EP0429436A2
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 by an acylamino substituent of formula wherein m is an integer from 1 to 3 and R₁ and R₂ are each hydrogen or an alkyl radical having from 1 to 3 carbon atoms or R₁ and R₂ 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
2026-11-07 18:26
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/12; C07D498/18
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
101 words
A process for preparing a water soluble pharmaceutically acceptable salt of a monoacyl derivative of rapamycin which comprises acylating rapamycin with an acylating agent containing an acylamino substituent having the configuration: wherein m is an integer from 1 to 3, wherein R₁ and R₂ are each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R₁ R₂ together with the nitrogen to which they are attached to form a saturated heterocyclic ring having four to five carbon atoms and isolating the major monoacyl product, if required acidifying the product to give a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
22 words
A process as claimed in Claim 1 wherein R₁ and R₂ are each an alkyl radical of 1 to 3 carbon atoms.
Claim 3
Dependent Claim
15 words
A process as claimed in Claim 2 wherein R₁ and R₂ are methyl or ethyl.
Claim 4
Dependent Claim
18 words
A process as claimed in any one of Claims 1 to 3 wherein m is 1 or 2.
Claim 5
Dependent Claim
17 words
The process as claimed in Claim 1 in which the mono-substituted derivative is prepared having the substituent
Claim 6
Dependent Claim
18 words
A process as claimed in Claim 1 in which the mono substituted derivative is prepared having the substituent
Claim 7
Dependent Claim
18 words
A process as claimed in Claim 1 in which the mono substituted derivative is prepared having the substituent
Claim 8
Dependent Claim
28 words
A process as claimed in Claim 1 wherein the acylating agent is the acid, the acid halide, the acid anhydride or an activated ester of said acylamino substituent.
Claim 9
Dependent Claim
25 words
A process as claimed in Claim 1 wherein the acylating agent is the acid of said acylamino substituent in the presence of a coupling agent.
Claim 10
Dependent Claim
19 words
A process as claimed in Claim 9 wherein the coupling agent is N, N'-dicyclohexylcarbodiimide, 1,1'-carbonyldiimidazole, diethylazodicarboxylate, 2,2'-dithiopyridine, or N,N-diisopropylcarbodiimide.
Claim 11
Dependent Claim
40 words
A process for preparing an injectable pharmaceutical composition which comprises bringing a water soluble derivative of rapamycin or a pharmaceutically acceptable salt thereof as defined in any one of Claims 1 to 7 into a form suitable for therapeutic administration.
References Cited (Backward Citations)
No citation records indexed.
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