JP2013510852A - フルオレノン誘導体による眼の病態の治療 - Google Patents

フルオレノン誘導体による眼の病態の治療 Download PDF

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JP2013510852A
JP2013510852A JP2012538861A JP2012538861A JP2013510852A JP 2013510852 A JP2013510852 A JP 2013510852A JP 2012538861 A JP2012538861 A JP 2012538861A JP 2012538861 A JP2012538861 A JP 2012538861A JP 2013510852 A JP2013510852 A JP 2013510852A
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tetrahydro
dichloro
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JP2013510852A5 (enExample
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コンスタンティン ペトルキン
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ザ トラスティーズ オブ コロンビア ユニヴァーシティ イン ザ シティ オブ ニューヨーク
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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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
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    • 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
    • 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
    • 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
    • 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
    • A61K9/08—Solutions
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/10—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D263/14—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/10—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2012538861A 2009-11-12 2010-11-05 フルオレノン誘導体による眼の病態の治療 Pending JP2013510852A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US26043909P 2009-11-12 2009-11-12
US61/260,439 2009-11-12
US37862410P 2010-08-31 2010-08-31
US61/378,624 2010-08-31
PCT/US2010/055540 WO2011059881A1 (en) 2009-11-12 2010-11-05 Treatment of ophthalmic conditions with fluorenone derivatives

Publications (2)

Publication Number Publication Date
JP2013510852A true JP2013510852A (ja) 2013-03-28
JP2013510852A5 JP2013510852A5 (enExample) 2013-12-26

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JP2012538861A Pending JP2013510852A (ja) 2009-11-12 2010-11-05 フルオレノン誘導体による眼の病態の治療

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US (1) US20130189246A1 (enExample)
EP (1) EP2501227A4 (enExample)
JP (1) JP2013510852A (enExample)
WO (1) WO2011059881A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013166037A1 (en) 2012-05-01 2013-11-07 The Trustees Of Columbia University In The City Of New York Non-retinoid antagonists for treatment of eye disorders
WO2014151959A1 (en) 2013-03-14 2014-09-25 The Trustees Of Columbia University In The City Of New York N-alkyl-2-phenoxyethanamines, their preparation and use
WO2014151936A1 (en) 2013-03-14 2014-09-25 The Trustees Of Columbia University In The City Of New York Octahydropyrrolopyrroles, their preparation and use
US10273243B2 (en) 2013-03-14 2019-04-30 The Trustees Of Columbia University In The City Of New York 4-phenylpiperidines, their preparation and use
EP2968303B1 (en) 2013-03-14 2018-07-04 The Trustees of Columbia University in the City of New York Octahydrocyclopentapyrroles, their preparation and use
WO2015168286A1 (en) 2014-04-30 2015-11-05 The Trustees Of Columbia University In The City Of New York Substituted 4-phenylpiperidines, their preparaiton and use
US11000492B2 (en) 2015-11-13 2021-05-11 The Trustees Of Columbia University In The City Of New York Fluorenone compound for the treatment of gout
CN116350790B (zh) * 2021-12-28 2025-02-07 沈阳兴齐眼药股份有限公司 组合物及其在制备用于治疗老花眼的药物中的用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6251898B1 (en) * 1999-08-24 2001-06-26 Questcor Pharmaceuticals, Inc. Medical use of fluorenone derivatives for treating and preventing brain and spinal injury

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
JPS5857319A (ja) * 1981-09-30 1983-04-05 Green Cross Corp:The 高粘性ヒアルロン酸製剤
JPH06145045A (ja) * 1992-11-05 1994-05-24 Koken Co Ltd 網膜剥離治療用シリコ−ンオイル及びその製造方法
US7186707B2 (en) * 2002-04-01 2007-03-06 University Of Florida Prodrugs for use as ophthalmic agents
JP2009525282A (ja) * 2006-01-30 2009-07-09 （オーエスアイ）アイテツク・インコーポレーテツド 血管新生疾患の治療のための組み合わせ療法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6251898B1 (en) * 1999-08-24 2001-06-26 Questcor Pharmaceuticals, Inc. Medical use of fluorenone derivatives for treating and preventing brain and spinal injury

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JPN6014047879; ＫＩＭＥＬＢＥＲＧ　Ｈ　Ｋ　ＥＴ　ＡＬ: 'ＡＳＴＲＯＣＹＴＩＣ　ＳＷＥＬＬＩＮＧ　ＩＮ　ＴＲＡＵＭＡＴＩＣ-ＨＹＰＯＸＩＣ　ＢＲＡＩＮ　ＩＮＪＵＲＹ　ＢＥＮＥＦＩＣＩＡＬ　ＥＦＦＥＣＴＳ　ＯＦ　ＡＮ　ＩＮＨＩＢＩＴＯＲ　ＯＦ　ＡＮＩＯＮ　ＥＸ' ＭＯＬＥＣＵＬＡＲ　ＡＮＤ　ＣＨＥＭＩＣＡＬ　ＮＥＵＲＯＰＡＴＨＯＬＯＧＹ ｖｏｌ．　１１，　ｎｏ．　１, 1989, ｐａｇｅｓ　１-３１ *
JPN6014047881; ＴＨＡＫＲＡＮ　Ｐ　ＥＴ　ＡＬ: 'Ｌｏｏｐ　ｄｉｕｒｅｔｉｃ　ｄｅｒｉｖａｔｉｖｅ　Ｌ-６４４，７１１　ｉｎｈｉｂｉｔｓ　Ｋ（＋）-ｓｔｉｍｕｌａｔｅｄ　ｃｅｌｌｕｌａｒ　ｉｎｊｕｒｙ　ｉｎ　ｎｅｏｎａｔａｌ　ｇｕｉｎｅａ　ｐｉｇ　ｃ' ＭＯＬＥＣＵＬＡＲ　ＡＮＤ　ＣＨＥＭＩＣＡＬ　ＮＥＵＲＯＰＡＴＨＯＬＯＧＹ Ｖｏｌ．２１，Ｎｏ．１, 1994, ｐ．２３-３９ *
JPN6014047883; ＩＺＵＭＩ　Ｙ　ｅｔ　ａｌ: 'Ｍｕｅｌｌｅｒ　Ｃｅｌｌ　Ｓｗｅｌｌｉｎｇ，　Ｇｌｕｔａｍａｔｅ　Ｕｐｔａｋｅ，　ａｎｄ　Ｅｘｃｉｔｏｔｏｘｉｃ　Ｎｅｕｒｏｄｅｇｅｎｅｒａｔｉｏｎ　ｉｎ　ｔｈｅ　Ｉｓｏｌａｔｅｄ　Ｒａｔ　Ｒｅｔｉｎ' ＧＬＩＡ Ｖｏｌ．２５，　Ｎｏ．４, Ｐａｇｅ．３７９-３８９ *

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WO2011059881A1 (en) 2011-05-19
EP2501227A4 (en) 2013-04-10
US20130189246A1 (en) 2013-07-25
EP2501227A1 (en) 2012-09-26

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