ES2639642T3 - Formas de base libre cristalina de un compuesto de bifenilo - Google Patents

Formas de base libre cristalina de un compuesto de bifenilo Download PDF

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Publication number
ES2639642T3
ES2639642T3 ES15178848.6T ES15178848T ES2639642T3 ES 2639642 T3 ES2639642 T3 ES 2639642T3 ES 15178848 T ES15178848 T ES 15178848T ES 2639642 T3 ES2639642 T3 ES 2639642T3
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ES
Spain
Prior art keywords
free base
crystalline free
compound
crystalline
values
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES15178848.6T
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English (en)
Spanish (es)
Inventor
Grahame Woollam
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Theravance Biopharma R&D IP LLC
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Publication date
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Application filed by Theravance Biopharma R&D IP LLC filed Critical Theravance Biopharma R&D IP LLC
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Classifications

    • 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
    • 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
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • 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)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ES15178848.6T 2009-07-15 2010-07-14 Formas de base libre cristalina de un compuesto de bifenilo Active ES2639642T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22580309P 2009-07-15 2009-07-15
US225803P 2009-07-15

Publications (1)

Publication Number Publication Date
ES2639642T3 true ES2639642T3 (es) 2017-10-27

Family

ID=42562758

Family Applications (2)

Application Number Title Priority Date Filing Date
ES15178848.6T Active ES2639642T3 (es) 2009-07-15 2010-07-14 Formas de base libre cristalina de un compuesto de bifenilo
ES10732616.7T Active ES2557553T3 (es) 2009-07-15 2010-07-14 Forma de base libre cristalina de un compuesto de bifenilo

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES10732616.7T Active ES2557553T3 (es) 2009-07-15 2010-07-14 Forma de base libre cristalina de un compuesto de bifenilo

Country Status (20)

Country Link
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) ES2639642T3 (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)

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TWI341836B (en) 2004-03-11 2011-05-11 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
EP2987490B1 (en) 2009-07-15 2017-06-14 Theravance Biopharma R&D IP, LLC Crystalline freebase forms of a biphenyl compound
PT2593429E (pt) 2010-07-13 2015-09-24 Theravance Biopharma R & D Ip Llc Processo para preparar um ácido bifenil-2-ilcarbâmico
KR101858913B1 (ko) * 2013-02-21 2018-05-16 화이자 인코포레이티드 고체 형태의 선택적인 cdk4/6 억제제
WO2015070366A1 (en) 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
WO2020047225A1 (en) 2018-08-30 2020-03-05 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
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
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
US20250136550A1 (en) 2023-10-27 2025-05-01 Theravance Biopharma R&D Ip, Llc Processes for preparing revefenacin and compositions comprising the same
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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PT2593429E (pt) 2010-07-13 2015-09-24 Theravance Biopharma R & D Ip Llc Processo para preparar um ácido bifenil-2-ilcarbâmico

Also Published As

Publication number Publication date
SG10201407913UA (en) 2015-01-29
JP2012533550A (ja) 2012-12-27
JP2015003929A (ja) 2015-01-08
US10100013B2 (en) 2018-10-16
KR101742252B1 (ko) 2017-05-31
US11691948B2 (en) 2023-07-04
BR112012000890A2 (pt) 2017-10-31
US9415041B2 (en) 2016-08-16
PL2987490T3 (pl) 2017-12-29
IL216995A (en) 2017-10-31
HK1168050A1 (zh) 2012-12-21
US11649209B2 (en) 2023-05-16
US20200308116A1 (en) 2020-10-01
IL216995A0 (en) 2012-02-29
HRP20151344T1 (hr) 2016-01-01
DK2453894T3 (en) 2016-01-25
PL2453894T3 (pl) 2016-04-29
US20110015163A1 (en) 2011-01-20
AU2010273514A1 (en) 2012-01-19
US9226896B2 (en) 2016-01-05
JP5651174B2 (ja) 2015-01-07
US20220306580A1 (en) 2022-09-29
WO2011008809A1 (en) 2011-01-20
CN102470130A (zh) 2012-05-23
CA2989129A1 (en) 2011-01-20
JP2016026214A (ja) 2016-02-12
CA2765621A1 (en) 2011-01-20
AU2010273514B2 (en) 2015-01-22
MX2012000682A (es) 2012-02-28
HK1219415A1 (en) 2017-04-07
CA2765621C (en) 2018-02-13
US10550081B2 (en) 2020-02-04
JP6338505B2 (ja) 2018-06-06
US8921396B2 (en) 2014-12-30
HUE026414T2 (hu) 2016-05-30
EP2987490B1 (en) 2017-06-14
US20160143897A1 (en) 2016-05-26
US20190248743A1 (en) 2019-08-15
SI2453894T1 (sl) 2016-02-29
SG178036A1 (en) 2012-03-29
US20250179019A1 (en) 2025-06-05
US9765028B2 (en) 2017-09-19
US20150164796A1 (en) 2015-06-18
US20180186740A1 (en) 2018-07-05
US20230303492A1 (en) 2023-09-28
ES2557553T3 (es) 2016-01-27
US11858898B2 (en) 2024-01-02
SMT201600019B (it) 2016-02-25
EP2987490A1 (en) 2016-02-24
EP2453894B1 (en) 2015-11-04
JP2017171692A (ja) 2017-09-28
EP2453894A1 (en) 2012-05-23
CN102470130B (zh) 2013-09-04
US11008289B2 (en) 2021-05-18
CA2989129C (en) 2021-03-09
US20220009890A1 (en) 2022-01-13
US20170081283A1 (en) 2017-03-23
US8541451B2 (en) 2013-09-24
US20130338191A1 (en) 2013-12-19
KR20130027004A (ko) 2013-03-14
PT2453894E (pt) 2016-02-02

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