412299-67-3Relevant academic research and scientific papers
Substituted benzothieno [2,3-c] tetrahydropyridine derivative and preparation method and application thereof
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Paragraph 0055; 0059, (2018/07/30)
The invention belongs to the technical field of medicinal chemistry and medicines, and relates to a substituted benzothieno [2,3-c] tetrahydropyridine derivative as shown in formula (I), a preparationmethod of the substituted benzothieno [2,3-c] tetrahydr
Discovery of novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors
Wang, Mingliang,Fang, Yanjia,Gu, Shoulai,Chen, Fangfang,Zhu, Zhengjiang,Sun, Xun,Zhu, Jidong
, p. 157 - 172 (2017/03/31)
The inhibition of CYP17 to block androgen biosynthesis is a well validated strategy for the treatment of prostate cancer. Herein we reported the design, synthesis and structure–activity relationship (SAR) study for a series of novel 1,2,3,4- tetrahydroben
An efficient five-component synthesis of thioether containing dihydropyrano[2,3-c]pyrazoles: a green domino strategy
Ramesh, Vediyappan,Shanmugam, Sivakumar,Devi, Natarajan Savitha
, p. 9993 - 10001 (2016/12/07)
An efficient route for the synthesis of novel thioether containing dihydropyrano[2,3-c]pyrazoles has been accomplished via a solvent-free, catalyst-free, one-pot, five component domino strategy. This synthetic approach offers several advantages such as an easy work-up, no need for purification techniques and a short reaction time with good atom economy and high yields of the products (81-86%).
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/
Arylsulfanyl pyrazolones block mutant SOD1-G93A aggregation. Potential application for the treatment of amyotrophic lateral sclerosis
Chen, Tian,Benmohamed, Radhia,Arvanites, Anthony C.,Ranaivo, Hantamalala Ralay,Morimoto, Richard I.,Ferrante, Robert J.,Watterson, D. Martin,Kirsch, Donald R.,Silverman, Richard B.
experimental part, p. 613 - 622 (2011/03/17)
Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. Mutations in copper/zinc superoxide dismutase 1 (SOD1) have been implicated in the pathophysiology of this disease. Using a high-throughput screening assa
Ru-catalyzed asymmetric hydrogenation of γ-heteroatom substituted β-keto esters
Fan, Weizheng,Li, Wanfang,Ma, Xin,Tao, Xiaoming,Li, Xiaoming,Yao, Ying,Xie, Xiaomin,Zhang, Zhaoguo
experimental part, p. 9444 - 9451 (2012/01/13)
A series of enantiomerically pure γ-heteroatom substituted β-hydroxy esters were synthesized with high enantioselectivities (up to 99.1% ee) by hydrogenation of γ-heteroatom substituted β-keto esters in the presence of Ru-(S)-SunPhos catalyst. These asymmetric hydrogenations provide key building blocks for a variety of naturally occurring and biologically active compounds.
TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
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Page/Page column 111, (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.
AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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Page/Page column 81, (2010/10/03)
MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N, E is C or N, Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N, D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C-C-, or 1,2-cyclopropyl; X is O, S or NR 11, R 1 , R 2 , and R 3 are ,independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12, G is O, S or -NR 15, D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety
A facile synthesis and discovery of highly functionalized tetrahydropyridines and pyridines as antimycobacterial agents
Raju, Suresh Kumar,Stephen, Michael Rajesh,Subbu, Perumal,Debjani, Banerjee,Perumal, Yogeeswari,Dharmarajan, Sriram
scheme or table, p. 602 - 610 (2010/08/20)
The four-component reaction of ethyl-3-oxo-4-(arylsulfanyl)butanoate, substituted aromatic aldehydes and ammonium acetate afforded novel ethyl 4-hydroxy-2,6-diaryl-5-(arylsulfanyl)-1,2,5,6-tetrahydro-3-pyridinecarboxylates. These tetrahydro-pyridine ester
Synthesis of functionalized diaryl sulfides based on regioselective one-pot cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-butadienes
Rashid, Muhammad A.,Rasool, Nasir,Adeel, Muhammad,Reinke, Helmut,Fischer, Christine,Langer, Peter
, p. 3782 - 3793 (2008/09/20)
Functionalized diaryl sulfides were prepared based on one-pot cyclizations of 1,3-bis(trimethylsilyloxy)-1,3-butadienes.
