- Solid dispersions comprising Telmisartan and the preparation method thereof
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The solid dispersions comprising telmisartan and a manufacturing method thereof, according to the present invention, unlike conventional methods requiring a low yield, can manufacture telmisartan of a high yield through simple and short steps by using a relatively inexpensive raw material, can secure excellent quality through reduction of generation of decomposition products, and can manufacture the solid dispersions on a mass production basis to be commercially available. Therefore, the solid dispersions of novel crystalline polymorph of the telmisartan of the present invention has improved storage stability and solubility, and can be synthesized at a high yield, thereby being expected to be very useful in the manufacture of pharmaceuticals.COPYRIGHT KIPO 2018
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Paragraph 0111; 0112; 0118
(2018/05/15)
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- Telmisartan alkyl ester (by machine translation)
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PROBLEM TO BE SOLVED: To provide a method for stably and efficiently producing a high quality telmisartan alkyl ester. SOLUTION: The method for producing the telmisartan alkyl ester comprises mixing 2-n-propyl-4-methyl-6-(1'-methylbenzimidazol-2-yl)benzimidazole with a polar aprotic solvent and a base, and then sequentially adding an alkyl 4'-bromomethylbiphenyl-2-carboxylate solution thereto. Thus, the telmisartan alkyl ester little containing impurities can efficiently be produced. COPYRIGHT: (C)2011,JPO&INPIT
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Paragraph 0049
(2018/10/31)
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- A modification to the synthesis of Telmisartan: An antihypertensive drug
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A highly efficient approach to the synthesis of Telmisartan is described. Directed ortho-metalation of 4,4-dimethyl-2-phenyl-4,5-dihydrooxazole provided the key organozinc intermediate for a palladium catalysed biaryl coupling with 3′-(4-bromobenzyl)-1,7′-dimethyl-2′-propyl-1 H,3′ H-2,5′-bibenzo[d]imidazole which was obtained from alkylation of 1,7′-dimethyl-2′-propyl-1 H,3′H-2,5′-bibenzo[d] imidazole. This methodology overcomes many of the drawbacks associated with previously reported syntheses.
- Kumar, A. Sanjeev,Ghosh, Samir,Mehta
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scheme or table
p. 95 - 97
(2010/07/05)
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- PROCESS FOR PREPARING TELMISARTAN
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The present invention refers to an improved process for the preparation of telmisartan or a pharmaceutical acceptable salt thereof through hydrolysis compounds of formula general (I) wherein R is tert-butyl ester (Ia) or salts thereof. Preferably, the invention discloses the preparation of telmisartan through hydrolysis of novel organic salts of compounds of formula (I), particularly wherein R is tert-butyl ester (Ia). The invention also relates to a process for the preparation of these novel organic salts, in particular wherein R is tert-butyl ester (Ia) and its use in the preparation of telmisartan.
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Page/Page column 14
(2011/01/12)
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- PROCESS FOR PREPARATION OF TELMISARTAN
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A process for preparation of telmisartan comprises: (i) oxidation of compound of formula (a), wherein R2 is a hydrogen atom or a substituent of formula (b), in which R1 is a protecting group for the carboxyl function, to an aldehyde of formula (c), in which R2 is defined as in the formula (a), and, optionally, (ii) in case R2 in the compound (c) thus obtained is a hydrogen atom, iV-alkylation of the compound (c) with a biphenyl derivative, (iii) treatment of the compound (c) thus obtained with N- methyl- o-nitroaniline in a cyclocondensation reaction, and (iv) cleavage of the protecting group R1.
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Page/Page column 18-19
(2009/10/30)
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- 6-Substituted benzimidazoles as new nonpeptide angiotensin II receptor antagonists: Synthesis, biological activity, and structure-activity relationships
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Starting from the recently reported nonpeptidic angiotensin II (AII) receptor antagonists DuP 753 (1) and Exp 7711 (2), we have designed and investigated novel substituted benzimidazoles. Systematic variation of several substituents at the benzimidazole ring positions 4-7 led to the finding that substitution in position 6 with acylamino groups results in highly active AII antagonists. Compounds with 6-membered lactam or sultam substituents in position 6 of benzimidazole showed receptor activities in the low nanomolar range but were only weakly active when given orally to rats. In contrast, analogous substitution of the benzimidazole moiety with basic heterocycles resulted in potent AII antagonists which were also well absorbed after oral application. The most active compound of this series, 33 (BIBR 277), was selected as a candidate for clinical development. On the basis of molecular modeling studies a binding model of this new class of AII antagonists to the AT1 receptor is proposed.
- Ries,Mihm,Narr,Hasselbach,Wittneben,Entzeroth,Van Meel,Wienen,Hauel
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p. 4040 - 4051
(2007/10/02)
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