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Trelagliptin (CAS 865759-25-7) is a potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes mellitus. Chemically known as 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl]methyl]-4-fluorobenzonitrile, Trelagliptin features a uracil core substituted with an aminopiperidine and a fluorobenzonitrile moiety.

Aprocitentan (CAS 1103522-45-7) is a potent, dual endothelin receptor antagonist developed for the treatment of resistant hypertension. Chemically known as N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]sulfamide, Aprocitentan features a pyrimidine core substituted with bromophenyl, bromopyrimidinyl, and sulfamide moieties. The molecular structure of Aprocitentan is derived from the active metabolite of macitentan (ACT-132577), and it functions as a dual ETA/ETB receptor antagonist.

Fezolinetant (CAS 1629229-37-3) is a first-in-class, orally available neurokinin-3 (NK3) receptor antagonist developed for the treatment of menopausal vasomotor symptoms (hot flashes). Chemically known as ((8R)-5,6-dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl)(4-fluorophenyl)methanone, Fezolinetant features a complex heterocyclic architecture incorporating a triazolopyrazine core fused to a fluorophenyl methanone moiety.

Delgocitinib (CAS 1263774-59-9) is a potent, pan-Janus kinase (JAK) inhibitor developed for the treatment of inflammatory and autoimmune diseases. Chemically known as 3-((3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl)-3-oxopropanenitrile, Delgocitinib features a unique spirocyclic scaffold fused to a pyrrolopyrimidine core—a structural motif that enables potent and selective inhibition of the JAK family of tyrosine kinases.

Zavegepant (CAS 1337918-83-8) is a potent, orally active calcitonin gene-related peptide (CGRP) receptor antagonist developed for the acute treatment of migraine. Chemically known as N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-1-oxopropan-2-yl]-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, Zavegepant features a complex molecular architecture incorporating a piperidine carboxamide core linked to an indazole moiety and a quinolinone scaffold.

Trifarotene (CD5789) is a potent and selective retinoic acid receptor gamma (RARγ) agonist featuring a unique terphenyl core structure with a 4′-(2-hydroxyethoxy) substituent and a 4″-(pyrrolidin-1-yl)-3″-(tert-butyl) substitution pattern . Structurally, the molecule consists of a [1,1′:3′,1″-terphenyl]-4-carboxylic acid scaffold with three distinct aromatic rings strategically functionalized to confer exceptional RARγ selectivity .