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    143.
    发明专利
    未知

    公开(公告)号：DK1140935T3

    公开(公告)日：2003-09-01

    申请号：DK99969220

    申请日：1999-12-17

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

    IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  C07D201/00

    Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X 1 -X 2 -X 3 - is a trivalent radical,; >Y 1 -Y 2 - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R 1 and R 2 are independently hydroxy, halo, cyano, C 1-6 alkyl, trihalomethyl, trihalomethoxy, C 2-6 alkenyl, C 1-6 alkyloxy, hydroxyC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkyloxyC 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, aminoC 1-6 alkyloxy, mono- or di(C 1-6 alkyl)amino, mono- or di(C 1-6 alkylaminoC 1-6 alkyloxy, aryl, arylC 1-6 alkyl, aryloxy or arylC 1-6 alkyloxy, hydroxycarbonyl, C 1-6 alkyloxycarbonyl; or two R 1 or R 2 on adjacent positions form together a bivalent radical; R 3 is hydrogen, halo, C 1-6 alkyl, cyano, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, cyanoC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, aminocarbonylC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl, C 1-6 alkyoxycarbonylC 1-6 alkyl, C 1-6 alkylcarbonylC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aryl, arylC 1-6 alkyloxyC 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyl, or a radical of formula -O-R 10 , -S-R 10 or -NR 11 R 12 ; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    INDAZOLILPIRROLOTRIAZINAS C-5 MODIFICADAS
    144.
    发明专利
    INDAZOLILPIRROLOTRIAZINAS C-5 MODIFICADAS 未知

    公开(公告)号：PE20030712A1

    公开(公告)日：2003-08-21

    申请号：PE2002001102

    申请日：2002-11-14

    Applicant: SQUIBB BRISTOL MYERS CO

    Inventor： MASTALERZ HAROLD ,  TARRANT JAMES G ,  VITE GREGORY D ,  ZHANG GUIFEN

    IPC: A61K31/53 ,  A61K31/5377 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D201/00 ,  C07D487/04

    Abstract: SE REFIERE A DERIVADOS DE INDAZOLILPIRROLOTRIAZINAS C-5 MODIFICADAS, DE FORMULA I SUS ENANTIOMEROS, DIASTEREOMEROS, SALES DONDE R ES SR2, SOR2, OR2, NR3R4; R1 ES ARILO, HETEROCICLO, ENTRE OTROS; R2 ES H, ALQUILO, ARILO, ARALQUILO, HETEROCICLO; R3 Y R4 SON H, ALQUILO, ARILO, HETEROCICLO; R2 Y R3 JUNTOS FORMAN UN ANILLO CARBOCICLO, HETEROCICLO. SON COMPUESTOS PREFERIDOS (5-[1,4]DIAZEPAN-1-ILMETIL-PIRROLO[2,1-f][1,2,4]TRIAZIN-4-IL)-[1-(3-FLUOR-BENCIL)-1H-INDAZOL-5-IL]-AMINA, [1-(3-FLUOR-BENCIL)-1H-INDAZOL-5-IL]-(5-IMIDAZOL-1-ILMETIL-PIRROLO[2,1-f][1,2,4]TRIAZIN-5-ILMETIL}-PIPERIDIN-3-CARBOXILICO, AMIDA DEL ACIDO 1-{4-[1-(3-FLUORO-BENCIL)-1H-INDAZOL-5-ILAMINO]-PIRROLO[2,1-f][1,2,4]TRIAZIN-5-ILMETIL}-PIPERIDIN-3-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS MENCIONADOS INHIBEN LA ACTIVIDAD DE LA TIROSINA CINASA DE LOS RECEPTORES DEL FACTOR DE CRECIMIENTO TALES COMO HER1, HER2, HER4 Y SON UTILES COMO AGENTES ANTIPROLIFERATIVOS

    New 5-thiol-4-pyridylcarbonyl-cyclohexene-dione derivatives, useful as herbicides and plant growth inhibitors, with improved leaching properties and selectivity
    146.
    发明专利
    New 5-thiol-4-pyridylcarbonyl-cyclohexene-dione derivatives, useful as herbicides and plant growth inhibitors, with improved leaching properties and selectivity 未知

    公开(公告)号：DE10256354A1

    公开(公告)日：2003-06-18

    申请号：DE10256354

    申请日：2002-12-03

    Applicant: SYNGENTA PARTICIPATIONS AG

    Inventor： EDMUNDS ANDREW ,  SCHAETZER JUERGEN ,  LUETHY CHRISTOPH ,  DIGGELMANN MARTIN

    IPC: A01N43/40 ,  C07D213/50 ,  C07D213/57 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D201/00

    Abstract: 5-substituted thiol-4-(pyridinylcarbonyl)-cyclohexene-1,3-dione derivatives (I) and their salts, all isomers and tautomers are new. 5-substituted thiol- 4-(pyridinylcarbonyl)-cyclohexene-1,3-dione derivatives of formula (I) and their salts, all isomers and tautomers are new. R = 1-12C alkyl, 2-12C alkenyl or alkynyl, 3-12C allenyl, 3-12C cycloalkyl, 5-12C cycloalkenyl, R1-(1-12C alkylene or 2-12C alkenylene) (where alkylene and alkenylene may be interrupted by oxygen, S(O)p, or CO and substituted by one or more R2, or phenyl (optionally substituted 1-5 times by R11)), 3-12 membered aromatic or partially or fully saturated mono- or bi-cyclic ring system, (optionally containing 1-5 heteroatoms (nitrogen, oxygen and/or sulfur)) or 1-2 carbonyl (optionally substituted by one or more R3), with the ring system attached, via C or N atoms, directly or through a 1-6C alkylene or alkenylene linker (optionally interrupted by O or S(O)p and/or substituted by R4) to the S of S(O)nR, and substituents on N are other than halo, or halo, 1-12C alkylthio, cyano, C(X1)R6, C(X2)X3R7, C(X4)NR8R9, or, if n = 0, also hydrogen, cyano or isocyano or hydroxy, or NR80R90 when n = 1 or 2; Z1 = 1-3C alkyl; Y = hydrogen, chloro, bromo or 1-2C (halo)alkyl; n and p = 0-2; q = 0 or 1; and X1-X4 = oxygen or sulfur; The full definitions are given in the DEFINITIONS (Full Definitions) Field. An Independent claim is also included for the preparation of (I).

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