509142-53-4Relevant academic research and scientific papers
Indoleamine 2, 3-dioxygenase inhibitor and use thereof
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, (2018/03/25)
The invention belongs to the technical field of medical technology and relates to a compound shown in the formula I and its pharmaceutically acceptable salt, isomer and prodrug. In the formula, R1, R2, R3, X, m, n and a ring A are defined in the specifica
Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists
Kanuma, Kosuke,Omodera, Katsunori,Nishiguchi, Mariko,Funakoshi, Takeo,Chaki, Shigeyuki,Nagase, Yasuko,Iida, Izumi,Yamaguchi, Jun-ichi,Semple, Graeme,Tran, Thuy-Anh,Sekiguchi, Yoshinori
, p. 3307 - 3319 (2007/10/03)
The optimization of the distance between two key pharmacophore features within our first hit compounds 1a and 2a led to the identification of a new class of potent non-peptidic antagonists for the MCH-R1, based around 4-amino-2-cyclohexylaminoquinazolines. In particular, ATC0065 (2c), N2-[cis-4-({2-[4-Bromo-2-(trifluoromethoxy)phenyl]ethyl}amino)cyclohexyl]-N4,N4-dimethylquinazoline-2,4-diamine dihydrochloride, bound with high affinity to the MCH-R1 (IC50 value of 16 nM) and showed good metabolic stability in liver microsomes from human and rat.
PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF
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Page/Page column 110; 111, (2008/06/13)
The present invention encompasses novel substituted pyrimidine compounds of Formula (I): which act as MCH receptor antagonists. These compounds are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson’s disease, epilepsy, and addiction.
QUINOLINE, TETRAHYDROQUINOLINE AND PYRIMIDINE DERIVATIVES AS MCH ANTAGONIST
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Page/Page column 165, (2010/02/08)
The present invention relates to compounds of the Formula (I) wherein Q is: which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.
