EP0227355A2
Expired / Lapsed
EP
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Prodrugs of rapamycin
Assignee: University of Kansas
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Filing: 1986-12-04
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Granted: —
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Expires: 2006-12-04
Abstract
Abstract Water soluble prodrugs of rapamycin are disclosed which are useful as components in injectable pharmaceutical formulations for the treatment of tumors in mammals. Said prodrugs are rapamycin derivatives or salts thereof mono substituted at position 28 or disubstituted at position 28 or and 43 by acylamino substituent of formula wherein m is an integer from 1 to 3 and R 1 and R 2 are each hydrogen or an alkyl radical having from 1 to 3 carbon atoms or R 1 and R 2 together with the nitrogen atom to which they are attached form a saturated heterocyclic ring having 4-5 carbon atoms.
Inventors
- 👤 Valentino John Stella
- 👤 Paul Edwin Kennedy
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-28 01:18
CPC Classifications
C; C07; C07H; C07H1/00; C07D; C07D498/00; C07D498/12; C07D498/18; A; A61; A61P; A61P31/00; A61P31/04; A61P43/00
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
92 words
A water soluble derivative of rapamycin which is a mono-substituted derivative at position 28 or disubstituted derivative at positions 28 and 43 of rapamycin with the substituent having the configuration: wherein m is an integer from 1 to 3, wherein R 1 and R 2 are each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R 1 and R 2 together with the nitrogen to which they are attached form a saturated heterocyclic ring having four to five carbon atoms, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
92 words
A water soluble derivative of rapamycin which is a mono-substituted derivative at position 28 or disubstituted derivative at positions 28 and 43 of rapamycin with the substituent having the configuration: wherein m is an integer from 1 to 3, wherein R 1 and R 2 are each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R 1 and R 2 together with the nitrogen to which they are attached form a saturated heterocyclic ring having four to five carbon atoms, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
25 words
A rapamycin derivative as claimed in Claim 1 wherein R 1 and R 2 are each an alkyl radical of 1 to 3 carbon atoms.
Claim 4
Dependent Claim
18 words
A rapamycin derivative as claimed in Claim 2 wherein R 1 and R 2 are methyl or ethyl.
Claim 5
Dependent Claim
19 words
A rapamycin derivative as claimed in any one of Claims 1 to 3 wherein m is 1 or 2.
Claim 6
Dependent Claim
10 words
The mono-substituted derivative of claim 1 wherein the substituent is
Claim 7
Dependent Claim
10 words
The mono-substituted derivative of claim 1 wherein the substituent is
Claim 8
Dependent Claim
10 words
The mono-substituted derivative of claim 1 wherein the substituent is
Claim 9
Dependent Claim
54 words
A process for preparing a water-soluble rapanycin derivative mono-substituted at position 28 or disubstituted at positions 28 and 43 by an acylamino substituent having the configuration wherein m, R 1 and R 2 are as defined in Claim 1, which comprises acylating rapamycin with an acylating agent containing the acylamino substituent having the configuration
Claim 10
Dependent Claim
28 words
A process as claimed in Claim 8 wherein the acylating agent is the acid, the acid halide, the acid anhydride or an activated ester of said acylamino substituent.
Claim 11
Dependent Claim
25 words
A process as claimed in Claim 9 wherein the acylating agent is the acid of said acylamino substituent in the presence of a coupling agent.
Claim 12
Dependent Claim
19 words
A process as claimed in Claim 10 wherein the coupling agent is N, N'-dicyclohexylcarbodiimide, 1,1'-carbonyldiimidazole, diethylazodicarboxylate, 2,2'-dithiopyridine, or N,N-diisopropylcarbodiimide.
Claim 13
Dependent Claim
28 words
A process for preparing a salt of a compound as claimed in any one of Claims 1 to 7 which canprises acidifying a basic compound of claim 1.
Claim 14
Dependent Claim
27 words
A process as claimed in any one of Claims 8 to 12 wherein R 1 and R 2 are each alkyl of 1 to 3 carbon atoms.
Claim 15
Dependent Claim
32 words
An injectable pharmaceutical composition comprising a water soluble derivative of rapamycin or a pharmaceutically acceptable salt thereof as claimed in any one of Claims 1 to 8 and a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
No citation records indexed.
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