Gepirone (CAS 83928-76-1) is a selective 5-HT1A receptor partial agonist developed for the treatment of major depressive disorder. Chemically known as 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)piperazin-1-yl]butyl]piperidine-2,6-dione, Gepirone features a glutarimide core linked to a pyrimidinyl piperazine moiety via a butyl spacer.
Mitapivat (CAS 1260075-17-9) is a first-in-class, oral, small-molecule activator of pyruvate kinase (PK) developed for the treatment of pyruvate kinase deficiency and other hemolytic anemias. Chemically known as N-(4-{4-[(cyclopropylamino)methyl]piperidin-1-yl}phenyl)-N'-(2,3-dihydroxypropyl)ethanediamide, Mitapivat features a piperidine-phenyl scaffold linked to an oxalamide moiety.
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.
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