97900-77-1Relevant academic research and scientific papers
ADME-guided design and synthesis of aryloxanyl pyrazolone derivatives to block mutant superoxide dismutase 1 (SOD1) cytotoxicity and protein aggregation: Potential application for the treatment of amyotrophic lateral sclerosis
Chen, Tian,Benmohamed, Radhia,Kim, Jinho,Smith, Karen,Amante, Daniel,Morimoto, Richard I.,Kirsch, Donald R.,Ferrante, Robert J.,Silverman, Richard B.
experimental part, p. 515 - 527 (2012/03/26)
Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. The arylsulfanyl pyrazolone (ASP) scaffold was one of the active scaffolds identified in a cell-based high throughput screening assay targeting mutant Cu/
PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND COMPOSITION FOR PREVENTION AND TREATMENT OF OSTEOPOROSIS CONTAINING SAME
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Page/Page column 9, (2012/09/22)
The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
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Page/Page column 113-114, (2010/07/10)
The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
Synthesis and Antiulcer Activity of 5,11-Dihydrobenzoxepinopyridines
Kumazawa, Toshiaki,Harakawa, Hiroyuki,Obase, Hiroyuki,Oiji, Yoshimasa,Tanaka, Hiroshi,et al.
, p. 779 - 785 (2007/10/02)
A series of substituted 5,11-dihydrobenzoxepinopyridines was synthesized and evaluated for antiulcer activity in water immersion/restrained stress ulcer assay in rats.Structure-activity relationships are described.Most of the tested compounds exhibited low affinity to the muscarinic acetylcholine receptor.The molecular features for the best activities are the 2-(diethylamino)ethylenediamine group at the 5-position of the oxepin ring and an oxepin skeleton rather than a thiepin or a pyran skeleton.Methyl and chlorine substitution on the benzene ring reduced the activity.Compound 11, 5-amino>-5,11-dihydrobenzoxepinopyridine trihydrochloride was selected for further evaluation.Synthesis and antiulcer activity of optically active 11 is described.There were no statistically significant differences between (+)-, (-), and (+/-)-11.Compound 11 showed weak antisecretory activity in pylorus-ligated rats.It is now under clinical evaluation as KW 5805.
