349-66-6Relevant academic research and scientific papers
Optical Control of CRAC Channels Using Photoswitchable Azopyrazoles
Yang, Xingye,Ma, Guolin,Zheng, Sisi,Qin, Xiaojun,Li, Xiang,Du, Lupei,Wang, Youjun,Zhou, Yubin,Li, Minyong
supporting information, p. 9460 - 9470 (2020/06/27)
The Ca2+ release-activated Ca2+ (CRAC) channels control many Ca2+-modulated physiological processes in mammals. Hyperactivating CRAC channels are known to cause several human diseases, including Stormorken syndrome. Here, we show the design of azopyrazole-derived photoswitchable CRAC channel inhibitors (designated piCRACs), which enable optical inhibition of store-operated Ca2+ influx and downstream signaling. Moreover, piCRAC-1 has been applied in vivo to alleviate thrombocytopenia and hemorrhage in a zebrafish model of Stormorken syndrome in a light-dependent manner.
Asymmetric Retro-Claisen Reaction by Synergistic Chiral Primary Amine/Palladium Catalysis
Han, Yanfang,Zhang, Long,Luo, Sanzhong
supporting information, p. 7258 - 7261 (2019/10/02)
We described herein a chiral primary amine/palladium catalyzed asymmetric retro-Claisen reaction of β-diketones with salicylic carbonates. A series of chiral α-alkylated ketones and macrolides were obtained with good yields and excellent enantioselectivities upon a sequence of decarboxylative benzylation, retro-Claisen cleavage, and enamine protonation. This strategy features broad substrate scope, mild conditions, as well as high atom economy with salicylic carbonates as the o-quinone methide precursors.
NOVEL SUBSTITUTED PYRIDO-PIPERAZINONE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Paragraph 0817-0818, (2018/11/26)
The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
NOVEL SUBSTITUTED PYRIDO-PIPERAZINONE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 102, (2014/08/06)
The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
MODULATORS OF DOPAMINE NEUROTRANSMISSION
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Page/Page column 37, (2009/12/05)
The present invention relates to novel1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
NOVEL 1 -BENZYL-4-PIPERIDINAMINES THAT ARE USEFUL IN THE TREATMENT OF COPD AND ASTHMA
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Page/Page column 51, (2010/11/27)
The invention provides 1 -benzyl- 4 -piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseses such a
Heteroaryl and benzyl amide compounds
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Page/Page column 13, (2008/06/13)
Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
