880160-63-4Relevant academic research and scientific papers
WDR5-MYC INHIBITORS
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Paragraph 00494; 00554-00555; 00894-00895, (2021/02/05)
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Method for preparing intermediate for drug for treating ovarian cancer
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Paragraph 0033; 0039-0041; 0044-0048; 0050-0055; 0057-0061, (2019/01/08)
The invention belongs to the technical field of chemical drugs, and particularly relates to a method for preparing an intermediate for a drug for treating ovarian cancer. According to the method, zirconium n-butoxide and ferric chloride serve as raw mater
Preparation method of key intermediate 1408282-26-7 of ovarian cancer resisting drug Rucaparib
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Paragraph 0040-0041; 0047-0048; 0054-0055, (2018/11/22)
The invention discloses a preparation method of a key intermediate 1408282-26-7 of an ovarian cancer resisting drug Rucaparib, and relates to preparation of medical intermediates. The preparation method comprises the following steps: reacting a compound 1 with potassium nitrate to obtain a compound 2; reacting the compound 2 with trimethylsilylacetylene to obtain a compound 3; reacting the compound 3 with hydrogen to obtain a compound 4; carrying out self cyclization on the compound 4 to obtain a compound 5; reacting the compound 5 with nitroethylene to obtain a compound 6; reacting the compound 6 with the hydrogen to obtain the key intermediate 1408282-26-7 of the ovarian cancer resisting drug Rucaparib. The method has the advantages that nitro-sulfuric acid mixed nitration reaction and the discharge of wastewater and waste gas are avoided, safe production is ensured, and safety and environment friendliness are realized; raw materials are easy to obtain and low in price and cost, thereby facilitating industrial production; the reaction yield is greatly improved, the reaction route is optimized, the product purification steps are simplified and the industrial production is facilitated.
BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 56, (2009/08/16)
A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
Method of preparing poly(ADP-ribose) polymerases inhibitors
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Page/Page column 5; 8, (2010/10/20)
This invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, via a key Sonogashira coupling reaction and a CuI-promoted indole formation.
