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    15.
    发明专利
    未知

    公开(公告)号：DE60205538T2

    公开(公告)日：2006-06-14

    申请号：DE60205538

    申请日：2002-06-12

    Applicant: SERVIER LAB

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

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

    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).

    Cycloheptene derivatives and pharmaceuticals thereof
    16.
    发明专利
    Cycloheptene derivatives and pharmaceuticals thereof 未知

    公开(公告)号：NZ516684A

    公开(公告)日：2003-06-30

    申请号：NZ51668402

    申请日：2002-01-17

    Applicant: SERVIER LAB

    Inventor： CASARA PATRIC ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS

    IPC: C07C317/00 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06 ,  C07D233/88 ,  A61K31/44 ,  A61K31/444

    Abstract: Compounds of formula (I); where: X is a bond, alkylene, CO, S(O)n, *-S(O)n-A1-, *-CO-A1-, -A1-S(O)n-A'1- or -A1-CO-A'1 (where A1 and A'1 independently represent an alkylene group, and n is 0, 1 or 2), the symbol "*" indicating the point of attachment of those groups to the cycloheptene; Y is an optionally substituted aryl, heteroaryl, cycloalkyl or heterocycloalkyl group; R1, R2, R3 and R4 are independently hydrogen, or optionally substituted aryl, heteroaryl, cycloalkyl or heterocycloalkyl; or R1 and R2, or R2 and R3, or R3 and R4, taken in pairs, together form a bond; or R1 and R2, or R2 and R3, or R3 and R4, taken in pairs with the carbon atoms to which they are bonded, form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, having 5 or 6 ring members and containing 1 or 2 heteroatoms selected from nitrogen, oxygen and sulfur, on the understanding that only one ring can be fused on the 7-membered structure; T is ?H(R5)-, -N(R5)- or *-N(R5)CO- (where R5 is a hydrogen atom or is an optionally substituted alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl group) , the symbol "*" indicating the point of attachment of this group to the cycloheptene; V is hydrogen or is an optionally substituted aryl or heteroaryl group; A2 is a [C(R6)(R'6)]p group where p is 0, 1, 2, 3 or 4 when T represents a -CH(R5)- or *-N(R5)CO- group, or p is 1, 2, 3 or 4 when T represents an -N(R5)- group. Pharmaceutical compositions comprising the compound of formula (I) are also described.

    Indenoindoline derivatives, their process of preparation and pharmaceutical compositions containing them
    19.
    发明专利
    Indenoindoline derivatives, their process of preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：SK8342002A3

    公开(公告)日：2003-01-09

    申请号：SK8342002

    申请日：2002-06-11

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU 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 ,  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).

    20.
    发明专利
    未知

    公开(公告)号：FR2826009A1

    公开(公告)日：2002-12-20

    申请号：FR0107718

    申请日：2001-06-13

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE FRANCOISE ,  ROUSSEAU 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 ,  C07D405/14 ,  C07D403/12 ,  A61K31/4045 ,  A61K31/4402 ,  A61K31/4453

    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).

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