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EP0128670A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

4-Demethoxy-3'-deamino-3'(4-morpholinyl) derivatives of anthracycline anticancer antibiotics

Assignee: Pharmacia and Upjohn Co
•
Filing: 1984-05-11
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Granted: —
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Expires: 2004-05-11
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Abstract

Abstract 3'-deamino-3'-(4-morpholinyl) and 3'-deamino-3'-(3-cyano-4-morpholinyl) derivatives of 4-demethoxydaunorubicin and 4-demethoxydoxorubicin together with their 13-dihydro analogues and their pharmaceutically acceptable acid addition salts are disclosed. These compounds have utility as antitumor agents.

Inventors

  • 👤 John Paul Carter
  • 👤 Richard L. Wolgemuth
  • 👤 Richard Alfred Carrano

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-05 18:04
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/24; C07H15/252; A; A61; A61P; A61P35/00

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 40 words
A compound of the formula (I) where R is COCH 3 , COCH2 0 H , CH(OH)CH 3 , or CH(OH)CH 20H and R ' is a hydrogen atom or a cyano group and its pharmaceutically acceptable acid addition salts.
Claim 2
Dependent Claim 40 words
A compound of the formula (I) where R is COCH 3 , COCH2 0 H , CH(OH)CH 3 , or CH(OH)CH 20H and R ' is a hydrogen atom or a cyano group and its pharmaceutically acceptable acid addition salts.
Claim 3
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-daunorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 4
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-daunorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 5
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-13-dihydrodaunorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 6
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-13-dihydrodaunorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 7
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-doxorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 8
Dependent Claim 13 words
The compound 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-doxorubicin of claim 1 and its pharmaceutically acceptable acid addition salts.
Claim 9
Dependent Claim 10 words
The compound 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-13-dihydrodoxorubicin and its pharmaceutically acceptable acid addition salts.
Claim 10
Dependent Claim 10 words
The compound 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-13-dihydrodoxorubicin and its pharmaceutically acceptable acid addition salts.
Claim 11
Dependent Claim 53 words
A pharmaceutical preparation comprising, in a non-toxic pharmaceutically acceptable carrier, a therapeutically effective amount of a compound of the formula (I) where R is COCH3, COCH 2 0H, CH(OH)CH 3 , or CH(OH)CH 2 OH and R ' is a hydrogen atom or a cyano group or a pharmaceutically acceptable acid salt thereof.
Claim 12
Dependent Claim 53 words
A pharmaceutical preparation comprising, in a non-toxic pharmaceutically acceptable carrier, a therapeutically effective amount of a compound of the formula (I) where R is COCH3, COCH 2 0H, CH(OH)CH 3 , or CH(OH)CH 2 OH and R ' is a hydrogen atom or a cyano group or a pharmaceutically acceptable acid salt thereof.
Claim 13
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-daunorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-daunorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 15
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-13-dihydrodaunorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 16
Dependent Claim 21 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3 1- (3-cyano-4-morpholinyl)-13-dihydrodaunorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 17
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-doxorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 18
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-doxorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 19
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(4-morpholinyl)-13-dihydrodoxorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 20
Dependent Claim 19 words
The pharmaceutical preparation of claim 10 wherein said compound is 3'-deamino-4-demethoxy-3'-(3-cyano-4-morpholinyl)-13-dihydrodoxorubicin or a pharmaceutically acceptable acid addition salt thereof.
Claim 21
Dependent Claim 27 words
A process of preparing the compound or pharmaceutical preparation, as the case may be, according to any one of the preceding claims and substantially as hereinbefore described.

References Cited (Backward Citations)

DE2652391A1 Cited
GB1509875A Cited
US4301277A Cited
US4374980A Cited
GB2124224A Cited

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