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Sulfur-containing compound based on glutaryl imide skeleton and application of compound
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A technology of compounds and mixtures, which is applied to sulfur-containing compounds based on glutarimide skeleton and its application field, and can solve the problems that biological activity needs to be further improved
Active Publication Date: 2020-09-01
SHANGHAI TECH UNIV
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[0005]
In summary, thalidomide and its derivatives play a vital role in the treatment of multiple myeloma and other related malignant tumors, but there are few reports of such compounds substituted by heteroatoms. The biological activity needs to be further improved, so it is urgent to design and synthesize a series of highly active thalidomide drugs in order to achieve better curative effect
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Embodiment approach 1
[0049] Therefore, one aspect of the present invention provides embodiment 1): a compound of formula (I) or a salt, solvate, isotopically enriched analog, tautomer, polymorph, stereoisomer (including Enantiomers), or mixtures of stereoisomers:
[0050]
[0051] in:
[0052] A means CH 2 or C(O);
[0053] B, U, V, W are the same or different and independently represent CH or N, wherein B, U, V and W are not N at the same time;
[0054] Y means O or S;
[0055] R means SH, and L and X 1 does not exist; or
[0056] R represents S, L represents optionally substituted linear or branched chain alkyl, and X 1 does not exist; or
[0057] R stands for S(O) or S(O) 2 , L represents an optionally substituted linear or branched chain alkyl or amino group, and X 1 does not exist; or
[0058] R stands for S, S(O) or S(O) 2 ,
[0059] L represents an optionally substituted linear or branched alkylene group, wherein the linear or branched alkylene group is optionally interrupted...
Embodiment approach 2
[0074]Embodiment 2): It relates to the compound of formula (I) or its salt, solvate, isotopically enriched analog, tautomer, polymorph, stereoisomer or stereoisomer as described in Embodiment 1). A mixture of isomers, wherein the ring atoms B, U, V, and W in formula (I) are the same and all are CH.
Embodiment approach 3
[0075] Embodiment 3): It relates to the compound of formula (I) or its salt, solvate, isotopically enriched analog, tautomer, polymorph, stereoisomer or stereoisomer as described in Embodiment 1). A mixture of isomers, wherein one of the ring atoms B, U, V, W in the formula (I) is N, and the rest are CH.
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Abstract
The present disclosure relates to compound shown in a formula (I) or salts, solvates, isotope-enriched analogs, tautomers, polymorphs, stereoisomers, or mixtures of stereoisomers of the compound, andthe application thereof in the treatment of tumours. The present disclosure also provides tumor treatment application of the compound showed in a formula (I') or pharmaceutically acceptable salts, solvates, isotope-enriched analogs, tautomers, polymorphic substances, stereoisomers, or mixtures of stereoisomers of the compound.
Description
technical field [0001] The present disclosure generally relates to compounds represented by general formula (I) or salts, solvates, isotopically enriched analogs, tautomers, polymorphs, stereoisomers (including enantiomers) ), or mixtures of stereoisomers, and their use in the treatment of tumors. [0002] Background technique [0003] Multiple myeloma (Multiple myeloma, MM) is a malignant blood cancer, accounting for about 1% of all tumors and 10% of hematological malignancies. The clinical manifestations are anemia, renal dysfunction, repeated infection, and osteolytic bone destruction, and it mostly occurs in middle-aged and elderly people. The main treatment for multiple myeloma is chemotherapy and early autologous stem celltransplantation, but this treatment has poor prognosis and high recurrence rate. The latest research results show that immunomodulatory drugs are an important cornerstone in the treatment of multiple myeloma, which has an important impact on the...
Claims
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