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公开(公告)号：US5932726A
公开(公告)日：1999-08-03
申请号：US838838
申请日：1997-04-11
申请人： Michael Ernest Pierce , Anusuya Choudhury , Rodney Lawrence Parsons, Jr. , Lilian Alicia Radesca
发明人： Michael Ernest Pierce , Anusuya Choudhury , Rodney Lawrence Parsons, Jr. , Lilian Alicia Radesca
IPC分类号： A61K31/535 , A61P31/18 , A61P43/00 , C07D265/18 , C07D265/16
CPC分类号： C07D265/18 , Y02P20/55
摘要： The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
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2.发明授权4,4-disubstituted-1,4-dihydro-2h-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same 失效可用作HIV逆转录酶抑制剂的4,4-二取代-1,4-二氢-2h-3,1-苯并恶嗪-2-酮及其制备方法公开(公告)号：US06303780B1
公开(公告)日：2001-10-16
申请号：US09627213
申请日：2000-07-27
IPC分类号： C07D26504
CPC分类号： C07D265/18
摘要： The present invention relates to benzoxazinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
摘要翻译： 本发明涉及式I的苯并恶嗪酮或其可用作HIV逆转录酶抑制剂的立体异构形式或其混合物或其药学上可接受的盐形式，以及包含其的药物组合物和诊断试剂盒，其使用方法为 治疗病毒感染或作为测定标准或试剂，以及制备其的中间体和方法。
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3.发明授权4,4-disubstituted-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same 有权可用作HIV逆转录酶抑制剂的4,4-二取代-1,4-二氢-2H-3,1-苯并恶嗪-2-酮及其制备方法
公开(公告)号：US6140499A
公开(公告)日：2000-10-31
申请号：US176491
申请日：1998-10-21
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： The present invention relates to benzoxazinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
摘要翻译： 本发明涉及式I的苯并恶嗪酮或其可用作HIV逆转录酶抑制剂的立体异构形式或其混合物或其药学上可接受的盐形式，以及包含其的药物组合物和诊断试剂盒，其使用方法为 治疗病毒感染或作为测定标准或试剂，以及制备其的中间体和方法。
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公开(公告)号：US6028237A
公开(公告)日：2000-02-22
申请号：US990471
申请日：1997-12-15
CPC分类号： C07C13/04 , C07C1/328 , C07C2101/02
摘要： The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
摘要翻译： 本发明一般涉及用于合成环己基乙炔的新方法，该环乙炔是不对称合成（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H- 苯并恶嗪-2-酮，其是有用的人类免疫缺陷病毒（HIV）逆转录酶抑制剂。
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5.发明授权Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone 失效（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-3,4-二氢-2（1H） - 喹唑啉酮公开(公告)号：US06225317B1
公开(公告)日：2001-05-01
申请号：US09442605
申请日：1999-11-18
IPC分类号： C07D23472
CPC分类号： C07D239/80 , C07D239/78
摘要： The potent reverse transcriptase inhibitor (−)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone is produced in solvate and crystalline form. These forms are designated Forms 1 and 2, and are characterized by x-ray powder diffraction and differential scanning calorimetry. Pharmaceutical compositions and methods are useful for the treatment of the human immunodeficiency virus (HIV).
摘要翻译： 以溶剂化物和结晶形式产生有效的逆转录酶抑制剂（ - ）-6-氯-4-环丙基乙炔基-4-三氟甲基-3,4-二氢-2（1H） - 喹唑啉酮。 这些形式指定为形式1和2，其特征在于X-射线粉末衍射和差示扫描量热法。 药物组合物和方法可用于治疗人类免疫缺陷病毒（HIV）。
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6.发明授权4,4-disubstitued-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same 失效可用作HIV逆转录酶抑制剂的4,4-二取代-1,4-二氢-2H-3,1-苯并恶嗪-2-酮及其制备方法
公开(公告)号：US5874430A
公开(公告)日：1999-02-23
申请号：US942031
申请日：1997-10-01
申请人： David Donald Christ , Anthony Joseph Cocuzza , Soo Sung Ko , Jay Andrew Markwalder , Abdul Ezaz Mutlib , Rodney Lawrence Parsons, Jr. , Mona Patel , Steven Paul Seitz
发明人： David Donald Christ , Anthony Joseph Cocuzza , Soo Sung Ko , Jay Andrew Markwalder , Abdul Ezaz Mutlib , Rodney Lawrence Parsons, Jr. , Mona Patel , Steven Paul Seitz
IPC分类号： C07D265/18 , A61K31/535 , A61K265/18
CPC分类号： C07D265/18
摘要： The present invention relates to benzoxazinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
摘要翻译： 本发明涉及式I的苯并恶嗪酮：其可用作HIV逆转录酶抑制剂的立体异构形式或其混合物或其药学上可接受的盐形式，以及包含其的药物组合物和诊断试剂盒，方法 使用它们来治疗病毒感染或作为测定标准或试剂，以及用于制备其的中间体和方法。
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