41885-98-7Relevant academic research and scientific papers
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol
Peprah, Kwakye,Zhu, Xue Y.,Eyunni, Suresh V.K.,Etukala, Jagan R.,Setola, Vincent,Roth, Bryan L.,Ablordeppey, Seth Y.
body text, p. 1671 - 1678 (2012/04/10)
Structure-activity relationship studies on 4-(4-(4-chlorophenyl)-1,4- diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one (SYA 013), a homopiperazine analog of haloperidol has resulted in an understanding of the effect of structural modifications on binding affinity at dopamine and serotonin receptor subtypes. Further exploration, using bioisosteric replacement strategies has led to the identification of several new agents including compounds 7, 8, 11 and 12 which satisfy the initial criteria for further exploration as new antipsychotic agents. In addition, compound 18, a D3 selective tropanol, has been identified as having the potential for further optimization into a useful drug which may combat neuropsychiatric diseases.
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one
Ablordeppey, Seth Y.,Altundas, Ramazan,Bricker, Barbara,Zhu, Xue Y.,Suresh Kumar, Eyunni V.K.,Jackson, Tanise,Khan, Abdul,Roth, Bryan L.
, p. 7291 - 7301 (2008/12/23)
The synthesis and exploration of novel butyrophenones have led to the identification of a diazepane analogue of haloperidol, 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one (compound 13) with an interesting multireceptor binding profile. Compound 13 was evaluated for its binding affinities at DA subtype receptors, 5HT subtype receptors, H-1, M-1 receptors and at NET, DAT, and SERT transporters. At each of these receptors, compound 13 was equipotent or better than several of the standards currently in use. In in vivo mouse and rat models to evaluate its efficacy and propensity to elicit catalepsy and hence EPS in humans, compound 13 showed similar efficacy as clozapine and did not produce catalepsy at five times its ED50 value.
THIENOPYRIDINE DERIVATIVES
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Page/Page column 97, (2010/11/26)
The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.
COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS
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Page/Page column 110; 120, (2008/06/13)
The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula (I) are provided or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer, and osteolytic bone disorders.
COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS
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Page/Page column 81, (2008/06/13)
The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
