CN109689042B - 用于治疗黄斑变性的与恩他卡朋相关的化合物 - Google Patents

用于治疗黄斑变性的与恩他卡朋相关的化合物 Download PDF

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CN109689042B
CN109689042B CN201780052192.2A CN201780052192A CN109689042B CN 109689042 B CN109689042 B CN 109689042B CN 201780052192 A CN201780052192 A CN 201780052192A CN 109689042 B CN109689042 B CN 109689042B
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macular degeneration
entacapone
alkyl
group
medicament
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CN109689042A (zh
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黄牛
彭士明
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National Institute of Biological Sciences Beijin
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    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A61K9/0051—Ocular inserts or implants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201780052192.2A 2016-08-24 2017-08-23 用于治疗黄斑变性的与恩他卡朋相关的化合物 Active CN109689042B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2016/096472 2016-08-24
CN2016096472 2016-08-24
PCT/CN2017/098575 WO2018036498A1 (en) 2016-08-24 2017-08-23 Entacapone-related compounds to treat macular degeneration

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CN109689042A CN109689042A (zh) 2019-04-26
CN109689042B true CN109689042B (zh) 2022-07-12

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US (1) US10980766B2 (https=)
EP (1) EP3503883B1 (https=)
JP (2) JP6898429B2 (https=)
CN (1) CN109689042B (https=)
AU (1) AU2017317129B2 (https=)
CA (1) CA3034547C (https=)
WO (1) WO2018036498A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10532976B2 (en) * 2015-06-23 2020-01-14 National Institute Of Biological Sciences, Beijing FTO inhibitors
AU2017317129B2 (en) * 2016-08-24 2020-04-30 National Institute Of Biological Sciences, Beijing Entacapone-related compounds to treat macular degeneration
US11103552B2 (en) 2018-05-10 2021-08-31 Regeneron Pharmaceuticals, Inc. High concentration VEGF receptor fusion protein containing formulations
CN118718181A (zh) 2019-06-05 2024-10-01 里珍纳龙药品有限公司 用于精确剂量递送的装置及方法
CN116963727A (zh) * 2020-11-13 2023-10-27 普莱克斯医药公司 用于治疗眼部病症的药剂
US20250074894A1 (en) * 2021-04-15 2025-03-06 Brown University Nitrophenyl-acrylamides and uses thereof
AU2023312773A1 (en) * 2022-07-29 2025-03-13 Rpxds Co., Ltd Fto inhibitors
USD1120314S1 (en) 2022-11-30 2026-03-24 Regeneron Pharmaceuticals, Inc. Dose delivery device
WO2025162373A1 (en) * 2024-01-30 2025-08-07 National Institute Of Biological Sciences, Beijing Electrophile-containing catechol-o-methyltransferase (comt) inhibitors for targeting the keap1/nrf2 pathway
WO2025162358A1 (en) * 2024-01-30 2025-08-07 Rpxds Co., Ltd Fto inhibitors of bicyclic structures

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007018943A2 (en) * 2005-08-02 2007-02-15 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
CN102186350A (zh) * 2008-08-19 2011-09-14 诺普神经科学股份有限公司 使用(r)-普拉克索的组合物与方法
CN102933217A (zh) * 2010-04-12 2013-02-13 株式会社·R-技术上野 用于治疗黄斑水肿的药物组合物

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI864875A0 (fi) 1986-11-28 1986-11-28 Orion Yhtymae Oy Nya farmakologiskt aktiva foereningar, dessa innehaollande kompositioner samt foerfarande och mellanprodukter foer anvaendning vid framstaellning av dessa.
TW200817315A (en) * 2006-06-16 2008-04-16 Sanol Arznei Schwarz Gmbh Entacapone-derivatives
EP1946756A1 (en) * 2007-01-17 2008-07-23 Revotar Biopharmaceuticals AG Use of entacapone in cosmetic, dermatological and pharmaceutical compositions
EP1978014A1 (en) 2007-04-02 2008-10-08 Esteve Quimica, S.A. Process for the preparation of entacapone and intermediates thereof
KR101760139B1 (ko) * 2007-06-29 2017-07-31 클라렌슈 피티와이 리미티드 안투여를 통한 신경 또는 신경정신 장애의 치료 또는 예방용 약학 조성물
WO2009129497A2 (en) * 2008-04-18 2009-10-22 Arizona Board Of Regents, A Body Corp. Of The State Of Arizona, Acting For And On Behalf Of The University Of Arizona Methods and compositions for treating and identifying compounds to treat age-related macular degeneration
WO2012142039A1 (en) * 2011-04-15 2012-10-18 University Of North Dakota Combination of liver x receptor modulator and estrogen receptor modulator for the treatment of age-related diseases
ES2858511T3 (es) * 2012-10-17 2021-09-30 Exonate Ltd Compuestos útiles para tratar neovascularización ocular
CN103845317B (zh) 2012-11-28 2018-05-08 北京生命科学研究所 恩他卡朋在预防或治疗肥胖等代谢综合征中的应用
WO2015095257A2 (en) * 2013-12-18 2015-06-25 Emory University Managing visual dysfunction or loss of vision for diabetic subjects
WO2016123577A1 (en) * 2015-01-30 2016-08-04 Lieber Institute For Brain Development Comt inhibiting methods and compositions
WO2016123576A1 (en) * 2015-01-30 2016-08-04 Lieber Institute For Brain Development Comt inhibiting methods and compositions
EP3885337B1 (en) 2015-06-23 2025-01-15 National Institute Of Biological Sciences, Beijing Fto inhibitors
AU2017317129B2 (en) 2016-08-24 2020-04-30 National Institute Of Biological Sciences, Beijing Entacapone-related compounds to treat macular degeneration

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007018943A2 (en) * 2005-08-02 2007-02-15 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
CN102186350A (zh) * 2008-08-19 2011-09-14 诺普神经科学股份有限公司 使用(r)-普拉克索的组合物与方法
CN102933217A (zh) * 2010-04-12 2013-02-13 株式会社·R-技术上野 用于治疗黄斑水肿的药物组合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Clinical characteristics and current treatment of age-related macular degeneration;Yoshihiro Yonekawa等;《Cold Spring Harbor Perspective Medicine》;20141031;第5卷(第3期);第1-18页 *

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Publication number Publication date
CN109689042A (zh) 2019-04-26
CA3034547A1 (en) 2018-03-01
US20190183842A1 (en) 2019-06-20
WO2018036498A1 (en) 2018-03-01
AU2017317129A1 (en) 2019-03-07
EP3503883B1 (en) 2022-05-04
JP2019526561A (ja) 2019-09-19
JP2021073265A (ja) 2021-05-13
CA3034547C (en) 2021-04-13
JP7116202B2 (ja) 2022-08-09
JP6898429B2 (ja) 2021-07-07
EP3503883A4 (en) 2020-04-15
US10980766B2 (en) 2021-04-20
EP3503883A1 (en) 2019-07-03
AU2017317129B2 (en) 2020-04-30

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