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1. WO2012134351 - CLATHRATE COMPLEXES OF BETA-CYCLODEXTRIN AND 5-HYDROXY-4-AMINOMETHYL-1-CYCLOHEXYL (OR CYCLOHEPTYL)-3-ALKOXYCARBONYL INDOLE DERIVATIVE, WHICH EXHIBIT AN ANTI-VIRAL EFFECT, AND METHODS FOR PRODUCING SAID COMPLEXES

Publication Number WO/2012/134351
Publication Date 04.10.2012
International Application No. PCT/RU2012/000222
International Filing Date 27.03.2012
IPC
C08B 37/16 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
16Cyclodextrin; Derivatives thereof
A61K 31/724 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
716Glucans
724Cyclodextrins
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07D 209/42 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with 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
42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/06 2006.01
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
06linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/404 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
CPC
A61K 47/6951
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6949inclusion complexes, e.g. clathrates, cavitates or fullerenes
6951using cyclodextrin
A61P 31/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
A61P 31/16
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
16for influenza or rhinoviruses
B82Y 5/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
5Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
C07D 209/42
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with 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
42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C08B 37/0015
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
0006Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
0009alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
0012Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof
0015Inclusion compounds, i.e. host-guest compounds, e.g. polyrotaxanes
Applicants
  • ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ «НАУЧНО-ИССЛЕДОВАТЕЛЬСКАЯ КОМПАНИЯ «МЕДБИОФАРМ» OBSCHESTVO S OGRANICHENNOY OTVETSTVENNOSTYU «NAUCHNO-ISSLEDOVATELSKAYA KOMPANIYA «MEDBIOPHARM» [RU]/[RU] (AllExceptUS)
  • ЦЫБ, Анатолий Федорович TSYB, Anatoliy Fedorovich [RU]/[RU] (UsOnly)
  • ГОНЧАРОВА, Анна Яковлевна GONCHAROVA, Anna Yakovlevna [RU]/[RU] (UsOnly)
  • РОЗИЕВ, Рахимджан Ахметджанович ROZIEV, Rahimdzhan Ahmetdzhanovich [RU]/[RU] (UsOnly)
  • ВОРОБЬЕВ, Илья Владимирович VOROBYEV, Ilya Vladimirovich [RU]/[RU] (UsOnly)
  • ПОДГОРОДНИЧЕНКО, Владимир Константинович PODGORODNICHENKO, Vladimir Konstantinovich [RU]/[RU] (UsOnly)
  • ХОМИЧЁНОКВиктор Владимирович KHOMICHENOK, Victor Vladimirovich [RU]/[RU] (UsOnly)
Inventors
  • ЦЫБ, Анатолий Федорович TSYB, Anatoliy Fedorovich
  • ГОНЧАРОВА, Анна Яковлевна GONCHAROVA, Anna Yakovlevna
  • РОЗИЕВ, Рахимджан Ахметджанович ROZIEV, Rahimdzhan Ahmetdzhanovich
  • ВОРОБЬЕВ, Илья Владимирович VOROBYEV, Ilya Vladimirovich
  • ПОДГОРОДНИЧЕНКО, Владимир Константинович PODGORODNICHENKO, Vladimir Konstantinovich
  • ХОМИЧЁНОКВиктор Владимирович KHOMICHENOK, Victor Vladimirovich
Agents
  • БАЗАНОВ, Юрий Борисович BAZANOV, Yuriy Borisovich
Priority Data
201111207331.03.2011RU
Publication Language Russian (RU)
Filing Language Russian (RU)
Designated States
Title
(EN) CLATHRATE COMPLEXES OF BETA-CYCLODEXTRIN AND 5-HYDROXY-4-AMINOMETHYL-1-CYCLOHEXYL (OR CYCLOHEPTYL)-3-ALKOXYCARBONYL INDOLE DERIVATIVE, WHICH EXHIBIT AN ANTI-VIRAL EFFECT, AND METHODS FOR PRODUCING SAID COMPLEXES
(FR) COMPLEXES DE CLATHRATES DE β-CYCLODEXTRINE ET DES DÉRIVÉS DE 5-HYDROXY-4-AMINOMÉTHYL-1-CYCLOHEXYL (OU CYCLOHEPTYL)-3-ALCOXYCARBONYLE INDOLE POSSÉDANT UN EFFET ANTIVIRAL ET PROCÉDÉ DE LEUR PRODUCTION
(RU) КЛАТРАТНЫЕ КОМПЛЕКСЫ БЕТТА-ЦИКЛОДЕКСТРИНА С ПРОИЗВОДНЫМ 5-ГИДРОКСИ-4-АМИНОМЕТИЛ-1-ЦИКЛОГЕКСИЛ (ИЛИ ЦИКЛОГЕПТИЛ)-3-АЛКОКСИКАРБОНИЛИНДОЛА, ОБЛАДАЮЩИЕ ПРОТИВОВИРУСНЫМ ДЕЙСТВИЕМ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ
Abstract
(EN)
The invention relates to novel clathrate complexes of β-cyclodextrin and 5-hydroxy-4-aminomethyl-1-cyclohexyl (or cycloheptyl)-3-alkoxycarbonyl indole derivatives, which are in the form of nanoparticles of a size of less than 100 nm, have a molar ratio of 1:1 to 1:5, exhibit an anti-viral effect and are highly active against influenza viruses. The clathrate complexes are produced using liquid-phase and solid-phase methods. The invention also relates to a pharmaceutical composition and a drug based on the aforesaid clathrate complexes.
(FR)
L'invention concerne de nouveaux complexes de clathrates de β-cyclodextrine et des dérivés de 5-hydroxy-4-aminométhyl-1-cyclohexyl (ou cycloheptyl)-3-alcoxycarbonyle indole qui se présentent comme des nanoparticules d'une taille inférieure à 100 nm, avec un rapport molaire de 1:1 à 1:5, possédant un effet antiviral et étant hautement actifs contre les virus de la grippe. Les complexes de clathrates sont obtenus par des procédés en phase solide ou en phase liquide. L'invention concerne aussi une composition pharmaceutique et un médicament basé sur ces complexes de clathrates.
(RU)
Изобретение относится к новым клатратным комплексам β-циклодекстрина с производными 5- гидрокси-4-аминометил-1-циклогексил(или гептил)-3-алкоксикарбонилиндола, представляющим собой наночастицы размером менее 100 нм, при мольном соотношении от 1:1 до 1:5, обладающим противовирусным действием и проявляющим высокую активность против вирусов гриппа. Клатратные комплексы получают жидкофазным и твердофазным методами. Изобретение также относится к фармацевтической композиции и лекарственному средству на основе указанных клатратных комплексов.
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