.

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: 5,434,171

« Back to Dashboard

Claims for Patent: 5,434,171

Title: Preparation of 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates and intermediates
Abstract:This invention relates to a process for preparing certain 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates, intermediates, and congeners. Finally, the invention provides new 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates with formulations and methods for using the compounds.
Inventor(s): Frank; Scott A. (Lebanon, IN), Prather; Douglas E. (Brownsburg, IN), Ward; Jeffrey A. (Indianapolis, IN), Werner; John A. (Indianapolis, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:08/164,074
Patent Claims: 1. A crystalline compound of the Formula 20 ##STR14## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; Z1.sup.- is selected from the group consisting of hydrochloride, malate, and sesquimalate;

wherein when Z1.sup.- is sesquimalate then 3 molecules of malate are associated with 2 molecules of 20; and

when Z1.sup.- is hydrochloride then each molecule of 20 is solvated with one molecule of acetone.

2. A crystalline compound of claim 1 wherein Z1.sup.- is hydrochloride.

3. A crystalline compound of claim 1 wherein Z1.sup.- is sesquimalate.

4. A crystalline compound of claim 1 wherein the compound of Formula 1 is (2S, 3R, 4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-ph enylpropyl]amino]acetic acid 2-methylpropyl ester.

5. A crystalline compound of claim 2 wherein the compound is (2S, 3R, 4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-ph enylpropyl]-amino]acetic acid 2-methylpropyl ester hydrochloride acetone monosolvate.

6. A crystalline compound of claim 3 wherein the compound is (2S, 3R, 4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-ph enylpropyl]-amino]acetic acid 2-methylpropyl ester.

7. A crystalline compound of claim 1 wherein the compound is (2S, 3R, 4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-ph enylpropyl]-amino]acetic acid 2-methylpropyl ester malate.

8. A crystalline dihydrate compound of the Formula 5 ##STR15##

9. A compound of claim 8 wherein the crystalline dihydrate compound is at least 97% (2S,3R,4R)dihydrate.

10. A method for binding a peripheral opioid receptor in a patient which comprises administering to said patient an effective amount of a compound of claim 1.

11. A method for binding a peripheral opioid receptor in a patient which comprises administering to said patient an effective amount of a compound of claim 8.

12. A method for treating a condition selected from the group consisting of irritable bowel syndrome, idiopathic constipation, and non-ulcer dyspepsia; comprising administering an effective amount of a compound of claim 1.

13. A method for treating a condition selected from the group consisting of irritable bowel syndrome, idiopathic constipation, and non-ulcer dyspepsia; comprising administering an effective amount of a compound of claim 8.

14. A pharmaceutical formulation comprising an effective amount of a compound of claim 1 in combination with one or more pharmaceutically acceptable excipients.

15. A pharmaceutical formulation comprising an effective amount of a compound of claim 8 in combination with one or more pharmaceutically acceptable excipients.

16. A formulation of claim 15 wherein the formulation is a hard gelatin capsule.

17. A process for preparing a crystalline monohydrate compound of Formula 3 ##STR16## comprising the crystallization of 3 from a solvent comprised of about 50% methanol and about 50% water (by weight).
« 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