Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving leading biopharmaceutical companies globally:

Cerilliant
Chinese Patent Office
UBS
Daiichi Sankyo
McKinsey
Federal Trade Commission
Merck
Cantor Fitzgerald
Baxter
Citi

Generated: February 20, 2018

DrugPatentWatch Database Preview

Claims for Patent: 4,364,921

« Back to Dashboard

Summary for Patent: 4,364,921
Title: Novel triiodinated isophthalic acid diamides as nonionic X-ray contrast media
Abstract:New triiodinated isophthalic acid diamides of the formula ##STR1## wherein the amide residues --CO--N.R.sub.1 R.sub.2 and --CO--N.R.sub.3 R.sub.4 are different from each other and R.sub.1 is hydrogen or C.sub.1-6 alkyl, R.sub.2 is mono- or polyhydroxyalkyl, R.sub.3 is hydrogen or C.sub.1-6 alkyl, R.sub.4 is mono- or polyhydroxylalkyl, R.sub.5 is C.sub.1-6 alkyl or mono- or polyhydroxy-C.sub.1-6 -alkyl or C.sub.1-3 -alkoxy-C.sub.1-3 -alkyl, and R.sub.6 is hydrogen, C.sub.1-6 alkyl or mono- or polyhydroxyalkyl provide superior nonionic X-ray contrast media.
Inventor(s): Speck; Ulrich (Berlin, DE), Blaszkiewicz; Peter (Berlin, DE), Seidelmann; Dieter (Berlin, DE), Klieger; Erich (Berlin, DE)
Assignee: Schering, Aktiengesellschaft (Berlin & Bergkamen, DE)
Application Number:06/127,613
Patent Claims: 1. A triiodinated isophthalic acid diamide of the formula ##STR8## wherein the amide residues --CO--N.R.sub.1 R.sub.2 and --CO--N.R.sub.3 R.sub.4 are different from each other and

R.sub.1 is hydrogen or C.sub.1-6 alkyl,

R.sub.2 is mono- or polyhydroxyalkyl,

R.sub.3 is hydrogen or C.sub.1-6 alkyl,

R.sub.4 is mono- or polyhydroxyalkyl,

R.sub.5 is C.sub.1-6 alkyl or monohydroxy-C.sub.1-6 -alkyl or C.sub.1-3 -alkoxy-C.sub.1-3 -alkyl, and

R.sub.6 is hydrogen or C.sub.1-6 alkyl or mono-.

2. 5-Methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-dihydroxypropyl)]diamide, a compound of claim 1.

3. 5-(S-2-Hydroxypropionylamino)-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-dihydroxypropyl)]diamide, a compound of claim 1.

4. 5-Methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2-hydroxy-1-hydroxymethylethyl)]diamide, a compound of claim 1.

5. The compound of claim 1, wherein at least one of R.sub.1, R.sub.2, R.sub.3 or R.sub.4 is dihydroxyalkyl.

6. A compound of claim 5, wherein at least one of R.sub.1 or R.sub.2 is dihydroxyalkyl and at least one of R.sub.3 and R.sub.4 is dihydroxyalkyl.

7. A compound of claim 5 or 6 wherein all alkyl moieties in R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have three carbon atoms.

8. A pharmaceutical composition for use as an X-ray contrast agent comprising a radiopaque amount of a compound of Claim 1 and a pharmaceutically acceptable carrier.

9. A method of conducting a radiological examination of a patient which comprises administering to the patient a radiopaque amount of a compound of claim 1.

10. 5-Acetylamino-2,4,6-triiodoisophthalic Acid [(2,3-dihydroxypropyl)-(2,3-dihydroxy-N-methyl-propyl)]diamide.

11. A compound of claim 1 wherein R.sub.5 is methoxymethyl 1-hydroxyethyl or methyl.

12. A compound of claim 1, wherein R.sub.1 and R.sub.3 each are H or CH.sub.3, and R.sub.2 and R.sub.4 each are --CH.sub.2 --CHOH--CH.sub.2 OH or ##STR9##

13. A composition of claim 8 wherein the carrier is pharmaceutically acceptable for angiography.

14. A method of claim 9, wherein the radiological examination is angiography.

15. A compound of claim 11, wherein R.sub.6 is H or C.sub.1-4 -alkyl.

For more information try a trial or see the plans and pricing

Serving hundreds of leading biopharmaceutical companies globally:

AstraZeneca
Fuji
Healthtrust
Federal Trade Commission
Julphar
Mallinckrodt
Queensland Health
Cantor Fitzgerald
Deloitte

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

botpot