7250-94-4Relevant articles and documents
Thermal and bromide ion-catalyzed rearrangement of benzofuran dioxetanes to 1-oxaspiro[2.5]octa-5,7-dien-4-ones
Adam, Waldemar,Ahrweiler, Michael,Reinhard, Dirk
, p. 6713 - 6718 (1994)
The reaction of the tetrasubstituted benzofuran dioxetanes 2 with various nucleophiles, e.g. Br-, Cl-, I-, and HN(i-Pr)2, was investigated and the unprecedented bromide ion-catalyzed rearrangement to the hithert
A medicinal composition for combining thioxanthone paclitaxel and STAT3 inhibitor
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Paragraph 0043; 0044; 0045; 0046, (2019/01/23)
A medicinal composition for combining thioxanthone paclitaxel and STAT3 inhibitor, comprising an active ingredient and a pharmaceutically acceptable adjuvant, characterized in that the active ingredient is composed of paclitaxel and a STAT3 inhibitor represented by formula (I) (shown in the description), and the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in theactive ingredient is (0.18 to 0.32): 1. The compound has an effect on MDA having persistently activated STAT3 activity-MB-468 cell, DU-145 cells had good inhibitory effect.
Medicinal composition for combination of paclitaxel and fluorene STAT3 inhibitor
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Paragraph 0045-0048, (2019/02/04)
The invention belongs to the field of pharmaceutical chemistry, and relates to a medicinal composition for combination of paclitaxel and fluorene STAT3 inhibitors. The medicinal composition comprisesan active ingredient consisting of paclitaxel and a STAT3 inhibitor represented by formula (I), and a pharmaceutically acceptable adjuvant, wherein the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in the active ingredient is (0.27 to 0.39): 1. The compound has an effect on having persistently activated STAT3 activity MDA-MB-468 cell, DU-145 cells had good inhibitory effect.
A carbazole class STAT inhibitors maleic acid salt crystal form II combination pharmaceutical composition and its preparation method
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Paragraph 0039-0042, (2019/02/13)
The invention belongs to the field of medicinal chemistry, and in particular relates to with tumor compound of 4 - (9 - ethyl - 9 H - carbazole - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - amine maleic acid salt of a new crystalline form, its preparation method, comprising the composition of said form, said form and said form or comprise the composition of use in the preparation of the medicament, the crystalline form II has good physical and chemical stability, solubility and bioavailability, is suitable for formulation development.
STAT3 inhibitors and application thereof
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Paragraph 0037-0040, (2019/01/20)
The invention belongs to the field of medical chemistry, relates to STAT3 inhibitors and an application thereof and particularly relates to compounds for inhibiting the signal transduction and transcription activator-3, a pharmaceutical composition containing the compound and a use of the compounds or the pharmaceutical composition as cancer treatment drugs. The compounds can well inhibit MDA-MB-468 cells and DU-145 cells with sustained STAT3 activity.
Preparation method of STAT3 inhibitor
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Paragraph 0047-0050, (2019/01/23)
The invention belongs to the field of medical chemistry, relates to a class-I STAT3 inhibitor and an application thereof, and particularly relates to a method for preparing compounds having signal transduction and transcriptional activator 3 inhibitory effects. The compounds can well inhibit MDA-MB-468 cells and DU-145 cells with continuous STAT3 activity.
A fluorene STAT3 inhibitor and its preparation method
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Paragraph 0044-0047, (2019/02/13)
The invention belongs to the field of medicinal chemistry, relates to a compound of formula (I) of fluorene STAT3 inhibitor and its application, in particular to a kind of with signal conduction with a transcription activating factor - 3 inhibiting effect of a compound, pharmaceutical composition containing the compound, and the compound or pharmaceutical composition as the use of the cancer therapy, the compounds with sustained activation of STAT3 activity of MDA - MB - 468 cell, DU - 145 cell good inhibition effect.
Combined pharmaceutical composition of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate
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Paragraph 0027-0030, (2019/01/24)
The invention provides a combined pharmaceutical composition of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate, comprising active ingredients and pharmaceutically acceptable excipients. The active ingredient consists of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate represented by formula (I), and the mass ratio of paclitaxel to dibenz [b, d] thiophene STAT inhibitor tartrate represented by formula (I) in the active ingredient is (0.09 to 0.21): 1. A tartrate salt in that composition has good water solubility, high bioavailability and good stability.
A medicinal composition for combine paclitaxel and fluorenone STAT3 inhibitor
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Paragraph 0042-0045, (2019/01/24)
Disclosed is a medicinal composition for combine paclitaxel and fluorenone STAT3 inhibitor comprising an active ingredient and a pharmaceutically acceptable adjuvant, characterized in that the activeingredient is composed of paclitaxel and a STAT3 inhibitor represented by formula (I), and the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in the active ingredient is (0.21 to 0.32): 1. The compound has an effect on MDA having persistently activated STAT3 activity-MB-468 cell, DU-145 cells had good inhibitory effect.
A paclitaxel and carbazole class STAT3 inhibitor crystalline form A combination pharmaceutical composition
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Paragraph 0029; 0040-0042, (2019/02/13)
The present invention provides a kind of paclitaxel and carbazole class STAT3 inhibitor crystalline form A combination pharmaceutical composition, comprising an active ingredient and a pharmaceutically acceptable auxiliary material, characterized in that the by the taxol the active ingredient of the formula (I) indicated by the STAT3 inhibitors A a crystalline form, the active ingredient of taxol in the formula (I) indicated by the STAT3 inhibitors the mass ratio of the crystalline form A (0.09 - 0.21): 1. The A crystalline form has good physical and chemical stability, solubility and bioavailability, suitable for formulation development.
