- Inhibition of platelet activation, aggregation and/or adhesion by hypothermia
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A method for treating acute coronary syndromes (i.e., unstable angina or non-Q-wave MI) or transient ischemic attacks in a human or animal patient by placing a heat exchange apparatus in the patient's vasculature and using that heat exchange apparatus to cool the patient to a temperature (e.g. 30-36 degrees C.) at which platelet inhibition (i.e., inhibition of platelet activation and/or aggregation and/or adhesion) occurs. Anti-shivering drugs or anesthesia may be administered to patients whose body temperature is cooled below that patient's shivering threshold (typically approximately 35.5 degrees C.). If it is determined that platelet inhibition is no longer desirable, such as when the patient is about to undergo a surgical or interventional procedure wherein bleeding could be problematic, the hypothermia-induced platelet inhibition may be rapidly reversed by using the intravascular heat exchange apparatus to re-warm the patient's body to normothermia or near normothermia.
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- 2-Chlorophenyl zinc bromide: A convenient nucleophile for the mannich-related multicomponent synthesis of clopidogrel and ticlopidine
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A methodological study devoted to the Mannich-like multicomponent synthesis of the antiplatelet agent (±)-clopidogrel (7) and the ethyl ester analogue 6 is described. The process involves the formation of 2-chlorophenyl zinc bromide (2) and its subsequent reaction with an alkyl glyoxylate and 4,5,6,7-tetrahydrothieno[3,2-c]pyridine (3). We demonstrate that the organozinc reagent 2 also constitutes a very convenient nucleophile for the multicomponent synthesis of the benzylamine core of ticlopidine (9).
- Isabelle, Aillaud,Haurena, Caroline,Gall, Erwan Le,Martens, Thierry,Ricci, Gino
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experimental part
p. 8144 - 8155
(2011/02/27)
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- METHOD OF PREPARING THIENO[3,2-C]PYRIDINE DERIVATIVES AND INTERMEDIATES USED THEREIN
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Ticlopidine and clopidogrel having high blood platelet aggregation inhibitory and anti-thrombotic activities are simply prepared by reacting a substituted thiophene derivative with a 2-chlorobenzylamine derivative.
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Page/Page column 22-23
(2010/02/14)
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- MEDICINAL COMPOSITION
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A pharmaceutical composition containing a drug (A), a waxy substance (B), and synthetic aluminum silicate and/or hydrous silicon dioxide (C). The invention provides a granular pharmaceutical composition suitable for providing a pharmaceutical characterized in that adhesion of granules thereof onto a granulation apparatus during granulation is minimized and caking of the granules is suppressed.
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- MEDICINAL COMPOSITIONS
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The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.
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- Preparation of 2-(2-thienyl) ethylamine and synthesis of thieno [3,2-C] pyridine derivatives therefrom
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Compounds of the formulae:and wherein:, R1, R2, R3 and R4 are independently hydrogen, lower alkyl of one to six carbon atoms, aryl or substituted aryl;, are advantageously converted to isocyanurate compounds, 2-(2-thienyl)ethylamine compounds and thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
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- 2-thienylglycidic derivative, process for its preparation and its use as synthesis intermediate
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The invention relates to isopropyl 2-thienylglycidate of formula: STR1 obtained by reaction of 2-thienylcarboxaldehyde with an isopropyl haloacetate. It is employed as a synthesis intermediate in the preparation of 2-thienylacetaldoxime and of medications derived from thieno[3,2-c]pyridine.
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- USE OF MERCAPTOACETALDEHYDE DIMER IN A NOVEL THIENOANNELATION SEQUENCE. A SHORT SYNTHESIS OF TICLOPIDINE
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A short synthesis of ticlopidine (1) was achieved by condensation of mercaptoacetaldehyde dimer (2) with piperidone (3b) in the presence of lithium diisopropylamide followed by dehydration.
- Gooding, Owen W.,Beard, Colin C.
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p. 1777 - 1780
(2007/10/02)
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- Carbamate salts of 2-(2'-thienyl)alkylamines
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The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): STR1 with CO2 in a hydrocarbon solvent to obtain the carbamate salt of formula II: STR2
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- Process for the production of 4,5,6,7-tetrahydrothieno-[3,2-C]-pyridines
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A process for the production of 4,5,6,7-tetrahydrothieno-[3,2-c]-pyridines of the formula: STR1 Thus, in the case of a 4-oxo-3-piperidine-3-carboxylic acid ester of the formula: STR2 an allyl group is introduced in the 3 position, the ester function in the 3 position is removed, the resultant compound of the formula: STR3 is ionized, reduced to the corresponding aldehyde of the formula: STR4 and with H2 S/HCl in the presence of a metal halide is cyclized to the end product. The synthesized compounds have antithrombotic action.
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- 2-(2-nitrovinyl)thiophene reduction and synthesis of thieno[3,2-c]pyridine derivatives
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An improved process for the reduction of 2-(2-nitrovinyl)thiophene to form 2-(2-thienyl)ethylamine employs a boron-containing reducing agent, preferably diborane. The 2-(2-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
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- SYNTHESIS OF THIENO- AND THIENOPYRID-3-ONES
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The Friedel-Crafts cyclization of N-(3-thenyl)- and N-(2-thenyl)-glycine derivatives is described.The method leads to an alternative synthesis of 1,2,3,4-tetrahydro-N--thienopyridine(ticlopidine) (6d).
- Satake, Kyosuke,Imai, Toshiyuki,Kimura, Masaru,Morosawa, Shiro
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p. 1271 - 1274
(2007/10/02)
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- Process for the preparation of thieno-pyridine derivatives
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This invention relates to a process for the preparation of thieno-pyridine derivatives having the structural formula: STR1 in which R1 represents an optionally substituted alkyl, aryl or aralkyl radical, and R2 and R3 represnt each hydrogen or a lower alkyl, aryl or heterocyclic radical, comprising: (a) reacting a derivative of the formula STR2 in which R2 and R3 are as defined for formula (I) and X represents hydrogen, or an alkali metal, or a radical Mg-Y in which Y represents halogen, with a halo-sulfonyl derivative having the formula: in which Hal represents halogen and R4 represents an optionally substituted alkyl, aryl or aralkyl group, to give a compound having the formula: STR3 (b) subsequently reacting the latter compound with an amine of the formula: in which R1 is as defined for the formula (I), to give a compound having the formula: STR4 and (c) subsequently cyclizing compound (VI) with formaldehyde to give the derivative of the formula (I).
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- Synthesis of thienopyridine and furopyridine derivatives of therapeutic interest
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5-Benzyl-4,5,6,7-tetrahydrothieno [3,2-c] pyridines and analogous furopyridines were synthesized by NaBH4 reduction of the corresponding quaternary ammonium salts (method A). In the former series, the same derivatives were obtained by condensing benzyl halides with tetrahydrothienopyridine (method B).
- Maffrand,Eloy
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p. 483 - 486
(2007/10/05)
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