RU2019139864A - Санфетринем или его соль или сложный эфир для применения при лечении микобактериальной инфекции - Google Patents
Санфетринем или его соль или сложный эфир для применения при лечении микобактериальной инфекции Download PDFInfo
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- RU2019139864A RU2019139864A RU2019139864A RU2019139864A RU2019139864A RU 2019139864 A RU2019139864 A RU 2019139864A RU 2019139864 A RU2019139864 A RU 2019139864A RU 2019139864 A RU2019139864 A RU 2019139864A RU 2019139864 A RU2019139864 A RU 2019139864A
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- RU
- Russia
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- tuberculosis
- prodrug
- mycobacterial infection
- Prior art date
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- 208000027531 mycobacterial infectious disease Diseases 0.000 title claims 14
- 206010062207 Mycobacterial infection Diseases 0.000 title claims 13
- 150000003839 salts Chemical class 0.000 title claims 13
- 239000000651 prodrug Substances 0.000 claims 17
- 229940002612 prodrug Drugs 0.000 claims 17
- 150000002148 esters Chemical class 0.000 claims 16
- 238000000034 method Methods 0.000 claims 9
- 201000008827 tuberculosis Diseases 0.000 claims 9
- -1 isoxil Chemical compound 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 claims 4
- 229940121383 antituberculosis agent Drugs 0.000 claims 3
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- 239000000814 tuberculostatic agent Substances 0.000 claims 3
- QJVHTELASVOWBE-AGNWQMPPSA-N (2s,5r,6r)-6-[[(2r)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(2r,3z,5r)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acid Chemical compound OC(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21.C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 QJVHTELASVOWBE-AGNWQMPPSA-N 0.000 claims 2
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- JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 claims 1
- 229960001225 rifampicin Drugs 0.000 claims 1
- WDZCUPBHRAEYDL-GZAUEHORSA-N rifapentine Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C(O)=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N(CC1)CCN1C1CCCC1 WDZCUPBHRAEYDL-GZAUEHORSA-N 0.000 claims 1
- YIBOMRUWOWDFLG-ONEGZZNKSA-N rilpivirine Chemical compound CC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 YIBOMRUWOWDFLG-ONEGZZNKSA-N 0.000 claims 1
- 229960000311 ritonavir Drugs 0.000 claims 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 1
- 229960001852 saquinavir Drugs 0.000 claims 1
- QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical compound C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 claims 1
- 229960001203 stavudine Drugs 0.000 claims 1
- FNDDDNOJWPQCBZ-ZDUSSCGKSA-N sutezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCSCC1 FNDDDNOJWPQCBZ-ZDUSSCGKSA-N 0.000 claims 1
- 229960003879 tedizolid Drugs 0.000 claims 1
- XFALPSLJIHVRKE-GFCCVEGCSA-N tedizolid Chemical compound CN1N=NC(C=2N=CC(=CC=2)C=2C(=CC(=CC=2)N2C(O[C@@H](CO)C2)=O)F)=N1 XFALPSLJIHVRKE-GFCCVEGCSA-N 0.000 claims 1
- 229960004556 tenofovir Drugs 0.000 claims 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims 1
- 229960003231 thioacetazone Drugs 0.000 claims 1
- SRVJKTDHMYAMHA-WUXMJOGZSA-N thioacetazone Chemical compound CC(=O)NC1=CC=C(\C=N\NC(N)=S)C=C1 SRVJKTDHMYAMHA-WUXMJOGZSA-N 0.000 claims 1
- 229960000523 zalcitabine Drugs 0.000 claims 1
- 229960002555 zidovudine Drugs 0.000 claims 1
- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 claims 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D463/00—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D463/10—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D463/12—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals attached in position 7
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
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- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/04—Antibacterial agents
- A61P31/08—Antibacterial agents for leprosy
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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Claims (53)
1. Соединение
или его фармацевтически приемлемая соль или сложноэфирное пролекарство, предназначенное для лечения заболевания, вызванного микобактериальной инфекцией.
2. Соединение или его фармацевтически приемлемая соль или сложноэфирное пролекарство для применения по п.1, где заболевание представляет собой туберкулез.
3. Соединение
или его фармацевтически приемлемая соль или сложноэфирное пролекарство для применения при лечении микобактериальной инфекции.
4. Соединение или его фармацевтически приемлемая соль или сложноэфирное пролекарство для применения по п.3, где микобактериальная инфекция представляет собой инфекцию Mycobacterium tuberculosis.
5. Соединение
или его фармацевтически приемлемая соль или сложноэфирное пролекарство для применения при лечении туберкулеза.
6. Соединение для применения по любому из пп.1–5, где соединение представляет собой сложноэфирное пролекарство
7. Соединение для применения по п.6, где сложноэфирное пролекарство представляет собой
8. Соединение для применения по п. 6 или 7, где пролекарство вводят перорально.
9. Соединение для применения по любому из пп. 1–5, где
находится в форме его натриевой соли.
10. Способ лечения заболевания, вызванного микобактериальной инфекцией, у пациента, нуждающегося в этом, включающий введение указанному пациенту терапевтически эффективного количества
или его фармацевтически приемлемой соли или сложноэфирного пролекарства.
11. Способ по п.10, где заболевание представляет собой туберкулез.
12. Способ лечения микобактериальной инфекции у пациента, нуждающегося в этом, включающий введение указанному пациенту терапевтически эффективного количества
или его фармацевтически приемлемой соли или сложноэфирного пролекарства.
13. Способ по п.12, где микобактериальная инфекция представляет собой инфекцию Mycobacterium tuberculosis.
14. Способ лечения туберкулеза у пациента, нуждающегося в этом, включающий введение указанному пациенту терапевтически эффективного количества
или его фармацевтически приемлемой соли или сложноэфирного пролекарства.
15. Способ по любому из пп.10–14, который включает введение сложноэфирного пролекарства
16. Способ по п.15, где сложноэфирное пролекарство представляет собой
17. Способ по любому из пп.10–14, где
находится в форме его натриевой соли.
18. Способ по любому из пп.10–17, где пациент является человеком.
19. Применение
или его фармацевтически приемлемой соли или сложноэфирного пролекарства при изготовлении лекарственного средства для применения при лечении туберкулеза, микобактериальной инфекции или заболевания, вызванного микобактериальной инфекцией.
20. Фармацевтическая композиция, включающая (a)
или его фармацевтически приемлемую соль или сложноэфирное пролекарство; и (b) фармацевтически приемлемый эксципиент для применения при лечении туберкулеза, микобактериальной инфекции или заболевания, вызванного микобактериальной инфекцией.
21. Комбинация (a)
или его фармацевтически приемлемой соли или сложноэфирного пролекарства; и (b) дополнительного противотуберкулезного средства для применения при лечении микобактериальной инфекции, заболевания, вызванного микобактериальной инфекцией, или туберкулеза.
22. Комбинация для применения по п.21, где дополнительное противотуберкулезное средство (b) выбрано из изониазида, рифампина, пиразинамида, этамбутола, моксифлоксацина, рифапентина, клофазимина, этионамида, протионамида, изоксила, тиацетазона, рифабутина, диарилхинолина, такого как бедаквилин (TMC207) или TBAJ–587, нитроимидазо–оксазина PA–824, деламанида (OPC–67683), оксазолидинона, такого как линезолид, тедизолид, радезолид, сутезолид (PNU–100480), посизолид (AZD–5847) или TBI–223, аналога EMB SQ109, OPC–167832, GSK3036656 (также известный как GSK070), GSK2556286, GSK3211830, бензотиазинона, такого как BTZ043 или PBTZ169, азаиндола, такого как TBA–7371, динитробензамида или бета–лактама, такого как меропенем, фаропенем, эртапенем, тебипенем или комбинаций бета–лактама, таких как аугментин (амоксициллин–клавуланат).
23. Комбинация для применения по п.21 или 22, где дополнительное противотуберкулезное средство (b) представляет собой аугментин (амоксициллин–клавуланат).
24. Комбинация для применения по п.21 или 22, дополнительно включающая противовирусное средство, включая антиретровирусное средство.
25. Комбинация для применения по п.24, где антиретровирусное средство выбрано из зидовудина, диданозина, ламивудина, залцитабина, абакавира, ставудина, адефовира, адефовир дипивоксила, фозивудина, тодоксила, эмтрицитабина, аловудина, амдоксовира, элвуцитабина, невирапина, делавирдина, эфавиренца, ловирида, иммунокала, олтипраза, каправирина, лерсивирина, GSK2248761, TMC–278, TMC–125, этравирина, саквинавира, ритонавира, индинавира, нелфинавира, ампренавира, фосампренавира, бреканавира, дарунавира, атазанавира, типранавира, палинавира, лазинавира, энфувиртида, T–20, T–1249, PRO–542, PRO–140, TNX–355, BMS–806, BMS–663068 и BMS–626529, 5–Helix, ралтегравира, элвитегравира, GSK1349572, GSK1265744, викривирока (Sch–C), Sch–D, TAK779, маравирока, TAK449, диданозина, тенофовира, лопинавира или дарунавира.
26. Комбинация (а) соединения или его фармацевтически приемлемой соли или сложноэфирного пролекарства по любому из пп.1–9; и (b) ингибитора β–лактамазы.
27. Комбинация по п.26, где ингибитор β–лактамазы представляет собой клавуланат или клавулановую кислоту.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17382255 | 2017-05-08 | ||
| EP17382255.2 | 2017-05-08 | ||
| PCT/EP2018/061615 WO2018206466A1 (en) | 2017-05-08 | 2018-05-04 | Sanfetrinem or a salt or ester thereof for use in treating mycobacterial infection |
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| RU2019139864A true RU2019139864A (ru) | 2021-06-09 |
| RU2019139864A3 RU2019139864A3 (ru) | 2021-06-28 |
| RU2757272C2 RU2757272C2 (ru) | 2021-10-12 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ435990A3 (cs) | 1989-09-08 | 1999-11-17 | Glaxo S.P.A. | Kyselina 10-(1-hydroxyethyl)-11-oxo-1-azatricyklo/7,2,0,03,8/-undec-2en-2-karboxylová a její deriváty, způsob jejich výroby, použití pro výrobu farmaceutických prostředků a farmaceutické prostředky s jejich obsahem |
| GB9018330D0 (en) * | 1990-08-21 | 1990-10-03 | Glaxo Spa | Heterocyclic compounds |
| ES2054502T3 (es) | 1990-08-21 | 1994-08-01 | Glaxo Spa | Esteres del acido 10-(1-hidroxietil)-11-oxo-1-azatriciclo(7.2.0.0(3.8))-undec-2-en-2-carboxilico y un procedimiento para su preparacion. |
| GB9104769D0 (en) | 1991-03-07 | 1991-04-17 | Glaxo Spa | Heterocyclic compounds |
| GB9305813D0 (en) | 1993-03-20 | 1993-05-05 | Glaxo Spa | Chemical process |
| EP2085084A1 (en) * | 2008-01-29 | 2009-08-05 | LEK Pharmaceuticals D.D. | Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics |
| EP2135871A1 (en) * | 2008-06-18 | 2009-12-23 | LEK Pharmaceuticals D.D. | New trinem antibiotics and inhibitors of beta-lactamases |
| WO2016046845A1 (en) * | 2014-09-25 | 2016-03-31 | Manu Chaudhary | Stealth, targeted nanoparticles (stn) for oral drug delivery |
| MA41495A (fr) * | 2015-02-12 | 2017-12-19 | Anacor Pharmaceuticals Inc | Composés benzoxaborole et leurs utilisations |
-
2018
- 2018-05-04 RU RU2019139864A patent/RU2757272C2/ru active
- 2018-05-04 HU HUE18721053A patent/HUE059818T2/hu unknown
- 2018-05-04 PL PL18721053.9T patent/PL3621609T3/pl unknown
- 2018-05-04 SI SI201830762T patent/SI3621609T1/sl unknown
- 2018-05-04 US US16/611,908 patent/US11253500B2/en active Active
- 2018-05-04 CN CN201880030277.5A patent/CN110869016B/zh active Active
- 2018-05-04 HR HRP20221212TT patent/HRP20221212T1/hr unknown
- 2018-05-04 KR KR1020197032729A patent/KR102575872B1/ko active IP Right Grant
- 2018-05-04 RS RS20220731A patent/RS63461B1/sr unknown
- 2018-05-04 EP EP18721053.9A patent/EP3621609B1/en active Active
- 2018-05-04 LT LTEPPCT/EP2018/061615T patent/LT3621609T/lt unknown
- 2018-05-04 BR BR112019023322-9A patent/BR112019023322B1/pt active IP Right Grant
- 2018-05-04 AU AU2018265192A patent/AU2018265192B2/en active Active
- 2018-05-04 PT PT187210539T patent/PT3621609T/pt unknown
- 2018-05-04 CA CA3060396A patent/CA3060396A1/en active Pending
- 2018-05-04 JP JP2019561315A patent/JP7123074B2/ja active Active
- 2018-05-04 ES ES18721053T patent/ES2925215T3/es active Active
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Also Published As
| Publication number | Publication date |
|---|---|
| RU2757272C2 (ru) | 2021-10-12 |
| AU2018265192A1 (en) | 2019-11-07 |
| RS63461B1 (sr) | 2022-08-31 |
| BR112019023322B1 (pt) | 2023-11-14 |
| WO2018206466A1 (en) | 2018-11-15 |
| PL3621609T3 (pl) | 2022-11-14 |
| DK3621609T3 (da) | 2022-08-29 |
| RU2019139864A3 (ru) | 2021-06-28 |
| CN110869016A (zh) | 2020-03-06 |
| KR102575872B1 (ko) | 2023-09-08 |
| EP3621609B1 (en) | 2022-07-27 |
| SI3621609T1 (sl) | 2022-10-28 |
| CA3060396A1 (en) | 2018-11-15 |
| EP3621609A1 (en) | 2020-03-18 |
| HRP20221212T1 (hr) | 2022-12-09 |
| PT3621609T (pt) | 2022-08-24 |
| KR20200003816A (ko) | 2020-01-10 |
| HUE059818T2 (hu) | 2022-12-28 |
| ES2925215T3 (es) | 2022-10-14 |
| AU2018265192B2 (en) | 2021-06-17 |
| US20200289462A1 (en) | 2020-09-17 |
| JP2020519592A (ja) | 2020-07-02 |
| BR112019023322A2 (pt) | 2020-06-16 |
| US11253500B2 (en) | 2022-02-22 |
| ZA201906810B (en) | 2021-03-31 |
| CN110869016B (zh) | 2023-09-12 |
| JP7123074B2 (ja) | 2022-08-22 |
| LT3621609T (lt) | 2022-10-10 |
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