448906-42-1Relevant articles and documents
2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE 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 00162-00163, (2021/06/26)
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene 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. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
Compound containing 2,4 - thiazole ring and preparation method and application thereof
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, (2021/08/25)
The invention provides a compound containing 2,4 - thiazole rings and a preparation method and application thereof, wherein the compound is shown in a formula X. A Is pyrazolopyrimidine or indole. Z Is carbonless. X Is O or S. Y Is - O - or - NH . R1 Hydrogen or C1 -6 Alkyl. R2 Be selected from C1 - C3 Alkyl. C5 - C15 Alkenyl, alkynyl, 5 - RMB 10 heterocyclic radicals, C6 - C12 Aryl, 5 -12 membered heteroaryl, sterol and 5-10 元 cycloalkyl. Y And R2 Connection, or Y and R2 Looping. R3 From hydrogen. Halogen, amino, hydroxyl, acetyl, 3 - RMB 10 heterocyclic group, C6 - C12 Aryl, 5 -12-membered heteroaryl, 3 -10-membered cycloalkyl, ester, carboxy, trihalomethyl and adamantyl. R2 Or R3 It is unsubstituted or is selected from C. 1 - C6 Alkyl. A hydroxy group, a halogen group, a trihalomethyl group, a carboxyl group, and a phenyl group. R2 Document C1 - C3 Alkyl, R3 Hydrogen.
A concise synthesis of an AHR endogenous ligand with the indolecarbonylthiazole skeleton
Grzywacz, Pawel,Sicinski, Rafal R.,DeLuca, Hector F.
, p. 1219 - 1224 (2007/10/03)
Short synthesis of an endogenous ligand for the arylhydrocarbon receptor (AHR), 2-(1′H-indole-3′-carbonyl)thiazole-4-carboxylic acid methyl ester (7), has been described. N-Acylation of the L-cysteine methyl ester (4) with indoleglyoxylyl chloride (1) pro