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1.
公开(公告)号:EP2336138A2
公开(公告)日:2011-06-22
申请号:EP10184668.1
申请日:2005-06-29
Applicant: ABBOTT LABORATORIES
Inventor: Degoey, DAvid A , Flosi, William J , Grampovnik, David J. , Klein, Larry L. , Kempf, Dale J. , Wang, Xiu C.
IPC: C07F9/09 , A61K31/661 , A61P35/00
CPC classification number: A61K45/06 , A61K31/661 , A61K2300/00
Abstract: A compound of the formula I, II or III is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions of inhibiting HIV protease activity and treating HIV infection are also disclosed.
Abstract translation: 公开了式I,II或III的化合物作为HIV蛋白酶抑制剂的前药。 还公开了抑制HIV蛋白酶活性和治疗HIV感染的方法和组合物。
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2.Intermediates for the preparation of retroviral protease inhibiting compounds 失效
Title translation: 中间体,用于逆转录病毒蛋白酶抑制化合物的制备公开(公告)号:EP0727419B1
公开(公告)日:2002-02-27
申请号:EP96106301.3
申请日:1993-12-16
Applicant: Abbott Laboratories
Inventor: Kempf, Dale J. , Norbeck, Daniel W. , Sham, Hing Leung , Zhao, Chen , Sowin, Thomas J. , Reno, Daniel S. , Haight, Anthony R. , Cooper, Arthur J.
IPC: C07D277/28 , A61K31/425 , C07D277/24 , C07D303/36 , C07D417/12
CPC classification number: C07D413/12 , A61K31/425 , A61K31/427 , A61K31/70 , A61K38/00 , A61K45/06 , C07C33/46 , 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 , 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 , 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 , A61K31/00 , A61K2300/00 , C07C49/233 , C07C49/255 , C07C49/215 , C07C49/245 , C07C49/235 , C07C49/223
Abstract: A retroviral protease inhibiting compound of formula (A) is disclosed for use in combination with other active pharmaceutical agents for treating a human infected by HIV. Intermediates and processes useful in the manufacture of compounds of formula (A) are also disclosed.
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3.Intermediates for preparating non-peptide retroviral protease inhibitors 失效
Title translation: Zvischenprodukte zur Herstellung von non-peptiden retroviralproteasehemmenden Verbindungen公开(公告)号:EP0839798A2
公开(公告)日:1998-05-06
申请号:EP97119700.9
申请日:1990-05-17
Applicant: ABBOTT LABORATORIES
Inventor: Kempf, Dale J. , Norbeck, Daniel W. , Erickson, John W. , Sham, Hing Leung , Codacovi, Lynn M. , Plattner, Jacob J.
IPC: C07C215/18 , C07C271/20 , C07C237/10 , C07D303/40 , C07D303/46
CPC classification number: C07D207/08 , A61K38/00 , C07C33/46 , 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 , 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 , C07C2601/14 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/16 , C07D217/26 , C07D231/12 , C07D233/56 , C07D233/84 , C07D239/38 , C07D249/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D295/088 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D307/42 , C07D317/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07F9/3241 , C07F9/5333 , C07K5/021 , C07K5/06043 , C07K5/06052 , C07K5/06139 , Y02P20/55 , C07C49/233 , C07C49/255 , C07C49/215 , C07C49/245 , C07C49/235 , C07C49/223
Abstract: Intermediates, for preparing non-peptide retroviral protease inhibitors, said intermediates having the formula:
or an acid addition salt thereof or an N-protected derivative thereof wherein at each occurrence the N-protecting group is independently selected from the group consisting of formyl, acetyl, pivaloyl, t-butylacetyl, t-butyloxycarbonyl, benzyloxycarbonyl, benzyl and isopropylaminocarbonyl; or said intermediates being selected from:
(2S,3R,4S,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3S,4S,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3R,4R,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3S,4S,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3R,4S,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3R,4R,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
(2S,3S,4R,5S)-2-(N-(t-butyloxy)carbonyl)amino)-5-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane;
2-(N-benzyl-N-(benzyloxycarbonyl)amino)-5-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide;
2-amino-5-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide; and
2,5-di-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide;
or an acid addition salt thereof.Abstract translation: 用于制备非肽逆转录病毒蛋白酶抑制剂的所述中间体,所述具有下式的中间体:其中在每次出现时,N-保护基团独立地选自由以下基团组成的组: 甲酰基,乙酰基,新戊酰基,叔丁基乙酰基,叔丁氧基羰基,苄氧羰基,苄基和异丙基氨基羰基; 或所述中间体选自:(2S,3R,4S,5S)-2,5-二 - (N-(Cbz-缬氨基)氨基)-3,4-二羟基-1,6-二苯基己烷; (2S,3S,4S,5S)-2,5-二 - (N-(Cbz-缬氨基)氨基)-3,4-二羟基-1,6-二苯基己烷; (2S,3R,4R,5S)-2,5-二(N-(Cbz-缬氨基)氨基)-3,4-二羟基-1,6-二苯基己烷; (2S,3S,4S,5S)-2,5-二 - (N-(缬氨酰基)氨基)-3,4-二羟基-1,6-二苯基己烷; (2S,3R,4S,5S)-2,5-二 - (N-(缬氨基)氨基)-3,4-二羟基-1,6-二苯基六氢; (2S,3R,4R,5S)-2,5-二 - (N-(缬氨酰基)氨基)-3,4-二羟基-1,6-二苯基己烷; (2S,3S,4R,5S)-2-(N-(叔丁氧基)羰基)氨基)-5-(N-(Cbz-缬氨酰基)氨基)-3,4-二羟基-1,6-二苯基己烷; 2-(N-苄基-N-(苄氧基羰基)氨基)-5-(叔丁氧基羰基氨基)-1,6-二苯基-3-己烯-3,4-氧化物; 2-氨基-5-(叔丁氧羰)-1,6-二苯基 - 3-己烯-3,4-氧化物; 和2,5-二(叔丁氧基羰基氨基)-1,6-二苯基-3-己烯-3,4-氧化物; 或其酸加成盐。
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公开(公告)号:EP1315698A1
公开(公告)日:2003-06-04
申请号:EP99917414.7
申请日:1999-04-12
Applicant: ABBOTT LABORATORIES
Inventor: Maring, Clarence J. , Gu, Yu-Gui , Chen, Hui-Ju , Chen, Yuanwei , Degoey, David A. , Flosi, William J. , Giranda, Vincent L. , Grampovnik, David J. , Kati, Warren M. , Kempf, Dale J. , Klein, Larry L. , Krueger, Allan C. , Lin, Zhen , Madigan, Darold L. , McDaniel, Keith F. , Muchmore, Steven W. , Sham, Hing L. , Stewart, Kent D. , Stoll, Vincent S. , Sun, Minghua , Wang, Gary T. , Wang, Sheldon , Xu, Yibo , Yeung, Ming C. , Zhao, Chen , Kennedy, April
IPC: C07D207/16
CPC classification number: C07D207/327 , C07D207/16 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/06 , C07D413/04 , C07D417/04 , C07D417/06 , C07F9/5722
Abstract: Disclosed are compounds of formula (I) which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.
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公开(公告)号:EP1170289A3
公开(公告)日:2002-11-13
申请号:EP01124290.6
申请日:1996-12-06
Applicant: Abbott Laboratories
Inventor: Sham, Hing Leung , Norbeck, Daniel W. , Chen, Xiaoqi , Betebenner, David A. , Kempf, Dale J. , Herrin, Thomas R. , Kumar, Gondi N. , Condon, Stephen L. , Cooper, Arthur J. , Dickman, Daniel A. , Hannick, Steven M. , Kolaczkowski, Lawrence , Oliver, Patricia A. , Plata, Daniel J. , Stengel, Peter J. , Stoner, Eric J. , Tien, Jieh-Heh J. , Liu, Jih-Hua , Patel, Ketan M.
IPC: C07D233/32 , C07D239/10 , C07D239/22 , C07D207/40 , C07D207/26 , C07D263/22 , C07D233/36 , C07D233/42 , C07D253/06 , C07D401/12 , A61K31/415 , A61P31/18
CPC classification number: C07D207/27 , C07D207/404 , C07D207/408 , C07D223/10 , C07D233/32 , C07D233/42 , C07D239/10 , C07D239/22 , C07D241/08 , C07D241/18 , C07D253/06 , C07D263/22 , C07D307/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/12
Abstract: A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
Abstract translation: 公开了包含式(II)的取代基的化合物作为HIV蛋白酶抑制剂。 还公开了制备此类化合物的中间体和制备此类中间体的方法。
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公开(公告)号:EP0402646A1
公开(公告)日:1990-12-19
申请号:EP90109319.5
申请日:1990-05-17
Applicant: ABBOTT LABORATORIES
Inventor: Kempf, Dale J. , Norbeck, Daniel W. , Erickson, John W. , Codacovi, Lynn M. , Sham, Hing Leung , Plattner, Jacob J.
IPC: C07D213/40 , C07D213/56 , C07D211/44 , C07D215/14 , C07D211/34 , C07D215/18 , C07D295/26 , C07D295/145 , C07D303/04 , C07D303/23 , C07D303/36
CPC classification number: C07D207/08 , A61K38/00 , C07C33/46 , 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 , 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 , C07C2601/14 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/16 , C07D217/26 , C07D231/12 , C07D233/56 , C07D233/84 , C07D239/38 , C07D249/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D295/088 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D307/42 , C07D317/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07F9/3241 , C07F9/5333 , C07K5/021 , C07K5/06043 , C07K5/06052 , C07K5/06139 , Y02P20/55 , C07C49/233 , C07C49/255 , C07C49/215 , C07C49/245 , C07C49/235 , C07C49/223
Abstract: A retroviral protease inhibiting compound of the formula
or a pharmaceutical acceptable salt, prodrug or ester thereof, wherein X is a linking group;
A is
(1) substituted amino,
(2) substituted carbonyl,
(3) functionalized imino,
(4) functionalized alkyl,
(5) functionalized acyl,
(6) functionalized heterocyclic or
(7) functionalized (heterocyclic)alkyl; and B is
(1) substituted carbonyl independently defined as herein,
(2) substituted amino independently defined as herein,
(3) functionalized imino independently defined as herein,
(4) functionalized alkyl independently defined as herein,
(5) functionalized acyl independently defined as herein,
(6) functionalized heterocyclic independently defined as herein or
(7) functionalized (heterocyclic)alkyl independently defined as herein.Abstract translation: 式A-X-B的逆转录病毒蛋白酶抑制化合物或其药学上可接受的盐,前药或酯,其中X是连接基团; A是(1)取代氨基,(2)取代羰基,(3)官能化亚氨基,(4)官能化烷基,(5)官能化酰基,(6)官能化杂环或(7)官能化(杂环)烷基; 并且B是本文独立定义的(1)取代的羰基,(2)独立地定义如本文的取代氨基,(3)如本文独立定义的官能化亚氨基,(4)独立地定义如本文的官能化烷基,(5)独立定义的官能化酰基 如本文所述,(6)如本文独立定义的官能化杂环或(7)如本文独立定义的官能化(杂环)烷基。 Ø
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公开(公告)号:EP0342541A2
公开(公告)日:1989-11-23
申请号:EP89108590.4
申请日:1989-05-12
Applicant: ABBOTT LABORATORIES
Inventor: Kempf, Dale J. , Plattner, Jacob J. , Norbeck, Daniel W. , Baker, William R. , Fung, Anthony K. L. , Boyd, Steven A. , Erickson, John W. , Crowley, Steven R.
IPC: C07K5/02 , C07K5/04 , A61K37/64 , C07C103/49 , C07D307/22 , C07C125/065 , C07D295/20 , C07D263/38 , C07D307/68
CPC classification number: C07D239/10 , A61K38/00 , C07C271/22 , C07C317/44 , C07C323/60 , C07C2601/06 , C07C2601/14 , C07D233/32 , C07D263/06 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D265/06 , C07D273/00 , C07D295/205 , C07D295/215 , C07D307/58 , C07D307/68 , C07D317/36 , C07D333/38 , C07D413/06 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/101 , C07K5/1016 , C07K7/02
Abstract: A retroviral protease inhibiting compound of the formula:
or a pharmaceutically acceptable salt, prodrug or ester thereof.Abstract translation: 具有下式的逆转录病毒蛋白酶抑制化合物:
或其药学上可接受的盐,前药或酯。 -
公开(公告)号:EP2336138A3
公开(公告)日:2011-11-16
申请号:EP10184668.1
申请日:2005-06-29
Applicant: ABBOTT LABORATORIES
Inventor: Degoey, DAvid A , Flosi, William J , Grampovnik, David J. , Klein, Larry L. , Kempf, Dale J. , Wang, Xiu C.
IPC: C07F9/09 , A61K31/661 , A61P35/00
CPC classification number: A61K45/06 , A61K31/661 , A61K2300/00
Abstract: A compound of the formula I, II or III is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions of inhibiting HIV protease activity and treating HIV infection are also disclosed.
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9.Intermediates for preparing retroviral protease inhibiting compounds 失效
Title translation: Zwischeprodukte用于逆转录病毒蛋白酶抑制剂的制备中公开(公告)号:EP0997459B1
公开(公告)日:2008-11-26
申请号:EP00101297.0
申请日:1991-11-04
Applicant: ABBOTT LABORATORIES
Inventor: Kempf, Dale J. , Codacovi, Lynn M. , Norbeck, Daniel W. , Plattner, Jacob J. , Sham, Hing L. , Wittenberger, Steven J. , Zhao, Chen
IPC: C07D277/24 , A61K31/425
CPC classification number: C07D213/30 , A61K38/00 , C07C53/134 , C07C215/18 , C07C215/20 , C07C215/28 , C07C233/40 , C07C237/10 , C07C237/22 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D213/26 , 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 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/10 , C07D417/12 , C07K5/06026 , C07K5/06078
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10.Intermediates for preparing retroviral protease inhibiting compounds 失效
Title translation: Zwischeprodukte zur Herstellung von retroviralen Protease-Hemmern公开(公告)号:EP0997459A1
公开(公告)日:2000-05-03
申请号:EP00101297.0
申请日:1991-11-04
Applicant: Abbott Laboratories
Inventor: Kempf, Dale J. , Codacovi, Lynn M. , Norbeck, Daniel W. , Plattner, Jacob J. , Sham, Hing L. , Wittenberger, Steven J. , Zhao, Chen
IPC: C07D277/24 , A61K31/425
CPC classification number: C07D213/30 , A61K38/00 , C07C53/134 , C07C215/18 , C07C215/20 , C07C215/28 , C07C233/40 , C07C237/10 , C07C237/22 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D213/26 , 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 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/10 , C07D417/12 , C07K5/06026 , C07K5/06078
Abstract: An intermediate of the formula:
and
an intermediate of the formula:
or an acid addition salt thereof.Abstract translation: 下式的中间体:
和式:CHEM的中间体或其酸加成盐
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