KR102582626B1 - Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체 - Google Patents

Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체 Download PDF

Info

Publication number
KR102582626B1
KR102582626B1 KR1020197029735A KR20197029735A KR102582626B1 KR 102582626 B1 KR102582626 B1 KR 102582626B1 KR 1020197029735 A KR1020197029735 A KR 1020197029735A KR 20197029735 A KR20197029735 A KR 20197029735A KR 102582626 B1 KR102582626 B1 KR 102582626B1
Authority
KR
South Korea
Prior art keywords
methyl
imidazo
quinoline
chloro
pyran
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
KR1020197029735A
Other languages
English (en)
Korean (ko)
Other versions
KR20190138793A (ko
Inventor
마이클 아론 브로드니
토마스 앨런 채피
진산 마이클 첸
요담 워즈워스 코
카렌 진 코프먼
폴 갈라트시스
미셀 르네 간지
크리스토퍼 존 헬랄
재클린 루이스 헨더슨
베서니 린 코모스
라비 지. 쿠룸바일
루이스 앤젤 마티네즈-알시나
마틴 영진 페테르손
매튜 리처드 리즈
콜린 리처드 로즈
안토니아 프리데리케 스테판
파트리크 로베르트 페르회스트
트래비스 티. 웨이저
조셉 스콧 워머스
유안 장
Original Assignee
화이자 인코포레이티드
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
Publication date
Application filed by 화이자 인코포레이티드 filed Critical 화이자 인코포레이티드
Publication of KR20190138793A publication Critical patent/KR20190138793A/ko
Application granted granted Critical
Publication of KR102582626B1 publication Critical patent/KR102582626B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
KR1020197029735A 2017-03-10 2018-03-06 Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체 Active KR102582626B1 (ko)

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)

Publication Number Publication Date
KR20190138793A KR20190138793A (ko) 2019-12-16
KR102582626B1 true KR102582626B1 (ko) 2023-09-22

Family

ID=61683855

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020197029735A Active KR102582626B1 (ko) 2017-03-10 2018-03-06 Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체

Country Status (13)

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

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112022022511A2 (pt) 2020-05-06 2022-12-13 Servier Lab Inibidores macrocíclicos de lrrk2 quinase
EP4236950A4 (en) 2020-10-29 2024-10-23 Merck Sharp & Dohme LLC N-LINKED ISOQUINOLINE AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
BR112023017834A2 (pt) 2021-03-18 2023-10-03 Servier Lab Inibidores de lrrk2 cinase macrocíclicos
WO2023220238A1 (en) * 2022-05-12 2023-11-16 Interline Therapeutics, Inc. Lrrk2 inhibitors
CN119403801A (zh) * 2022-05-12 2025-02-07 因特来治疗公司 Lrrk2抑制剂
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2011144622A1 (en) 2010-05-17 2011-11-24 Boehringer Ingelheim International Gmbh 1h - imidazo [4, 5 - c] quinolines
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

Family Cites Families (57)

* 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
CA1335996C (en) * 1988-02-16 1995-06-20 Susumu Takada 2-substituted carbonylimidazo¬4,5-c|quinolines
WO1992018106A1 (fr) 1991-04-16 1992-10-29 Nippon Shinyaku Co., Ltd. Procede de production d'une dispersion solide
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
ATE239797T1 (de) 1993-01-25 2003-05-15 Takeda Chemical Industries Ltd Antikörper gegen beta-amyloid oder derivative davon und seine verwendung
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
ES2287971T3 (es) 1997-08-11 2007-12-16 Pfizer Products Inc. Dispersiones farmaceuticas solidas con biodisponibilidad incrementada.
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
US6905686B1 (en) 1997-12-02 2005-06-14 Neuralab Limited Active immunization for treatment of alzheimer's disease
DE1257584T1 (de) 2000-02-24 2003-05-28 Lilly Co Eli Humanisierte antikörper, die amyloid beta peptid demarkieren
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
CA2451998A1 (en) 2001-08-17 2003-02-27 Eli Lilly And Company Anti-a.beta. antibodies
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
US20040146512A1 (en) 2002-10-09 2004-07-29 Arnon Rosenthal Methods of treating Alzheimer's disease using antibodies directed against amyloid beta peptide and compositions thereof
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
BRPI0410630A (pt) 2003-06-19 2006-06-13 Pfizer Prod Inc antagonista de nk1
MY157827A (en) 2003-06-27 2016-07-29 3M Innovative Properties Co Sulfonamide substituted imidazoquinolines
EP1666061A1 (en) 2003-09-09 2006-06-07 Takeda Pharmaceutical Company Limited Use of antibody
AR046845A1 (es) 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
EP1720847A1 (en) 2004-02-02 2006-11-15 Pfizer Products Incorporated Histamine-3 receptor modulators
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
UY29504A1 (es) 2005-04-29 2006-10-31 Rinat Neuroscience Corp Anticuerpos dirigidos contra el péptido amiloide beta y métodos que utilizan los mismos.
DE602006018301D1 (de) 2005-06-22 2010-12-30 Pfizer Prod Inc Histamin-3-rezeptorantagonisten
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
CA2624625A1 (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
WO2007088462A1 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Spirochromane antagonists of the h-3 receptor
WO2007088450A2 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Chromane antagonist 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
CA2643055A1 (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
JP4585610B2 (ja) 2007-01-22 2010-11-24 ファイザー・プロダクツ・インク 治療用化合物のトシル酸塩およびその医薬組成物
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
WO2012028629A1 (en) 2010-09-02 2012-03-08 Glaxo Group Limited 2 - (benzyloxy) benzamides as lrrk2 kinase inhibitors
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
US20150218172A1 (en) 2012-10-04 2015-08-06 Pfizer Limited Pyrrolo[2,3-D]Pyrimidine Tropomyosin-Related Kinase Inhibitors
WO2014060113A1 (en) 2012-10-19 2014-04-24 Origenis Gmbh Novel 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
RU2722149C1 (ru) * 2015-09-14 2020-05-27 Пфайзер Инк. Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2
EP3463344A4 (en) 2016-06-01 2020-02-12 Harold Richard Hellstrom TREATMENT OF DRY EYE WITH PARASYMPATHIC AND ANTISYMPATHIC AGENTS
WO2018163030A1 (en) * 2017-03-10 2018-09-13 Pfizer Inc. Cyclic substituted imidazo[4,5-c]quinoline derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2011144622A1 (en) 2010-05-17 2011-11-24 Boehringer Ingelheim International Gmbh 1h - imidazo [4, 5 - c] quinolines
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

Also Published As

Publication number Publication date
JP2020510046A (ja) 2020-04-02
AU2018230236A1 (en) 2019-10-31
JP7219223B2 (ja) 2023-02-07
CN111051304A (zh) 2020-04-21
EP3592741B1 (en) 2023-02-15
SG11201908322WA (en) 2019-10-30
US20210355117A1 (en) 2021-11-18
BR112019018688A2 (pt) 2020-04-07
NZ757971A (en) 2024-12-20
WO2018163066A1 (en) 2018-09-13
RU2019131727A3 (https=) 2021-04-26
US11312713B2 (en) 2022-04-26
TWI701246B (zh) 2020-08-11
TW201900642A (zh) 2019-01-01
MX2019010756A (es) 2020-01-20
IL269214B (en) 2022-03-01
EP3592741A1 (en) 2020-01-15
AU2018230236B2 (en) 2022-05-19
SG10202110112TA (en) 2021-10-28
RU2019131727A (ru) 2021-04-12
IL269214A (en) 2019-11-28
CA3056030A1 (en) 2018-09-13
CN111051304B (zh) 2022-12-27
KR20190138793A (ko) 2019-12-16

Similar Documents

Publication Publication Date Title
KR102582626B1 (ko) Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체
US10039753B2 (en) Imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives as LRRK2 inhibitors
TWI675826B (zh) 環狀經取代之咪唑并[4,5-c]喹啉衍生物
BR112018015191B1 (pt) Compostos de 6,7-di-hidro-5h-pirazolo[5,1-b][1,3]oxazina-2-carboxamida, seu uso e composição farmacêutica que os compreende
RU2773516C2 (ru) Новые производные имидазо[4,5-с]хинолина в качестве ингибиторов LRRK2
HK40028779B (en) Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors
HK40028779A (en) Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors
HK40021310B (en) Cyclic substituted imidazo[4,5-c]quinoline derivatives
HK40021310A (en) Cyclic substituted imidazo[4,5-c]quinoline derivatives
HK40025037A (en) Cyclic substituted imidazo[4,5-c]quinoline derivatives
HK1258857B (en) Novel imidazo [4,5-c]quinoline and imidazo [4,5-c][1,5]naphthyridine derivatives as lrrk2 inhibitors
HK1204619A1 (en) 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20191010

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20210308

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20230214

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20230825

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20230920

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20230920

End annual number: 3

Start annual number: 1

PG1601 Publication of registration