EA201991618A1 - Кристаллические формы тебипенема пивоксила, композиции, содержащие их, способы изготовления и способы применения - Google Patents
Кристаллические формы тебипенема пивоксила, композиции, содержащие их, способы изготовления и способы примененияInfo
- Publication number
- EA201991618A1 EA201991618A1 EA201991618A EA201991618A EA201991618A1 EA 201991618 A1 EA201991618 A1 EA 201991618A1 EA 201991618 A EA201991618 A EA 201991618A EA 201991618 A EA201991618 A EA 201991618A EA 201991618 A1 EA201991618 A1 EA 201991618A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- salt
- tebipenem pivoxil
- pivoxil
- methods
- crystalline
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 2
- 229950009297 pivoxil Drugs 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title 1
- SNUDIPVBUUXCDG-QHSBEEBCSA-N tebipenem pivoxil Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(=O)OCOC(=O)C(C)(C)C)=O)[C@H](O)C)SC(C1)CN1C1=NCCS1 SNUDIPVBUUXCDG-QHSBEEBCSA-N 0.000 abstract 10
- 229950007537 tebipenem pivoxil Drugs 0.000 abstract 9
- 150000003839 salts Chemical group 0.000 abstract 7
- 229940049920 malate Drugs 0.000 abstract 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 abstract 2
- KPGXRSRHYNQIFN-UHFFFAOYSA-L 2-oxoglutarate(2-) Chemical compound [O-]C(=O)CCC(=O)C([O-])=O KPGXRSRHYNQIFN-UHFFFAOYSA-L 0.000 abstract 1
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 230000003115 biocidal effect Effects 0.000 abstract 1
- YKGMKSIHIVVYKY-UHFFFAOYSA-N dabrafenib mesylate Chemical compound CS(O)(=O)=O.S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 YKGMKSIHIVVYKY-UHFFFAOYSA-N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 abstract 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- C07D477/10—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 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and 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
- C07D477/12—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 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and 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 6
- C07D477/16—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 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and 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 6 with hetero atoms or carbon atoms 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 3
- C07D477/20—Sulfur atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- 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
- A61K31/425—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
- A61K31/431—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 containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Настоящее изобретение направлено на новые кристаллические солевые формы тебипенема пивоксила, включая кристаллическую солевую форму этансульфоната тебипенема пивоксила (форму A), кристаллическую солевую форму кетоглутарата тебипенема пивоксила (форму A), солевые формы малеата тебипенема пивоксила (формы A и B), солевую форму малата тебипенема пивоксила (форму A), солевую форму метансульфоната тебипенема пивоксила (форму B), солевую форму гидробромида тебипенема пивоксила (форму B) и солевую форму эдизилата тебипенема пивоксила (форму A). Настоящее изобретение также включает композицию, содержащую кристаллическую соль тебипенема пивоксила и фармацевтически приемлемый носитель, и дополнительно включает способ лечения устойчивой к действию антибиотиков бактериальной инфекции, включающий введение пациенту, нуждающемуся в таком лечении, терапевтически эффективного количества кристаллической соли тебипенема пивоксила.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762455109P | 2017-02-06 | 2017-02-06 | |
PCT/US2018/017067 WO2018145089A1 (en) | 2017-02-06 | 2018-02-06 | Tebipenem pivoxil crystalline forms, compositions including the same, methods of manufacture, and methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201991618A1 true EA201991618A1 (ru) | 2020-01-30 |
Family
ID=61244766
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201991618A EA201991618A1 (ru) | 2017-02-06 | 2018-02-06 | Кристаллические формы тебипенема пивоксила, композиции, содержащие их, способы изготовления и способы применения |
Country Status (16)
Country | Link |
---|---|
US (3) | US10889587B2 (ru) |
EP (1) | EP3577119A1 (ru) |
JP (1) | JP7309607B2 (ru) |
KR (1) | KR102608037B1 (ru) |
CN (2) | CN110234651A (ru) |
AU (2) | AU2018215687B2 (ru) |
BR (1) | BR112019015487A2 (ru) |
CA (1) | CA3049690C (ru) |
CO (1) | CO2019007879A2 (ru) |
EA (1) | EA201991618A1 (ru) |
IL (1) | IL268092B2 (ru) |
MX (1) | MX2019009288A (ru) |
NZ (1) | NZ753781A (ru) |
PH (1) | PH12019501245A1 (ru) |
WO (1) | WO2018145089A1 (ru) |
ZA (2) | ZA201903310B (ru) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
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KR102608037B1 (ko) | 2017-02-06 | 2023-11-30 | 스페로 테라퓨틱스, 인코퍼레이티드 | 테비페넴 피복실 결정질 형태, 이를 포함하는 조성물, 제조 방법, 및 사용 방법 |
CN110804057A (zh) * | 2019-11-11 | 2020-02-18 | 浙江海翔药业股份有限公司 | 替比培南酯氢溴酸盐晶型及其制备方法、药物组合物和制药用途 |
CA3201497A1 (en) * | 2020-11-11 | 2022-05-19 | Spero Therapeutics, Inc. | High dosage tebipenem pivoxil tablet formulation |
CN112812116A (zh) * | 2020-12-31 | 2021-05-18 | 山东华鲁制药有限公司 | 一种药用替比培南匹伏酯的制备方法 |
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IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
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TW420681B (en) | 1995-12-08 | 2001-02-01 | Lederle Japan Ltd | Carbapenem-3-carboxylic acid ester derivatives |
JP3317649B2 (ja) * | 1997-01-13 | 2002-08-26 | 日本ワイスレダリー株式会社 | 結晶形態のカルバペネム化合物 |
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KR100950699B1 (ko) * | 2008-03-28 | 2010-03-31 | 국제약품공업주식회사 | 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르유도체의 산부가염, 이의 제조방법 및 이를 포함하는 약학조성물 |
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KR100930586B1 (ko) * | 2007-11-23 | 2009-12-09 | 한국화학연구원 | 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체,이의 제조방법 및 이를 포함하는 약학 조성물 |
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US20200016126A1 (en) * | 2016-12-15 | 2020-01-16 | Spero Therapeutics, Inc. | Novel tebipenem pivoxil immediate and modified release oral dosage forms |
KR102608037B1 (ko) | 2017-02-06 | 2023-11-30 | 스페로 테라퓨틱스, 인코퍼레이티드 | 테비페넴 피복실 결정질 형태, 이를 포함하는 조성물, 제조 방법, 및 사용 방법 |
CN108640920B (zh) | 2018-04-03 | 2020-03-27 | 科兴生物制药股份有限公司 | 一种替比培南酯的制备方法 |
CN109096283A (zh) | 2018-09-03 | 2018-12-28 | 成都倍特药业有限公司 | 一种高纯度替比培南酯晶体的制备方法 |
CN109651372A (zh) | 2018-12-27 | 2019-04-19 | 开封制药(集团)有限公司 | 一种替比培南酸的制备方法 |
-
2018
- 2018-02-06 KR KR1020197023950A patent/KR102608037B1/ko active IP Right Grant
- 2018-02-06 CA CA3049690A patent/CA3049690C/en active Active
- 2018-02-06 CN CN201880009327.1A patent/CN110234651A/zh active Pending
- 2018-02-06 EP EP18706094.2A patent/EP3577119A1/en active Pending
- 2018-02-06 MX MX2019009288A patent/MX2019009288A/es unknown
- 2018-02-06 WO PCT/US2018/017067 patent/WO2018145089A1/en active Application Filing
- 2018-02-06 EA EA201991618A patent/EA201991618A1/ru unknown
- 2018-02-06 US US16/483,989 patent/US10889587B2/en active Active
- 2018-02-06 BR BR112019015487-6A patent/BR112019015487A2/pt active Search and Examination
- 2018-02-06 JP JP2019542373A patent/JP7309607B2/ja active Active
- 2018-02-06 CN CN202311492390.4A patent/CN117551102A/zh active Pending
- 2018-02-06 NZ NZ753781A patent/NZ753781A/en unknown
- 2018-02-06 AU AU2018215687A patent/AU2018215687B2/en active Active
-
2019
- 2019-05-24 ZA ZA2019/03310A patent/ZA201903310B/en unknown
- 2019-06-04 PH PH12019501245A patent/PH12019501245A1/en unknown
- 2019-07-16 IL IL268092A patent/IL268092B2/en unknown
- 2019-07-22 CO CONC2019/0007879A patent/CO2019007879A2/es unknown
-
2020
- 2020-12-03 AU AU2020281120A patent/AU2020281120A1/en not_active Abandoned
- 2020-12-29 US US17/136,759 patent/US11718621B2/en active Active
-
2021
- 2021-05-24 ZA ZA2021/03498A patent/ZA202103498B/en unknown
-
2023
- 2023-06-09 US US18/332,566 patent/US12098155B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
CN117551102A (zh) | 2024-02-13 |
JP2020506196A (ja) | 2020-02-27 |
AU2018215687A1 (en) | 2019-06-13 |
AU2020281120A1 (en) | 2021-01-07 |
CA3049690C (en) | 2023-03-21 |
IL268092A (en) | 2019-09-26 |
MX2019009288A (es) | 2019-09-10 |
US20210122753A1 (en) | 2021-04-29 |
BR112019015487A2 (pt) | 2020-03-31 |
ZA202103498B (en) | 2023-01-25 |
US12098155B2 (en) | 2024-09-24 |
US20230331728A1 (en) | 2023-10-19 |
CO2019007879A2 (es) | 2019-07-31 |
IL268092B (en) | 2022-10-01 |
US20200055857A1 (en) | 2020-02-20 |
EP3577119A1 (en) | 2019-12-11 |
US10889587B2 (en) | 2021-01-12 |
US11718621B2 (en) | 2023-08-08 |
KR102608037B1 (ko) | 2023-11-30 |
ZA201903310B (en) | 2021-09-29 |
IL268092B2 (en) | 2023-02-01 |
PH12019501245A1 (en) | 2020-03-02 |
CA3049690A1 (en) | 2018-08-09 |
JP7309607B2 (ja) | 2023-07-18 |
CN110234651A (zh) | 2019-09-13 |
AU2018215687B2 (en) | 2020-09-03 |
NZ753781A (en) | 2022-10-28 |
KR20190115000A (ko) | 2019-10-10 |
WO2018145089A1 (en) | 2018-08-09 |
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