156589-82-1Relevant academic research and scientific papers
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; 00351, (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).
Synthesis production process of thiazole lithium salt
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Paragraph 0052-0065, (2021/08/19)
The invention belongs to the technical field of synthesis production processes of thiazole lithium salt, and particularly relates to a synthesis production process of thiazole lithium salt, which comprises the following steps: adding absolute ethyl alcohol, ethyl thiooxamide and dichloromethane of bromomethyl isopropyl ketone, heating to reflux, adding NaHCO3 and water into a 1000L kettle, evaporating to remove an organic solvent at normal pressure, adding MTBE for extraction, combining organic phases, and washing twice with a 10% saline solution; adding 480Kg of methanol and 160Kg of thiazole ethyl ester into a 1000L reaction kettle, uniformly mixing, adding lithium hydroxide monohydrate, stirring overnight, desolventizing under normal pressure, adding MTBE, stirring and centrifuging; and pumping methanol into a 2000L reaction kettle, adding lithium salt, starting stirring, adding EA, stirring, centrifuging, rinsing with EA, and drying with hot air. According to the present invention, the scheme of first modifying the required functional group and then forming the ring is adopted, such that the reaction condition is mild, the crude product purity is high, the purification can be performed by using the simple crystallization scheme, the conversion efficiency is high, the economic benefit is good, and the environmental protection is easily achieved.
Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV infections
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, (2016/06/28)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
COMPOUNDS AS HEPATITIS C INHIBITORS AND USES THEREOF IN MEDICINE
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Paragraph 00167, (2016/09/22)
Provided herein are compounds as hepatitis C inhibitors and uses thereof in medicine. Specifically, provided herein is a compound of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or hepatitis C diseases. Also provided herein are a pharmaceutically acceptable composition containing such compound and a method of treating HCV infection or hepatitis C diseases comprising administering the compound or pharmaceutical composition thereof disclosed herein.
ANTIMICROBIAL AGENTS
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Paragraph 0208, (2015/05/26)
The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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, (2013/10/22)
Provided are 1-(dihydronaphthalenyl)pyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy for the treatment of obesity and diabetes.
MACROCYCLIC SERINE PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE FOR TREATING HCV INFECTIONS
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, (2012/08/28)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
MACROCYCLIC SERINE PROTEASE INHIBITORS USEFUL AGAINST VIRAL INFECTIONS, PARTICULARLY HCV
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, (2011/02/24)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (Ia) or (Ib), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
MACROCYCLIC SERINE PROTEASE INHIBITORS
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, (2010/11/03)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Macrocylic Inhibitors of Hepatitis C Virus
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, (2009/05/28)
Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl;R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl;p is independently 1 or 2;n is 3, 4, 5 or 6; — denotes an optional double bond;L is N or CRz; Rz is H or forms a double bond with the asterisked carbon;Rq is H or when L is CRz, Rq can also be C1-C6alkyl;Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl;R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl;R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV
