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公开(公告)号:CY1116278T1
公开(公告)日:2017-02-08
申请号:CY151100245
申请日:2015-03-12
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , JONES ANDREW D , NYCE PHILIP L , TRUDEAU MARTIN , GUERIN DAVID J , SNOONIAN JOHN R
IPC: C07D405/12
Abstract: Ηεφεύρεσηαφοράσεμίαμέθοδοπαρασκευήςμίαςένωσηςπουπεριλαμβάνεικαθαρισμόμίγματος, όπου R8 είναιπροστατευτικήομάδακαιο καθαρισμόςπεριλαμβάνειχρωματογραφία, επιλεκτικώςκρυστάλλωσηή δυναμικώςκρυστάλλωσητουμίγματος.
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公开(公告)号:CY1114916T1
公开(公告)日:2016-12-14
申请号:CY141100149
申请日:2014-02-25
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , COCHRAN JOHN E
IPC: C07D209/52 , A61K31/403 , C07D471/08
Abstract: Ηεφεύρεσηαφοράσεενώσειςκαιμεθόδουςχρήσιμεςγιατηνπαρασκευήαναστολέωνπρωτεάσης, ιδιαιτέρωςαναστολέωνπρωτεάσηςσερίνης. Οιαναστολείςπρωτεάσηςείναιχρήσιμοιγιατηνθεραπείαμολύνσεων HCV.
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43.
公开(公告)号:ES2532967T3
公开(公告)日:2015-04-06
申请号:ES11178126
申请日:2005-03-11
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , JONES ANDREW D , NYCE PHILIP L , TRUDEAU MARTIN , GUERIN DAVID J , SNOONIAN JOHN R
IPC: C07D405/12 , C07B43/04 , C07B57/00
Abstract: Un proceso de preparación de un compuesto de beta-amidocarbonilo de fórmula XXX:**Fórmula** que comprende las etapas de: a) hacer reaccionar un compuesto de fórmula XII:**Fórmula** con un compuesto de fórmula XIII:**Fórmula** en presencia de un catalizador de paladio, un ligando de paladio, una base y un disolvente que incluye opcionalmente un catalizador de transferencia de fase y que incluye opcionalmente agua, para producir un compuesto de fórmula XXXI:**Fórmula** en la que: X es un grupo saliente; cada Ra es H, un alquilo opcionalmente sustituido, un arilo opcionalmente sustituido, -CN, -C(O)-Oalquilo o halógeno; cada R2 es independientemente un grupo alifático opcionalmente sustituido, un grupo heterocíclico opcionalmente sustituido o un grupo arilo opcionalmente sustituido; cada R4 es independientemente un alifático opcionalmente sustituido, un heterociclo opcionalmente sustituido, un arilo opcionalmente sustituido, o R2 y R4, junto con los grupos a los que están unidos, forman un anillo heterocíclico de 5 a 8 miembros opcionalmente sustituido; y cada R3 es un resto orgánico.
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44.
公开(公告)号:PT2399916E
公开(公告)日:2015-03-17
申请号:PT11178128
申请日:2005-03-11
Applicant: VERTEX PHARMA
Inventor: NYCE PHILIP L , CHEN MINZHANG , TANOURY GERALD J , JONES ANDREW D , TRUDEAU MARTIN , GUERIN DAVID J , SNOONIAN JOHN R
IPC: C07D405/12 , C07B43/04 , C07B57/00
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公开(公告)号:AU2014224107A1
公开(公告)日:2014-10-02
申请号:AU2014224107
申请日:2014-09-12
Applicant: VERTEX PHARMA
Inventor: JONES ANDREW D , GUERIN DAVID J , TANOURY GERALD J , NYCE PHILIP L , TRUDEAU MARTIN , CHEN MINZHANG , SNOONIAN JOHN R
IPC: C07B43/04 , C07B57/00 , C07D405/12
Abstract: PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF ASPARTIC ACETAL CASPASE INHIBITORS Abstract The invention relates to processes such as that shown in the scheme and compounds 5 useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
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公开(公告)号:PL2194043T3
公开(公告)日:2014-07-31
申请号:PL10155058
申请日:2006-08-18
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , COCHRAN JOHN E
IPC: C07D209/52 , A61K31/403 , C07D471/08
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公开(公告)号:SG2014013338A
公开(公告)日:2014-06-27
申请号:SG2014013338
申请日:2006-08-18
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , COCHRAN JOHN E
Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
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公开(公告)号:PL1934179T4
公开(公告)日:2014-03-31
申请号:PL06813568
申请日:2006-08-18
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , COCHRAN JOHN E
IPC: C07D209/52
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公开(公告)号:NZ595817A
公开(公告)日:2014-03-28
申请号:NZ59581710
申请日:2010-04-27
Applicant: VERTEX PHARMA
Inventor: LOOKER ADAM , CHEN MINZHANG , JURKAUSKAS VALDAS , TANOURY GERALD J , COCHRAN JOHN E
IPC: C07D209/52 , A61K31/403 , C07D471/08 , C07K7/02
Abstract: 595817 Disclosed herein are processes for preparing a mixture of cis- and trans-octctahydropenta[c]pyrrole-1-carboxylic acids of formula 7, wherein R’ substituents are described in the specification, comprising carboxylation of an azabicyclooctane of formula 6, and equilibrating in the presence of a suitable base wherein the trans-/cis-ratio is greater than 80 to 20, or 90 to 10 or 98 to 2. Also disclosed herein are processes for preparing a compound of formula 4, comprising providing a compound of Formula 7 forming a salt with an optically active amine; crystallizing the salt; esterifying the acid provided in step iii); removing the N-alkoxycarbonyl group to produce (1S,3aR,6aS)-t-butyl-octahydrocyclopenta[c]pyrrole-1-carboxylate, t-butyl ester; reacting the bicyclic aminoester of step v) with a protected amino acid of Formula 26, wherein Z is an amine protecting group, in the presence of a coupling reagent, to produce an amide-ester of Formula 27; removing the protecting group Z from the amide-ester of step vi) to produce the amino compound of Formula 28; reacting the amino compound of Formula 28 with a protected amino acid of Formula 29in the presence of a coupling reagent to produce a tripeptide of Formula 30; removing the protecting group Z in the tripeptide of Formula 30 to produce a free amino-tripeptide of Formula 31; reacting the amino-tripeptide of Formula 31 with pyrazine-2-carboxylic acid in the presence of a coupling reagent to produce an amide-tripeptide ester of Formula 33; hydrolyzing the ester of the amide-tripeptide ester of Formula 33 to produce an amide-tripeptide acid of Formula 34; reacting the amide-tripeptide acid of Formula 34 with an aminohydroxy-amide of Formula 18in the presence of a coupling reagent to produce a hydroxy-tetrapeptide of Formula 35; and oxidizing the hydroxy group of Formula 35 to produce the compound of Formula 4.
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公开(公告)号:ES2449268T3
公开(公告)日:2014-03-19
申请号:ES10155058
申请日:2006-08-18
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , CHEN MINZHANG , COCHRAN JOHN E
IPC: C07D209/52 , A61K31/403 , C07D471/08
Abstract: Proceso de purificación del compuesto de Fórmula 4, que comprende:**Fórmula** a) disolver el compuesto de Fórmula 4 en un disolvente orgánico para obtener una solución del compuesto deFórmula 4, b) añadir un ácido a la solución del compuesto de Fórmula 4, y c) concentrar la solución del compuesto de Fórmula 4 para obtener el compuesto en una forma sólida.
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