multi-kilogram quantities of the desired active pharmaceutical ingredient (API), meeting stringent purity requirements. Graphical Abstract: [Figure not available: see fulltext.].

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Heterocyclic compounds containing nitrogen and sulfur, processes for their preparation and pharmaceutical compositions thereof

The invention relates to nitrogen- and sulfur-?containing heterocyclic compounds of the formula (I), wherein, Ar represents an optionally mono- or polysubstituted aryl or heteroaryl group;, R? represents a carbonyl or (C2 6alkenyl)-?carbonyl group;, R? represents a hydrogen atom, or a C1 6alkyl, phenyl or phenyl(C1 4alkyl) group;, R? represents a hydrogen atom or a (C1 6 alkoxy)carbonyl group;, R4 and R5, which may be the same or different, represent a hydrogen atom or a C1 6alkyl group;, R6 represents a hydrogen atom or a C1 6alkyl group or halophenyl group;, m is 0 or 1; and, n is 1 or 2,with the proviso that R? is a hydrogen atom when m is 0, and acid addition salts of the compounds of formula (I) and pharmaceutical compositions thereof. The invention also relates to processes for the preparation of these compounds. The compounds of formula (I) show a significant cerebral antihypoxic activity.

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Protective effects of zingerone derivate on ionizing radiation-induced intestinal injury

Intestinal injury is the primary toxicity of radiotherapy for pelvic and abdominal tumors, and it is also one of the common acute complications of radiotherapy. At present, there are no effective drugs to prevent intestinal injury in the clinic. Zingerone is a natural product with radioprotective effects. In this study, a novel compound (thiazolidine hydrochloride, TZC01) was synthesized by structural modification of zingerone. The effects of TZC01 on preventing intestinal injury from radiation were further investigated in this study. C57BL/6N mice were exposed to a lethal dose of abdominal irradiation (ABI) with and without TZC01 treatments. The morphological changes of the intestine and various makers of intestinal crypt cells were investigated. Treatment with TZC01 improved the survival rate of mice exposed to 12 Gy ABI. Moreover, TZC01 protected the intestinal morphology of mice, decreased the apoptotic rate of intestinal crypt cells, maintained cell regeneration and promoted crypt cell proliferation and differentiation. This study suggests that TZC01 has preventive and therapeutic effects on radiation enteritis by promoting the proliferation and differentiation of crypt cells to protect the small intestine from the toxic effects of ionizing radiation. Furthermore, the study of TCZ01 lays a strong foundation for developing novel radioprotectors with multiple properties.

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Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors

Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice.

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Synthesis of 2,3,4,7-tetrahydro[1,4]thiazepines from thiazolidines and beta-enaminonitriles

A wide library of 2,3,4,7-tetrahydro[1,4]thiazepines have been prepared by simple heating of thiazolidine and beta-enaminonitrile derivatives in acetonitrile. The procedure, whose yields depend on the nature and position of the substituents, gave good results if the substituents were not very bulky but it is less effective when starting from 2-substituted thiazolidines.

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Related Products of 14446-47-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 14446-47-0, molcular formula is C3H8ClNS, introducing its new discovery.

COMBINATION THERAPY FOR GLYCAEMIC CONTROL

The present invention relates to method of treatment, in particular to a method for the treatment of diabetes mellitus, especiall non-insulin dependent diabetes mellitus (NIDDM) or Type 2 diabetes and conditions associat d with diabetes mellitus the predi,tbetic state and/or obesity and to compositions for use in s ch method.

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Application of 14446-47-0, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 14446-47-0, Thiazolidine hydrochloride, introducing its new discovery.

Heterocyclic compounds containing nitrogen and sulfur, pharmaceutical compositions containing them and process for preparing same

The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) STR1 Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group; R1 means a carbonyl or (C2-6 alkenyl)carbonyl group; R2 stands for hydrogen C1-6 alkyl, phenyl or phenyl (C1-4 alkyl) group; R3 means hydrogen or (C1-6 alkoxy)carbonyl group; R4 and R5 stand, independently from each other, for hydrogen or C1-6 alkyl group; R6 ogen, C1-6 alkyl group or halophenyl group; m is 0 or 1; and n is 1 or 2, with the proviso that R2 means hydrogen when m is 0. The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer’s disease or disturbances of the cognitive function.

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SUBSTITUTED 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRIDINE-3(2H)-ONES AND 2,5,6,7-TETRAHYDRO-3H-PYRROLO[2,1-C][1,2,4]TRIAZOL-3-ONES, AND USE THEREOF

The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.

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Thiazolidine derivatives, process for their preparation and pharmaceutical compositions

Compounds of formula I STR1 wherein A represents: a saturated or unsaturated acyclic residue; a saturated cyclic or heterocyclic residue; a saturated or unsaturated bicyclic residue; and R represents OH, a C1 -C4 alkoxy group or a straight or heterocycle aminoresidue; R1 represents hydrogen, an alkyl group or an aromatic or heteroaromatic residue. Compounds I are endowed with valuable therapeutic characteristics.

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