公开(公告)号：RU95115135A

公开(公告)日：1997-06-10

申请号：RU95115135

申请日：1993-12-04

Applicant: BASF AG

Inventor： ANDREAS KHAUPT ,  BERND JANSSEN ,  KURT RITTER ,  DAGMAR KLINGE ,  GERKHARD KEJL KHAUER ,  SINTIJA ROMERDAL ,  TEREZA BARLOZZARI ,  KSIAO-DONG KVIAN

IPC: A61K38/00 ,  C07K5/103 ,  A61K38/07 ,  A61K38/08 ,  A61P35/00 ,  C07K1/00 ,  C07K5/02 ,  C07K5/027 ,  C07K7/02 ,  C07K7/06

Abstract: Описаныновыепептидыформулы I,вкоторойзначения R, R, X, А, R, В, D, E, R, M, Q, a, b и d указаныв описании, испособыихполучения. Новыевеществаобладаютантинеопластическимдействием.

公开(公告)号：RU2132334C1

公开(公告)日：1999-06-27

申请号：RU95115135

申请日：1993-12-04

Applicant: BASF AG

Inventor： ANDREAS KHAUPT ,  BERND JANSSEN ,  KURT RITTER ,  DAGMAR KLINGE ,  GERKHARD KEJL KHAUER ,  SINTIJA ROMERDAL ,  TEREZA BARLOZZARI ,  KSIAO-DONG KVIAN

IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K1/00 ,  C07K5/02 ,  C07K5/027 ,  C07K7/02 ,  C07K7/06

Abstract: FIELD: organic chemistry, peptides. SUBSTANCE: invention relates to peptides of the general formula (I) where R is C 1-7 -alkyl; R is C 1-4 -alkyl; X is C 1-5 -alkyl; R is a lower alkyl; B - is C 1-5 -alkyl; D is C 1-5 -alkoxy; M - phenylalanine; R - H; R - H or benzyl; d = 0 or 1, or their salts showing the improved therapeutic properties for treatment of patients with neoplasms as compared with dolostatine-10. Proposed analog can be synthesized by conventional methods unlike to the latter. EFFECT: improved therapeutic properties. 2 cl, 2 tbl, 2 ex

公开(公告)号：RU2116312C1

公开(公告)日：1998-07-27

申请号：RU94046434

申请日：1993-05-10

Applicant: BASF AG

Inventor： ANDREAS KHAUPT ,  FRANTS EHMLING ,  SINTIJA ROMERDAL

IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  A61P35/02 ,  C07K5/062 ,  C07K5/08 ,  C07K5/083 ,  C07K5/087 ,  C07K5/10 ,  C07K5/103 ,  C07K5/107 ,  C07K7/06

Abstract: FIELD: chemistry of peptides. SUBSTANCE: invention proposes peptide derivatives of the general formula (I): R 1 R 2 -N-CH(X)CO-A-B-D-(E) u -(F) v -(G) w -K where R is AlkO, (lower)-Alk, FAlk, cyclo-Alk, aminosulfonyl being the latter can be substituted with Alk, OH or NR 3 R where each R and R can be hydrogen or alkyl; R - hydrogen, Alk, FAlk, cyclo-Alk; R and R together form 5-membered heterocycle; A is a residue of amino acid taken from: Val, Ile, Leu, allo-Ile, alpha-aminoisobutanoyl, 3-tert.-butyl-Ala, 2-tert. -butyl-Gly, 3-cyclohexyl-Ala, 2-ethyl-Gly, 2-cyclohexyl-Gly, Nle, NVal; B is a residue: N-Alk-Val, NVal, Leu, Ile, 2-tert.-butyl-Gly, 3-tert. -butyl-Ala, 3-cyclohexyl-Ala, Phe, 2-cyclohexyl-Gly; D, E, F and G are taken independently from group containing: Pro, homo-Pro, hydroxy-Pro, thiazolidinyl-4-carbonyl, 1-aminopentyl-1-carbonyl, Val, 2-tert.-butyl-Gly, Ile, Leu, 2-cyclohexyl-Ala, Phe, N-methyl-Phe, tetrahydroisoquinolyl-2-carbonyl, 3-thiazolyl-Ala, 3-thienyl-Ala, His, 1-aminoindolyl-1-carbonyl, Arg, 3-pyridyl-Ala, 3-tert.-butyl-Ala, 2-cyclohexyl-Gly, NVal, NLeu and 3-naphthyl-Ala; x is hydrogen, alkyl, cycloalkyl, -CH 2 -cyclohexyl or arylalkyl; E and F together form five-membered heterocyclic ring containing nitrogen and/or oxygen, sulfur; u, v and w are similar and mean independently 0 or 1; K is OH, AlkO, phenoxy, benxyloxy, substituted of free amino-group, or their salts with physiologically compatible acids, and pharmaceutical composition containing a carrier and an active component of the formula (I) taken at effective amount. Synthesized peptides is used in medicine since they provide potentially improved therapeutic effectiveness for neoplastic diseases treatment. EFFECT: improved method of synthesis of new peptides indicated above, enhanced effectiveness of peptides. 10 cl, 2 ex, 4 tbl, 3 dwgK

公开(公告)号：RU94046434A

公开(公告)日：1996-10-27

申请号：RU94046434

申请日：1993-05-10

Applicant: BASF AG

Inventor： ANDREAS KHAUPT ,  FRANTS EHMLING ,  SINTIJA ROMERDAL

IPC: A61K38/00 ,  C07K7/06 ,  A61K38/08 ,  A61P35/00 ,  A61P35/02 ,  C07K5/062 ,  C07K5/08 ,  C07K5/083 ,  C07K5/087 ,  C07K5/10 ,  C07K5/103 ,  C07K5/107

Abstract: Предлагаютсяновыепептидыформулы I, вкоторой R, R, A, B, D, E, F, G, K, X, t, u, v и w имеютзначения, приведенныев описании, иихполучение. Новыевеществаобладаютантинеопластическимэффектом.