• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:

    公开号:SU1266472A3
    申请号:SU843801005
    申请日:1984-10-17
    公开日:1986-10-23
    发明作者:Фабр Жан-Луи；Фарж Даниель；Жамес Клод；Лаве Даниель
    申请人:Рон-Пуленк Санте (Фирма)；
    IPC主号:
    专利说明:

    at
    TL 1 The invention relates to the preparation of new derivatives of 1H, 3N pyrrole- (1,2-c) -thiazole, namely (1-imidazolyl-carbonyl-7- / 3- (3-pyridyl) 1H, 3H-pyrrole- (1, 2 -c) -thiazole formulations Oz s -l -NJ / having antiaggregate activity- The aim of the invention is to develop, using a known method, a method for producing novel compounds with valuable pharmacological properties. Example: Solution of 2 g 3- (3-pyridyl) -1H, 3N-pyrrole-l, 2-c 7-thiazolecarboxylic acid and 1.45 g -N, N.-carbonyldiimidazole in 40 cm anhydrous tetrahydrofuran is stirred at a temperature The solution is added to 0.5 g of bleaching coal, filtered, and concentrated to dry npti under reduced pressure (20 mm pF.c., 2.7 kPa) at a temperature of about 45 ° C. The residue is taken up in 100 cm of distilled water and the resulting suspension is stirred at a temperature of about 20 s for 30 minutes, the crystals are separated by filtration, washed with always 60 cm of distilled water and dried under reduced pressure (20 mm Hg, 2.7 kPa) at a temperature of about 20 ° C in the presence of potassium compound in tablets. In this way, 2 g of crude product is obtained. This product is dissolved in 35 cm of boiling isopropanol. The resulting solution is cooled to a temperature of about 4 ° C for 1 hour. The crystallized crystals are separated by filtration, washed with 2 times all, 20 cm of isopropanol, cooled to a temperature of about, and 2 times with only 0 cm of isopropyl oxide, then dried under reduced pressure (20 mm Hg, 2.7 kPa) at at a temperature of about 20 ° C in the presence of potassium compounds in tablets. In this way, 1.7 g of (1-imidazolylcarbonyl-7- [3- (3-pyridyl) -1H, 3N-pyr] rol- (1,2-c) -thiazole are obtained in the form of crista 72 s of cream color with a melting point. A study in vitro of ormobilization of platelet aggregation caused by PAF-Acether (1-octadecyl-2-oacetyl-pZ-3-glycerophosphorylcholine). when stirring, it is measured by increasing the transmission of light through the mixture. The citric acid and fresh rabbit blood is centrifuged at 100G for 20 minutes at 15 C. In this way, plasma is obtained platelet-rich, which contains at least 500,000 platelets / mm. Inject 0.2 cm of the obtained plasma into a polystyrene tube containing a rod of soft iron coated with silicone and add 0.025 cm of trisHCf 0.05-molar buffer solution (H 7.4). The tube was stirred vigorously and incubated for 10 min at 37 ° C. After this preincubation, 0.025 cm of PAE –Acether equilibrium was added at 0, Mgm / L. The transmission of light by the plasma is measured in the aggregate for 5 minutes. The difference D, TM is calculated between the transmission of plasma light before the start of aggregation and the transmission of plasma light, which was observed during the maximum transmission time on the aggregation curve. To investigate the inhibitory activity of the product with respect to the aggregation of thrombocytes caused by PAFAcether, replace the 0.025 cm Tris-HC 0.05 molar buffer (pY 7.4) by 0.025 cm of the test product dissolved in the same buffer solution. After 10 minutes pre-incubation at 37 ° C, a solution of PAF-Acether is added. For each concentration, the difference iXg is calculated from the test product (light transmission before the start of aggregation minus light transmission at time t) i Then, a curve is drawn that gives the dependence of dTe on C expressed in mg / l of the reaction medium. The point of the LCT curve f (s) the ordinate of which is yTM, and the abscissa corresponds with the SC, is; product concentration causing inhibition of 50% aggregation caused by PAF-Ac ether.
    312664724
    The dose of the product (DLjo) is determined. Biological results: toxicant, given to mice via mouse (DL), mg / kg (
    mouth, death is 50% of the mouth), aggregation with PAF-Acether
    Ihhx (rabbit) Clfg 3.9 mg / l.
    权利要求:
    Claims (1)
    [1]
    METHOD FOR PRODUCING (1-IMIDA30LYL-CARBONIL) -7 / 3- (3-PYRIDYL) -1H, 3H-PYRR0L- (1,2-c) -THIAZOLES of the formula characterized in that Ν, Ν -carbonyldiimidazolyl is reacted with 3- (3-pyridyl) -1H, 3H-pyrrole (1,2-c) thiazolecarboxylic acid of the formula
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US3544590A|1967-04-28|1970-12-01|Exxon Research Engineering Co|Cyclic amines and the process for their formation|
    US3865839A|1973-03-01|1975-02-11|Hoechst Co American|Thiopyranopyrrolylsalicyclic acids and derivatives thereof|FR2557111B1|1983-12-21|1986-04-11|Rhone Poulenc Sante|NOVEL ORTHO-CONDENSES OF PYRROLE, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM|
    FR2601015B1|1986-07-04|1988-08-05|Rhone Poulenc Sante|NOVEL 1H, 3H-PYRROLOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    FR2601016B1|1986-07-04|1988-10-07|Rhone Poulenc Sante|NOVEL 1H, 3H-PYRROLOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    CN1030415A|1987-02-20|1989-01-18|山之内制药株式会社|Saturated heterocycle carboxamide derivatives and its preparation method|
    FR2617484B1|1987-07-02|1989-10-20|Rhone Poulenc Sante|PROCESS FOR THE PREPARATION OF ACID-3 1H-3H-PYRROLOTHIAZOLECARBOXYLIQUE-7 DEXTROGYRE|
    FR2626004B1|1988-01-20|1991-08-02|Rhone Poulenc Sante|PROCESS FOR THE PREPARATION OF-3 1H, 3H-PYRROLOTHIAZOLECARBONITRILE-7|
    FR2644456B1|1989-03-17|1991-07-05|Rhone Poulenc Sante|NOVEL 1H, 3H-PYRROLOTHIAZOLECARBOXAMIDE-7 DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    JPH05501103A|1989-06-26|1993-03-04|
    FR2678834A1|1991-07-09|1993-01-15|Rhone Poulenc Rorer Sa|NOVEL THERAPEUTIC APPLICATION OF PYRIDYLPYRROLOTHIAZOLE CARBOXAMIDE.|
    US5459152A|1991-07-17|1995-10-17|Abbott Laboratories|Platelet activating factor antagonists|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    FR8300453A|FR2541280B1|1983-01-13|1983-01-13|NEW DERIVATIVES OF 1H, 3H-PYRROLOTHIAZOLECARBOXAMIDE-7, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM|
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