AU2011276416B2 - Crystalline form of a 3-phenoxymethylpyrrolidine compound - Google Patents

Crystalline form of a 3-phenoxymethylpyrrolidine compound Download PDF

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Publication number
AU2011276416B2
AU2011276416B2 AU2011276416A AU2011276416A AU2011276416B2 AU 2011276416 B2 AU2011276416 B2 AU 2011276416B2 AU 2011276416 A AU2011276416 A AU 2011276416A AU 2011276416 A AU2011276416 A AU 2011276416A AU 2011276416 B2 AU2011276416 B2 AU 2011276416B2
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Prior art keywords
disorder
pain
compound according
compound
crystalline
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Ceased
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AU2011276416A
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AU2011276416A1 (en
Inventor
Miroslav Rapta
Daisuke Roland Saito
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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Publication of AU2011276416A1 publication Critical patent/AU2011276416A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Psychology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2011276416A 2010-07-09 2011-06-30 Crystalline form of a 3-phenoxymethylpyrrolidine compound Ceased AU2011276416B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36277310P 2010-07-09 2010-07-09
US61/362,773 2010-07-09
PCT/US2011/042518 WO2012006205A1 (en) 2010-07-09 2011-06-30 Crystalline form of a 3-phenoxymethylpyrrolidine compound

Publications (2)

Publication Number Publication Date
AU2011276416A1 AU2011276416A1 (en) 2013-02-14
AU2011276416B2 true AU2011276416B2 (en) 2015-04-02

Family

ID=44510052

Family Applications (1)

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AU2011276416A Ceased AU2011276416B2 (en) 2010-07-09 2011-06-30 Crystalline form of a 3-phenoxymethylpyrrolidine compound

Country Status (20)

Country Link
US (4) US8163794B2 (enExample)
EP (1) EP2590941A1 (enExample)
JP (2) JP5823512B2 (enExample)
KR (1) KR20130041916A (enExample)
CN (1) CN103038211B (enExample)
AR (1) AR083512A1 (enExample)
AU (1) AU2011276416B2 (enExample)
BR (1) BR112013000602A2 (enExample)
CA (1) CA2803090A1 (enExample)
CL (1) CL2013000085A1 (enExample)
CO (1) CO6680604A2 (enExample)
IL (1) IL223584A0 (enExample)
MX (1) MX2013000334A (enExample)
NZ (1) NZ605490A (enExample)
PH (1) PH12013500051A1 (enExample)
RU (1) RU2013105479A (enExample)
SG (1) SG186789A1 (enExample)
TW (1) TW201206882A (enExample)
WO (1) WO2012006205A1 (enExample)
ZA (1) ZA201300154B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010273645B2 (en) * 2009-07-13 2014-12-04 Theravance Biopharma R&D Ip, Llc 3-phenoxymethylpyrrolidine compounds
CN103038211B (zh) * 2010-07-09 2015-04-15 施万生物制药研发Ip有限责任公司 3-苯氧基甲基吡咯烷化合物的结晶形式
US12369722B2 (en) 2018-05-23 2025-07-29 L&P Property Management Company Method of disassembling pocketed spring assembly with dimensionally stabilizing substrate
US11013340B2 (en) 2018-05-23 2021-05-25 L&P Property Management Company Pocketed spring assembly having dimensionally stabilizing substrate

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008023258A1 (en) * 2006-08-23 2008-02-28 Pfizer Products Inc. Piperidine derivatives
WO2010011811A2 (en) * 2008-07-24 2010-01-28 Theravance, Inc. 3-(phenoxyphenylmethyl)pyrrolidine compounds
WO2011008666A2 (en) * 2009-07-13 2011-01-20 Theravance, Inc. 3-phenoxymethylpyrrolidine compounds

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
EP1184372B1 (en) * 2000-08-31 2006-04-26 Pfizer Limited Phenoxyphenylheterocycle derivatives as selective serotonin reuptake inhibitors (SSRIs)
WO2005092835A1 (en) * 2004-03-05 2005-10-06 Eli Lilly And Company Pharmaceutical compounds
CA2687721A1 (en) * 2007-06-08 2008-12-18 Arena Pharmaceuticals, Inc. Crystalline forms of (r)-1-{2-[4'-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and compositions, and methods related thereto
EP2419405A1 (en) * 2009-04-15 2012-02-22 Theravance, Inc. 3-(phenoxypyrrolidin-3-yl-methyl)heteroaryl, 3-(phenylpyrrolidin-3-ylmethoxy)heteroaryl, and 3-(heteroarylpyrrolidin-3-ylmethoxy)heteroaryl compounds
CN103038211B (zh) * 2010-07-09 2015-04-15 施万生物制药研发Ip有限责任公司 3-苯氧基甲基吡咯烷化合物的结晶形式

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008023258A1 (en) * 2006-08-23 2008-02-28 Pfizer Products Inc. Piperidine derivatives
WO2010011811A2 (en) * 2008-07-24 2010-01-28 Theravance, Inc. 3-(phenoxyphenylmethyl)pyrrolidine compounds
WO2011008666A2 (en) * 2009-07-13 2011-01-20 Theravance, Inc. 3-phenoxymethylpyrrolidine compounds

Also Published As

Publication number Publication date
AU2011276416A1 (en) 2013-02-14
US9120746B2 (en) 2015-09-01
EP2590941A1 (en) 2013-05-15
KR20130041916A (ko) 2013-04-25
IL223584A0 (en) 2013-03-05
US8791151B2 (en) 2014-07-29
TW201206882A (en) 2012-02-16
US20150080450A1 (en) 2015-03-19
CA2803090A1 (en) 2012-01-12
CN103038211A (zh) 2013-04-10
NZ605490A (en) 2014-10-31
MX2013000334A (es) 2013-02-26
US8163794B2 (en) 2012-04-24
US20120010265A1 (en) 2012-01-12
AR083512A1 (es) 2013-03-06
CN103038211B (zh) 2015-04-15
CO6680604A2 (es) 2013-05-31
US8383669B2 (en) 2013-02-26
ZA201300154B (en) 2013-09-25
WO2012006205A1 (en) 2012-01-12
JP5823512B2 (ja) 2015-11-25
SG186789A1 (en) 2013-02-28
JP2013532170A (ja) 2013-08-15
PH12013500051A1 (en) 2017-10-25
JP2015120752A (ja) 2015-07-02
RU2013105479A (ru) 2014-08-20
US20120178790A1 (en) 2012-07-12
US20140018407A1 (en) 2014-01-16
CL2013000085A1 (es) 2013-03-15
BR112013000602A2 (pt) 2016-07-05

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Owner name: THERAVANCE BIOPHARMA R&D IP, LLC

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired