公开(公告)号：RU2182911C2

公开(公告)日：2002-05-27

申请号：RU98113945

申请日：1996-12-11

Applicant: BASF AG

Inventor： AMBERG VIL GEL M ,  BARLOTSARI TEREZA ,  BERNARD KHARAL D ,  BUSHMANN EHRNST ,  KHAUPT ANDREAS ,  KHEGE KHANS-GJUNTER ,  JANSSEN BERND ,  KLING ANDREAS ,  LITS KHEL MUT ,  RITTER KURT ,  ULL RIKH MARTINA ,  VEJMANN JURGEN ,  TSIRKE TOMAS

IPC: A61K31/00 ,  A61K38/08 ,  A61P35/00 ,  A61K38/00 ,  A61P35/02 ,  C07K1/00 ,  C07K7/06

Abstract: organic chemistry, chemistry of peptides, oncology. SUBSTANCE: invention describes novel peptides of the general formula (I): (CH3)2-N- CHX-CO-A-B-D-E-K where A means valine residue; B means N-methylvaline residue; D means proline residue; E means proline residue; X means isopropyl-group; K means , NH-cyclohexyl, NH- cycloheptyl, or and their physiologically tolerant salts. New compounds show an antitumor activity. These compounds show high resistance to decomposition as compared with the known analogues, for example, dolastatine-10 or dolastatine-15 and they can be used orally. EFFECT: new peptides indicated above, valuable medicinal and chemical properties. 4 cl, 2 ex

公开(公告)号：RU2199529C2

公开(公告)日：2003-02-27

申请号：RU99104297

申请日：1997-07-14

Applicant: BASF AG

Inventor： MAK KHEL TUT ,  PFAJFER TOMAS ,  ZAJTTS VERNER ,  TSIRKE TOMAS ,  BAL KENKHOL FRIDKHEL M ,  LANGE UDO

IPC: C12P17/04 ,  C07D207/22 ,  C07D401/12

公开(公告)号：RU2195462C2

公开(公告)日：2002-12-27

申请号：RU2000103960

申请日：1998-07-07

Applicant: BASF AG

Inventor： JANSSEN BERND ,  BARLOTSTSARI TEREZA ,  KHAUPT ANDREAS ,  TSIRKE TOMAS ,  KLING ANDREAS

IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K7/06 ,  C12P19/34

Abstract: FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of dolastatin-15 of the general formula (I): A-B-D-E-F-(G)r-(K)s-L where A, B, D, E, F, G and K mean residues of alpha-amino acids; s and r each means independently 0 or 1; L means monovalent radical, for example, amino-group, N-substituted amino-group, beta-hydroxylamino-group, hydrazido-group, alkoxy-group, thioalkoxy-group, aminooxy-group or oximato-group. Except for, invention involves method of cancer treatment in mammal, for example, in humans that includes administration to mammal the effective amount of compound of the formula (I). EFFECT: valuable medicinal properties of derivatives. 39 cl, 3 tbl

公开(公告)号：RU2152953C1

公开(公告)日：2000-07-20

申请号：RU97112398

申请日：1995-11-25

Applicant: BASF AG

Inventor： BEM KHANS JOAKHIM ,  KOZER SHTEFAN ,  MAK KHEL MUT ,  PFAJFFER TOMAS ,  ZAJTTS VERNER ,  KHEFFKEN KHANS VOL FGANG ,  KHORNBERGER VIL FRID ,  TSIRKE TOMAS

IPC: A61K38/00 ,  A61K38/05 ,  A61K38/55 ,  A61P7/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087

Abstract: organic chemistry, peptide derivatives. SUBSTANCE: invention describes the novel derivatives of dipeptide p-amidinobenzylamides with N-terminal residues of the general formula (I) where R is alkyl with 1-20 carbon atoms, fluoroalkyl with 1-3 carbon atoms, arylalkyl with 1-10 carbon atoms in alkyl moiety, aryl, heteroaryl that is five- or six-membered aromatic cycle containing one nitrogen or sulfur as heteroatom, hydroxyl or R2R3N where R2 and R3 are similar or different and mean hydrogen atom, alkyl with 1-10 carbon atoms; A means residue of alpha-amino acid of the formula (II) where R4 means hydrogen atom, cycloalkyl with 3-7 carbon atoms or aryl; R5 means hydrogen atom, cycloalkylalkyl with 3-7 carbon atoms in cycloalkyl moiety and 1-3 carbon atoms in alkyl moiety, arylalkyl with 1-3 carbon atoms in alkyl moiety; B means residue of cyclic alpha-amino acid of the formula (III) where m = 2, 3 or 4 and if m = 3 or 4 then two adjacent hydrogen atoms can be replaced with double bond, or their salt with physiologically acceptable acids. Compounds of the formula (I) show biological activity, in part, they inhibit activity of thrombin. EFFECT: new compounds indicated above, valuable pharmacological activity. 2 cl, 1 tbl, 22 ex