.

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: 4,277,479

« Back to Dashboard

Claims for Patent: 4,277,479

Title: Tetrazolylalkoxycarbostyril derivatives and pharmaceutical compositions containing them
Abstract:Novel tetrazolylalkoxycarbostyril derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a low alkenyl group, a lower alkanoyl group, a benzoyl group or phenylalkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## R.sup.3 is a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, a phenyl group or a phenylalkyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is either single or double bond; and the substituted position of a group of the formula, ##STR3## in the carbostyril skeleton is either 4-, 5-, 6-, 7- or 8-position provided that the only one such group of the formula can be substituted in the whole carbostyril skeleton, thus when R.sup.2 in 4-position is a group of the formula ##STR4## then 5-, 6-, 7- or 8-position will have no such substituted group; furthermore, the phenyl group in the above-mentioned benzoyl group, phenylalkyl group or phenyl group may have substituted group(s). The above-mentioned novel tetrazolylalkoxycarbostyril derivatives have pharmacological activities such as platelet aggregation inhibitory action, antiinflammatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful as anti-thrombosis agent, cerebral blood flow improving agent, antiinflammatory agent, antiulcer agent, anti-hypertensive agent and anti-asthmatic agent.
Inventor(s): Nishi; Takao (Tokushima, JP), Nakagawa; Kazuyuki (Tokushima, JP)
Assignee: Otsuka Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:06/070,710
Patent Claims: 1. A compound of the general formula, ##STR15## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkanoyl group, a benzoyl group or a phenyl-C.sub.1-4 alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR16## R.sup.3 is a lower alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl group, a phenyl group or a phenyl-C.sub.1-4 alkyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is either single or double bond; and the substituted position of the group represented by the formula, ##STR17## in the carbostyril skeleton is either 4-, 5-, 6-, 7- or 8-position provided that only one such group of the formula can be substituted in the whole carbostyril skeleton, thus when R.sup.2 in 4-position is ##STR18## then 5-, 6-, 7- or 8-position will have no such substituted group; furthermore, the phenyl group in the above-mentioned benzoyl group, phenyl-C.sub.1-4 alkyl group or phenyl group may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy.

2. A compound of the general formula (I) according to claim 1, wherein the substituted position of the group of the formula ##STR19## is 5-position of the carbostyril skeleton.

3. A compound of the general formula (I) according to claim 2, wherein R.sup.3 is a C.sub.3-8 cycloalkyl group or a C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl group.

4. A compound of the general formula (I) according to claim 2, wherein R.sup.3 is a phenyl-C.sub.1-4 alkyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy, a phenyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy or a lower alkyl group.

5. A compound of the general formula (I) according to claim 1, wherein the substituted position of the group of the formula ##STR20## is 6-position of the carbostyril skeleton.

6. A compound of the general formula (I) according to claim 5, wherein R.sup.3 is a C.sub.3-8 cycloalkyl group or a C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl group.

7. A compound of the general formula (I) according to claim 5, where R.sup.3 is a phenyl-C.sub.1-4 alkyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy, a phenyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy, or a lower alkyl group.

8. A compound of the general formula (I) according to claim 1, wherein the substituted position of the group of the formula ##STR21## is 4-, 7- or 8-position of the carbostyril skeleton.

9. A compound of the general formula (I) according to claim 8, wherein R.sup.3 is a C.sub.3-8 cycloalkyl group or a C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl group.

10. A compound of the general formula (I) according to claim 8, where R.sup.3 is a phenyl-C.sub.1-4 alkyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy, a phenyl group which may have substituted group(s) selected from the group consisting of lower alkoxy, lower alkyl, halogen, di-lower alkylamino, nitro, and lower alkenedioxy or a lower alkyl group.

11. 6-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]carbostyril.

12. 6-[3-(1-Benzyltetrazol-5-yl)propoxy]carbostyril.

13. 5-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]-3,4-dihydrocarbostyril.

14. 6-[3-(1-Phenyltetrazol-5-yl)propoxy]carbostyril.

15. 4-Methyl-6-[3-(1-cyclohexyltetrazol-5-yl)-propoxy]carbostyril.

16. 6-[3-(1-Cyclohexylmethyltetrazol-5-yl)propoxy]-carbostyril.

17. 6-[3-(1-Cyclooctyltetrazol-5-yl)propoxy]-carbostyril.

18. 6-[3-(1-Cyclopentyltetrazol-5-yl)propoxy]-carbostyril.

19. 6-[4-(1-Cyclohexyltetrazol-5-yl)butoxy]carbostyril.

20. 6-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]-3,4-dihydrocarbostyril.

21. 6-[3-(1-Cyclohexylmethyltetrazol-5-yl)propoxy]-3,4-dihydrocarbostyril.

22. 7-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]-3,4-dihydrocarbostyril.

23. 8-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]-3,4-dihydrocarbostyril.

24. 4-[3-(1-Cyclohexyltetrazol-5-yl)propoxy]-carbostyril.

25. A platelet aggregation inhibitor composition containing as an active ingredient a pharmacologically effective amount of a compound of the formula (I) of claim 1 and a pharmaceutically acceptable carrier.

26. A phosphodiesterase inhibitor composition containing as an active ingredient a pharmacologically effective amount of a compound of the formula (I) of claim 1 and a pharmaceutically acceptable carrier.

27. A cerebral blood flow improver composition containing as an active ingredient a pharmacologically effective amount of a compound of the formula (I) of claim 1 and a pharmaceutically acceptable carrier.

28. An anti-hypertensive agent composition containing as an active ingredient a pharmacologically effective amount of a compound of the formula (I) of claim 1 and a pharmaceutically acceptable carrier.
« 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