RU2017109814A - Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота - Google Patents
Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота Download PDFInfo
- Publication number
- RU2017109814A RU2017109814A RU2017109814A RU2017109814A RU2017109814A RU 2017109814 A RU2017109814 A RU 2017109814A RU 2017109814 A RU2017109814 A RU 2017109814A RU 2017109814 A RU2017109814 A RU 2017109814A RU 2017109814 A RU2017109814 A RU 2017109814A
- Authority
- RU
- Russia
- Prior art keywords
- hydrochloride salt
- fluoropyrrolidin
- cyclopropylamino
- dihydroquinoline
- fluoroethyl
- Prior art date
Links
- -1 CYCLOPROPYLAMINO Chemical class 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 16
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 9
- 239000003242 anti bacterial agent Substances 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 4
- YQHZQIJEMFMUGH-DFIJPDEKSA-N 7-[(3s,4s)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxoquinoline-3-carboxylic acid;hydrochloride Chemical compound Cl.C([C@@H]1[C@H](F)CN(C1)C1=C(C2=C(C(C(C(O)=O)=CN2CCF)=O)C=C1F)OC)NC1CC1 YQHZQIJEMFMUGH-DFIJPDEKSA-N 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- ZFIOCUITTUUVPV-MEDUHNTESA-N 7-[(3s,4s)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxoquinoline-3-carboxylic acid Chemical compound C([C@@H]1[C@H](F)CN(C1)C1=C(C2=C(C(C(C(O)=O)=CN2CCF)=O)C=C1F)OC)NC1CC1 ZFIOCUITTUUVPV-MEDUHNTESA-N 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 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
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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 containing two hetero rings
- C07D401/04—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 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2011246209 | 2011-11-10 | ||
| JP2011-246209 | 2011-11-10 | ||
| JP2012-071739 | 2012-03-27 | ||
| JP2012071739 | 2012-03-27 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014123567A Division RU2615509C2 (ru) | 2011-11-10 | 2012-11-09 | Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017109814A true RU2017109814A (ru) | 2019-01-23 |
| RU2017109814A3 RU2017109814A3 (https=) | 2020-04-08 |
Family
ID=48289529
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017109814A RU2017109814A (ru) | 2011-11-10 | 2012-11-09 | Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота |
| RU2014123567A RU2615509C2 (ru) | 2011-11-10 | 2012-11-09 | Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014123567A RU2615509C2 (ru) | 2011-11-10 | 2012-11-09 | Кристаллическая 7-{ (3s,4s)-3-[(циклопропиламино)метил]-4-фторпирролидин-1-ил} -6-фтор-1-(2-фторэтил)-8-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновая кислота |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US9090587B2 (https=) |
| EP (2) | EP3112359B1 (https=) |
| JP (4) | JP5871948B2 (https=) |
| KR (2) | KR20140098074A (https=) |
| CN (2) | CN103930414B (https=) |
| AU (1) | AU2016273899B2 (https=) |
| BR (1) | BR112014010765B1 (https=) |
| CA (1) | CA2855022C (https=) |
| ES (2) | ES2747303T3 (https=) |
| IN (1) | IN2014DN03277A (https=) |
| MX (1) | MX375073B (https=) |
| NZ (1) | NZ623808A (https=) |
| RU (2) | RU2017109814A (https=) |
| SA (1) | SA112330992B1 (https=) |
| SG (2) | SG10201608167UA (https=) |
| TW (1) | TWI547492B (https=) |
| WO (1) | WO2013069297A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12594418B2 (en) | 2011-03-10 | 2026-04-07 | Electrocore, Inc. | Devices and methods for nerve stimulation |
| SA112330992B1 (ar) * | 2011-11-10 | 2015-09-13 | كيورين فارماسوتيكال كو.، ليمتد | صورة متبلرة من 7-{(s4، s3)-3-[(سيكلو بروبيل أمينو) ميثيل]-4-فلورو بيروليدين-1-يل}-6-فلورو-1-(2-فلورو إيثيل)- 8-ميثوكسي-4-أوكسو-1، 4-داي هيدرو كينولين-3- حمض كربوكسيلي |
| WO2014174847A1 (ja) * | 2013-04-25 | 2014-10-30 | 杏林製薬株式会社 | 固形医薬組成物 |
| JP6349306B2 (ja) * | 2013-04-25 | 2018-06-27 | 杏林製薬株式会社 | 錠剤 |
| US9603804B2 (en) | 2013-04-25 | 2017-03-28 | Kyorin Pharmaceutical Co., Ltd. | Solid pharmaceutical composition |
| GB201402071D0 (en) | 2014-02-07 | 2014-03-26 | Galapagos Nv | Novel salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| US10154993B2 (en) | 2014-10-23 | 2018-12-18 | Kyorin Pharmaceutical Co., Ltd. | Solid pharmaceutical composition |
| EP3210608A4 (en) * | 2014-10-23 | 2018-06-20 | Kyorin Pharmaceutical Co., Ltd. | Solid pharmaceutical composition |
| WO2016148066A1 (ja) | 2015-03-13 | 2016-09-22 | 杏林製薬株式会社 | 呼吸器感染症治療剤 |
| WO2016195021A1 (ja) * | 2015-06-02 | 2016-12-08 | 杏林製薬株式会社 | 水性液剤 |
| EP3305294A4 (en) * | 2015-06-02 | 2019-02-20 | Kyorin Pharmaceutical Co., Ltd. | AQUEOUS MEDICINE |
| JP6675396B2 (ja) * | 2015-06-02 | 2020-04-01 | 杏林製薬株式会社 | 水性液剤 |
| BR112019025960A2 (pt) | 2017-06-16 | 2020-11-03 | Kyorin Pharmaceutical Co., Ltd. | agente terapêutico para pneumonia aspirativa, supuração pulmonar ou abcesso pulmonar |
| TW202415375A (zh) | 2017-06-16 | 2024-04-16 | 日商杏林製藥股份有限公司 | 吸入性肺炎、肺化膿症或肺膿瘍之治療劑 |
| GB201808575D0 (en) | 2018-05-24 | 2018-07-11 | Galapagos Nv | Methods for the treatment of psoriatic arthrits |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA944369B (en) * | 1993-08-27 | 1995-02-13 | Hokuriku Seuyaku Co Ltd | 5-amino-8-methyl-7-pyrrolidinylquinoline-3-carboxylic acid derivative |
| CN1158846A (zh) * | 1995-05-09 | 1997-09-10 | 昆山市康壮达兽药厂 | 盐酸氟哌酸的合成工艺 |
| US20030124028A1 (en) | 2001-08-10 | 2003-07-03 | Carlson Eric D. | Apparatuses and methods for creating and testing pre-formulations and systems for same |
| WO2003076428A1 (en) * | 2002-03-08 | 2003-09-18 | Daiichi Pharmaceutical Co., Ltd. | Quinolonecarboxylic acid derivative |
| CN100410249C (zh) | 2003-09-10 | 2008-08-13 | 杏林制药株式会社 | 7-(4-取代-3-环丙基氨基甲基-1-吡咯烷基)喹诺酮羧酸衍生物 |
| CN101003540A (zh) * | 2006-01-18 | 2007-07-25 | 广州白云山制药股份有限公司广州白云山制药总厂 | 一种抗感染化合物和用途 |
| SA112330992B1 (ar) * | 2011-11-10 | 2015-09-13 | كيورين فارماسوتيكال كو.، ليمتد | صورة متبلرة من 7-{(s4، s3)-3-[(سيكلو بروبيل أمينو) ميثيل]-4-فلورو بيروليدين-1-يل}-6-فلورو-1-(2-فلورو إيثيل)- 8-ميثوكسي-4-أوكسو-1، 4-داي هيدرو كينولين-3- حمض كربوكسيلي |
-
2012
- 2012-11-07 SA SA112330992A patent/SA112330992B1/ar unknown
- 2012-11-09 BR BR112014010765-3A patent/BR112014010765B1/pt not_active IP Right Cessation
- 2012-11-09 IN IN3277DEN2014 patent/IN2014DN03277A/en unknown
- 2012-11-09 MX MX2017006000A patent/MX375073B/es unknown
- 2012-11-09 TW TW101141841A patent/TWI547492B/zh active
- 2012-11-09 JP JP2013542858A patent/JP5871948B2/ja active Active
- 2012-11-09 SG SG10201608167UA patent/SG10201608167UA/en unknown
- 2012-11-09 SG SG11201401817TA patent/SG11201401817TA/en unknown
- 2012-11-09 ES ES16177827T patent/ES2747303T3/es active Active
- 2012-11-09 KR KR1020147012681A patent/KR20140098074A/ko not_active Ceased
- 2012-11-09 WO PCT/JP2012/007195 patent/WO2013069297A1/ja not_active Ceased
- 2012-11-09 CA CA2855022A patent/CA2855022C/en not_active Expired - Fee Related
- 2012-11-09 RU RU2017109814A patent/RU2017109814A/ru unknown
- 2012-11-09 RU RU2014123567A patent/RU2615509C2/ru active
- 2012-11-09 KR KR1020197015481A patent/KR102162208B1/ko active Active
- 2012-11-09 CN CN201280055120.0A patent/CN103930414B/zh active Active
- 2012-11-09 ES ES12846895.6T patent/ES2621664T3/es active Active
- 2012-11-09 NZ NZ623808A patent/NZ623808A/en not_active IP Right Cessation
- 2012-11-09 EP EP16177827.9A patent/EP3112359B1/en not_active Not-in-force
- 2012-11-09 EP EP12846895.6A patent/EP2778159B1/en not_active Not-in-force
- 2012-11-09 CN CN201510329284.3A patent/CN104945375B/zh active Active
- 2012-11-09 US US14/352,141 patent/US9090587B2/en not_active Expired - Fee Related
-
2015
- 2015-06-17 US US14/741,713 patent/US9328089B2/en not_active Ceased
- 2015-08-25 JP JP2015165879A patent/JP6514069B2/ja active Active
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2016
- 2016-12-14 AU AU2016273899A patent/AU2016273899B2/en not_active Ceased
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2017
- 2017-05-08 JP JP2017092125A patent/JP6349435B2/ja active Active
-
2018
- 2018-05-02 US US15/969,342 patent/USRE47785E1/en not_active Expired - Fee Related
- 2018-07-13 JP JP2018132781A patent/JP6818719B2/ja active Active
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