JP5651174B2 - ビフェニル化合物の結晶性遊離塩基形 - Google Patents

ビフェニル化合物の結晶性遊離塩基形 Download PDF

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JP5651174B2
JP5651174B2 JP2012520734A JP2012520734A JP5651174B2 JP 5651174 B2 JP5651174 B2 JP 5651174B2 JP 2012520734 A JP2012520734 A JP 2012520734A JP 2012520734 A JP2012520734 A JP 2012520734A JP 5651174 B2 JP5651174 B2 JP 5651174B2
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free base
crystalline free
crystalline
compound
ethyl
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JP2012533550A (ja
JP2012533550A5 (enExample
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グラハム ウォーラム，
グラハム ウォーラム，
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セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー
セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー
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Application filed by セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー, セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー filed Critical セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー
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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • A61K31/44—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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A61K9/124—Aerosols; Foams characterised by the propellant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/64—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
JP2012520734A 2009-07-15 2010-07-14 ビフェニル化合物の結晶性遊離塩基形 Active JP5651174B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22580309P 2009-07-15 2009-07-15
US61/225,803 2009-07-15
PCT/US2010/041903 WO2011008809A1 (en) 2009-07-15 2010-07-14 Crystalline freebase forms of a biphenyl compound

Related Child Applications (1)

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JP2014206123A Division JP6338505B2 (ja) 2009-07-15 2014-10-07 ビフェニル化合物の結晶性遊離塩基形

Publications (3)

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JP2012533550A JP2012533550A (ja) 2012-12-27
JP2012533550A5 JP2012533550A5 (enExample) 2013-06-20
JP5651174B2 true JP5651174B2 (ja) 2015-01-07

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JP2012520734A Active JP5651174B2 (ja) 2009-07-15 2010-07-14 ビフェニル化合物の結晶性遊離塩基形
JP2014206123A Active JP6338505B2 (ja) 2009-07-15 2014-10-07 ビフェニル化合物の結晶性遊離塩基形
JP2015216372A Pending JP2016026214A (ja) 2009-07-15 2015-11-04 ビフェニル化合物の結晶性遊離塩基形
JP2017134632A Pending JP2017171692A (ja) 2009-07-15 2017-07-10 ビフェニル化合物の結晶性遊離塩基形

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JP2015216372A Pending JP2016026214A (ja) 2009-07-15 2015-11-04 ビフェニル化合物の結晶性遊離塩基形
JP2017134632A Pending JP2017171692A (ja) 2009-07-15 2017-07-10 ビフェニル化合物の結晶性遊離塩基形

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US (12) US8541451B2 (enExample)
EP (2) EP2987490B1 (enExample)
JP (4) JP5651174B2 (enExample)
KR (1) KR101742252B1 (enExample)
CN (1) CN102470130B (enExample)
AU (1) AU2010273514B2 (enExample)
BR (1) BR112012000890A2 (enExample)
CA (2) CA2765621C (enExample)
DK (1) DK2453894T3 (enExample)
ES (2) ES2557553T3 (enExample)
HR (1) HRP20151344T1 (enExample)
HU (1) HUE026414T2 (enExample)
IL (1) IL216995A (enExample)
MX (1) MX2012000682A (enExample)
PL (2) PL2987490T3 (enExample)
PT (1) PT2453894E (enExample)
SG (2) SG178036A1 (enExample)
SI (1) SI2453894T1 (enExample)
SM (1) SMT201600019B (enExample)
WO (1) WO2011008809A1 (enExample)

Cited By (1)

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JP2015003929A (ja) * 2009-07-15 2015-01-08 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ビフェニル化合物の結晶性遊離塩基形

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CN112694434B (zh) * 2020-12-29 2023-06-16 浙江和泽医药科技股份有限公司 一种雷芬那辛新中间体及其活性亲电砌块和雷芬那辛的新制备方法
CN118401497A (zh) 2021-12-09 2024-07-26 医药化学公司 雷芬那辛的结晶型丙酮溶剂化物
CN114276290B (zh) * 2021-12-24 2024-05-28 浙江和泽医药科技股份有限公司 一种雷芬那辛无水晶型及其制备方法
CN117180235A (zh) * 2023-09-19 2023-12-08 山东京卫制药有限公司 一种无定型雷芬那辛吸入制剂
CN117263848A (zh) * 2023-09-19 2023-12-22 山东京卫制药有限公司 一种雷芬那辛的吸入喷雾剂
CN117263849A (zh) * 2023-09-19 2023-12-22 山东京卫制药有限公司 一种雷芬那辛三水合物晶型及其制备方法
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Publication number Priority date Publication date Assignee Title
JP2015003929A (ja) * 2009-07-15 2015-01-08 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ビフェニル化合物の結晶性遊離塩基形

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AU2010273514B2 (en) 2015-01-22
US20180186740A1 (en) 2018-07-05
KR101742252B1 (ko) 2017-05-31
US8541451B2 (en) 2013-09-24
SMT201600019B (it) 2016-02-25
PT2453894E (pt) 2016-02-02
JP2012533550A (ja) 2012-12-27
US11649209B2 (en) 2023-05-16
KR20130027004A (ko) 2013-03-14
US9226896B2 (en) 2016-01-05
HK1219415A1 (en) 2017-04-07
EP2987490B1 (en) 2017-06-14
US10100013B2 (en) 2018-10-16
US20160143897A1 (en) 2016-05-26
HUE026414T2 (hu) 2016-05-30
SG178036A1 (en) 2012-03-29
CA2989129A1 (en) 2011-01-20
EP2987490A1 (en) 2016-02-24
US8921396B2 (en) 2014-12-30
US11691948B2 (en) 2023-07-04
JP2016026214A (ja) 2016-02-12
JP2015003929A (ja) 2015-01-08
PL2453894T3 (pl) 2016-04-29
HRP20151344T1 (hr) 2016-01-01
SI2453894T1 (sl) 2016-02-29
WO2011008809A1 (en) 2011-01-20
JP6338505B2 (ja) 2018-06-06
MX2012000682A (es) 2012-02-28
US11858898B2 (en) 2024-01-02
US20220009890A1 (en) 2022-01-13
US9415041B2 (en) 2016-08-16
US9765028B2 (en) 2017-09-19
US20190248743A1 (en) 2019-08-15
US20230303492A1 (en) 2023-09-28
US20250179019A1 (en) 2025-06-05
BR112012000890A2 (pt) 2017-10-31
CN102470130A (zh) 2012-05-23
CA2989129C (en) 2021-03-09
CA2765621C (en) 2018-02-13
US20170081283A1 (en) 2017-03-23
IL216995A0 (en) 2012-02-29
ES2639642T3 (es) 2017-10-27
CN102470130B (zh) 2013-09-04
IL216995A (en) 2017-10-31
JP2017171692A (ja) 2017-09-28
ES2557553T3 (es) 2016-01-27
EP2453894A1 (en) 2012-05-23
SG10201407913UA (en) 2015-01-29
EP2453894B1 (en) 2015-11-04
US20220306580A1 (en) 2022-09-29
PL2987490T3 (pl) 2017-12-29
US20130338191A1 (en) 2013-12-19
DK2453894T3 (en) 2016-01-25
CA2765621A1 (en) 2011-01-20
US10550081B2 (en) 2020-02-04
US20110015163A1 (en) 2011-01-20
AU2010273514A1 (en) 2012-01-19
HK1168050A1 (zh) 2012-12-21
US11008289B2 (en) 2021-05-18
US20200308116A1 (en) 2020-10-01
US20150164796A1 (en) 2015-06-18

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