SG11201908322WA - Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors - Google Patents

Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors

Info

Publication number
SG11201908322WA
SG11201908322WA SG11201908322WA SG11201908322WA SG 11201908322W A SG11201908322W A SG 11201908322WA SG 11201908322W A SG11201908322W A SG 11201908322WA SG 11201908322W A SG11201908322W A SG 11201908322WA
Authority
SG
Singapore
Prior art keywords
connecticut
massachusetts
international
street
road
Prior art date
Application number
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
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of SG11201908322WA publication Critical patent/SG11201908322WA/en

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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)

Abstract

International Patent Classification: CO7D 471/04 (2006.01) A61P 25/16 (2006.01) CO7D 519/00 (2006.01) A61P 25/28 (2006.01) A61K 31/437 (2006.01) A61P 25/18 (2006.01) (21) International Application Number: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 13 September 2018 (13.09.2018) WIPO I PCT ~~ll~~~~~~~~ 011101010VIIIOH olo omio111111111flo ow (10) International Publication Number WO 2018/163066 Al PCT/IB2018/051439 (22) International Filing Date: 06 March 2018 (06.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/469,756 10 March 2017 (10.03.2017) US 62/629,152 12 February 2018 (12.02.2018) US (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (72) Inventors: BRODNEY, Michael Aaron; 100 Upland Av- enue, Newton, Massachusetts 02461 (US). CHAPPIE, Thomas Allen; 59 Hemlock Hill Road, Carlisle, Massachu- setts 01741 (US). CHEN, Jinshan Michael; 39 Governors Way, Madison, Connecticut 06443 (US). COE, Jotham Wadsworth; 8 Bush Hill Drive, Niantic, Connecticut 06357 (US). COFFMAN, Karen Jean; 3 Clarence Ave., Paw- catuck, Connecticut 06379 (US). GALATSIS, Paul; 375 Cherry Street, Newton, Massachusetts 02465 (US). GAR- NSEY, Michelle Renee; 386 Morris Ave., Providence, Rhode Island 02906 (US). HELAL, Christopher John; 18 Elm Street, Mystic, Connecticut 06355 (US). HEN- DERSON, Jaclyn Louise; 36 Highland Avenue, Apt. 54, Cambridge, Massachusetts 02139 (US). KORMOS, Bethany Lyn; 46 Quincy Street, #3, Somerville, Massa- chusetts 02143 (US). KURUMBAIL, Ravi G.; 4 Harvest Glen, East Lyme, Connecticut 06333 (US). MARTINEZ- Declarations under Rule 4.17: ALSINA, Luis Angel; 58 Eagle Ridge Drive, Gales Ferry, Connecticut 06335 (US). PETTERSSON, Mar- tin Youngjin; 3 Gilson Road, Littleton, Massachusetts 01460 (US). REESE, Matthew Richard; 25 Ocean View Avenue, Mystic, Connecticut 06355 (US). ROSE, Colin Richard; 35 B Lower Bartlett Road, Quaker Hill, Connecti- cut 06375 (US). STEPAN, Antonia Friederike; Rotdorn- weg 8, 88400 Biberach An Der Riss (DE). VERHOEST, Patrick Robert; 23 Calvin Road, Newton, Massachusetts 02460 (US). WAGER, Travis T.; 465 Washington Street, Apt. 6, Brookline, Massachusetts 02446 (US). WARMUS, Joseph Scott; 18 Sable Drive, Ledyard, Connecticut 06339 (US). ZHANG, Yuan; 12103 Maple Tree Lane, East Lyme, Connecticut 06333 (US). (74) Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd Street, MS 235/9/S20, New York, New York 10017 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) W O 20 18/ 163066 Al (54) Title: NOVEL IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS (57) : The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R 1 , R 2 and R 3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's dis- ease or Alzheimer's disease, cancer, Crohn's disease or leprosy. (I) [Continued on next page] WO 2018/163066 Al MIDEDIMOMMIDIIMEIEWHIDIENIEMIEMOVOIS Published: with international search report (Art. 21(3)) in black and white; the international application as filed contained color or greyscale and is available for download from PATENTSCOPE
SG11201908322W 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors SG11201908322WA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762469756P 2017-03-10 2017-03-10
US201862629152P 2018-02-12 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 (1)

Publication Number Publication Date
SG11201908322WA true SG11201908322WA (en) 2019-10-30

Family

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Family Applications (2)

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SG11201908322W SG11201908322WA (en) 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors
SG10202110112T SG10202110112TA (en) 2017-03-10 2018-03-06 Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors

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Country Status (13)

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

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BR112022022511A2 (en) 2020-05-06 2022-12-13 Servier Lab MACROCYCLIC LRRK2 KINASE INHIBITORS
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WO2023220247A1 (en) * 2022-05-12 2023-11-16 Interline Therapeutics, Inc. Lrrk2 inhibitors
WO2023220238A1 (en) * 2022-05-12 2023-11-16 Interline Therapeutics, Inc. Lrrk2 inhibitors
CN115728413A (en) * 2022-11-09 2023-03-03 内蒙古帕默康创医疗仪器有限公司 Quantitative analysis method for blood concentration of sertraline
CN116879450A (en) * 2023-07-25 2023-10-13 江苏汉邦科技股份有限公司 Method for separating and purifying reed-keatinib precursor by using supercritical fluid chromatography system
CN118440041B (en) * 2024-07-02 2024-09-27 苏州凯瑞医药科技有限公司 Preparation method of chiral 4-amino-3-hydroxytetrahydropyran

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Also Published As

Publication number Publication date
US11312713B2 (en) 2022-04-26
CN111051304A (en) 2020-04-21
AU2018230236B2 (en) 2022-05-19
JP7219223B2 (en) 2023-02-07
CA3056030A1 (en) 2018-09-13
IL269214A (en) 2019-11-28
KR102582626B1 (en) 2023-09-22
CN111051304B (en) 2022-12-27
US20210355117A1 (en) 2021-11-18
KR20190138793A (en) 2019-12-16
RU2019131727A3 (en) 2021-04-26
EP3592741B1 (en) 2023-02-15
RU2019131727A (en) 2021-04-12
EP3592741A1 (en) 2020-01-15
MX2019010756A (en) 2020-01-20
SG10202110112TA (en) 2021-10-28
TW201900642A (en) 2019-01-01
JP2020510046A (en) 2020-04-02
BR112019018688A2 (en) 2020-04-07
IL269214B (en) 2022-03-01
AU2018230236A1 (en) 2019-10-31
TWI701246B (en) 2020-08-11
WO2018163066A1 (en) 2018-09-13

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