24515-53-5Relevant articles and documents
PYRROLE DERIVATIVES AS ACC INHIBITORS
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Page/Page column 47; 48, (2019/07/19)
Novel pyrrole derivatives of Formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Acetyl- CoA carboxylase (ACC).
PRODRUGS OF LANICEMINE AND THEIR METHOD OF USE
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Paragraph 0661, (2018/06/12)
Pharmaceutical compositions of the invention include substituted Lanicemine prodrugs useful for the treatment of conditions associated with dysregulation of NMDA receptor activity such as depression and depressive disordersthrough the release of Lanicemine, Prodrugs of Lanicemine have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release Lanicemine in the plasma via either an enzymatic or general biophysical release process.
Olumacostat glasaretil
Baroudi,Shealy,Cardwell,Alinia,Feldman
, p. 175 - 179 (2018/06/11)
Acne vulgaris is a common dermatologic condition affecting adolescents and adults. Systemic and topical therapies have been developed to target different mechanisms in the pathogenesis of acne. Olumacostat glasaretil (OG) is a novel topical agent that targets sebum production in the treatment of acne vulgaris. OG’s active metabolite acts as a competitive inhibitor of the rate-limiting enzyme of fatty acid synthesis, acetyl-coenzyme A (CoA) carboxylase (ACC). ACC catalyzes malonyl-CoA formation and sebum production. OG is efficacious in the treatment of acne vulgaris and has a low side effect profile. Phase IIa and IIb trials note side effects including application-site erythema and dryness, and nasopharyngitis. Phase III trials are currently underway. The new mechanism of action of OG is sensible, attractive and exciting, but the available data do not demonstrate that it provides a quantum leap forward over existing therapies.