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    81.
    发明专利
    未知

    公开(公告)号：BR0202279A

    公开(公告)日：2003-04-29

    申请号：BR0202279

    申请日：2002-06-13

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRACOISE ,  ROUSSEAU ANNE ,  ATASSI GHANAEM ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE ,  GUILBAUD NICOLAS ,  KRAUS-BERTHIER LAURENCE

    IPC: C07D209/80 ,  A61K31/403 ,  A61K31/433 ,  A61K31/4439 ,  A61P35/00 ,  C07D209/94 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/056 ,  A61K31/15 ,  A61K31/407 ,  C07D209/56

    Abstract: Indenoindolone derivatives (I), their isomers and salts with acids and bases are new. Indenoindolone derivatives (I), their isomers and salts with acids and bases are new; R = H, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or NR10R11), or alkenyl; R1-R8 = H, alkyl (optionally substituted by aryl, carboxy or alkoxycarbonyl), OH, acyloxy, NR12R13, carboxy, alkoxy (optionally substituted by aryl or NR14R15), alkenyloxy, or to adjacent groups R1-R8 = 1 or 2C alkylenedioxy; R9 = H, aryl, heteroaryl or alkyl (optionally containing one or more unsaturations and optionally substituted by one or more aryl, heteroaryl, 3-8C cycloalkyl, CN, or NR17R18 groups); X = O or NR16; R10, R11, R14, R15, R17, R18 = alkyl; NR10+R11, NR14+R15, NR17+R18 = nitrogen heterocycle; R12, R13 = H, alkyl, or NR14R15; R16 = H, alkyl, aryl, or aryl alkyl. Where alkyl, alkoxy, acyloxy, alkenyl and alkenyloxy groups have up to 6 C atoms, aryl is defined as phenyl, biphenyl, or naphthyl (optionally substituted by one or more halogen, alkyl, alkenyl, alkoxy, phenoxy, nitro, CN, amino, mono- and di-alkylamino or 1-2C alkylenedioxy groups) and heteroaryl groups may be mono- or bicyclic of 5-12 members with 1-3 heteroatoms (O, N, S) and optionally substituted by halogen, alkyl, OH, alkoxy, polyhaloalkyl, amino, mono- and di-alkylamino groups, and nitrogen heterocycles are monocyclic having 5-7 members including 1-3 heteroatoms, one of which is N and the others may be O, N, or S. An Independent claim is also included for the preparation of (I).

    Indenoidolone compounds, a process for their preparation and pharmaceutical compositions containing them.
    84.
    发明专利
    Indenoidolone compounds, a process for their preparation and pharmaceutical compositions containing them. 未知

    公开(公告)号：ZA200204757B

    公开(公告)日：2003-02-17

    申请号：ZA200204757

    申请日：2002-06-13

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROSSEAU ANNE ,  ATASSI GHANEM ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE ,  GUILBAUD NICOLAS ,  KRAUS-BERTHIER LAURENCE

    IPC: C07D209/80 ,  A61K31/403 ,  A61K31/433 ,  A61K31/4439 ,  A61P35/00 ,  C07D209/94 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/056 ,  C07D ,  A61K

    Abstract: Indenoindolone derivatives (I), their isomers and salts with acids and bases are new. Indenoindolone derivatives (I), their isomers and salts with acids and bases are new; R = H, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or NR10R11), or alkenyl; R1-R8 = H, alkyl (optionally substituted by aryl, carboxy or alkoxycarbonyl), OH, acyloxy, NR12R13, carboxy, alkoxy (optionally substituted by aryl or NR14R15), alkenyloxy, or to adjacent groups R1-R8 = 1 or 2C alkylenedioxy; R9 = H, aryl, heteroaryl or alkyl (optionally containing one or more unsaturations and optionally substituted by one or more aryl, heteroaryl, 3-8C cycloalkyl, CN, or NR17R18 groups); X = O or NR16; R10, R11, R14, R15, R17, R18 = alkyl; NR10+R11, NR14+R15, NR17+R18 = nitrogen heterocycle; R12, R13 = H, alkyl, or NR14R15; R16 = H, alkyl, aryl, or aryl alkyl. Where alkyl, alkoxy, acyloxy, alkenyl and alkenyloxy groups have up to 6 C atoms, aryl is defined as phenyl, biphenyl, or naphthyl (optionally substituted by one or more halogen, alkyl, alkenyl, alkoxy, phenoxy, nitro, CN, amino, mono- and di-alkylamino or 1-2C alkylenedioxy groups) and heteroaryl groups may be mono- or bicyclic of 5-12 members with 1-3 heteroatoms (O, N, S) and optionally substituted by halogen, alkyl, OH, alkoxy, polyhaloalkyl, amino, mono- and di-alkylamino groups, and nitrogen heterocycles are monocyclic having 5-7 members including 1-3 heteroatoms, one of which is N and the others may be O, N, or S. An Independent claim is also included for the preparation of (I).

    NOVEL BENZO[B]PYRANE[3,2-H]ACRIDIN-7-ONES, METHOD OF OBTAINING THEM AND PHARMACOLOGICAL COMPOSITION CONTAINING SUCH COMPOUNDS
    85.
    发明专利
    NOVEL BENZO[B]PYRANE[3,2-H]ACRIDIN-7-ONES, METHOD OF OBTAINING THEM AND PHARMACOLOGICAL COMPOSITION CONTAINING SUCH COMPOUNDS 未知

    公开(公告)号：PL355188A1

    公开(公告)日：2003-01-27

    申请号：PL35518802

    申请日：2002-07-24

    Applicant: SERVIER LAB

    Inventor： KOCH MICHEL ,  TILLEQUIN FRANCOIS ,  MICHEL SYLVIE ,  SEGUIN ELISABETH ,  EL OMRI ABDELHAKIM ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE

    IPC: A61K31/4741 ,  A61K31/5377 ,  A61P35/00 ,  C07D221/04 ,  C07D491/048 ,  C07D311/00 ,  C07D491/04 ,  C07D491/052 ,  C07D491/153 ,  C07D491/056 ,  C07D497/02 ,  C07D498/02

    Abstract: Benzo(b)pyrano(3,2-h)acridin-7-one derivatives (I), their isomers, N-oxides, and salts with acids and bases are new. Benzo(b)pyrano(3,2-h)acridin-7-one derivatives (I), their isomers, N-oxides, and salts with acids and bases are new. X, Y = H, halogen, SH, CN, NO2, 1-6C alkyl, trihaloalkyl or trihaloalkylcarbonylamino, ORa, NRaRb, -NRa-C(O)-T1, -O-T2-NRaRb, -O-T2-O-Ra, -N-Ra-T2-ORa, -NRa-T2-NRaRb, -OC(O)-T1- or -NRa-T2-COO-Ra, or when they are on adjacent positions X and Y together may form methylenedioxy or ethylenedioxy; Ra, Rb = H, 1-6C alkyl, aryl, or aryl 1-6C alkyl; or NRaRb = 5 or 6 membered heterocycle which may contain O or N as a second heteroatom; T1 = 1-6C alkyl, 2-6C alkenyl, aryl, aryl-1-6C alkyl, 1-6C alkylene substituted by ORa or NRaRb; T2 = 1-6C alkylene; R1 = H or 1-6C alkyl; R2 = H, 1-6C alkyl, ORa, NRaRb, -NRa-C(O)-T1, -O-T2-NRaRb, -O-T2-O-Ra, -N-Ra-T2-ORa, -NRa-T2-NRaRb, -OC(O)-T1- or -NRa-T2-COO-Ra; R3, R4 = H or 1-6C alkyl; W = -CH(R5)-CH(R6)-, -CH=C(R7)-, -C(R7)=CH-, or -C(O)-CH(R8)-; R5, R6 = A1 or A2; A1 = -W1-C(W2)-W3-T1, -W4-C(W2)-T1, -W1-S(O)n-W3-T1, or -W1-S(O)n-T1; A2 = H, OH, 1-6C alkoxy, alkylcarbonyloxy, arylcarbonyloxy, arylalkyl carbonyloxy, or amino (optionally substituted by one or two 1-6C alkyl groups); W1, W3 = O, S, or N substituted by H, alkyl, aryl, or aralkyl; W2 = O or S; W4 = S or N substituted by H, alkyl, aryl, or aralkyl; n = 1 or 2; R7 = OH, 1-6C alkoxy, -C(W2)-T1, -W1-C(W2)-W3-T1, -W1-C(W2)-T1, -W1-S(O)n-W3-T1, -W1-S(O)n-T1 or H; and R8 = 1-6C alkoxy, alkylcarbonyloxy or OH. Provided that: (1) either R5 and R6 are both A1, or one is A1 and the other is A2; (2) R7 is only H when R2 is -O-T2-ORa and/or X is H and Y is in position 13 of the naphthyl system in the pentacyclic skeleton and is amino optionally substituted by alkyl, acyl, or trihaloalkylcarbonyl; and (3) R8 is only OH when R2 is -O-T2-ORa. An Independent claim is also included for the preparation of (I).

    89.
    发明专利
    未知

    公开(公告)号：AT222253T

    公开(公告)日：2002-08-15

    申请号：AT00403108

    申请日：2000-11-09

    Applicant: SERVIER LAB

    Inventor： LAVIELLE GILBERT ,  HAUTEFAYE PATRICK ,  PIERRE ALAIN ,  ATASSI GHANEM ,  HICKMAN JOHN ,  CIMETIERE BERNARD

    IPC: C07D491/22 ,  A61K31/4375 ,  A61K31/4745 ,  A61P35/00 ,  C07D401/02 ,  C07D471/14 ,  C07D221/00 ,  C07D209/00

    Abstract: Camptothecin analogs (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Camptothecin analogs of formula (I), their enantiomers, diastereoisomers, and salts are new. n = 0-2; R1-R5 = H, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, OH, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, NO2, CN, aminocarbonyl (optionally substituted on the N by one or two alkyl groups), -(CH2)p-NRaRb, or -O-CO- NRaRb; or two adjacent groups of R2-R5 = -O-(CH2)t-O-; p = 0 - 6; Ra, Rb = H, alkyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, acyl, optionally substituted aryl or optionally substituted arylalkyl; or NRaRb = pyrrolyl, piperidinyl, or piperazinyl each of the cyclic groups being optionally substituted; t = 1-3; R60, R70n, R80, and R90 = H, OH, alkoxy, or -O-CO-X or -O-CO-NXW; X, W = alkyl, alkenyl, alkynyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, optionally substituted aryl, or optionally substituted aryl alkyl; R61, R71n, R81, and R91 = H, alkyl, alkenyl or alkynyl; or vicinal pairs may together form a bond or an oxirane group; or R60+R61, R70n+R71n, R80+R81n and/or R90+R91 = oxo or -O-(CH2)t1-O-; t1 = 1-3 with the proviso that R60, R70n, R80, R90, R61, R71n, R81, and R91 are not all H. Alkyl, alkoxy and acyl groups have 1-6C; alkenyl have 2-6C and 1-3 double bonds; alkynyl have 2-6C and 1-3 triple bonds; aryl = phenyl or naphthyl; 'substituted' on aryl or aryl alkyl groups means by one or more halogens, alkyl, alkoxy, OH, CN, NO2, amino or mono- or dialkylamino groups; 'substituted' on heterocyclic groups means by one or more alkyl, alkoxy, aryl, aryl alkyl, aryloxy and/or aryloxy alkyl groups. An Independent claim is included for the preparation of (I).

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