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1. WO2019043372 - SUBSTITUTES SULFONYL AZACYCLES AS MODULATORS OF HEDGEHOG (HH) SIGNALLING PATHWAY

Publication Number WO/2019/043372
Publication Date 07.03.2019
International Application No. PCT/GB2018/052429
International Filing Date 29.08.2018
IPC
C07D 403/12 2006.1
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 401/14 2006.1
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 405/14 2006.1
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
14containing three or more hetero rings
C07D 213/74 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 231/56 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring systems
56Benzopyrazoles; Hydrogenated benzopyrazoles
C07D 401/04 2006.1
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
04directly linked by a ring-member-to-ring- member bond
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
C07D 211/96
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92with a hetero atom directly attached to the ring nitrogen atom
96Sulfur atom
C07D 213/74
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 231/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring-systems
56Benzopyrazoles; Hydrogenated benzopyrazoles
C07D 295/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
22with hetero atoms directly attached to ring nitrogen atoms
26Sulfur atoms
Applicants
  • E-THERAPEUTICS PLC [GB]/[GB]
Inventors
  • JURKOVIC, Mihaela
  • LANDEK, Ivana Ozimec
  • POLJAK, Tanja
  • ROŠCIC, Maja
  • STUBBERFIELD, Colin
  • VADLAMUDI, Srinivasamurthy
Agents
  • GILHOLM, Stephen Philip
Priority Data
1713780.329.08.2017GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) SUBSTITUTES SULFONYL AZACYCLES AS MODULATORS OF HEDGEHOG (HH) SIGNALLING PATHWAY
(FR) SUBSTITUTS DE SULFONYLAZACYCLES UTILISÉS EN TANT QUE MODULATEURS DE LA VOIE DE SIGNALISATION HEDGEHOG (HH)
Abstract
(EN) There are described compounds of formula (I) in which X, R1, R2 and n are each as herein defined; and their use as a medicament in the treatment of conditions involving abnormal activation and/or malfunction of the hedgehog pathway, such as cancer, fibrosis and chronic graft-versus-host disease (c GVHD).
(FR) L'invention concerne des composés de formule (I) dans laquelle X, R1, R2 et n sont chacun tels que définis dans la description ; et leur utilisation en tant que médicament dans le traitement d'états pathologiques impliquant une activation et/ou un dysfonctionnement anormal de la voie hedgehog, tels que le cancer, la fibrose et la maladie du greffon contre l'hôte chronique (c GVHD).
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