- A novel benzimidazole pyridine salt compound and its synthetic method (by machine translation)
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The present invention provides a benzimidazole pyridine salt compound, its pharmaceutically acceptable salts, solvates, isomers, their metabolites form, or their mixtures, and the synthetic method of the compound, the compound has anticoagulant effect, and potentially of officinal property, can be used for the prevention or treatment of thrombin active disease related to use. (by machine translation)
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- Synthesis, Crystal Structure, and Anti-Gastric Cancer Activity of Ethyl 3-(3-Amino-4-(Methylamino)-N-(Pyridin-2-Yl) Benzamido)Propanoate
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A new heterocyclic compound ethyl 3-(3-amino-4-(methylamino)-N-(pyridin-2-yl)benzamido)propanoate (1), designed using 4-(methylamino)-3-nitrobenzoic acid (2) as a starting material is successfully obtained via a multiple synthesis route and finally characterized by IR, 1H NMR, and single crystal X-ray crystallography. In addition, the in vitro anti-cancer activity of newly synthesized complex 1 is emulated against three human gastric cancer cell lines SGC-790, MKN-4, and MKN45.
- Liu,Peng,Yue,Li,Zhang
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p. 2009 - 2014
(2020/01/11)
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- METHOD FOR PREPARING DABIGATRAN ETEXILATE INTERMEDIATE, AND INTERMEDIATE COMPOUND
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Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises; reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.
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Paragraph 0064
(2017/08/01)
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- Multi-substituted 4-methyl ester derivative of amino benzonitrile trunk and its preparation and use
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The invention provides new ester derivatives with a general formula (I) shown in the specification of multi-substituted 4-methylamino-benzamidine or pharmaceutically acceptable salts, wherein A1, A2, A3 and A4 in the formula are as defined in the specification. The compounds have an anticoagulant effect and can be used for preparing medicaments for preventing and treating thromboembolic diseases.
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- A darbey adds the group ester method for the preparation of intermediates
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The invention discloses a preparation method of a dabigatran etexilate intermediate. The preparation method of the dabigatran etexilate intermediate 2 comprises that in an aprotic organic solvent, a compound 1 and a C1-C3 alkyl alcohol solution of methylamine undergo a reaction to produce the dabigatran etexilate intermediate, wherein X represents chlorine, bromine or iodine. The preparation method of the dabigatran etexilate intermediate has simple processes, can be operated easily, has a high reaction rate and a high yield, can be purified easily and can produce the product having high purity.
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Paragraph 0032-0033
(2017/03/08)
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- A darbey adds the group ester and process for the preparation of intermediates intermediate compound
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The invention discloses a preparation method for a dabigatran etexilate intermediate and an intermediate compound. The preparation method of the dabigatran etexilate intermediate 4 comprises the following step: in a protic organic solvent, reacting a compound 3 with a C1-C3 alkanol solution of methylamine. In the formula of the compound 3, X is chlorine, bromine or iodine. The invention also discloses the intermediate compound 3 and a preparation method of the intermediate compound 3. The preparation method for the dabigatran etexilate intermediate is simple and easy to operate, the yield is high, the product is easy to purity, and the preparation method is suitable for industrial production. The formula of the preparation method for the dabigatran etexilate intermediate is shown in the specification.
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Paragraph 0062-0065
(2017/02/28)
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- A PROCESS FOR PREPARATION OF DABIGATRAN ETEXILATE MESYLATE AND INTERMEDIATES THEREOF
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The present invention relates to an improved process for the preparation of Dabigatran etexilate and its acid addition salts thereof, wherein the said process substantially eliminates the potential impurities. The present invention also relates to an intermediate of Dabigatran etexilate and process for preparation thereof.
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- Process for the Synthesis of Dabigatran and Its Intermediates
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The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-I), a pharmaceutically acceptable salt for the treatment of thromboses, cardiovascular diseases etc. and intermediates involved in the synthesis.
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- PROCESS FOR THE PREPARATION OF DABIGATRAN ETEXILATE MESYLATE AND POLYMORPHS OF INTERMEDIATES THEREOF
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The present invention provides crystalline form of intermediates of Formula 2A, The present invention also provides process for the preparation of dabigatran etexilate mesylate; polymorph of intermediates thereof; particularly processes for the preparation of crystalline form of intermediates. The present invention also relates to the use of crystalline intermediates for the preparation of dabigatran etexilate mesylate.
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- Process For The Preparation Of Benzimidazole Derivatives And Salts Thereof
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Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.
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- PROCESS FOR THE PREPARATION OF DABIGATRAN ETEXILATE MESYLATE AND POLYMORPHS OF INTERMEDIATES THEREOF
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The present invention provides crystalline form of intermediates of Formula 2A, Formula 2B and Formula E. The present invention also provides process for the preparation of dabigatran etexilate mesylate; polymorph of intermediates thereof; particularly processes for the preparation of crystalline form of intermediates. The present invention also relates to the use of crystalline intermediates for the preparation of dabigatran etexilate mesylate.
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- Structure-based design of novel potent nonpeptide thrombin inhibitors
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The clinical syndromes of thromboembolism are evoked by an excessive stimulation of the coagulation cascade. In this context, the serine protease thrombin plays a key role. Considerable efforts have therefore been devoted to the discovery of safe, orally active inhibitors of this enzyme. On the basis of the X-ray crystal structure of the peptidelike thrombin inhibitor NAPAP complexed with bovine thrombin, we have designed a new structural class of nonpeptidic inhibitors employing a 1,2,5-trisubstituted benzimidazole as the central scaffold. Supported by a series of X-ray structure analyses, we optimized the activity of these compounds. Thrombin inhibition in the lower nanomolar range could be achieved although the binding energy mainly results from nonpolar, hydrophobic interactions. To improve in vivo potency, we increased the overall hydrophilicity of the molecules by introducing carboxylate groups. The very polar compound 24 (BIBR 953) exhibited the most favorable activity profile in vivo. This zwitterionic molecule was converted into the double-prodrug 31 (BIBR 1048), which showed strong oral activity in different animal species. On the basis of these results, 31 was chosen for clinical development.
- Hauel, Norbert H.,Nar, Herbert,Priepke, Henning,Ries, Uwe,Stassen, Jean-Marie,Wienen, Wolfgang
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p. 1757 - 1766
(2007/10/03)
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