170353-35-2Relevant articles and documents
COMPOUNDS AND METHODS OF THEIR USE
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, (2020/05/19)
Provided are agents capable of binding the KIX domain of CBP or MED15 to inhibit the binding between SREBP1 and the KIX domain of MED15 or CBP. Also provided are compositions containing the agents and methods of their use.
Polycyclic compound and its pharmaceutical composition and application
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Paragraph 0198; 0199; 0203; 0204; 0205, (2018/03/26)
The invention discloses a polycyclic compound and its preparation method, pharmaceutical composition and application. The polycyclic compound (I) and its isomer, prodrug, stable isotope derivative ora pharmaceutically acceptable salt have the structure shown in the description. The polycyclic compound has good IDO1 inhibitory effects and can be used for effectively treating, alleviating and/or preventing various related diseases such as tumors and infectious diseases caused by immunosuppression.
N-substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as 92 antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents
Birch, Alan M.,Bradley, Paul A.,Gill, Julie C.,Kerrigan, Frank,Needham, Pat L.
, p. 3342 - 3355 (2007/10/03)
A series of N-substituted 1-(2,3-dihydro-1,4-benzodioxin-2- yl)methylamine derivatives with D2 antagonist/5-HT(1A) partial agonist activity has been prepared as potential atypical antipsychotic agents. Optimization of in vitro receptor binding activity and in vivo activity in rodent models of psychosis has led to compound 24, which showed good affinities for human D2, D3, and 5-HT(1A) receptors but significantly less affinity for human α1 adrenoceptors and rat H1 and muscarinic receptors. In rodents, 24 showed functional D2-like antagonism and 5-HT(1A) partial agonism. After oral dosing, 24 showed good activity in rodent antipsychotic tests and very little potential to cause extrapyramidal side effects (EPS), as measured by its ability to induce catalepsy in rats only at very high doses. In the light of this promising profile of activity, 24 has been selected for clinical investigation as a novel antipsychotic agent with a predicted low propensity to cause EPS.
Bicyclic aromatic compounds as therapeutic agents
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, (2008/06/13)
Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; and g is 0, 1, 2, 3 or 4; R1, R2, R3, R4, U, Q and T are defined in claim 1. The compounds have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.