- HETEROCYCLIC COMPOUNDS
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The invention provides new heterocyclic compounds having the general formula (I) wherein A, L1, X, m, n and R1 to R4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
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Paragraph 0831-0832
(2021/04/02)
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- Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-containing pyrazolo[3,4-b]pyridinones as a new series of AMPKɑ1β1γ1 activators
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Adenosine monophosphate-activated protein kinase (AMPK) plays a key role in maintaining whole-body homeostasis and has been regarded as a therapeutic target for the treatment of diabetic nephropathy (DN). Herein, a series of 1,2,4-oxadiazole-containing py
- Xiao, Zhihong,Peng, Yajun,Zheng, Bifeng,Chang, Qi,Guo, Yating,Chen, Zhuo,Li, Qianbin,Hu, Gaoyun
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- KCNT1 INHIBITORS AND METHODS OF USE
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The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
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Paragraph 000390
(2020/11/23)
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- Synthesis and Biological Evaluation of Sigma-1 (σ1) Receptor Ligands Based on Phenyl-1,2,4-oxadiazole Derivatives
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In this study, a series of phenyl-1,2,4-oxadiazole derivatives were synthesized and evaluated for anti-allodynic activity. Structure–activity relationship studies identified 1-{4-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]butyl}piperidine (39) with excellent affinity for the σ1 receptor and selectivity for the σ2 receptor, with poor activity to other central nervous system neurotransmitter receptors and transporters associated with pain. Compound 39 exhibited dose-dependent efficacy in suppressing the formalin-induced flinching and attenuating mechanical allodynia in chronic constriction injury-induced neuropathic rats. These results suggest that compound 39 exerts potent antihyperalgesic activity and could be considered as a promising candidate for treating neuropathic pain.
- Cao, Xudong,Yao, Zhongyuan,Dou, Fei,Zhang, Yifang,Qiu, Yinli,Zhao, Song,Xu, Xiangqing,Liu, Xin,Liu, Bi-Feng,Chen, Yin,Zhang, Guisen
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- A cascade process for directly converting nitriles (RCN) to cyanamides (RNHCN) via SO2F2-activated Tiemann rearrangement
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A simple, mild and practical process for the direct conversion of nitriles to cyanamides was newly discovered and exhibited a wide substrate scope as well as great functional group-tolerability (36 examples). In this efficient strategy, the in situ generated amidoximes obtained from the reaction of nitriles with hydroxylamine subsequently underwent Tiemann rearrangement, producing the corresponding cyanamides with great isolated yields under SO2F2. Additionally, the control experiments reportedly shed light on the tentative mechanism involved in the formation and elimination of the key intermediate: a sulfonyl ester.
- Zhang, Guofu,Zhao, Yiyong,Ding, Chengrong
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supporting information
p. 7684 - 7688
(2019/08/30)
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- Iron(III) Chloride/l-Proline as an Efficient Catalyst for the Synthesis of 3-Substituted 1,2,4-Oxadiazoles from Amidoximes and Triethyl Orthoformate
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A general, facile, and efficient method is presented for the synthesis of 3-substituted 1,2,4-oxadiazoles from amidoximes and triethyl orthoformate. The procedure employs an iron(III) chloride/l-proline catalytic system and the 3-substituted 1,2,4-oxadiaz
- Kaboudin, Babak,Kazemi, Foad,Pirouz, Maryam,Khoshkhoo, Aysan Baharian,Kato, Jun-Ya,Yokomatsu, Tsutomu
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p. 3597 - 3602
(2016/10/18)
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- Mild and efficient one-pot synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from nitriles mediated by K 3PO 4
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Potassium phosphate, K3PO4, has been proved to be a cheap, strong, and efficient reagent for the one-pot synthesis of 3,5-disubstituted-1,2,4-oxadiazoles from nitriles and acid chlorides under mild conditions. [Supplementary material
- Movassagh, Barahman,Talebsereshki, Farzaneh
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supporting information
p. 188 - 194
(2013/12/04)
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- Formation of aromatic amidoximes with hydroxylamine using microreactor technology
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In this contribution, the application of microreactor technology for amidoxime formation is demonstrated, with different aromatic nitriles reacted with a 50% solution of hydroxylamine (HA) under homogeneous conditions to reach full conversion. All reactio
- Voeroes, Attila,Baan, Zoltan,Mizsey, Peter,Finta, Zoltan
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p. 1717 - 1726
(2013/01/15)
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- Organic reactions in water: An efficient method for the synthesis of 1,2,4-oxadiazoles in water
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A simple and efficient process has been developed for the synthesis of 1,2,4-oxadiazoles in good yields through the reaction of amidoximes with anhydrides under catalyst-free conditions in water.
- Kaboudin, Babak,Malekzadeh, Leila
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supporting information; experimental part
p. 6424 - 6426
(2011/12/22)
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- Clean one-pot synthesis of 1,2,4-oxadiazoles under solvent-free conditions using microwave irradiation and potassium fluoride as catalyst and solid support
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Potassium fluoride was found to be an efficient catalyst and solid support for the synthesis of 3,5-disubstituted-1,2,4-oxadiazoles. In this work, a one-pot method for the synthesis of these compounds from the reaction of nitriles with hydroxylamine hydro
- Rostamizadeh, Shahnaz,Ghaieni, Hamid Reza,Aryan, Reza,Amani, Ali Mohammad
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experimental part
p. 494 - 497
(2010/03/03)
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- NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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The present invention relates to novel compounds of formula (I) wherein W, n, X and W’ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors - subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
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Page/Page column 119
(2008/06/13)
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- Novel method for the synthesis of 1,2,4-oxadiazoles using alumina supported ammonium fluoride under solvent-free condition
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Alumina supported ammonium fluoride was found as an efficient reagent for the synthesis of 1,2,4-oxadiazoles of amidoximes under solvent free conditions using microwave irradiation. This method is a one-pot, easy, rapid, and high-yielding reaction for the
- Kaboudin, Babak,Saadati, Fariba
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p. 699 - 701
(2007/10/03)
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- Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: An approach for inhibiting protein-protein interactions
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Fragment assembly has shown promise for discovering small-molecule antagonists for difficult targets, including protein-protein interactions. Here, we describe a process for identifying a 60 nM inhibitor of the interleukin-2 (IL-2)/IL-2 receptor (IL-2Rα)
- Raimundo, Brian C.,Oslob, Johan D.,Braisted, Andrew C.,Hyde, Jennifer,McDowell, Robert S.,Randal, Mike,Waal, Nathan D.,Wilkinson, Jennifer,Yu, Chul H.,Arkin, Michelle R.
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p. 3111 - 3130
(2007/10/03)
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- Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- One-pot synthesis of 1,2,4-oxadiazoles mediated by microwave irradiation under solvent-free condition
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Microwave-assisted synthesis of 1,2,4-oxadiazoles of amidoximes under solvent free conditions was found to be an efficient method for one-pot synthesis of 1,2,4-oxadiazole derivatives from amidoximes and acyl chlorides. This method is an easy, rapid, and
- Kaboudin, Babak,Navaee, Kian
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p. 2287 - 2292
(2007/10/03)
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