1034975-35-3Relevant academic research and scientific papers
Preparation method and application of broad-spectrum anticancer drug entrectinib intermediate
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Paragraph 0052-0067, (2021/06/13)
The invention relates to the field of preparation of 2-amino-4-(4-methyl-1-piperazine) tert-butyl benzoate, in particular to a preparation method and application of a broad-spectrum anticancer drug emtricitinib intermediate. The preparation method of the broad-spectrum anticancer drug emtricitinib intermediate comprises the step of reacting 2-nitro-4-(4-methyl-1-piperazinyl)-tert-butyl benzoate with sulfur-containing alkali metal at the temperature of 5-100 DEG C in a solvent in the presence of inorganic alkali to obtain the product. Based on the low-cost and easily available sodium hydrosulfite reduction process, the use of a controlled dangerous hydrogenation process and special equipment is avoided, the reaction condition is mild, the stability is good, the production cost is greatly reduced. the preparation method is environmentally friendly, economical and suitable for large-scale production.
Indazole compound for inhibiting kinase activity as well as composition and application thereof
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Paragraph 0202; 0205; 0209; 0210, (2018/10/27)
The invention relates to an indazole compound for inhibiting kinase activity and relates to preparation and application of the indazole compound. Specifically, the invention discloses the indazole compound shown as a formula (I), or crystal forms, prodrugs, pharmaceutically acceptable salts, stereoisomers, tautomers, solvates or pharmaceutical compositions of hydrates of the indazole compound. Thecompound and the composition containing the compound, provided by the invention, have excellent inhibition performance on kinase protein, and also have better pharmacokinetics parameter characteristics at the same time; the medicine concentration of the compound in animals can be improved and the curative effect and safety of the medicine are improved. The formula (I) is shown in the description.
HETEROCYCLIC DERIVATIVES MODULATING ACTIVITY OF CERTAIN PROTEIN KINASES
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Page/Page column 45, (2016/07/05)
The present invention relates to novel heterocyclic derivatives having general formula (I) and their therapeutic use for diseases such as cancer, inflammation, pain, autoimmune diseases or neurodegenerative diseases like Alzheimer's or Parkinson's disease that can be treated by modulation of certain protein kinases. Compounds of formula (I) can be used for treatment of patients who do not respond to kinase inhibition therapy that comprises currently available medications.
Derivatives of azaindoles or diazaindoles for treating pain
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Paragraph 0278-0279, (2014/02/15)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING PAIN
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Page/Page column 87; 88, (2014/02/16)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING A CANCER OVEREXPRESSING TRK
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Page/Page column 87, (2014/02/16)
The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk
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Paragraph 0367-0370, (2014/02/15)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
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Paragraph 0468; 0469; 0470; 0471, (2013/04/13)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
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Page/Page column 88-89, (2012/08/08)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Page/Page column 71, (2010/08/05)
Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may
