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Title:
標的細胞毒性アントラサイクリン類似体
Document Type and Number:
Japanese Patent JP3987575
Kind Code:
B2
Abstract:
The following are claimed: (A) anthracycline compounds of formula Q-O-R-P (I) Q = a group of formula (i):R = H (sic) or C(O)-(CH2)n-C(O);n = 0-7;R' = NH2; or an aromatic or hydrogenated 5 or 6 membered heterocycle having at least one ring nitrogen, optionally having a butadiene moiety bonded to adjacent carbon atoms to form a bicyclic system;P = H or a peptide; Provided that: (a) where R' is NH2, then R and P are other than H; and (b) where R and P are H, then R' is other than NH2. (B) Conversion of the nitrogen of a primary amino group of an ~a,~b- or ~a,~c-hydroxy primary amine into the nitrogen of a monounsaturated nitrogen-containing heterocyclic compound having 5-6 ring atoms, comprising: (a) treating the hydroxy amine with an excess of a haloaldehyde having an aldehyde carbon, a halo-bearing carbon and having 2 or 3 moieties between the aldehyde carbon and the halo-bearing carbon selected from CH2, CH2CH2 and OCH2; (b) adding an excess (relative to the hydroxyamine) of an organic base; (c) neutralising the base with a weak acid; and (d) treating with a dilute aqueous acid. X' = halo; Y = CH2, OCH2 or CH2-CH2; Z is absent or is CH2.

Inventors:
Andrew V. Charlie
Attila Energy
Renji Kai
Application Number:
JP52012397A
Publication Date:
October 10, 2007
Filing Date:
November 14, 1996
Export Citation:
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Assignee:
Administrators of the Tulane Educational Fund
International Classes:
C07H15/252; A61K31/00; C07K7/23; A61K31/70; A61K31/7028; A61K31/7034; A61K31/704; A61K38/00; A61K47/48; A61P35/00; C07B43/00; C07B61/00; C07H
Domestic Patent References:
JP6041194A
JP4247096A
JP5238951A
JP8231581A
JP61221194A
JP60224696A
JP6500770A
JP4503679A
JP3504609A
Foreign References:
US4202967
US4314054
DE3325816A
Other References:
Anti-Cancer Drugs,(1994),5,p115-130
J.Med.Chem.,(1992),35,p3208-3214
Attorney, Agent or Firm:
Toshio Yano
Toshiomi Yamazaki
Takuya Kuno
Einzel Felix-Reinhard