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

    • 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

Landscapes

  • 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)
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
CA3182162A1 (en) 2020-05-06 2021-11-11 Les Laboratoires Servier New macrocyclic lrrk2 kinase inhibitors
EP4236950A4 (en) 2020-10-29 2024-10-23 Merck Sharp & Dohme LLC N-LINKED ISOQUINOLINE AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
TW202304935A (zh) 2021-03-18 2023-02-01 法商施維雅藥廠 新穎的巨環lrrk2激酶抑制劑
CN119546607A (zh) * 2022-05-12 2025-02-28 因特来治疗公司 Lrrk2抑制剂
EP4522616A4 (en) * 2022-05-12 2026-04-22 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 (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
KR0182801B1 (ko) 1991-04-16 1999-05-01 아만 히데아키 고체 분산체의 제조방법
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
EP0683234B2 (en) 1993-01-25 2007-06-06 Takeda Chemical Industries, Ltd. Antibody against beta-amyloid or their derivative and use thereof
DE19504832A1 (de) 1995-02-14 1996-08-22 Basf Ag Feste Wirkstoff-Zubereitungen
EP2006303A1 (en) 1997-04-09 2008-12-24 Intellect Neurosciences, Inc. Recombinant antibodies specific for Beta-Amyloid ends, DNA encoding and methods of use thereof
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
ATE364374T1 (de) 1997-08-11 2007-07-15 Pfizer Prod Inc 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
US6905686B1 (en) 1997-12-02 2005-06-14 Neuralab Limited Active immunization for treatment of alzheimer's disease
BRPI0108676B8 (pt) 2000-02-24 2021-05-25 Lilly Co Eli anticorpos humanizados que sequestram peptídeo amilóide beta e seus usos no tratamento de condições caracterizadas por formação de placas amiloides, bem como composição farmacêutica que compreende os referidos anticorpos
WO2002042429A2 (en) 2000-11-03 2002-05-30 Proteotech, Inc. Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from uncaria tomentosa and related plants
JP2005503789A (ja) 2001-08-17 2005-02-10 イーライ・リリー・アンド・カンパニー 抗Ａβ抗体
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
MXPA05003621A (es) 2002-10-09 2005-10-19 Rinat Neuroscience Corp Metodos de tratamiento de la enfermedad de alzheimer usando anticuerpos dirigidos contra el peptido beta amiloide y composiciones de los mismos.
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
MXPA05013770A (es) 2003-06-19 2006-03-08 Pfizer Prod Inc Antagonista de neuroquinina 1.
MY157827A (en) 2003-06-27 2016-07-29 3M Innovative Properties Co Sulfonamide substituted imidazoquinolines
US20070031416A1 (en) 2003-09-09 2007-02-08 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
BRPI0513959A (pt) 2004-07-30 2008-05-20 Rinat Neuroscience Corp anticorpos dirigidos contra o peptìdeo beta-amilóide, suas composições farmacêuticas, kit e métodos de fabricação dos mesmos
WO2006069081A2 (en) 2004-12-22 2006-06-29 Washington University In St. Louis USE OF ANTI-Aβ ANTIBODY TO TREAT TRAUMATIC BRAIN INJURY
PE20061323A1 (es) 2005-04-29 2007-02-09 Rinat Neuroscience Corp Anticuerpos dirigidos contra el peptido amiloide beta y metodos que utilizan los mismos
JP2008543923A (ja) 2005-06-22 2008-12-04 ファイザー・プロダクツ・インク ヒスタミン−３受容体アンタゴニスト
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
EP2124933B1 (en) 2007-01-22 2012-10-17 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
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
EP2903989A1 (en) 2012-10-04 2015-08-12 Pfizer Limited Pyrrolo[2,3-d]pyrimidine tropomyosin-related kinase inhibitors
US10000482B2 (en) * 2012-10-19 2018-06-19 Origenis Gmbh 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
KR102161364B1 (ko) * 2015-09-14 2020-09-29 화이자 인코포레이티드 LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체
JP2019517580A (ja) 2016-06-01 2019-06-24 ハロルド・リチャード・ヘルストロムＨａｒｏｌｄ Ｒｉｃｈａｒｄ ＨＥＬＬＳＴＲＯＭ 副交感神経薬および抗交感神経薬でのドライアイ疾患の処置
EP3592740B1 (en) * 2017-03-10 2022-02-09 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
US20210355117A1 (en) 2021-11-18
EP3592741A1 (en) 2020-01-15
TW201900642A (zh) 2019-01-01
CN111051304B (zh) 2022-12-27
NZ757971A (en) 2024-12-20
AU2018230236B2 (en) 2022-05-19
SG11201908322WA (en) 2019-10-30
IL269214A (en) 2019-11-28
CA3056030A1 (en) 2018-09-13
KR20190138793A (ko) 2019-12-16
BR112019018688A2 (pt) 2020-04-07
IL269214B (en) 2022-03-01
CN111051304A (zh) 2020-04-21
US11312713B2 (en) 2022-04-26
TWI701246B (zh) 2020-08-11
EP3592741B1 (en) 2023-02-15
WO2018163066A1 (en) 2018-09-13
MX2019010756A (es) 2020-01-20
AU2018230236A1 (en) 2019-10-31
RU2019131727A3 (https=) 2021-04-26
JP7219223B2 (ja) 2023-02-07
SG10202110112TA (en) 2021-10-28
JP2020510046A (ja) 2020-04-02
RU2019131727A (ru) 2021-04-12

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
HK40021310A (en) Cyclic substituted imidazo[4,5-c]quinoline derivatives
HK40021310B (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