.

Deeper Knowledge, Faster

  • Find suppliers and generic API sources
  • Uncover prior art in expired and abandoned patents
  • Drug patents in 130+ countries

► See Plans & Pricing

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

Serving 500+ biopharmaceutical companies globally:

Novartis
Baxter
US Army
Fuji
Farmers Insurance
Mallinckrodt
Healthtrust
QuintilesIMS
McKesson
Medtronic

Generated: July 22, 2017

DrugPatentWatch Database Preview

Claims for Patent: 5,776,944

« Back to Dashboard

Claims for Patent: 5,776,944

Title: 7-(4-aminomethyl-3-methyloxyiminopyrroplidin-1-yl)-1-cyclopropyl-6-flu oro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid and the process for the preparation thereof
Abstract:The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid represent by the following formula: ##STR1## or its isomer.
Inventor(s): Hong; Chang Yong (Daejeon, KR), Kim; Young Kwan (Daejeon, KR), Kim; Se Ho (Daejeon, KR), Chang; Jay Hyok (Daejeon, KR), Choi; Hoon (Daejeon, KR), Nam; Do Hyun (Daejeon, KR), Kim; Ae Ri (Daejeon, KR), Lee; Jin Hwa (Daejeon, KR), Park; Ki Sook (Daejeon, KR)
Assignee: LG Chemical Ltd. (Seoul, KR)
Application Number:08/825,992
Patent Claims: 1. 7-(4-aminomethyl -3-methyloxylminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid represents by the following formula: ##STR269## or a pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, or isomer thereof.

2. The compound according to claim 1 in the from of the Z isomer.

3. 7-(4-aminomethyl-3-methyloxylminopyrrolidin-1-yl)-1-cyclopropy l-6-fluoro-4-oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate or a hydrate thereof represented by the following formula: ##STR270## or its isomer, in which n denotes 0, 1, 1.5, 2, 2.5, 3, 3.5 or 4; or an isomer thereof.

4. The compound according to claim 3, wherein n is 3.

5. The compound according to claim 3, which has a moisture content of from 9 to 11% by weight.

6. The compound according to claim 3, wherein n is 1.5.

7. The compound according to claim 3, which has a moisture content of from 4 to 6% by weight.

8. A process for preparing 7-(4-aminomethyl-3-methyloxylminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid represented by the following formula: ##STR271## or its isomer, methanesulfonate and hydrate of the methanesulfonate, which comprises reacting a quinolone compound represented by the following formula, ##STR272## in which X represents a halogen, with a pyrrolidine oxime compound represented by the following formula, or a salt thereof. ##STR273## in a solvent in the presence of an acid acceptor.

9. The process of claim 8, wherein the ratio of the number of moles of the pyrrolidine oxime compound to the number of moles of the quinolone compound ranges from one(1), to ten(10).

10. The process of claim 8, wherein said solvent is selected from the group consisting of acetonitrile, dimethylformamide, dimethylsulfoxide, pyridine, N-methylpyrrolidinone, hexamethylphosphoramide, ethanol, and aqueous mixtures thereof .

11. The process of claim 8, wherein said acid acceptor is selected from inorganic bases consisting of sodium hydrogen carbonate and potassium carbonate and organic bases consisting of triethylamine, diisopropylethylamine, pyridine, N,N-dimethylaniline, N,N-dimethylaminopyridine, 1,8-diazabicyclo-undec-7-ene, and 1,4-diazabicyclo-octane.

12. The process of claim 8, wherein the reaction is carried out at a temperature ranging from room temperature to 200.degree. C.

13. An antibacterial composition comprising as an active component the compound defined in claim 1, together with a pharmaceutically acceptable carrier.

14. The composition of claim 13 comprising 1 to 100 mg of the compound in a unit dosage form.

15. An antibacterial composition comprising as an active component the compound defined in claim 3, together with a pharmaceutically acceptable carrier.

16. The composition of claim 15 comprising 1 to 100 mg of the compound in a unit dosage form.
« Back to Dashboard

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

Serving 500+ biopharmaceutical companies globally:

Fish and Richardson
Teva
Covington
Cerilliant
Johnson and Johnson
Cipla
Queensland Health
Argus Health
Colorcon
McKinsey

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.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted Heap | Mobile and Web Analytics

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot