IP Library Granted Patent US 8,399,507
Granted Patent B2
US 8,399,507 · App. 12/738,857 · Granted Mar 19, 2013

Antidiabetic tricyclic compounds

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Quick Facts
Patent No.
US 8,399,507
App. No.
12/738,857
Granted
Mar 19, 2013
Kind
B2
Abstract

Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Claims (26)

1. A compound which is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method of treating type 2 diabetes mellitus in a patient in need of treatment comprising the administration to the patient of a therapeutically effective amount of compound of claim 1 , or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising

(1) a compound of claim 1 or a pharmaceutically acceptable salt thereof;

(2) one or more compounds selected from the group consisting of:

(a) PPAR gamma agonists and partial agonists;

(b) biguanides;

(c) protein tyrosine phosphatase-1B (PTP-1B) inhibitors;

(d) dipeptidyl peptidase IV (DP-IV) inhibitors;

(e) insulin or an insulin mimetic;

(f) sulfonylureas;

(g) α-glucosidase inhibitors;

(h) agents which improve a patient's lipid profile, said agents being selected from the group consisting of (i) HMG-CoA reductase inhibitors, (ii) bile acid sequestrants, (iii) nicotinyl alcohol, nicotinic acid or a salt thereof, (iv) PPARα agonists, (v) cholesterol absorption inhibitors, (vi) acyl CoA:cholesterol acyltransferase (ACAT) inhibitors, (vii) CETP inhibitors, and (vii) phenolic anti-oxidants;

(i) PPARα/γ dual agonists,

(j) PPARδ agonists,

(k) antiobesity compounds,

(l) ileal bile acid transporter inhibitors;

(m) anti-inflammatory agents;

(n) glucagon receptor antagonists;

(o) GLP-1;

(p) GIP-1;

(q) GLP-1 analogs; and

(r) HSD-1 inhibitors; and

(3) a pharmaceutically acceptable carrier.

Assignments (5)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2010
From: LIANG, GUI-BAI; LIAO, XIBIN; LIU, WEIGUO; FINKE, PAUL E.; KIM, DOOSEOP; YANG, LIHU; LIN, SONGNIAN
To: MERCK & CO., INC.
Reel/Frame 024257/0954 →
CHANGE OF NAME Recorded Apr 20, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP
Reel/Frame 024258/0056 →