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1.发明授权
公开(公告)号：US5625092A
公开(公告)日：1997-04-29
申请号：US419168
申请日：1995-04-10
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. J. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , David Scarpetti , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. J. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , David Scarpetti , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao
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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2.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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3.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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4.发明授权
公开(公告)号：US5491253A
公开(公告)日：1996-02-13
申请号：US281502
申请日：1994-07-27
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 , David Scarpetti , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao
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 , David Scarpetti , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao
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
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，且R 7为R 7 a OC（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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5.发明授权
公开(公告)号：US5543552A
公开(公告)日：1996-08-06
申请号：US419327
申请日：1995-04-10
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin
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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6.发明授权
公开(公告)号：US5543549A
公开(公告)日：1996-08-06
申请号：US415403
申请日：1995-04-03
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien
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 , C07C255/00 , C07C233/00 , C07C261/00 , 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 R7a 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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7.发明授权
公开(公告)号：US5565604A
公开(公告)日：1996-10-15
申请号：US414974
申请日：1995-03-31
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Linda M. Lijewski , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Linda M. Lijewski , Howard E. Morton , Daniel S. Reno , Hing L. Sham , Thomas J. Sowin
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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8.发明授权Process for the preparation of a disubstituted 2,5-diamino-3-hydroxyhexane 失效二取代的2,5-二氨基-3-羟基己烷的制备方法
公开(公告)号：US5654466A
公开(公告)日：1997-08-05
申请号：US625783
申请日：1996-02-29
申请人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Howard E. Morton , Daniel S. Reno , Hing Leung Sham , Thomas J. Sowin , Jien-Heh J. Tien
发明人： Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Howard E. Morton , Daniel S. Reno , Hing Leung Sham , Thomas J. Sowin , Jien-Heh J. Tien
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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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：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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