Abstract:
BACKGROUND:Not only hypercholesterolemia, but also low levels of high-density lipoprotein cholesterol is a critical risk factor for atherosclerosis-related disease. Therefore, there has been great interest in identifying effective and selective cholesteryl ester transfer protein (CETP) inhibitors that can raise high-density lipoprotein. Recently, Phase III clinical studies of torcetrapib, one of the CETP inhibitors developed by researchers at Pfizer, were unexpectedly terminated because of an increase in cardiovascular events and mortality. Torcetrapib has some compound-specific and off-target effects, such as raising blood pressure and aldosterone, which could affect an increase in cardiovascular events and mortality. OBJECTIVE:The aim of this review is to provide an update (from 2000 to early 2009) on the patenting activity in the field of CETP inhibitors and the status of the most advanced compounds. CONCLUSION:Dalcetrapib (JTT-705) and anacetrapib, which have not been reported to have the off-target effects of torcetrapib, are currently in Phase III. They are expected to reveal whether CETP inhibition is beneficial for atherosclerosis-related diseases.
journal_name
Expert Opin Ther Patjournal_title
Expert opinion on therapeutic patentsauthors
Shinkai Hdoi
10.1517/13543770903198451subject
Has Abstractpub_date
2009-09-01 00:00:00pages
1229-37issue
9eissn
1354-3776issn
1744-7674journal_volume
19pub_type
杂志文章,评审abstract:INTRODUCTION:Monoacylglycerol lipase (MAGL) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol. Importantly, it was found that MAGL degradation of lipids in cancer cells enhances the availability of free fatty acids for new cellular membrane formation...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章
doi:10.1080/13543776.2021.1841166
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abstract:INTRODUCTION:Chymase is primarily found in mast cells (MCs), fibroblasts, and vascular endothelial cells. MC chymase is released into the extracellular interstitium in response to inflammatory signals, tissue injury, and cellular stress. Among many functions, chymase is a major extravascular source for angiotensin II (...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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更新日期:2016-08-01 00:00:00
abstract:INTRODUCTION:The appetite stimulating effects of melanin-concentrating hormone (MCH) continues to be of high interest, and there is substantial support to investigate the use of MCH 1-receptor antagonists for the treatment of obesity. Other areas of potential use for MCH 1-receptor antagonists include depression and an...
journal_title:Expert opinion on therapeutic patents
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abstract::Introduction: Discoidin domain receptor 1 (DDR1) is a collagen-activated receptor tyrosine kinase. Upon collagen binding, DDR1 undergoes tyrosine autophosphorylation, which consequently triggers downstream genetic and cellular pathways and plays critical roles in the regulation of cellular morphogenesis, differentiati...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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abstract::A small series of aryl(1-arylamino)ethyl,1,5-naphthyridine derivatives that selectively inhibit PI3Kδ was prepared. The compounds are claimed to be useful in the treatment of cancer, inflammatory and autoimmune diseases. The compounds represent further variations around a structural motif explored in a number of previ...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章
doi:10.1517/13543776.2011.622749
更新日期:2011-11-01 00:00:00
abstract:INTRODUCTION:New drug formulations against hypertension have a vital role in the quality of human life, as this risk factor for cardiovascular disease can be life threatening. A modern life style characterized by less exercise, smoking, drinking and poor diet has increased the risk of developing hypertension, the so-ca...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
abstract:INTRODUCTION:Nuclear factor (NF)-κB, as transcription factor, is linked to the expression of various genes and plays an essential role in immune and inflammatory responses. Abnormal NF-κB signaling results in human diseases, such as immune disorders, inflammation and various cancers. Therefore, regulation of NF-κB may ...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1517/13543776.2011.638285
更新日期:2011-12-01 00:00:00
abstract:BACKGROUND:The application (WO2010075475) is involved in the diagnosis of angiogenesis-dependent diseases related with the soluble FMS-like tyrosine kinase-1 (sFlt-1) biomarker. OBJECTIVE:It aims to identify, characterize and produce antibodies raised against sFlt-1 for the diagnosis of preeclampsia as well as other c...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章
doi:10.1517/13543776.2011.577071
更新日期:2011-06-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2020-03-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2017-03-01 00:00:00
abstract:INTRODUCTION:The cyclic nucleotides cAMP and cGMP are ubiquitous intracellular second messengers regulating a large variety of biological processes. The intracellular concentration of these biologically relevant molecules is modulated by the activity of phosphodiesterases (PDEs), a class of enzymes that is grouped in 1...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1080/13543776.2016.1203902
更新日期:2016-08-01 00:00:00
abstract::Introduction: Phosphodiesterase 10 (PDE10) is one of at least 11 different PDE families, which are the enzymes that degrade adenosine 3',5'-cyclic monophosphate (cAMP) and/or guanosine 3',5'-cyclic monophosphate (cGMP) by hydrolyzing the phosphodiester bonds. Inhibition of PDE10A represents a molecular target in the t...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2020-02-01 00:00:00
abstract::A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore att...
journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2017-06-01 00:00:00
abstract:INTRODUCTION:In the last 10 years, nutraceuticals have grown in interest to researchers, industry, and consumers and are now familiar in the collective imagination as a tool for preventing the onset of a disease. Often nutraceuticals are confused with biologically active phytochemicals/botanicals which can have health ...
journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2018-04-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2009-09-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2018-02-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2017-07-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2017-08-01 00:00:00
abstract::This application claims salts and crystalline forms of a previously disclosed DP2 receptor antagonist (2-[3-[2-(tert-butylsulfanylmethyl)-4-(2,2-dimethylpropanoylamino)phenoxy]-4-methoxy-phenyl]acetic acid (1)). It also claims compositions containing the free acid and its salts, especially the sodium salt and their us...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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