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1. WO2011011522 - POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF

Publication Number WO/2011/011522
Publication Date 27.01.2011
International Application No. PCT/US2010/042759
International Filing Date 21.07.2010
IPC
C07D 239/88 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
86with hetero atoms directly attached in position 4
88Oxygen atoms
C07D 239/93 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
86with hetero atoms directly attached in position 4
93Sulfur atoms
C07D 239/94 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
86with hetero atoms directly attached in position 4
94Nitrogen atoms
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 405/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 417/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61P 1/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
18for pancreatic disorders, e.g. pancreatic enzymes
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
Applicants
  • PRESIDENT AND FELLOWS OF HARVARD COLLEGE [US]/[US] (AllExceptUS)
  • SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY [CN]/[CN] (AllExceptUS)
  • YUAN, Junying [US]/[US] (UsOnly)
  • MA, Dawei [CN]/[CN] (UsOnly)
  • LIU, Junli [CN]/[CN] (UsOnly)
  • ZHANG, Lihong [CN]/[CN] (UsOnly)
Inventors
  • YUAN, Junying
  • MA, Dawei
  • LIU, Junli
  • ZHANG, Lihong
Agents
  • SMITH, DeAnn, F.
Priority Data
61/227,16421.07.2009US
61/296,73520.01.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF
(FR) PETITES MOLÉCULES DOTÉES D'UNE PUISSANTE ACTIVITÉ INHIBITRICE DE L'AUTOPHAGIE, ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity. (I)
(FR)
La présente invention concerne des petites molécules dotées d'une puissante activité inhibitrice de l'autophagie, et leur utilisation pour le traitement et la prévention des cancers et de la pancréatite aiguë. Selon l'invention, une petite molécule inhibitrice de l'autophagie a été identifiée à partir d'un criblage à base d'images dans une banque de molécules bioactives connues. On a découvert que cet inhibiteur de l'autophagie fonctionne en favorisant la dégradation du complexe des PI3-kinases de type III qui est nécessaire à l'initiation de l'autophagie. Des études de chimie médicinale ont permis d'obtenir des petites molécules inhibitrices de l'autophagie dotées d'une activité et d'une sélectivité améliorées.
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