CN111448193B - Srpk1抑制剂 - Google Patents

Srpk1抑制剂 Download PDF

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Publication number
CN111448193B
CN111448193B CN201880075104.5A CN201880075104A CN111448193B CN 111448193 B CN111448193 B CN 111448193B CN 201880075104 A CN201880075104 A CN 201880075104A CN 111448193 B CN111448193 B CN 111448193B
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CN
China
Prior art keywords
methyl
compound
phenyl
cyclopropyl
hydrogen
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
CN201880075104.5A
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English (en)
Chinese (zh)
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CN111448193A (zh
Inventor
安德鲁·道格拉斯·巴克斯特
J·莫里斯
安德鲁·大卫·莫利
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exonate Ltd
Original Assignee
Exonate Ltd
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
Priority claimed from GBGB1715637.3A external-priority patent/GB201715637D0/en
Priority claimed from GBGB1810765.6A external-priority patent/GB201810765D0/en
Application filed by Exonate Ltd filed Critical Exonate Ltd
Publication of CN111448193A publication Critical patent/CN111448193A/zh
Application granted granted Critical
Publication of CN111448193B publication Critical patent/CN111448193B/zh
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    • 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880075104.5A 2017-09-27 2018-09-26 Srpk1抑制剂 Active CN111448193B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1715637.3A GB201715637D0 (en) 2017-09-27 2017-09-27 SRPK1 Inhibitors
GB1715637.3 2017-09-27
GB1810765.6 2018-06-29
GBGB1810765.6A GB201810765D0 (en) 2018-06-29 2018-06-29 SRPK1 inhibitors
PCT/GB2018/052735 WO2019063996A1 (en) 2017-09-27 2018-09-26 INHIBITORS OF SRPK1

Publications (2)

Publication Number Publication Date
CN111448193A CN111448193A (zh) 2020-07-24
CN111448193B true CN111448193B (zh) 2023-12-22

Family

ID=63722692

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880075104.5A Active CN111448193B (zh) 2017-09-27 2018-09-26 Srpk1抑制剂

Country Status (7)

Country Link
US (2) US11420969B2 (https=)
EP (1) EP3687990A1 (https=)
JP (1) JP7261793B2 (https=)
CN (1) CN111448193B (https=)
AU (1) AU2018341084B2 (https=)
CA (1) CA3077749A1 (https=)
WO (1) WO2019063996A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3821947A1 (en) * 2019-11-13 2021-05-19 Libra Therapeutics, Inc. Heterocyclic trpml1 agonists
GB202010829D0 (en) 2020-07-14 2020-08-26 Exonate Ltd Compounds for treatment of neovascular diseases
EP4646263A1 (en) * 2023-01-20 2025-11-12 Allianthera (Suzhou) Biopharmaceutical Co., Ltd. Sprk1 inhibitors and methods of use
WO2025243082A2 (en) * 2024-05-24 2025-11-27 The Chinese University Of Hong Kong Covalent protein-protein interaction inhibitor against srpks

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101837125A (zh) * 2003-12-26 2010-09-22 萩原正敏 Sr蛋白质的磷酸化控制方法以及以包含sr蛋白质活性控制剂的试剂为有效成分的抗病毒剂
WO2014060763A1 (en) * 2012-10-17 2014-04-24 The University Of Bristol Compounds useful for treating ocular neovasculan
WO2015159103A1 (en) * 2014-04-17 2015-10-22 The University Of Nottingham Piperazine derivatives for treating disorders
WO2017064512A1 (en) * 2015-10-16 2017-04-20 Exonate Limited Compounds

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7820178B2 (en) 2001-08-01 2010-10-26 University of Brisol VEGF isoforms and their use as anti-angiogenic, anti-vasodilatory, anti-permeability and anti-proliferative agents
US7429603B2 (en) * 2003-04-25 2008-09-30 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
MX2009009304A (es) 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
US20140249135A1 (en) 2007-03-01 2014-09-04 Novartis Ag Pim kinase inhibitors and methods of their use
GB0704678D0 (en) 2007-03-09 2007-04-18 Univ Bristol Pro- and anti-angiogenic treatments
WO2009020198A1 (ja) 2007-08-03 2009-02-12 Kinopharma, Inc. 抗dnaウイルス作用を有するアニリン誘導体
GB0803912D0 (en) 2008-02-29 2008-05-07 Univ Bristol Novel Uses of VEGFxxxb
JP2012509306A (ja) 2008-11-22 2012-04-19 ザ ユニバーシティ オブ ブリストル VEGFxxxbの新規な使用
WO2011036429A1 (en) 2009-09-25 2011-03-31 The University Of Bristol Detection of risk of pre-eclampsia
GB201009173D0 (en) 2010-05-28 2010-07-14 Univ Bristol Treatment of pain

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101837125A (zh) * 2003-12-26 2010-09-22 萩原正敏 Sr蛋白质的磷酸化控制方法以及以包含sr蛋白质活性控制剂的试剂为有效成分的抗病毒剂
WO2014060763A1 (en) * 2012-10-17 2014-04-24 The University Of Bristol Compounds useful for treating ocular neovasculan
WO2015159103A1 (en) * 2014-04-17 2015-10-22 The University Of Nottingham Piperazine derivatives for treating disorders
WO2017064512A1 (en) * 2015-10-16 2017-04-20 Exonate Limited Compounds

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease;Jennifer,等;《ACS Chemical Biology》;20170130;第12卷(第3期);825-832 *
STN-REGISTRY.REGISTRY-RN.《REGISTRY-数据库记录》.2015, *
Topical Antiangiogenic SRPK1 Inhibitors Reduce Choroidal Neovascularization in Rodent Models of Exudative AMD;Gammons,等;《INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE》;20130930;第54卷(第9期);6052-6062 *

Also Published As

Publication number Publication date
JP2020535172A (ja) 2020-12-03
CA3077749A1 (en) 2019-04-04
US12325704B2 (en) 2025-06-10
CN111448193A (zh) 2020-07-24
AU2018341084A1 (en) 2020-04-23
WO2019063996A1 (en) 2019-04-04
JP7261793B2 (ja) 2023-04-20
US20200270249A1 (en) 2020-08-27
EP3687990A1 (en) 2020-08-05
US20220389015A1 (en) 2022-12-08
US11420969B2 (en) 2022-08-23
AU2018341084B2 (en) 2023-04-13

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