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EP0323171A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Novel K-252 derivatives having anti-tumor activity and pharmaceutical compositions containing them

Assignee: KH Neochem Co Ltd
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Filing: 1988-12-22
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Granted: —
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Expires: 2008-12-22
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Abstract

Abstract Pharmaceutically active derivatives of K-252 are disclosed, i.e. com­pounds of the formula: wherein R¹ and R² are independently H or OH; X represents COOH, COOR, or CH₂OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl. Such compounds have C-kinase inhibitory activity and are expected to be useful as an active ingredient of anti-tumor pharmaceutical preparations, etc.

Inventors

  • 👤 Chikara C/O Patent Department Murakata
  • 👤 Akira C/O Patent Department Sato
  • 👤 Masaji C/O Patent Department Kasai
  • 👤 Eiji C/O Patent Department Kobayashi
  • 👤 Makoto C/O Patent Department Morimoto
  • 👤 Shiro C/O Patent Department Akinaga

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-08 12:39
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/23; A; A61; A61P; A61P35/00

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 44 words
K-252 derivatives of the formula: in any and all stereoisomeric forms, wherein R¹ and R² are independently H or OH; X represents COOH, COOR, or CH₂OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl.
Claim 2
Dependent Claim 44 words
K-252 derivatives of the formula: in any and all stereoisomeric forms, wherein R¹ and R² are independently H or OH; X represents COOH, COOR, or CH₂OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl.
Claim 3
Dependent Claim 29 words
Compounds of the formula defined claim 1, wherein the defini­tions of X, Y and Z,R is a straight chain or branched alkyl group having 1 to 4 carbon atoms.
Claim 4
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is COOCH₃, Y is CH₃ and Z is OCH₃.
Claim 5
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is COOCH₃, Y is COCH₃ and Z is OC₂H₅.
Claim 6
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is COOCH₃, Y is H and Z is OC₂H₅.
Claim 7
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is COOCH₃, Y is H and Z is SC₂H₅.
Claim 8
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is COOCH₃, Y is H and Z is OH.
Claim 9
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is CH₂OH, Y is H and Z is OH.
Claim 10
Dependent Claim 28 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ and R² are H, X is CH₂OH, Y is H and Z is SC₂H₅.
Claim 11
Dependent Claim 29 words
The compound according to claim 1, in any and all stereoisomeric forms, wherein R¹ is OH, R² is H, X is COOCH₃, Y is H and Z is OH.
Claim 12
Dependent Claim 13 words
Pharmaceutically acceptable salts of the K-252 derivatives claimed in claim 1 or 2.
Claim 13
Dependent Claim 31 words
A pharmaceutical composition comprising a K-252 derivative of the formula defined in claim 1 or 2, or a pharmaceutically acceptable salt thereof, in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 14
Dependent Claim 23 words
A composition according to claim 12, wherein the K-252 derivative is a compound as claimed in any one of claims 3 to 10.

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