AU2018230236B2 - Novel imidazo[4,5-c]quinoline derivatives as LRRK2 inhibitors - Google Patents

Novel imidazo[4,5-c]quinoline derivatives as LRRK2 inhibitors Download PDF

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Publication number
AU2018230236B2
AU2018230236B2 AU2018230236A AU2018230236A AU2018230236B2 AU 2018230236 B2 AU2018230236 B2 AU 2018230236B2 AU 2018230236 A AU2018230236 A AU 2018230236A AU 2018230236 A AU2018230236 A AU 2018230236A AU 2018230236 B2 AU2018230236 B2 AU 2018230236B2
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Prior art keywords
methyl
imidazo
quinoline
chloro
pyran
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AU2018230236A1 (en
Inventor
Michael Aaron Brodney
Thomas Allen Chappie
Jinshan Michael Chen
Jotham Wadsworth Coe
Karen Jean Coffman
Paul Galatsis
Michelle Renee GARNSEY
Christopher John Helal
Jaclyn Louise HENDERSON
Bethany Lyn KORMOS
Ravi G. Kurumbail
Luis Angel MARTINEZ-ALSINA
Martin Youngjin Pettersson
Matthew Richard Reese
Colin Richard ROSE
Antonia Friederike STEPAN
Patrick Robert Verhoest
Travis T. Wager
Joseph Scott Warmus
Yuan Zhang
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Pfizer Corp SRL
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Pfizer Corp Belgium
Pfizer Corp SRL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2018230236A 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as LRRK2 inhibitors Active AU2018230236B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762469756P 2017-03-10 2017-03-10
US62/469,756 2017-03-10
US201862629152P 2018-02-12 2018-02-12
US62/629,152 2018-02-12
PCT/IB2018/051439 WO2018163066A1 (en) 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors

Publications (2)

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AU2018230236A1 AU2018230236A1 (en) 2019-10-31
AU2018230236B2 true AU2018230236B2 (en) 2022-05-19

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AU2018230236A Active AU2018230236B2 (en) 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as LRRK2 inhibitors

Country Status (13)

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US (1) US11312713B2 (OSRAM)
EP (1) EP3592741B1 (OSRAM)
JP (1) JP7219223B2 (OSRAM)
KR (1) KR102582626B1 (OSRAM)
CN (1) CN111051304B (OSRAM)
AU (1) AU2018230236B2 (OSRAM)
BR (1) BR112019018688A2 (OSRAM)
CA (1) CA3056030A1 (OSRAM)
IL (1) IL269214B (OSRAM)
MX (1) MX2019010756A (OSRAM)
SG (2) SG11201908322WA (OSRAM)
TW (1) TWI701246B (OSRAM)
WO (1) WO2018163066A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021224320A1 (en) 2020-05-06 2021-11-11 Les Laboratoires Servier New macrocyclic lrrk2 kinase inhibitors
EP4308570A1 (en) 2021-03-18 2024-01-24 Les Laboratoires Servier Macrocyclic lrrk2 kinase inhibitors
JP2025517688A (ja) * 2022-05-12 2025-06-10 インターライン セラピューティクス インコーポレイティド Ｌｒｒｋ２阻害剤
WO2023220247A1 (en) * 2022-05-12 2023-11-16 Interline Therapeutics, Inc. Lrrk2 inhibitors
CN115728413A (zh) * 2022-11-09 2023-03-03 内蒙古帕默康创医疗仪器有限公司 舍曲林血药浓度的定量分析方法
CN116879450A (zh) * 2023-07-25 2023-10-13 江苏汉邦科技股份有限公司 一种利用超临界流体色谱系统分离纯化芦可替尼前体的方法
CN118440041B (zh) * 2024-07-02 2024-09-27 苏州凯瑞医药科技有限公司 一种手性4-氨基-3-羟基四氢吡喃的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0329073A2 (en) * 1988-02-16 1989-08-23 Shionogi & Co., Ltd. 2-Substituted carbonylimidazo[4,5-c]quinolines
WO2005054238A1 (en) * 2003-11-21 2005-06-16 Novartis Ag 1h-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
WO2014060113A1 (en) * 2012-10-19 2014-04-24 Origenis Gmbh Novel kinase inhibitors
WO2017046675A1 (en) * 2015-09-14 2017-03-23 Pfizer Inc. Novel imidazo [4,5-c] quinoline and imidazo [4,5-c][1,5] naphthyridine derivatives as lrrk2 inhibitors

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1146866A (en) 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
IL73534A (en) * 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
DE3438830A1 (de) 1984-10-23 1986-04-30 Rentschler Arzneimittel Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung
US5389640A (en) * 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
DE69222847T3 (de) 1991-04-16 2005-09-15 Nippon Shinyaku Co., Ltd. Verfahren zur herstellung einer festen dispersion
US5340591A (en) 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
JP3265680B2 (ja) 1992-03-12 2002-03-11 大正製薬株式会社 経口製剤用組成物
WO1994017197A1 (fr) 1993-01-25 1994-08-04 Takeda Chemical Industries, Ltd. ANTICORPS DIRIGE CONTRE LE β-AMYLOIDE OU UN DERIVE DE CE DERNIER ET SON UTILISATION
DE19504832A1 (de) 1995-02-14 1996-08-22 Basf Ag Feste Wirkstoff-Zubereitungen
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
NZ337765A (en) 1997-04-09 2001-09-28 Mindset Biopharmaceuticals Usa Recombinant antibodies having specificity for beta-amyloid N-terminus and C-terminus and use in treating Alzheimer's Disease
DE69837903T2 (de) 1997-08-11 2008-02-14 Pfizer Products Inc., Groton Feste pharmazeutische Dispersionen mit erhöhter Bioverfügbarkeit
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
US6743427B1 (en) 1997-12-02 2004-06-01 Neuralab Limited Prevention and treatment of amyloidogenic disease
SI1257584T2 (sl) 2000-02-24 2013-07-31 Washington University St. Louis Humanizirana protitelesa, ki veĹľejo amiloidni peptid beta
CA2427661C (en) 2000-11-03 2013-05-28 Proteotech, Inc. Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from uncaria tomentosa and related plants
US20040192898A1 (en) 2001-08-17 2004-09-30 Jia Audrey Yunhua Anti-abeta antibodies
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
BR0315157A (pt) 2002-10-09 2005-08-09 Rinat Neuroscience Corp Métodos de tratar doença de alzheimer empregando-se anticorpos direcionados contra peptìdeo beta amilóide e composições deste
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
EP1638935A1 (en) 2003-06-19 2006-03-29 Pfizer Products Inc. Nk1 antagonist
MY157827A (en) 2003-06-27 2016-07-29 3M Innovative Properties Co Sulfonamide substituted imidazoquinolines
CA2538220A1 (en) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited Use of antibody
BRPI0507374A (pt) 2004-02-02 2007-07-10 Pfizer Prod Inc moduladores do receptor de histamina-3
US7456164B2 (en) 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
EP1595881A1 (en) 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
MX2007000998A (es) 2004-07-30 2007-07-11 Rinat Neuroscience Corp Anticuerpos dirigidos peptido beta-amiloide y procedimientos que usan los mismos.
US20090074775A1 (en) 2004-12-22 2009-03-19 David Michael Holtzman Use Of Anti-AB Antibody To Treat Traumatic Brain Injury
MY148086A (en) 2005-04-29 2013-02-28 Rinat Neuroscience Corp Antibodies directed against amyloid-beta peptide and methods using same
US7812040B2 (en) 2005-06-22 2010-10-12 Pfizer Inc. Histamine-3 receptor antagonists
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
WO2007052124A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
WO2007063385A2 (en) 2005-12-01 2007-06-07 Pfizer Products Inc. Spirocyclic amine histamine-3 receptor antagonists
WO2007069053A1 (en) 2005-12-14 2007-06-21 Pfizer Products Inc. Benzimidazole antagonists of the h-3 receptor
WO2007088450A2 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Chromane antagonist of the h-3 receptor
WO2007088462A1 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Spirochromane antagonists of the h-3 receptor
WO2007099423A1 (en) 2006-03-02 2007-09-07 Pfizer Products Inc. 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists
WO2007105053A2 (en) 2006-03-13 2007-09-20 Pfizer Products Inc. Tetralines antagonists of the h-3 receptor
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
CA2676456C (en) 2007-01-22 2012-03-27 Pfizer Products Inc. Tosylate salt of a therapeutic compound and pharmaceutical compositions thereof
ITMI20070890A1 (it) 2007-05-04 2008-11-05 Sifi Spa Composizioni oftalmiche per il trattamento della ipertensione oculare e del glaucoma
GB201008134D0 (en) 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
EP2571877B1 (en) * 2010-05-17 2018-08-15 Boehringer Ingelheim International GmbH 1h-imidazo[4,5-c]quinolines
ES2524892T3 (es) 2010-09-02 2014-12-15 Glaxosmithkline Intellectual Property Development Limited 2-(Benciloxi)benzamidas como inhibidores de LRRK2 quinasa
US9233977B2 (en) 2010-10-29 2016-01-12 Merck Sharp & Dohme Corp. Leucine-rich repeat kinase enzyme activity
EP2462921A1 (en) 2010-11-11 2012-06-13 Novaliq GmbH Liquid pharmaceutical compositions for the treatment of a posterior eye disease
WO2013007768A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
CA2885253A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[2,3-d]pyrimidine tropomyosin-related kinase inhibitors
ITTO20130694A1 (it) * 2013-08-14 2015-02-15 Umbra Meccanotecnica Giunto washpipe per un impianto di perforazione petrolifera
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
WO2016009297A1 (en) 2014-07-18 2016-01-21 Pfizer Inc. Pyridine derivatives as muscarinic m1 receptor positive allosteric modulators
WO2016108130A1 (en) 2014-12-30 2016-07-07 Sun Pharmaceutical Industries Limited Topical pharmaceutical compositions comprising nebivolol for the treatment of diabetic wounds
CA3026053A1 (en) 2016-06-01 2017-12-07 Harold Richard Hellstrom Treatment of dry eye disease with parasympathetic and anti-sympathetic agents
IL269215B (en) * 2017-03-10 2022-09-01 Pfizer Disubstituted imidazole[4,5-c]quinoline derivatives

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0329073A2 (en) * 1988-02-16 1989-08-23 Shionogi & Co., Ltd. 2-Substituted carbonylimidazo[4,5-c]quinolines
WO2005054238A1 (en) * 2003-11-21 2005-06-16 Novartis Ag 1h-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
WO2014060113A1 (en) * 2012-10-19 2014-04-24 Origenis Gmbh Novel kinase inhibitors
WO2017046675A1 (en) * 2015-09-14 2017-03-23 Pfizer Inc. Novel imidazo [4,5-c] quinoline and imidazo [4,5-c][1,5] naphthyridine derivatives as lrrk2 inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Journal of Medicinal Chemistry, 1996, 39(14), 2844-51 *

Also Published As

Publication number Publication date
JP7219223B2 (ja) 2023-02-07
TWI701246B (zh) 2020-08-11
IL269214B (en) 2022-03-01
CN111051304A (zh) 2020-04-21
CN111051304B (zh) 2022-12-27
RU2019131727A (ru) 2021-04-12
MX2019010756A (es) 2020-01-20
SG11201908322WA (en) 2019-10-30
EP3592741B1 (en) 2023-02-15
KR20190138793A (ko) 2019-12-16
BR112019018688A2 (pt) 2020-04-07
KR102582626B1 (ko) 2023-09-22
WO2018163066A1 (en) 2018-09-13
IL269214A (en) 2019-11-28
AU2018230236A1 (en) 2019-10-31
RU2019131727A3 (OSRAM) 2021-04-26
NZ757971A (en) 2024-12-20
US20210355117A1 (en) 2021-11-18
TW201900642A (zh) 2019-01-01
JP2020510046A (ja) 2020-04-02
US11312713B2 (en) 2022-04-26
EP3592741A1 (en) 2020-01-15
CA3056030A1 (en) 2018-09-13
SG10202110112TA (en) 2021-10-28

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