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1. 发明授权

US5395934A 3(2H)-pyridazinone derivatives and process for the preparation thereof 失效
标题翻译： 3（2H） - 哒嗪酮衍生物及其制备方法
公开(公告)号：US5395934A
公开(公告)日：1995-03-07
申请号：US995295
申请日：1992-12-21
申请人： Peter Matyus , Klara Czako , Ildiko Varga , Andrea Jednakovics , Agnes Papp , Ilona Bodi , Gyorgy Rabloczky , Andras Varro , Laszlo Jaszlits , Aniko Miklos , Luca Levay , Gvorgy Schmidt , Marton Fekete , Maria Kurthy , Katalin Szemeredi , Erzsebet Zara
发明人： Peter Matyus , Klara Czako , Ildiko Varga , Andrea Jednakovics , Agnes Papp , Ilona Bodi , Gyorgy Rabloczky , Andras Varro , Laszlo Jaszlits , Aniko Miklos , Luca Levay , Gvorgy Schmidt , Marton Fekete , Maria Kurthy , Katalin Szemeredi , Erzsebet Zara
IPC分类号： A61K31/50 , A61K31/501 , A61K31/535 , A61K31/5377 , A61P9/06 , C07D237/14 , C07D237/22 , C07D403/04 , C07D403/06 , C07D413/06 , C07D413/14 , C07D237/10
CPC分类号： C07D237/14
摘要： Racemic or optically active new 3(2H)-pyridazinone derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said 3(2H)-pyridazinone derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 3(2H)-pyridazinone derivatives according to the invention correspond to the general formula (I), ##STR1##
摘要翻译：外消旋或光学活性的新的3（2H） - 哒嗪酮衍生物，其制备方法，包含它们的药物组合物，使用所述3（2H） - 哒嗪酮衍生物用于治疗疾病和用于制备药物适用于治疗疾病的组合物。根据本发明的新的3（2H） - 哒嗪酮衍生物对应于通式（I），（I）

2. 发明授权

US4829076A Novel dihydropyridines having calcium antagonistic and antihypertensive activity 失效
标题翻译：具有钙拮抗作用和抗高血压活性的新型二氢吡啶类
公开(公告)号：US4829076A
公开(公告)日：1989-05-09
申请号：US97111
申请日：1987-09-16
申请人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
发明人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
IPC分类号： A61K31/445 , A61K31/451 , A61K31/455 , A61P3/00 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , C07D211/90 , C07D405/12
摘要： The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.
摘要翻译：本发明涉及通式（I）的新的取代二氢吡啶衍生物，其中R 1和R 6如本文所定义，外消旋和光学活性变体及其混合物，此外，这些化合物的酸加成盐，含有该组合物的药物组合物及其制备方法。通式（I）的化合物可以有利地用于治疗病态严重的高血压，其毒性低，并且具有有利的治疗指标。

3. 发明授权

US5441948A 1,3,4-benzotraizepin-5(4H)-one derivatives and process for the preparation thereof 失效
标题翻译： 1,3,4-benzotraizepin-5（4H） - 酮衍生物及其制备方法
公开(公告)号：US5441948A
公开(公告)日：1995-08-15
申请号：US115688
申请日：1993-09-03
申请人： Ilona Bodi , Eva Gal , Melinda Gal , Laszlo Jaszlits , Andrea Jednakovits , Adrina Kiss , Aniko Miklos nee Kovacs , Gyorgy Mathe , Istvan Pallagi , Gyorgy Rabloczky , Antal Simai , Endre Tihanyi
发明人： Ilona Bodi , Eva Gal , Melinda Gal , Laszlo Jaszlits , Andrea Jednakovits , Adrina Kiss , Aniko Miklos nee Kovacs , Gyorgy Mathe , Istvan Pallagi , Gyorgy Rabloczky , Antal Simai , Endre Tihanyi
IPC分类号： A61K31/55 , A61P9/00 , C07D255/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07F7/08 , C07D403/06
CPC分类号： C07D401/06 , C07D255/04 , C07D401/12 , C07D403/12 , C07F7/0812
摘要： The invention relates to racemic or optically active 1,3,4-benzotriazepin-5(4H)-one derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said compounds for the treatment of diseases and for the preparation of pharmaceutical compositions containing the said compounds as active agent.The new compounds according to the invention correspond to the general formula (I), ##STR1## wherein R.sup.1 represents hydrogen or straight or branched chain C.sub.1-4 alkyl optionally carrying a pyridyl or a phenyl substituent;R.sup.2 stands for cyanoimino;R.sup.3 denotes hydrogen or straight or branched chain C.sub.1-4 alkyl;R.sup.4 stands for C.sub.1-4 alkyl; andthe dotted line does not represent a valency bond; orR.sup.2 stands for a group of the formula R.sup.9 R.sup.10 N, whereinR.sup.9 and R.sup.10 are independently hydrogen or straight or branched chain C.sub.1-10 alkyl, orR.sup.9 R.sup.10 N together form a 5- to 7-membered heterocyclic group; orR.sup.9 R.sup.10 N together form a group of the formula N.dbd.C(NR.sup.12 R.sup.13)NH.sub.2, wherein R.sup.12 and R.sup.13 are independently hydrogen or straight or branched chain C.sub.1-10 alkyl, orNR.sup.12 R.sup.13 together form a 5- to 7-membered heterocyclic group;R.sup.4 stands for C.sub.1-4 alkyl; andthe dotted line represents a valency bond, consequently substituent R.sup.1 is missing;with the proviso that if R.sup.9 and R.sup.10 are the same, they are other than hydrogen.The 1,3,4-benzotriazepin-5(4H)-one derivatives of the general formula (I) affect the circulatory system and possess antianginal, antihypertensive and peripheral vasodilating effects.
摘要翻译：本发明涉及外消旋或光学活性的1,3,4-苯并三氮杂-5（4H） - 酮衍生物，其制备方法，含有该衍生物的药物组合物，涉及所述化合物用于治疗疾病和用于制备含有所述化合物作为活性剂的药物组合物。根据本发明的新化合物对应于通式（I），其中R 1表示氢或任选带有吡啶基或苯基取代基的直链或支链C 1-4烷基; R2代表氰基亚氨基; R3表示氢或直链或支链C 1-4烷基; R4代表C1-4烷基; 虚线不代表价债券; 或R 2表示式R9R 10 N的基团，其中R 9和R 10独立地为氢或直链或支链C 1-10烷基，或R 9 R 10 N一起形成5-至7-元杂环基; 或R9R10N一起形成式N = C（NR 12 R 13）NH 2的基团，其中R 12和R 13独立地为氢或直链或支链C 1-10烷基或NR 12 R 13一起形成5-至7-元杂环基; R4代表C1-4烷基; 虚线表示价键，因此取代基R1缺失; 条件是如果R9和R10相同，它们不是氢。通式（I）的1,3,4-苯并三氮杂-5（4H） - 酮衍生物影响循环系统，具有抗心绞痛，抗高血压和外周血管扩张作用。

4. 发明授权

US4748175A Pyrimido[5,4-B][1,4]oxazine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US4748175A
公开(公告)日：1988-05-31
申请号：US947700
申请日：1986-12-30
申请人： Endre Kasztreiner , Gyorgy Rabloczky , Nandor Makk , Gyorgy Cseh , Maria Kuhar nee Kurthy , Eszter Diesler , Laszlo Jaszlits , Laszlo Sebestyen , Janos Wellmann , Aniko Tegdes , Judit Sarossy nee Kincsesy , Peter Matyus , Andras Varro , Laszlo Szam , Sarolta Vegvari nee Gyurki
发明人： Endre Kasztreiner , Gyorgy Rabloczky , Nandor Makk , Gyorgy Cseh , Maria Kuhar nee Kurthy , Eszter Diesler , Laszlo Jaszlits , Laszlo Sebestyen , Janos Wellmann , Aniko Tegdes , Judit Sarossy nee Kincsesy , Peter Matyus , Andras Varro , Laszlo Szam , Sarolta Vegvari nee Gyurki
IPC分类号： A61K31/535 , A61K31/5383 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D498/04
CPC分类号： C07D498/04
摘要： The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.1-4 alkyl or benzyl group; furtherNR.sup.5 R.sup.6 may also represents a 6-membered, saturated, nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.2-4 alkoxycarbonyl or C.sub.1-4 hydroxyalkyl group;R.sup.3 and R.sup.4 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group;R.sup.9 stands for hydrogen or a C.sub.1-4 alkyl group unsubstituted or monosubstituted by an oxo, cyano, aminocarbonyl, C.sub.2-5 alkoxycarbonyl, pyridiyl, morpholinocarbonyl, or phenyl group or mono- or polysubstituted by OH group(s), with the proviso that R.sup.2 is different from chlorine, 4-morpholinyl and piperidyl group when R.sup.9 stands for hydrogen; orR.sup.2 is different from chlorine and 4-morpholinyl group when R.sup.9 stands for a methyl or benzyl group.The compounds of the formula (I) are capable to increase the myocardial contractile force (the performance of the failing heart) and the coronary blood flow, thus they can therapeutically be used for the treatment of the chronic heart failure and coronary disturbances.

5. 发明授权

US4731383A Aminoguanidine compounds, their compositions and pharmaceutical uses 失效
标题翻译：氨基胍化合物，其组成和药物用途
公开(公告)号：US4731383A
公开(公告)日：1988-03-15
申请号：US925489
申请日：1986-10-29
申请人： Istvan Erczi , Jeno Marosfalvi , Gyorgy Rabloczky , Andras Varro , Maria Kuhar nee Kurthy , Istvan Elekes , Laszlo Szatmary , Laszlo Jaszlits
发明人： Istvan Erczi , Jeno Marosfalvi , Gyorgy Rabloczky , Andras Varro , Maria Kuhar nee Kurthy , Istvan Elekes , Laszlo Szatmary , Laszlo Jaszlits
IPC分类号： C07C281/16 , A61K31/155 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P9/06 , C07C281/10 , C07D211/10 , C07D265/30 , C07D295/14 , C07D295/215 , C07C133/10
CPC分类号： C07D295/215 , C07D265/30
摘要： The invention relates to new aminoguanidine derivatives of the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent hydrogen or halogen atom, C.sub.1-4 alkyl, nitro, trifluoromethyl or C.sub.1-4 alkoxy group,R.sup.4 and R.sup.5 represent a C.sub.1-4 alkyl group, furthermore NR.sup.4 R.sup.5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups,R.sup.6 and R.sup.7 each represent a hydrogen atom, normal or branched C.sub.1-4 alkyl or C.sub.2-4 alkenyl group,and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof.The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.
摘要翻译：本发明涉及通式（I）的新氨基胍衍生物，其中R 1，R 2和R 3各自表示氢或卤素原子，C 1-4烷基，硝基，三氟甲基或C 1-4烷氧基，R 4和R 5 代表C1-4烷基，此外，NR4R5可以形成含有一个或两个氮原子或氮和氧原子的5至7元饱和杂环基，并且任选被一个或两个甲基，羟甲基或羟乙基取代，R6 和R 7各自表示氢原子，正构或支链C 1-4烷基或C 2-4链烯基，以及它们的药学上可接受的酸加成盐以及其制备方法。本发明的新化合物具有有价值的抗心律不齐活性，并且没有已知抗心律失常化合物的不期望的循环副作用。

6. 发明授权

US4826845A 3(2H)-pyridazinones and pharmaceutical compositions thereof 失效
标题翻译： 3（2H） - 哒嗪酮及其药物组合物
公开(公告)号：US4826845A
公开(公告)日：1989-05-02
申请号：US924445
申请日：1986-10-29
申请人： Endre Kasztreiner , Gyorgy Rablocsky , Nandor Makk , Laszlo Jaszlits , Peter Matyus , Gyorgy Cseh , Ildiko Pribusz nee Rapp , Klara Czako , Eszter Diesler , Istvan Elekes , Laszlo Kaufer , Maria Kuhar nee Kurthy , Judit Kincsessy , Judit Kosary , Gyongyi Nagy nee Csokas
发明人： Endre Kasztreiner , Gyorgy Rablocsky , Nandor Makk , Laszlo Jaszlits , Peter Matyus , Gyorgy Cseh , Ildiko Pribusz nee Rapp , Klara Czako , Eszter Diesler , Istvan Elekes , Laszlo Kaufer , Maria Kuhar nee Kurthy , Judit Kincsessy , Judit Kosary , Gyongyi Nagy nee Csokas
IPC分类号： C07D237/00 , A61K31/50 , A61K31/535 , A61P9/12 , C07D237/08 , C07D237/12 , C07D237/14 , C07D237/20 , C07D237/22 , C07D319/00 , C07D403/04 , C07D405/12 , C07D521/00 , C07D405/06
CPC分类号： C07D231/12 , C07D233/56 , C07D237/08 , C07D237/12 , C07D237/20 , C07D249/08 , C07D403/04 , C07D405/12
摘要： The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) ##STR1## stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR.sup.1 R.sup.2 group, whereinR.sup.1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group;R.sup.2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH.sub.2).sub.n --R.sup.3 group, whereinn is 2 or 3; andR.sup.3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; andX stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g. an oxygen, sulfur or nitrogen atom,with the proviso that R is different from an ethyl or propyl group substituted terminally by a hydroxyl group or halogen atom when X represents a hydrogen or chlorine atom.The compounds of general formula (I) selectively inhibit the adrenergic alpha.sub.1 receptors, have a calcium-antagonistic effect and exert blood pressure lowering action.
摘要翻译：本发明涉及通式（I）的新的3（2H） - 哒嗪酮衍生物，含有它们的药物组合物及其制备方法。在通式（I）中，（I）表示被末端卤素原子或羟基或NR 1 R 2基团取代的乙基或丙基，其中R 1表示氢原子或未取代或任意取代的苄基; R 2表示氢原子或未取代或任选取代的苯并[1,4]二氧杂环己烷-2-基 - 甲基或 - 乙基或（CH 2）n -R 3基团，其中n为2或3; R3代表未取代或任选取代的苯氧基或苯硫基; X代表氢或卤素原子，或未取代或任选取代的饱和或不饱和的含有氮原子和任选另外的杂原子的5或6元杂环基团。氧，硫或氮原子，条件是当X表示氢或氯原子时，R不同于被羟基或卤素原子末端取代的乙基或丙基。通式（I）的化合物选择性地抑制肾上腺素α1受体，具有钙拮抗作用并发挥降血压作用。

7. 发明授权

US6002002A Anti-ischaemic hydroxylamine derivatives and pharmaceutical compositions 失效
标题翻译：抗缺血性羟胺衍生物和药物组合物
公开(公告)号：US6002002A
公开(公告)日：1999-12-14
申请号：US914115
申请日：1998-05-13
申请人： Laszlo Urogdi , Ede Marvanyos , Mihaly Barabas , Laszlo Jaszlits , Katalin Biro , Andrea Jednakovits , Erzsebet Radvanyne , Maria Kurthy , Istvanne Udvardy Nagy
发明人： Laszlo Urogdi , Ede Marvanyos , Mihaly Barabas , Laszlo Jaszlits , Katalin Biro , Andrea Jednakovits , Erzsebet Radvanyne , Maria Kurthy , Istvanne Udvardy Nagy
IPC分类号： C07D295/08 , A61K31/17 , A61K31/27 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/08 , A61P9/10 , C07C275/64 , C07D213/75 , C07D295/088 , C07D295/092 , C07D211/08 , C07C239/04 , C07D241/04 , C07D265/30
CPC分类号： C07D213/75 , C07C275/64 , C07D295/088
摘要： The present invention provides novel hydroxylamine derivatives represented by the general formula: wherein:X is O, --NH, or a group of formula NR', wherein R and R' are independently selected from alkyl, cycloalkyl, phenylalkyl, phenyl optionally substituted with halo, haloalkyl,alkyl, alkoxy or nitro; and a N-containing heterocyclic ring;R.sup.1 is H or alkanoyl,R.sup.2 is H or hydroxy optionally acylated with alkanoyl, andR.sup.3 is a group of the formula --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected fromH, alkyl, and a group of the formula --CO--NH--R wherein R is as defined above, orwherein R.sup.4 and R.sup.5 when taken together form a 5- to 7-membered heterocyclic ring which may optionally contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl or phenylalkyl.Also provided are pharmaceutically acceptable acid addition salts of the compounds defined above, as well as pharmaceutical compositions containing the compounds or their acid addition salts as active ingredients. The compounds of the invention have been shown to have anti-ischemic effects.
摘要翻译： PCT No.PCT / HU96 / 00033 Sec。 371日期1998年5月13日 102（e）1998年5月13日PCT PCT 1996年6月14日PCT公布。出版物WO97 / 00251 日本1997年1月3日本发明提供由以下通式表示的新型羟胺衍生物：其中：X为O，-NH或式NR'基团，其中R和R'独立地选自烷基，环烷基，苯基烷基，任选被卤素，卤代烷基，烷基，烷氧基或硝基取代的苯基; 和含N的杂环; R1是H或烷酰基，R2是H或羟基，任选地被烷酰基酰化，R3是式-NR4R5的基团，其中R4和R5独立地选自H，烷基和式-CO-NH-R的基团其中R如上所定义，或者其中R 4和R 5一起形成5至7元杂环，其可以任选地含有一个选自氮，氧和硫的另外的杂原子，并且其任选被烷基或苯基烷基取代。还提供了上述化合物的药学上可接受的酸加成盐，以及含有化合物或其酸加成盐作为活性成分的药物组合物。已经显示本发明的化合物具有抗缺血作用。

8. 发明授权

US4259328A Morpholino pyridazinylhydrazones 失效
标题翻译：吗啉代哒嗪基腙
公开(公告)号：US4259328A
公开(公告)日：1981-03-31
申请号：US914778
申请日：1978-06-12
申请人： Geza Szilagyi , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Szilagyi , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/50 , A61P9/12 , C07D237/20 , C07D237/22 , C07D237/24 , C07D401/04 , C07D295/00 , A61K31/535
CPC分类号： C07D237/24 , C07D237/20 , C07D237/22
摘要： Pyridazinylhydrazones capable of lowering blood pressure having the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is morpholino; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.
摘要翻译：能够降低血压的哒嗪基腙类具有下式：其中R1是氢，氯，具有1-4个碳原子的烷基，甲氧基，羟基，氨基甲酰基或氰基; R2是吗啉代; 并且K是具有式“IMAGE”的基团，其中R 3，R 4，R 5或R 6中的一个是羧基或烷氧基羰基。

9. 发明授权

US4308386A Novel pyridazinylhydrazones and method of administering same 失效
标题翻译：新型哒嗪基腙及其施用方法
公开(公告)号：US4308386A
公开(公告)日：1981-12-29
申请号：US89859
申请日：1979-10-31
申请人： Szilagyi Geza , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Szilagyi Geza , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/50 , A61P9/12 , C07D237/20 , C07D237/22 , C07D237/24 , C07D401/04
CPC分类号： C07D237/24 , C07D237/20 , C07D237/22
摘要： Pyridazinylhydrazones capable of lowering blood pressure have the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is chloro; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.
摘要翻译：能够降低血压的哒嗪基腙具有式“IMAGE”，其中R 1是氢，氯，具有1至4个碳原子的烷基，甲氧基，羟基，氨基甲酰基或氰基; R2是氯; 并且K是具有式“IMAGE”的基团，其中R 3，R 4，R 5或R 6中的一个是羧基或烷氧基羰基。

10. 发明授权

US5919796A Hydroximic acid derivatives, pharmaceutical compositions containing them, and processes for preparing the same 失效
标题翻译：含羟基酸衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5919796A
公开(公告)日：1999-07-06
申请号：US737168
申请日：1996-11-05
申请人： Mihaly Barabas , Ede Marvanyos , Laszlo Urogdi , Laszlo Vereczkey , Laszlo Jaszlits , Katalin Biro , Andrea Jednakovits , Erzsebet Radvanyi nee Hegedus , Istvanne Udvardy-Nagy
发明人： Mihaly Barabas , Ede Marvanyos , Laszlo Urogdi , Laszlo Vereczkey , Laszlo Jaszlits , Katalin Biro , Andrea Jednakovits , Erzsebet Radvanyi nee Hegedus , Istvanne Udvardy-Nagy
IPC分类号： C07D213/53 , C07C251/48 , C07C259/02 , C07C259/18 , C07D213/78 , C07D295/088 , A61K31/44 , A61K31/445 , C07D211/34 , C07D401/12
CPC分类号： C07D295/088 , C07C259/02 , C07C259/18 , C07D213/78
摘要： Hydroximic acid derivatives possess anti-ischemic effects, and therefore, they are useful for treating ischemic states and diseases, such as myocardial ischemia (which may be induced by occlusion of coronary arteries). These derivatives include compounds of formula (I): ##STR1## wherein: X represents a halogen; Z represents an aromatic group, a pyridinyl group, a picolyl group, or a lutidyl group; and R represents an --A--N(R.sub.1)R.sub.2 group, wherein:R.sub.1 and R.sub.2 represent, independently from each other, hydrogen or an alkyl group;or R.sub.1 and R.sub.2, together with the adjacent nitrogen atom, form a 5- to 7-membered,saturated heterocyclic group optionally containing an additional nitrogen, oxygen,or sulfur atom, the heterocyclic group optionally being substituted by at least one alkyl group; andA represents a straight or branched chain alkylene group, as well as pharmaceutically acceptable acid addition salts thereof. The invention further relates to processes for preparing the above noted compounds, and pharmaceutical compositions containing these compounds or their pharmaceutically acceptable acid addition salts as an active ingredient. Additionally, the invention relates to intermediate compounds of formula II used in preparing the compounds of formula I. Formula II is as follows: ##STR2## In formula II, the variables Z and R have the same definitions provided above.
摘要翻译： PCT No.PCT / HU95 / 00014 Sec。 371日期：1996年11月5日 102（e）日期1996年11月5日PCT提交1995年5月4日PCT公布。公开号WO95 / 30649 日期1995年11月16日海洛因衍生物具有抗缺血作用，因此它们可用于治疗缺血状态和疾病，例如心肌缺血（其可能由冠状动脉闭塞引起）。这些衍生物包括式（I）的化合物：其中：X表示卤素; Z表示芳基，吡啶基，吡啶甲基或联脂基; 并且R表示-A-N（R1）R2基团，其中：R1和R2彼此独立地表示氢或烷基; 或R 1和R 2与相邻的氮原子一起形成任选地含有另外的氮，氧或硫原子的5至7元饱和杂环基，所述杂环基任选被至少一个烷基取代; A表示直链或支链亚烷基，以及其药学上可接受的酸加成盐。本发明还涉及制备上述化合物的方法和含有这些化合物或其药学上可接受的酸加成盐作为活性成分的药物组合物。此外，本发明涉及用于制备式I化合物的式II的中间体化合物。式II如下：在式II中，变量Z和R具有与上述相同的定义。

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