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Cannabinoid receptor ligands and uses thereof

A halogen, compound technology, applied in diseases and/or disorders, CB1 receptor antagonists, treatment of diseases regulated by cannabinoid receptor antagonists, can solve problems such as liver toxicity in patients

Inactive Publication Date: 2006-07-26
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Current treatments for alcohol abuse or alcohol dependence often leave patients suffering from non-adherence or possible hepatotoxicity; thus, there is an unmet need for more effective treatments for alcohol abuse / dependence

Method used

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  • Cannabinoid receptor ligands and uses thereof
  • Cannabinoid receptor ligands and uses thereof
  • Cannabinoid receptor ligands and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0178] 2-(2-Chloro-phenyl)-5-isopropyl-3-(4-methoxy-phenyl)-5,6-dihydro-2H-pyrrolo[3,4-c]pyr Preparation of oxazol-4-one (1A-1):

[0179]

[0180] 2-(2-Chloro-phenyl)-3-iodo-5-isopropyl-5,6-dihydro-2H-pyrrolo[3,4-c]pyrazol-4-one purged with nitrogen I-1a (50 mg), cesium fluoride (38 mg), 3-methoxyphenylboronic acid (74 mg) and 1,2-dimethoxy The solution in ethane (1 mL) was stirred at 100°C in a sealed vial for 7 hours. The reaction was cooled and partitioned between ethyl acetate / water. The organic phase was dried (Na 2 SO 4 ), and concentrated in vacuo to give an oil. Silica gel chromatography (25% to 35% ethyl acetate: hexane) gave the title compound (1A-1) as an off-white solid, 27 mg. in CDCl 3 (ppm) in

[0181] h 1 NMR: δ7.56-7.40 (m, 6H), 6.80 (d, 2H), 4.63 (m, 1H), 4.38 (br d, 2H), 1.25 (d, 6H); ms (LCMS) m / z = 382.3 (M+1).

[0182] Using methods similar to those described above for the synthesis of compound 1A-1, the following compounds listed in Tab...

Embodiment 2

[0191] Using methods similar to those described above for the synthesis of compound 1A-1 and outlined in Scheme II above, using suitable starting materials either commercially available or prepared using formulations well known to those skilled in the art, the following Compounds listed in Table 2A.

[0192] Table 2A

[0193]

[0194]

Embodiment 3

[0196] Compounds were synthesized using a method similar to that described above for 1A-1 The following compounds listed in Table 3A were prepared using the appropriate starting materials, either commercially available or prepared using formulations well known to those skilled in the art, as outlined in Scheme IV above.

[0197] Table 3A

[0198]

[0199]

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PUM

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Abstract

Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.

Description

field of invention [0001] The present invention relates to bicyclic pyrazolyl and imidazolyl compounds that are ligands for cannabinoid receptors, especially CB1 receptor antagonists, and their use in the treatment of diseases, conditions and / or disorders modulated by cannabinoid receptor antagonists. Background technique [0002] Obesity is a major public health concern due to its increasing prevalence and associated health risks. Obesity and overweight are often defined by body mass index (BMI), which is related to total body fat and used to assess relative risk of disease. BMI is calculated by dividing weight in kilograms by the square of height in meters (kg / m 2 ). Overweight is typically defined as a BMI of 25-29.9 kg / m 2 , obesity is typically defined as a BMI of 30kg / m 2 . See, e.g., National Heart, Lung, and Blood Institute, "Clinical Guidelines on the Identification, Evaluation, and Treatment of Overweight and Obesity in Adults," The Evidence Report, Washingto...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D487/04A61P3/04A61K31/4745C07D471/02
CPCC07D471/04C07D487/04A61P1/04A61P1/14A61P15/10A61P25/08A61P25/16A61P25/18A61P25/24A61P25/28A61P25/30A61P25/32A61P25/34A61P29/00A61P3/04A61P43/00A61P3/10
Inventor 菲利普·A·卡皮诺罗伯特·L·道
Owner PFIZER PRODS ETAT DE CONNECTICUT
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