公开(公告)号：JPH101495A

公开(公告)日：1998-01-06

申请号：JP5598397

申请日：1997-03-11

Applicant: HOECHST AG

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

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

Abstract: PROBLEM TO BE SOLVED: To obtain a new compound, a glycosyl group-bearing specific active compound, high in stability and slight in side effects, and useful as a prodrug for preventing/treating tumors, autoimmune diseases and chronic inflammatory diseases such as chronic arthrorheumatism. SOLUTION: This new compound is shown by formula I [glycosyl is derived from a polysaccharide, oligosaccharide or monosaccharide each subject to scission by an enzyme; W is a 5- to 14-membered aromatic group, 5- to 14-membered heterocyclic group, 1-6C alkyl, 2-6C alkenyl, etc.; R is H, a 1-4C alkyl, phenyl, CN, OH, NO2 , halogen, etc.; X is O, NH, methyleneoxy, etc.; Y is O or NH; Z is a 1-4C alkylamino, N(CH3 ) or NH; (p) is 0 or 1; (n) is 0 or 1-3] and useful as a preventive/therapeutic agent for cancerous diseases, autoimmune diseases, chronic inflammatory diseases, etc. This compound is obtained by reaction of a compound of formula II with an active compound bearing activated carboxyl, amino or imino group in the presence of a solvent such as acetonitrile followed by eliminating the protecting group.

公开(公告)号：JPH1077279A

公开(公告)日：1998-03-24

申请号：JP20757497

申请日：1997-08-01

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: PROBLEM TO BE SOLVED: To obtain a compound which is useful as a β-gluculonidase inhibitor which inhibit tumors from growing and metastasizing. SOLUTION: This compound is represented by formula I [Y is -COOH, -PO3 H2 , -P(O)(OR )(OH); R is a 1-4 alkyl; X is NH, O, S; R is H, -C(O)NHC6 (R )5 ; R is H, OH, a halogen] and formula II (R -R is H, OH a halogen, -COOH, -PO3 H2 ), typically (Z)-O-(D-glucopyranuronosilidene)amino-N- phenyl carbamate. The formulation of the compound of formula I and formula II affords a medicine effective for treatment of postoperative carcinomatous diseases or the inhibition of tumor metastasis and treatment of inflammatory diseases. The compounds of formulas I and II can be prepared by a known process. The does is

公开(公告)号：BRPI9701248B1

公开(公告)日：2022-01-18

申请号：BR9701248

申请日：1997-03-11

Applicant: AVENTIS PHARMA DEUTSCHLAND GMBH ,  HOECHST AG ,  SANOFI AVENTIS DEUTSCHLAND

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

IPC: A61K47/54 ,  C07H15/203 ,  A61K31/70 ,  A61K31/7012 ,  A61K31/7028 ,  A61K31/7034 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H15/26

Abstract: patente de invenção: "novos pró-medicamentos para a terapia de tumores e distúrbios inflamatórios" . novos pró-medicamentos para a terapia de tumores e distúrbios inflamatórios. são descritos compostos da fórmula i: glocosil-y[-c(=y)x-]~ p~-w(r)~ n~-z-c(=y)-composto ativo que são adequados para o tratamento de doenças carcinomatosas, doenças auto-imunes e doenças inflamatórias crônicas, tais como a artrite reumatóide.

公开(公告)号：RO120951B1

公开(公告)日：2006-10-30

申请号：RO9700402

申请日：1997-03-03

Applicant: HOECHST AG

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

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

Abstract: Prezenta invenţie se referă la un compus cu activitate antitumoralăşi antiinflamatoare, la un procedeu pentru producerea acestui compus, la o compoziţie farmaceuticăşi la utilizarea acestui compus pentru fabricarea unui medicament pentru profilaxia şi tratamentul bolilor carcinomatoase, bolilor autoimune şi al bolilor inflamatoare cronice.

公开(公告)号：AU740694B2

公开(公告)日：2001-11-15

申请号：AU6600598

申请日：1998-05-15

Applicant: HOECHST AG

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

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：AT193326T

公开(公告)日：2000-06-15

申请号：AT92102197

申请日：1992-02-10

Applicant: HOECHST AG

Inventor： SEEMANN GERHARD ,  BOSSLET KLAUS ,  CZECH JOERG ,  KOLAR CENEK ,  HOFFMANN DIETER ,  SEDLACEK HANS-HARALD

IPC: C12N15/09 ,  A61K38/00 ,  A61K39/395 ,  A61K47/48 ,  A61P35/00 ,  C07K1/113 ,  C07K16/00 ,  C07K16/30 ,  C07K19/00 ,  C12N1/15 ,  C12N9/24 ,  C12N15/56 ,  C12N15/62 ,  C12P21/02 ,  C12P21/08 ,  C12R1/91

公开(公告)号：DE59310018D1

公开(公告)日：2000-05-31

申请号：DE59310018

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：AU3241997A

公开(公告)日：1998-02-12

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：HU9700579D0

公开(公告)日：1997-04-28

申请号：HU9700579

申请日：1997-03-12

Applicant: HOECHST AG

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

IPC: C07H15/203 ,  A61K31/70 ,  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.

公开(公告)号：NO971116D0

公开(公告)日：1997-03-11

申请号：NO971116

申请日：1997-03-11

Applicant: HOECHST AG

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

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

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.