公开(公告)号：WO2003068203A1

公开(公告)日：2003-08-21

申请号：PCT/CZ2003/000008

申请日：2003-01-30

Applicant: LECIVA, a.s. ,  DOLEZAL, Tomàs ,  KRSIAK, Miloslav ,  TOMASEK, Vaclav

Inventor： DOLEZAL, Tomàs ,  KRSIAK, Miloslav ,  TOMASEK, Vaclav

IPC: A61K31/09

CPC classification number: A61K31/09 ,  A61K31/522 ,  A61K2300/00

Abstract: The use of the combination of a non-steroidal anti-inflammatory agent and 3-(2-methoxyphenoxy)-1, 2-propanediol (guaifenesin) and optionally caffeine, for the manufacture of a pharmaceutical intended for the treatment of acute pains.

Abstract translation: 使用非甾体抗炎剂和3-（2-甲氧基苯氧基）-1,2-丙二醇（愈创甘油醚）和任选的咖啡因的组合来制造用于治疗急性疼痛的药物。

公开(公告)号：WO2004020443A1

公开(公告)日：2004-03-11

申请号：PCT/CZ2003/000049

申请日：2003-08-26

Applicant: LECIVA, a.s. ,  VEVERKA, Miroslav ,  VODNY, Stefan ,  VEVERKOVA, Eva ,  HAJICEK, Josef ,  STEPANKOVA, Hana

Inventor： VEVERKA, Miroslav ,  VODNY, Stefan ,  VEVERKOVA, Eva ,  HAJICEK, Josef ,  STEPANKOVA, Hana

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: A method for manufacturing hydrogen sulphate (alpha S) of the alpha-(2-chlorophenyl)-6,7­dihydro-thieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester (clopidogrel hydrogen sulphate) of formula I, in crystalline Form I, wherein the compound of formula is separated out of a solution of clopidogrel in the form of the free base or salt in a solvent selected from the series of primary, secondary or tertiary C1-C5 alcohols, their esters with Cl-C4 carboxylic acids, or optionally of mixtures thereof.

Abstract translation: 制备α-（2-氯苯基）-6,7-二氢 - 噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯（氯吡格雷硫酸氢盐）的硫酸氢盐（αS） 式I的结晶形式I，其中将式I化合物在游离碱或盐形式的氯吡格雷溶液中从选自一级，二级或三级C 1 -C 5醇的溶剂中分离出来，其酯 与C 1 -C 4羧酸或任选地其混合物。

公开(公告)号：WO2003068739A1

公开(公告)日：2003-08-21

申请号：PCT/CZ2003/000007

申请日：2003-01-30

Applicant: LECIVA, a.s. ,  RADL, Stanislav ,  STACH, Jan

Inventor： RADL, Stanislav ,  STACH, Jan

IPC: C07D207/34

CPC classification number: C07D207/337

Abstract: A method of manufacturing an amorphous form of the hemi-calcium salt of (3R, 5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid of formula (I), in which (3R, 5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid or its salt with a cation M + wherein M + is either a cation of an alkali metal or an ammonium cation of formula R n N (+) H (4-n) wherein R is lower C 1 -C 5 alkyl, n may reach values ranging between 0 and 3, is, without isolating the intermediate in the form of the hemi-calcium salt or of another salt, acid or lactone, converted, in a solution, by the treatment with the calcium salt or calcium hydroxide, or a calcium C 1 -C 5 alcoholate, to the hemi-calcium salt, and the latter is precipitated with a C 1 -C 5 hydrocarbon or dialkylether of formula R 1 OR 2 , wherein each of R 1 and R 2 is a C 1 -C 5 alkyl group. The starting acid or its salt is prepared starting from (3R, 5R) tert-butyl (6-{2-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-ethyl}-2,2-dimethyl-[1,3]dioxane-4-yl)-acetate of formula II.

Abstract translation: 制备（3R，5R）7- [3-苯基-4-苯基氨基甲酰基-2-（4-氟苯基）-5-异丙基 - 吡咯-1-基] -3（3H） - 嘧啶的半钙盐的无定形形式的方法 （I）的5-二羟基庚酸，其中（3R，5R）7- [3-苯基-4-苯基氨基甲酰基-2-（4-氟苯基）-5-异丙基 - 吡咯-1-基] 5-羟基庚酸或其盐与阳离子M +，其中M +是碱金属的阳离子或式RnN（+）H（4-n）的铵阳离子，其中R为低级C1-C5烷基，n可达到值 范围在0和3之间，是不分离半钙盐或另一种盐，酸或内酯形式的中间体，在溶液中通过用钙盐或氢氧化钙处理或钙 C1-C5醇化物与半钙盐反应，后者用式R1OR2的C1-C5烃或二烷基醚沉淀，其中R1和R2各自为C1-C5烷基。 起始酸或其盐由（3R，5R）（6- {2- [3-苯基-4-苯基氨基甲酰基-2-（4-氟苯基）-5-异丙基 - 吡咯-1-基 ] - 乙基} -2,2-二甲基 - [1,3]二氧杂环己烷-4-基） - 乙酸乙酯。

公开(公告)号：WO2003053473A3

公开(公告)日：2003-07-03

申请号：PCT/CZ2002/000070

申请日：2002-12-20

Applicant: LECIVA, A.S. ,  ULBRICH, Karel ,  ETRYCH, Tomás ,  RIHOVA, Blanka ,  JELINKOVA, Markéta ,  KOVAR, Marek

Inventor： ULBRICH, Karel ,  ETRYCH, Tomás ,  RIHOVA, Blanka ,  JELINKOVA, Markéta ,  KOVAR, Marek

IPC: A61K47/48

Abstract: Conjugates consisting of a polymeric carrier constituted by 30 to 3,000 monomer units linked to form a polymeric chain, composed of a) 60 to 99 % of N -(2-hydroxypropyl)methacrylamide units, b) 1 to 25% of units of methacryloylated hydrazones of α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides terminated with a molecule of an anthracycline cancerostatic, c) 0.5 to 15 % of units of methacryloylated α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides or their sodium salts.

公开(公告)号：WO2003035608A1

公开(公告)日：2003-05-01

申请号：PCT/CZ2002/000053

申请日：2002-10-03

Applicant: LECIVA, A.S. ,  HAJICEK, Josef ,  SLAVÍKOVÁ, Marketa

Inventor： HAJICEK, Josef ,  SLAVÍKOVÁ, Marketa

IPC: C07C303/40

CPC classification number: C07C303/40 ,  C07C311/37

Abstract: The compound of formula (I) is obtained via reaction of a compound of formula (III), or (VII), with a compound of formula (IV).

Abstract translation: 式（I）化合物通过式（III）或（VII）化合物与式（IV）化合物的反应得到。