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项与 Calyx Therapeutics, Inc. 相关的药物

CLX-0900

靶点-

作用机制

胰岛素增敏剂

在研机构-

原研机构

Calyx Therapeutics, Inc.

在研适应症-

非在研适应症

2型糖尿病 [+1]

最高研发阶段终止

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首次获批日期-

CLX-0301

靶点

Protein kinases

作用机制

蛋白激酶抑制剂

在研机构-

原研机构

Theracos, Inc.

在研适应症-

非在研适应症

糖尿病

最高研发阶段终止

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CLX-0101

靶点-

作用机制-

在研机构-

原研机构

Calyx Therapeutics, Inc.

在研适应症-

非在研适应症

2型糖尿病

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

100 项与 Calyx Therapeutics, Inc. 相关的临床结果

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0 项与 Calyx Therapeutics, Inc. 相关的专利（医药）

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2

项与 Calyx Therapeutics, Inc. 相关的文献（医药）

2003-09-01·Bioorganic & Medicinal Chemistry3区 · 医学

Synthesis and structure–Activity relationship studies of cinnamic acid-based novel thiazolidinedione antihyperglycemic agents

3区 · 医学

Article

作者: Gross, Coleman ; Gowri, Maya ; Sharma, Somesh D. ; Nag, Bishwajit ; Lakner, Fredrick J. ; Neogi, Partha ; Pickford, Lesley B. ; Cheng, Jin ; Medicherla, Satyanarayana ; Dey, Debendranath

A number of 2,4-thiazolidinedione derivatives of -phenyl substituted cinnamic acid were synthesized and studied for their PPAR agonist activity. The E-isomer of cinnamic acid, 11, showed moderate PPAR transactivation. The corresponding Z-isomer, 23, and double bond reduced derivative, 15, were found to be much less potent. Although the E-isomer showed a moderate PPAR gamma transactivation, it demonstrated a strong glucose-lowering effect in a genetic rodent model of diabetes. Results of pharmacokinetic, metabolism and permeability studies are consistent with 11 being an active prodrug with an active metabolite, 14, that has similar glucose lowering and PPAR gamma agonist properties.

Backbone modifications of 2,4-thiazolidinedione derivatives of α-phenyl acrylic esters and their effect on glucose uptake

作者: Peng, Ivan ; Neogi, Partha ; Pickford, Lesley ; Lee, Arthur ; Gross, Coleman

Our previous work has shown that 2,4-thiazolidinedione derivatives of E-α-Ph acrylic esters are potent antihyperglycemic agents with PPARγ agonist activity.To determine the contribution on antihyperglycemic activity of the α-Ph acrylic ester moiety, the skeleton was modified by sequential deletion of the carboxylate group and olefin moiety.These modifications provided a series of cis-stilbene analogs by deletion of the carboxylate group, or biphenyl compounds by removing both carboxylate group and olefin moiety.The resulting compounds were tested for their ability to stimulate ¹⁴C glucose uptake in murine 3T3-L1 adipocyte assay.Peak activity was enhanced relative to parent mol. at equimolar concentration (10 μM) and a dose response shift was apparent with decrease in relative potency.Thus modified skeletons may have different PPARγ agonist properties.An investigation of the effect on glucose uptake of substituent on the Ph ring was also carried out.

100 项与 Calyx Therapeutics, Inc. 相关的药物交易

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100 项与 Calyx Therapeutics, Inc. 相关的转化医学

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当前项目

药物(靶点)	适应症	全球最高研发状态

CLX-0900	高脂血症更多	终止
CLX-1100 ( IL-1β x TNF )	类风湿关节炎更多	终止
CLX-0301 ( Protein kinases )	糖尿病更多	终止
CLX-0101	2型糖尿病更多	终止
CLX-090502 ( TNF )	炎症更多	终止