- PYRIMIDO[5,4-d]PYRIMIDINE DERIVATIVES AS ENT INHIBITORS FOR THE TREATMENT OF CANCERS, AND COMBINATION THEREOF WITH ADENOSINE RECEPTOR ANTAGONISTS
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The present invention relates to pyrimido[5,4-d]pyrimidine derivatives of formula (I), including pharmaceutically acceptable salts and solvates thereof. Compounds of the invention are inhibitors of ENT family transporter, especially of ENT1, and are useful as therapeutic compounds for the treatment of cancers. The invention also relates to the combined use of the pyrimido[5,4-d]pyrimidine derivatives with an adenosine receptor antagonist, for the treatment of cancers.
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Paragraph 134; 198
(2021/09/04)
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- Synthesis method of 4-formyl-2-(trifluoromethyl) benzoic acid
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The invention belongs to the technical field of medical intermediates and relates to a synthetic method of 4-formyl-2-(trifluoromethyl) benzoic acid. A compound A is used as an initial raw material; the compound A reacts with triethanolamine, PdCl2 (dppf) CH2Cl2 and the like, so that a compound B can be synthesized; a compound C is formed through the compound B; and the 4-formyl-2-(trifluoromethyl) benzoic acid is prepared from the compound C. The target product is synthesized by three steps; the synthesis route is short, the design is reasonable, the operation is simple, and the control is easy; the synthesis method of the 4-formyl-2-(trifluoromethyl) benzoic acid is provided for the first time, and the synthesis route is provided for the synthesis method of the 4-formyl-2-(trifluoromethyl) benzoic acid.
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Paragraph 0013; 0017; 0021
(2020/12/10)
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- PYRAZOLE MAGL INHIBITORS
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Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
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Paragraph 00262
(2018/12/13)
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- PYRAZOLE MAGL INHIBITORS
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Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the subject compounds and compositions are useful for the treatment of pain.
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Paragraph 00282; 00325
(2018/12/13)
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- INSECTICIDAL COMPOUNDS
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A compound of formula (I), wherein A1, A2, A3, A4, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a sal
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Page/Page column 47
(2009/07/25)
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- FXR AGONISTS
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Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
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Page/Page column 58
(2008/06/13)
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- COMPOUNDS AND METHODS FOR MODULATING FXR
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Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
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Page/Page column 36
(2008/06/13)
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