中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

244 records (took 0.025 seconds)

    NUEVOS DERIVADOS TRICICLICOS SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    34.
    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

    35.
    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.

    37.
    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.

    Cycloheptene derivatives and pharmaceuticals thereof
    38.
    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.

Patent Agency Ranking