96729-89-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of pyrimidine-2-carboxamide analogs: Investigation for novel RAGE inhibitors with reduced hydrophobicity and toxicity
Kim, Seok-Ho,Han, Young Taek
, p. 1952 - 1962 (2015/11/24)
This paper describes an investigation of novel RAGE inhibitors with improved drug-like properties. To identify the improved drug-like RAGE inhibitor, we designed and synthesized pyrimidine-2-carboxamide analogs based on our previous work. Several potent a
Novel heteroarylcarboxamide derivative or pharmacutically acceptable salt thereof, process for the preparation thereof and pharmaceutical composition for prevention or treatment of RAGE receptor related diseases containing the same as an active ingredient
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Paragraph 0261; 0267-0268; 0359; 0363-0364, (2021/11/02)
The present invention refers to novel heterocyclic biting Carbox probably the id derivative acceptable salt, and manufacturing method thereof including RAGE associated active acetylcholinesterase receptor or pharmaceutical composition for preventing or treating disease is directed to. Heterocycle by the present invention a derivative biting Carbox probably the id RAGE receptor antagonism in by, nerve cells with the beta loss oh with wheat id RAGE conjunction with receptor, inhibiting moving into brain, the resulting beta Amyloid plaque formed 21 is known to effectively inhibit generation.. Furthermore, memory a chemicals that are important in the acetylcholine for decomposing an aromatic thus inhibiting acetylcholine s reel sacrifice , RAGE disease associated active acetylcholinesterase receptor or Alzheimer's disease, cerebrovascular dementia, dementia due to damage bean curd, multi blockade dementia, Alzheimer's disease or the like dementia alcoholic or mixed dementia multi blockade and including dementia, pick (pick) bottle, a smartcrew [...] -Jakob (Creutzfeldt-jakob) bottle, that thyroid gland symptoms , bean curd a blade Parkinson (Parkinson) bottle, Huntington's disease (Huntington) which is useful in preventing or treating, can be used.
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849
Witty, David R.,Bateson, John H.,Hervieu, Guillaume J.,Jeffrey, Phillip,Johnson, Christopher N.,Muir, Alison I.,O'Hanlon, Peter J.,Stemp, Geoffrey,Stevens, Alex J.,Thewlis, Kevin M.,Wilson, Shelagh,Winborn, Kim Y.
, p. 4865 - 4871 (2007/10/03)
We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were
3-(4-PIPERIDINE-1YLMETHYL-PHENYL)-PROPION ACID-PHENYLAMIDE-DERIVATIVES AND RELATED COMPOUNDS USED IN THE FORM OF MCH ANTAGONISTS (MELANINE CONCENTRATING HORMONE) FOR TREATING EATING DISORDERS
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Page/Page column 252, (2008/06/13)
The invention relates to amid compounds of general formula (I), wherein groups and residuals A, B, b, W, X, Y, Z, R1, R2 and R3 have significances given in a claim 1. In addition, said invention relates to drugs containing at least one type of inventive amid. Because of the antagonist activity of an MCH-receptor, the inventive drugs are suitable for treating metabolic disturbances and/or eating disorders, in particular adiposity, bulimia, anorexia, hyperphagia and diabetes.
BETA-KETOAMIDE COMPOUNDS HAVING AN MCH-ANTAGONISTIC EFFECT AND MEDICAMENTS CONTAINING SAID COMPOUNDS
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Page/Page column 74, (2008/06/13)
The invention relates to β-ketoamide compounds of general formula (I) wherein the groups and radicals A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the designations cited in patent claim 1. The invention also relates to medicaments containing at least one inventive amide. As a result of the MCH receptor antagonistic activity, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, especially adipositas, bulimia, anorexia, hyperphagia and diabetes.
Beta-ketoamide compounds with MCH antagonistic activity
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Page/Page column 74, (2008/06/13)
Compounds of formula I wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one amide according to the invention. As a result of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes.
NOVEL AMIDE COMPOUNDS WITH MCH ANTAGONISTIC EFFECT AND MEDICAMENTS COMPRISING SAID COMPOUNDS
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Page/Page column 84, (2008/06/13)
The invention relates to amide compounds of general formula (I), in which the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. The invention further relates to medicaments comprising at least one of said amides. Said medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia, and diabetes as a result of the MCH receptor antagonism.
