CU20230045A7 - Compuestos multicíclicos que comprenden estructuras heteroaromáticos o aromáticas bicíclicos útiles como inhibidores de la peptidasa 5 relacionada con calicreína (klk5) - Google Patents

Compuestos multicíclicos que comprenden estructuras heteroaromáticos o aromáticas bicíclicos útiles como inhibidores de la peptidasa 5 relacionada con calicreína (klk5)

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Publication number
CU20230045A7
CU20230045A7 CU2023000045A CU20230045A CU20230045A7 CU 20230045 A7 CU20230045 A7 CU 20230045A7 CU 2023000045 A CU2023000045 A CU 2023000045A CU 20230045 A CU20230045 A CU 20230045A CU 20230045 A7 CU20230045 A7 CU 20230045A7
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CU
Cuba
Prior art keywords
klk5
inhibitors
compounds
related peptidase
kallycrene
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CU2023000045A
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English (en)
Inventor
Yarlagadda Babu
zhao Dang
Pravin Kotian
peng-cheng Lu
Krishnan Raman
Weihe Zhang
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Biocryst Pharm Inc
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Publication date
Application filed by Biocryst Pharm Inc filed Critical Biocryst Pharm Inc
Publication of CU20230045A7 publication Critical patent/CU20230045A7/es

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Abstract

<p>La activación inadecuada de las calicreínas tisulares (KLK), incluida la peptidasa 5 relacionada con la calicreína (KLK5), está implicada en una serie de enfermedades y afecciones humanas. En particular, las enfermedades de la piel como el síndrome de Netherton se caracterizan por una actividad aberrante de KLK5. En el presente documento se describen compuestos de fórmulas (I) - (IV) y sales farmacéuticamente aceptables de los mismos, que son inhibidores de Ia peptidasa 5 relacionada con calicreína (KLK5), y útiles en el tratamiento o prevención de enfermedades o afecciones que presentan actividad aberrante de KLK5, inlcuido el síndrome de Netherton.</p>
CU2023000045A 2021-04-14 2022-04-14 Compuestos multicíclicos que comprenden estructuras heteroaromáticos o aromáticas bicíclicos útiles como inhibidores de la peptidasa 5 relacionada con calicreína (klk5) CU20230045A7 (es)

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