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1. 发明申请

WO2005073235A3 PROCESS FOR THE SYNTHESIS OF N- [3-(3-CYANOPYRAZOLO [1,5A] PYRIMIDIN-7-YL)-PHENYL]-N-ETHYL-ACETAMIDE 审中-公开
标题翻译：合成N- [3-（3-氰基吡唑并[1,5-a]嘧啶-7-基） - 苯基] -N-乙基 - 乙酰胺的方法
公开(公告)号：WO2005073235A3
公开(公告)日：2005-10-06
申请号：PCT/HU2005000008
申请日：2005-01-31
申请人： RICHTER GEDEON VEGYESZET , CZIBULA LASZLO , DOBAY LASZLO , SZOKE KATALIN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , TARKANYI GABOR
发明人： CZIBULA LASZLO , DOBAY LASZLO , SZOKE KATALIN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , TARKANYI GABOR
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07C233/43
摘要： The invention relates to N- [3- (3-cyanopyrazolo [1,5-a] pyrimidin-7-yl) - phenyl]-N-ethyl-acetamide of formula (IV) containing less than 0.2 % impurities, which is suitable for therapeutic application. Furthermore the invention relates to a process for the synthesis of therapeutically applicable compound of formula (IV) containing less than 0.2 % impurities by reacting the new intermediate N-{3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethylacetamide hydrochloride of formula (II) and 3-amino-4-pyrazol-carbonitrile base of formula (III) in an acid free medium. The invention also relates to the new N- {3- [3- (dimethylamino) -1- oxo -2- propenyl]phenyl } -N-ethyl-acetamide hydrochloride of formula (II). The invention also relates to a process for the synthesis of the new N- [3- [3, (dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl-acetamide hydrochloride of formula (II) having a purity of more than 99.5 %. Furthermore the invention relates to N-{3-[3-cyanopyrazolo (1,5-a) pyrimidin]6 -yl-3- [ (3-N-ethyl-acetamido-phenyl) -3-oxo-propen-1-yl] - (pyrimidin-7-yl) -phenyl} - N-ethyl-acet-amide of formula (V), which is an isolated new impurity formed in 0.07 % yield during the synthesis of compound of formula (IV).
摘要翻译：本发明涉及含有少于0.2％杂质的式（IV）的N- [3-（3-氰基吡唑并[1,5-a]嘧啶-7-基） - 苯基] -N-乙基 - 乙酰胺，用于治疗应用。此外，本发明涉及一种通过使新的中间体N- {3- [3-（二甲基氨基）-1-氧代-2-丙烯基] -1,3,5-三嗪与式（IV）化合物反应合成含有少于0.2％苯基} -N-乙基乙酰胺盐酸盐和式（III）的3-氨基-4-吡唑甲腈碱在无酸介质中反应。本发明还涉及式（II）的新的N- {3- [3-（二甲基氨基）-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐。本发明还涉及合成式（II）的新的N- [3- [3（二甲基氨基）-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐的方法，超过99.5％。此外，本发明涉及N- {3- [3-氰基吡唑并（1,5-a）嘧啶] -6-基-3 - [（3-N-乙基 - 乙酰氨基 - 苯基）-3-氧代 - 嘧啶-7-基] - 苯基} -N-乙基 - 乙酰胺，其是在合成式（IV）化合物期间以0.07％收率形成的分离的新杂质。

2. 发明申请

WO1993013076A1 GASTRIC ACID SECRETION-INHIBITING, AND GASTROCYTOPROTECTIVE PHARMACEUTICAL COMPOSITIONS, NOVEL FAMOTIDINE SALTS AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：胃酸分泌抑制和胃肠道保护性药物组合物，新型孕激素及其制备方法
公开(公告)号：WO1993013076A1
公开(公告)日：1993-07-08
申请号：PCT/HU1992000057
申请日：1992-12-18
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , FODOR, Tamás , FISCHER, János , DOBAY, László , MARVANYOS, Ede , SZOKE, Katalin , BALLO, Ildikó , TRISCHLER, Ferenc , PERÉNYI, Éva , GASPAR, Katalin , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D233/88
CPC分类号： C07D335/06 , C07C59/76 , C07C59/84 , C07C59/86 , C07C317/44 , C07C323/54 , C07D215/48 , C07D277/48 , C07D311/24
摘要： The invention relates to a novel gastric acid secretion-inhibiting and gastrocytoprotective pharmaceutical composition, which comprises as active ingredient a 10:1 to 1:10 mixture by weight of a compound of formula (II), wherein A means a group of formula (A1), wherein R stands for a hydrogen atom or a hydroxy, C1-4alkyl or alkoxy group; X means oxygen or sulfur or NH group; or A means a group of formula (A2), wherein Q stands for a hydrogen atom or a phenyl or substituted phenyl group; m is 0 or 1; n is 0, 1 or 2; p is 1 when the dotted line represents a chemical bond, or p is 2 when the dotted line means no chemical bond; or A means a group of formula (A3), wherein R means methyl, phenyl, substituted phenyl, C-4-alkyl, C1-4alkoxy or tetrahydronaphthyl group with the compound of formula (III) or a new compound of formula (I), wherein A is as defined above and B represents the protonated form of the compound of formula (III). The invention furthermore relates to the novel compounds of formula (I), wherein A and B are as defined above, and a process for preparing these novel compounds. The compounds of formula (I) and the compositions according to the invention are useful for curing and/or preventing the inflammatory and ulcerative diseases of esophagus, stomach and duodenum of mammal.
摘要翻译：本发明涉及一种新型胃酸分泌抑制和胃镜保护性药物组合物，其包含作为活性成分的式（II）化合物的10:1至1:10混合物，其中A表示式（A1 ），其中R代表氢原子或羟基，C1-4烷基或烷氧基; X表示氧或硫或NH基; 或A表示式（A2）的基团，其中Q表示氢原子或苯基或取代的苯基; m为0或1; n为0,1或2; 当虚线表示化学键时，p为1，当虚线表示无化学键时，p为2; 或A表示式（A3）的基团，其中R 1表示甲基，苯基，取代的苯基，C 1-4 - 烷基，C 1-4烷氧基或四氢萘基与式（III）的化合物或新的式（I），其中A如上所定义，B +表示式（III）化合物的质子化形式。本发明还涉及式（I）的新化合物，其中A和B +如上所定义，以及制备这些新化合物的方法。式（I）化合物和根据本发明的组合物可用于治疗和/或预防哺乳动物食管，胃和十二指肠的炎性和溃疡性疾病。

3. 发明申请

WO1993012079A1 NOVEL PHENYLSULFONYLACRYLATE ESTER DERIVATIVES 审中-公开
标题翻译：新型丙烯基丙烯酸酯衍生物
公开(公告)号：WO1993012079A1
公开(公告)日：1993-06-24
申请号：PCT/HU1992000054
申请日：1992-12-11
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , FISCHER, János , BALLO, Ildikó , FODOR, Tamás , SZOKE, Katalin , PETÉNYI GALLO, Éva , MARVANYOS, Ede , WALLERSTEIN, Szilvia , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07C317/44
CPC分类号： C07D311/46 , C07C317/44
摘要： The invention relates to novel phenylsulfonylacrylate ester derivatives of formula (I), wherein R stands for a C1-4alkyl group; a phenyl group optionally substituted by a C1-4alkoxy or a C1-4alkylcarbonyloxy group; an aralkyl group optionally substituted by a C1-4alkoxy group on the aromatic ring; a phenylsulfonylvinyl or phenylcarbonylvinyl group optionally substituted by a halogen on their phenyl moiety; methylsulfonylvinyl group; 4-oxo-4H-1-benzopyran-2-yl or 4-oxo-4H-1-benzothiopyran-2-yl group; R means hydrogen or a halogen; and n is 2 or 3. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the compounds of formula (I). The compounds of the invention possess gastric acid secreto-inhibitory and gastrocytoprotective effects. Thus, they are useful for the prevention and/or healing of inflammatory and ulcerative diseases of esophagus, stomach or duodenum.
摘要翻译：本发明涉及式（I）的新型苯磺酰基丙烯酸酯衍生物，其中R代表C1-4烷基; 任选被C 1-4烷氧基或C 1-4烷基羰基氧基取代的苯基; 任选被芳环上的C 1-4烷氧基取代的芳烷基; 任选在其苯基部分上被卤素取代的苯基磺酰基乙烯基或苯基羰基乙烯基; 甲基磺酰基乙烯基; 4-氧代-4H-1-苯并吡喃-2-基或4-氧代-4H-1-苯并噻喃-2-基; R 1表示氢或卤素; 本发明还涉及含有这些化合物的药物组合物以及制备式（I）化合物的方法。本发明的化合物具有胃酸分泌抑制和胃保护作用。因此，它们可用于预防和/或愈合食道，胃或十二指肠的炎性和溃疡性疾病。

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