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1. WO2021032992 - PHARMACEUTICAL COMPOUNDS

Publication Number WO/2021/032992
Publication Date 25.02.2021
International Application No. PCT/GB2020/052008
International Filing Date 20.08.2020
IPC
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 31/14 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
A61K 31/519 2006.1
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/5025 2006.1
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50Pyridazines; Hydrogenated pyridazines
5025ortho- or peri-condensed with heterocyclic ring systems
CPC
A61K 31/551
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogen atoms, e.g. dilazep
A61K 31/5513
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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogen atoms, e.g. dilazep
55131,4-Benzodiazepines, e.g. diazepam ; or clozapine
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 31/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 519/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Applicants
  • REVIRAL LIMITED [GB]/[GB]
Inventors
  • COCKERILL, George Stuart
  • GOOD, James
  • AVERY, Craig Alex
  • COCHRANE, Edward James
  • WARNER, Andrew Joseph
Agents
  • J A KEMP LLP
Priority Data
1911944.520.08.2019GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PHARMACEUTICAL COMPOUNDS
(FR) COMPOSÉS PHARMACEUTIQUES
Abstract
(EN) Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, ---a--- and --­c--- are bonds, and ---b--- and ---d--- are absent; or (ii) T is C, Z is N, ---b--- and ---d--- are bonds, and ---a--- and ---c--- are absent; each of R3 and R4 is independently halo, -OR6, -NR6R7, -COR8, -C(O)OR8, -CON(R8)2 or -R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
(FR) L'invention concerne des dérivés de benzodiazépine de formule (I) : (I) dans laquelle : chacun de R1 et R2 est indépendamment H ou un halo ; soit (i) T est N, Z est C, ---a--- et --­c--- sont des liaisons, et ---b--- et ---d--- sont absents ; soit (ii) T est C, Z est N, ---b--- et ---d--- sont des liaisons, et ---a--- et ---c--- sont absents ; chacun de R3 et R4 est indépendamment un halo, -OR6, -NR6R7, -COR8, -C(O)OR8, -CON(R8)2 ou -R6 ; R5 est H ou un halo ; chacun de R6 et R7 est indépendamment H ou un groupe sélectionné parmi un alkyle en C1-C6, un cycloalkyle en C3-C10, un aryle en C6-C10, un hétérocyclyle à 4 à 10 chaînons et un hétéroaryle à 4 à 10 chaînons, le groupe étant substitué ou non substitué ; R8 est H ou un alkyle en C1-C6, chaque R8 étant identique ou différent lorsque deux sont présents ; n est 0 ou 1 ; et l'un de V, W, X et Y est N ou CH et les trois autres sont CH ; et les sels pharmaceutiquement acceptables de ceux-ci sont des inhibiteurs du VRS et peuvent donc être utilisés pour traiter ou prévenir une infection par le VRS.
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