US4376765A
Expired / Lapsed
US
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Medicaments, their preparation and compositions containing same
Assignee: Institut International de Pathologie Cellulaire et Moleculaire
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Filing: 1981-03-31
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Granted: 1983-03-15
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Expires: 2001-03-31
Abstract
Abstract The invention relates to a new pharmaceutical form of a medicament of the formula Carrier-Spacer arm-Drug in which "Drug" represents an active principle provided with a free amino function "Spacer arm" represents a peptidic chain of the X-L-Leu type and "Carrier" is a proteinic macromolecule adapted to the drug.
Inventors
- 👤 Andre B. L. Trouet
- 👤 Michele M. L. G. Masquelier
- 👤 Roger M. Baurain
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 18:04
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6801; A61K47/6803; A61K47/6811; A61K47/6817; A61K47/6829; A61K47/62; A61K47/65; A61K47/6889; Y; Y10; Y10S; Y10S530/00; Y10S530/81; Y10S530/812; Y10S530/815; Y10S530/816; Y10S930/00; Y10S930/01; Y10S930/28; Y10S930/29; Y10S930/31
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
142 words
A medicament compound of the formula Carrier-spacer arm-Drug wherein "drug" represents the therepeutically active principle containing a free amino function, said drug being selected from the group consisting of antitumoral anthracyclines, antimalarial and antileishmanial quinoleines, "spacer arm" is a chain of peptidic nature represented by the sequence X--L--Leu wherein L--Leu represents a L--leucyl moiety bound through its carboxylic amino function to the amino function of the drug and X represents 1, 2 or 3 aminoacids which may be identical or different, selected from the group consisting of L-alanine, glycine and L--leucine and having a possible succinylated terminal amino function, and --"carrier" is a macromolecule of proteinic nature, the nature of which is related to the transport and/or affinity of action intended for the drug, said carrier being selected from the group consisting of bovine serum albumin, fetuine, immuno-globuline, asiafetuine or peptidic hormones.
Claim 2
Dependent Claim
142 words
A medicament compound of the formula Carrier-spacer arm-Drug wherein "drug" represents the therepeutically active principle containing a free amino function, said drug being selected from the group consisting of antitumoral anthracyclines, antimalarial and antileishmanial quinoleines, "spacer arm" is a chain of peptidic nature represented by the sequence X--L--Leu wherein L--Leu represents a L--leucyl moiety bound through its carboxylic amino function to the amino function of the drug and X represents 1, 2 or 3 aminoacids which may be identical or different, selected from the group consisting of L-alanine, glycine and L--leucine and having a possible succinylated terminal amino function, and --"carrier" is a macromolecule of proteinic nature, the nature of which is related to the transport and/or affinity of action intended for the drug, said carrier being selected from the group consisting of bovine serum albumin, fetuine, immuno-globuline, asiafetuine or peptidic hormones.
Claim 3
Dependent Claim
20 words
The medicament according to claim 1, wherein the drug is selected from the group consisting of daunorubicine, doxorubicine and primaquine.
Claim 4
Dependent Claim
21 words
The medicament according to claim 1, wherein the spacer arm contains the sequence L-ala-L-leu, L-leu-L-ala-L-leu, L-ala-L-leu-L-ala-L-leu, (L-ala) 3 -L-leu, gly-L-leu-gly-L-leu, L-ala-L-leu-gly-L-leu.
Claim 5
Dependent Claim
22 words
The medicament according to claim 1, wherein the peptidic hormone is selected from the group consisting of lactotropine or lactogenous placentary hormone.
Claim 6
Dependent Claim
22 words
The medicament according to claim 2, wherein the peptidic hormone is selected from the group consisting of lactotropine or lactogenous placentary hormone.
Claim 7
Dependent Claim
22 words
The medicament according to claim 3, wherein the peptidic hormone is selected from the group consisting of lactotropine or lactogenous placentary hormone.
Claim 8
Dependent Claim
22 words
A medicinal composition comprising the medicament according to claim 1, in a compatible pharmaceutically acceptable vehicle in effective concentrations for pharmacological application.
Claim 9
Dependent Claim
22 words
The medicament according to claim 1, wherein the "spacer arm" is selected from the group consisting of tri- and tetrapeptidic spacer arms.
Claim 10
Dependent Claim
22 words
The medicament according to claim 2, wherein the "spacer arm" is selected from the group consisting of tri- and tetrapeptidic spacer arms.
Claim 11
Dependent Claim
26 words
The medicament according to claim 8, wherein the "spacer arm" contains a sequence selected from the group consisting of L-leu-L-ala-L-leu; L-ala-L-leu-L-ala-L-leu; (L-ala) 3 -L-leu; gly-L-leu-gly-L-leu; L-ala-L-leu-gly-L-leu.
Claim 12
Dependent Claim
26 words
The medicament according to claim 9, wherein the "spacer arm" contains a sequence selected from the group consisting of L-leu-L-ala-L-leu; L-ala-L-leu-L-ala-L-leu; (L-ala) 3 -L-leu; gly-L-leu-gly-L-leu; L-ala-L-leu-gly-L-leu.
Claim 13
Dependent Claim
14 words
The medicament according to claim 8, wherein the "spacer arm" contains the sequence ala-leu-ala-leu.
Claim 14
Dependent Claim
14 words
The medicament according to claim 9, wherein the "spacer arm" contains the sequence ala-leu-ala-leu.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-03-14 | 1986-09-13 | 1987-03-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-03-14 | 1990-09-13 | 1991-03-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-03-14 | 1994-09-13 | 1995-03-15 | $7700.00 | Window Closed / Lapsed |