公开(公告)号：ZA200502829B

公开(公告)日：2006-08-30

申请号：ZA200502829

申请日：2005-04-07

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPFIRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

IPC: A61K20060101 ,  A61P20060101 ,  A61P35/00 ,  C07D20060101 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14

Abstract: 1,4-benzodioxino(2,3-e)isoindole derivatives (I) are new. 1,4-benzodioxino(2,3-e)isoindole derivatives of formula (I) and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. A = atoms that complete groups of formula (a) or (b); W1 = atoms that complete a phenyl or pyridyl ring; Z' = H, halogen, 1-6C alkyl or alkoxy (both optionally substituted by aryl), nitro, cyano, hydroxy, aryl, or NR5R6; R5, R6 = H or 1-6C alkyl; R4 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COOR'5; R'5 = 1-6C alkyl, aryl or aryl(1-6C)alkyl; Y' = oxygen or methylene; R2 = H; and R3 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or trifluoromethylsulfonyl; or R2+R3 = bond; R1 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl, or 1-6C alkylene, substituted by one or more of OR5 or NR5R6; Z1, Z2 = H or; Z1+Z2 = fused phenyl; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy, amino or mono- or di-1-6C alkylamino. Provided that if Z' is H, then R1 is not H. Independent claims are included for preparing (I).

公开(公告)号：FR2826653B1

公开(公告)日：2005-10-14

申请号：FR0108615

申请日：2001-06-29

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  ROUTIER SYLVAIN ,  COUDERT GERARD ,  MEROUR JEAN YVES ,  HICKMAN JOHN ,  PIERRE ALAIN ,  RENARD PIERRE ,  PFEIFFER BRUNO

IPC: C07H19/23 ,  A61K31/706 ,  A61P35/00 ,  C07H15/252 ,  C07D471/22 ,  C07D493/22 ,  A61K31/4439 ,  A61K31/4985

Abstract: Compounds of formula (I):

公开(公告)号：AR041654A1

公开(公告)日：2005-05-26

申请号：ARP030103789

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  C07D498/22 ,  A61K31/4353 ,  A61K31/5365

Abstract: Reivindicación 1: Compuestos de fórmula (1) donde A representa con los átomos de C al que está unido un grupo de fórmula (2) o (3) donde: W1 representa con los átomos de C a los cuales está unido, un grupo fenilo o un grupo piridinilo; Z representa un grupo elegido entre átomo de H, halógeno, grupo alquilo C1-6 lineal o ramificado, nitro, ciano, hidroxi, alcoxi C1-6 lineal o ramificado, arilo, arilalquilo C1-6 lineal o ramificado, ariloxi, arilalcoxi C1-6 lineal o ramificado, -NR5R6, donde R5 y R6, idénticos o diferentes, independientemente uno de otro, representan cada uno un grupo elegido entre átomo de H, grupo alquilo C1-6 lineal o ramificado; R4 representa un grupo elegido entre átomo de H, grupo alquilo C1-6 lineal o ramificado, arilo, arilalquilo C1-6 lineal o ramificado, o un grupo -C(O)-OR´5, donde R´5 representa un grupo elegido entre grupo alquilo c1-6 lineal o ramificado, arilo, o arilalquilo c1-6 lineal o ramificado; Y representa un grupo elegido entre átomo de O o grupo metileno; R2 representa un átomo de H, y en este caso: R3 representa un grupo elegido entre átomo de H, grupo alquilo C1-6 lineal o ramificado, arilo, arilalquilo C1-6 lineal o ramificado, o -SO2CF3, o bien R2 y R3 forman una unión; R1 representa un grupo elegido entre átomo de H, grupo alquilo C1-6 lineal o ramificado, arilo, arilalquilo C1-6 lineal o ramificado, o una cadena alquileno C1-6 lineal o ramificada, sustituida por uno o varios grupos, idénticos o diferentes, elegidos entre -OR"5 y NR"5R"6, donde R"5 y R"6 tienen las mismas definiciones que R5 y R6 tal como se los definió anteriormente; Z1 y Z2 representan cada uno un átomo de H o Z1 y Z2 forman ambos, con los átomos de C que los contienen, un grupo fenilo, y se entiende que, cuando Z representa un átomo de H, entonces R1 es diferente de átomo de H, sus enantiómeros, diastereoisómeros, N-óxidos, como así también sus sales de adición a un ácido o a una base farmacéuticamente aceptable, y se entiende que, por arilo, debe comprenderse un grupo fenilo, naftilo, dihidronaftilo, tetrahidronaftilo, indenilo o indanilo, y que cada uno de esos grupos puede estar sustituido eventualmente por uno o varios grupos, idénticos o diferentes, elegidos entre halógeno, alquilo C1-6 lineal o ramificado, trihalógenoalquilo C1-6 lineal o ramificado, hidroxi, alcoxi C1-6 lineal o ramificado, y amino eventualmente sustituido por uno o dos grupos alquilo C1-6 lineal o ramificado.

公开(公告)号：NO20052330A

公开(公告)日：2005-05-12

申请号：NO20052330

申请日：2005-05-12

Applicant: SERVIER LAB

Inventor： PIERRE ALAIN ,  RENARD PIERRE ,  HICKMAN JOHN ,  ROUTIER SYLVAIN ,  LEONCE STEPHANE ,  COUDERT GERARD ,  CAIGNARD DANIEL-HENRI ,  AYERBE NATHALIE ,  LEPIFRE FRANCK

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  A61K31/5365 ,  C07D498/22

CPC classification number: C07D471/14 ,  C07D487/04 ,  C07D491/14

公开(公告)号：AU2003301532A1

公开(公告)日：2004-05-13

申请号：AU2003301532

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  A61K31/5365 ,  C07D498/22

Abstract: 1,4-benzodioxino(2,3-e)isoindole derivatives (I) are new. 1,4-benzodioxino(2,3-e)isoindole derivatives of formula (I) and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. A = atoms that complete groups of formula (a) or (b); W1 = atoms that complete a phenyl or pyridyl ring; Z' = H, halogen, 1-6C alkyl or alkoxy (both optionally substituted by aryl), nitro, cyano, hydroxy, aryl, or NR5R6; R5, R6 = H or 1-6C alkyl; R4 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COOR'5; R'5 = 1-6C alkyl, aryl or aryl(1-6C)alkyl; Y' = oxygen or methylene; R2 = H; and R3 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or trifluoromethylsulfonyl; or R2+R3 = bond; R1 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl, or 1-6C alkylene, substituted by one or more of OR5 or NR5R6; Z1, Z2 = H or; Z1+Z2 = fused phenyl; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy, amino or mono- or di-1-6C alkylamino. Provided that if Z' is H, then R1 is not H. Independent claims are included for preparing (I).

公开(公告)号：FR2826653A1

公开(公告)日：2003-01-03

申请号：FR0108615

申请日：2001-06-29

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  ROUTIER SYLVAIN ,  COUDERT GERARD ,  MEROUR JEAN YVES ,  HICKMAN JOHN ,  PIERRE ALAIN ,  RENARD PIERRE ,  PFEIFFER BRUNO

IPC: C07H19/23 ,  A61K31/706 ,  A61P35/00 ,  C07H15/252 ,  C07D471/22 ,  C07D493/22 ,  A61K31/4439 ,  A61K31/4985

Abstract: Compounds of formula (I) wherein: WI and W2 represent, with the carbon atoms to which they are bound, a phenyl group or a pyridinyl group, and at least one of the groups W1 or W2 represent a pyridinyl group; R1 and R2 each represent a group of formula U-V as defined in the description, X and X1 each represent a hydrogen atom, a hydroxy, alkoxy, mercapto or alkylthio group; Y and Y1 each represent a hydrogen atom; or X and Y, X1 and Y1 represent, together with the carbon atom that they include, a carbonyl or thiocarbonyl group; R4 and R5 are as defined in the description; Q1, Q2 represent a hydrogen atom, or Q1 and Q2, together with the carbon atoms that they include, form an aromatic link. The inventive compounds are used in medicaments.

公开(公告)号：NZ539195A

公开(公告)日：2007-05-31

申请号：NZ53919503

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PEIRRE ALAIN ,  LEONCE STEPHANE

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  C07D498/22 ,  A61K31/5365

Abstract: Disclosed are compounds of formula (I) wherein: A, together with the carbon atoms to which it is bonded represents a group of formula (a) or (b) with substituents as defined in the specification; Y represents an oxygen atom or a methylene group; R2 represents H and R3 represents H, alkyl, aryl, aryl-alkyl and SO2CF3, or R2 and R3 form a bond; R1 represents a group selected from hydrogen or optionally substituted alkyl, aryl, aryl-alkyl or alkylene; Z1 and Z2 each represent a hydrogen atom or Z1 and Z2 together with the carbon atoms carrying them, form a phenyl group. Also disclosed are methods of forming the above compounds and their use in the treatment of tumours.

公开(公告)号：AT344800T

公开(公告)日：2006-11-15

申请号：AT03809363

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  C07D498/22 ,  A61K31/5365

Abstract: 1,4-benzodioxino(2,3-e)isoindole derivatives (I) are new. 1,4-benzodioxino(2,3-e)isoindole derivatives of formula (I) and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. A = atoms that complete groups of formula (a) or (b); W1 = atoms that complete a phenyl or pyridyl ring; Z' = H, halogen, 1-6C alkyl or alkoxy (both optionally substituted by aryl), nitro, cyano, hydroxy, aryl, or NR5R6; R5, R6 = H or 1-6C alkyl; R4 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COOR'5; R'5 = 1-6C alkyl, aryl or aryl(1-6C)alkyl; Y' = oxygen or methylene; R2 = H; and R3 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or trifluoromethylsulfonyl; or R2+R3 = bond; R1 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl, or 1-6C alkylene, substituted by one or more of OR5 or NR5R6; Z1, Z2 = H or; Z1+Z2 = fused phenyl; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy, amino or mono- or di-1-6C alkylamino. Provided that if Z' is H, then R1 is not H. Independent claims are included for preparing (I).

公开(公告)号：EA007221B1

公开(公告)日：2006-08-25

申请号：EA200301301

申请日：2002-06-28

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  ROUTIER SYLVAIN ,  COUDERT GERARD ,  MEROUR JEAN-YVES ,  HICKMAN JOHN ,  PIERRE ALAIN ,  RENARD PIERRE ,  PFEIFFER BRUNO

IPC: C07D471/22 ,  C07H19/23 ,  A61K31/44 ,  A61K31/706 ,  A61P35/00 ,  C07D498/22 ,  C07H15/252

Abstract: Соединенияформулы (I)вкоторой Wи W, вместес атомамиуглерода, скоторымионисвязаны, представляютсобойфенильнуюгруппуилипиридильнуюгруппуи покрайнеймереоднаизгрупп Wили Wпредставляетсобойпиридильнуюгруппу, Rи Rкаждыйпредставляетсобойгруппуформулы U-V, котораяпринимаетзначения, указанныев описании, Rимеетзначения, указанныев описании, X и Y вместес атомомуглерода, несущимих, образуюткарбонильнуюилитиокарбонильнуюгруппу, Xи Yвместес атомомуглерода, несущимих, образуюткарбонильнуюилитиокарбонильнуюгруппу, Rи Rпринимаютзначения, указанныев описании, Q, Qпредставляетсобойатомводородаили Qи Qвместес атомамиуглерода, несущимиих, образуютароматическуюсвязь. Лекарственныесредства.

公开(公告)号：BR0314878A

公开(公告)日：2005-08-02

申请号：BR0314878

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  C07D498/22 ,  A61K31/5365

Abstract: 1,4-benzodioxino(2,3-e)isoindole derivatives (I) are new. 1,4-benzodioxino(2,3-e)isoindole derivatives of formula (I) and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. A = atoms that complete groups of formula (a) or (b); W1 = atoms that complete a phenyl or pyridyl ring; Z' = H, halogen, 1-6C alkyl or alkoxy (both optionally substituted by aryl), nitro, cyano, hydroxy, aryl, or NR5R6; R5, R6 = H or 1-6C alkyl; R4 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COOR'5; R'5 = 1-6C alkyl, aryl or aryl(1-6C)alkyl; Y' = oxygen or methylene; R2 = H; and R3 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or trifluoromethylsulfonyl; or R2+R3 = bond; R1 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl, or 1-6C alkylene, substituted by one or more of OR5 or NR5R6; Z1, Z2 = H or; Z1+Z2 = fused phenyl; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy, amino or mono- or di-1-6C alkylamino. Provided that if Z' is H, then R1 is not H. Independent claims are included for preparing (I).