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US 2008/0076810 A1Published application
Benzoureas Having Anti-Diabetic Activity
OwnerWeiguo Lui, Harold B. Wood +1inventors
InventorsWeiguo Lui, Harold B. Wood, Fiona Wai-Yu Lau-Phua
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Abstract
Benzourea compounds of Formula I having aryl-(CH2)x-oxazolidinedione or aryl-(CH2)x-thiazolidinedione substituents on one of the N atoms of the benzourea ring, wherein x is 0 or 1, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia and other symptoms such as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity, that are often associated with type 2 diabetes.
Claims19
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is —X-Aryl-Y-Z, wherein Aryl is optionally substituted with 1-3 groups independently selected from A;
- Aryl is phenyl or naphthyl;
- X and Y are each independently selected from the group consisting of a bond and —CR4R5—;
- Z is
- Q is selected from the group consisting of S and O;
- A is selected from the group consisting of C1-C4 alkyl, C2-C4 alkenyl, —OC1-C4 alkyl, and halogen, wherein alkyl, alkenyl, and —Oalkyl are each optionally substituted with 1-5 halogens;
- R2 is selected from the group consisting of
- (a) Benzisoxazolyl,
- (b) Aryl,
- (c) —(CH2)Aryl,
- (d) —(C═O)Aryl, and
- (e) benzothiazolyl, wherein
- R2 is optionally substituted with 1-3 substituent groups independently selected from halogen, C1-C3 alkyl, and —OC1-C3 alkyl, wherein C1-C3 alkyl and —OC1-C3 alkyl are optionally substituted with 1-5 halogens;
- R3 is selected from the group consisting of halogen, C1-C3 alkyl, and —OC1-C3 alkyl, wherein C1-C3 alkyl and —OC1-C3 alkyl are optionally substituted with 1-5 halogens;
- R4 and R5 are each independently selected from the group consisting of hydrogen, halogen, C1-C3 alkyl, and —OC1-C3 alkyl, wherein C1-C3 alkyl and —OC1-C3 alkyl are optionally substituted with 1-5 halogens;
- R6 is selected from the group consisting of H, C1-C3 alkyl, and halogen, wherein C1-C3 alkyl is optionally substituted with 1-3F;
- and
- p is an integer from 0 to 4.
16 more elements
(canceled)
Dependencies are inferred from the claim text.