364631-73-2Relevant articles and documents
Novel ASM direct inhibition compound 2-amino-2-(1,2,3-triazol-4-yl)propane-1,3-diol derivatives and uses thereof
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Paragraph 0196-0199, (2019/12/11)
The present invention relates to a composition for preventing or treating neurodegenerative diseases or depression including 2-amino-2-(1,2,3-triazol-4-yl)propane-1,3-diol derivatives as an active ingredient, and more specifically, to a pharmaceutical composition for preventing or treating neurodegenerative diseases or depression including the compound having an effect of directly inhibiting ASM activities as an active ingredient. According to the present invention, an ASM inhibiting compound of chemical formula 1 can be very useful in development of a preventive or therapeutic agent for neurodegenerative diseases including Alzheimerandprime;s disease, or a composition for diagnosing neurodegenerative diseases since the ASM inhibiting compound is directly combined with an ASM protein to obtain an excellent effect of inhibiting ASM; has treatment effects such as Aandbeta; plaque reduction, improvements in memory and anxiety, relief in neuroinflammatory diseases and the like in Alzheimerandprime;s brain environment; has a very high distribution in the brain and is very excellent in metabolic stability due to liver microsome. Further, a novel ASM inhibiting compound of chemical formula 1 can be useful used as a preventive or therapeutic agent for neurodegenerative diseases including depression as described in a conventional report that inhibition of ASM is effective in depression relief.COPYRIGHT KIPO 2020
Construction of Quaternary Carbon Stereocenter of α-Tertiary Amine through Remote C-H Functionalization of Tris Derivatives: Enantioselective Total Synthesis of Myriocin
Miyagawa, Takashi,Inuki, Shinsuke,Oishi, Shinya,Ohno, Hiroaki
, p. 5485 - 5490 (2019/08/01)
We describe the development of a strategy for the construction of the quaternary carbon stereocenter of α-tertiary amines. This strategy highlights a site-selective C-H functionalization involving an alkoxy-radical-triggered 1,5-hydrogen transfer (1,5-HAT
Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography
Shaikh, Rizwan S.,Schilson, Stefanie S.,Wagner, Stefan,Hermann, Sven,Keul, Petra,Levkau, Bodo,Sch?fers, Michael,Haufe, Günter
, p. 3471 - 3484 (2015/05/05)
Sphingosine-1-phosphate (S1P) is a lysophospholipid that evokes a variety of biological responses via stimulation of a set of cognate G-protein coupled receptors (GPCRs): S1P1-S1P5. S1P and its receptors (S1PRs) play important roles in the immune, cardiovascular, and central nervous systems and have also been implicated in carcinogenesis. Recently, the S1P analogue Fingolimod (FTY720) has been approved for the treatment of patients with relapsing multiple sclerosis. This work presents the synthesis of various fluorinated structural analogues of FTY720, their in vitro and in vivo biological testing, and their development and application as [18F]radiotracers for the study of S1PR biodistribution and imaging in mice using small-animal positron emission tomography (PET).
Highly efficient aerobic oxidation of alcohols by using less-hindered nitroxyl-radical/copper catalysis: Optimum catalyst combinations and their substrate scope
Sasano, Yusuke,Kogure, Naoki,Nishiyama, Tomohiro,Nagasawa, Shota,Iwabuchi, Yoshiharu
, p. 1004 - 1009 (2015/03/31)
The oxidation of alcohols into their corresponding carbonyl compounds is one of the most fundamental transformations in organic chemistry. In our recent report, 2-azaadamantane N-oxyl (AZADO)/copper catalysis promoted the highly chemoselective aerobic oxidation of unprotected amino alcohols into amino carbonyl compounds. Herein, we investigated the extension of the promising AZADO/copper-catalyzed aerobic oxidation of alcohols to other types of alcohol. During close optimization of the reaction conditions by using various alcohols, we found that the optimum combination of nitroxyl radical, copper salt, and solution concentration was dependent on the type of substrate. Various alcohols, including highly hindered and heteroatom-rich ones, were efficiently oxidized into their corresponding carbonyl compounds under mild conditions with lower amounts of the catalysts.
NEW LIGANDS FOR TARGETING OF S1P RECEPTORS FOR IN VIVO IMAGING AND TREATMENT OF DISEASES
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Page/Page column 0333; 0334; 0335; 0336; 0337; 0338; 0339, (2014/06/25)
The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogues, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
NEW LIGANDS FOR TARGETING OF S1P RECEPTORS FOR IN VIVO IMAGING AND TREATMENT OF DISEASES
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Page/Page column 42, (2013/03/26)
The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogues, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
Stereoselective functionalization of pyrrolidinone moiety towards the synthesis of salinosporamide A
Barbion, Julien,Sorin, Geoffroy,Selkti, Mohamed,Kellenberger, Esther,Baati, Rachid,Santoro, Stefano,Himo, Fahmi,Pancrazi, Ange,Lannou, Marie-Isabelle,Ardisson, Janick
experimental part, p. 6504 - 6512 (2012/08/27)
An important feature of the synthesis of salinosporamide A, a potent proteasome inhibitor, is the establishment of the quaternary stereocenter at C3. A new route has been developed based on the methylation of a functionalized pyrrolidinone. Direct methylation reaction led to the unwanted diastereomer; however, by means of a Corey-Chaykovsky reaction followed by LiAlH4 epoxide opening, the desired alcohol was obtained. The pyrrolidinone was elaborated through a key allylation reaction between a tertiary allyltitanium reagent and an aldehyde bearing a spiroketal moiety in α-position.
A convenient synthesis of the immunosuppressive agent FTY720
Feng, Xiangjun,Mei, Yuhua,Luo, Yu,Lu, Wei
experimental part, p. 161 - 164 (2012/07/03)
This paper describes a practical synthetic approach to preparation of an immunosuppressant, FTY720. The key steps involve an iron-catalyzed cross-coupling reaction and a Wittig reaction. The advantages of this synthesis include readily available starting
AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Page/Page column 30-31, (2010/04/25)
Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
AGONISTS OF THE SPHINGOSINE- 1- PHOSPHATE RECEPTOR (SLP)
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Page/Page column 67; 68, (2008/06/13)
The invention provides compounds of formula I and formula II, their preparation, a their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.