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1. WO2018140907 - NOVEL SPIRO AND CYCLIC BIS-BENZYLIDINE PROTEASOME INHIBITOR FOR THE TREATMENT OF CANCER, DIABETES AND NEUROLOGICAL DISORDERS

Publication Number WO/2018/140907
Publication Date 02.08.2018
International Application No. PCT/US2018/015826
International Filing Date 30.01.2018
IPC
A61K 31/439 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
439the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/45 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
45having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
C07D 211/74 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
68having one double bond between ring members or between a ring member and a non-ring member
72with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
74Oxygen atoms
CPC
A61K 31/397
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
397having four-membered rings, e.g. azetidine
A61K 31/40
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/403
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
A61K 31/438
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
Applicants
  • UP THERAPEUTICS INC. [US]/[US]
Inventors
  • CHANG, Yung-Nien
Agents
  • MCGOWAN, Malcolm K.
  • CERMAK, Shelly, Guest
  • CERMAK, Adam, J.
  • NAKAJIMA, Tomoko
Priority Data
62/451,92030.01.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL SPIRO AND CYCLIC BIS-BENZYLIDINE PROTEASOME INHIBITOR FOR THE TREATMENT OF CANCER, DIABETES AND NEUROLOGICAL DISORDERS
(FR) NOUVEL INHIBITEUR DU PROTÉASOME SPIRO ET CYCLIQUE BIS-BENZYLIDINE POUR LE TRAITEMENT DU CANCER, DU DIABÈTE ET DE TROUBLES NEUROLOGIQUES
Abstract
(EN)
Described herein are spiro and cyclic bis-benzylidine proteasome inhibitors, which inhibit the proteasome function through either ubiquitin receptor ADRM1/RPN13 or proteasome DUB enzymes (USP14, UCH37 and RPN11), and which can be used for the treatment of cancers/diabetes/neurological disorders.
(FR)
L'invention concerne des inhibiteurs du protéasome spiro et cycliques bis-benzylidine, qui inhibent la fonction du protéasome par l'intermédiaire soit de récepteurs d'ubiquitine ADRM1/RPN13, soit d'enzymes DUB du protéasome (USP14, UCH37 et RPN11), et qui peuvent être utilisés pour le traitement de cancers/diabètes/troubles neurologiques.
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