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    45.
    发明专利
    未知

    公开(公告)号：NO953204L

    公开(公告)日：1996-02-19

    申请号：NO953204

    申请日：1995-08-15

    Applicant: HOECHST AG

    Inventor： KIRSCH REINHARD ,  KLEIM JORG-PETER ,  RIESS GUNTHER ,  ROSNER MANFRED ,  WINKLER IRVIN

    IPC: A61K31/47 ,  A61P31/12 ,  A61P31/18 ,  C07D215/22 ,  C07D215/227 ,  C07D215/24 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D215/58 ,  C07D221/20 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

    Abstract: 4-Methylene-2-quinolones of formula (I) and their tautomers of formula (Ia) and their isomers, salts and prodrugs are new: n = 0-4; R1 = halo, CF3, OCF3, OH, alkyl, cycloalkyl, alkoxy, alkoxyalkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, NO2, NH2, azido, alkylamino, dialkylamino, piperidino, morpholino, pyrrolidino, acyl, acyloxy, acylamino, CONH2, COOH, alkoxycarbonyl, SO3H, SO2NH2, Ar, OAr, COOAr, SAr, SOAr, SO2Ar, SO3Ar, OSO2Ar, SO2NHAr, NHSO2Ar, COAr, Ar', etc.; Ar,Ar' = phenyl and heteroaryl resp., etc.; X = O, S, Se, NR2 or NOR2; R2 = H; alkyl opt. substd. by halogen, CN, NH2, OH, etc.;R5, R6 = COOH or gps. as defined for R2; or R5+R6 forms a 3-8C carbocyclic ring; R3,R4 = alkyl, alkenyl, cycloalkyl or cycloalkenyl,etc.; or R3+R4 = a 3-8C carbocyclic ring; or R3+R4 = CZ1Z2 gp., where Z1 and Z2 are as defined for R3 and R4 as above; provided that X is not O when R1=R2=R5=R6=H and R3=R4=Me or R3+R4= (CH2)4.

    47.
    发明专利
    未知

    公开(公告)号：NO953204D0

    公开(公告)日：1995-08-15

    申请号：NO953204

    申请日：1995-08-15

    Applicant: HOECHST AG

    Inventor： KIRSCH REINHARD ,  KLEIM JORG-PETER ,  RIESS GUNTHER ,  ROSNER MANFRED ,  WINKLER IRVIN

    IPC: A61K31/47 ,  A61P31/12 ,  A61P31/18 ,  C07D215/22 ,  C07D215/227 ,  C07D215/24 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D215/58 ,  C07D221/20 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D

    Abstract: 4-Methylene-2-quinolones of formula (I) and their tautomers of formula (Ia) and their isomers, salts and prodrugs are new: n = 0-4; R1 = halo, CF3, OCF3, OH, alkyl, cycloalkyl, alkoxy, alkoxyalkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, NO2, NH2, azido, alkylamino, dialkylamino, piperidino, morpholino, pyrrolidino, acyl, acyloxy, acylamino, CONH2, COOH, alkoxycarbonyl, SO3H, SO2NH2, Ar, OAr, COOAr, SAr, SOAr, SO2Ar, SO3Ar, OSO2Ar, SO2NHAr, NHSO2Ar, COAr, Ar', etc.; Ar,Ar' = phenyl and heteroaryl resp., etc.; X = O, S, Se, NR2 or NOR2; R2 = H; alkyl opt. substd. by halogen, CN, NH2, OH, etc.;R5, R6 = COOH or gps. as defined for R2; or R5+R6 forms a 3-8C carbocyclic ring; R3,R4 = alkyl, alkenyl, cycloalkyl or cycloalkenyl,etc.; or R3+R4 = a 3-8C carbocyclic ring; or R3+R4 = CZ1Z2 gp., where Z1 and Z2 are as defined for R3 and R4 as above; provided that X is not O when R1=R2=R5=R6=H and R3=R4=Me or R3+R4= (CH2)4.

    3'-derivatized oligonucleotide analogs with nonnucleotidic groupings, their preparation and use
    50.
    发明专利
    3'-derivatized oligonucleotide analogs with nonnucleotidic groupings, their preparation and use 未知

    公开(公告)号：AU657191B2

    公开(公告)日：1995-03-02

    申请号：AU3191193

    申请日：1993-01-21

    Applicant: HOECHST AG

    Inventor： UHLMANN EUGEN ,  PEYMAN ANUSCHIRWAN ,  O'MALLEY GERARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN

    IPC: A61K31/70 ,  A61K31/7125 ,  A61K48/00 ,  A61P31/12 ,  A61P35/00 ,  C07F9/24 ,  C07F9/44 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/68 ,  C07F9/572 ,  C07F9/06 ,  C07F9/576 ,  C07F9/59 ,  C07F9/28 ,  A61K31/73

    Abstract: Oligonucleotide analogs (I) and their physiologically tolerable salts. Oligonucleotide analogs and their physiologically tolerable salts of formula (I) are new. R = H, a substituent or -P(=W)ZZ'; R = H, OH, 1-18C alkoxy, halo, azido or amino; B = nucleotide base residue; A = oxy or methylene; d, e, f = 0-50; i = 1-10; r = 0 or 1; W = oxo, selenoxo or thioxo; V = oxy, sulfandiyl or imino; Y = oxy, sulfandiyl, imino or methylene; Y' = oxy, sulfandiyl, imino, (CH2)m or V(CH2)m; m = 1-18; X = OH or SH; U, R , R = substituents; p = 1-100; q = 0-18; R = H or functional group; Sp = a (3',5'-) spacer group of formula (i); g, g' = 0 or 1; h = 0-10; G = 1-12C alkylene (optionally substituted), (6-14C)aryldi-(1-8C)alkylene, 6-18C arylene, (CH2CH2V) alpha CH2CH2, (CH2V) alpha CH2, -(G-Y-P(=W)(U)-Y'-) beta or a group of formula (ii); alpha = 1-11; beta = 1-6; Z, Z' = OH, (seleno)thio or a substituent; provided that r is 0 when V is Y' and is 1 if i is greater than 1. Positions of R and the adjacent phosphoryl residue can be reversed; each nucleoside had D- or L-configuration and each B has alpha or beta configuration. Independent claims are also included for: (1) a method for producing (I); (2) the phosphitylation reagent of formula DMTr-X'-G'-Y''-P(U')(NR R ); and (3) a pharmaceutical composition containing at least one compound (I) and optionally auxiliary, carrier and/or other active agents. R , R = 1-12C alkyl or together form a 5-6 membered ring; DMTr = dimethoxytrityl; X', Y'' = oxy or sulfandiyl; U' = 1-4C alkyl or protected OH; G' = (CH2CH2O) alpha CH2CH2 or CH2CH(OR')CH2; and R' = 1-18C alkyl, 6-14C aryl or 6-14C aryl(1-8C) alkyl.

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