433332-27-5Relevant academic research and scientific papers
Antibacterial Mimics of Natural Products by Side-Chain Functionalization of Bicyclic Tetramic Acids
Josa-Culleré, Laia,Pretsch, Alexander,Pretsch, Dagmar,Moloney, Mark G.
, p. 10303 - 10317 (2018)
Tetramic acids with unsaturated acyl chains are widely found in natural products possessing a range of biological activities, and bicyclic tetramates represent a suitable scaffold to prepare simple mimics of such complex molecules. An efficient route to functionalize the C(6)-acyl group of a bicyclic tetramate was developed and utilized to prepare a small chemical library with a range of saturated and unsaturated side-chains. The analogues with lipophilic residues possessed highly potent antibacterial activity, which was selective for Gram-positive bacteria, and the best compound was 37-fold more potent than the cephalosporin C control and with an appropriate therapeutic window.
TROPOLONE DERIVATIVES AND TAUTOMERS THEREOF FOR IRON REGULATION IN ANIMALS
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Page/Page column 136, (2021/04/23)
Disclosed are a series of compounds or their tautomers having a general structure represented by Formula la or lb and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising said compounds or tautomers or pharmaceutically acceptable salts thereof. Further disclosure relates to a method of treating a disease or condition associated with iron dysregulation or dysfunctional iron homeostasis, comprising administering to a subject in need thereof a therapeutically effective amount of Formula la or lb compounds or tautomers or pharmaceutically acceptable salts thereof.
ACC inhibitor and application thereof
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Paragraph 0250-0252, (2021/05/12)
The invention provides a compound suitable for being used as an acetyl CoA carboxylase (ACC) inhibitor, in particular a thienopyridine derivative, and application of the compound in preparation of medicines for treating metabolic diseases, cancers or other proliferative diseases.
4-PHENYL-N-(PHENYL)THIAZOL-2-AMINE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
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Paragraph 00221; 00232, (2021/06/26)
4-phenyl-N-(phenyl)thiazol-2-amine and 4-(pyridin-3-yl)-N-( phenyl) thiazol-2-amine derivatives and the corresponding thiadiazole, thiophene, oxazole, oxadiazole, imidazole and triazole derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders.
COMPOSITIONS FOR THE TREATMENT OF BRAIN TUMORS
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Page/Page column 48, (2020/05/19)
The instant invention describes pharmaceutical compositions and dosing regimens comprising radiation therapy and seviteronel with or without dexamethasone, and methods of treating diseases, disorders or symptoms thereof.
MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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Paragraph 1220, (2020/10/09)
The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
Preparation method of thienopyrimidinedione compound
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Paragraph 0140-0142, (2020/02/20)
The invention provides a preparation method of a compound shown as a general formula c, wherein the definition of substituent is as defined in the specification. Please see the specification for the formula.
Widely Exploited, Yet Unreported: Regiocontrolled Synthesis and the Suzuki–Miyaura Reactions of Bromooxazole Building Blocks
Solomin, Vitalii V.,Radchenko, Dmytro S.,Slobodyanyuk, Evgeniy Y.,Geraschenko, Oleksandr V.,Vashchenko, Bohdan V.,Grygorenko, Oleksandr O.
, p. 2884 - 2898 (2019/03/07)
An approach to synthesis of 2-, 4-, and 5-bromooxazoles is described. The method was optimized, and its scope was extended to all three isomeric parents, as well as various alkyl- and aryl-substituted bromooxazoles. It was found that direct regiocontrolled lithiation followed by reaction with electrophilic bromine source was common for all substrates and led exclusively to the target substituted 2-, 4- and 5-bromooxazoles on multigram scale. The utility of the multipurpose building blocks obtained in this work was demonstrated in the Suzuki–Miyaura cross-coupling reaction under parallel synthesis conditions.
COMPOSITIONS FOR THE TREATMENT OF BRAIN TUMORS
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Page/Page column 45-46, (2019/10/15)
The instant invention describes pharmaceutical compositions and dosing regimens comprising seviteronel and/or dexamethasone, and methods of treating diseases, disorders symptoms thereof.
Asymmetric Total Synthesis of (-)-(3 R)-Inthomycin C
Balcells, Sandra,Haughey, Maxwell B.,Walker, Johannes C. L.,Josa-Culleré, Laia,Towers, Christopher,Donohoe, Timothy J.
supporting information, p. 3583 - 3586 (2018/06/26)
A short (10 step) and efficient (15% overall yield) synthesis of the natural product (-)-(3R)-inthomycin C is reported. The key steps comprise three C-C bond-forming reactions: (i) a vinylogous Mukaiyama aldol, (ii) an olefin cross-metathesis reaction, and (iii) an asymmetric Mukaiyama-Kiyooka aldol. This route is notable for its brevity and has the advantage of lacking stoichiometric tin-promoted cross-coupling reactions present in previous approaches. Initial investigations on the biological activity of (-)-(3R)-inthomycin C and structural analogues on human cancer cell lines are also described for the first time.
