WO2005000815A3 - Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic m3 receptor - Google Patents

Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic m3 receptor Download PDF

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Publication number
WO2005000815A3
WO2005000815A3 PCT/EP2004/006795 EP2004006795W WO2005000815A3 WO 2005000815 A3 WO2005000815 A3 WO 2005000815A3 EP 2004006795 W EP2004006795 W EP 2004006795W WO 2005000815 A3 WO2005000815 A3 WO 2005000815A3
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WO
WIPO (PCT)
Prior art keywords
muscarinic
receptor
piperidinium
ligands
compounds
Prior art date
Application number
PCT/EP2004/006795
Other languages
French (fr)
Other versions
WO2005000815A2 (en
Inventor
Stephen Paul Collingwood
Urs Baettig
Clive Mccarthy
Original Assignee
Novartis Ag
Novartis Pharma Gmbh
Stephen Paul Collingwood
Urs Baettig
Clive Mccarthy
Priority date (The priority date 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 date listed.)
Filing date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33554160&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2005000815(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0314697A external-priority patent/GB0314697D0/en
Priority claimed from GB0327526A external-priority patent/GB0327526D0/en
Priority to JP2006516038A priority Critical patent/JP2008529965A/en
Priority to MXPA05013823A priority patent/MXPA05013823A/en
Priority to CA2526991A priority patent/CA2526991C/en
Priority to EP04740214A priority patent/EP1638940B1/en
Priority to AU2004251867A priority patent/AU2004251867B2/en
Application filed by Novartis Ag, Novartis Pharma Gmbh, Stephen Paul Collingwood, Urs Baettig, Clive Mccarthy filed Critical Novartis Ag
Priority to AT04740214T priority patent/ATE478845T1/en
Priority to CN200480016629.XA priority patent/CN1805935B/en
Priority to US10/561,366 priority patent/US7947730B2/en
Priority to DE602004028821T priority patent/DE602004028821D1/en
Priority to BRPI0411738-7A priority patent/BRPI0411738A/en
Priority to PL04740214T priority patent/PL1638940T3/en
Publication of WO2005000815A2 publication Critical patent/WO2005000815A2/en
Publication of WO2005000815A3 publication Critical patent/WO2005000815A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/08Heterocyclic 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
    • 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
    • A61P11/02Nasal agents, e.g. decongestants
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • C07D211/08Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compounds of formula (I) in salt or zwitterionic form wherein, wherein R1, R2, R3, R4, R5, J, L and M have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
PCT/EP2004/006795 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic m3 receptor WO2005000815A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
DE602004028821T DE602004028821D1 (en) 2003-06-24 2004-06-23 PYRROLIDINIUM DERIVATIVES AS LIGANDS FOR THE MUSCARIN M3 RECEPTOR
BRPI0411738-7A BRPI0411738A (en) 2003-06-24 2004-06-23 organic compounds
PL04740214T PL1638940T3 (en) 2003-06-24 2004-06-23 Pyrrolidinium derivatives as ligands for the muscarinic m3 receptor
CN200480016629.XA CN1805935B (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic M3 receptor
CA2526991A CA2526991C (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic m3 receptor
EP04740214A EP1638940B1 (en) 2003-06-24 2004-06-23 Pyrrolidinium derivatives as ligands for the muscarinic m3 receptor
AU2004251867A AU2004251867B2 (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic M3 receptor
JP2006516038A JP2008529965A (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for muscarinic M3 receptors
AT04740214T ATE478845T1 (en) 2003-06-24 2004-06-23 PYRROLIDINIUM DERIVATIVES AS LIGANDS FOR THE MUSCARINE M3 RECEPTOR
MXPA05013823A MXPA05013823A (en) 2003-06-24 2004-06-23 Organic compounds.
US10/561,366 US7947730B2 (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic M3 receptor

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0314697A GB0314697D0 (en) 2003-06-24 2003-06-24 Organic compounds
GB0314697.4 2003-06-24
GB0327526.0 2003-11-26
GB0327526A GB0327526D0 (en) 2003-11-26 2003-11-26 Organic compounds

Publications (2)

Publication Number Publication Date
WO2005000815A2 WO2005000815A2 (en) 2005-01-06
WO2005000815A3 true WO2005000815A3 (en) 2005-04-14

Family

ID=33554160

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/006795 WO2005000815A2 (en) 2003-06-24 2004-06-23 Piperidinium and pyrrolidinium derivatives as ligands for the muscarinic m3 receptor

Country Status (15)

Country Link
US (1) US7947730B2 (en)
EP (1) EP1638940B1 (en)
JP (1) JP2008529965A (en)
AR (1) AR044851A1 (en)
AT (1) ATE478845T1 (en)
AU (1) AU2004251867B2 (en)
BR (1) BRPI0411738A (en)
CA (1) CA2526991C (en)
DE (1) DE602004028821D1 (en)
MX (1) MXPA05013823A (en)
PE (1) PE20050231A1 (en)
PL (1) PL1638940T3 (en)
PT (1) PT1638940E (en)
TW (1) TW200526573A (en)
WO (1) WO2005000815A2 (en)

Families Citing this family (17)

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GB0410712D0 (en) 2004-05-13 2004-06-16 Novartis Ag Organic compounds
GB0428416D0 (en) 2004-12-24 2005-02-02 Novartis Ag Organic compounds
GB0428418D0 (en) * 2004-12-24 2005-02-02 Novartis Ag Organic compounds
ATE529400T1 (en) * 2005-11-10 2011-11-15 Nicholas S Bodor SOFT ANTICHOLINERGIC ZWITTERIONS
ATE529399T1 (en) * 2005-11-10 2011-11-15 Nicholas S Bodor GENTLE ANTICHOLINER ESTERS
JP2009519310A (en) * 2005-12-16 2009-05-14 アージェンタ ディスカバリー リミテッド Cyclic amine derivatives and their use
US20090233965A1 (en) * 2006-04-24 2009-09-17 Astrazeneca Ab Alkyl Esters Of Cyclic Amino Alcohols With Muscarinic M3 Receptor Antagonist Activity, Useful For Treating E.G. Chronic Bronchial Obstruction, Asthma And Overactive Bladder
TW200825084A (en) 2006-11-14 2008-06-16 Astrazeneca Ab New compounds 521
WO2008076269A2 (en) * 2006-12-13 2008-06-26 Gilead Sciences, Inc. MONOPHOSPHATES AS MUTUAL PRODRUGS OF MUSCARINIC RECEPTOR ANTAGONISTS AND β-AGONISTS FOR THE TREATMENT OF COPD AND CHRONIC BRONCHITIS
BRPI0807615A8 (en) * 2007-02-23 2017-12-05 Theravance Inc QUATERNARY AMMONIUM DIPHENYLMETHYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
CA2697752C (en) 2007-09-07 2016-01-26 Theravance, Inc. Guanidine-containing compounds useful as muscarinic receptor antagonists
EP2222637A1 (en) 2007-12-14 2010-09-01 Theravance, Inc. Amidine-containing compounds useful as muscarinic receptor antagonists
CN102089304A (en) 2008-05-13 2011-06-08 阿斯利康(瑞典)有限公司 Quinuclidine derivatives as muscarinic M3 receptor antagonists
AU2010242646A1 (en) * 2009-04-30 2011-11-03 Teijin Pharma Limited Quaternary ammonium salt compound
US9156833B2 (en) 2012-07-16 2015-10-13 Barry University, Inc. Bitopic muscarinic agonists and antagonists and methods of synthesis and use thereof
PL3111978T3 (en) 2015-07-03 2022-01-24 Novartis Ag Inhaler adapted to read information stored in a data storage means of a container
CN115279731A (en) * 2020-03-11 2022-11-01 诺西恩医疗公司 Charged ion channel blockers and methods of use thereof

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JPS5427570A (en) * 1977-07-30 1979-03-01 Ota Pharma Stereoisomer of 44acyloxyy11 alkyll11*1*33dioxolanee44 ylmethyl* pideridinium salt derivative
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WO2003087094A2 (en) * 2002-04-16 2003-10-23 Almirall Prodesfarma Ag Pyrrolidinium derivatives as antagonists of m3 muscarinic receptors

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JPS5427570A (en) * 1977-07-30 1979-03-01 Ota Pharma Stereoisomer of 44acyloxyy11 alkyll11*1*33dioxolanee44 ylmethyl* pideridinium salt derivative
JPS5679688A (en) * 1979-12-04 1981-06-30 Ota Seiyaku Kk 4-acyloxy-1- 1,3-dioxoran-2-ylmethyl piperidine derivative and its production
EP0073645A2 (en) * 1981-08-26 1983-03-09 Dainippon Pharmaceutical Co., Ltd. 2-Cyclic amino-2-(1,2-benzisoxazol-3-yl)acetic acid ester derivatives, process for the preparation thereof and composition containing the same
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EP1302458A1 (en) * 2000-07-11 2003-04-16 Banyu Pharmaceutical Co., Ltd. Ester derivatives
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Also Published As

Publication number Publication date
EP1638940B1 (en) 2010-08-25
AU2004251867A1 (en) 2005-01-06
MXPA05013823A (en) 2006-02-28
ATE478845T1 (en) 2010-09-15
CA2526991C (en) 2012-03-27
CA2526991A1 (en) 2005-01-06
BRPI0411738A (en) 2006-08-08
PT1638940E (en) 2010-11-08
DE602004028821D1 (en) 2010-10-07
PL1638940T3 (en) 2011-02-28
AR044851A1 (en) 2005-10-05
AU2004251867B2 (en) 2008-08-07
WO2005000815A2 (en) 2005-01-06
US20060287362A1 (en) 2006-12-21
EP1638940A2 (en) 2006-03-29
PE20050231A1 (en) 2005-05-20
TW200526573A (en) 2005-08-16
US7947730B2 (en) 2011-05-24
JP2008529965A (en) 2008-08-07

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