29176-90-7Relevant academic research and scientific papers
Benzooxazolone or benzothiazolone derivatives preparation method therof, and pharmaceutical composition for use in preventing or treating Urotensin-Ⅱ receptor activity related diseases containing the same as an active ingredient
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, (2016/10/09)
The present invention relates to benzoxazolone and benzothiazolone derivatives or a pharmaceutically acceptable salt thereof, a producing method thereof, and a pharmaceutical composition for preventing or treating urotensin-II receptor activity-related diseases containing the same as an active ingredient. Benzoxazolone and benzothiazolone derivatives act as an antagonist of a urotensin-II receptor, and thus can be usefully used for preventing or treating urotensin-II receptor activity-related diseases such as congestive heart failure, heart ischemia, myocardial infarction, cardiomegalia, myofibrosis cordis, coronary artery disease, arteriosclerosis, hypertension, asthma, renal failure, diabetes, vascular inflammation, degenerative neuronal disease, stroke, pain, depression, mental illness, and cancer.COPYRIGHT KIPO 2016
HETEROCYCLIC ACETAMIDE COMPOUND
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, (2014/10/29)
[Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.
Development of potent and selective small-molecule human Urotensin-II antagonists
McAtee, John J.,Dodson, Jason W.,Dowdell, Sarah E.,Girard, Gerald R.,Goodman, Krista B.,Hilfiker, Mark A.,Sehon, Clark A.,Sha, Deyou,Wang, Gren Z.,Wang, Ning,Viet, Andrew Q.,Zhang, Daohua,Aiyar, Nambi V.,Behm, David J.,Carballo, Luz H.,Evans, Christopher A.,Fries, Harvey E.,Nagilla, Rakesh,Roethke, Theresa J.,Xu, Xiaoping,Yuan, Catherine C.K.,Douglas, Stephen A.,Neeb, Michael J.
scheme or table, p. 3500 - 3503 (2009/04/16)
This work describes the development of potent and selective human Urotensin-II receptor antagonists starting from lead compound 1, (3,4-dichlorophenyl)methyl{2-oxo-2-[3-phenyl-2-(1-pyrrolidinylmethyl)-1-piperidinyl]ethyl}amine. Several problems relating to oral bioavailability, cytochrome P450 inhibition, and off-target activity at the kappa opioid receptor and cardiac sodium channel were addressed during lead development. hUT binding affinity relative to compound 1 was improved by more than 40-fold in some analogs, and a structural modification was identified which significantly attenuated both off-target activities.
NOVEL HETEROCYCLIC COMPOUND
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Page/Page column 34, (2010/11/24)
A drug having a high affinity for benzodiazepine ω3 receptors and showing curative and preventive effects for anxiety and depression, which comprises as the active ingredient, for example, a compound of the formula (1): wherein R1 an
Inhibition of nitric oxide synthase by benzoxazolones
Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Humes, John L.,Pacholok, Stephen G.,Grant, Stephan K.,Green, Barbara G.,MacCoss, Malcolm
, p. 2887 - 2892 (2007/10/03)
A series of benzoxazolones has been synthesized using modifications of literature methods. The synthetic benzoxazolone analogs, along with commercially available analogs, were evaluated as inhibitors of nitric oxide synthases (NOS). Structure-activity relationships are also discussed.
