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1. (WO2018141854) PIPERAZINE DERIVATIVES FOR INFLUENZA VIRUS INHIBITION
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Pub. No.: WO/2018/141854 International Application No.: PCT/EP2018/052537
Publication Date: 09.08.2018 International Filing Date: 01.02.2018
IPC:
C07D 263/57 (2006.01) ,C07D 413/14 (2006.01) ,A61P 31/16 (2006.01) ,A61K 31/496 (2006.01) ,C07D 417/04 (2006.01) ,C07D 277/66 (2006.01) ,C07D 498/04 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01) ,C07D 307/81 (2006.01) ,C07D 487/08 (2006.01) ,C07D 417/10 (2006.01) ,C07D 413/10 (2006.01) ,C07D 413/04 (2006.01) ,C07D 235/18 (2006.01) ,C07D 401/10 (2006.01) ,A61K 31/4995 (2006.01) ,A61K 31/454 (2006.01) ,A61K 31/551 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
52
condensed with carbocyclic rings or ring systems
54
Benzoxazoles; Hydrogenated benzoxazoles
56
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
57
Aryl or substituted aryl radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
14
for RNA viruses
16
for influenza or rhinoviruses
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496
Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic 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
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
60
condensed with carbocyclic rings or ring systems
62
Benzothiazoles
64
with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
66
with aromatic rings or ring systems directly attached in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic 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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77
ortho- or peri-condensed with carbocyclic rings or ring systems
78
Benzo [b] furans; Hydrogenated benzo [b] furans
79
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
81
Radicals substituted by nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
08
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic 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
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
18
with aryl radicals directly attached in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4995
Pyrazines or piperazines forming part of bridged ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
Applicants:
JANSSEN VACCINES & PREVENTION B.V. [NL/NL]; Archimedesweg 4 2333 CN Leiden, NL
Inventors:
VAN DONGEN, Maria; NL
JURASZEK, Jaroslaw; NL
SCHEPENS, Wim, Bert, Griet; BE
LAWSON, Edward, Charles; US
SHOOK, Brian, C; US
JONCKERS, Tim, Hugo, Maria; BE
TAHRI, Abdellah; BE
RABOISSON, Pierre, Jean-Marie, Bernard; BE
BUYCK, Christophe, Francis, Robert, Nestor; BE
Agent:
MANTEN, Annemieke; NL
VERHAGE, Richard, A; NL
BESLIER, Victor; NL
Priority Data:
17156448.716.02.2017EP
62/453,67302.02.2017US
Title (EN) PIPERAZINE DERIVATIVES FOR INFLUENZA VIRUS INHIBITION
(FR) DÉRIVÉS DE PIPÉRAZINE POUR L'INHIBITION DU VIRUS DE LA GRIPPE
Abstract:
(EN) The present invention provides piperazine derivatives exhibiting high affinity to the stem region (viral membrane proximal part) of influenza hemagglutinin as determined through competition binding and high virus neutralization activity while having low cytotoxity. Furthermore, the present invention relates to pharmaceutical compositions comprising said piperazine derivatives, methods of preparing said piperazine derivatives, as well as said piperazine derivatives for use in medical prevention or treatment, especially for preventing or treating influenza.
(FR) La présente invention concerne des dérivés de pipérazine présentant une affinité élevée vis-à-vis de la région de tige (partie proximale de membrane virale) de l'hémagglutinine de la grippe telle que déterminée par liaison compétitive et une forte activité de neutralisation de virus, tout en ayant une faible cytotoxité. La présente invention concerne en outre, des compositions pharmaceutiques comprenant lesdits dérivés de pipérazine, des procédés de préparation de ces derniers, ainsi que leur utilisation dans la prévention ou le traitement médical, particulièrement, dans la prévention ou le traitement de la grippe.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)