100861-38-9Relevant academic research and scientific papers
Nucleoside analogs useful as PRMT5 inhibitors
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Paragraph 0548; 0549; 0550; 0551, (2021/08/11)
The invention relates to the technical field of biological medicines, and particularly discloses a nucleoside analogue used as a PRMT5 inhibitor. According to the nucleoside analogue as shown in the formula (I) or the pharmaceutically acceptable salt of the nucleoside analogue, the nucleoside analogue or the pharmaceutically acceptable salt of the nucleoside analogue shows relatively high inhibition on the activity of PRMT5 and can be used for preventing and/or treating PRMT5-mediated diseases, and the PRMT5-mediated diseases comprise cell abnormal proliferative diseases.
3-SUBSTITUTED COMPOUNDS FOR REDUCING URIC ACID
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Page/Page column 84, (2011/05/05)
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula 1. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including g
Controlled anion migrations with a mixed metal Li/K-TMP amide: General application to benzylic metalations
Fleming, Patricia,Oshea, Donal F.
supporting information; experimental part, p. 1698 - 1701 (2011/04/17)
A general method is described for benzylic metalation of o-, m-, and p-substituted toluenes using a mixed metal amide base generated from BuLi/KOtBu/TMP at -78 °C in THF. The excellent selectivity achieved can be rationalized by the ability of the mixed metal amide base to facilitate an anion migration from the kinetic (o-aryl) to the benzylic metalation site. Remarkably, this controlled anion migration is achievable with catalytic amounts of TMP at -78 °C.
COMPOUNDS AND METHOD FOR REDUCING URIC ACID
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Page/Page column 92-93, (2010/01/07)
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. In Formula (I) m is 0, 1, 2, 3 or 4; n is 0 or 1; m + n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are -CH2CH2-. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of Formula (I) by a ring carbon; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently monosubstituted by methyl or ethyl. The uric acid-lowering effects of the Compounds of Formula (I) are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, and cognitive impairment.
ARYL AND HETEROARYL TETRAHYDROBENZAZEPINE DERIVATIVES AND THEIR USE FOR TREATING GLAUCOMA
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Page/Page column 7, (2010/11/29)
Aryl tetrahydrobenzazepine derivatives with minimal 5-HT2B activity relative to 5-HT2A and 5-HT2C activity that are useful for treating glaucoma are disclosed.
