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    NUEVOS DERIVADOS TRICICLICOS SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    31.
    发明专利
    NUEVOS DERIVADOS TRICICLICOS SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：CO6230990A2

    公开(公告)日：2010-12-20

    申请号：CO09080210

    申请日：2009-07-31

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  GENESTE OLIVIER ,  HICKMAN JOHN

    IPC: A61K31/4985 ,  A61P35/00 ,  C07D471/04

    Abstract: Compuestos de fórmula (I):en la que: ° A representa un ciclo (hetero)aromático o no que contiene 5, 6 ó 7 eslabones, ° n y n' representan 0, 1 ó 2 ° X representa una cadena alquileno tal como se ha definido en la descripción, ° R3 representa un grupo arilo o heteroarilo, ° uno de los grupos R1 o R2 representa un átomo de hidrógeno y el otro representa un grupo de fórmula (II) tal como se ha definido en la descripción. 1.- Compuestos de fórmula (I):en la que: ° A representa un ciclo aromático o no que contiene 5, 6 ó 7 eslabones y que puede contener 1 ó 2 heteroátomos elegidos entre oxígeno, azufre y nitrógeno, pudiendo estar éste último sustituido con un grupo alquilo (C1-C6) lineal o ramificado, entendiéndose que el ciclo A así definido no puede contener 2 átomos de azufre ni 2 átomos de oxígeno y que uno de los eslabones puede representar un grupo C=O, ° n y n', idénticos o diferentes, representan 0, 1 ó 2, con 0

    33.
    发明专利
    未知

    公开(公告)号：DK1953161T3

    公开(公告)日：2009-11-30

    申请号：DK08290088

    申请日：2008-02-01

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  GENESTE OLIVIER ,  HICKMAN JOHN

    IPC: C07D471/04 ,  A61K31/498 ,  A61P35/00 ,  C07D487/04

    Abstract: Tricyclic diazacycloalkane derivatives (I) are new. Tricyclic diazacycloalkane derivatives of formula (I) are new. A : a 5- to 7-membered ring with 0-2 heteroatoms (O, S, N, NR), where one member can be C=O; R : 1-6C alkyl; n, n' : 0-2, provided that n+n'= 1-3; R 3aryl or heteroaryl; X : 1-6C alkylene, mono- or dioxaalkylene, cycloalkylene, arylene, heteroarylene or SO 2; R 1, R 2H or Q, provided that one is H and the other is Q; Q : YNHSO 2Ar; Y : CO or CH 2; Ar : R 4-substituted 3-R 5-4 R6-phenyl; R 5H; R 6H, NR 7R' 7 or CH 2NR 7R' 7; R 5+R 6groups forming a 5- or 6-membered ring including N para to to the SO 2 group, optionally containing another N atom and/or a SO 2 group, the ring being substituted with R 7; R 7, R' 7H or 1-6C alkyl substituted with aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, heterocycloalkyl or NR 10R' 10; R 10, R' 10H, 1-6C alkyl, 1-6C alkoxy, aryl or heteroaryl, or R 10+R' 10 forms an optionally oxo-substituted mono- or bicyclic group optionally containing another heteroatom; R 4H, NO 2, R 7, SO 2R 9, R or OR; R 9NH 2 or 1-6C (halo)alkyl. Independent claims are also included for: (1) two processes for preparing (I); (2) combination of a compound (I) and an anticancer agent selected from genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors and kinase inhibitors. [Image] ACTIVITY : Cytostatic. N-((4aR)-3-(4'-chloro-2-biphenylylmethyl)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolin-8-ylcarbonyl)-4-((1R)-3-dimethylamino-1-(phenylthiomethyl)propylamino)-3-nitrobenzenesulfonamide dihydrochloride had an IC50 of 0.305 mu M against H146 tumore cells. MECHANISM OF ACTION : Apoptosis promoter; Caspase 3 promoter.

    35.
    发明专利
    未知

    公开(公告)号：FR2912145B1

    公开(公告)日：2009-03-06

    申请号：FR0700741

    申请日：2007-02-02

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  GENESTE OLIVIER ,  HICKMAN JOHN

    IPC: C07D471/04 ,  A61K31/4985 ,  A61P35/00 ,  C07D215/06 ,  C07D241/04

    Abstract: Tricyclic diazacycloalkane derivatives (I) are new. Tricyclic diazacycloalkane derivatives of formula (I) are new. A : a 5- to 7-membered ring with 0-2 heteroatoms (O, S, N, NR), where one member can be C=O; R : 1-6C alkyl; n, n' : 0-2, provided that n+n'= 1-3; R 3aryl or heteroaryl; X : 1-6C alkylene, mono- or dioxaalkylene, cycloalkylene, arylene, heteroarylene or SO 2; R 1, R 2H or Q, provided that one is H and the other is Q; Q : YNHSO 2Ar; Y : CO or CH 2; Ar : R 4-substituted 3-R 5-4 R6-phenyl; R 5H; R 6H, NR 7R' 7 or CH 2NR 7R' 7; R 5+R 6groups forming a 5- or 6-membered ring including N para to to the SO 2 group, optionally containing another N atom and/or a SO 2 group, the ring being substituted with R 7; R 7, R' 7H or 1-6C alkyl substituted with aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, heterocycloalkyl or NR 10R' 10; R 10, R' 10H, 1-6C alkyl, 1-6C alkoxy, aryl or heteroaryl, or R 10+R' 10 forms an optionally oxo-substituted mono- or bicyclic group optionally containing another heteroatom; R 4H, NO 2, R 7, SO 2R 9, R or OR; R 9NH 2 or 1-6C (halo)alkyl. Independent claims are also included for: (1) two processes for preparing (I); (2) combination of a compound (I) and an anticancer agent selected from genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors and kinase inhibitors. [Image] ACTIVITY : Cytostatic. N-((4aR)-3-(4'-chloro-2-biphenylylmethyl)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolin-8-ylcarbonyl)-4-((1R)-3-dimethylamino-1-(phenylthiomethyl)propylamino)-3-nitrobenzenesulfonamide dihydrochloride had an IC50 of 0.305 mu M against H146 tumore cells. MECHANISM OF ACTION : Apoptosis promoter; Caspase 3 promoter.

    NOVEL AZABICYCLIC DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    36.
    发明专利
    NOVEL AZABICYCLIC DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 未知

    公开(公告)号：HRP20080184T5

    公开(公告)日：2008-10-31

    申请号：HRP20080184

    申请日：2008-04-22

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  BERT LIONEL ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: A61K31/403 ,  A61P25/00 ,  C07D209/52 ,  C07D403/12

    Abstract: Azabicyclic derivatives (I) are new. Azabicyclic derivatives of formula (I) and their enantiomers, diastereoisomers or acid or base addition salts are new. ALK : alkylene, 2-6C alkenylene (contains 1-3 double bonds) or 2-6C alkynylene (contains 1-3 triple bonds); Y, Y 1> : H, halo, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, SH, OH, perhaloalkyl, nitro, amino (optionally substituted by one or two alkyl), acyl of formula C(O)R1a, aminocarbonyl (optionally N-substituted by one or two alkyl), acylamino (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; R1a : H or alkyl; X : O, S or NR; R : H or alkyl; W 1> : CN (only when X = O or NR), N(R 1>)Z 1>R 2>or Z 1>NR 1>R 2>; Z 1> : C(O), C(S), C(NR 4>), C(O)N(R 3>), C(S)N(R 3>), C(NR 4>)N(R 3>), C(O)O, C(S)O or S(O) r; r : 1 or 2; Z 2> : C(O), C(S), C(NR 4>), S(O) ror bond; R 1>-R 4> : alkyl, 3-6C alkenyl (contains 1-3 double bonds), 3-6C alkynyl (contains 1-3 triple bonds), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted), alkoxy or H; or R 1>+R 2>or R 2>+R 3> : heterocyclyl or heteroaryl (both optionally substituted); m, n : 0-2, where the sum of m+n is 2 or 3; and p, q : 0-2. alkyl = 1-6C unless specified; perhaloalkyl = 1-3C with 1-7 halogen; aryl = phenyl, naphthyl, indanyl, indenyl, dihydronaphthyl or tetrahydronaphthyl; cycloalkyl = 3-11 membered mono- or bi-cyclic ring system, optionally with 1 or 2 unsaturations; heterocyclyl = 4-11 membered mono- or bicyclic ring system optionally with 1 or 2 unsaturations and/or 1-4 heteroatoms from N, O and/or S; heteroaryl = 5-11 membered mono- or bicyclic ring system with 1-4 heteroatoms from N, O and/or S; for cycloalkyl, aryl, heteroaryl or heterocyclyl, 'optionally substituted' comprises 1-3 substituents from alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halogen, OH, SH, perhaloalkyl, nitro, amino or aminocarbonyl (optionally substituted by 1 or 2 alkyl), C(O)R1a, NHC(O)R1a (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; or aryl, heteroaryl, cycloalkyl, heterocyclyl or benzyl with one or two optional oxo substituents where possible; for alkyl, alkenyl or alkynyl, 'optionally substituted ' comprises one or two of alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxy, halogen, OH, SH, nitro, amino, C(O)R1a, aminocarbonyl, NHC(O)R1a, alkoxycarbonyl, COOH, sulfo, CN or aryl, heteroaryl, cycloalkyl, heterocylyl or aryloxy (all optionally substituted). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic. MECHANISM OF ACTION : Histamine (H3) activator. The ability of (I) to activate histamine was tested in mice. The results showed that 4-(3-hexahydrocyclopenta[c]-pyrrol-2(1H)-ylpropoxy)benzonitrile oxalate exhibited the percentage increase of N-methylhistamine in brain of 92%.

    NEW TRICYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    37.
    发明专利
    NEW TRICYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：SG144892A1

    公开(公告)日：2008-08-28

    申请号：SG2008008963

    申请日：2008-01-31

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  DIGUARHER THIERRY LE ,  GENESTE OLIVIER ,  HICKMAN JOHN

    Abstract: Tricyclic diazacycloalkane derivatives (I) are new. Tricyclic diazacycloalkane derivatives of formula (I) are new. A : a 5- to 7-membered ring with 0-2 heteroatoms (O, S, N, NR), where one member can be C=O; R : 1-6C alkyl; n, n' : 0-2, provided that n+n'= 1-3; R 3aryl or heteroaryl; X : 1-6C alkylene, mono- or dioxaalkylene, cycloalkylene, arylene, heteroarylene or SO 2; R 1, R 2H or Q, provided that one is H and the other is Q; Q : YNHSO 2Ar; Y : CO or CH 2; Ar : R 4-substituted 3-R 5-4 R6-phenyl; R 5H; R 6H, NR 7R' 7 or CH 2NR 7R' 7; R 5+R 6groups forming a 5- or 6-membered ring including N para to to the SO 2 group, optionally containing another N atom and/or a SO 2 group, the ring being substituted with R 7; R 7, R' 7H or 1-6C alkyl substituted with aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, heterocycloalkyl or NR 10R' 10; R 10, R' 10H, 1-6C alkyl, 1-6C alkoxy, aryl or heteroaryl, or R 10+R' 10 forms an optionally oxo-substituted mono- or bicyclic group optionally containing another heteroatom; R 4H, NO 2, R 7, SO 2R 9, R or OR; R 9NH 2 or 1-6C (halo)alkyl. Independent claims are also included for: (1) two processes for preparing (I); (2) combination of a compound (I) and an anticancer agent selected from genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors and kinase inhibitors. [Image] ACTIVITY : Cytostatic. N-((4aR)-3-(4'-chloro-2-biphenylylmethyl)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolin-8-ylcarbonyl)-4-((1R)-3-dimethylamino-1-(phenylthiomethyl)propylamino)-3-nitrobenzenesulfonamide dihydrochloride had an IC50 of 0.305 mu M against H146 tumore cells. MECHANISM OF ACTION : Apoptosis promoter; Caspase 3 promoter.

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