206555-77-3Relevant articles and documents
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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Page/Page column 14-15; 40; 52; 56, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
2-Amino-4-arylthiazoles through One-Pot Transformation of Alkylarenes with NBS and Thioureas
Shibasaki, Kaho,Togo, Hideo
, p. 2520 - 2527 (2019/04/04)
Treatment of alkylarenes with N-bromosuccinimide in a mixture of ethyl acetate and water at 60 °C, a mixture of acetonitrile and water at 80 °C, or a mixture of diethyl carbonate and water under irradiation with a tungsten lamp, followed by a reaction with thioureas or arenethioamides provided the corresponding 2-amino- 4-arylthiazoles or 2,4-diarylthiazoles in good to moderate yields, respectively, in one pot. The present reaction is an efficient one-pot transformation method of alkylarenes into 2-amino-4-arylthiazoles and 2,4-diarylthiazoles directly under mild and transition-metal-free conditions.
4 - substituted -2 - amino thiazole compound preparation method
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Paragraph 0024; 0025; 0026; 0027; 0028; 0029-0044; 0075-0079, (2017/08/24)
The invention discloses a preparation method of a 4-substituted-2-aminothiazole compound. The method comprises the following step: olefin azide shown by the formula I reacts with potassium thiocyanate under the catalysis of palladium acetate to obtain the 4-substituted-2-aminothiazole compound, wherein the molar ratio of the olefin azide compound to potassium thiocyanate to palladium acetate is 20:(59-61):1, the reaction temperature is 75-85 DEG C, and the reaction time is 11-13 hours; and in the formula I, R1 is phenyl, 2-bromophenyl, 3-bromophenyl, 4-bromophenyl, 4-methylphenyl, 4-ethyoxy-3-bromophenyl, 3-nitrophenyl, 4-methoxyacylphenyl, 1-naphthyl, phenylaminomethyl or trans-4-(3-phenylallyloxymethyl).
Selective Access to 4-Substituted 2-Aminothiazoles and 4-Substituted 5-Thiocyano-2-aminothiazoles from Vinyl Azides and Potassium Thiocyanate Switched by Palladium and Iron Catalysts
Chen, Binhui,Guo, Shanshan,Guo, Xiao,Zhang, Guolin,Yu, Yongping
supporting information, p. 4698 - 4701 (2015/10/12)
A highly selective construction of 4-substituted 2-aminothiazoles and 4-substituted 5-thiocyano-2-aminothiazoles, respectively, catalyzed by palladium(II) acetate and promoted by iron(III) bromide from vinyl azides and potassium thiocyanate has been developed. Use of readily available starting materials, high selectivity, as well as mild reaction conditions make this practical method particularly attractive.
Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA
Annadurai, Sivakumar,Martinez, Rogelio,Canney, Daniel J.,Eidem, Tess,Dunman, Paul M.,Abou-Gharbia, Magid
supporting information, p. 7719 - 7725 (2013/02/21)
Privileged structure-based libraries have been shown to provide high affinity lead compounds for a variety of important biological targets. The present study describes the synthesis and screening of a 2-aminothiazole based compound library to determine th
Direct preparation of thiazoles, imidazoles, imidazopyridines and thiazolidines from alkenes
Donohoe, Timothy J.,Kabeshov, Mikhail A.,Rathi, Akshat H.,Smith, Ian E. D.
, p. 1093 - 1101 (2012/04/04)
A range of heterocycles, namely thiazoles, imidazoles, imidazopyridines, thiazolidines and dimethoxyindoles, have been synthesised directly from alkenes via a two-step ketoidoination/cyclisation protocol. The alkene starting materials are themselves readily accessible using many different and well-established approaches, and allow access to a variety of heterocycles with excellent yields and regioselectivity.
ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND MEDICINAL APPLICATION
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Page/Page column 29, (2010/12/29)
Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or m
CHEMICAL COMPOUNDS
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Page/Page column 59, (2008/12/05)
Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also desc
DERIVATIVES OF THIAZOLE AND THIADIAZOLE INHIBITORS OF TYROSINE PHOSPHATASES
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Page/Page column 71, (2010/10/20)
Provided herein are compounds and compositions for modulation of tyrosine phosphatase activity. In one embodiment, compounds and compositions for inhibiting protein tyrosine phosphatase activity are provided. In another embodiment, provided herein are compounds and compositions that are useful in the treatment, prevention, or amelioration of one or more symptoms of diseases caused by dysfunctional signal transduction, or in which dysfunctional signal transduction is implicated. In another embodiment, provided herein are compounds and compositions for treatment, prevention, or amelioration of one or more symptoms of diabetes. The compounds have following formulas: (II), (I), (III), and (IV).
NOVEL ETHYLENEDIAMINE DERIVATIVES
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Page/Page column 109, (2010/02/14)
A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.