.

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: 5,270,317

« Back to Dashboard

Claims for Patent: 5,270,317

Title: N-substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present
Abstract:The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula ##STR1## in which the substituents are as defined in the specification. Application: Angiotensin II antagonists
Inventor(s): Bernhart; Claude (Saint Gely du Fesc, FR), Breliere; Jean-Claude (Montpellier, FR), Clement; Jacques (Saussan, FR), Nisato; Dino (Saint Georges d'Orques, FR), Perreault; Pierre (Montpellier, FR), Muneaux; Claude (Les Matelles, FR), Muneaux; Yvette (Les Matelles, FR)
Assignee: Elf Sanofi (Paris, FR)
Application Number:07/794,497
Patent Claims: 1. A compound of the formula ##STR43## in which: R.sub.1 and R.sub.2 are similar or different and are each independently hydrogen or a group selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.4 alkoxy, an amino, an aminomethyl, a carboxyl, an alkoxycarbonyl in which the alkoxy is C.sub.1 -C.sub.4, a cyano, a tetrazolyl, a methyltetrazolyl, a methylsulfonylamino, a trifluoromethylsulfonylamino, a trifluoromethylsulfonylaminomethyl, an N-cyanoacetamide, an N-hydroxyacetamide, an N-(4-carboxy-1,3-thiazol-2-yl)acetamide, a ureido, a 2-cyanoguanidinocarbonyl, a 2-cyanoguanidinomethyl, an imidazol-1-ylcarbonyl and a 3-cyano-2-methylisothioureidomethyl, with the proviso that at least one of the substituents R.sub.1 or R.sub.2 is other than hydrogen;

R.sub.3 is a hydrogen, a C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by one or more halogen atoms, a C.sub.2 -C.sub.6 alkenyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl, a phenylalkyl in which the alkyl is C.sub.1 -C.sub.3, or a phenylalkenyl in which the alkenyl is C.sub.2 -C.sub.3, said phenyl groups being unsubstituted or monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.1 -C.sub.4 halogenoalkyl, a C.sub.1 -C.sub.4 polyhalogenoalkyl, a hydroxyl or a C.sub.1 -C.sub.4 alkoxy; and

either

R.sub.4 and R.sub.5 are each independently a C.sub.1 -C.sub.6 alkyl, a phenyl or a phenylalkyl in which the alkyl is C.sub.1 -C.sub.3, said alkyl, phenyl and phenylalkyl groups being unsubstituted or substituted by one or more halogen atoms or by a group selected from a C.sub.1 -C.sub.4 perfluoroalkyl, a hydroxyl and a C.sub.1 -C.sub.4 alkoxy;

or R.sub.4 and R.sub.5 together form a group of the formula .dbd.CR.sub.7 R.sub.8, in which R.sub.7 is hydrogen, a C.sub.1 -C.sub.4 alkyl or a phenyl and R.sub.8 is a C.sub.1 -C.sub.4 alkyl or a phenyl;

or else R.sub.4 and R.sub.5 together are either a group of the formula (CH.sub.2).sub.n or a group of the formula (CH.sub.2).sub.p Y-(CH.sub.2).sub.q, in which Y is either an oxygen atom, or a sulfur atom, or a carbon atom substituted by a C.sub.1 -C.sub.4 alkyl group, a phenyl or a phenylalkyl in which the alkyl is C.sub.1 -C.sub.3, or a group N--R.sub.6, in which R.sub.6 is a hydrogen, a C.sub.1 -C.sub.4 alkyl, a phenylalkyl in which the alkyl is C.sub.1 -C.sub.3, a C.sub.1 -C.sub.4 alkylcarbonyl, a C.sub.1 -C.sub.4 halogenoalkylcarbonyl, a C.sub.1 -C.sub.4 polyhalogenoalkylcarbonyl, a benzoyl, an alpha-aminoacyl or an N-protecting group, or R.sub.4 and R.sub.5, together with the carbon atom to which they are bonded, form an indane or an adamantane;

p+q=m;

n is an integer between 2 and 11; and

m is an integer between 2 and 5; or

R.sub.4 is a C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by one or more halogen atoms; and

R.sub.5 is a cycloalkyl or a cycloalkylmethyl, the cycloalkyl being C.sub.3 -C.sub.7, which is unsubstituted or substituted by one or more halogen atoms;

or R.sub.4 and R.sub.5 are each a cyclopropyl;

X is an oxygen atom or sulfur atom; and

z and t are zero or one is zero and the other is one; and its salts.

2. A compound according to claim 1 wherein R.sub.1 is in the ortho position and is a carboxyl or tetrazolyl group and R.sub.2 is hydrogen.

3. A compound according to claim 1 wherein R.sub.4 and R.sub.5 form a cyclopentane or a cyclohexane with the carbon to which they are bonded.

4. A compound according to claim 1 wherein R.sub.4 is methyl and R.sub.5 is cyclohexyl.

5. A compound according to claim 1 wherein R.sub.3 is a linear C.sub.1 -C.sub.6 alkyl group.

6. A compound according to claim 1 wherein X is oxygen.

7. A compound according to claim 1 wherein z=t=0.

8. A compound according to claim 1 which is 2-n-butyl-4-spirocyclopentane-1-[(2'-(tetrazol-5-yl)biphenyl-4-yl)methyl]- 2-imidazolin-5-one or one of its salts with acids or bases.

9. A compound according to claim 1 which is 2-n-butyl-4-methyl-4-cyclohexyl-1-[(2'-(tetrazol-5-yl)biphenyl-4-yl)methyl ]-2-imidazolin-5-one or one of its salts with acids or bases.

10. A pharmaceutical composition in which a compound according to claim 1 is present as the active principle.

11. A pharmaceutical composition in which 0.1 to 1000 mg of a compound according to claim 1 is present in associated with a beta-blocking compound.

12. A pharmaceutical composition in which 0.1 to 1000 mg of a compound according to claim 1 is present in associated with a diuretic.

13. A pharmaceutical composition in which 0.1 to 1000 mg of a compound according to claim 1 is present in association with a non-steroidal antiinflammatory.

14. A pharmaceutical composition in which 0.1 to 1000 mg of a compound according to claim 1 is present in association with a calcium antagonist.

15. A pharmaceutical composition in which 0.1 to 1000 mg of a compound according to claim 1 is present in association with a tranquilizer.
« Back to Dashboard

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

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