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1. 发明申请

WO1996038441A1 3(2H)-PYRIDAZINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： 3（2H） - 吡啶酮衍生物和含有这些化合物的药物组合物
公开(公告)号：WO1996038441A1
公开(公告)日：1996-12-05
申请号：PCT/HU1996000030
申请日：1996-05-28
申请人： GYOGYSZERKUTATO INTÉZET KFT , MATYUS, Péter , HARSING, László , KARIM, Mariann , KOSARY, Judit , PAPP, Agnes , SIMAY, Antal , TILAHUN, Yemane , TOMORI, Éva , HORVATH, Edit , HORVATH, Katalin , VARGA, Ildikó , ZARA, Erzsébet , BIDLO, Margit , DRUGA, Alice , RABLOCZKY, György , VARGA, Márta , KARPATI, Egon , KASZTREINER, Endre , KIRALY, István , MATHÉ, Ildikó , MATHÉ, György , SEBESTYÉN, László , MAKK, Nándor
发明人： GYOGYSZERKUTATO INTÉZET KFT
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D319/20
摘要： The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (1), and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess alpha 1- and alpha 2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.
摘要翻译：本发明涉及式（1）的R-2- [3 - （[1,4]苯并二恶烷-2-基甲基氨基）-1-丙基] -3（2H） - 哒嗪酮，以及S-2- [3- （2）的（[1,4]苯并二恶烷-2-基甲基氨基）-1-丙基] -3（2H） - 哒嗪酮及其酸加成盐以及含有这些化合物的药物组合物。此外，本发明涉及制备上述化合物的方法。式（4）和（5）的新起始化合物也参与本发明的范围。根据本发明的化合物具有α1-和α2-肾上腺素受体拮抗作用和泌尿生殖选择性。因此，它们可用于治疗良性前列腺增生。

2. 发明申请

WO1995013268A1 ULCER-INHIBITING TRIAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：抑制三唑衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1995013268A1
公开(公告)日：1995-05-18
申请号：PCT/HU1993000063
申请日：1993-11-12
申请人： GYOGYSZERKUTATO INTÉZET KFT. , MARTONNÉ, Merész, Magdolna , KUSZMANN, János , ANDRASI, Ferenc , BERZSENYI, Pál , SEBESTYÉN, László , MORAVCSIK, Imre , SZIRAKI, István
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07D249/12
CPC分类号： C07D249/12
摘要： The invention relates to novel 1,2,4-triazole derivatives of formulae (Ia) and (Ib), wherein R1 and R2, which are the same or different, stand for hydrogen; C1-4 alkyl or C1-4 alkenyl group; or a phenyl group optionally substituted by C1-4 alkyl or alkoxy group; and n is 0, 1 or 2, and acid-addition salts of these compounds. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the compounds of formulae (Ia) and (Ib). The compounds of formulae (Ia) and (Ib) inhibit gastric-acid secretion and exert a significant protective effect on the gastric mucosa (cytoprotective action). Thus, they can be used for inhibiting and treating ulcers of the digestive system.
摘要翻译：本发明涉及式（Ia）和（Ib）的新的1,2,4-三唑衍生物，其中相同或不同的R 1和R 2代表氢; C 1-4烷基或C 1-4烯基; 或任选被C 1-4烷基或烷氧基取代的苯基; 和n为0,1或2，以及这些化合物的酸加成盐。本发明还涉及含有这些化合物的药物组合物以及制备式（Ia）和（Ib）化合物的方法。式（Ia）和（Ib）的化合物抑制胃酸分泌并对胃粘膜发挥显着的保护作用（细胞保护作用）。因此，它们可用于抑制和治疗消化系统的溃疡。

3. 发明申请

WO1992012137A1 NOVEL 3(2H)-PYRIDAZINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新的3（2H） - 吡啶酮，含有它们的药物组合物及其制备方法
公开(公告)号：WO1992012137A1
公开(公告)日：1992-07-23
申请号：PCT/HU1991000054
申请日：1991-12-20
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , MATYUS, Péter , RABLOCZKY, György , JASZLITS, László , KOSARY, Judit , KÜRTHY, Mária , PAPPNÉ BEHR, Agnes , ZARA, Dénesné , KARPATI, Egon , KOVACS, Anikó , SEBESTYÉN, László , FARKAS, Lajos , CZAKO, Klára , VARGA, Ildikó , ELEK, Sándor , MAGO, Istvánné , MATHÉ, György , SZEDERKÉNYI, Ferenc , JEDNAKOVITS, Andrea , BODI, Ilona , PODANYI, Benjamin
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D237/22
CPC分类号： C07D401/06 , C07D237/22 , C07D401/12 , C07D405/06
摘要： The invention relates to novel, racemic and optically active 3(2H)-pyridazinone derivatives of general formula (I), wherein R means hydrogen; a C1-4alkyl group optionally substituted by an R R N- group where R and R , being the same or different, stand for a C1-4alkyl group or R R N- together represents a 6-membered heterocyclic group optionally containing an oxygen or an R N- moiety where R is a C1-4alkyl optionally substituted by a phenyoxy group or a C3-5alkenyl optionally substituted by a phenyl group; or a C1-4alkyl group substituted by a mono- or polysubstituted phenyl, phenoxy or benzyloxy group; or a C3-5alkenyl or C3-5alkynyl optionally substituted by an unsubstituted or optionally substituted phenyl group; or a phenyl group; R means hydrogen; or a C1-4alkyl optionally substituted by a morpholino, pyridyl, 1,4-benzodioxanyl or an optionally substituted phenyl group; R means hydrogen or an optionally substituted phenyl group; R means hydrogen; or R CO- group where R is a C1-4alkyl, phenyl or pyridyl group or an amino group substituted by a C1-4alkyl group; or an -SO3M moiety where M is hydrogen or an organic or inorganic cation; X means halogen; and n is 1, 2 or 3, with the proviso that R is different from a C1-4alkyl, alkenyl, aralkyl and phenyl group when n is 1, as well as their tautomers and the acid addition salts of these compounds. The invention further relates to pharmaceutical compositions containing as active ingredient a compound of general formula (I) as well as to a process for the preparation of compounds of general formula (I). The compounds of the invention possess a significant calmodulin-antagonizing effect, decrease the coronary resistance and are less toxic. Thus, these compounds are useful for treating cardiovascular diseases, particularly angina pectoris.
摘要翻译：本发明涉及通式（I）的新型外消旋和光学活性的3（2H） - 哒嗪酮衍生物，其中R 1表示氢; 任选被R 5 R 6 N-基团取代的C 1-4烷基，其中R 5和R 6相同或不同，代表C 1-4烷基或R 5 R N-一起表示任选含有氧或R 7 N-部分的6元杂环基，其中R 7是任选被苯氧基取代的C 1-4烷基或任选被苯基; 或被一或多取代的苯基，苯氧基或苄氧基取代的C 1-4烷基; 或任选被未取代或任选取代的苯基取代的C3-5烯基或C3-5炔基; 或苯基; R 2表示氢; 或任选被吗啉代，吡啶基，1,4-苯并二恶烷基或任意取代的苯基取代的C 1-4烷基; R 3表示氢或任选取代的苯基; R 4表示氢; 或R 8 CO-基团，其中R 8是C 1-4烷基，苯基或吡啶基或被C 1-4烷基取代的氨基; 或其中M为氢或有机或无机阳离子的-SO 3 M部分; X表示卤素; n为1,2或3，条件是当n为1时，R 1不同于C 1-4烷基，烯基，芳烷基和苯基，以及它们互变异构体和这些化合物的酸加成盐。本发明还涉及含有通式（I）化合物作为活性成分的药物组合物以及制备通式（I）化合物的方法。本发明化合物具有显着的钙调素拮抗作用，降低冠状动脉阻力并且毒性较小。因此，这些化合物可用于治疗心血管疾病，特别是心绞痛。

4. 发明申请

WO1997014685A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO1997014685A1
公开(公告)日：1997-04-24
申请号：PCT/HU1996000058
申请日：1996-10-14
申请人： GYOGYSZERKUTATO INTÉZET KFT , TOLDY, Rózsa +hf , TOLDY, Márta +hm , TOLDY, András +hm , ZUBOVICS, Zoltán , SZILAGYI, Katalin , VIDA, Franciska , ANDRASI, Ferenc , SUTKA, Klára , HODULA, Eszter , SZEKERES, Tibor , FEHÉR, Gábor , MORAVCSIK, Imre , MATYUS, Péter , SEBESTYÉN, László , SZABO, Hilda , ZARA, Erzsébet , HORVATH, Edit
发明人： GYOGYSZERKUTATO INTÉZET KFT , TOLDY, Rózsa +hf , TOLDY, Márta +hm , TOLDY, András +hm , TOLDY, Lajos +di
IPC分类号： C07D239/50
CPC分类号： C07D295/13 , C07D239/50
摘要： The invention refers to novel pyrimidine derivatives of formula (I), wherein R stands for a group of formula (a), wherein Ar means an aromatic homocyclic group, R and R represent hydrogen, halogen, hydroxy, alkyl, optionally substituted alkoxy, alkylthio group and oxidized derivatives thereof, optionally substituted amino, carboxy and derivatives thereof, sulfo and/or sulfonamido; and p, q and r are 0 or 1; R and R stand for amino; or a moiety derived from a nitrogen-containing heterocycle; X means a single bond; an optionally oxidized sulfur atom; or an optionally substituted nitrogen atom; A stands for an optionally substituted alkylene group; and n is 1 or 2. The invention relates also to a process and the intermediates for the preparation of the compounds of formula (I). The compounds according to the invention possess a remarkable lipid peroxidation inhibiting effect which is detectable both under in vitro and in vivo conditions. Thus, these compounds are useful for the prevention and/or treatment e.g. of injuries of the head, brain and spinal cord; as well as tissue damages arising from ischemia (including e.g. reperfusion injuries), myocardial infarction or coronary heart disease.
摘要翻译：本发明涉及式（I）的新颖的嘧啶衍生物，其中R 1代表式（a）的基团，其中Ar表示芳族的双环基团，R 4和R 5表示氢，卤素，羟基，烷基，任选取代的烷氧基，烷硫基及其氧化衍生物，任选取代的氨基，羧基及其衍生物，磺基和/或亚磺酰氨基; 和p，q和r为0或1; R 2和R 3代表氨基; 或衍生自含氮杂环的部分; X表示单键; 任选氧化的硫原子; 或任选取代的氮原子; A代表任选取代的亚烷基; 并且n为1或2.本发明还涉及用于制备式（I）化合物的方法和中间体。根据本发明的化合物具有显着的脂质过氧化抑制作用，其在体外和体内条件下均可检测。因此，这些化合物可用于预防和/或治疗。头部，脑部和脊髓受伤; 以及由缺血（包括例如再灌注损伤），心肌梗死或冠心病引起的组织损伤。

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