公开(公告)号：PL375370A1

公开(公告)日：2005-11-28

申请号：PL37537003

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: A process for the preparation of a class of phenylalanine enamide derivatives is described: wherein: Ar 1 is an optionally substituted aromatic or heteroaromatic group; L 2 is a linker group selected from -N(R 4 )- [where R 4 is a hydrogen atom or an optionally substituted straight or branched C 1-6 alkyl group], -CON(R 4 )-, or -S(O) 2 N(R 4 )-; R 1 is a carboxylic acid (-CO 2 H) or a derivative or biostere thereof; R 2 is a hydrogen atom or a C 1-6 alkyl group; R x , R y and R z which may be the same or different is each an atom or group -L 1 (Alk 1 ) n (R 3 ) v ; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Q a is a group -N(R 4 )H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar 1 W wherein W is a group selected from X 1 (wherein X 1 is a leaving atom or group), -COX 2 (wherein X 2 is a halogen atom or a -OH group) or -SO 2 X 3 (in which X 3 is a halogen atom).

公开(公告)号：EA007155B1

公开(公告)日：2006-08-25

申请号：EA200500212

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07C227/18 ,  C07B61/00 ,  C07C229/36 ,  C07C231/02 ,  C07C303/38 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04

Abstract: Способполученияклассаенамидныхпроизводныхфенилаланина, описанныхформулой (1), вкоторой Arпредставляетсобойнеобязательнозамещеннуюароматическуюилигетероароматическуюгруппу; Lпредставляетсобойсвязующуюгруппу, выбраннуюиз -N(R) [где Rявляетсяатомомводородаилинеобязательнозамещеннойнормальнойилиразветвленной C-алкильнойгруппой], -CON(R) или S(О)N(R)-; Rпредставляетсобойкарбоновуюкислоту (-СОН) илиеепроизводноеилибиостер; Rпредставляетсобойатомводородаили C-алкильнуюгруппу; R, Rи R, которыемогутбытьодинаковымиилиразными, представляютсобойатомилигруппу L(Alk)(R); иегосоли, сольваты, гидратыи N-оксиды; которыйвключаетвзаимодействиесоединенияформулы (2), где Qпредставляетсобойгруппу -N(R)H; иегосоли, сольваты, гидратыи N-оксиды; ссоединением ArW, вкотором W представляетсобойгруппу, выбраннуюиз X(причем Xявляетсяудаляемыматомомилигруппой), -СОХ(причем XявляетсяатомомгалогенаилиОН-группой) или -SOX(вкоторой Xявляетсяатомомгалогена).

公开(公告)号：MXPA05000596A

公开(公告)日：2005-04-28

申请号：MXPA05000596

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: Un proceso para la preparacion de una clase de derivados de fenilalanina enamida es descrito (formula 1) en donde: Ar1 es un grupo aromatico o heteroaromatico opcionalmente substituido; L2 es un grupo enlazador seleccionado de -N(R4)- [en donde R4 es un atomo de hidrogeno o un grupo alquilo de C1-6 recto o ramificado, opcionalmente substituido], -CON(R)4-; o -S(O)2N(R4)-; R1 es un acido carboxilico (-CO2H) o un derivado o bioester de los mismos; R2 es un atomo de hidrogeno o un grupo alquilo de C1-6; RX, RY RZ los cuales pueden ser los mismos o diferentes en cada atomo o grupo -L1(Alq1)n (R3)V y las sales, solvatos, hidratos y N-oxidos de los mismos; que comprende hacer reaccionar un compuesto de la formula (2) : en donde: Qa es un grupo -N(R4)H; y las sales, solvatos, hidratos y N-oxidos de los mismos; con un compuesto Ar1W en donde W es un grupo seleccionado de X1 (en donde X1 es un atomo o grupo saliente) -COX2 (en donde X2 es un atomo de halogeno o un grupo -OH) o -S02X3 (en el cual X3 es un atomo de halogeno).

公开(公告)号：NO20050826L

公开(公告)日：2005-04-15

申请号：NO20050826

申请日：2005-02-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: A process for the preparation of a class of phenylalanine enamide derivatives is described: wherein: Ar 1 is an optionally substituted aromatic or heteroaromatic group; L 2 is a linker group selected from -N(R 4 )- [where R 4 is a hydrogen atom or an optionally substituted straight or branched C 1-6 alkyl group], -CON(R 4 )-, or -S(O) 2 N(R 4 )-; R 1 is a carboxylic acid (-CO 2 H) or a derivative or biostere thereof; R 2 is a hydrogen atom or a C 1-6 alkyl group; R x , R y and R z which may be the same or different is each an atom or group -L 1 (Alk 1 ) n (R 3 ) v ; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Q a is a group -N(R 4 )H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar 1 W wherein W is a group selected from X 1 (wherein X 1 is a leaving atom or group), -COX 2 (wherein X 2 is a halogen atom or a -OH group) or -SO 2 X 3 (in which X 3 is a halogen atom).

公开(公告)号：CA2492441A1

公开(公告)日：2004-01-22

申请号：CA2492441

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： JONES STEPHEN WILFRED ,  TYRRELL NICHOLAS DAVID ,  SKEAD BENJAMIN MARK ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: A process for the preparation of a class of phenylalanine enamide derivative s is described formula (1) wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 i s a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group - L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; whic h comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H ; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group ), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).

公开(公告)号：NZ538160A

公开(公告)日：2006-03-31

申请号：NZ53816003

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: A process for the preparation of a class of phenylalanine enamide derivatives of formula (1) is disclosed, wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).

公开(公告)号：BR0312677A

公开(公告)日：2005-04-26

申请号：BR0312677

申请日：2003-07-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

Abstract: A process for the preparation of a class of phenylalanine enamide derivatives is described: wherein: Ar 1 is an optionally substituted aromatic or heteroaromatic group; L 2 is a linker group selected from -N(R 4 )- [where R 4 is a hydrogen atom or an optionally substituted straight or branched C 1-6 alkyl group], -CON(R 4 )-, or -S(O) 2 N(R 4 )-; R 1 is a carboxylic acid (-CO 2 H) or a derivative or biostere thereof; R 2 is a hydrogen atom or a C 1-6 alkyl group; R x , R y and R z which may be the same or different is each an atom or group -L 1 (Alk 1 ) n (R 3 ) v ; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Q a is a group -N(R 4 )H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar 1 W wherein W is a group selected from X 1 (wherein X 1 is a leaving atom or group), -COX 2 (wherein X 2 is a halogen atom or a -OH group) or -SO 2 X 3 (in which X 3 is a halogen atom).

公开(公告)号：NO20050826A

公开(公告)日：2005-04-15

申请号：NO20050826

申请日：2005-02-16

Applicant: CELLTECH R&D LTD

Inventor： SKEAD BENJAMIN MARK ,  TYRRELL NICHOLAS DAVID ,  JONES STEPHEN WILFRED ,  BROOKES MICHAEL HANDFORTH

IPC: C07B61/00 ,  C07C229/36 ,  C07D213/81 ,  C07D311/96 ,  C07D471/04 ,  C07C227/18 ,  C07C231/02 ,  C07C303/38

CPC classification number: C07D213/81 ,  C07D311/96 ,  C07D471/04