.

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

Details for Patent: 7,393,861

« Back to Dashboard

Details for Patent: 7,393,861

Title:Derivatives of 4-aminopiperidine and their use as a medicament
Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula ##STR00001## in which R.sub.1, R.sub.2 and R.sub.3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
Inventor(s): Thurieau; Christophe (Paris, FR), Gonzalez; Jerome (Annemasse, FR), Moinet; Christophe (Montreal, CA)
Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.) (Paris, FR) N/A (N/A)
Filing Date:May 04, 2005
Application Number:11/122,293
Claims:1. A compound of the formula ##STR01216## in racemic, enantiomeric form or all combinations of these forms wherein R.sub.1 is --(CH.sub.2).sub.m-Z.sub.12 wherein Z.sub.12 is aryl optionally substituted by at least one member independently selected from the group consisting of fluoro, chloro, bromo, iodo, alkyl and alkoxy, R.sub.2 is --C(Y)NHX.sub.1, Y is oxygen or sulfur; X.sub.1 is --(CH.sub.2).sub.p-Z.sub.22 wherein Z.sub.22 is aryl optionally substituted by at least one member selected from the group consisting of fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, CF.sub.3, OCF.sub.3, nitro, cyano, azido, piperidinosulfonyl, --C(O)--O-alkyl, --C(O)-alkyl, and phenyl, R.sub.3 is alkyl, m is 1; p is 0; and their non-toxic pharmaceutically acceptable acid addition salts.

2. A compound of claim 1 wherein R.sub.1 is --(CH.sub.2).sub.m-Z.sub.12 wherein Z.sub.12 is selected from the group consisting of naphthyl, bis-phenyl, substituted by oxy or phenyl, optionally substituted by at least one member selected from the group consisting of bromo, fluoro, chloro, alkyl, alkoxy, CF.sub.3 and OCF.sub.3.

3. A compound of claim 1 wherein R.sub.2 is --C(Y)NHX.sub.1, X.sub.1 is --(CH.sub.2).sub.p-Z.sub.22, Z.sub.22 is selected from the group consisting of bis-phenyl, or phenyl and naphthyl, all optionally substituted by at least one member selected from the group consisting of fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, CF.sub.3, OCF.sub.3, nitro, cyano, azido, piperidinosulfonyl, --C(O)--O-alkyl, --C(O)-alkyl and phenyl.

4. A compound of claim 1 wherein R.sub.3 is methyl.

5. A process for the preparation, in liquid phase, of a compound of claim 1 comprising reducing amination of a N-substituted piperidone of the formula ##STR01217## wherein R is methyl or Boc, in the presence of an amine of the formula R.sub.1NH.sub.2 wherein R.sub.1 has the meaning of claim 1 to obtain the compound of the formula ##STR01218## and reacting the latter with a compound of the formula X.sub.1NC(Y) wherein X.sub.1 and Y have the meaning of claim 1 to obtain a compound of the formula ##STR01219## which compound is a compound of formula I wherein R.sub.3 is Me.

6. The process, in solid phase, for a compound of claim 1 comprising reducing amination of a ketonic resin of the formula ##STR01220## in the presence of an amine of the formula R.sub.1NH.sub.2 wherein R.sub.1 has the meaning of claim 1 to obtain the compound of the formula ##STR01221## reacting the latter with a compound of the formula X.sub.1NC(O) wherein X.sub.1 has the meaning of claim 1 to obtain a compound of the formula ##STR01222## reacting the latter with a compound of the formula R.sub.3X wherein R.sub.3 is as defined in claim 1 and X is Br or I, followed by cleavage of the resin to obtain the corresponding compound of formula I.

7. A pharmaceutical composition containing, as active ingredient, a compound of claim 1, in combination with a pharmaceutically acceptable support.

8. A composition for treating acromegalia, hypophyseal adenomas and endocrine gastroenteropancreatic tumors comprising an effective amount of a compound of claim 1 and a pharmaceutical carrier.

9. A method of treating acromegalia, hypophyseal adenomas and endocrine gastroenteropancreatic tumors in warm-blooded animals comprising administering to warm-blooded animals in need thereof an effective amount of a compound of claim 1.
« 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