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1. WO2020140043 - COMPOUNDS FOR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR PREVENTION OF NEURORETINAL DISEASES

Publication Number WO/2020/140043
Publication Date 02.07.2020
International Application No. PCT/US2019/068759
International Filing Date 27.12.2019
IPC
A61P 27/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
C07D 213/40 2006.01
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
24with substituted hydrocarbon radicals attached to ring carbon atoms
36Radicals substituted by singly-bound nitrogen atoms
40Acylated substituent nitrogen atom
C07D 263/32 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A61K 31/4164 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
A61K 31/4409 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
4409only substituted in position 4, e.g. isoniazid, iproniazid
CPC
A61K 9/0019
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
A61K 9/0048
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0048Eye, e.g. artificial tears
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
C07D 213/40
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
24with substituted hydrocarbon radicals attached to ring carbon atoms
36Radicals substituted by singly-bound nitrogen atoms
40Acylated substituent nitrogen atom
C07D 213/56
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
24with substituted hydrocarbon radicals attached to ring carbon atoms
54Radicals substituted by carbon atoms having three bonds to heteroatoms, with at the most one to halogen, e.g. ester or nitrile radicals
56Amides
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Applicants
  • ENDOGENA THERAPEUTICS, INC. [US]/[US]
Inventors
  • STEGER, Matthias
  • MUELLER, Alex
  • MARIGO, Mauro
  • FASCHING, Bernhard
  • MOKADY, Daphna
Agents
  • ARMSTRONG, Joel S.
  • BROWN, Christopher W.
Priority Data
16/235,54328.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS FOR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR PREVENTION OF NEURORETINAL DISEASES
(FR) COMPOSÉS DESTINÉS À ÊTRE UTILISÉS EN TANT QUE SUBSTANCES THÉRAPEUTIQUEMENT ACTIVES DANS LE TRAITEMENT ET/OU LA PRÉVENTION DE MALADIES NEURORÉTINIENNES
Abstract
(EN)
A compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, R1 is selected from the group consisting of fluoro and chloro; R2, R3, R4, R5 and R6 of the phenyl ring B are independently from each other selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino; and at least two of R2, R3, R4, R5 and R6 are hydrogens, with the proviso that if R1 is chloro, R5 is not methoxy. Said compounds are useful as therapeutically active substances in the treatment and / or prevention of neuroretinal diseases, and in particular in the treatment and/or prevention of neuroretinal diseases leading to photoreceptor loss or degeneration of the outer retina.
(FR)
La présente invention concerne un composé de formule (I) ou un sel pharmaceutiquement acceptable correspondant : A étant un résidu 5-oxazolyle ou un résidu pyridine-4-yle, R1 étant choisi dans le groupe constitué par le fluoro et le chloro ; R2, R3, R4, R5 et R66 du cycle phényle B étant choisis indépendamment les uns des autres dans le groupe constitué par un atome d'hydrogène, un alkyle linéaire ou ramifié ayant 1 à 4 atomes de carbone, le trifluorométhyle, le 2,2,2-trifluoroéthyle, le méthylsulfanyle, l'éthylsulfanyle, le méthylsulfonyle, l'éthylsulfonyle, le difluorométhoxy, le trifluorométhoxy, le fluoro, le bromo, le chloro, le méthoxy, l'éthoxy, le propoxy, le butoxy, l'hydroxy et l'amino ; et au moins deux parmi R2, R3, R4, R5 et R6 représentant des atomes d'hydrogène, à condition que si R1 représente un chloro, R5 ne soit pas un méthoxy. Lesdits composés sont utiles en tant que substances thérapeutiquement actives dans le traitement et/ou la prévention de maladies neurorétiniennes, et en particulier dans le traitement et/ou la prévention de maladies neurorétiniennes conduisant à une perte ou à une dégénérescence des photorécepteurs de la rétine externe.
Also published as
Latest bibliographic data on file with the International Bureau