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1. (WO2018088920) 3-TRIAZENOINDOLES EXHIBITING ANTIMYCOBACTERIAL ACTIVITY
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/088920 International Application No.: PCT/RU2016/000765
Publication Date: 17.05.2018 International Filing Date: 10.11.2016
IPC:
C07D 209/42 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/12 (2006.01) ,C07D 413/12 (2006.01) ,A61K 31/404 (2006.01) ,A61K 31/04 (2006.01) ,A61K 31/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
42
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
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
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
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
404
Indoles, e.g. pindolol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
04
Nitro compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
045
Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
05
Phenols
06
the aromatic ring being substituted by nitro groups
Applicants: APT, Alexander Solomonovich[RU/RU]; RU
VELEZHEVA, Valeriya Sergeevna[RU/RU]; RU
NIKONENKO, Boris Vladimirovich[RU/RU]; RU
GAIDAR, Peter Egorovich[RU/RU]; RU
KAZARIAN, Konstantin Alexandrovich[RU/RU]; RU
Inventors: APT, Alexander Solomonovich; RU
VELEZHEVA, Valeriya Sergeevna; RU
NIKONENKO, Boris Vladimirovich; RU
KORNIENKO, Albert Grigor'evich; RU
MAJOROV, Konstantin Borisovich; RU
IVANOV, Pavel Yur'evich; RU
KONDRATIEVA, Tatiana Konstantinovna; RU
KOROTETSKAYA, Maria Valer'yevna; RU
SALINA, Elena Gennadievna; RU
Agent: PATENT & LAW FIRM "YUS", LIMITED LIABILITY COMPANY; Prospekt Mira, 6 Moscow, 129090, RU
Priority Data:
Title (EN) 3-TRIAZENOINDOLES EXHIBITING ANTIMYCOBACTERIAL ACTIVITY
(FR) 3-TRIAZÉNOINDOLES POSSÉDANT UNE ACTIVITÉ DIRIGÉE CONTRE LES MYCOBACTÉRIES
(RU) 3-ТРИАЗЕНОИНДОЛЫ, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ ПРОТИВ МИКОБАКТЕРИЙ
Abstract:
(EN) The invention relates to compounds which exhibit antimycobacterial activity. More particularly, it relates to substituted 3-triazenoindoles which exhibit activity against different mycobacteria, including against the multi-drug resistant strains thereof. The aim of the present invention is to search for novel compounds demonstrating high activity against mycobacteria, including against the multi-drug resistant strains thereof, while having low cytotoxicity. The present substituted 3-triazenoindoles have demonstrated high in vitro activity against an isoniazid-resistant strain of M. tuberculosis and M. avium. The data provided indicate the high efficacy of the claimed invention in terms of developing molecular candidates exhibiting activity against both susceptible and resistant strains of M. tuberculosis.
(FR) L'invention concerne des composés qui possèdent une activité anti-mycobactérienne. Elle concerne plus particulièrement des 3-triazénoindoles substitués possédant une activité contre différentes mycobactéries, y compris leurs souches à résistance multiple. L'objectif de la présente invention consiste à rechercher de nouveaux composés qui, tout en ayant une faible cytotoxicité, manifestent une activité élevée contre les mycobactéries, y compris leurs souches à résistance multiple. Les 3-triazénoindoles ont manifesté une activité élevée in vitro contre la souche à résistance à l'isoniazide M. tuberculosis et M. avium. Les données citées témoignent d'un degré élevé des résultats de l'invention par rapport aux molécules candidates actives contre les souches sensibles ou les souches résistantes de M. tuberculosis.
(RU) Изобретение относится к соединениям, которые обладают антимикобактериальной активностью. Более конкретно, оно относится к замещенным 3-триазеноиндолам, обладающим активностью против различных микобактерий, в том числе против их мультирезистентных штаммов. Задачей настоящего изобретения является поиск новых соединений, которые при низкой цитотоксичности проявляли бы высокую активность против микобактерий, в том числе против их мультирезистентных штаммов. Замещенные 3-триазеноиндолы показали высокую in vitro активность против изониазид-резистентного штамма М. tuberculosis и М. avium. Приведенные данные свидетельствуют о высокой результативности заявленного изобретения в отношении конструирования молекул-кандидатов, активных как против чувствительных, так и против резистентных штаммов М. tuberculosis.
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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, JP, KE, KG, 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: Russian (RU)
Filing Language: Russian (RU)