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1.发明授权3,4-(Bis-substituted)-1,2,5-oxdiazole 2-oxides, their use and pharmaceutical formulations containing them 失效3,4-双（二取代）-1,2,5-氧二唑2-氧化物，它们的用途和含有它们的药物制剂
公开(公告)号：US4356178A
公开(公告)日：1982-10-26
申请号：US332234
申请日：1981-12-18
申请人： Karl Schonafinger , Rudi Beyerle , Anton Mogilev , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Anton Mogilev , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
IPC分类号： A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/445 , A61K31/475 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D271/08 , C07D413/14
CPC分类号： A61K31/704 , A61K31/42 , A61K31/475 , A61K31/50 , A61K31/505 , A61K31/54 , A61K31/55 , C07D271/08
摘要： Pharmacologically-valuable 3,4-(bis-substituted)-1,2,5-oxdiazole 2-oxides of formula I ##STR1## [wherein R denotes --NHR.sup.1, --NR.sup.2 R.sup.3, --NHR.sup.4 OR.sup.2, --NHR.sup.5 COR.sup.6 or ##STR2## R.sup.1 denotes alkyl having from 1 to 6 C atoms or cycloalkyl having 4 to 7 ring C atoms, R.sup.2 and R.sup.3 denote alkyl having from 1 to 4 C atoms, R.sup.4 denotes an alkylene radical of the formula --C.sub.n H.sub.2n --(wherein n denotes 2, 3 or 4), R.sup.5 denotes an alkylene radical of the formula --C.sub.m H.sub.2m -- (wherein m denotes 1, 2 or 3), R.sup.6 denotes --OR.sup.2, --NHR.sup.1, --NR.sup.2 R.sup.3 or --NH.sub.2, X denotes --(CH.sub.2).sub.p --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 -- or ##STR3## and p is 4, 5 of 6] and their pharmacologically-acceptable acid-addition compounds are prepared by elimination of hydrogen chloride from a hydroxamoyl chloride of the formulaR--CO--C(Cl).dbd.NOH (II)and dimerization. If desired, the resulting reaction product is subsequently converted into an acid-addition compound. The compounds and pharmaceutical preparations thereof are useful for treating and for prophylaxis of cardiovascular diseases.
摘要翻译： （I）[其中R表示-NHR1，-NR2R3，-NHR4OR2，-NHR5COR6或
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2.发明授权3-[N-(Lower alkyl)-N-(tetrahydro-3-thienyl 5,5-dioxide)]sydnonimines 失效3- [N-（低级烷基）-N-（四氢-3-噻吩基-5,5-二氧化物）]脱水亚胺
公开(公告)号：US4436743A
公开(公告)日：1984-03-13
申请号：US350366
申请日：1982-02-19
申请人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
IPC分类号： C07D409/12 , A61K31/41 , A61K31/4245 , A61K31/495 , A61K31/496 , A61P9/00 , A61P9/12 , C07D271/04 , C07D413/12
CPC分类号： C07D271/04
摘要： Pharmacologically-active 3-aminosydnonimines (which are optionally substituted in the N.sup.6 -position) and their physiologically-acceptable acid-addition salts are compounded into standard dosage-form medicament compositions and are useful for prophylaxis for and treatment of cardiovascular-system disorders, such as high blood pressure and angina pectoris. The 3-aminosydnonimines are 3-[4-(lower alkoxy)carbonylpiperazin-1-yl]sydnonimines and 3-[N-(lower alkyl)-N-(tetrahydro-3-thienyl S,S-dioxide)]-sydnonimines.
摘要翻译： 将药理学活性的3-氨基二氢亚胺（其在N6位任选被取代）及其生理上可接受的酸加成盐复合到标准剂型药物组合物中，并且可用于预防和治疗心血管系统疾病，例如 作为高血压和心绞痛。 3-氨基二膦酰亚胺是3- [4-（低级烷氧基）羰基哌嗪-1-基]次氨基亚胺和3- [N-（低级烷基）-N-（四氢-3-噻吩基S，S-二氧化物）] - 二氢亚胺。
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3.发明授权3-(4-Alkoxycarbonylpiperazin-1-yl)-sydnonimines, a process for their preparation and use 失效3-（4-烷氧基羰基哌嗪-1-基） - 二氢亚胺，其制备和使用方法
公开(公告)号：US4551454A
公开(公告)日：1985-11-05
申请号：US477146
申请日：1983-05-06
申请人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
IPC分类号： C07D409/12 , A61K31/41 , A61K31/4245 , A61K31/495 , A61K31/496 , A61P9/00 , A61P9/12 , C07D271/04 , C07D413/12 , C07D413/04
CPC分类号： C07D271/04
摘要： Pharmacologically-active 3-aminosydnonimines (which are optionally substituted in the N.sup.6 -position) and their physiologically-acceptable acid-addition salts are compounded into standard dosage-form medicament compositions and are useful for prophylaxis for and treatment of cardiovascular-system disorders, such as high blood pressure and angina pectoris. The 3-aminosydnonimines are 3-[4-(lower alkoxy)carbonylpiperazin-1-yl]sydnonimines and 3-[N-(lower alkyl)-N-(tetrahydro-3-thienyl S,S-dioxide)]-sydnonimines.
摘要翻译： 将药理学活性的3-氨基二氢亚胺（其在N6位任选被取代）及其生理上可接受的酸加成盐复合到标准剂型药物组合物中，并且可用于预防和治疗心血管系统疾病，例如 作为高血压和心绞痛。 3-氨基二膦酰亚胺是3- [4-（低级烷氧基）羰基哌嗪-1-基]次氨基亚胺和3- [N-（低级烷基）-N-（四氢-3-噻吩基S，S-二氧化物）] - 二氢亚胺。
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4.发明授权Substituted 1,2,5-oxadiazole-2-oxides in human cardiovascular system disease 失效人心血管系统疾病中取代的1,2,5-恶二唑-2-氧化物
公开(公告)号：US4416893A
公开(公告)日：1983-11-22
申请号：US246954
申请日：1981-03-24
申请人： Karl Schonafinger , Rudi Beyerle , Anton Mogilev , Helmut Bohn , Piero Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Anton Mogilev , Helmut Bohn , Piero Martorana , Rolf-Eberhard Nitz
IPC分类号： A61K31/41 , A61K31/4245 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D271/08 , A61K31/42
CPC分类号： A61K31/41 , C07D271/08
摘要： Pharmaceutical compositions comprising as pharmacologically active component a 1,2,5-oxadiazole-2-oxide of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 have the following meaning:______________________________________ R.sup.1 R.sup.2 ______________________________________ 1. CO--NH.sub.2 CH.sub.3 2. COOC.sub.2 H.sub.5 CH.sub.3 3. CO--NHNH.sub.2 CH.sub.3 4. COOH CH.sub.3 5. --NH--COOC.sub.2 H.sub.5 CH.sub.3 6. --NH--COOC.sub.3 H.sub.7 (n) CH.sub.3 7. --NH--COOC.sub.3 H.sub.7 (i) CH.sub.3 8. --NH--COOC.sub.4 H.sub.9 (n) CH.sub.3 9. --NH--COOCH.sub.2 --phenyl CH.sub.3 10. CO--NH.sub.2 CO--NH.sub.2 11. CN CN 12. COOH COOCH.sub.3 13. COOCH.sub.3 COOCH.sub.3 14. COOC.sub.2 H.sub.5 COOC.sub.2 H.sub.5 15. CH.sub.3 CO--NH.sub.2 16. CH.sub.3 COOC.sub.2 H.sub.5 17. CH.sub.3 CO--NHNH.sub.2 18. CH.sub.3 COOH 19. CN CO--NH.sub.2 20. CO--NH--phenyl CO--NH--phenyl 21. CH.sub.3 NH--COOC.sub.2 H.sub.5 22. CH.sub.3 NH--COOC.sub.3 H.sub.7 (n) 23. CH.sub.3 NH--COOC.sub.3 H.sub.7 (i) 24. CH.sub.3 NH--COOC.sub.4 H.sub.9 (n) 25. CH.sub.3 NH--COOCH.sub.2 --phenyl 26. CO--NH--phenyl CH.sub.3 or CH.sub.3 CO--NH--phenyl ______________________________________ They are useful for treating or preventing cardiovascular system disease in man.
摘要翻译： 包含作为药理学活性成分的通式I（I）的1,2,5-恶二唑-2-氧化物的药物组合物，其中R1和R2具有以下含义：-R1R2-1。 CO-NH2 CH3-2。 COOC2H5 CH3 -3。 CO-NHNH2 CH3-4。 COOH CH3 -5。 -NH-COOC 2 H 5 CH 3 -6。 -NH-COOC 3 H 7（n）CH 3 -7。 -NH-COOC 3 H 7（i）CH 3 -8。 -NH-COOC 4 H 9（n）CH 3 -9。 -NH-COOCH 2 - 苯基CH 3 -10。 CO-NH2 CO-NH2 -11。 CN CN -12。 COOH COOCH3 -13。 COOCH3 COOCH3 -14。 COOC2H5 COOC2H5 -15。 CH3 CO-NH2 -16。 CH3 COOC2H5 -17。 CH3 CO-NHNH2 -18。 CH3 COOH -19。 CN CO-NH2 -20。 CO-NH-苯基CO-NH-苯基-21。 CH3 NH-COOC2H5-22。 CH3 NH-COOC3H7（n）-23。 CH3 NH-COOC3H7（i）-24。 CH3 NH-COOC4H9（n）-25。 CH3 NH-COOCH2-苯基-26。 CO-NH-苯基CH 3或-CH 3 CO-NH-苯基 - 它们可用于治疗或预防人类心血管系统疾病。
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5.发明授权Substituted 3-amino-sydnonimines, their use and pharmaceutical products containing them 失效取代的3-氨基 - 脱水亚胺，其使用和含有它们的药物
公开(公告)号：US4845091A
公开(公告)日：1989-07-04
申请号：US885081
申请日：1986-07-14
申请人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero Martorana , Rolf-Eberhard Nitz
IPC分类号： A61K31/41 , A61K31/4245 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/54 , A61P9/08 , A61P9/10 , A61P9/12 , C07D271/04 , C07D317/00 , C07D413/12 , C07D493/04
CPC分类号： C07D413/12 , C07D271/04 , C07D493/04
摘要： Optically active substituted 3-aminosydnonimines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, the radical R.sup.3 (R.sup.4)N-,R.sup.2 denotes the radical 1-methoxyethyl (--CH(CH.sub.3)OCH.sub.3), acetoxy-phenyl-methyl (--CH(C.sub.6 H.sub.5)O--COCH.sub.3), 1-(ethoxycarbonyl)-ethoxy (--O--CH.sub.3)CO.sub.2 C.sub.2 H.sub.5),R.sup.3 denotes alkyl(C.sub.1 -C.sub.4) andR.sup.4 denotes for example alkyl(C.sub.1 -C.sub.4),possess valuable pharmaceutical properties.
摘要翻译： 通式Ⅰ的光学活性的取代的3-氨基二氨基亚胺及其药学上可接受的酸加成盐，其中R1表示例如基团R3（R4）N-，R2表示基团1-甲氧基乙基（-CH（ CH 3）OCH 3），乙酰氧基 - 苯基 - 甲基（-CH（C 6 H 5）O-COCH 3），1-（乙氧基羰基） - 乙氧基（-O-CH 3）CO 2 C 2 H 5），R 3表示烷基（C 1 -C 4） 烷基（C1-C4）具有有价值的药物性质。
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公开(公告)号：US4305939A
公开(公告)日：1981-12-15
申请号：US166951
申请日：1980-07-08
IPC分类号： C07D413/04 , A61K31/4245 , A61K31/425 , A61K31/495 , A61K31/496 , A61K31/54 , A61P9/00 , A61P9/12 , C07D271/04 , C07D295/28 , C07D413/06 , C07D417/04 , A61K31/38 , A61K31/41 , C07D279/10
CPC分类号： C07D295/30 , C07D271/04
摘要： Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than --H, acylating that product.
摘要翻译： 当配制成药物剂型时，式（I）的生理学上可接受的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐可用于降低全身血压，肺动脉压和左心室舒张末期压 口服给予需要减压的患者。 这些化合物通过将其游离碱状态为具有式（II）的化合物环化成相应的产物，其在其游离碱状态下具有式（Ia） 并且当R2不是-H时，酰化该产物。
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公开(公告)号：US4452797A
公开(公告)日：1984-06-05
申请号：US233055
申请日：1981-02-10
IPC分类号： C07D413/04 , A61K31/4245 , A61K31/425 , A61K31/495 , A61K31/496 , A61K31/54 , A61P9/00 , A61P9/12 , C07D271/04 , C07D295/28 , C07D413/06 , C07D417/04 , C07D403/04 , A61K31/38 , A61K31/41
CPC分类号： C07D295/30 , C07D271/04
摘要： Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than -H, acylating that product.
摘要翻译： 当配制成药物剂型时，式（I）的生理学上可接受的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐可用于降低全身血压，肺动脉压和左心室舒张末期压 口服给予需要减压的患者。 这些化合物通过将其游离碱状态为具有式（II）的化合物环化成相应的产物，其在其游离碱状态下具有式（Ia） 并且当R2不是-H时，酰化该产物。
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公开(公告)号：US4332801A
公开(公告)日：1982-06-01
申请号：US233054
申请日：1981-02-10
IPC分类号： C07D413/04 , A61K31/4245 , A61K31/425 , A61K31/495 , A61K31/496 , A61K31/54 , A61P9/00 , A61P9/12 , C07D271/04 , C07D295/28 , C07D413/06 , C07D417/04 , A61K31/38 , A61K31/41 , C07D417/14
CPC分类号： C07D295/30 , C07D271/04
摘要： Physiologically-acceptable 3-aminosyndnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than --H, acylating that product.
摘要翻译： 当配制成药物剂型时，式（I）的生理学上可接受的3-氨基异恶唑酮及其药理学上可接受的酸加成盐可用于降低全身血压，肺动脉压和左心室舒张末期压 口服给予需要减压的患者。 这些化合物通过将其游离碱状态为具有式（II）的化合物环化成相应的产物，其在其游离碱状态下具有式（Ia） 并且当R2不是-H时，酰化该产物。
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9.发明授权Substituted 3-aminosydnonimines, processes for their preparation and their use 失效取代的3-氨基亚氨基亚胺，其制备方法及其用途
公开(公告)号：US5006540A
公开(公告)日：1991-04-09
申请号：US422502
申请日：1989-10-17
申请人： Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
发明人： Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
IPC分类号： A61K31/41 , A61K31/4245 , A61P7/02 , A61P9/00 , C07D271/04 , C07D413/12
CPC分类号： C07D271/04
摘要： Substituted 3-aminosydnonimines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, alkyl having 1 to 8 C atoms, R.sup.2 denotes hydrogen or the radical --COR.sup.3 and R.sup.3 denotes, for example, an aliphatic radical having 1 to 4 C atoms, are prepared, for example, by cyclization of a compound of the formula II ##STR2## and if appropriate subsequent acylation and have useful pharmacological properties.
摘要翻译： 式I（I）的取代的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐，其中R 1表示例如具有1至8个C原子的烷基，R 2表示氢或基团-COR 3，R 3表示用于 例如，具有1至4个C原子的脂族基团，例如通过使式II化合物（II）环化，并且如果合适，则随后进行酰化并具有有用的药理学性质。
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公开(公告)号：US5179206A
公开(公告)日：1993-01-12
申请号：US534832
申请日：1990-06-07
申请人： Eckard Kujath , Christian Baumgartner , Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
发明人： Eckard Kujath , Christian Baumgartner , Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
IPC分类号： A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , C07D271/04 , C07D413/04
CPC分类号： C07D271/04
摘要： Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sup.1 denotes e.g. hydrogen;R.sup.2 denotes e.g. an alkyl radical;at least two of the radicals R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote alkyl radicals and the others denote hydrogen, are prepared by cyclization of a compound of the formula II ##STR2## and, if appropriate, subsequent acylation, and have useful pharmacological properties.
摘要翻译： 取代的式I（I）的3-氨基茚三酮及其药理学上可接受的酸加成盐，其中R1表示例如。 氢; R2表示例如 烷基; 基团R3，R4，R5和R6中的至少两个表示烷基，而其它表示氢，是通过使式II化合物（II）环化并且如果合适的话进行后续酰化制备的，并且具有有用的 药理性质。
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