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公开(公告)号：JP2008115189A
公开(公告)日：2008-05-22
申请号：JP2007327351
申请日：2007-12-19
Applicant: Abbott Lab , アボット・ラボラトリーズAbbott Laboratories
Inventor： SHAM HING LEUNG , NORBECK DANIEL W , CHEN XIAOQI , BETEBENNER DAVID A , DALE J KEMP , THOMAS R HERIN , GONDEI N KUMAA , STEVEN L CONDON , ARTHUR J COOPER , DANIEL A DICKMAN , STEVEN M HANNIKKU , LAWRENCE KORATSUEKOUSUKII , PATRICIA A OLIVER , DANIEL J PRATA , PETER J STENGEL , ERIK J SUTOONAA , JII-HAA J TEIEN , JII-HOWA RIU , KETAN M PATEL
IPC: C07D207/27 , C07D253/00 , A61K31/00 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4178 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/427 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/53 , A61K31/55 , A61K38/05 , A61K45/00 , A61P31/18 , A61P43/00 , C07C231/12 , C07C235/20 , C07C273/18 , C07C275/16 , C07D20060101 , C07D207/22 , C07D207/26 , C07D207/273 , C07D207/34 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/416 , C07D211/72 , C07D211/84 , C07D223/06 , C07D233/28 , C07D233/30 , C07D233/32 , C07D233/34 , C07D233/36 , C07D233/40 , C07D233/42 , C07D233/66 , C07D239/06 , C07D239/10 , C07D239/20 , C07D239/22 , C07D241/06 , C07D241/08 , C07D241/18 , C07D243/04 , C07D253/06 , C07D263/16 , C07D263/20 , C07D263/22 , C07D263/34 , C07D265/04 , C07D267/04 , C07D277/12 , C07D277/32 , C07D277/34 , C07D279/06 , C07D281/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
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: PROBLEM TO BE SOLVED: To provide a new compound as an HIV protease inhibiting compound, and to provide a production intermediate thereof. SOLUTION: A compound represented by formula (1) is provided. Wherein, R1 and R2 are independently selected from the group consisting of an alkyl, a cycloalkyl and an arylalkyl; R3 is a lower alkyl, a hydroxyalkyl, or a cycloalkylalkyl; R4 is an aryl or a heterocycle; R5 is a 5-7 membered ring containing nitrogen atom and having a hetero atom directly bonded with the heterocycle; and L1 is a bivalent bonding group such as -O- or -S-. COPYRIGHT: (C)2008,JPO&INPIT
Abstract translation: 待解决的问题：提供新的化合物作为HIV蛋白酶抑制化合物，并提供其生产中间体。 解决方案：提供由式（1）表示的化合物。 其中R1和R2独立地选自烷基，环烷基和芳基烷基; R3是低级烷基，羟基烷基或环烷基烷基; R4是芳基或杂环; R5是含有氮原子的5-7元环，并且具有与杂环直接键合的杂原子; 并且L1是二价键合基团，例如-O-或-S-。 版权所有（C）2008，JPO＆INPIT
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公开(公告)号：JP2001058979A
公开(公告)日：2001-03-06
申请号：JP2000190510
申请日：2000-06-26
Applicant: ABBOTT LAB
Inventor： SHAM HING LEUNG , NORBECK DANIEL W , CHEN XIAOQI , BETEBENNER DAVID A , DALE J KEMP , THOMAS R HERIN , GONDEI N KUMAA , STEVEN L CONDON , ARTHUR J COOPER , DANIEL A DICKMAN , STEVEN M HANNIKKU , LAWRENCE KORATSUEKOUSUKII , PATRICIA A OLIVER , DANIEL J PRATA , PETER J STENGEL , ERIK J SUTOONAA , JII-HAA J TEIEN , JII-HOWA RIU , KETAN M PATEL
IPC: C07D253/00 , A61K31/00 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/427 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/513 , A61K31/53 , A61K31/55 , A61K38/05 , A61K45/00 , A61P31/18 , A61P43/00 , C07C231/12 , C07C235/20 , C07C273/18 , C07C275/16 , C07D20060101 , C07D207/22 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/34 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/416 , C07D211/72 , C07D211/84 , C07D223/06 , C07D233/28 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/40 , C07D233/42 , C07D233/66 , C07D239/06 , C07D239/10 , C07D239/20 , C07D239/22 , C07D241/06 , C07D241/08 , C07D241/18 , C07D243/04 , C07D253/06 , C07D263/16 , C07D263/20 , C07D263/22 , C07D263/34 , C07D265/04 , C07D267/04 , C07D277/12 , C07D277/32 , C07D277/34 , C07D279/06 , C07D281/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: PROBLEM TO BE SOLVED: To obtain a new compound having retrovirus protease inhibiting activities, and useful for treatment of disease caused by retrovirus. e.g. Acquired Immune Deficiency Syndrome(AIDS) and human acute cellular leukemia. SOLUTION: This new compound is represented by formula I [R1 and R2 are each a lower alkyl, a cycloalkyl or an arylalkyl; R3 is a lower alkyl, a hydroxyalkyl or the like; R4 is an aryl or the like; R5 is a group of formula II (n is 1-3; X is O, S or the like; Y is CH2 or the like) or the like; L1 is O, S or the like], and exemplified by (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl) amino-3-hydroxy-5-[2S-(1-tetrahydropyrimid-2-onyl)-3-methylbutanoyl]am ino-1,6- diphenylhexane. The compound of formula I is obtained by reacting a compound of formula III with a compound of formula IV in the presence of a diimide to provide a compound of formula V, deprotecting the N, and reacting the deprotected N with a carboxylic acid.
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公开(公告)号：JP2013047266A
公开(公告)日：2013-03-07
申请号：JP2012245536
申请日：2012-11-07
Applicant: Abbott Lab , アボット・ラボラトリーズAbbott Laboratories
Inventor： SHAM HING LEUNG , NORBECK DANIEL W , CHEN XIAOQI , BETEBENNER DAVID A , DALE J KEMP , THOMAS R HERIN , GONDEI N KUMAA , STEVEN L CONDON , ARTHUR J COOPER , DANIEL A DICKMAN , STEVEN M HANNIKKU , LAWRENCE KORATSUEKOUSUKII , PATRICIA A OLIVER , DANIEL J PRATA , PETER J STENGEL , ERIK J SUTOONAA , JII-HAA J TEIEN , JII-HOWA RIU , KETAN M PATEL
IPC: C07D207/26 , C07D253/00 , A61K31/00 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4178 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/427 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/53 , A61K31/55 , A61K38/05 , A61K45/00 , A61P31/18 , A61P43/00 , C07C231/12 , C07C235/20 , C07C273/18 , C07C275/16 , C07D20060101 , C07D201/08 , C07D207/22 , C07D207/27 , C07D207/273 , C07D207/34 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/416 , C07D211/72 , C07D211/84 , C07D223/06 , C07D233/28 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/40 , C07D233/42 , C07D233/66 , C07D233/70 , C07D233/84 , C07D239/06 , C07D239/10 , C07D239/20 , C07D239/22 , C07D239/36 , C07D239/47 , C07D239/54 , C07D241/06 , C07D241/08 , C07D241/18 , C07D243/04 , C07D253/06 , C07D263/16 , C07D263/20 , C07D263/22 , C07D263/34 , C07D265/04 , C07D267/04 , C07D277/12 , C07D277/32 , C07D277/34 , C07D279/06 , C07D281/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
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: PROBLEM TO BE SOLVED: To provide novel compounds and a composition and method for inhibiting retroviral proteases and in particular for inhibiting human immunodeficiency virus (HIV) protease, a composition and method for inhibiting a retroviral infection and in particular an HIV infection, processes for making the compounds and synthetic intermediates employed in the processes.SOLUTION: There are provided a compound of formula (I) as HIV protease inhibitor or its pharmaceutically acceptable salt, ester or prodrug, and intermediates thereof.
Abstract translation: 待解决的问题：为了提供新的化合物和用于抑制逆转录病毒蛋白酶，特别是用于抑制人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，用于抑制逆转录病毒感染，特别是HIV感染的组合物和方法， 用于制备在该方法中使用的化合物和合成中间体的方法。 提供式（I）化合物作为HIV蛋白酶抑制剂或其药学上可接受的盐，酯或前药及其中间体。 版权所有（C）2013，JPO＆INPIT
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公开(公告)号：JP2006206597A
公开(公告)日：2006-08-10
申请号：JP2006052376
申请日：2006-02-28
Applicant: Abbott Lab , アボット・ラボラトリーズAbbott Laboratories
Inventor： STUK TIMOTHY L , KERDESKY FRANCIS A J , LIJEWSKI LINDA M , NORBECK DANIEL W , SCARPETTI DAVID , TIEN JIEN-HEH J , ALLEN MICHAEL S , LANGRIDGE DENTON C , MELCHER LAURA , RENO DANIEL S , SHAM HING LEUNG , ZHAO CHEN , HAIGHT ANTHONY R , LEANNA M ROBERT , MORTON HOWARD E , ROBBINS TIMOTHY A , SOWIN THOMAS J
IPC: C07C215/28 , C07B61/00 , C07C213/00 , C07C225/14 , C07C225/16 , C07C227/18 , C07C229/36 , C07C231/12 , C07C233/35 , C07C251/38 , C07C251/40 , C07C255/27 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07D221/14
CPC classification number: C07D221/14 , C07B2200/07 , C07C213/00 , C07C215/28 , C07C225/16 , C07C251/40 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07C215/08
Abstract: PROBLEM TO BE SOLVED: To provide a substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors, and to provide a method for producing the compound.
SOLUTION: The substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors is represented by general formula I.
COPYRIGHT: (C)2006,JPO&NCIPIAbstract translation: 待解决的问题：提供可用于产生HIV蛋白酶抑制剂的取代的2,5-二氨基-3-羟基己烷，并提供一种生产该化合物的方法。 解决方案：用于生产HIV蛋白酶抑制剂的取代的2,5-二氨基-3-羟基己烷由通式I表示。（C）2006，JPO和NCIPI
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公开(公告)号：EP0683772A4
公开(公告)日：1995-09-27
申请号：EP94908018
申请日：1994-02-08
Applicant: ABBOTT LAB
Inventor： NORBECK DANIEL W , SHAM HING LEUNG , KEMPF DALE J , ZHAO CHEN
IPC: A61K31/42 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P35/00 , A61P43/00 , C07C281/02 , C07C281/06 , C07D213/30 , C07D213/38 , C07D213/40 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/24 , C07D277/28 , C07D307/52 , C07D309/04 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D263/34 , C07D277/587
CPC classification number: C07D213/30 , C07C281/02 , C07C281/06 , C07C2601/14 , C07D213/38 , C07D213/40 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/24 , C07D277/28 , C07D307/52 , C07D309/04 , C07D405/12 , C07D413/12 , C07D417/12
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Patent Agency Ranking
公开(公告)号：CA2585898C
公开(公告)日：2009-10-20
申请号：CA2585898
申请日：1993-12-16
Applicant: ABBOTT LAB
Inventor： ZHAO CHEN , NORBECK DANIEL W , SHAM HING LEUNG , KEMPF DALE J
IPC: A61K31/7064 , C07D275/02 , A61K31/395 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/47 , A61K31/4709 , A61K31/4725 , 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: A combination of pharmaceutical agents for the treatment of an HIV infectio n comprising (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl) - amino)carbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6- diphenyl-3- hydroxyhexane or a pharmaceutically acceptable salt thereof and another HIV protease inhibiting compound and uses of the same to inhibit an HIV infection.
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公开(公告)号：AU2007231810A1
公开(公告)日：2007-11-29
申请号：AU2007231810
申请日：2007-11-01
Applicant: ABBOTT LAB
Inventor： PLATA DANIEL J , TIEN JIEH-HEH J , COOPER ARTHUR J , KEMPF DALE J , PATEL KETAN M , CHEN XIAOQI , DICKMAN DANIEL A , STONER ERIC J , KOLACZKOWSKI LAWRENCE , CONDON STEPHEN L , BETEBENNER DAVID A , OLIVER PATRICIA A , KUMAR GONDI N , STENGEL PETER J , HANNICK STEVEN M , HERRIN THOMAS R , NORBECK DANIEL W , SHAM HING LEUNG , LIU JIH-HUA
IPC: C07D239/10 , A61K31/415 , C07D207/26 , C07D207/40 , C07D233/32 , C07D239/22 , C07D241/08 , C07D263/22
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公开(公告)号：CZ296915B6
公开(公告)日：2006-07-12
申请号：CZ2004762
申请日：1996-12-06
Applicant: ABBOTT LAB
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: C07D239/10 , C07D253/00 , A61K31/00 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/427 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/513 , A61K31/53 , A61K31/55 , A61K38/05 , A61K45/00 , A61P31/00 , A61P31/18 , A61P31/22 , A61P43/00 , C07C231/12 , C07C235/20 , C07C273/18 , C07C275/16 , C07D20060101 , C07D207/22 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/34 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/416 , C07D211/72 , C07D211/84 , C07D223/06 , C07D233/28 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/40 , C07D233/42 , C07D233/66 , C07D239/06 , C07D239/20 , C07D239/22 , C07D241/06 , C07D241/08 , C07D241/18 , C07D243/04 , C07D253/06 , C07D263/16 , C07D263/20 , C07D263/22 , C07D263/34 , C07D265/04 , C07D267/04 , C07D277/12 , C07D277/32 , C07D277/34 , C07D279/06 , C07D281/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: Slouceniny obecného vzorce III a IV, které jsou meziprodukty pro prípravu inhibitoru retrovirových proteáz.
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公开(公告)号：CA2285119C
公开(公告)日：2005-09-20
申请号：CA2285119
申请日：1996-12-06
Applicant: ABBOTT LAB
Inventor： HERRIN THOMAS R , BETEBENNER DAVID A , KEMPF DALE J , KOLACZKOWSKI LAWRENCE , OLIVER PATRICIA A , CHEN XIAOQI , PLATA DANIEL J , NORBECK DANIEL W , COOPER ARTHUR J , DICKMAN DANIEL A , SHAM HING LEUNG , STENGEL PETER J , HANNICK STEVEN M , CONDON STEPHEN L , STONER ERIC J , TIEN JIEH-HEH J , LIU JIH-HUA , KUMAR GONDI N , PATEL KETAN M
IPC: C07D253/00 , A61K31/00 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/427 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/513 , A61K31/53 , A61K31/55 , A61K38/05 , A61K45/00 , A61P31/18 , A61P43/00 , C07C231/12 , C07C235/20 , C07C273/18 , C07C275/16 , C07D20060101 , C07D207/22 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/34 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/416 , C07D211/72 , C07D211/84 , C07D223/06 , C07D233/28 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/40 , C07D233/42 , C07D233/66 , C07D239/06 , C07D239/10 , C07D239/20 , C07D239/22 , C07D241/06 , C07D241/08 , C07D241/18 , C07D243/04 , C07D253/06 , C07D263/16 , C07D263/20 , C07D263/22 , C07D263/34 , C07D265/04 , C07D267/04 , C07D277/12 , C07D277/32 , C07D277/34 , C07D279/06 , C07D281/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclose d. (see formula I)
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公开(公告)号：AT238983T
公开(公告)日：2003-05-15
申请号：AT99101692
申请日：1994-09-26
Applicant: ABBOTT LAB
Inventor： STUK TIMOTHY L , KERDESKY FRANCIS A J , LIJEWSKI-LINCH LINDA M , NORBECK DANIEL W , SCARPETTI DAVID , TIEN JIEN-HEH J , ALLEN MICHAEL S , LANGRIDGE DENTON C , MELCHER LAURA , RENO DANIEL S , SHAM HING LEUNG , ZHAO CHEN , HAIGHT ANTHONY R , LEANNA M ROBERT , MORTON HOWARD E , ROBBINS TIMOTHY A , SOWIN THOMAS J
IPC: 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
Abstract: Processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy, and halo; or R6 is as defined above and R7 is R7aOC (O)- wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen, and trifluoromethyl and R8 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.
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