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Use of sulfonamide derivatives in the treatment of disordersof the metabolism and the nervous system

A technology of benzenesulfonamide and sulfonyl, which is applied in the application field of sulfonamide derivatives in the treatment of metabolic and nervous system diseases, and can solve the problems of limited use of peptides, difficulty in drug administration, and stability in vivo

Inactive Publication Date: 2009-04-08
SMITHKLINE BECKMAN CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of peptides in clinical therapy is severely limited due to difficult administration and in vivo stability

Method used

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  • Use of sulfonamide derivatives in the treatment of disordersof the metabolism and the nervous system
  • Use of sulfonamide derivatives in the treatment of disordersof the metabolism and the nervous system
  • Use of sulfonamide derivatives in the treatment of disordersof the metabolism and the nervous system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0508] Intermediate Example 1: 5-(Chlorosulfonyl)-2-methoxyphenyl methanesulfonate

[0509] a). Preparation of 2-methoxyphenyl methanesulfonate: Triethylamine ( 8.5 mL, 61.04 mmol) and methanesulfonyl chloride (4.72 mL, 61.04 mmol). After stirring for 2 h, the reaction was complete as shown by TLC. The reaction solution was diluted with saturated ammonium chloride and water, the organic phase was separated and concentrated in vacuo to an oil. The crude material was purified by silica gel chromatography eluting with ethyl acetate / hexanes. The desired product was obtained as a clear oil (7.5 g, 91% yield). 1 HNMR (DMSO-d6, 400MHz) δ: 7.31 (1H, dq), 7.28 (1H, dd), 7.19 (1H, dd), 6.97 (1H, dq), 3.82 (s, 3H), 3.32 (3H, s ).

[0510] b). Preparation of 5-(chlorosulfonyl)-2-methoxyphenyl methanesulfonate: To cooled (-10°C) chlorosulfonic acid (1 1.78mL, 176.5mmol) and 100mL DCM solution A solution of 2-methoxyphenyl methanesulfonate (7.13 g, 35.3 mmol) dissolved in 15 mL of DCM...

Embodiment 2

[0514] Example 2: 1-{[3,4-di(methoxy)phenyl]sulfonyl}-4-{[4-(1,3-oxazol-5-yl)phenyl]sulfonyl}piper Zinc

[0515] This compound was prepared as described in Example 1 except that 3-fluoro-4-(methoxy)benzenesulfonyl chloride was replaced by 4-(1,3-oxazol-5-yl)benzenesulfonyl chloride.

Embodiment 3

[0516] Example 3: 1-{[3,4-bis(methoxy)phenyl]sulfonyl}-4-{[4-methyl-2-(methoxy)phenyl]sulfonyl}piperazine

[0517] This compound was prepared as described in Example 1, except that 3-fluoro-4-(methoxy)benzenesulfonyl chloride was replaced by 4-methyl-2-(methoxy)benzenesulfonyl chloride.

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Abstract

The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same.

Description

field of invention [0001] The present invention generally relates to novel therapeutic compounds and AXOR 109 agonists and methods of their preparation and use. Background of the invention [0002] Diabetes is an ever-increasing threat to human health. For example, in the United States, it is currently estimated that about 16 million people have diabetes. [0003] Type II diabetes accounts for about 90-95% of diabetes cases and kills about 193,000 Americans each year. Type 2 diabetes is the seventh leading cause of all deaths. Type 2 diabetes currently affects 6% of the adult population in the Western world and is projected to increase worldwide by 6% per year. Although there are certain genetic traits that may predispose specific individuals to develop type 2 diabetes, the driving forces behind the current increase in incidence are increased sedentary lifestyles, diets and obesity, which is now prevalent in developed countries. About 80% of diabetics with type 2 diabete...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/132A61K31/135A61K31/145A61K31/353A61K31/357A61K31/36A61K31/40A61K31/4166A61K31/4184A61K31/422A61K31/4462A61K31/473A61K31/495A61K31/496A61K31/498
CPCA61K31/132A61K31/4995A61K31/353A61K31/551C07D207/48C07D241/50C07D295/26C07D265/36A61K31/496A61K31/135A61K31/538A61K31/4462C07D321/10C07D243/08A61K31/495A61K31/422C07D233/38C07D241/08A61K31/4184C07D319/18C07D487/08A61K31/4166C07D223/12C07D405/12C07D211/96A61K31/357A61K31/145A61K31/36C07D241/04C07D263/32C07D401/12A61K31/498C07C311/29A61K31/473A61K31/40A61K31/55A61P25/22A61P25/28A61P29/00A61P3/04A61P3/06A61P9/00A61P9/10A61P3/10C07D413/12
Inventor J·R·塞夫奇克C·P·劳德曼K·A·埃文斯李跃虎S·T·多克Z·陈
Owner SMITHKLINE BECKMAN CORP