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1. WO2020110008 - CYCLIC PENTAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDER

Publication Number WO/2020/110008
Publication Date 04.06.2020
International Application No. PCT/IB2019/060200
International Filing Date 26.11.2019
IPC
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 401/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 403/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 403/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
C07D 407/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
407Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 403/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • NOVARTIS AG [CH]/[CH]
Inventors
  • BECKER, Christopher
  • DECHRISTOPHER, Brian Addison
  • FLYER, Alec Nathanson
  • FRIEDMAN, Adam
  • GAMPE, Christian
  • GOLOSOV, Andrei Alexandrovich
  • GROSCHE, Philipp
  • HARRISON, Tyler
  • LIU, Qian
  • LIU, Eugene Yuejin
  • MAO, Justin Yik Ching
  • MONOVICH, Lauren Gilchrist
  • PATEL, Tajesh Jayprakash
  • SANCHEZ, Carina Cristina
  • SU, Liansheng
  • YANG, Lihua
  • ZHENG, Rui
Agents
  • NOVARTIS AG
Priority Data
62/772,02927.11.2018US
62/925,10823.10.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CYCLIC PENTAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDER
(FR) COMPOSÉS PENTAMÈRES CYCLIQUES SERVANT D'INHIBITEURS DE PROPROTÉINE CONVERTASE SUBTILISINE/KEXINE DE TYPE 9 (PCSK9) POUR LE TRAITEMENT D'UN TROUBLE MÉTABOLIQUE
Abstract
(EN)
The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I):, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein X1, R1, R2, R3, R4, R5, R6, R6', R7, R7', R8, R9, R9', R10, R11, R12, and n are described herein.
(FR)
L'invention concerne des inhibiteurs de PCSK9 utiles dans le traitement du métabolisme lipidique du cholestérol, ainsi que d'autres maladies dans lesquelles PCSK9 joue un rôle, ayant la formule (I) : (I), ou un sel pharmaceutiquement acceptable, hydrate, solvate, promédicament, stéréoisomère, N-oxyde, ou tautomère de ceux-ci, dans la formule X1, R1, R2, R3, R4, R5, R6, R6', R7, R7', R8, R9, R9', R10, R11, R12 et n sont définis dans la description.
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