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1.发明授权Synthesis of substituted N-heteroaromatic compounds and methods of use thereof 失效取代的N-杂芳族化合物的合成及其使用方法
公开(公告)号：US5886186A
公开(公告)日：1999-03-23
申请号：US548009
申请日：1995-10-25
IPC分类号： C07B61/00 , C07D213/61 , C07D213/89 , C07D211/72
CPC分类号： C07D213/89 , C07D213/61 , C40B40/00
摘要： The subject invention features substituted N-heteroaromatic compounds, libraries of substituted N-heteroaromatic compounds, and methods of synthesis thereof. For example, the present invention provides methods for synthesizing substituted N-heteroaromatic compounds, and is particularly amenable to the generation of libraries of substituted N- heteroaromatic compounds by combinatorial chemistry. The methods of the invention generally feature the reaction of O-linked heteroaromatic N-oxides with nucleophiles to produce substituted N-heteroaromatic compounds.
摘要翻译： 本发明的特征在于取代的N-杂芳族化合物，取代的N-杂芳族化合物的文库及其合成方法。 例如，本发明提供了合成取代的N-杂芳族化合物的方法，特别适用于通过组合化学产生取代的N-杂芳族化合物的文库。 本发明的方法通常特征在于O-连接的杂芳族N-氧化物与亲核试剂的反应以产生取代的N-杂芳族化合物。
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2.发明授权Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic compositions including same, and their uses 失效萘啶酮和吡啶并恶嗪酮 - 吡啶酮化合物，包括它们的强心剂组合物及其用途
公开(公告)号：US5015638A
公开(公告)日：1991-05-14
申请号：US432070
申请日：1989-11-03
IPC分类号： C07D471/04 , C07D498/04
CPC分类号： C07D471/04
摘要： This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.
摘要翻译： 本发明涉及可用作治疗充血性心力衰竭的强心剂的取代吡啶并恶嗪酮和萘乙酮吡喃酮，使用所述化合物增加心脏收缩力的方法以及包含其的药物组合物。
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公开(公告)号：US5002944A
公开(公告)日：1991-03-26
申请号：US350366
申请日：1989-05-11
申请人： Alfred P. Spada , Henry F. Campbell , Donald E. Kuhla , William L. Studt , William C. Faith , Bruce F. Molino
发明人： Alfred P. Spada , Henry F. Campbell , Donald E. Kuhla , William L. Studt , William C. Faith , Bruce F. Molino
IPC分类号： C07D471/04 , C07D475/00
CPC分类号： C07D471/04 , C07D475/00
摘要： Compounds useful for increasing cardiotonic contractility in humans or other animals and pharmaceutical compositions including these compounds are disclosed. The compounds have the general structure: ##STR1## where A is ##STR2## R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, and R.sub.10 are H, lower alkyl of 1-4 carbon atoms, phenyl, substituted phenyl, phenyl lower alkyl of 1-4 carbon atoms or substituted phenyl lower alkyl of 1-4 carbon atoms; and n is 0 or 1.
摘要翻译： 公开了可用于增加人或其他动物的强心收缩性的化合物和包括这些化合物的药物组合物。 这些化合物具有以下通式：其中A为R 1，R 2，R 3，R 4，R 9和R 10为H，1-4个碳原子的低级烷基，苯基，取代的苯基，苯基低级 1-4个碳原子的烷基或1-4个碳原子的取代的苯基低级烷基; n为0或1。
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4.发明授权Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in the treatment of congestive heat failure 失效吡啶并哒嗪酮和吡啶基吡唑啉酮化合物及其在治疗充血性热衰竭中的应用
公开(公告)号：US4954494A
公开(公告)日：1990-09-04
申请号：US303879
申请日：1989-01-30
IPC分类号： C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： This invention relates to pyridyl-pyrazolinone compounds of the formula ##STR1## uses of said compounds as cardiotonic agents including methods for increasing cardia contractility and the treatment of congestive heart failure, pharmaceutical compositions including the same and methods for the preparation thereof.
摘要翻译： 本发明涉及下式的吡啶基 - 吡唑啉酮化合物：所述化合物用作强心剂，包括增加贲门收缩力和治疗充血性心力衰竭的方法，包括其的药物组合物及其制备方法。
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公开(公告)号：US4924010A
公开(公告)日：1990-05-08
申请号：US351685
申请日：1989-07-31
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Certain specific substituted 9-N-(1-azabicycolo-[2.2.2.]octan-3-yl)carboxamido-2,3,4,5-tetrahydro-1-benzoxepins and their valuable use as 5-HT.sub.3 antagonists having CNS and gastric prokinetic activity and void of any significant D.sub.2 receptor binding properties are disclosed. Methods for their preparation also are described.
摘要翻译： 某些特异性取代的9-N-（1-氮杂双环[2.2.2。]辛-3-基）甲酰胺基-2,3,4,5-四氢-1-苯并氧杂基因及其作为具有CNS的5-HT 3拮抗剂的有价值的用途 并且公开了胃动力学活性和无任何显着的D2受体结合性质。 还描述了其制备方法。
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6.发明授权3- and 5-(bicyclic ether or bicyclic alkylene thioether) alkylene amino thiatriazines 失效3-和5-（双环醚或双环亚烷基硫醚）亚烷基氨基硫杂三嗪
公开(公告)号：US4816583A
公开(公告)日：1989-03-28
申请号：US130393
申请日：1987-12-09
申请人： Donald E. Kuhla , Henry F. Campbell , William L. Studt , Stuart A. Dodson , Robert A. Galemmo, Jr. , Pamela J. Durham
发明人： Donald E. Kuhla , Henry F. Campbell , William L. Studt , Stuart A. Dodson , Robert A. Galemmo, Jr. , Pamela J. Durham
IPC分类号： C07D285/00 , C07D285/15 , C07F7/18
CPC分类号： C07D285/15 , C07F7/1896
摘要： A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including gastrointestinal anti-ulcerogenic and cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
摘要翻译： 一类具有药理活性的包括胃肠道抗溃疡发生和细胞保护活性的药物组合物的药用组合物，以及使用所述组合物治疗哺乳动物胃肠胃酸过多和溃疡性疾病的方法的3-和5-氨基硫代三嗪化合物。
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7.发明授权Benzodiazinone-hydroxypyrazolyl compounds, cardiotonic compositions including the same and their uses 失效苯并二嗪酮 - 羟基吡唑基化合物，包括它们的强心剂组合物及其用途
公开(公告)号：US4785101A
公开(公告)日：1988-11-15
申请号：US63481
申请日：1987-06-17
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： Benzodiazinone-pyridazinone and -hydroxypyrazolyl compounds possess cardiotonic activity and are included in therapeutic cardiotonic compositions useful in methods for increasing cardiac contractility and for the treatment of congestive heart failure.
摘要翻译： 苯并二氮烯酮哒嗪酮和羟基吡唑基化合物具有强心活性，并且被包括在用于增加心脏收缩力和治疗充血性心力衰竭的方法中的治疗强心剂组合物中。
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8.发明授权Bicyclic benzonoid alkylene amino thieno [3,4-D] isothiazole ethers and thioethethers, pharmaceutical compositions and use 失效双环苯并醌亚烷基氨基噻吩并[3,4-D]异噻唑醚和硫代醚，药物组合物和用途
公开(公告)号：US4748164A
公开(公告)日：1988-05-31
申请号：US104849
申请日：1987-10-05
IPC分类号： C07C43/23 , C07C45/71 , C07D209/48 , C07D249/14 , C07D275/04 , C07D275/06 , C07D285/10 , C07D295/073 , C07D295/096 , C07D295/135 , C07D303/22 , C07D401/06 , C07D405/06 , C07D513/04 , A61K31/425 , A61K31/535
CPC分类号： C07D209/48 , C07C43/23 , C07C45/71 , C07D249/14 , C07D275/04 , C07D275/06 , C07D285/10 , C07D295/073 , C07D295/096 , C07D295/135 , C07D303/22 , C07D401/06 , C07D405/06 , C07D513/04
摘要： A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcero-genic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
摘要翻译： 一类具有药理活性的双环苯并氨基亚烷基醚和硫醚化合物，包括抗分泌和抗溃疡基因活性，包含这些化合物的药物组合物，以及使用所述组合物治疗哺乳动物的胃肠胃酸过多和溃疡性疾病的方法。
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9.发明授权Benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds, cardiotonic compositions including the same, and their uses 失效苯并二吖酮酮 - 哒嗪酮和羟基 - 吡唑基化合物，包括它们的强心剂组合物及其用途
公开(公告)号：US4725686A
公开(公告)日：1988-02-16
申请号：US800986
申请日：1985-11-22
IPC分类号： A61K31/50 , A61K31/505 , A61K31/53 , A61K31/55 , C07D403/00 , C07D403/04 , C07D403/10
CPC分类号： C07D403/04
摘要： A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinonepryidazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.
摘要翻译： 一种使用一类苯并二氮茚并哒嗪酮和羟基 - 吡唑基化合物增加人或其他动物的强心收缩力的方法和包含它们的药物组合物。
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10.发明授权
公开(公告)号：US4692445A
公开(公告)日：1987-09-08
申请号：US929592
申请日：1986-11-12
IPC分类号： C07C43/23 , C07C45/71 , C07D209/48 , C07D249/14 , C07D275/04 , C07D285/10 , C07D295/073 , C07D295/096 , C07D295/135 , C07D303/22 , C07D401/06 , C07D405/06 , A61K31/425 , A61K31/535 , C07D275/06 , C07D413/12
CPC分类号： C07D209/48 , C07C43/23 , C07C45/71 , C07D249/14 , C07D275/04 , C07D285/10 , C07D295/073 , C07D295/096 , C07D295/135 , C07D303/22 , C07D401/06 , C07D405/06
摘要： A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
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