Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
摘要:
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.
Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
摘要:
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.
申请人:NATIONAL INSTITUTE OF INFORMATION AND COMMUNICATIONS
TECHNOLOGY
公开号:US20210032228A1
公开(公告)日:2021-02-04
The present invention provides an electro-optic polymer (EO polymer) comprising an electro-optic molecule (EO molecule) and a base polymer. The EO polymer of the present invention has good performance over the entire optical communication wavelength range and therefore can preferably be used for the production of optical modulators, optical switches, optical transceivers, optical phased arrays, LiDAR (light detection and ranging) devices, electric field sensors, terahertz wave generators and detectors, etc.
π電子供与体とπ電子受容体がπ共役ブリッジを介して共役した電気光学分子とベースポリマーを含み、光通信波長帯全域(波長1260nm~1625nm)での、電気光学係数(EO係数)が30pm/V以上であり、かつ、下記数式で定義される性能指数(Figure of Merit:FOM)が10×10-6cm/dBV以上である、電気光学ポリマー。本発明の電気光学ポリマーは、光通信波長帯全域における性能に優れることから、光変調器、光スイッチ、光トランシーバー、光フェーズドアレイ、LiDAR(Light and Detection and Ranging)、電界センサー、又はテラヘルツ発生・検出装置等に好適に用いることができる。〔式中、n:屈折率、r:EO係数、a max:使用波長帯での吸収係数の最大値、λ:波長〕
Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
作者:Jae-Kyu Jung、Benjamin R. Johnson、Tracy Duong、Marc Decaire、Jane Uy、Tawfik Gharbaoui、P. Douglas Boatman、Carleton R. Sage、Ruoping Chen、Jeremy G. Richman、Daniel T. Connolly、Graeme Semple
DOI:10.1021/jm070022x
日期:2007.4.1
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.