51171-02-9Relevant academic research and scientific papers
THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS
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Paragraph 0305, (2013/04/10)
The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.
Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists
Duan, Hongliang,Ning, Mengmeng,Chen, Xiaoyan,Zou, Qingan,Zhang, Liming,Feng, Ying,Zhang, Lina,Leng, Ying,Shen, Jianhua
supporting information, p. 10475 - 10489 (2013/02/22)
4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.
THIENO (2, 3B) PYRAZINE COMPOUNDS AS B - RAF INHIBITORS
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Page/Page column 94, (2011/12/14)
The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.
Pyrazine-2-carboxyamide derivatives
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Page/Page column 15, (2008/06/13)
The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
NEUROPEPTIDE Y4 RECEPTOR AGONISTS
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Page/Page column 47, (2008/06/13)
This invention provides peptides that act as selective NPY4 receptor agonists in vitro and are efficacious in vivo to reduce food intake. The invention is a peptide selected from a specific group of derivatized PP-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the peptides to said mammal to reduce food intake and body weight.
SELECTIVE NEUROPEPTIDE Y2 RECEPTOR AGONISTS
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Page/Page column 45-46, (2010/11/30)
This invention provides peptides that act as selective NPY2 receptor agonists and may be used to reduce food intake. The invention includes a peptide selected from a specific group of derivatized NPY-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating obesity or related diseases in a mammal comprising administering a therapeutically effective amount of the peptide to said mammal to reduce food intake and body weight.
PITUITARY ADENYLATE CYCLASE ACTIVATING PEPTIDE (PACAP) RECEPTOR (VPAC2) AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
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Page/Page column 51, (2008/06/13)
This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the VPAC2 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.
GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
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Page/Page column 51, (2010/11/24)
This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These GLP-1 modified peptides function in vivo as agonists of the GLP-1 receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.
GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE (GIP) RECEPTOR AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
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Page/Page column 51, (2010/11/24)
This invention provides peptides with novel modifications that provide suitable derivatization sites to improve the pharmacokinetic properties of the peptides. These modified peptides function in vivo as agonists of the GIP receptor. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, for example, type 2 diabetics.
NOVEL BENZYLAMINE DERIVATIVES AS CETP INHIBITORS
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Page/Page column 261, (2008/06/13)
The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
