- Novel O-acylated amidoximes and substituted 1,2,4-oxadiazoles synthesised from (+)-ketopinic acid possessing potent virus-inhibiting activity against phylogenetically distinct influenza A viruses
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This article describes the synthesis and antiviral activity evaluation of new substituted 1,2,4-oxadiazoles containing a bicyclic substituent at position 5 of the heterocycle and O-acylated amidoximes as precursors for their synthesis. New compounds were
- Borisevich, Sophia S.,Chernyshov, Vladimir V.,Esaulkova, Iana L.,Popadyuk, Irina I.,Salakhutdinov, Nariman F.,Sinegubova, Ekaterina,Yarovaya, Olga I.,Zarubaev, Vladimir V.
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- An Efficient Synthesis of 2-Substituted Quinazolin-4(3H)-ones by Using Recyclable Wang Resin Supported Sulfonic Acid Catalyst
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An efficient synthesis of 2-substituted Quinazolin-4(3H)-ones has been developed from isatoic anhydride with various amidoximes by using a recyclable polymer-supported sulphonic acid catalyst. Excellent functional group compatibility and high yields are the important features of this protocol.
- Kallam, Srinivasa Reddy,Kalyani, K.
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p. 790 - 796
(2022/03/01)
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- SO2F2-Mediated one-pot cascade process for transformation of aldehydes (RCHO) to cyanamides (RNHCN)
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A simple, mild and practical cascade process for the direct conversion of aldehydes to cyanamides was developed featuring a wide substrate scope and great functional group tolerability. This method allows for transformations of readily available, inexpensive, and abundant aldehydes to highly valuable cyanamides in a pot, atom, and step-economical manner with a green nitrogen source. This protocol will serve as a robust tool for the installation of the cyanamide moiety in various complicated molecules.
- Ding, Chengrong,Ge, Shuting,Wei, Junjie,Zhang, Guofu,Zhao, Yiyong
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p. 17288 - 17292
(2020/05/18)
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- SSAO INHIBITOR
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The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
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Paragraph 0183-0185; 0197; 0198; 0199
(2020/04/02)
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- SUBSTITUTED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS
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Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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Page/Page column 264; 267
(2020/08/28)
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- 5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein
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The HIV-1 nucleocapsid (NC) protein is a small basic DNA and RNA binding protein that is absolutely necessary for viral replication and thus represents a target of great interest to develop new anti-HIV agents. Moreover, the highly conserved sequence offers the opportunity to escape the drug resistance (DR) that emerged following the highly active antiretroviral therapy (HAART) treatment. On the basis of our previous research, nordihydroguaiaretic acid 1 acts as a NC inhibitor showing moderate antiviral activity and suboptimal drug-like properties due to the presence of the catechol moieties. A bioisosteric catechol replacement approach led us to identify the 5-dihydroxypyrimidine-6-carboxamide substructure as a privileged scaffold of a new class of HIV-1 NC inhibitors. Hit validation efforts led to the identification of optimized analogs, as represented by compound 28, showing improved NC inhibition and antiviral activity as well as good ADME and PK properties.
- Malancona, Savina,Mori, Mattia,Fezzardi, Paola,Santoriello, Marisabella,Basta, Andreina,Nibbio, Martina,Kovalenko, Lesia,Speziale, Roberto,Battista, Maria Rosaria,Cellucci, Antonella,Gennari, Nadia,Monteagudo, Edith,Di Marco, Annalise,Giannini, Alessia,Sharma, Rajhans,Pires, Manuel,Real, Eleonore,Zazzi, Maurizio,Dasso Lang, Maria Chiara,De Forni, Davide,Saladini, Francesco,Mely, Yves,Summa, Vincenzo,Harper, Steven,Botta, Maurizio
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supporting information
p. 766 - 772
(2020/07/14)
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- Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes
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As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments
- Choung, Wonken,Yang, Deokmo,Kim,Choi, Hyukjoon,Lee, Bo Ram,Park, Min,Jang, Su Min,Lim, Jae Soo,Kim, Woo Sik,Kim, Kyung-Hee,Chin, Jungwook,Jung, Kyungjin,Lee, Geumwoo,Hong,Jang, Tae-ho,Joo, Jeongmin,Hwang, Hayoung,Myung, Jayhyuk,Kim, Seong Heon
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p. 2275 - 2282
(2019/06/27)
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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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- Copper-catalyzed one-pot synthesis of 1,2,4-triazoles from nitriles and hydroxylamine
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A simple and efficient copper-catalyzed one-pot synthesis of substituted 1,2,4-triazoles through reactions of two nitriles with hydroxylamine has been developed. The protocol uses simple and readily available nitriles and hydroxylamine hydrochloride as th
- Xu, Hao,Ma, Shuang,Xu, Yuanqing,Bian, Longxiang,Ding, Tao,Fang, Xiaomin,Zhang, Wenkai,Ren, Yanrong
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supporting information
p. 1789 - 1794
(2015/02/19)
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- An Efficient Synthesis of 2-Substituted Quinazolin-4(3 H)-ones Catalyzed by Iron(III) Chloride
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A simple and highly efficient synthesis of 2-substituted quinazolin-4(3H)-ones by the iron(III) chloride catalyzed reaction of isatoic anhydride with various amidoxime derivatives was developed. Several aryl and alkyl amidoximes were screened to demonstra
- Mekala, Ramamohan,Akula, Raghunadh,Kamaraju, Raghavendra Rao,Bannoth, Chandrasekhar Kothapalli,Regati, Sridhar,Sarva, Jayaprakash
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supporting information
p. 821 - 826
(2014/04/03)
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- Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4- methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases
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Class I phosphoinositide 3-kinases (PI3Ks), particularly PI3Kγ, have become attractive drug targets for inflammatory and autoimmune disorders such as rheumatoid arthritis. Herein, we describe the synthesis and the structure-activity relationships (SAR) of a series of 2-amino-5-oxadiazolyl thiazoles, culminating in the identification of 8j (TASP0415914), an orally potent inhibitor of phosphoinositide 3-kinase γ (PI3Kγ). TASP0415914 demonstrated good potency in a cell-based assay and, furthermore, exhibited in vivo efficacy in a collagen induced arthritis (CIA) model in mice after oral administration.
- Oka, Yusuke,Yabuuchi, Tetsuya,Oi, Takahiro,Kuroda, Shoichi,Fujii, Yasuyuki,Ohtake, Hidenori,Inoue, Tomoyuki,Wakahara, Shunichi,Kimura, Kayo,Fujita, Kiyoko,Endo, Mayumi,Taguchi, Kyoko,Sekiguchi, Yoshinori
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p. 7578 - 7583
(2014/01/06)
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- AMINOTHIAZOLE DERIVATIVE
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A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase 3 inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn''s disease, irritable colitis, Sjoegren''s syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.
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Page/Page column 9
(2012/09/10)
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- Sulfone compounds which modulate the CB2 receptor
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Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating p
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Page/Page column 34
(2012/03/08)
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- FUSED HETEROCYCLIC RING COMPOUND
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A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: -COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.
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Page/Page column 95
(2012/01/11)
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- SULFONE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating p
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Page/Page column 55-56
(2009/12/23)
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- Development of 2-tbutyl-N-methyl pyrimidones as potent inhibitors of HIV integrase
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A series of novel 2-tbutyl-N-methyl pyrimidone HIV-1 integrase inhibitors have been identified. Optimization of the initial lead resulted in compounds such as 9d and 14a, which showed high levels of activity in cell culture inhibiting viral rep
- Di Francesco, M. Emilia,Pace, Paola,Fiore, Fabrizio,Naimo, Francesca,Bonelli, Fabio,Rowley, Michael,Summa, Vincenzo
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p. 2709 - 2713
(2008/12/21)
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- (1,5-DIPHENYL-1H-PYRAZOL-3-YL)OXADIAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS
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The invention relates to compounds having formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to a method of preparing said compounds and to the application thereof in therapeutics.
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Page/Page column 23
(2008/06/13)
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- ARYLSULFONAMIDE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) and the formula (IA) wherein, R1, R2, R3, R4, R5/sup
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Page/Page column 49; 51
(2008/12/08)
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- Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
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GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of dia
- Semple, Graeme,Fioravanti, Beatriz,Pereira, Guillherme,Calderon, Imelda,Uy, Jane,Choi, Karoline,Xiong, Yifeng,Ren, Albert,Morgan, Michael,Dave, Vibha,Thomsen, William,Unett, David J.,Xing, Charles,Bossie, Stuart,Carroll, Chris,Chu, Zhi-Liang,Grottick, Andrew J.,Hauser, Erin K.,Leonard, James,Jones, Robert M.
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scheme or table
p. 5172 - 5175
(2009/07/01)
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- Synthesis of various 3-substituted 1,2,4-oxadiazole-containing chiral β3- and α-amino acids from Fmoc-protected aspartic acid
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Various 3-substituted chiral 1,2,4-oxadiazole-containing Fmoc-β 3- and α-amino acids were synthesized from FmoC-(L or D)-Asp(OtBu)-OH and Fmoc-L-Asp-OtBu, respectively, in three steps (i.e., condensation of an aspartyl derivative with different
- Hamze?, Abdallah,Hernandez, Jean-Franc?ois,Fulcrand, Pierre,Martinez, Jean
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p. 7316 - 7321
(2007/10/03)
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- Aryl and heteroaryl alkoxynaphthalene derivatives
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Compounds of the formula wherein R1, R2, R4, R23, R24, R25 and R26 are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.
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- Use of naphthalene derivatives in treating lung carcinoma
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A method of inhibiting cell growth in human small cell lung carcinoma comprising administering to a mammal in need of such treatment a cell growth inhibitory amount of a compound of the formula STR1
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- Use of naphthalene derivatives in treating lung carcinoma
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The use of a compound of the formula or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for inhibiting cell growth in human small cell lung carcinoma through inhibition of the 5HT1D receptor.
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- New Acetonylsubstituted Azoles, I. 5-Acetonyl-1,2,4-oxadiazoles
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Aliphatic amidoximes R-C(NH2)=NOH react with diketene to yield 5-acetonyl-3-alkyl-1,2,4-oxadiazoles, which are susceptible to a wide variety of reactions at the keto-group as well as at the methylene-group.Their transformations into 1-methyl-2-oxadiazolyl
- Kuebel, Boerries
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p. 781 - 792
(2007/10/02)
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