中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

914 records (took 0.028 seconds)

    81.
    发明专利
    未知

    公开(公告)号：DK1413579T3

    公开(公告)日：2005-05-09

    申请号：DK03292634

    申请日：2003-10-22

    Applicant: SERVIER LAB

    Inventor： KOPP MARINA ,  LANCELOT JEAN-CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL-HENRI ,  BIZOT-ESPIARD JEAN-GUY ,  RAULT SYLVAIN ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    Heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them.
    86.
    发明专利
    Heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them. 未知

    公开(公告)号：ZA200405893B

    公开(公告)日：2005-01-24

    申请号：ZA200405893

    申请日：2004-07-23

    Applicant: SERVIER LAB

    Inventor： LECLERC VERONIQUE ,  PAILLOUX SYLVIE ,  CARATO PASCAL ,  INTROVIGNE CARINE ,  LEBEGUE NICOLAS ,  BERTHELOT PASCAL ,  DACQUET CATHERINE ,  BOUTIN JEAN ALBERT ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

    IPC: C07D235/26 ,  A61K31/426 ,  A61K31/427 ,  A61P1/04 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/04 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/04 ,  A61P25/28 ,  A61P27/02 ,  A61P35/00 ,  C07D235/12 ,  C07D277/68 ,  C07D417/10 ,  C07D417/12 ,  A61K ,  A61P ,  C07D

    Abstract: Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

    88.
    发明专利
    未知

    公开(公告)号：NO20050214L

    公开(公告)日：2005-01-13

    申请号：NO20050214

    申请日：2005-01-13

    Applicant: SERVIER LAB

    Inventor： RENARD PIERRE ,  LESTAGE PIERRE ,  CAIGNARD DANIEL-HENRI ,  TANG XI-CAN ,  QIN GUO-WEI

    IPC: A61K31/47 ,  A61P25/28 ,  C07D209/96 ,  C07D217/20

    Abstract: The invention relates to acutumine and compounds thereof and also to compounds of formula (I): wherein R 1 and R 2 each represent hydrogen or together form an additional bond, R 3 represents hydrogen or alkoxy, R 5 represents hydrogen or chlorine, R 6 represents hydrogen or alkyl, alkylcarbonyl or aroyl, R 7 and R 10 each represent alkoxy, R 10 represents alkoxy, R 4 , R 8 , R 9 , R 11 , R 12 , R 13 and R 14 are as defined in the description. and medicinal products containing the same which are useful in treating deficiencies of memory.

    New benzo(a)pyrano(3,2-h)acridin-7-one compounds, a process for their preparation and pharmaceutical compositions containing them
    89.
    发明专利
    New benzo(a)pyrano(3,2-h)acridin-7-one compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2004202864A1

    公开(公告)日：2005-01-13

    申请号：AU2004202864

    申请日：2004-06-25

    Applicant: SERVIER LAB

    Inventor： RENARD PIERRE ,  PFEIFFER BRUNO ,  LEONCE STEPHANE ,  PIERRE ALAIN ,  HICKMAN JOHN ,  MICHEL SYLVIE ,  TILLEQUIN FRANCOIS ,  KOCH MICHEL

    IPC: C07D491/048 ,  A61K31/4741 ,  A61P35/00 ,  C07D491/04 ,  C07D491/052 ,  C07D491/14 ,  C07D491/153 ,  C07D491/02 ,  A61K31/473 ,  C07D498/12 ,  C07D491/12

    Abstract: 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
    未知

    公开(公告)号：FR2856687A1

    公开(公告)日：2004-12-31

    申请号：FR0307664

    申请日：2003-06-25

    Applicant: SERVIER LAB

    Inventor： KOCH MICHEL ,  TILLEQUIN FRANCOIS ,  MICHEL SYLVIE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE ,  PFEIFFER BRUNO ,  RENARD PIERRE

    IPC: C07D491/048 ,  A61K31/4741 ,  A61P35/00 ,  C07D491/04 ,  C07D491/052 ,  C07D491/14 ,  C07D491/153 ,  A61K31/4738

    Abstract: 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.

Patent Agency Ranking