.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

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

DrugPatentWatch Database Preview

Claims for Patent: 6,417,175

« Back to Dashboard

Claims for Patent: 6,417,175

Title: Phosphonocephem derivatives, process for the preparation of the same, and use thereof
Abstract:A novel cephem compound of the formula: ##STR1## wherein R.sup.1 is a phosphono group or a group convertible to a phosphono group; R.sup.2 is a hydrogen atom or a group having a linkage through a carbon atom; each of Q and X is a nitrogen atom or CH; Y is S, O or CH.sub.2 ; n is 0 or 1; one of R.sup.3 and R.sup.4 is a pyridinium group which may be substituted and the other is a hydrogen atom or hydrocarbon group which may be substituted, or R.sup.3 and R.sup.4 taken together may form a quaternalized nitrogen-containing heterocyclic ring which may be substituted, or its ester or its salt, which has a superior anti-bacterial activity, stability, absorbability, etc., a production thereof and a pharmaceutical composition containing it, is provided.
Inventor(s): Ishikawa; Tomoyasu (Otsu, JP), Hashiguchi; Shohei (Toyonaka, JP), Iizawa; Yuji (Muko, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:09/555,949
Patent Claims: 1. A compound of the formula: ##STR20##

wherein R.sup.1 is a phosphono group;

R.sup.2 is a hydrogen atom, an optionally substituted C.sub.1-6 alkyl group or a C.sub.3-5 cycloalkyl group;

each of Q and X is a nitrogen atom or CH;

Y is S;

n is 0 or 1;

one of R.sup.3 and R.sup.4 is a pyridinium group which may be substituted and the other is a hydrogen atom or a hydrocarbon group which may be substituted, or R.sup.3 and R.sup.4 taken together may form a quaternized nitrogen-containing heterocyclic ring which may be substituted,

wherein when R.sup.3 and R.sup.4 are taken together, the group of the formula ##STR21##

wherein R.sup.5 is an optionally substituted hydrocarbon group; or salt thereof.

2. 7.beta.-[2(Z)-ethoxyimino-2-(5-phosphonoamino-1,2,4-thiadiazole-3-yl)aceta mido]-3-[4-(1-methyl-4-pyridinio)-2-thiazolylthio]-3-cephem-4-carboxylate.

3. A method for producing a pharmaceutical composition comprising

mixing a compound of claim 1 with a pharmaceutically acceptable carrier, diluent or bulking agent.

4. 7.beta.-[2(Z)-ethoxyimino-2-(5-phosphonoamino 1,2,4-thiadiazole-3-yl)acetamido]-3-[4-(1-methyl-4-pyridinio)-2-thiazolyth io]-3-cephem-4-carboxylate or its salt.

5. A method for treating a bacterial infection which comprises administering an effective amount of a compound as claimed in claim 1 to a patient suffering from the bacterial infection.

6. A method for treating a bacterial infection which comprises administering an effective amount of a compound as claimed in claim 1 together with at least one of pharmaceutically acceptable carriers, diluents and excipients to a patient suffering from the bacterial infection.

7. A method as claimed in claim 5, wherein the bacterial infection is a MRSA infection.

8. A compound as claimed in claim 1, wherein R.sup.3 is a pyridinium group which may be substituted and R.sup.4 is a hydrogen atom.

9. A compound as claimed in claim 1, wherein Q is a nitrogen atom.

10. A compound as claimed in claim 1, wherein X is a nitrogen atom.

11. A compound as claimed in claim 1, wherein n is 0.

12. A method for treating a bacterial infection which comprises administering an effective amount of a compound as claimed in claim 4 to a patient suffering from the bacterial infection.

13. A compound as claimed in claim 1, which is 7.beta.-[2(Z)-fluoromethoxyimino-2-(5phophonoamino-1,2,4-thiadiazole-3-yl) acetamido]-3-[4-(1-methyl-4-pyridinio)-2-thiazolylthio]-3-cephem-4carboxyla te or its salt.

14. A method for producing a compound as claimed in claim 1, which comprises reacting a compound of the formula: ##STR22##

or its salt;

wherein each symbol has the meaning given in claim 1; with a compound of the formula: ##STR23##

its salt or its reactive derivative;

wherein each symbol has the meaning given in claim 1.

15. A method as claimed in claim 5, wherein the compound is administered by injection.

16. A method for treating a bacterial infection which comprises administering an effective amount of a compound as claimed in claim 4 together with at least one of pharmaceutically acceptable carriers, diluents and excipients to a patient suffering from the bacterial infection.

17. A pharmaceutical composition containing the compound shown in claim 1 and at least one of pharmaceutically acceptable carriers, diluents and bulking agents.

18. A pharmaceutical composition containing the compound of claim 4 and at least one of pharmaceutically acceptable carriers, diluents and bulking agents.

19. A method for producing a pharmaceutical composition comprising mixing a compound of claim 4 with a pharmaceutically acceptable carrier, diluent or bulking agent.

20. A method as claimed in claim 12, wherein the compound is administered by injection.

21. A method as claimed in claim 12, wherein the bacterial infection is a MRSA infection.
« Back to Dashboard

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

How are People Using DrugPatentWatch?

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.

`abc