DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Zerencotrep
CAS 1628287-16-0
MF C23H20ClF3N4O5, MW 524.88
7-[(4-chlorophenyl)methyl]-1-(3-hydroxypropyl)-3-methyl-8-[3-(trifluoromethoxy)phenoxy]purine-2,6-dione
7-[(4-chlorophenyl)methyl]-1-(3-hydroxypropyl)-3-
methyl-8-[3-(trifluoromethoxy)phenoxy]-3,7-dihydro1H-purine-2,6-dione
transient receptor potential channel 4 and 5 (TRPC4, TRPC5) inhibitor, Pico 145, HC 608, HMIMSYLCWQ
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
Zerencotrep is a small molecule drug. The usage of the INN stem ‘-cotrep’ in the name indicates that Zerencotrep is a transient receptor potential canonical channel 5 (TRPC5) antagonist. Zerencotrep has a monoisotopic molecular weight of 524.11 Da.
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014143799&_cid=P22-MJF454-30876-1
The following examples 7a through 7k were prepared using the method of example 6, step 1.
Example 7a 7-(4-chlorobenzyl)-l -(3-hydroxypropyl)-3-methyl-8-(3-(trifluoromethoxy)phenoxy)-l -purine-2,6(3H,7H)-dione
The title compound was prepared using the method of example 6, step 1 and purified
preparative HPLC to give 7-(4-chlorobenzyl)-l -(3-hydroxypropyl)-3-methyl-8-(3-
(trifluoromethoxy)phenoxy)-lH-purine-2,6(3H,7H)-dione (10 mg, 17.3% yield) as white solid. lH-NMR (CD3OD) δ 7.57-7.53(t, IH), 7.46-7.44(d, 2H), 7.37-7.33(m, 4H), 7.26-7.24(d, IH), 5.49(s, 2H), 4.13-4.09(t, IH), 3.64-3.60(t, 2H), 3.42(s, 3H), 1.89-1.86(m, 2H). LCMS retention time 3.059 min; LCMS MH+ 525.
PAT
- Side chain unsaturated 1α-hydroxyvitanim D homologsPublication Number: US-5250523-APriority Date: 1988-04-29Grant Date: 1993-10-05
- Antiviral methods utilizing ribofuranosylthiazolo[4,5-d]pyrimdine derivativesPublication Number: US-4880784-APriority Date: 1987-12-21Grant Date: 1989-11-14
- NEW NUCLEOSIDES AND NUCLEOTIDES AND PROCEDURES FOR THE PREPARATION.Publication Number: NO-893343-LPriority Date: 1987-12-21
- New amidino derivativesPublication Number: JP-H01131145-APriority Date: 1987-09-21
- Oligonucleotides, a process for preparing the same and their application as mediators of the action of interferonPublication Number: US-4476301-APriority Date: 1982-04-29Grant Date: 1984-10-09
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- Pico145 inhibits TRPC4-mediated mICAT and postprandial small intestinal motilityPublication Name: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapiePublication Date: 2023-12PMID: 37857250DOI: 10.1016/j.biopha.2023.115672
- Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding sitePublication Name: Communications BiologyPublication Date: 2020-11-23PMCID: PMC7683545PMID: 33230284DOI: 10.1038/s42003-020-01437-8
- Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis ModelPublication Name: ACS Medicinal Chemistry LettersPublication Date: 2019-10-22PMCID: PMC6862342PMID: 31749913DOI: 10.1021/acsmedchemlett.9b00430
- Potent, selective, and subunit‐dependent activation of TRPC5 channels by a xanthine derivativePublication Name: British Journal of PharmacologyPublication Date: 2019-09-06PMCID: PMC6811774PMID: 31277085DOI: 10.1111/bph.14791
- Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and DiseasesPublication Name: Journal of Medicinal ChemistryPublication Date: 2019-04-03PMID: 30943030DOI: 10.1021/acs.jmedchem.8b01954
///////////zerencotrep, Pico 145, HC 608, HMIMSYLCWQ
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