WO2008105408A1 - ウレイド基とアミノカルボニル基を置換基として有する新規ピロール誘導体 - Google Patents

ウレイド基とアミノカルボニル基を置換基として有する新規ピロール誘導体 Download PDF

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Publication number
WO2008105408A1
WO2008105408A1 PCT/JP2008/053297 JP2008053297W WO2008105408A1 WO 2008105408 A1 WO2008105408 A1 WO 2008105408A1 JP 2008053297 W JP2008053297 W JP 2008053297W WO 2008105408 A1 WO2008105408 A1 WO 2008105408A1
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WIPO (PCT)
Prior art keywords
group
substituent
salt
substituents
ureide
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PCT/JP2008/053297
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English (en)
French (fr)
Inventor
Kenji Kawashima
Hiroshi Enomoto
Noriko Ishizaka
Minoru Yamamoto
Kazuhiro Kudou
Masaaki Murai
Takaaki Inaba
Kazuyoshi Okamoto
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Santen Pharmaceutical Co., Ltd.
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Publication date
Application filed by Santen Pharmaceutical Co., Ltd. filed Critical Santen Pharmaceutical Co., Ltd.
Priority to DK08720883.1T priority Critical patent/DK2116530T3/da
Priority to RU2009135755/04A priority patent/RU2485101C2/ru
Priority to PL08720883T priority patent/PL2116530T3/pl
Priority to CA002678735A priority patent/CA2678735A1/en
Priority to EP08720883A priority patent/EP2116530B1/en
Priority to CN2008800062227A priority patent/CN101622229B/zh
Priority to US12/449,794 priority patent/US7977371B2/en
Priority to ES08720883T priority patent/ES2396741T3/es
Publication of WO2008105408A1 publication Critical patent/WO2008105408A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/10—Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

　本発明は、ウレイド基とアミノカルボニル基を置換基として有する新規ピロール誘導体又はその塩の合成研究及びその誘導体又はその塩の薬理作用を見出すこと、及び、経口投与において、網膜疾患等に対する予防及び／又は治療効果のある薬剤を見出すことを課題とする。一般式（１）で表される化合物又はその塩はインターロイキン－６産生阻害活性及び／又は脈絡膜血管新生阻害効果を有し、インターロイキン－６が関与する疾患、眼炎症性疾患及び／又は網膜疾患の予防及び/又は治療剤として有用である。式中、環Ａはベンゼン環等；Ｒ1はハロゲン原子、水素原子、低級アルキル基等；Ｒ2はハロゲン原子、置換基を有してもよい低級アルキル基、低級アルケニル基、置換基を有してもよい低級アルキニル基、低級シクロアルキル基、アリール基、ヒドロキシ基、置換基を有してもよい低級アルコキシ基等；ｎは０、１、２、３等を示す。
PCT/JP2008/053297 2007-02-26 2008-02-26 ウレイド基とアミノカルボニル基を置換基として有する新規ピロール誘導体 WO2008105408A1 (ja)

Priority Applications (8)

Application Number Priority Date Filing Date Title
DK08720883.1T DK2116530T3 (da) 2007-02-26 2008-02-26 Nyt pyrrolderivat, der har en ureidgruppe og en aminobonylgruppe som substituenter
RU2009135755/04A RU2485101C2 (ru) 2007-02-26 2008-02-26 Новое производное пиррола, имеющее в качестве заместителей уреидную и аминокарбонильную группу
PL08720883T PL2116530T3 (pl) 2007-02-26 2008-02-26 Nowa pochodna pirolu zawierająca jako podstawniki grupę ureidową i grupę aminokarbonylową
CA002678735A CA2678735A1 (en) 2007-02-26 2008-02-26 Novel pyrrole derivative having ureido group and aminocarbonyl group as substituents
EP08720883A EP2116530B1 (en) 2007-02-26 2008-02-26 Novel pyrrole derivative having ureide group and aminocarbonyl group as substituents
CN2008800062227A CN101622229B (zh) 2007-02-26 2008-02-26 具有脲基和氨基羰基作为取代基的吡咯衍生物
US12/449,794 US7977371B2 (en) 2007-02-26 2008-02-26 Pyrrole derivative having ureido group and aminocarbonyl group as substituents
ES08720883T ES2396741T3 (es) 2007-02-26 2008-02-26 Nuevo derivado de pirrol que tiene un grupo ureído y un grupo aminocarbonilo como sustituyentes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-045582 2007-02-26
JP2007045582 2007-02-26

Publications (1)

Publication Number Publication Date
WO2008105408A1 true WO2008105408A1 (ja) 2008-09-04

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PCT/JP2008/053297 WO2008105408A1 (ja) 2007-02-26 2008-02-26 ウレイド基とアミノカルボニル基を置換基として有する新規ピロール誘導体

Country Status (11)

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US (1) US7977371B2 (ja)
EP (1) EP2116530B1 (ja)
JP (1) JP4990184B2 (ja)
KR (1) KR20090115749A (ja)
CN (1) CN101622229B (ja)
CA (1) CA2678735A1 (ja)
DK (1) DK2116530T3 (ja)
ES (1) ES2396741T3 (ja)
PL (1) PL2116530T3 (ja)
RU (1) RU2485101C2 (ja)
WO (1) WO2008105408A1 (ja)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010024226A1 (ja) * 2008-08-25 2010-03-04 参天製薬株式会社 ウレイド基、アミノカルボニル基及び置換フェニル基を置換基として有するピロール誘導体を有効成分として含有する骨・関節疾患の予防又は治療剤
WO2010024227A1 (ja) * 2008-08-25 2010-03-04 参天製薬株式会社 ウレイド基、アミノカルボニル基及び置換基を有してもよい二環式基を置換基として有する新規ピロール誘導体
JP2013506639A (ja) * 2009-10-02 2013-02-28 アヴェクシン エーエス 抗炎症性２−オキソチアゾールおよび２−オキソオキサゾール
CN104829592A (zh) * 2015-05-22 2015-08-12 河南科技大学第一附属医院 4-哌啶基-1h-吡咯-3-甲酰胺类化合物盐酸盐的合成方法

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CN101812007B (zh) * 2010-04-27 2011-11-23 浙江大学 氨基吡咯类化合物及其制备方法
EP2951164B1 (en) 2013-01-29 2019-06-05 Avexxin AS Antiinflammatory and antitumor 2-oxothiazoles compounds
CN106102766A (zh) * 2014-01-22 2016-11-09 皮埃尔与玛丽·居里大学 - 巴黎第六大学 用于治疗视网膜炎症的试剂
EP2898896A1 (en) * 2014-01-22 2015-07-29 Université Pierre et Marie Curie (Paris 6) Agents for use in the treatment of retinal inflammation
GB201413695D0 (en) 2014-08-01 2014-09-17 Avexxin As Compound
WO2017151409A1 (en) 2016-02-29 2017-09-08 University Of Florida Research Foundation, Incorporated Chemotherapeutic methods
GB201604318D0 (en) 2016-03-14 2016-04-27 Avexxin As Combination therapy
US11834430B2 (en) 2017-09-12 2023-12-05 Agency For Science, Technology And Research Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase
CN109956893B (zh) * 2017-12-22 2022-07-22 甘肃森瀚石油科技有限公司 一种多取代3-氨基吡咯化合物的制备方法

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010024226A1 (ja) * 2008-08-25 2010-03-04 参天製薬株式会社 ウレイド基、アミノカルボニル基及び置換フェニル基を置換基として有するピロール誘導体を有効成分として含有する骨・関節疾患の予防又は治療剤
WO2010024227A1 (ja) * 2008-08-25 2010-03-04 参天製薬株式会社 ウレイド基、アミノカルボニル基及び置換基を有してもよい二環式基を置換基として有する新規ピロール誘導体
US8088817B2 (en) 2008-08-25 2012-01-03 Santen Pharmaceutical Co., Ltd. Pyrrole derivative having, as substituents, ureido group, aminocarbonly group and bicyclic group which may have substituent
JP2013506639A (ja) * 2009-10-02 2013-02-28 アヴェクシン エーエス 抗炎症性２−オキソチアゾールおよび２−オキソオキサゾール
CN104829592A (zh) * 2015-05-22 2015-08-12 河南科技大学第一附属医院 4-哌啶基-1h-吡咯-3-甲酰胺类化合物盐酸盐的合成方法

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Publication number Publication date
RU2485101C2 (ru) 2013-06-20
ES2396741T3 (es) 2013-02-25
CA2678735A1 (en) 2008-09-04
JP2008239614A (ja) 2008-10-09
EP2116530B1 (en) 2012-11-14
RU2009135755A (ru) 2011-04-10
US7977371B2 (en) 2011-07-12
DK2116530T3 (da) 2013-01-28
CN101622229A (zh) 2010-01-06
CN101622229B (zh) 2013-02-27
EP2116530A1 (en) 2009-11-11
JP4990184B2 (ja) 2012-08-01
KR20090115749A (ko) 2009-11-05
US20100099675A1 (en) 2010-04-22
EP2116530A4 (en) 2010-08-11
PL2116530T3 (pl) 2013-03-29

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