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公开(公告)号:SI1556387T1
公开(公告)日:2007-08-31
申请号:SI200330818
申请日:2003-10-17
Applicant: SERVIER LAB
Inventor: COUDERT GERARD , LEPIFRE FRANCK , CAIGNARD DANIEL-HENRI , RENARD PIERRE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE
IPC: C07D498/00 , A61K31/00 , A61P35/00 , C07D265/00 , C07D497/04 , C07D497/14
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公开(公告)号:FR2892418A1
公开(公告)日:2007-04-27
申请号:FR0510808
申请日:2005-10-24
Applicant: SERVIER LAB
Inventor: LA VIELLE GILBERT , HAUTEFAYE PATRICK , PIERRE ALAIN , HICKMAN JOHN , LEONCE STEPHANE
IPC: C07D471/14 , A61K31/4745 , A61P35/00 , C07D207/456 , C07D215/12 , C07D217/02
Abstract: Composé de formule (I) : dans laquelle :&circlef; R1, R2, R3, R4, R5, R70, R80, R90, R71, R81, R91, Alk, Alk', X, X' et G sont tels que définis dans la description.Médicaments.
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公开(公告)号:AT358677T
公开(公告)日:2007-04-15
申请号:AT03809362
申请日:2003-10-17
Applicant: SERVIER LAB
Inventor: COUDERT GERARD , LEPIFRE FRANCK , CAIGNARD DANIEL-HENRI , RENARD PIERRE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE
IPC: A61P35/00 , C07D497/04 , C07D497/14 , C07D498/04 , A61K31/535 , C07D498/14 , C07D265/38
Abstract: Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives of formula (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new W1 = atoms that complete phenyl or pyridyl; Z = hydrogen, halo, 1-6C alkyl or alkoxy (both optionally substituted by aryl), aryl, aryloxy or hydroxy; R1 = hydrogen, 1-6C alkyl, optionally substituted by aryl, aryl, COR5 or 1-6C alkylene, substituted by one or more of halo, cyano, OR6, NR6R7, COOR6, COR6 or CONHR6; R2 = hydrogen or -CH2CH2OR8; R3 and R4 = hydrogen, 1-6C alkyl, optionally substituted by aryl, or aryl, or together they complete a 5 or 6-membered, monocyclic heterocycle, optionally including an additional oxygen or nitrogen; n = 1-6; R5 = hydrogen, 1-6C alkyl or alkoxy, hydroxy, aryl, aryl(1-6C)alkyl or aryloxy; R6 and R7 = hydrogen, 1-6C alkyl, aryl(1-6C)alkyl or aryl, or together they complete a heterocycle as above; R8 = hydrogen, 1-6C alkyl, aryl, aryl(1-6C)alkyl, S(O)tR6 or -T1-R9; t = 0-2; T1 = 1-6C alkylene; R9 = halo, cyano, OR6, NR6R7, CHO, COOR6 or CONR6R7; 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 or amino, optionally substituted by 1 or 2 1-6C alkyl. Independent claims are also included for the following:0041658 (1) methods for the preparation of (I); and (2) intermediates of formulae (X), (XI) and (XIV). Boc = tert-butoxycarbonyl; and Pg = Boc or phenoxycarbonyl.
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公开(公告)号:FR2889527A1
公开(公告)日:2007-02-09
申请号:FR0508364
申请日:2005-08-05
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , HAUTEFAYE PATRICK , PIERRE ALAIN , HICKMAN JOHN , LEONCE STEPHANE
IPC: C07D471/14 , A61K31/4745 , A61P35/00 , C07D207/44 , C07D213/64 , C07D215/12
Abstract: Composé de formule (I) : dans laquelle :&circlef; n, R1, R2, R3, R4, R5, R80, R90, R81, R91, Alk et G sont tels que définis dans la description.Médicaments.
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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).
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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.
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公开(公告)号:NO20056091L
公开(公告)日:2006-06-23
申请号:NO20056091
申请日:2005-12-21
Applicant: SERVIER LAB
Inventor: KOCH MICHEL , PIERRE ALAIN , MICHEL SYLVIE , HICKMAN JOHN , KRAUS-BERTHIER LAURENCE , LEONCE STEPHANE , PFEIFFER BRUNO , TILLEQUIN FRANCOIS
IPC: C07D491/04 , C07D491/22 , A61K31/436 , A61P35/00
Abstract: Benzo pyarano[3,2-h]acridin-7-one cinnamate compounds (I) and their enantiomers, diastereoisomers, hydrates, solvates, acids, bases or addition salts are new. Benzo pyarano[3,2-h]acridin-7-one cinnamate compounds of formula (I) and their enantiomers, diastereoisomers, hydrates, solvates, acids, bases or addition salts are new. X, Y 1H, halo, OH, (1-6C) alkoxy, nitro, CN, (1-6C) alkyl (optionally substituted by one or more OH or halo), (2-6C) alkenyl or -NRaRb; either R-a, R-b : H or (1-6C) alkyl; or N-R-aR-b : a monocyclic or 5-7-membered heterocycle optionally having a second heteroatom of O or N in the cyclic system; Z : O or NR-c; R-c : H, (1-6C) alkyl, aryl or aryl-(1-6C)alkyl; Ar : (hetero)aryl; R 1, R 3, R 4H or (1-6C) alkyl; R 2H, (1-6C) alkyl, OR-a or NR-aR-b; R 5OR-c, NR-cR-d, W 1-C(W 2)-U 1-V 1, W-a-C(W 2)-W 3-T 1 or -Z-CO-CH=CHAr; W-a, W 3O or NR-c; W 2O; U 1(1-8C) alkylene or (2-8C) alkenylene; V 1H, (hetero) aryl, OR, CO 2R-c, COR-c, CON-aaR-bb, NR-aaR-bb, N(R-c)-CO 2R-cc or N(R-c)COR-cc; R-cc : R-c; either R-aa, R-bb : R-a, R-b or aryl-(1-6C)alkyl; or N-R-aaR-bb : N-R-aR-b; and T 1H, (1-6C) alkyl or (2-6C) alkenyl, aryl or aryl-(1-6C) alkyl (all optionally substituted by OR-c or NR-aaR-bb). where the aryl is phenyl or naphthyl optionally substituted by one or more substituents of (1-6C) alkyl (optionally substituted by one or more OH or halo), OH, halo, carboxy, NO 2, NH 2, or mono- or di-(1-6C) alkylamino, where the alkyl moiety is (1-6C) alkoxy, (1-6C) acyl or (1-6C) alkylcarbonyloxy; and the heteroaryl is 5-12-membered (monocyclic, aromatic or bicyclic with aromatic ring(s)), and has 1, 2 or 3 heteroatoms of O, N or S, and optionally substituted by one or more groups of halo, (1-6C) alkyl optionally substituted by one or more OH, halo, (1-6C) alkoxy or NH 2 optionally substituted by one or two (1-6C)alkyl. [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.
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公开(公告)号:NO20056091A
公开(公告)日:2006-06-23
申请号:NO20056091
申请日:2005-12-21
Applicant: SERVIER LAB
Inventor: KOCH MICHEL , PIERRE ALAIN , MICHEL SYLVIE , HICKMAN JOHN , KRAUS-BERTHIER LAURENCE , LEONCE STEPHANE , PFEIFFER BRUNO , TILLEQUIN FRANCOIS
IPC: C07D491/04 , C07D491/22 , A61K31/436 , A61P35/00
CPC classification number: C07D491/04
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公开(公告)号:FR2879600A1
公开(公告)日:2006-06-23
申请号:FR0413682
申请日:2004-12-22
Applicant: SERVIER LAB , CENTRE NAT RECH SCIENT , UNIV PARIS DESCARTES
Inventor: KOCH MICHEL , TILLEQUIN FRANCOIS , MICHEL SYLVIE , HICKMAN JOHN , PIERRE ALAIN , LEONCE STEPHANE , PFEIFFER BRUNO , KRAUS BERTHIER LAURENCE
IPC: C07D491/04 , C07D491/052 , A61K31/436 , A61K31/4741 , A61P35/00 , C07D219/06 , C07D309/10
Abstract: dans laquelle :. X et Y représentent chacun un groupement choisi parmi hydrogène, halogène, alkoxy, nitro, cyano, alkyle, alkényle, polyhalogénoalkyle, et -NRaRb dans lequel Ra et Rb sont tels que définis dans la description,. Z représente un atome d'oxygène ou NRc dans lequel Rc, est tel que défini dans la description,. Ar représente aryle ou hétéroaryle,. R1 représente un atome d'hydrogène ou un groupement alkyle,. R2 représente un groupement choisi parmi atome d'hydrogène, alkyle, -ORa ; NRaRb dans lesquels Ra et Rb sont tels que définis dans la description,. R3, R4 représentent un atome d'hydrogène ou un groupement alkyle,. R5 représente atome d'hydrogène ou un groupement de formule ORc, NRcRd, W1-C(W2)-U-V, W1-C(W2)-W3-T1, Z-CO-CH=CHAr dans lesquels Rc, Rd, W1, W2, W3, U, V, T, Z et Ar sont tels que définis dans la description,leurs isomères, ainsi que leurs sels d'addition à un acide ou à une base pharmaceutiquement acceptable.Médicaments.
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公开(公告)号:FR2859208B1
公开(公告)日:2006-01-21
申请号:FR0310367
申请日:2003-09-02
Applicant: SERVIER LAB , CENTRE NAT RECH SCIENT
Inventor: MONNERET CLAUDE , DAUZONNE DANIEL , HICKMAN JOHN , PIERRE ALAIN , KRAUS BERTHIER LAURENCE , PFEIFFER BRUNO , RENARD PIERRE
IPC: C07D493/04 , A61K31/36 , A61P35/00 , C07D307/33 , C07D317/50
Abstract: Composés de formule (I) :dans laquelle :R1 représente un groupement choisi parmi hydrogène, alkyle, aryle, arylalkyle, hétéroaryle, hétéroarylalkyle, alkylcarbonyle, arylcarbonyle, arylalkylcarbonyle, alkoxycarbonyle, aryloxycarbonyle, arylalkoxycarbonyle, hétérocycloalkoxycarbonyle, alkylsulfonyle, arylsulfonyle, arylalkylsulfonyle, phosphonique et Si(Ra)2Rb,Y représente un groupement choisi parmi HN-NH et N-R2,R3 représente un atome d'hydrogène, un groupement alkyle, cycloalkyle, aryle, arylalkyle,R4 représente un atome d'hydrogène ou un groupement alkyle,leurs énantiomères, diastéréoisomères ainsi que leurs sels d'addition à un acide ou à une base pharmaceutiquement acceptable.
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