- HETEROCYCLIC COMPOUND AND USE THEREOF
-
Provided is a heterocyclic compound that can have an antagonistic action on an NMD A receptor containing the NR2B subunit and that is expected to be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like. A compound represented by the formula (I), wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.
- -
-
Page/Page column 67
(2021/04/02)
-
- Hetero-aromatic compound and its use in medicine
-
The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.
- -
-
Paragraph 0883; 0886-0888; 1250; 1253-1257; 1296-1297
(2019/07/04)
-
- Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists
-
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.
- Duan, Hongliang,Ning, Mengmeng,Chen, Xiaoyan,Zou, Qingan,Zhang, Liming,Feng, Ying,Zhang, Lina,Leng, Ying,Shen, Jianhua
-
p. 10475 - 10489
(2013/02/22)
-
- Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors
-
11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution.
- Scott, James S.,Gill, Adrian L.,Godfrey, Linda,Groombridge, Sam D.,Rees, Amanda,Revill, John,Schofield, Paul,S?rme, Pernilla,Stocker, Andrew,Swales, John G.,Whittamore, Paul R.O.
-
p. 6756 - 6761
(2013/01/14)
-
- NOVEL PYRIMIDINE DERIVATIVE FOR INHIBITING THE GROWTH OF CANCER CELLS
-
The present invention provides a novel pyrimidine derivative or pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, which can effectively inhibit the growth of cancer cells induced by the overexpression of EGFR incl
- -
-
Page/Page column 36
(2011/09/15)
-
- AZA-BENZOFURANYL COMPOUNDS AND METHODS OF USE
-
The invention relates to azabenzofuranyl compounds of Formula (I) with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
- -
-
Page/Page column 79
(2008/06/13)
-
- PITUITARY ADENYLATE CYCLASE ACTIVATING PEPTIDE (PACAP) RECEPTOR (VPAC2) AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
-
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
-
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
-
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.
- -
-
-
- NEUROPEPTIDE Y4 RECEPTOR AGONISTS
-
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.
- -
-
Page/Page column 40
(2008/06/13)
-
- SELECTIVE NEUROPEPTIDE Y2 RECEPTOR AGONISTS
-
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.
- -
-
Page/Page column 38
(2010/11/30)
-
- Cyclic compounds and their use
-
The present invention relates to a compounds represented by the following formula or salts thereof. STR1 The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for
- -
-
-
