WO2008093691A1 - 網膜神経又は視神経の保護剤 - Google Patents

網膜神経又は視神経の保護剤 Download PDF

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Publication number
WO2008093691A1
WO2008093691A1 PCT/JP2008/051338 JP2008051338W WO2008093691A1 WO 2008093691 A1 WO2008093691 A1 WO 2008093691A1 JP 2008051338 W JP2008051338 W JP 2008051338W WO 2008093691 A1 WO2008093691 A1 WO 2008093691A1
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Prior art keywords
nerve
protective agent
atom
compound
retinal
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PCT/JP2008/051338
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English (en)
French (fr)
Inventor
Sookja Kim Chung
Stephen Chung
Chihiro Hibi
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Sanwa Kagaku Kenkyusho Co., 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
Application filed by Sanwa Kagaku Kenkyusho Co., Ltd. filed Critical Sanwa Kagaku Kenkyusho Co., Ltd.
Priority to AU2008210970A priority Critical patent/AU2008210970B2/en
Priority to EP08704120A priority patent/EP2110141B1/en
Priority to PL08704120T priority patent/PL2110141T3/pl
Priority to US12/517,882 priority patent/US8536212B2/en
Priority to JP2008556121A priority patent/JP5363123B2/ja
Priority to DK08704120.8T priority patent/DK2110141T3/da
Priority to KR1020097013856A priority patent/KR20090104014A/ko
Priority to CA2673751A priority patent/CA2673751C/en
Priority to ES08704120T priority patent/ES2409930T3/es
Publication of WO2008093691A1 publication Critical patent/WO2008093691A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
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    • A61P27/06—Antiglaucoma agents or miotics
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  • Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

【課題】 　本発明は、既存の治療薬とは異なる機序で有効性を示し、長期服用が可能な、網膜神経又は視神経の保護剤を提供することを課題とする。 【解決手段】 　本発明は、アルドース還元酵素阻害作用を有する化合物、例えば、下記一般式で示す化合物を有効成分とする、網膜神経又は視神経の保護剤である。化合物としては、(2Ｓ,4Ｓ)-6-フルオロ-2',5'-ジオキソスピロ[クロマン-4,4'-イミダゾリジン]-2-カルボキサミドが好ましい。 【化１】 （式中、Ｘはハロゲン原子又は水素原子を意味し、R1、R2は、それぞれ独立して水素原子又は置換されていてもよいC1-6アルキル基を示すか、或いはR1とR2と付け根の窒素原子と共に又は更に他の窒素原子若しくは酸素原子と共に形成する５～６員の複素環を示す。）
PCT/JP2008/051338 2007-01-31 2008-01-30 網膜神経又は視神経の保護剤 WO2008093691A1 (ja)

Priority Applications (9)

Application Number Priority Date Filing Date Title
AU2008210970A AU2008210970B2 (en) 2007-01-31 2008-01-30 Protective agent for retinal nerve or optic nerve
EP08704120A EP2110141B1 (en) 2007-01-31 2008-01-30 Protective agent for retinal nerve or optic nerve
PL08704120T PL2110141T3 (pl) 2007-01-31 2008-01-30 Środek ochronny dla nerwu siatkówki lub nerwu wzrokowego
US12/517,882 US8536212B2 (en) 2007-01-31 2008-01-30 Protective agent for retinal nerve or optic nerve
JP2008556121A JP5363123B2 (ja) 2007-01-31 2008-01-30 網膜神経又は視神経の保護剤
DK08704120.8T DK2110141T3 (da) 2007-01-31 2008-01-30 Middel til beskyttelse af retinalnerve eller synsnerve
KR1020097013856A KR20090104014A (ko) 2007-01-31 2008-01-30 망막신경 또는 시신경의 보호제
CA2673751A CA2673751C (en) 2007-01-31 2008-01-30 Protective agent for retinal nerve or optic nerve
ES08704120T ES2409930T3 (es) 2007-01-31 2008-01-30 Agente protector del nervio de la retina o del nervio óptico

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-021852 2007-01-31
JP2007021852 2007-01-31

Publications (1)

Publication Number Publication Date
WO2008093691A1 true WO2008093691A1 (ja) 2008-08-07

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ID=39674000

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PCT/JP2008/051338 WO2008093691A1 (ja) 2007-01-31 2008-01-30 網膜神経又は視神経の保護剤

Country Status (11)

Country Link
US (1) US8536212B2 (ja)
EP (2) EP2110141B1 (ja)
JP (1) JP5363123B2 (ja)
KR (1) KR20090104014A (ja)
CN (2) CN103222974A (ja)
AU (1) AU2008210970B2 (ja)
CA (1) CA2673751C (ja)
DK (1) DK2110141T3 (ja)
ES (1) ES2409930T3 (ja)
PL (1) PL2110141T3 (ja)
WO (1) WO2008093691A1 (ja)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011087066A1 (ja) 2010-01-14 2011-07-21 株式会社三和化学研究所 眼内血管新生及び／又は眼内血管透過性亢進を伴う疾患の予防又は治療のための医薬
WO2011136161A1 (ja) 2010-04-28 2011-11-03 株式会社 三和化学研究所 内耳障害の予防又は治療薬
WO2012105610A1 (ja) 2011-02-02 2012-08-09 公立大学法人名古屋市立大学 眼内血管新生及び／又は眼内血管透過性亢進を伴う疾患の予防又は治療のための医薬
JP2015528825A (ja) * 2012-08-17 2015-10-01 ファーマキング カンパニー リミテッドＰｈａｒｍａｋｉｎｇ Ｃｏ．， Ｌｔｄ． Ｓ−アリル−ｌ−システインを有効成分として含む眼疾患予防または治療用組成物、およびこれを含む医薬製剤
WO2016039422A1 (ja) * 2014-09-11 2016-03-17 大日本住友製薬株式会社 点眼用懸濁製剤

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2139330B1 (en) * 2007-03-23 2014-09-24 The Board of Regents of The University of Texas System Methods involving aldose reductase inhibitors
KR102007640B1 (ko) 2017-11-29 2019-08-07 퓨쳐메디신 주식회사 아데노신 유도체를 포함하는 망막 질환 또는 시신경 질환 예방 및 치료용 약학적 조성물
CN112004563A (zh) 2018-02-01 2020-11-27 施菲姆德控股有限责任公司 血管内血泵以及使用和制造方法

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JPH04173791A (ja) 1990-11-07 1992-06-22 Sanwa Kagaku Kenkyusho Co Ltd 循環器系疾患の予防及び治療剤
JPH06135968A (ja) 1992-10-27 1994-05-17 Sanwa Kagaku Kenkyusho Co Ltd ヒダントイン誘導体及びその塩並びにこれらを有効成分とするメイラード反応阻害剤
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WO2001085183A2 (en) * 2000-05-08 2001-11-15 N.V. Nutricia Preparation for the prevention and treatment of ocular disorders
US6936043B2 (en) * 2001-11-13 2005-08-30 Minu, Llc Method to treat age-related macular degeneration

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4609663A (en) * 1984-09-11 1986-09-02 Alcon Laboratories, Inc. Aldose reductase inhibitors useful in glaucoma therapy
JPS61200991A (ja) 1985-03-04 1986-09-05 Sanwa Kagaku Kenkyusho:Kk スピロ―３―ヘテロアゾリジン化合物、その製法及びそれを有効成分とする糖尿病合併症の予防及び治療剤
JPH04173791A (ja) 1990-11-07 1992-06-22 Sanwa Kagaku Kenkyusho Co Ltd 循環器系疾患の予防及び治療剤
JPH06135968A (ja) 1992-10-27 1994-05-17 Sanwa Kagaku Kenkyusho Co Ltd ヒダントイン誘導体及びその塩並びにこれらを有効成分とするメイラード反応阻害剤
JPH07242547A (ja) 1994-03-02 1995-09-19 Sanwa Kagaku Kenkyusho Co Ltd 糖尿病性単純網膜症の進行阻止剤乃至治療剤
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WO2011087066A1 (ja) 2010-01-14 2011-07-21 株式会社三和化学研究所 眼内血管新生及び／又は眼内血管透過性亢進を伴う疾患の予防又は治療のための医薬
JP2013049701A (ja) * 2010-01-14 2013-03-14 Sanwa Kagaku Kenkyusho Co Ltd 眼内血管新生及び／又は眼内血管透過性亢進を伴う疾患の予防又は治療のための医薬
WO2011136161A1 (ja) 2010-04-28 2011-11-03 株式会社 三和化学研究所 内耳障害の予防又は治療薬
WO2012105610A1 (ja) 2011-02-02 2012-08-09 公立大学法人名古屋市立大学 眼内血管新生及び／又は眼内血管透過性亢進を伴う疾患の予防又は治療のための医薬
JP2015528825A (ja) * 2012-08-17 2015-10-01 ファーマキング カンパニー リミテッドＰｈａｒｍａｋｉｎｇ Ｃｏ．， Ｌｔｄ． Ｓ−アリル−ｌ−システインを有効成分として含む眼疾患予防または治療用組成物、およびこれを含む医薬製剤
WO2016039422A1 (ja) * 2014-09-11 2016-03-17 大日本住友製薬株式会社 点眼用懸濁製剤
US10034880B2 (en) 2014-09-11 2018-07-31 Sumitomo Dainippon Pharma Co., Ltd. Ophthalmic suspension formulation

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EP2110141A1 (en) 2009-10-21
PL2110141T3 (pl) 2013-09-30
EP2110141A4 (en) 2011-01-19
EP2110141B1 (en) 2013-04-03
CA2673751A1 (en) 2008-08-07
CN101594884A (zh) 2009-12-02
CA2673751C (en) 2012-05-08
US20100216856A1 (en) 2010-08-26
JP5363123B2 (ja) 2013-12-11
US8536212B2 (en) 2013-09-17
KR20090104014A (ko) 2009-10-05
ES2409930T3 (es) 2013-06-28
AU2008210970A1 (en) 2008-08-07
JPWO2008093691A1 (ja) 2010-05-20
DK2110141T3 (da) 2013-06-17
CN103222974A (zh) 2013-07-31
AU2008210970B2 (en) 2012-11-29
EP2594267A1 (en) 2013-05-22

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