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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:JP2001354663A
公开(公告)日:2001-12-25
申请号:JP2001151585
申请日:2001-05-21
Applicant: ABBOTT LAB
Inventor: KEMPF DALE J , NORBECK DANIEL W , CODACOVI LYNN M , PLATTNER JACOB J , SHAM HING L , CHEN ZUAO , WITTENBERGER STEVEN J
IPC: A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C53/134 , C07C211/00 , C07C215/18 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/80 , C07C219/18 , C07C233/40 , C07C237/10 , C07C237/22 , C07C269/04 , C07C271/02 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/24 , C07D20060101 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/36 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D213/79 , C07D215/20 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D237/10 , C07D239/26 , C07D241/12 , C07D261/08 , C07D261/12 , C07D263/20 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/02 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/34 , C07D307/42 , C07D307/66 , C07D333/16 , C07D333/36 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K14/81
Abstract: PROBLEM TO BE SOLVED: To obtain a new compound for inhibiting a retrovirus protease, especially inhibiting a human immunodeficiency virus(HIV) protease. SOLUTION: This retrovirus inhibitory compound is represented by the formula: A-X-B, specifically a compound in which A is 5-thiazolyl group; X is carbonatomethyl group; and B is p-nitrophenyl group). A composition for inhibiting the retrovirus protease is obtained and a method for inhibiting the retrovirus protease is provided. A composition for treating the HIV infection is obtained and a method for treating the HIV infection is provided. A method and an intermediate effective for producing the retrovirus protease inhibitor are provided.
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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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6.NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME 审中-公开
Title translation: 新型乙酰胆碱酯酶(ACC)抑制剂及其在糖尿病,肥胖和代谢综合征中的应用公开(公告)号:WO2007095601A3
公开(公告)日:2007-10-04
申请号:PCT/US2007062179
申请日:2007-02-15
Applicant: ABBOTT LAB , KEYES ROBERT F , GU YU GUI , SHAM HING L
Inventor: KEYES ROBERT F , GU YU GUI , SHAM HING L
IPC: C07D277/68 , A61K31/428 , A61P3/10 , C07D417/12
CPC classification number: C07D277/68 , C07D277/82 , C07D417/12
Abstract: The present invention relates to compounds of Formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
Abstract translation: 本发明涉及抑制乙酰辅酶A羧化酶(ACC)的式(I)化合物,可用于预防或治疗人类代谢综合征,II型糖尿病,肥胖症,动脉粥样硬化和心血管疾病。
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公开(公告)号:WO03051838A2
公开(公告)日:2003-06-26
申请号:PCT/US0239641
申请日:2002-12-12
Applicant: ABBOTT LAB
Inventor: LIN NAN-HORNG , SHAM HING L , XIA PING
IPC: A61K31/404 , A61K31/437 , A61K31/4439 , A61P35/00 , A61P43/00 , C07D209/34 , C07D401/06 , C07D403/06 , C07D471/04 , C07D209/00
CPC classification number: C07D401/06 , C07D209/34 , C07D403/06 , C07D471/04
Abstract: Compounds having the formula (I) or therapeutically acceptable salts thereof, are protein kinase inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
Abstract translation: 具有式(I)的化合物或其治疗上可接受的盐是蛋白激酶抑制剂。 公开了化合物的制备,含有该化合物的组合物以及使用该化合物治疗疾病。
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公开(公告)号:WO0109103A3
公开(公告)日:2001-05-31
申请号:PCT/US0020053
申请日:2000-07-21
Applicant: ABBOTT LAB
Inventor: WANG LE , LI QUN , SHAM HING L , WOODS KEITH W
IPC: C07D233/64 , A61K31/4164 , A61P35/00 , A61P43/00 , C07D233/54
CPC classification number: C07D233/64
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein R is selected from the group consisting of hydrogen, methyl, ethyl, propyl, and isolpropyl; and one of R or R is 3,4,5-trimethoyxphenyl, and the other is phenyl substituted with one, two, or three substitutents independently selected from the group consisting of alkoxy, halo, and -NR R , wherein R and R are independently selected from the group consisting of hydrogen and alkyl, inhibit celluar proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
Abstract translation: 式(I)化合物或其药学上可接受的盐或前药,其中R 1选自氢,甲基,乙基,丙基和异丙基; 并且R 2或R 3中的一个是3,4,5-三甲氧基苯基,另一个是被一个,两个或三个取代基取代的苯基,所述取代基独立地选自烷氧基,卤素和-NR 2 R 3; 其中R 4和R 5独立地选自氢和烷基,抑制细胞增殖。 公开了制备该化合物的方法,含有该化合物的药物组合物以及使用该化合物的治疗方法。
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9.PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF C-JUN N-TERMINAL KINASES 审中-公开
Title translation: 吡啶衍生物作为C-JUN N-TERMINAL KINASES的抑制剂有用公开(公告)号:WO2006083673A3
公开(公告)日:2006-12-21
申请号:PCT/US2006002789
申请日:2006-01-24
Applicant: ABBOTT LAB , LIU GANG , SHAM HING L , SZCZEPANKIEWICZ BRUCE G , XIN ZHILI , ZHAO HONGYU , SERBY MICHAEL D , LIU BO , LIU MEI
Inventor: LIU GANG , SHAM HING L , SZCZEPANKIEWICZ BRUCE G , XIN ZHILI , ZHAO HONGYU , SERBY MICHAEL D , LIU BO , LIU MEI
IPC: C07D213/85 , A61K31/44 , A61P3/00 , A61P19/00 , A61P25/00 , C07D213/73 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12
CPC classification number: C07D417/12 , C07D213/73 , C07D213/81 , C07D213/84 , C07D213/85 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/06 , C07D417/10
Abstract: The present invention relates to compounds of formula (I), that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.
Abstract translation: 本发明涉及式(I)化合物,其为c-jun N-末端激酶1,2或3(JNK1,JNK2或JNK3)的抑制剂,含有该化合物的组合物和该化合物在 预防或治疗由JNK1,JNK2和JNK3激活调节的疾病。
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公开(公告)号:WO0181316A3
公开(公告)日:2002-05-23
申请号:PCT/US0113678
申请日:2001-04-25
Applicant: ABBOTT LAB
Inventor: WANG WEI-BO , CURTIN MICHAEL L , FAKHOURY STEPHEN A , GWALTNEY STEPHEN L II , HASVOLD LISA A , HUTCHINS CHARLES W , LI QUI , LIN NAN-HORNG , JENNINGS NELSON LISSA TAKA , O'CONNOR STEPHEN J , SHAM HING L , SULLIVAN GERALD M , WANG GARY T , WANG XILU
IPC: C07D233/22 , A61K31/381 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4245 , A61K31/426 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P17/06 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/80 , C07D213/82 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/26 , C07D233/54 , C07D249/04 , C07D249/08 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D333/16 , C07D333/24 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D409/10 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , A61K31/33 , C07D213/74 , C07D409/12
CPC classification number: C07D213/30 , C07D213/36 , C07D231/12 , C07D233/64 , C07D249/04 , C07D249/08 , C07D277/24 , C07D277/28 , C07D277/30 , C07D333/16 , C07D333/24 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/10 , C07D413/12 , C07D417/06
Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
Abstract translation: 式(I)化合物或其药学上可接受的盐抑制法呢基转移酶。 公开了制备该化合物的方法,含该化合物的药物组合物和使用该化合物的治疗方法。
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