- Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer
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Co-targeting PARP and PI3K by PARP/PI3K dual inhibitors has been recognized as a promising chemotherapeutic strategy for the treatment of triple negative breast cancer (TNBC) in our previous work. To further explore novel and more potent PARP/PI3K dual in
- Wang, Junwei,He, Guangchao,Li, Hui,Ge, Yiran,Wang, Shuping,Xu, Yungen,Zhu, Qihua
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- PREPARATION OF A 1,3,5-TRIAZINYL BENZIMIDAZOLE
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Described herein is the preparation of a 1,3,5-triazinyl benzimidazole and chemical intermediates used in the synthetic process.
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Paragraph 0111-0113
(2021/10/15)
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- PARP-1 and PI3K double-target inhibitor containing benzofuran
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The invention relates to the field of medicinal chemistry, in particular to a PARP-1 and PI3K double-target inhibitor containing a benzofuran structure (I) (the formula I is shown in the description),a preparation method and a medicine composition containing thereof. Proved by a pharmacodynamic test, the PARP-1 and PI3K double-target inhibitor has the anti-tumor effect.
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Paragraph 0110; 0112-0113
(2019/06/08)
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- 1. 3, 5 - Triazine derivatives and use thereof
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The invention relates to novel 1,3,5-triazine derivatives represented by the formula I, and pharmaceutically-acceptable salts, hydrates, solvate, and prodrug thereof; wherein the definitions of substituent R1 and substituent R2 are represented in the description. The invention also relates to a preparation method and an application of the derivatives represented by the formula (I) in antitumor drugs.
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Paragraph 0068-0070
(2018/07/30)
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- NOVEL 1,3,5 -TRIAZINE BASED PI3K INHIBITORS AS ANTICANCER AGENTS AND A PROCESS FOR THE PREPARATION THEREOF
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The present invention describes heterocyclic compounds of general Formula 1 and their method of preparation thereof. The present invention describes general Formula 1 which inhibits phosphoinositide 3-kinase (PI3K) and can be used as the anticancer agents
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Paragraph 027
(2016/06/15)
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- PHOSPHOINOSITIDE 3-KINASE (PI3K) INHIBITORS
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The invention relates to compounds, and uses of the compounds, that are inhibitors of the enzyme phosphoinositide 3-kinase (PI3K). More particularly the compounds are selective inhibitors of one or more isoforms of PI3K. In particular embodiments the compounds are selective inhibitors of one isoform of PI3K
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- DUAL MEK/PI3K INHIBITORS AND THERAPEUTIC METHODS USING THE SAME
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Dual inhibitors of MEK and PI3K and compositions containing the same are disclosed. Methods of using the dual MEK/PI3K inhibitors in the treatment of diseases and conditions wherein inhibition of MEK and PI3K provides a benefit, like cancers, also are disclosed.
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Paragraph 0206-0207
(2014/10/18)
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- L-aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target nonconserved Asp862 of PI3Kβ
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A series of aminoacyl-triazine derivatives based upon the pan-PI3K inhibitor ZSTK474 were identified as potent and isoform-selective inhibitors of PI3Kβ. The compounds showed selectivity based upon stereochemistry with l-amino acyl derivatives preferring PI3Kβ, while their d-congeners favored PI3Kδ. The mechanistic basis of this inhibition was studied using site-directed mutants. One Asp residue, D862, was identified as a critical participant in binding to the PI3Kβ-selective inhibitors, distinguishing this class from other reported PI3Kβ-selective inhibitors. The compounds show strong inhibition of cellular Akt phosphorylation and growth of PTEN-deficient MD-MBA-468 cells.
- Pinson, Jo-Anne,Zheng, Zhaohua,Miller, Michelle S.,Chalmers, David K.,Jennings, Ian G.,Thompson, Philip E.
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p. 206 - 210
(2013/03/29)
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- SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES
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The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.
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Paragraph 0237; 0239
(2013/03/26)
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- PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS
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The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.
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Paragraph 0087
(2013/03/26)
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- SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES
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The invention relates to new triazines (G = Q = U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.
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Page/Page column 74
(2011/10/10)
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- PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS
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The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl- sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.
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Page/Page column 29-30
(2011/11/13)
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- SUBSTITUTED PYRIMIDINES AND TRIAZINES AND THEIR USE IN CANCER THERAPY
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Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with
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Page/Page column 87-88
(2009/10/22)
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- Treatment of prostate cancer, melanoma or hepatic cancer
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The present application describes a method of treating prostate cancer, melanoma or hepatic cancer in a subject in need thereof, the method comprising administering to said subject a therapeutically effective amount of the heterocyclic compound represented by Formula I or its pharmaceutically acceptable salt:
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Page/Page column 4
(2008/06/13)
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- HETEROCYCLIC COMPOUND AND ANTITUMOR AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT
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The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; R1 represents CHnF3-n (wherein n is 1 or 2), hydroxy C1-C6 alkyl, NHR6 [wherein R6 represents hydrogen atom or COR (wherein R represents hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy)]; R2 represents morpholino (which may be substituted with one to four C1-C6 alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C1-C6 alkyl), oxazolidinyl (which may be substituted with one or two C1-C6 alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R3 and R4 each represent hydrogen atom or C1-C6 alkyl; and R5 represents hydrogen atom, amino or hydroxyl.
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