MX375073B - Cristal de acido 7-{(3s,4s)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxilico. - Google Patents
Cristal de acido 7-{(3s,4s)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxilico.Info
- Publication number
- MX375073B MX375073B MX2017006000A MX2017006000A MX375073B MX 375073 B MX375073 B MX 375073B MX 2017006000 A MX2017006000 A MX 2017006000A MX 2017006000 A MX2017006000 A MX 2017006000A MX 375073 B MX375073 B MX 375073B
- Authority
- MX
- Mexico
- Prior art keywords
- fluoropyrrolidine
- cyclopropylamino
- dihydroquinoline
- fluoroethyl
- oxo
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 6
- 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 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 238000000354 decomposition reaction Methods 0.000 abstract 1
- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 abstract 1
- 238000004321 preservation Methods 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-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
-
- 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)
Abstract
Se describe una técnica para mejorar la solubilidad en agua y estabilidad de almacenamiento de ácido 7-{(3S,4S)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(2-fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxílico (compuesto (1)) que es seguro y no solamente tiene una fuerte acción antibacteriana sino también es efectiva para bacterias resistentes para las cuales agentes antibacterianos convencionales son menos efectivos. Se proporcionan cristales de la sal de clorhidrato del compuesto (1), cristales de la sal de clorhidrato hidratada del compuesto (1), y cristales de la sal de metansulfonato del compuesto (1). En estos cristales, se elimina la descomposición debido a influencias de luz en comparación a la misma en cristales libres del compuesto (1), y su estabilidad de almacenamiento es alta. Estos cristales tienen solubilidad más alta en el agua que los cristales libres del compuesto (1).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2011246209 | 2011-11-10 | ||
| JP2012071739 | 2012-03-27 | ||
| PCT/JP2012/007195 WO2013069297A1 (ja) | 2011-11-10 | 2012-11-09 | 7-{(3s、4s)-3-[(シクロプロピルアミノ)メチル]-4-フルオロピロリジン-1-イル}-6-フルオロ-1-(2-フルオロエチル)-8-メトキシ-4-オキソ-1、4-ジヒドロキノリン-3-カルボン酸の結晶 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX375073B true MX375073B (es) | 2025-03-06 |
Family
ID=48289529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017006000A MX375073B (es) | 2011-11-10 | 2012-11-09 | Cristal de acido 7-{(3s,4s)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxilico. |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US9090587B2 (es) |
| EP (2) | EP3112359B1 (es) |
| JP (4) | JP5871948B2 (es) |
| KR (2) | KR102162208B1 (es) |
| CN (2) | CN103930414B (es) |
| AU (1) | AU2016273899B2 (es) |
| BR (1) | BR112014010765B1 (es) |
| CA (1) | CA2855022C (es) |
| ES (2) | ES2621664T3 (es) |
| IN (1) | IN2014DN03277A (es) |
| MX (1) | MX375073B (es) |
| NZ (1) | NZ623808A (es) |
| RU (2) | RU2017109814A (es) |
| SA (1) | SA112330992B1 (es) |
| SG (2) | SG10201608167UA (es) |
| TW (1) | TWI547492B (es) |
| WO (1) | WO2013069297A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2014174848A1 (ja) * | 2013-04-25 | 2014-10-30 | 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 |
| WO2014174847A1 (ja) * | 2013-04-25 | 2014-10-30 | 杏林製薬株式会社 | 固形医薬組成物 |
| GB201402071D0 (en) | 2014-02-07 | 2014-03-26 | Galapagos Nv | Novel salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| JP6018334B2 (ja) * | 2014-10-23 | 2016-11-02 | 杏林製薬株式会社 | 固形医薬組成物 |
| EP3210608A4 (en) * | 2014-10-23 | 2018-06-20 | Kyorin Pharmaceutical Co., Ltd. | Solid pharmaceutical composition |
| SG10201908007UA (en) * | 2015-03-13 | 2019-10-30 | Kyorin Pharmaceutical Co Ltd | Respiratory infection treating agent |
| US10617684B2 (en) | 2015-06-02 | 2020-04-14 | Kyorin Pharmaceutical Co., Ltd. | Aqueous drug |
| WO2016195020A1 (ja) * | 2015-06-02 | 2016-12-08 | 杏林製薬株式会社 | 水性液剤 |
| US10406149B2 (en) | 2015-06-02 | 2019-09-10 | Kyorin Pharmaceutical Co., Ltd. | Aqueous liquid formulation |
| WO2018230686A1 (ja) | 2017-06-16 | 2018-12-20 | 杏林製薬株式会社 | 誤嚥性肺炎、肺化膿症又は肺膿瘍の治療剤 |
| BR112019025960A2 (pt) | 2017-06-16 | 2020-11-03 | Kyorin Pharmaceutical Co., Ltd. | agente terapêutico para pneumonia aspirativa, supuração pulmonar ou abcesso pulmonar |
| 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 |
| US20030119060A1 (en) | 2001-08-10 | 2003-06-26 | Desrosiers Peter J. | 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 |
| SI1666477T1 (sl) | 2003-09-10 | 2013-10-30 | Kyorin Pharmaceutical Co., Ltd. | Derivati 7-(4-substituiran 3-ciklopropilaminometil-1-pirolidinil) kinolonkarboksilne kisline |
| 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 KR KR1020197015481A patent/KR102162208B1/ko active Active
- 2012-11-09 CN CN201280055120.0A patent/CN103930414B/zh active Active
- 2012-11-09 WO PCT/JP2012/007195 patent/WO2013069297A1/ja not_active Ceased
- 2012-11-09 EP EP16177827.9A patent/EP3112359B1/en not_active Not-in-force
- 2012-11-09 US US14/352,141 patent/US9090587B2/en not_active Expired - Fee Related
- 2012-11-09 RU RU2017109814A patent/RU2017109814A/ru unknown
- 2012-11-09 MX MX2017006000A patent/MX375073B/es unknown
- 2012-11-09 BR BR112014010765-3A patent/BR112014010765B1/pt not_active IP Right Cessation
- 2012-11-09 RU RU2014123567A patent/RU2615509C2/ru active
- 2012-11-09 CN CN201510329284.3A patent/CN104945375B/zh active Active
- 2012-11-09 JP JP2013542858A patent/JP5871948B2/ja active Active
- 2012-11-09 IN IN3277DEN2014 patent/IN2014DN03277A/en unknown
- 2012-11-09 KR KR1020147012681A patent/KR20140098074A/ko not_active Ceased
- 2012-11-09 NZ NZ623808A patent/NZ623808A/en not_active IP Right Cessation
- 2012-11-09 SG SG10201608167UA patent/SG10201608167UA/en unknown
- 2012-11-09 EP EP12846895.6A patent/EP2778159B1/en not_active Not-in-force
- 2012-11-09 CA CA2855022A patent/CA2855022C/en not_active Expired - Fee Related
- 2012-11-09 SG SG11201401817TA patent/SG11201401817TA/en unknown
- 2012-11-09 ES ES12846895.6T patent/ES2621664T3/es active Active
- 2012-11-09 ES ES16177827T patent/ES2747303T3/es active Active
- 2012-11-09 TW TW101141841A patent/TWI547492B/zh active
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2015
- 2015-06-17 US US14/741,713 patent/US9328089B2/en not_active Ceased
- 2015-08-25 JP JP2015165879A patent/JP6514069B2/ja active Active
-
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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