会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 85. 发明专利
    • NO20050572L
    • 2005-08-04
    • NO20050572
    • 2005-02-02
    • SERVIER LAB
    • TILLEQUIN FRANCOISKOCH MICHELPIERRE ALAINRENARD PIERREMICHEL SYLVIEHICKMAN JOHNLEONCE STEPHANEPFEIFFER BRUNO
    • C07D491/147A61K31/4375A61K31/4985A61P35/00C07B61/00C07D491/14C07D491/22
    • Benzo[b]chromeno[g]naphthyridone or pyrano[2',3':7,8]quinolino[2,3-b]quinoxalinone derivatives (I) are new. Benzo[b]chromeno[g]naphthyridone or pyrano[2',3':7,8]quinolino[2,3-b]quinoxalinone derivatives of formula (I) and their isomers, N-oxides and salts are new: B 1, B 2C or N, at least one being N; X, Y : H, halo, OH, 1-6C alkoxy, NO 2, CN, 1-6C alkyl, 2-6C alkenyl, 1-6C polyhaloalkyl or NR aR b; R a, R bH, COCF 3, CONH 2 or 1-6C alkyl optionally substituted with NR' aR' b or NR aR b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); R' a, R' bH or 1-6C alkyl, or NR' aR' b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); X 1, Y 1X and Y or are absent when B 1, B 2 is N; R 1H or 1-6C alkyl; R 2H, 1-6C alkyl, OR" a, NR' aR' b, OT aOR" a, NR" aT aNR' aR' b, NR" aCOT aH, OCOT aH, OT aNR' aR' b, NR" aT aOR" a, NR" aT aCOOR" a or NR" aCOT aNR' aR' b; T a1-6C alkylene; R" aH or 1-6C alkyl; R 3, R 4H or 1-6C alkyl or together form a 3- to 6-membered ring; A : CHR 5CHR 6, CH=CR 7, CR 7=CH, COCHR 8 or CHR 8CO; R 5, R 6H, OR c, NR cR d, SR c, W 1C(W 2)U'V', W 1C(W 2)W 3T 1, W 1SO nW 3T 1, W 1SO nT 1 or C(W 2)T 1, or together form OC(Z)O, NHC(Z)O, OC(Z)NH, NHC(Z)NH, O(CH 2) mO, OCOB'COO, NHCOB'COO or OCOB'CONH, or CR 5R 6 is an oxirane or optionally N-substituted aziridine group; R c, R dH, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COR e; R eH, aryl or NR"' aR"' b; R"' a, R"' bH or NR"' aR"' b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); W 1O, S or NR c; W 2O or S; U' : 1-8C alkylene or 2-8C alkenylene, or is a bond when W 2 is not O and V' is not H, aryl or NH 2; V' : H, aryl, OR c, COOR c, COR c, CONR' aR' b, NR cR d, N(R c)COOR' c or N(R c)COR' c; R' c1-6C alkyl, aryl or aryl(1-6C)alkyl; W 3O, S or NR c; T 1H, 1-6C alkyl, 2-6C alkenyl, aryl, aryl(1-6C)alkyl, or 1-6C alkyl or 2-6C alkenyl substituted with OR c or NR' aR' b; n : 1 or 2; Z : O or S; m : 1-4; B' : bond, 1-6C alkylene or 2-6C alkenylene; R 7H, OR" a, W 1C(W 2)U'V', W 1C(W 2)W 3T 1, W 1SO nW 3T 1, W 1SO nT 1 or C(W 2)T 1; and R 8H, 2-7C alkanoyloxy or OR" a. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Cytostatic. cis-1,2-Acetoxy-6-methoxy-3,3,14-trimethyl-1,2,3,14-tetrahydro-7H-benzo[b]chromeno[6,5-g][1,8]naphthyridin-7-one had IC50 values of 0.32 mu M against L1210 murine leukemia cells and 0.037 mu M against KB-3-1 human epidermoid carcinoma cells. MECHANISM OF ACTION : Cell cycle blocker.
    • 87. 发明专利
    • BRPI0402500A
    • 2005-06-14
    • BRPI0402500
    • 2004-06-23
    • SERVIER LAB
    • KOCH MICHELTILLEQUIN FRANCOISMICHEL SYLVIEHICKMAN JOHNPIERRE ALAINLEONCE STEPHANEPFEIFFER BRUNORENARD PIERRE
    • C07D491/048A61K31/4741A61P35/00C07D491/04C07D491/052C07D491/14C07D491/153C07D491/056C07D491/147A61K31/4748A61P35/04
    • 1,2,3,14-Tetrahydro- or 3,14-dihydro-7H-benzo-(a)-pyrano-(3,2-h)-acridin-7-one derivatives (I) are new. Pentacyclic acridone derivatives of formula (I) and their enantiomers, diastereomers, N-oxides and acid or base addition salts are new. [Image] X, Y : H, halo, OH, alkoxy, NO 2, CN, alkyl, 2-6C alkenyl, polyhaloalkyl or NR aR b; R a, R bH, COCF 3, CONH 2 or alkyl (optionally substituted (os) by NR' aR' b); or NR aR b = Het; R' a, R' bH, alkyl or aralkyl; or NR' aR' bHet; R 1H or alkyl; R 2H, alkyl, OR'' a, NR' aR' b, -O-T a-OR'' a, -NR'' a-T a-NR' aR' b, -NR'' a-CO-Ta-H, -O-CO-T a-H, -O-T a-NR' aR' b, -NR'' a-T a-OR'' a, -NR'' a-T a-COOR'' a or -NR'' a-CO-T a-NR' aR' b; T a1-6C alkylene; R'' aH or alkyl; R 3, R 4H or alkyl; or CR 3R 43-6 membered monocyclic ring (e.g. cycloalkyl); A : -CHR 5-CHR 6-, -CH=C(R 7)-, -C(R 7)=CH-, -CO-CH(R 8)- or -CH(R 8)-CO-; R 5, R 6H, OR c, NR cR d, SR c, -W 1-C(W 2)-U-V, -W 1-C(W 2)-W 3-T 1, -W 1-S(O) n-W 3-T 1, -W 1-S(O) n-U'-V' or -C(W 2)-T 1; or R 5 + R 6-O-C(Z)-O-, -NH-C(Z)-O-, -O-C(Z)-NH-, -NH-C(Z)-NH-, -O-(CH 2) m-O-, -O-C(O)-B-CO-O-, -NH-C(O)-B-CO-O-, -O-C(O)-B-CO-NH-, O, NH or N(alkyl); R c, R dH, alkyl, aryl, aralkyl or -CO-R e; R eH, aryl or NR''' aR''' b; R''' a, R''' bH or alkyl; or NR''' aR''' bHet; W 1O, S or NR c; W 2, Z : O or S; U : 1-8C alkylene or 2-8C alkenylene; or may also be a direct bond if W 2 is S and V is other than H, aryl or NH 2; V : H, aryl, OR c, COOR c, CONR' aR' b, NR' aR' b, N(R c)COOR' c or N(R c)COR' c; R' cH, alkyl, aryl or aralkyl; W 3O, S or NR c; T 1H, aryl or aralkyl; or alkyl or 2-6C alkenyl (both os by OR c or NR' aR' b); n : 1 or 2; U' : 1-8C alkylene or 2-8C alkenylene; V : H, aryl, OR c, COOR c, COR c, CONR' aR' b, NR' aR' b, N(R c)COOR' c or N(R c)COR' c; m : 1-4; B : direct bond, 1-6C alkylene or 2-6C alkenylene; R 7H, OR'' a, -W 1-C(W 2)-U-V, -W 1-C(W 2)-W 3-T 1, -W 1-S(O) n-W 3-T 1, -W 1-S(O) n-U'-V' or -C(W 2)-T 1; R 8H, alkylcarbonyloxy or OR'' a; aryl moieties : phenyl or naphthyl (both os by one or more of OH, halo, COOH, NO 2, NH 2, mono- or dialkylamino, aloxy, 1-6C acyl and/or alkylcarbonyloxy); Het : 5-7 membered monocyclic heterocycle (optionally containing a second O or N heteroatom), e.g. pyrrolidinyl, isoxazolidinyl, oxazolidinyl, pyrazolidinyl, imidazolidinyl, piperidinyl, oxazinanyl, morphol;inyl, hexahydropyridazinyl, hexahydropyrimidinyl, piperazinyl, azepanyl, oxazepanyl or diazepanyl; alkyl moieties have 1-6C unless specified otherwise. Independent claims are included for the preparation of (I). ACTIVITY : Cytostatic. In tests in mice with transplanted C38 colon adenocarcinoma, ()-cis-1,2-diacetoxy-6-methoxy-3,3,14-trimethyl-1,2,3,14-tetrahydro-7H-benzo-(a)-pyrano-(3,2-h)-acridin-7-one (Ia) at the optimum dose of 4 mg/kg i.v. (administered twice on days 12 and 22) inhibited tumor growth by 95% (T/C = 5%). For comparison, acronycin at the optimum dose of 100 mg/kg gave a T/C value of 27%. MECHANISM OF ACTION : Specific cell cycle blocker.
    • 90. 发明专利
    • NO20050572D0
    • 2005-02-02
    • NO20050572
    • 2005-02-02
    • SERVIER LAB
    • TILLEQUIN FRANCOISKOCH MICHELPIERRE ALAINRENARD PIERREMICHEL SYLVIEHICKMAN JOHNLEONCE STEPHANEPFEIFFER BRUNO
    • C07D491/147A61K31/4375A61K31/4985A61P35/00C07B61/00C07D491/14C07D491/22C07D
    • Benzo[b]chromeno[g]naphthyridone or pyrano[2',3':7,8]quinolino[2,3-b]quinoxalinone derivatives (I) are new. Benzo[b]chromeno[g]naphthyridone or pyrano[2',3':7,8]quinolino[2,3-b]quinoxalinone derivatives of formula (I) and their isomers, N-oxides and salts are new: B 1, B 2C or N, at least one being N; X, Y : H, halo, OH, 1-6C alkoxy, NO 2, CN, 1-6C alkyl, 2-6C alkenyl, 1-6C polyhaloalkyl or NR aR b; R a, R bH, COCF 3, CONH 2 or 1-6C alkyl optionally substituted with NR' aR' b or NR aR b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); R' a, R' bH or 1-6C alkyl, or NR' aR' b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); X 1, Y 1X and Y or are absent when B 1, B 2 is N; R 1H or 1-6C alkyl; R 2H, 1-6C alkyl, OR" a, NR' aR' b, OT aOR" a, NR" aT aNR' aR' b, NR" aCOT aH, OCOT aH, OT aNR' aR' b, NR" aT aOR" a, NR" aT aCOOR" a or NR" aCOT aNR' aR' b; T a1-6C alkylene; R" aH or 1-6C alkyl; R 3, R 4H or 1-6C alkyl or together form a 3- to 6-membered ring; A : CHR 5CHR 6, CH=CR 7, CR 7=CH, COCHR 8 or CHR 8CO; R 5, R 6H, OR c, NR cR d, SR c, W 1C(W 2)U'V', W 1C(W 2)W 3T 1, W 1SO nW 3T 1, W 1SO nT 1 or C(W 2)T 1, or together form OC(Z)O, NHC(Z)O, OC(Z)NH, NHC(Z)NH, O(CH 2) mO, OCOB'COO, NHCOB'COO or OCOB'CONH, or CR 5R 6 is an oxirane or optionally N-substituted aziridine group; R c, R dH, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COR e; R eH, aryl or NR"' aR"' b; R"' a, R"' bH or NR"' aR"' b is a 5- to 7-membered ring optionally containing another heteroatom (O or N); W 1O, S or NR c; W 2O or S; U' : 1-8C alkylene or 2-8C alkenylene, or is a bond when W 2 is not O and V' is not H, aryl or NH 2; V' : H, aryl, OR c, COOR c, COR c, CONR' aR' b, NR cR d, N(R c)COOR' c or N(R c)COR' c; R' c1-6C alkyl, aryl or aryl(1-6C)alkyl; W 3O, S or NR c; T 1H, 1-6C alkyl, 2-6C alkenyl, aryl, aryl(1-6C)alkyl, or 1-6C alkyl or 2-6C alkenyl substituted with OR c or NR' aR' b; n : 1 or 2; Z : O or S; m : 1-4; B' : bond, 1-6C alkylene or 2-6C alkenylene; R 7H, OR" a, W 1C(W 2)U'V', W 1C(W 2)W 3T 1, W 1SO nW 3T 1, W 1SO nT 1 or C(W 2)T 1; and R 8H, 2-7C alkanoyloxy or OR" a. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Cytostatic. cis-1,2-Acetoxy-6-methoxy-3,3,14-trimethyl-1,2,3,14-tetrahydro-7H-benzo[b]chromeno[6,5-g][1,8]naphthyridin-7-one had IC50 values of 0.32 mu M against L1210 murine leukemia cells and 0.037 mu M against KB-3-1 human epidermoid carcinoma cells. MECHANISM OF ACTION : Cell cycle blocker.