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    101.
    发明专利
    未知

    公开(公告)号：AT271558T

    公开(公告)日：2004-08-15

    申请号：AT00402985

    申请日：2000-10-27

    Applicant: SERVIER LAB

    Inventor： MONNERET CLAUDE ,  BERTOUNESQUE EMMANUEL ,  MERESSE PHILIPPE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE

    IPC: C07D493/06 ,  A61K31/357 ,  A61K31/36 ,  A61K31/365 ,  A61K31/70 ,  A61P35/00 ,  C07B61/00 ,  C07D493/04 ,  C07D519/00 ,  C07H17/04

    Abstract: 9-(3,5-Dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro (3',4':6,7)-naphtho(2,3-d)(1,3)-dioxol-6(5aH)-one derivatives (I) are new. Podophyllotoxin derivatives of formula (I) and their isomers and acid or base addition salts are new. R = -A-G or a bicyclic group of formula (a); X,Y = H, OH, alkoxy, NH2 or mono- or di-alkylamino; W = H, alkyl, aryl or heteroaryl; A = a direct bond or optionally unsaturated 1-6C alkylene (optionally substituted (os) by one or more of halo and OH); G = H, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, OR2, -O-T1-NR3R4, -O-T1-NR2-T1'-NR3R4, NR3R4, -NR2-T1-NR3R4, -NR2-T1-OR5, -NR2-T1-COOR6, -NR2-T1-COR6, -CONR3R4, -CO-NR2-T2, -O-CO-NR2-T2, -O-CS-NR2-T2, -NR2-CO-T2, -NR2-CS-T2, -OCOOT2, -OCONR2-T2, -OC(S)OT2, -OC(S)NR2-T2, -NR2-COOT2, -NR2-CO-NR6-T2, -NR2-C(S)OT2, -NR2-CS-NR6-T2 or -NR2-SO2T3; R2 = H, alkyl, aryl or arylalkyl; T1, T1' = 1-6C alkylene; R3, R4 = H, alkyl (os by one or more OH), aryl, arylalkyl, cycloalkyl, heteroarylalkyl, heteroaryl, heterocycloalkyl or heterocycloalkylalkyl, or NR3R4 = 5-7 membered heterocyclyl, optionally containing a second O or N heterocyclyl and os by one or more of halo, OH, alkyl and heterocyclyl; R5 = alkyl, aryl or arylalkyl; T2 = H, alkyl (os by one or more halo), aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or 1-6C alkylene substituted by one or more of NR3R4, OR2, COOR6, NR2COR6, NR2COOR6, COR6, CONR3R4, -NR2-T1-NR3R4, -NR2-T1-OR6 or -O-T1-NR3R4; T3 = 1-20C alkyl (os by one or more of halo, OR2, NR2R6, NO2, CN or N3), aryl, arylalkyl, cycloalkyl, cycloalkylakyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl or heteroarylalkyl; R1 = H, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, heterocycloalkylcarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylasulfonyl, phosphono, alkoxycarbonyl, aryloxycarbonyl or arylalkoxycarbonyl; aryl moieties = phenyl, biphenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all os by one or more of halo, OH, alkyl, alkoxy, CN, NO2, NH2, mono- or dialkylamino, alkylsulfonyl, alkylsulfonylamino, COOH, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, hydroxyalkyl, trihaloalkyl, OCH2O, OCH2CH2O, morpholinyl, piperidyl, piperazinyl, alkylcarbonyloxy or alkylcarbonyl); heteroaryl moieties = 5-12 membered mono- or bi-cyclic aromatic system (where one ring of a bicyclic system is optionally partially hydrogenated), containing 1-3 of O, N and S as heteroatom(s) and os as for aryl; cycloalkyl moieties = 3-10C mono- or bi-cyclic saturated or unsaturated (but not aromatic) system (os by one or more of halo, alkyl, trihaloalkyl, OH, hydroxyalkyl, NH2, mono- or dialkylamino, piperidyl, piperazinyl and morpholinyl), and heterocycloalkyl moieties = as for cycloalkyl but containing 1 or 2 of O, N and S as heteroatom(s); provided that R1 is not Me if R is H; alkyl moieties have 1-6C unless specified otherwise. Independent claims are included for the following: (i) new intermediates (A), having formula as for (I) but with R replaced by N3, Cl, Br or -A1-CHO (A1 = 1-5C alkylene); and (ii) preparation of (I).

    103.
    发明专利
    未知

    公开(公告)号：BR0304575A

    公开(公告)日：2004-07-20

    申请号：BR0304575

    申请日：2003-10-15

    Applicant: SERVIER LAB

    Inventor： PRUDHOMME MICHELLE ,  HUGON BERNADETTE ,  ANIZON FABRICE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  GOLSTEYN ROY ,  RENARD PIERRE ,  PFEIFFER BRUNO

    IPC: A61K31/40 ,  A61K31/407 ,  A61K31/437 ,  A61K31/7056 ,  A61K31/706 ,  A61P35/00 ,  A61P43/00 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07H19/23 ,  C07D487/22 ,  C07D407/04

    Abstract: (3,4-a:3,4-c) Carbazole derivatives (I), their enantiomers, diastereoisomers and salts with acids and bases. (3,4-a:3,4-c) Carbazole derivatives of formula (I), their enantiomers, diastereoisomers and salts with acids and bases A = ring that is saturated, partially, or fully unsaturated, and that may be aromatic; W' = phenyl or pyridinyl; Z' = U'-V', methylene dioxy or ethylenedioxy; U' = bond, 1-6C alkylene, 2-6C alkenylene, optionally substituted by 1 or 2 halo or OH groups; V' = H, halo, CN, NO2, azido, 1-6C alkyl or alkoxy, aryl, aralkyl, OH, aryloxy, arylalkoxy, formyl, COOH, NH2CO, NR3R4, -C(O)-T1, -C(O)-NR3-T1, NR3C(O)T1, -O-C(O)-T1, -C(O)-OT1, -NR3-T2-NR3R4, -NR3-T2-OR3, -NR3-T2-COOR3, -O-T'2-NR3R4, -O-T'2-OR3, -O-T'2-COOR3, or -S(O)t-R3; R3, R4 = H, 1-6C alkyl, aryl, aralkyl or together form 5-10 membered saturated mono or bicyclic heterocycle, optionally with a second hetero atom (O or N) and optionally substituted by alkyl, aryl, aralkyl, OH, alkoxy, amino mono- or dialkylamino; T1 = alkyl (optionally substituted by -OR3, -NR3R4, -COOR3, -C(O)R3, or -C(O)NR3R4), 2-6C alkenyl, optionally substituted; T2 = 1-6C alkylene; T'2 = 1-6C alkylene optionally substituted by one or more OH groups; t = 0, 1, or 2; Q1 = O or NR2; R2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; Q2 = O or NR'2; R'2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; X1 = H, OH, alkoxy, mercapto, alkylthio; Y1 = H or X1 and Y1 together form carbonyl or thiocarbonyl; X2 = H, OH, alkoxy, mercapto, alkylthio; Y2 = H or X2 and Y2 together form carbonyl or thiocarbonyl; X'1 = H, OH, alkoxy, mercapto, alkylthio; Y'1 = H or X'1 and Y'1 together form carbonyl or thiocarbonyl; X'2 = H, OH, alkoxy, mercapto, alkylthio; Y'2 = H or X'2 and Y'2 together form carbonyl or thiocarbonyl; R1 = H, 1-6C alkyl (optionally substituted by one or more OH, alkoxy, hydroxyalkoxy, or NR3R4 groups) or it is a group of formula (a); Ra - Rd = a bond, H, halo, OH, alkoxy, aryloxy, arylalkoxy, alkyl, aralkyl, aryl, -NR3R4, azido, -N=NR3, or -O-C(O)-R5; R5 = alkyl optionally substituted by one or more halo, OH, amino, mono- or dialkylamino, aryl, aralkyl, cycloalkyl, or heterocycloalkyl; Re = methylene or -U1-Ra; U1 = a bond or methylene; and n = 0 or 1. with the proviso that the following compounds are not within the scope of (I): 3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 5-ethyl-3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 3b, 6a, 7, 11c-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; and 3b, 6a, 6b, 7-tetrahydrofuro(3,4a)pyrrolo(3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone.

    SUBSTITUTED BENZOL(E) (1,4) OXAZINO(3,2-G) ISOINDOLE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    108.
    发明专利
    SUBSTITUTED BENZOL(E) (1,4) OXAZINO(3,2-G) ISOINDOLE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 未知

    公开(公告)号：AU2003301531A1

    公开(公告)日：2004-05-13

    申请号：AU2003301531

    申请日：2003-10-17

    Applicant: SERVIER LAB

    Inventor： LEPIFRE FRANCK ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  KRAUS-BERTHIER LAURENCE ,  COUDERT GERARD

    IPC: A61P35/00 ,  C07D497/04 ,  C07D497/14 ,  C07D498/04 ,  A61K31/535 ,  C07D498/14 ,  C07D265/38

    Abstract: Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives of formula (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new W1 = atoms that complete phenyl or pyridyl; Z = hydrogen, halo, 1-6C alkyl or alkoxy (both optionally substituted by aryl), aryl, aryloxy or hydroxy; R1 = hydrogen, 1-6C alkyl, optionally substituted by aryl, aryl, COR5 or 1-6C alkylene, substituted by one or more of halo, cyano, OR6, NR6R7, COOR6, COR6 or CONHR6; R2 = hydrogen or -CH2CH2OR8; R3 and R4 = hydrogen, 1-6C alkyl, optionally substituted by aryl, or aryl, or together they complete a 5 or 6-membered, monocyclic heterocycle, optionally including an additional oxygen or nitrogen; n = 1-6; R5 = hydrogen, 1-6C alkyl or alkoxy, hydroxy, aryl, aryl(1-6C)alkyl or aryloxy; R6 and R7 = hydrogen, 1-6C alkyl, aryl(1-6C)alkyl or aryl, or together they complete a heterocycle as above; R8 = hydrogen, 1-6C alkyl, aryl, aryl(1-6C)alkyl, S(O)tR6 or -T1-R9; t = 0-2; T1 = 1-6C alkylene; R9 = halo, cyano, OR6, NR6R7, CHO, COOR6 or CONR6R7; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl, all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy or amino, optionally substituted by 1 or 2 1-6C alkyl. Independent claims are also included for the following:0041658 (1) methods for the preparation of (I); and (2) intermediates of formulae (X), (XI) and (XIV). Boc = tert-butoxycarbonyl; and Pg = Boc or phenoxycarbonyl.

    New dihydroimidazolylaminopyridine derivatives useful in the treatment of diabetes, obesity, insulin resistance and glucose intolerance
    110.
    发明专利
    New dihydroimidazolylaminopyridine derivatives useful in the treatment of diabetes, obesity, insulin resistance and glucose intolerance 未知

    公开(公告)号：FR2846655A1

    公开(公告)日：2004-05-07

    申请号：FR0213801

    申请日：2002-11-05

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN CHARLES ,  LEMAITRE STEPHANE ,  PFEIFFER BRUNO ,  BIZOT ESPIARD JEAN GUY ,  RENARD PIERRE

    IPC: A61P3/04 ,  A61P3/10 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D413/14 ,  A61K31/4439 ,  C07D401/14

    Abstract: 3-Dihydroimidazolyl-2-aminopyridine derivatives (I) their enantiomers, diastereoisomers, tautomers, and salts with acids and bases are new. 3-Dihydroimidazolyl-2-aminopyridine derivatives (I) their enantiomers, diastereoisomers, tautomers, and salts with acids and bases are new; R1, R2 = H, alkyl, cycloalkyl, aryl (optionally substituted), heteroaryl (optionally substituted), or Ra-C(Y)-; NR1R2 = aromatic or non-aromatic heterocycle of 5-8 members including 1-3 heteroatoms (O, N, S)and optionally substituted by 1 or 2 groups selected from halogens, alkyl, polyhaloalkyl, alkoxy, OH, CN, NO2, amino, mono- or di-alkylamino, -COOH, -COO-alkyl, or -CONH2; Ra = H, alkyl, alkoxy, aryl (optionally substituted), or heteroaryl (optionally substituted); Y = O, S, or NRb; Rb = H or alkyl; R3 = H, alkyl, alkoxy, OH, CN, NO2, amino, mono- or di-alkylamino, -COOH, -COO-alkyl, or -CONH2; R4, R5 = H or alkyl; X = O, S, or NRe; Re = H or alkyl. With the proviso that (I) is not 3-(4,5-dihydro-1H-imidazol-2-yl)-2-pyridinamine, 3-(4,5-dihydro-1H-imidazol-2-yl)-N-phenyl-2-pyridinamine, 3-(4,5-dihydro-1H-imidazol-2-yl)-N-methyl-2-pyridinamine, or N-(3-(4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl)-2-pyridinyl)-N-phenylamine. In the above definitions, alkyl and alkoxy groups have 1-6 C atoms, polyhaloalkyl groups have 1-3 C atoms and 1-7 halogen atoms, heteroaryl groups have 5-11 members, are mono- or bicyclic, at least one of which is aromatic, and have 2 or 3 heteroatoms (O, N, S), cycloalkyl groups are mono- or bicyclic with 3-10 C atoms and optionally 1 or 2 unsaturations, and optional substituents on cycloalkyl and heteroaryl groups are 1 or 2 groups selected from halogens, alkyl, alkoxy, polyhaloalkyl, OH, CN, NO2, NH2, alkylamino, dialkylamino, -COOH, -COO-alkyl, -CONH2, and non-aromatic rings on heteroaryl groups may also be substituted by oxo. An Independent claim is also included for the preparation of (I).

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