144432-72-4Relevant academic research and scientific papers
A new method for the synthesis of nonsymmetrical sulfamides using Burgess-type reagents
Nicolaou,Longbottom, Deborah A.,Snyder, Scott A.,Nalbanadian, Annie Z.,Huang, Xianhai
, p. 3866 - 3870 (2002)
A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N′-differentiated sulfamides has been developed from a wide range of amino alcohols and simple amines using Burgess-type reagents (see scheme). This method
Synthesis of N-substituted 1,2,5-thiadiazolidine and 1,2,6-thiadiazinane 1,1-dioxides from primary amines
Johnson, Paul D.,Jewell, Sarah A.,Romero, Donna L.
, p. 5483 - 5485 (2003)
Alkyl and aryl N-substituted 1,2,5-thiadiazolidine and 1,2,6-thiadiazinane 1,1-dioxides 6 were synthesized in good yields from the reaction of sulfuryl chloride with 2-chloroethylamine or 3-chloropropylamine hydrochlorides, respectively, followed by treatment with a primary amine and triethylamine, and ring closure with K2CO3 in DMSO.
Discovery of New Imidazo[2,1- b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising in Vitro and in Vivo Anti-melanoma Activity
Abdel-Maksoud, Mohammed S.,El-Gamal, Mohammed I.,Lee, Bong S.,Gamal El-Din, Mahmoud M.,Jeon, Hong R.,Kwon, Dow,Ammar, Usama M.,Mersal, Karim I.,Ali, Eslam M. H.,Lee, Kyung-Tae,Yoo, Kyung Ho,Han, Dong Keun,Lee, Jae Kyun,Kim, Garam,Choi, Hong Seok,Kwon, Young Jik,Lee, Kwan Hyi,Oh, Chang Hyun
, p. 6877 - 6901 (2021/06/25)
BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major obstacle against treatment of many cancer types. In this work, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing a terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect of the new series was investigated, and structure-activity relationship is discussed. Antiproliferative activity of the target compounds was tested against the NCI-60 cell line panel. The most active compounds were further tested to obtain their IC50 values against cancer cells. Compound 27c with terminal open chain sulfonamide and 38a with a cyclic sulfamide moiety showed the highest activity in enzymatic and cellular assay, and both compounds were able to inhibit phosphorylation of MEK and ERK. Compound 38a was selected for testing its in vivo activity against melanoma. Cellular and animal activities are reported.
Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors
Chen, Shulun,Guo, Wei,Liu, Xiaohua,Sun, Pu,Wang, Yi,Ding, Chunyong,Meng, Linghua,Zhang, Ao
, p. 38 - 55 (2019/06/25)
Indoleamine 2, 3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism which is an important mechanism in immune tolerance. The small molecule epacadostat is the most advanced IDO1 inhibitor, but its phase III trials as a single agent or in combi
A kind of IDO inhibitor and use thereof
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Paragraph 0474-479, (2019/07/11)
The embodiment of the invention provides general formula (I) compound or its pharmaceutically acceptable salts, stereoisomers, a tautomeric form each other, polymorphs, solvate, prodrug, metabolite or isotope derivatives, wherein the substituents R1
6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE AND 6,7-DIHYDRO-4H-TRIAZOLO[1,5-A]PYRAZINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES
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Page/Page column 30; 31, (2018/03/28)
The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 and Q are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
Aromatic polycyclic carboxylic acid derivatives
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Paragraph 0383; 0384; 0385, (2017/08/26)
The invention specifically relates to aromatic polycyclic carboxylic acid derivative GPR40 receptor agonists as shown in a general formula (I) which is described in the specification, and pharmaceutically acceptable salts, esters or stereoisomers thereof,
Carbazole-Containing Sulfonamides as Cryptochrome Modulators
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Paragraph 0435-0436, (2013/11/19)
The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
Synthesis of new 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl) imidazo[2,1-b] thiazole derivatives and their antiproliferative activity against melanoma cell line
Park, Jin-Hun,Oh, Chang-Hyun
experimental part, p. 2854 - 2860 (2012/04/17)
Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated.
ORGANIC COMPOUNDS
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Page/Page column 97-98, (2008/12/08)
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
