公开(公告)号：PT822192E

公开(公告)日：2002-03-28

申请号：PT97112940

申请日：1997-07-28

Applicant: HOECHST AG

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  VASELLA ANDREA ,  HOOS ROLAND

IPC: A61K31/35 ,  A61K31/351 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/74 ,  C07D309/28 ,  C07D211/78 ,  C07D309/30 ,  C07D335/02 ,  C07F9/59 ,  C07F9/655 ,  C07F9/6553

Abstract: Trihydroxyheterocyclylamino compounds of formula (I) and their salts are new. Y = COOH, PO3H2, P(O)(OR6)(OH), P(O)R6(OH), tetrazole or SO3H; R6 = 1-4C alkyl; X = NH, O or S; R = H or CONH-C6(R7)5; and R7 = H, OH, halo, COOH, PO3H2 or SO3H.

公开(公告)号：DK0822192T3

公开(公告)日：2002-02-11

申请号：DK97112940

申请日：1997-07-28

Applicant: HOECHST AG

Inventor： HOOS ROLAND ,  CZECH JOERG ,  BOSSLET KLAUS ,  VASELLA ANDREA

IPC: C07D309/28 ,  A61K31/35 ,  A61K31/351 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/74 ,  C07D211/78 ,  C07D309/30 ,  C07D335/02 ,  C07F9/59 ,  C07F9/655 ,  C07F9/6553

Abstract: Trihydroxyheterocyclylamino compounds of formula (I) and their salts are new. Y = COOH, PO3H2, P(O)(OR6)(OH), P(O)R6(OH), tetrazole or SO3H; R6 = 1-4C alkyl; X = NH, O or S; R = H or CONH-C6(R7)5; and R7 = H, OH, halo, COOH, PO3H2 or SO3H.

公开(公告)号：DE59704940D1

公开(公告)日：2001-11-22

申请号：DE59704940

申请日：1997-07-28

Applicant: HOECHST AG

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  VASELLA ANDREA ,  HOOS ROLAND

IPC: C07D309/28 ,  A61K31/35 ,  A61K31/351 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/74 ,  C07D211/78 ,  C07D309/30 ,  C07D335/02 ,  C07F9/59 ,  C07F9/655 ,  C07F9/6553

Abstract: Trihydroxyheterocyclylamino compounds of formula (I) and their salts are new. Y = COOH, PO3H2, P(O)(OR6)(OH), P(O)R6(OH), tetrazole or SO3H; R6 = 1-4C alkyl; X = NH, O or S; R = H or CONH-C6(R7)5; and R7 = H, OH, halo, COOH, PO3H2 or SO3H.

公开(公告)号：ES2147189T3

公开(公告)日：2000-09-01

申请号：ES93115418

申请日：1993-09-24

Applicant: HOECHST AG

Inventor： GEHRMANN MATHIAS ,  SEEMANN GERHARD ,  BOSSLET KLAUS ,  CZECH JOERG

IPC: A01K67/027 ,  A61K38/00 ,  A61P35/00 ,  C07K14/00 ,  C07K14/705 ,  C07K16/00 ,  C07K16/18 ,  C07K19/00 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/00 ,  C12N9/24 ,  C12N15/09 ,  C12N15/62 ,  C12N15/81 ,  C12P21/02 ,  C12R1/865 ,  G01N33/53 ,  G01N33/68

Abstract: The invention relates to compounds which contain an antigen binding region which is bound to at least one enzyme which is able to metabolise a compound which has little or no cytotoxicity (prodrug) into a cytotoxic compound (drug), where the antigen binding region consists of a single polypeptide chain. Covalently bonded carbohydrates are advantageously present on the polypeptide chain.

公开(公告)号：DE69425356D1

公开(公告)日：2000-08-31

申请号：DE69425356

申请日：1994-09-09

Applicant: HOECHST AG ,  HOECHST HOUDE S A LAB

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  HOFFMANN DIETER ,  TILLEQUIN FRANCOIS ,  FLORENT JEAN-CLAUDE ,  AZOULAY MICHEL ,  MONNERET CLAUDE ,  JACQUESY JEAN-CLAUDE ,  GESSON JEAN-PIERRE ,  KOCH MICHEL

IPC: C07H15/244 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K47/48 ,  A61P43/00

Abstract: Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.

公开(公告)号：AU717219B2

公开(公告)日：2000-03-23

申请号：AU3241997

申请日：1997-07-31

Applicant: HOECHST AG

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  VASELLA ANDREA ,  HOOS ROLAND

IPC: C07D309/28 ,  A61K31/35 ,  A61K31/351 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/74 ,  C07D211/78 ,  C07D309/30 ,  C07D335/02 ,  C07F9/59 ,  C07F9/655 ,  C07F9/6553

Abstract: Trihydroxyheterocyclylamino compounds of formula (I) and their salts are new. Y = COOH, PO3H2, P(O)(OR6)(OH), P(O)R6(OH), tetrazole or SO3H; R6 = 1-4C alkyl; X = NH, O or S; R = H or CONH-C6(R7)5; and R7 = H, OH, halo, COOH, PO3H2 or SO3H.

公开(公告)号：CA2237450A1

公开(公告)日：1998-11-15

申请号：CA2237450

申请日：1998-05-13

Applicant: HOECHST AG

Inventor： CZECH JOERG ,  BOSSLET KLAUS ,  STRAUB RAINER ,  BLUMRICH MATTHIAS ,  GERKEN MANFRED

IPC: C07H15/20 ,  A61K9/20 ,  A61K9/48 ,  A61K31/047 ,  A61K31/70 ,  A61K31/7004 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/715 ,  A61K47/10 ,  A61K47/26 ,  A61K47/36 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H5/06 ,  C07H15/244 ,  C07H15/252

Abstract: A preparation comprising a glycosyl-Y¢-C(=Y)-X-!p-W(R)n-X-C(=Y)-active compound, sugar or sugar alcohol and, if appropriate, divalent ions and a pharmaceutically tolerable carrier has improved in vitro tolerability.

公开(公告)号：HU9801087D0

公开(公告)日：1998-07-28

申请号：HU9801087

申请日：1998-05-14

Applicant: HOECHST AG

Inventor： BLUMRICH MATTHIAS ,  BOSSLET KLAUS ,  CZECH JOERG ,  GERKEN MANFRED ,  STRAUB RAINER

IPC: C07H15/20 ,  A61K9/20 ,  A61K9/48 ,  A61K31/047 ,  A61K31/70 ,  A61K31/7004 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/715 ,  A61K47/10 ,  A61K47/26 ,  A61K47/36 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H5/06 ,  C07H15/244 ,  C07H15/252

Abstract: Compositions containing a glycosylated drug derivative of formula (I) and/or its salts, a carrier and optionally divalent ions, is new. G-Y-(C(=Y)-X)p-W(R)n-X-C(=Y)-A (I) Also claimed is the production of the preparation by processing the ingredients into a pharmaceutical dosage form. G = enzymatically cleavable poly-, oligo- or monosaccharide residue; W = aromatic or heteroaromatic residue, aliphatic residue containing conjugated double bonds or amino acid residue which cyclises after cleavage of G; R = H, Me, OMe, COOH, CN, COOMe, OH, NO2, F, Cl, Br, sulphonyl, sulphonamide or (1-4C alkyl)-sulphonamide; p = 0 or 1; n = integer; X = O, NH, methyleneoxy, methyleneamino or methylene-(1-4C) alkylamino; Y = O or NH; and A = biologically active agent bonded via a hydroxy, amino or imino group.

公开(公告)号：TR9700178A2

公开(公告)日：1997-09-21

申请号：TR9700178

申请日：1997-03-10

Applicant: HOECHST AG

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  GERKEN MANFRED ,  STRAUB RAINER ,  MONNERET CLAUDE ,  FLORENT JEAN-CLAUDE ,  SCHMIDT FREDERIC

IPC: C07H15/203 ,  A61K31/70 ,  A61K31/7012 ,  A61K31/7028 ,  A61K31/7034 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H15/26

CPC classification number: A61K47/549 ,  A61K47/54

公开(公告)号：TR199700178A2

公开(公告)日：1997-09-21

申请号：TR9700178

申请日：1997-03-10

Applicant: HOECHST AG

Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  GERKEN MANFRED ,  STRAUB RAINER ,  MONNERET CLAUDE ,  FLORENT JEAN-CLAUDE ,  SCHMIDT FREDERIC

IPC: A61K31/70 ,  C07H15/203 ,  A61K31/7012 ,  A61K31/7028 ,  A61K31/7034 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H15/26

Abstract: Glycosyl derivatives of formula Glycosyl-YÄ-C(=Y)-X-Üp-W(R)n-Z-C(=Y)-active agent (I) and their salts are new: glycosyl = enzymatically cleavable poly-, oligo- or mono-saccharide; W = 5-14 membered aryl, naphthyl, indenyl, anthryl, phenanthryl, 5-14 membered heterocyclyl (containing 1-4 O, N or S), 1-6C alkyl, 2-6C alkenyl, 3-6C cycloalkyl or phenyl; R = H, 1-4C alkyl, phenyl, methoxy, carboxy, methyloxycarbonyl, CN, OH, NO2, F, Cl, Br, sulphonyl, sulphonamide or 1-4C sulphonalkylamide; p = 0-1; n = 0-3; X = O, NH, methyleneoxy, methyleneamino, methylene-1-4C alkylamino, 1-4C alkylamino, 3-6C cycloalkylamino; Y = O or NH; Z = 1-4C alkylamino, NCH3, C(CH3)2NH, CH(CH3)NH, C(CH3)2N(R ) or NH if W = 1-6C alkyl; R = 1-4C alkyl; and active agent = a compound with biological effect bonded via an oxygen, primary or secondary amine or an imino group.