170033-52-0Relevant academic research and scientific papers
BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION
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, (2017/02/24)
The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto- temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
QUINOLINE DERIVATIVES AS SMO INHIBITORS
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, (2017/02/28)
Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist
Hong, Qingmei,Bakshi, Raman K.,Palucki, Brenda L.,Park, Min K.,Ye, Zhixiong,He, Shuwen,Pollard, Patrick G.,Sebhat, Iyassu K.,Liu, Jian,Guo, Liangqin,Cashen, Doreen E.,Martin, William J.,Weinberg, David H.,MacNeil, Tanya,Tang, Rui,Tamvakopoulos, Constantin,Peng, Qianping,Miller, Randy R.,Stearns, Ralph A.,Chen, Howard Y.,Chen, Airu S.,Strack, Alison M.,Fong, Tung M.,MacIntyre, D. Euan,Wyvratt, Matthew J.,Nargund, Ravi P.
, p. 2330 - 2334 (2011/05/15)
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Asymmetric Synthesis of 2,6-Methylated Piperazines
Mickelson, John W.,Belonga, Kenneth L.,Jacobsen, Jon E.
, p. 4177 - 4183 (2007/10/02)
The complete series of enantiopure 2,6-methylated piperazines was synthesized utilizing two alternative reactions in the key bond-forming step.The dimethyl enantiomers, (2R,6R)- and (2S,6S)-2,6-dimethylpiperazine (1, 2), were prepared using either a diastereoselective triflate alkylation or a novel intermolecular Mitsunobu reaction to set the required stereochemistry.The monomethyl derivatives, (R)- and (S)-tert-butyl 2-methyl-1-piperazinecarboxylate (3, 4) were also synthesized employing the Mitsunobu cyclization strategy while the trimethyl compounds, (R)- and (S)-2,2,6- trimethylpiperazine (5, 6) were prepared using an enantiospecific triflate alkylation as the principal reaction.These methods represent efficient, general strategies for preparing a variety of 2,6-methylated piperazines for which the absolute stereochemistry can be readily controlled.
Asymmetric Synthesis of (2R,6R) and (2S,6S)-2,6-Dimethylpiperazine
Mickelson, John W.,Jacobsen, E. Jon
, p. 19 - 22 (2007/10/02)
The title compounds were prepared via two efficient routes.The first sequence utilized a diastereospecific triflate alkylation in the key bond forming step while the second method relied on a novel intramolecular Mitsunobu reaction to set the required stereochemistry.
