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公开(公告)号：JPH1087639A
公开(公告)日：1998-04-07
申请号：JP13236996
申请日：1996-05-27
Applicant: ABBOTT LAB
Inventor： KEMPF DALE J , NORBECK DANIEL W , SHAM HING L , CHEN ZUAO , THOMAS J SOOUIN , DANIEL S RENO , HAIGHT ANTHONY R , ARTHUR J COOPER
IPC: 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
Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound used as an intermediate for synthesizing compounds inhibiting the proteases of retroviruses, especially the protease of human immunodeficiency virus causing human acquired immunodeficiency syndrome and for synthesizing medicines for treating the disease. SOLUTION: Compounds of formulas I and II (R is H, a lower alkyl), e.g. N-(((benzyl)oxy)carbonyl)-L-phenylalaninal. The compound of formula I, etc., is obtained e.g. by binding a protected O-aminoaldehyde of formula III to a compound of the formula VCl3 (tetrahydrofuran)3 and Zn to produce a diol mixture, isolating a compound of formula IV, and subsequently hydrolyzing the isolated compound of formula IV with Ba(OH)2 to produce an aminodiol of formula V.
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公开(公告)号：JP2006232845A
公开(公告)日：2006-09-07
申请号：JP2006103462
申请日：2006-04-04
Applicant: Abbott Lab , アボツト・ラボラトリーズ
Inventor： KEMPF DALE J , NORBECK DANIEL W , SHAM HING L , CHEN ZUAO , THOMAS J SOOUIN , DANIEL S RENO , HAIGHT ANTHONY R , ARTHUR J COOPER
IPC: C07D263/32 , 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 , C07D263/48 , C07D265/30 , C07D277/20 , C07D277/22 , C07D277/24 , C07D277/26 , 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 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: PROBLEM TO BE SOLVED: To provide an HIV protease inhibitor useful for treating or preventing AIDS. SOLUTION: The retroviral protease-inhibiting compound is represented by general formula (A). Preferably, in the formula, R 1 is a thiazolyl or oxazolyl which may be substituted; n is 1; R 2 is hydrogen; R 3 is a 1-4C alkyl; R 4 and R 4a are each phenyl; R 6 is hydrogen; R 7 is thiazolyl, oxazolyl or the like; and Z is O. COPYRIGHT: (C)2006,JPO&NCIPI
Abstract translation: 待解决的问题：提供可用于治疗或预防艾滋病的HIV蛋白酶抑制剂。 解决方案：逆转录病毒蛋白酶抑制化合物由通式（A）表示。 优选地，在该式中，R SB 1是可被取代的噻唑基或恶唑基; n为1; R SB 2是氢; R SB 3是一个1-4C烷基; R SB 4和R SB 4各自为苯基; R SB 6是氢; R 7是噻唑基，恶唑基等; Z为O.版权所有（C）2006，JPO＆NCIPI
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公开(公告)号：JP2010215650A
公开(公告)日：2010-09-30
申请号：JP2010126002
申请日：2010-06-01
Applicant: Abbott Lab , アボツト・ラボラトリーズ
Inventor： KEMPF DALE J , NORBECK DANIEL W , SHAM HING L , CHEN ZUAO , THOMAS J SOOUIN , DANIEL S RENO , HAIGHT ANTHONY R , ARTHUR J COOPER
IPC: A61K31/422 , C07D275/02 , A61K31/395 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K38/00 , A61K45/00 , 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 , C07D277/20 , 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 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: PROBLEM TO BE SOLVED: To provide new compounds and compositions inhibiting retroviral protease especially human immunodeficiency virus (HIV) protease, and to provide compositions treating retroviral infection especially HIV infection.
SOLUTION: There are provided combinations of a compound of formula A1 or a pharmaceutically permissible salt thereof with another kind of retroviral protease inhibitors. Such retroviral protease inhibitor is preferably a HIV protease inhibitor especially one selected from Ro31-8959, SC-52151, KNI-227 and KNI-272.
COPYRIGHT: (C)2010,JPO&INPITAbstract translation: 要解决的问题：提供抑制逆转录病毒蛋白酶，特别是人类免疫缺陷病毒（HIV）蛋白酶的新化合物和组合物，并提供治疗逆转录病毒感染，特别是HIV感染的组合物。 解决方案：提供式A1化合物或其药学上允许的盐与另一种逆转录病毒蛋白酶抑制剂的组合。 这种逆转录病毒蛋白酶抑制剂优选为HIV蛋白酶抑制剂，特别是选自Ro31-8959，SC-52151，KNI-227和KNI-272中的一种。 版权所有（C）2010，JPO＆INPIT
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公开(公告)号：JP2002322159A
公开(公告)日：2002-11-08
申请号：JP2002054592
申请日：2002-02-28
Applicant: ABBOTT LAB
Inventor： KEMPF DALE J , NORBECK DANIEL W , SHAM HING L , CHEN ZUAO , THOMAS J SOOUIN , DANIEL S RENO , HAIGHT ANTHONY R , ARTHUR J COOPER
IPC: 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
Abstract: PROBLEM TO BE SOLVED: To provide a new compound that inhibits retrovirus proteases, especially proteases of human immunodeficiency virus(HIV), a composition for treating retrovirus infection, especially for treating HIV infection, a production method of the compound, and a synthetic intermediate used in the method. SOLUTION: A compound represented by formula (A) is provided [wherein, R1 , R2 , R3 and R6 are each H or a lower alkyl group; R4 and R4a are each a phenyl, thiazolyl, oxazolyl, isoxazolyl or isothiazolyl group; X and Y are each H or OH; Z is none or O]. For example, (2S, 3S, 5S)-5-(N-(N-((N-methyl- N-((2-cyclohexyl-4-thiazolyl)methyl)amino)carbonyl)valinyl)amino-2-(N- ((5- thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl-3-hydroxyhexane is provided.
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