This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
However, TZDs and ISEs are generally ineffective in preventing the cardiovascular manifestations of Syndrome X because their administration fails to lower triglyceride and LDL-cholesterol levels while increasing HDL-cholesterol levels
In addition, side effects commonly associated with TZD treatment include severe weight gain and—in the case of troglitazone—hepatotoxicity
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0221] Compound 1(1)
[0222] Compound 1 shown below was prepared according to the following steps: Step A: Preparation:
[0223] To a suspension of 4-(4-hydroxyphenyl)butanylhydrazide (0.5 g, 2.58 mmol) in isopropanol (5 mL) was added 3-chlorobenzaldehyde (Aldrich, 420 mg, 3 mmol) followed by p-toluene Sulfonic acid (25 mg). The reaction was stirred at room temperature for 20 hours. A solid precipitated out which was filtered, washed with isopropanol (0.25 mL) and dried to give the product as a solid. MS: m / z (M + +1): 317
[0224] R
MS: m / z (M + +1)
3-Methylphenyl
297
Phenyl
283
2,4-Difluorophenyl
319
2-Methylphenyl
297
3-methoxyphenyl
313
[0225] To a solution of the product from Step A (650 mg, 2.05 mmol, Example 1) in 5 mL of a mixture of isopropanol, tetrahydrofuran and acetic acid (1:1:0.3) was added sodium cyanoborohydride (1.25 g, 20 mmol)....
Embodiment 2
[0236] Compound 2(1)
[0237] The compound represented by the following formula was prepared as follows: Step A: Preparation:
[0238] Add boron tribromide (50 g, 200 mmol) to CH in CH over 1 hour 2 Cl 2 To a cold (0°C) solution in (50 mL) was added dropwise methyl 4-(4-methoxyphenyl)butanoate (15.5 g, 74.4 mmol) in CH 2 Cl 2 (100mL). After continuing to stir at 0 °C for 1 hour, the reaction mixture was washed with 1:1 CH 3 OH:CH 2 Cl 2 (120 mL) and stirred overnight at room temperature. The mixture was concentrated to give an oil which was partitioned between ethyl acetate (150 mL) and water (150 mL). The aqueous layer was extracted with ethyl acetate (2×50 mL), and the combined organic extracts were washed with water (50 mL), brine (50 mL), and dried (Na 2 SO 4 ), followed by concentration to obtain the desired phenol as an oil. C 11 h 14 o 3 (MW=194.23); MS: m / z (M + +1)=195 Step B: Preparation:
[0239] The phenol (18.6 g, 96 mmo...
Embodiment 3
[0248] Compound 3(1) Step A: Preparation:
[0249] To a solution of the methyl ester—compound 2(1) (100 mg, 0.29 mmol) in DMF (2 mL) was added 3,4,5-trimethoxybenzyl chloride (129 mg, 0.6 mmol) and potassium carbonate powder (350 mg , 2.53 mmol), and the resulting mixture was heated at 45°C for 24 hours. After cooling to room temperature, the reaction mixture was diluted with water (10 mL) and extracted with ethyl acetate (3 x 3 mL). The combined organic extracts were concentrated to an oil and purified by flash chromatography (gradient elution, 1:4 EtOAc:Hexane - 4:1 EtOAc:Hexane) to afford the desired product as an oil thing. C 27 h 35 N 3 o 7 (MW=513.60); MS: m / z (M + +1)=514
[0250] R
MS: m / z (M + +1)
3,5-dimethoxyphenyl
484
4-biphenyl
500
3-Chlorophenyl
458
3-Chloro-4-methylphenyl
472
Bis-trifluoromethylphenyl
560
3,4-Difluorophenyl ...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
Abstract
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
Description
Background of the invention [0001] Peroxisome proliferator-activated receptors (PPARs), members of the nuclear hormone receptor superfamily, are ligand-activated transcription factors that regulate gene expression. A number of different PPAR isoforms have been discovered. These subtypes include PPARaα, NUC1, PPARγ and PPAR8. [0002] The PPARα receptor subtype has been reported to be activated by medium-chain and long-chain fatty acids. They are involved in stimulating β-oxidation of fatty acids and have activity as fibrates, which have been reported to significantly reduce plasma triglycerides and moderate low-density lipoprotein (LDL) cholesterol reduction. [0003] PPARα, PPARγ and PPAR8 receptors have been implicated in diabetes, cardiovascular disease, obesity, Syndrome X and gastrointestinal disorders such as inflammatory bowel disease. Syndrome X is a group of syndromes that includes hyperinsulinemia in combination with hypertension, weight gain, high triglycerides,...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More 
