EA031348B1 - КРИСТАЛЛИЧЕСКИЙ ИНГИБИТОР β-ЛАКТАМАЗЫ - Google Patents
КРИСТАЛЛИЧЕСКИЙ ИНГИБИТОР β-ЛАКТАМАЗЫ Download PDFInfo
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- EA031348B1 EA031348B1 EA201690963A EA201690963A EA031348B1 EA 031348 B1 EA031348 B1 EA 031348B1 EA 201690963 A EA201690963 A EA 201690963A EA 201690963 A EA201690963 A EA 201690963A EA 031348 B1 EA031348 B1 EA 031348B1
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- EA
- Eurasian Patent Office
- Prior art keywords
- methyl
- formula
- crystalline compound
- compound according
- crystalline
- Prior art date
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- 239000003781 beta lactamase inhibitor Substances 0.000 title abstract description 7
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title abstract description 7
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 title abstract description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 91
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- 208000035143 Bacterial infection Diseases 0.000 claims abstract description 8
- 208000022362 bacterial infectious disease Diseases 0.000 claims abstract description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 70
- 239000000203 mixture Substances 0.000 claims description 62
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- 238000000034 method Methods 0.000 claims description 52
- 238000001228 spectrum Methods 0.000 claims description 42
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- 239000002904 solvent Substances 0.000 claims description 25
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 24
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 23
- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 18
- 239000012296 anti-solvent Substances 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 18
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 15
- ZMXDDKWLCZADIW-UHFFFAOYSA-N dimethylformamide Substances CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 14
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 12
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- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 9
- 239000000126 substance Substances 0.000 claims description 9
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims description 8
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D499/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D499/86—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with only atoms other than nitrogen atoms directly attached in position 6 and 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
-
- 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
-
- 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
- C07D499/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D499/87—Compounds being unsubstituted in position 3 or with substituents other than only two methyl radicals attached in position 3, 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
-
- 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
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- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
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- General Chemical & Material Sciences (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1319776.9A GB201319776D0 (en) | 2013-11-08 | 2013-11-08 | Compound |
| GBGB1408643.3A GB201408643D0 (en) | 2013-11-08 | 2014-05-15 | Compound |
| PCT/EP2014/074108 WO2015067787A1 (en) | 2013-11-08 | 2014-11-07 | Crystalline beta-lactamase inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201690963A1 EA201690963A1 (ru) | 2016-10-31 |
| EA031348B1 true EA031348B1 (ru) | 2018-12-28 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201690963A EA031348B1 (ru) | 2013-11-08 | 2014-11-07 | КРИСТАЛЛИЧЕСКИЙ ИНГИБИТОР β-ЛАКТАМАЗЫ |
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| US (2) | US20160289245A1 (enExample) |
| EP (1) | EP3066103A1 (enExample) |
| JP (2) | JP7045795B2 (enExample) |
| KR (1) | KR20160081964A (enExample) |
| CN (1) | CN105873935B (enExample) |
| AU (1) | AU2014345507B2 (enExample) |
| CA (1) | CA2929199C (enExample) |
| CL (1) | CL2016001097A1 (enExample) |
| EA (1) | EA031348B1 (enExample) |
| GB (2) | GB201319776D0 (enExample) |
| IL (1) | IL245386A0 (enExample) |
| MX (1) | MX2016005869A (enExample) |
| PE (1) | PE20160890A1 (enExample) |
| WO (1) | WO2015067787A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB201319776D0 (en) * | 2013-11-08 | 2013-12-25 | Allecra Therapeutics Sas | Compound |
| WO2026086730A1 (zh) * | 2024-10-21 | 2026-04-30 | 齐鲁制药有限公司 | 恩美他唑巴坦的晶型及其制备方法 |
Citations (1)
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|---|---|---|---|---|
| WO2008010048A2 (en) * | 2006-07-12 | 2008-01-24 | Orchid Chemicals & Pharmaceuticals Limited | Novel 2-substituted methyl penam derivatives |
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| US4562073A (en) * | 1982-12-24 | 1985-12-31 | Taiho Pharmaceutical Company Limited | Penicillin derivatives |
| US6156745A (en) * | 1997-12-29 | 2000-12-05 | Research Corporation Technologies, Inc. | 2β-substituted-6-alkylidene penicillanic acid derivatives as β-lactamase inhibitors |
| US7273935B2 (en) * | 2003-08-21 | 2007-09-25 | Orchid Chemicals & Pharmaceuticals, Ltd. | Process for the preparation of 3-methylcepham derivatives |
| US7417143B2 (en) * | 2004-04-07 | 2008-08-26 | Orchid Chemicals & Pharmaceuticals Limited | Process for the preparation of Tazobactam in pure form |
| NZ610247A (en) * | 2010-11-25 | 2014-09-26 | Allecra Therapeutics Gmbh | Β-lactamase inhibitors and their use |
| EP2847205A4 (en) * | 2012-05-07 | 2016-01-20 | Univ California | NOVEL OXYSTEROL ANALOGUE OXY149 FOR THE INDUCTION OF OSTEOGENESIS AND HEDGEHOG SIGNAL PATH AND THE INHIBITION OF ADIPOGENESIS |
| US9683009B2 (en) * | 2013-05-02 | 2017-06-20 | The Regents Of The University Of California | Bone-selective osteogenic oxysterol-bone targeting agents |
| GB201319776D0 (en) | 2013-11-08 | 2013-12-25 | Allecra Therapeutics Sas | Compound |
| GB201408649D0 (en) * | 2014-05-15 | 2014-07-02 | Allecra Therapeutics Sas | Method |
| KR20170101940A (ko) * | 2014-12-09 | 2017-09-06 | 워쏘우 오르쏘페딕 인코포레이티드 | 스테롤 관련 화합물 및 방법 |
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2013
- 2013-11-08 GB GBGB1319776.9A patent/GB201319776D0/en not_active Ceased
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2014
- 2014-05-15 GB GBGB1408643.3A patent/GB201408643D0/en not_active Ceased
- 2014-11-07 US US15/035,176 patent/US20160289245A1/en not_active Abandoned
- 2014-11-07 KR KR1020167014701A patent/KR20160081964A/ko not_active Withdrawn
- 2014-11-07 EA EA201690963A patent/EA031348B1/ru not_active IP Right Cessation
- 2014-11-07 JP JP2016527458A patent/JP7045795B2/ja active Active
- 2014-11-07 CA CA2929199A patent/CA2929199C/en active Active
- 2014-11-07 AU AU2014345507A patent/AU2014345507B2/en active Active
- 2014-11-07 WO PCT/EP2014/074108 patent/WO2015067787A1/en not_active Ceased
- 2014-11-07 EP EP14799382.8A patent/EP3066103A1/en not_active Withdrawn
- 2014-11-07 MX MX2016005869A patent/MX2016005869A/es unknown
- 2014-11-07 PE PE2016000598A patent/PE20160890A1/es not_active Application Discontinuation
- 2014-11-07 CN CN201480071497.4A patent/CN105873935B/zh active Active
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2016
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- 2016-05-06 CL CL2016001097A patent/CL2016001097A1/es unknown
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2018
- 2018-10-31 US US16/177,406 patent/US11124526B2/en active Active
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2021
- 2021-03-26 JP JP2021052653A patent/JP7346485B2/ja active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008010048A2 (en) * | 2006-07-12 | 2008-01-24 | Orchid Chemicals & Pharmaceuticals Limited | Novel 2-substituted methyl penam derivatives |
Non-Patent Citations (1)
| Title |
|---|
| YU L: "AMORPHOUS PHARMACEUTICAL SOLIDS: PREPARATION, CHARACTERIZATION AND STABILIZATION", ADVANCED DRUG DELIVERY REVIEWS, ELSEVIER, AMSTERDAM, NL, vol. 48, no. 01, 16 May 2001 (2001-05-16), AMSTERDAM, NL, pages 27 - 42, XP009065056, ISSN: 0169-409X, DOI: 10.1016/S0169-409X(01)00098-9 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3066103A1 (en) | 2016-09-14 |
| GB201319776D0 (en) | 2013-12-25 |
| CA2929199A1 (en) | 2015-05-14 |
| GB201408643D0 (en) | 2014-07-02 |
| US20190071456A1 (en) | 2019-03-07 |
| JP7045795B2 (ja) | 2022-04-01 |
| CN105873935B (zh) | 2019-03-19 |
| CA2929199C (en) | 2023-01-03 |
| CL2016001097A1 (es) | 2016-12-02 |
| AU2014345507A1 (en) | 2016-05-19 |
| WO2015067787A1 (en) | 2015-05-14 |
| JP2016535054A (ja) | 2016-11-10 |
| US20160289245A1 (en) | 2016-10-06 |
| AU2014345507B2 (en) | 2018-11-22 |
| JP2021102642A (ja) | 2021-07-15 |
| JP7346485B2 (ja) | 2023-09-19 |
| KR20160081964A (ko) | 2016-07-08 |
| PE20160890A1 (es) | 2016-08-25 |
| CN105873935A (zh) | 2016-08-17 |
| MX2016005869A (es) | 2017-01-05 |
| US11124526B2 (en) | 2021-09-21 |
| IL245386A0 (en) | 2016-06-30 |
| EA201690963A1 (ru) | 2016-10-31 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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