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Prodrug compounds and uses thereof
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A technology of compounds and uses, applied in the field of prodrug compounds and their uses, which can solve the problems of different liver targeting efficiencies
Pending Publication Date: 2022-04-29
LIGAND PHARMA INC
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The liver-targeting effect of these agents is based on hepatic first-pass metabolism of orally administered agents, and the efficiency of liver targeting is very variable, depending on the pharmacokinetic properties of the agent, and not as efficient as Cyp3A-activating prodrugs
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[0410] According to the synthetic strategy of Scheme I, compound 101 was prepared as a mixture of two diastereoisomers from (4-chloro-1,2-phenylene)dimethanol and nucleoside derivatives. [M+H] + C 21 h 23 ClFN 2 o 9 Calculated value of P: 533.08; measured value: 533.1. 1 H NMR (400MHz, DMSO-d 6 ( d,J=8.4,1H),5.40-5.10(m,4H),4.45-4.31(m,3H),3.41-3.31(m,1H),2.46(q,J=7.6,2H),1.33(d ,J=22.8,3H), and 1.06(t,J=7.6,3H).
[0414] Compound 102 can be prepared from 3-chlorobenzaldehyde and nucleoside derivatives according to the synthetic strategy of Scheme I. MH + = 534.06 (calculated value).
[0418] According to the synthetic strategy of Scheme II, two diastereomers of 1 were prepared from 3-amino-1-(3-chlorophenyl)-2,2-dimethylpropan-1-ol and nucleoside derivatives: 1 Compound 103 in the form of a mixture. [M+H] + C 23 h 28 ClFN 3 o 8 Calculated value of P: 561.13; measured value: 561.2. 1 H NMR (400MHz, DMSO-d 6 )11.60(s,0.5H),11.50(s,0.5H),7.80-7.20(m,5H),6.02(bs,1H),5.55-5.50(m,1H),5.40(s,1H),4.38 -4.02(m, 5H), 2.13(s, 3H), 1.34(d, J=15.5, 1.5H), 1.28(d, J=15.5, 1.5H), 0.92(s, 3H, and 0.73(s, 3H).
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Abstract
Provided herein are prodrug compounds and uses thereof, such as by interfering with molecular pathways in the liver to treat liver diseases or non-liver diseases. The present application describes novel prodrug compounds of acid / alcohol derivatives, such as phosphoric acid esters, phosphonic acid esters, phosphoramidates, phosphoramidates, carboxylic acid esters, phenolic esters and alkoxylates, their preparation and their use. Some novel prodrug compounds described herein do not produce vinyl ketone reactive intermediates during activation. Another aspect includes the use of the prodrugs for the treatment of diseases that benefit from enhancing the distribution of drugs in the liver or similar tissues and cells.
Description
[0001] This application is a divisional application of the Chinese invention patent application 201580008367.0 with the filing date of February 11, 2015 and the title of the invention being "prodrug compounds and their uses". [0002] Cross References to Related Applications [0003] This application claims U.S. Provisional Application No. 61 / 939,615, filed February 13, 2014, U.S. Provisional Application No. 61 / 988,101, filed May 2, 2014, and 61 / 988,118, filed May 2, 2014 Priority of the U.S. Provisional Application, which is incorporated herein by reference in its entirety. technical field [0004] This application discloses compositions and methods in the fields of medicine and chemistry. Some disclosed embodiments relate to pharmaceutical prodrug compounds, pharmaceutical compositions, methods of their preparation and methods of their use. Some embodiments include prodrug compounds of acid / alcohol derivatives, their preparation and their use. In some embodiments, such pr...
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