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Last Updated: December 18, 2025

Claims for Patent: 8,247,415


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Summary for Patent: 8,247,415
Title:Hydroxymethyl pyrrolidines as β3 adrenergic receptor agonists
Abstract:The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
Inventor(s):Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-ming Shen, Liping Wang, Cheng Zhu
Assignee:Merck Sharp and Dohme LLC
Application Number:US12/417,239
Patent Claims: 1. A compound of Formula Ia, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof: wherein n is 0, 1 or 2; Y is selected from the group consisting of methylene, —CH(CH3)— and a bond; Z is selected from the group consisting of R3 is selected from the group consisting of: (1) methyl, (2) oxo, and (3) —NH2.

2. The compound of claim 1 wherein Z is selected from the group consisting of:

3. The compound of claim 2, wherein n is 1; Y is a bond; Z is R3 is oxo.

4. A compound of claim 1 selected from the group consisting of: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable stereoisomer thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof.

5. A compound of claim 4, wherein the compound is selected from the group consisting of: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable stereoisomer thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof.

6. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

7. A method for the treatment or prevention of a disease or disorder selected from the group consisting of (1) overactive bladder, (2) urinary incontinence, (3) urge urinary incontinence, and (4) urinary urgency, wherein said method comprises administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1.

8. A method for the treatment or prevention of a disease or disorder selected from the group consisting of (1) overactive bladder, (2) urinary incontinence, (3) urge urinary incontinence, and (4) urinary urgency, wherein the method comprises administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 and a second active agent.

9. The method of claim 8, wherein the second active agent is a muscarinic receptor antagonist.

10. The compound of claim 1 having the following chemical structure: or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 having the following chemical structure: or a pharmaceutically acceptable salt thereof.

12. A compound having the following chemical structure:

13. A compound having the following chemical structure:

14. A pharmaceutical composition comprising a compound of claim 1, a second active agent and a pharmaceutically acceptable carrier.

15. The pharmaceutical composition of claim 14, wherein the second active agent is a muscarinic receptor antagonist.

16. The pharmaceutical composition of claim 15, wherein the second active agent is a tolterodine.

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