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公开(公告)号：US06168913A
公开(公告)日：2001-01-02
申请号：US08949987
申请日：1997-10-14
申请人： Jill Edie Hochlowski , Thomas J. Sowin , Daniel W. Norbeck , Warren S. Wade , David N. Whittern
发明人： Jill Edie Hochlowski , Thomas J. Sowin , Daniel W. Norbeck , Warren S. Wade , David N. Whittern
IPC分类号： C12Q100
CPC分类号： C40B50/16 , B01J2219/00576 , C07K1/047 , C40B99/00
摘要： The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching “tags” that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.
摘要翻译： 本发明涉及通过以组合和/或比率附着包含含氟化合物的“标签”，在多个固体支持物上合成的组合化学文库编码。 可以通过氟核磁共振光谱法附着到固体支持物上来对标签进行解码，以跟踪单个珠粒的反应历程，并确定附着在珠粒上的文库的特定成员。
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公开(公告)号：US6150530A
公开(公告)日：2000-11-21
申请号：US207881
申请日：1998-12-08
申请人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
发明人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
IPC分类号： C07D275/02 , A61K31/395 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K38/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/04 , A61P43/00 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D20060101 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/10 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/06 , C07D261/08 , C07D263/24 , C07D263/30 , C07D263/32 , C07D263/48 , C07D265/30 , C07D277/22 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D521/00 , C07F5/02 , C07F5/04 , C07K5/06 , C07K5/065
CPC分类号： C07D413/12 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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3.发明授权
公开(公告)号：US5541328A
公开(公告)日：1996-07-30
申请号：US415385
申请日：1995-04-03
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao , David Scarpetti
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao , David Scarpetti
IPC分类号： C07C213/00 , C07C215/28 , C07C225/16 , C07C227/18 , C07C229/36 , C07C231/12 , C07C233/35 , C07C251/40 , C07C255/27 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07D221/14 , C07C251/78 , C07C209/44 , C07C221/14
CPC分类号： C07D221/14 , C07C213/00 , C07C215/28 , C07C225/16 , C07C251/40 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07B2200/07
摘要： A substantially pure compound of formula: ##STR1## wherein R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.l are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; andR.sub.g is hydrogen, loweralkyl or benzyl; or an acid addition salt thereof.
摘要翻译： （I）其中R a和R b独立地选自氢，低级烷基和苯基，R c，R d和R 10独立地选自氢，低级烷基 ，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，且R 7为R 7aa（O） - ，其中R 7a为低级烷基; 或者R 6和R 7与它们所键合的氮原子一起是其中R f，R g，R h和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基; R g为氢，低级烷基或苄基; 或其酸加成盐。
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公开(公告)号：US07320986B2
公开(公告)日：2008-01-22
申请号：US10792564
申请日：2004-03-03
申请人： Yunsong Tong , Akiyo K. Claiborne , Gaoquan Li , Nan-Horng Lin , Hing L. Sham , Thomas J. Sowin , Zhi-Fu Tao
发明人： Yunsong Tong , Akiyo K. Claiborne , Gaoquan Li , Nan-Horng Lin , Hing L. Sham , Thomas J. Sowin , Zhi-Fu Tao
IPC分类号： A61K31/4745 , A61K31/4162 , C07D487/14
CPC分类号： C07D249/08 , C07D231/12 , C07D231/54 , C07D233/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译： 具有式（I）的化合物可用于抑制蛋白激酶。 还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。
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公开(公告)号：US07163939B2
公开(公告)日：2007-01-16
申请号：US10980740
申请日：2004-11-03
申请人： Nan-Horng Lin , Gaoquan Li , Magdalena K. Przytulinska , Thomas J. Sowin , Gerard M. Sullivan , Zhi-Fu Tao , Yunsong Tong , Le Wang
发明人： Nan-Horng Lin , Gaoquan Li , Magdalena K. Przytulinska , Thomas J. Sowin , Gerard M. Sullivan , Zhi-Fu Tao , Yunsong Tong , Le Wang
IPC分类号： C07D513/08 , A61K31/529
CPC分类号： C07D487/08
摘要： Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译： 具有下式的化合物可用于抑制蛋白激酶。 还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。
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公开(公告)号：US5580984A
公开(公告)日：1996-12-03
申请号：US412253
申请日：1995-03-28
申请人： Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
发明人： Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
IPC分类号： A61K31/425 , A61K31/427 , A61K38/00 , A61K45/06 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07K5/06 , C07K5/065
CPC分类号： C07D207/08 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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公开(公告)号：US5565418A
公开(公告)日：1996-10-15
申请号：US417304
申请日：1995-04-05
申请人： Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Michael S. Allen , Arthur J. Copper , Jien-Heh J. Tien
发明人： Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Michael S. Allen , Arthur J. Copper , Jien-Heh J. Tien
IPC分类号： A61K31/425 , A61K31/427 , A61K38/00 , A61K45/06 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07K5/06 , C07K5/065
CPC分类号： C07D207/08 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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公开(公告)号：US6017928A
公开(公告)日：2000-01-25
申请号：US944351
申请日：1997-10-06
申请人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
发明人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
IPC分类号： C07D275/02 , A61K31/395 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K38/00 , A61K45/06 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/04 , A61P43/00 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D20060101 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/10 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/06 , C07D261/08 , C07D263/24 , C07D263/30 , C07D263/32 , C07D263/48 , C07D265/30 , C07D277/22 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D521/00 , C07F5/02 , C07F5/04 , C07K5/06 , C07K5/065 , A01N43/42 , A01N43/78
CPC分类号： C07D413/12 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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公开(公告)号：US5696270A
公开(公告)日：1997-12-09
申请号：US411140
申请日：1995-03-27
申请人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
发明人： Dale J. Kempf , Daniel W. Norbeck , Hing Leung Sham , Chen Zhao , Thomas J. Sowin , Daniel S. Reno , Anthony R. Haight
IPC分类号： A61K31/425 , A61K31/427 , A61K38/00 , A61K45/06 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07K5/06 , C07K5/065 , C07D277/20
CPC分类号： C07D207/08 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
摘要翻译： 公开了下式的逆转录病毒蛋白酶抑制化合物：
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10.发明授权
公开(公告)号：US5543551A
公开(公告)日：1996-08-06
申请号：US419301
申请日：1995-04-10
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-heh J. Tien , Chen Zhao , David Scarpetti
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-heh J. Tien , Chen Zhao , David Scarpetti
IPC分类号： C07C213/00 , C07C215/28 , C07C225/16 , C07C227/18 , C07C229/36 , C07C231/12 , C07C233/35 , C07C251/40 , C07C255/27 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07D221/14 , C07C261/00 , C07C233/00 , C07D209/04
CPC分类号： C07D221/14 , C07C213/00 , C07C215/28 , C07C225/16 , C07C251/40 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07B2200/07
摘要： Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.
摘要翻译： 公开了用于制备基本上纯的下式化合物的中间体和方法：其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ）其中R a和R b独立地为 选自氢，低级烷基和苯基，R c，R d和R e独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; （ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，R 7为R 7aa（O） - ，其中R 7a为低级烷基或苄基; 其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或-C（O） R“其中R”为低级烷基，烷氧基，苄氧基或苯基，其中苯环未被取代或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。
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