AU2010273514B2 - Crystalline freebase forms of a biphenyl compound - Google Patents

Crystalline freebase forms of a biphenyl compound Download PDF

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Publication number
AU2010273514B2
AU2010273514B2 AU2010273514A AU2010273514A AU2010273514B2 AU 2010273514 B2 AU2010273514 B2 AU 2010273514B2 AU 2010273514 A AU2010273514 A AU 2010273514A AU 2010273514 A AU2010273514 A AU 2010273514A AU 2010273514 B2 AU2010273514 B2 AU 2010273514B2
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AU
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Prior art keywords
crystalline
crystalline freebase
compound
ethyl
ester
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AU2010273514A
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AU2010273514A1 (en
Inventor
Grahame Woollam
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • A61K9/124Aerosols; Foams characterised by the propellant
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon 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
    • C07D211/64Carbon 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
AU2010273514A 2009-07-15 2010-07-14 Crystalline freebase forms of a biphenyl compound Active AU2010273514B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2010273514A1 AU2010273514A1 (en) 2012-01-19
AU2010273514B2 true AU2010273514B2 (en) 2015-01-22

Family

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AU2010273514A Active AU2010273514B2 (en) 2009-07-15 2010-07-14 Crystalline freebase forms of a biphenyl compound

Country Status (20)

Country Link
US (12) US8541451B2 (https=)
EP (2) EP2453894B1 (https=)
JP (4) JP5651174B2 (https=)
KR (1) KR101742252B1 (https=)
CN (1) CN102470130B (https=)
AU (1) AU2010273514B2 (https=)
BR (1) BR112012000890A2 (https=)
CA (2) CA2989129C (https=)
DK (1) DK2453894T3 (https=)
ES (2) ES2557553T3 (https=)
HR (1) HRP20151344T1 (https=)
HU (1) HUE026414T2 (https=)
IL (1) IL216995A (https=)
MX (1) MX2012000682A (https=)
PL (2) PL2453894T3 (https=)
PT (1) PT2453894E (https=)
SG (2) SG10201407913UA (https=)
SI (1) SI2453894T1 (https=)
SM (1) SMT201600019B (https=)
WO (1) WO2011008809A1 (https=)

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KR101742253B1 (ko) 2010-07-13 2017-05-31 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 비페닐-2-일카르밤산의 제조방법
MX386473B (es) * 2013-02-21 2025-03-18 Pfizer Formas solidas de un inhibidor de cdk4/6 selectivo
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US11484531B2 (en) 2018-08-30 2022-11-01 Theravance Biopharma R&D Ip, Llc Methods for treating chronic obstructive pulmonary disease
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
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
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
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
US20250136550A1 (en) 2023-10-27 2025-05-01 Theravance Biopharma R&D Ip, Llc Processes for preparing revefenacin and compositions comprising the same
CN117700354A (zh) * 2023-12-12 2024-03-15 江苏百奥信康医药科技有限公司 一种雷芬那辛的晶体形式及其制备方法
CN119775192B (zh) * 2024-12-31 2025-11-28 山东京卫制药有限公司 一种三苯乙酸雷芬那辛晶型及其制备方法

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US11858898B2 (en) 2024-01-02
US10100013B2 (en) 2018-10-16
JP2015003929A (ja) 2015-01-08
KR20130027004A (ko) 2013-03-14
SMT201600019B (it) 2016-02-25
US20110015163A1 (en) 2011-01-20
IL216995A (en) 2017-10-31
US20230303492A1 (en) 2023-09-28
PL2453894T3 (pl) 2016-04-29
HRP20151344T1 (hr) 2016-01-01
CA2989129A1 (en) 2011-01-20
US9226896B2 (en) 2016-01-05
US8921396B2 (en) 2014-12-30
HK1219415A1 (en) 2017-04-07
JP2016026214A (ja) 2016-02-12
CA2765621A1 (en) 2011-01-20
PT2453894E (pt) 2016-02-02
US20220009890A1 (en) 2022-01-13
US20170081283A1 (en) 2017-03-23
US20200308116A1 (en) 2020-10-01
US11649209B2 (en) 2023-05-16
HK1168050A1 (zh) 2012-12-21
US20150164796A1 (en) 2015-06-18
IL216995A0 (en) 2012-02-29
US20160143897A1 (en) 2016-05-26
KR101742252B1 (ko) 2017-05-31
US20180186740A1 (en) 2018-07-05
US20190248743A1 (en) 2019-08-15
US9765028B2 (en) 2017-09-19
JP6338505B2 (ja) 2018-06-06
US20220306580A1 (en) 2022-09-29
JP5651174B2 (ja) 2015-01-07
US11691948B2 (en) 2023-07-04
SG178036A1 (en) 2012-03-29
JP2012533550A (ja) 2012-12-27
CA2765621C (en) 2018-02-13
EP2453894A1 (en) 2012-05-23
CN102470130B (zh) 2013-09-04
PL2987490T3 (pl) 2017-12-29
EP2453894B1 (en) 2015-11-04
SI2453894T1 (sl) 2016-02-29
SG10201407913UA (en) 2015-01-29
JP2017171692A (ja) 2017-09-28
US9415041B2 (en) 2016-08-16
ES2639642T3 (es) 2017-10-27
US20250179019A1 (en) 2025-06-05
AU2010273514A1 (en) 2012-01-19
US20130338191A1 (en) 2013-12-19
US10550081B2 (en) 2020-02-04
HUE026414T2 (hu) 2016-05-30
MX2012000682A (es) 2012-02-28
CN102470130A (zh) 2012-05-23
BR112012000890A2 (pt) 2017-10-31
US8541451B2 (en) 2013-09-24
EP2987490A1 (en) 2016-02-24
DK2453894T3 (en) 2016-01-25
WO2011008809A1 (en) 2011-01-20
EP2987490B1 (en) 2017-06-14
ES2557553T3 (es) 2016-01-27
US11008289B2 (en) 2021-05-18
CA2989129C (en) 2021-03-09

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