US4957939A
Expired / Lapsed
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Sterile pharmaceutical compositions of gadolinium chelates useful enhancing NMR imaging
Assignee: Bayer Pharma AG
•
Filing: 1986-06-20
•
Granted: 1990-09-18
•
Expires: 2006-06-20
Abstract
Abstract Pharmaceutical compositions comprising gadolinium chelates are useful for enhancing NMR images.
Inventors
- 👤 Heinz Gries
- 👤 Douwe Rosenberg
- 👤 Hanns-Joachim Weinmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 15:09
CPC Classifications
C; C07; C07C; C07C323/00; C07C323/23; C07C323/24; C07C323/25; A; A61; A61K; A61K49/00; A61K49/04; A61K49/06; A61K49/08; A61K49/085; A61K49/10; A61K49/101; A61K49/103; A61K49/105; A61K49/106; A61K49/108; A61K49/14; A61K49/143; A61K49/16; A61K49/18; A61K49/1806; A61K49/1809; A61K49/1812; C07D; C07D257/00; C07D257/02; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3808; C07F9/3817; C07F9/3839; C07F9/386; G; G01; G01R; G01R33/00; G01R33/20; G01R33/44; G01R33/48; G01R33/54; G01R33/56; G01R33/5601; Y; Y10; Y10S; Y10S436/00; Y10S436/806; Y10T; Y10T436/00; Y10T436/24
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
25 words
A pharmaceutical composition for enhancement of NMR imaging comprising a physiologically compatible gadolinium chelate complex and a pharmaceutically acceptable carrier, wherein said composition is sterile.
Claim 2
Dependent Claim
25 words
A pharmaceutical composition for enhancement of NMR imaging comprising a physiologically compatible gadolinium chelate complex and a pharmaceutically acceptable carrier, wherein said composition is sterile.
Claim 3
Dependent Claim
24 words
A composition according to claim 1, wherein gadolinium is chelated by an open-chain or cyclic complexing agent containing organic nitrogen, phosphorous, oxygen or sulfur.
Claim 4
Dependent Claim
15 words
A composition according to claim 1, wherein gadolinium is chelated by an open-chain chelating agent.
Claim 5
Dependent Claim
15 words
A composition according to claim 1, wherein gadolinium is chelated by a cyclic chelating agent.
Claim 6
Dependent Claim
14 words
A composition according to claim 1, wherein gadolinium is chelated by an aminopolycarboxylic acid.
Claim 7
Dependent Claim
27 words
A pharmaceutical composition according to claim 1, wherein gadolinium is chelated by nitrilotriacetic acid (NTA), N,N,N',N'-ethylenediaminetetraacetic acid (EDTA), N-hydroxyethyl-N,N',N'-ethylenediaminetriacetic acid (HEDTA), N,N,N',N",N"-diethylenetriaminepentaacetic acid (DTPA), or N-hydroxyethyliminodiacetic acid.
Claim 8
Dependent Claim
47 words
A composition according to claim 1, wherein gadolinium is chelated by an amine of the formula ##STR9## wherein R 1 and R 1 ', being identical or different, are H or alkyl of 1 to 4 C atoms and n is a number from 0 to 4.
Claim 9
Dependent Claim
17 words
A composition according to claim 1, wherein gadolinium is chelated by ethylenediamine, diethylenetriamine, triethylenetetraamine, tetraethylenepentaamine, or pentaethylenehexaamine.
Claim 10
Dependent Claim
170 words
A composition according to claim 1, wherein gadolinium is chelated by a macrocyclic compound of the formula ##STR10## wherein R 2 is H, a hydrocarbon radical or an alkoxycarbonyl radical or both radicals R 2 together form a group of subformula ##STR11## A is in each case a hydrocarbon radical; X is in each case N or P; D is in each case O, S, a group of formula ##STR12## wherein R is H or a hydrocarbon radial, or a hydrocarbon radical; and m, n and p are whole numbers from 0 to 5; with the proviso that at least two of the D groups are O, S, or a group of formula ##STR13## and in cases in which each R 2 radical is a hydrogen atom, a hydrocarbon radical or an alkoxycarbonyl radical and X is a N atom, one of these two radicals or atoms which D represents, is an O or S atom and the other radical is an O atom or a group of formula ##STR14##
Claim 11
Dependent Claim
20 words
A composition according to claim 1, wherein no free acid or free base groups are present in the chelate complex.
Claim 12
Dependent Claim
21 words
A composition according to claim 1, wherein a free acid or a free base group is present in the chelate complex.
Claim 13
Dependent Claim
34 words
A composition of claim 1, wherein a free acid or a free base group of the chelate complex is in the form of a salt thereof with an inorganic or organic base or acid.
Claim 14
Dependent Claim
33 words
A composition according to claim 1, wherein said chelate complex is both a salt of gadolinium and the chelating agent thereof, and also a salt with an inorganic or organic base or acid.
Claim 15
Dependent Claim
34 words
A composition according to claim 1, wherein said chelate complex is only a salt of gadolinium and the chelating agent thereof and not also a salt with an inorganic or organic base or acid.
Claim 16
Dependent Claim
18 words
A composition according to claim 1, wherein the chelating agent which forms said chelate complex is diethylenetriaminepentaacetic acid.
Claim 17
Dependent Claim
33 words
A composition according to claim 1, wherein said chelate complex consists of a single gadolinium chelated by a chelating agent which optionally is a salt with an organic or inorganic acid or base.
Claim 18
Dependent Claim
39 words
A composition according to claim 13, wherein said inorganic or organic acid or base is hydrochloric acid, sulfuric acid, acetic acid, citric acid, aspartic acid, glutamic acid, sodium hydroxide, glucamine, N-methylglucamine, N,N-dimethylglucamine, ethanolamine, diethanolamine, morpholine, lysine, ornithine or arginine.
Claim 19
Dependent Claim
12 words
A composition according to claim 1, further comprising a conventional galenic stabilizer.
Claim 20
Dependent Claim
10 words
A composition according to claim 1, further comprising sodium chloride.
Claim 21
Dependent Claim
14 words
A pharmaceutical composition according to claim 1, comprising said chelate complex dissolved in water.
Claim 22
Dependent Claim
18 words
A composition according to claim 1, which is an aqueous solution containing 5-250 mmole/l of said chelate complex.
Claim 23
Dependent Claim
16 words
A composition according to claim 1, which is an aqueous solution having a pH of 6.5-8.0.
Claim 24
Dependent Claim
13 words
A composition according to claim 1, which is physiologically suitable for oral administration.
Claim 25
Dependent Claim
13 words
A composition according to claim 1, which is physiologically suitable for neural administration.
Claim 26
Dependent Claim
13 words
A composition according to claim 1, which is physiologically suitable for intravascular administration.
Claim 27
Dependent Claim
16 words
A composition according to claim 1, which is an aqueous solution isotonic with respect to blood.
Claim 28
Dependent Claim
18 words
A composition according to claim 1, wherein said chelate complex is the di-N-methyl glucamine salt of gadolinium(III)-diethylenetriaminepentaacetic acid.
Claim 29
Dependent Claim
22 words
A pharmaceutical composition of claim 1, with the proviso that the gadolinium chelate is not a gadolinium citrate or a gadolinium edetate.
Claim 30
Dependent Claim
12 words
A composition according to claim 1, wherein said chelate complex is nonionic.
Claim 31
Dependent Claim
12 words
A composition according to claim 3, wherein said chelate complex is nonionic.
Claim 32
Dependent Claim
12 words
A composition according to claim 4, wherein said chelate complex is nonionic.
Claim 33
Dependent Claim
12 words
A composition according to claim 28, wherein said chelate complex is nonionic.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-09-17 | 1994-03-19 | 1994-09-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-09-17 | 1998-03-19 | 1998-09-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-09-17 | 2002-03-19 | 2002-09-18 | $7700.00 | Window Closed / Lapsed |