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1.发明授权Alkyloxyamino substituted fluorenones and their use as protein kinase-C inhibitors 失效烷氧基氨基取代的芴酮及其作为蛋白激酶C抑制剂的用途
公开(公告)号：US6004959A
公开(公告)日：1999-12-21
申请号：US844209
申请日：1997-04-18
IPC分类号： C07C217/24 , C07C225/22 , C07D295/092 , A61K31/40 , A61K31/535 , C07D295/116
CPC分类号： C07D295/088 , C07C217/24 , C07C225/22 , C07C2103/18
摘要： The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).
摘要翻译： 本发明描述了抑制蛋白激酶C的某些烷氧基氨基取代的芴酮，以及包括这些化合物的药物组合物以及使用这些化合物控制哺乳动物（包括人）中的蛋白激酶C活性的方法。 更具体地，本发明化合物可用于治疗肿瘤性疾病状态，与异常血流（包括高血压，缺血，动脉粥样硬化，凝血障碍）和炎性疾病（包括免疫疾病，哮喘，肺纤维化和牛皮癣）相关的疾病， 。
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公开(公告)号：US5182293A
公开(公告)日：1993-01-26
申请号：US590524
申请日：1990-10-03
申请人： Sai P. Sunkara , Winton D. Jones
发明人： Sai P. Sunkara , Winton D. Jones
IPC分类号： A61K31/44 , A61K31/475 , A61K38/14
CPC分类号： A61K31/70 , A61K31/44 , A61K31/475 , A61K38/14 , Y10S514/922
摘要： This invention relates to pyridinyloxazole-2-ones which are useful in the treatment of multi-drug resistant tumors. The pyridinyloxazole-2-ones act to prevent drug resistance and thus allow conventional chemotherapeutic agents to kill tumor cells as if drug resistance were not present.
摘要翻译： 本发明涉及可用于治疗多重耐药性肿瘤的吡啶基恶唑-2-酮。 吡啶基恶唑-2-酮用于预防耐药性，从而允许常规化学治疗剂杀死肿瘤细胞，就好像耐药性不存在一样。
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公开(公告)号：US4999431A
公开(公告)日：1991-03-12
申请号：US483831
申请日：1990-02-23
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： This invention relates to novel quinolyloxazole-2-ones which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.
摘要翻译： 本发明涉及可用作治疗高血压和哮喘的蛋白激酶C抑制剂的新型喹喔啉-2-酮。 本发明还包括一种制备涉及溴 - 喹啉化合物与丁基锂反应的中间体酮化合物的新方法，并进一步使锂化化合物与N-甲基-N-甲氧基烷酰胺反应。
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公开(公告)号：US4886811A
公开(公告)日：1989-12-12
申请号：US261435
申请日：1988-10-24
IPC分类号： A61K31/47 , A61P9/08 , A61P9/12 , A61P11/08 , A61P43/00 , C07D215/14 , C07D413/04
CPC分类号： C07D413/04
摘要： This invention relates to novel quinolyloxazole-2-ones which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.
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公开(公告)号：US4803210A
公开(公告)日：1989-02-07
申请号：US183537
申请日：1988-04-14
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D498/04
摘要： Tricyclic oxazolones enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.
摘要翻译： 三环恶唑酮增强心肌收缩力，可用作心力衰竭治疗心力衰竭。
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公开(公告)号：US4568751A
公开(公告)日：1986-02-04
申请号：US490081
申请日：1983-04-29
IPC分类号： C07D213/64 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/455 , A61P9/04 , A61P9/06 , C07C67/00 , C07C213/00 , C07C225/14 , C07C225/16 , C07D213/60 , C07D213/85 , C07D213/73 , C07D401/06 , C07D405/06 , C07D409/06
CPC分类号： C07D213/85
摘要： Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
摘要翻译： 新型5-酰基-2-（1H）吡啶酮及其作为强心剂的用途。 典型的化合物是通过将阴离子氰基乙酰胺与3 - [（二甲基氨基）亚甲基] -2,4-戊二酮缩合而制备的5-乙酰基-1,2-二氢-6-甲基-2-氧代-3-吡啶腈 惰性有机溶剂。
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公开(公告)号：US5428045A
公开(公告)日：1995-06-27
申请号：US111814
申请日：1993-08-25
IPC分类号： C07D213/85 , A61K31/44 , C07D213/55 , C07D213/56 , C07D213/57
CPC分类号： C07D213/85
摘要： Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
摘要翻译： 新型5-酰基-2-（1H）吡啶酮及其作为强心剂的用途。 典型的化合物是通过将阴离子氰基乙酰胺与3 - [（二甲基氨基）亚甲基] -2,4-戊二酮缩合而制备的5-乙酰基-1,2-二氢-6-甲基-2-氧代-3-吡啶腈 惰性有机溶剂。
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公开(公告)号：US5212315A
公开(公告)日：1993-05-18
申请号：US703936
申请日：1991-07-29
IPC分类号： C07D213/42 , C07D213/64 , C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85
CPC分类号： C07D213/42 , C07D213/64 , C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85
摘要： This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.
摘要翻译： 本发明涉及5-酰基-2（1H） - 吡啶酮的烷氧基亚氨基醚衍生物及其用作治疗心力衰竭的强心剂，以及其制备方法。
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9.发明授权
公开(公告)号：US5118696A
公开(公告)日：1992-06-02
申请号：US612157
申请日：1990-11-09
IPC分类号： C07D213/85
CPC分类号： C07D213/85
摘要： Novel 5-acyl-2-(1H)pyrdinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
摘要翻译： 新型5-酰基-2-（1H）哒嗪酮及其作为强心剂的用途。 典型的化合物是通过将阴离子氰基乙酰胺与3 - [（二甲基氨基）亚甲基] -2,4-戊二酮缩合而制备的5-乙酰基-1,2-二氢-6-甲基-2-氧代-3-吡啶腈 惰性有机溶剂。
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10.发明授权Prevention of glycoprotein enveloped virus infectivity by pyridinyloxazole-2-ones 失效通过吡啶基恶唑-2-酮预防糖蛋白包膜病毒感染
公开(公告)号：US5063238A
公开(公告)日：1991-11-05
申请号：US590522
申请日：1990-10-03
申请人： Sai P. Sunkara , Winton D. Jones
发明人： Sai P. Sunkara , Winton D. Jones
IPC分类号： A61K31/44
CPC分类号： A61K31/44
摘要： This invention relates to pyridinyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.
摘要翻译： 本发明涉及作为蛋白激酶C抑制剂的能力的有用的抗包膜病毒剂的吡啶基恶唑-2-酮。 这些衍生物被公开以有效地治疗包括HIV感染的包膜病毒感染，因此可用于治疗AIDS和ARC。
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